International Journal of Pharmaceutical Investigation

A Review on Natural Sources of Antimalarials: Fungi and Plants

Tehzeeb Tehzeeb, Dhanabalan Dhanabalan — Thu, 10 Dec 2020 00:00:00 +0000

Recent progress in drug discovery in past decades reduced the high level of pain experienced due to infectious diseases by humans. A significant impact has been made on developing novel antimicrobial agents but is failing regularly due to development of resistance to drugs by the parasite or microbe. A continuing need of antimicrobials is there to protect humans from resistant microbes from different sources such as semisynthetic sources, synthetic and natural sources. Research in developing natural antimicrobials such as plant and fungal sources is still in its initial stages. In this review, we have concentrated on devastating disease malaria which is seen in several parts of world. Even though there are newly developed antimalarial artemisinin based combination therapy, recent reports are suggesting that resistance may also develop soon against the newer artemesinin products. Our search for literature and survey for natural antimicrobials motivated us to give concern to fungal source as promising antimalarial and most unexplored source for the same. This review throws light on recent reports on disease malaria, causative species and outline of its lifecycle, targets of drug action and mainly the fungal sources of antimalarial.

Clinical Utilization of Non-Anticoagulant - A Review

Pitchaimuthu Pandian — Thu, 10 Dec 2020 00:00:00 +0000

Heparin is used as anticoagulant for long period and also other activities both experimentally and clinically. The heparin is prepared by many methods namely enzymatic hydrolysis, chemical hydrolysis by removing the antithrombin binding sites or inactivating functional groups or units of this sequence. In non-anticoagulant treatments the therapeutic spectrum helps to the structural variations to treat different diseases. Sulfated nonanticoagulant heparins (S-NACHs) might be preferred for potential clinical use in cancer patients without affecting hemostasis. Among still some of the drugs or its derivatives are undergoing the clinical trials for various non-anticoagulant diseases. This review analyses the effects of this group of drugs on non-anticoagulant heparin, acute pulmonary embolism, oral pulmonary embolism, Non anticoagulant in cancer, Antitumor activities of LMWHs, dermatology, Effects of non-anticoagulant on Fractures such as bone metabolism, bone mineral density, Anti-inflammatory, asthma, Malaria Parasites, Anti-Human Immunodeficiency Virus, Non-anticoagulant activities of LMWHs with their mechanism, Non-anticoagulant pharmacological activities in clinical trials are discussed in this review.

Solubility Enhancement of BCS Classified II/IV Drug – Solid Dispersion of Apixaban by Solvent Evaporation

Thu, 10 Dec 2020 00:00:00 +0000

Background: Solubility is an important physico-chemical factor affecting absorption of drug and its therapeutic effectiveness. One of the major problems responsible for the low turnout in the development of new molecular entities as drug formulations is poor solubility and poor permeability of the lead compounds. Objectives: The present research work was aimed to enhance the solubility of Apixaban drug by using Solid Dispersion Technique. Methods: The solid dispersion is the technique for the formulation of water insoluble drugs to enhance their aqueous solubility, absorption as well as dissolution rate, which leading to enhancement of bioavailability of drugs as compared to conventional directly compressed tablets. In this study, Apixaban was opted for formulating Solid dispersion with Hydrophilic polymers like HPMC E50 LV, HPMC E5, PEG 6000 and PVP K-30 by Spray drying method using a structured I optimal screening DOE. To screen out the ratio of polymer and suitable polymer type for solid dispersion resulted into highest solubility as a response. Results: The Solid dispersion of Apixaban showed improvement in the solubility in water by multiple folds when Apixaban used in combination with Hydrophilic polymers. The Apixaban solid dispersion with polymer HPMC K15M resulted into highest increase in the solubility as compared to the other evaluated hydrophilic polymers. Conclusion: From the present study, we can concluded that the optimized Apixaban solid dispersion may prove to be a suitable potential option for solubility enhancement, increased in-vitro drug release and effective delivery of BCS class II and IV drugs.

Physiochemical and Structural Characterization of Biosurfactant Produced by Halophilic Pseudomonas aeruginosa ENO14 Isolated from Seawater

Ekramul Haque, Mohd Aamir Bin Riyaz, Sriram Shankar, Saqib Hassan — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: The aim of this study was to isolate a potent biosurfactant producing bacterium and characterize the produced biosurfactant for its application in pharmaceutical, petrochemical, cosmetic and food industry. Methods: Enrichment method was carried out followed by serial dilution technique to isolate the bacteria from oil contaminated seawater. Various qualitative assays such as haemolytic assay, oil displacement assay, foaming index and emulsification index was carried out for the screening of the best isolate. Morphological, biochemical, physiological and 16S rDNA sequencing was used to identify the potent bacterium. For the production of biosurfactant, Bushnell Hass Broth (BHB), supplemented with 1% glucose was used. Various physiochemical and structural analysis of biosurfactant were carried out by different techniques. Results: The bacteria producing biosurfactant were isolated and screened for biosurfactant production using various qualitative assays from crude oil contaminated seawater. A potent bacterial isolate was selected on the basis of oil displacement activity and highest biosurfactant producing capability. Based on the morphological, physio-biochemical characteristics and sequencing of 16S rDNA of the isolate, ENO14, was revealed to be Pseudomonas aeruginosa. The biosurfactant exhibited high surface activity (critical micelle concentration, CMC=3.85 mg/ml) and excellent emulsifying activity against different hydrocarbons (emulsifying activity, EA₂₄ =100% against crude oil). The biosurfactant showed stability over a temperature range of 20-70°C, pH range of 2-12 and salinity range of 2- 12% (w/v). Compositional analysis of the purified biosurfactant by chemical method as well as by Ultraviolet-Visible Spectroscopy (UV-Vis), Energy Dispersive X-ray Spectroscopy (EDX), Fourier Transform Infrared Spectroscopy (FT-IR), reveals it is a type of glycolipid biosurfactant. Conclusion: We conclude that Pseudomonas aeruginosa ENO14 is an efficient biosurfactant producer. The produced biosurfactant was well characterized for its application in pharmaceutical, petrochemical, food and cosmetic industry.

Preparation and Investigation of Gastro-Retentive Mucoadhesive Microspheres of Clarithromycin-Resin Complex

Johnson Stephin, Mr., Koland Marina — Thu, 10 Dec 2020 00:00:00 +0000

Introduction: Helicobacter pylori infection is strongly associated with chronic gastritis and duodenal ulcers which can benefit from gastroretentive delivery of clarithromycin. Objectives: The objective of this study was to investigate mucoadhesive microspheres of the antibiotic – resin complex for gastro-retention, thereby increasing the local effective concentrations of clarithromycin. Methods: Clarithromycin-resin complex granules were coated with the mucoadhesive polymers, Carbopol 934 and Polycarbophil in different ratios of 1:1, 1:2, 1:3 and 1:4 by solvent evaporation method. Prepared microspheres were subjected to characterization for particle size and shape, drug content, in vitro mucoadhesion, in vitro drug release and in vivo gastric residence time in albino rats. Results and Discussion: Particle sizes of the microspheres were found to be in the range of 83 μm-87μm. Scanning electron microscopic images of the formulation showed spherical particles with almost smooth surface morphology for carbopol microspheres. Formulations with both polymers showed mucoadhesion for a period of more than 6 hr. In vitro drug release using the USP dissolution test apparatus appeared to follow first order kinetics. Fluorescence imaging of histo-pathological slides of rats gastric and intestinal mucosa reveal that gastric residence time was found to be longer than 6 h for carbopol microspheres and at least 4 h in the case of polycarbophil microspheres. Conclusion: Carbopol coated microspheres of ion exchange resin complexes of clarithromycin for the gastro-retentive delivery of clarithromycin can be a promising alternative to the conventional oral solid dosage forms in the control of H. pylori induced chronic gastritis or duodenal ulcers.

Formulation, Development and Evaluation of Atorvastatin Ethosomal Gel

S Agarwal, G Gautam — Thu, 10 Dec 2020 00:00:00 +0000

Background: The present investigation was held to develop vesicular ethosomal gel system for anti-hypertensive drug atorvastatin. Atorvastatin is a HMG-CoA reeducates inhibitor and utilized for minimizing cholesterol level in the treatment of congestive heart failure (CHF). In order to enhance the systemic bioavailability and to decrease the first pass metabolism atorvastatin drug was designed into ethosomal gel. Methods: Ethosomes composed of phospholipid soya lecithin, ethanol and cholesterol were formulated by cold method followed by ultra-sonication. The atorvastatin ethosomes were then distinguished for their particle size, zeta potential followed by in vitro drug release profile. The optimized ethosomal formulation was then incorporated into gelling agent, carbopol 934 to prepare ethosomal gel formulation. Results: The ethosomal gel formulation was then subjected to physico-chemical characterization, spreadibility and in vitro drug release profile. The ethosomal gel formulation showed 15.69g. cm2 spreadibility and 98.47% in vitro drug release within 48 hr as compared to plan drug ethosomal formulation which shows 65.37% in 48 hr. Conclusion: It was concluded that ethosomal gel delivery system provide a good design for topical delivery of drug with enhanced bioavailability and patient compliance.

Design, Formulation and Evaluation of Oxymel Containing Andrographis paniculata Extract

Prasad Suhas Kshirsagar, Darshana Sanjay Mote, Shriniwas Pramod Patil — Thu, 10 Dec 2020 00:00:00 +0000

Introduction: Andrographis paniculata is medicinal plant of family Acanthaceae, consists of bitter principles and traditionally used in treatment of several gastrointestinal diseases. To mask its bitter taste, it could be formulated in honey based oral formulations like oxymel. Honey, as a saturated solution of various sugars, as per Ayurvedic system of medicine, could be consumed along with drug. Aim: This research attempt was aimed towards aqueous extraction of A. paniculata powder; formulation of oxymel by addition to honey and evaluation for different parameters. Methods: Oxymel was formulated as per procedure mentioned in United State Pharmacopeia for squill oxymel; and evaluated for pharmaceutical parameters those applied for oral syrups. Results: The oxymel formulated was dark brownish with agreeable odour and sweet taste. It was pourable with viscosity of 27.14 CP at 45.02 torque measured at 100 rpm while density was found to be 1.25 gm/ml. There was also ease in cap opening of its container, also no crystallization of honey was observed. Its andrographolide content was found to be 411.0 μg/ml. Conclusion: Bitters of A. paniculata have significant pharmacological activities in human being, if administered orally. To mask their bitter taste and facilitate their increase in absorption, A. paniculata can successfully be formulated in honey based oral formulation of oxymel.

Formulation, Characterization and Evaluation of Behavioral Effects of Suspension and Effervescent Granules of Evolvulus alsinoides Linn. and Convolvulus pluricaulis Choisy

Garima Jain, Umesh K Patil — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: The objective of the present study was to formulate, characterize and evaluate herbal formulations of Evolvulus alsinoides and Convolvulus pluricaulis against scopolamine-induced behavioral disturbances for Alzheimer’s disease. Methods: The herbal drugs were extracted using ethanol. The herbal suspension and effervescence granules were prepared using the extract and evaluated on rats. Scopolamine was used to induce behavioral and locomotor disturbances. Results: Results revealed that both the formulations were stable and effective in enhancing cognition against scopolamine-induced behavioral disturbance. The activity score of suspension of Evolvulus alsinoides and Convolvulus pluricaulis in the actophotometer were 128.19 and 110.23 while in effervescent granules of Evolvulus alsinoides and Convolvulus pluricaulis were 124.21 and 120.29 after 60 min, respectively. Suspension of Evolvulus alsinoides and Convolvulus pluricaulis reduced the fall off time to 94.18 and 102.03 while effervescent granules of Evolvulus alsinoides and Convolvulus pluricaulis reduced 98.01 and 98.16 after 30 min using the rota-rod, respectively. Suspension of Evolvulus alsinoides and Convolvulus pluricaulis reduce the activity of acetylcholinesterase as 19.10 and 18.01 Units/L while effervescent granules of Evolvulus alsinoides and Convolvulus pluricaulis reduce the activity of acetylcholinesterase as 17.69 and 14.36 Units/L. Conclusion: The formulations were significantly reduced locomotor activity using actophotometer, rotarod activity and the level of acetylcholinesterase. Thus, herbal suspension and effervescent granules of Evolvulus alsinoides and Convolvulus pluricaulis may be a safe alternative for Alzheimer’s disease against scopolamine-induced behavioral disturbances.

Pharmaceutical Development of Nitrosourea Compound for the Treatment of Neuroendocrine Tumours

Zoya Shprakh — Thu, 10 Dec 2020 00:00:00 +0000

Background: Nitrosoureas are chemotherapeutic alkylating agents, widely used in the treatment of malignant diseases. One of them (streptozotocin) is the standard for the therapy of neuroendocrine tumours. We synthesised a nitrosourea compound, aranoza, which has been effective in preclinical studies on experimental tumour models. Objectives: The current research deals with the development of the pharmaceutical dosage form of aranoza and the evaluation of the quality of the finished product. Methods: Sterilizing filtration followed by freeze drying was used to prepare the finished product. The acidity of the solutions was determined potentiometrically. Aranoza content in solution and lyophilisate was determined by spectrophotometry method. Results: We suggested the composition of the drug for parenteral use. The created product includes polyvinylpyrolidone and sorbic acid for solution stabilization and regulation of acidity, respectively. We also selected the method for aranozasolution preparation and showed that filters of mixed cellulose esters have optimal characteristics for filtration sterilisation. We chose lyophilisation to obtain a stable product: the freezing temperature was determined as -40°C to -45°C and the duration of freezing as 3–4 hr. The finished product has characteristics corresponding to requirements of the European Pharmacopoeia and State Pharmacopoeia of the Russian Federation and maintained its quality for the time of observation of 36 months. Conclusion: We created the algorithm for the development of a lyophilised antitumor drug, which allowed to obtain an appropriate pharmaceutical dosage form of a nitrosourea compound, aranoza, purposed for the treatment of neuroendocrine tumours.

Formulation and Evaluation of Dolutegravir Proliposomal Powder for Pediatric HIV Patients

Naseeb Basha Shaik, Divya Shakelli, Lakshmi PK, Basava Rao VV — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: The objective of the present study was to improve the absorption of dolutegravir sodium by developing oral proliposomal formulation. Methods: Proliposomal formulations were prepared by film deposition on carrier method using cholesterol along with various lipids and different carriers. Three factors (independent variables) such as different lipids (X1), different carriers (X2) and different ratio of lipid: cholesterol (X3) were studied at all three levels, while % entrapment efficiency (%EE) (Y) was taken as the response (dependent variable). The proliposomes were optimized by Taguchi OA (L9) experimental design using Minitab 18 English software. Results and Discussion: Proliposomes were evaluated and the % EE of optimized proliposomal formulation (PL7) found to be 84.02 %. In vitro drug release was performed in 0.1N HCl and in 6.8 pH phosphate buffer with SLS using USP type II dissolution apparatus, the % drug release found to be 12.71 % in 120 min. and 98.95% in 80 min. respectively, which indicates the drug is not released in acidic medium. Surface morphology was coarse, non-porous and irregular in shape, hydration is rapid and complete conversion of proliposomes to liposomes vesicles within 2-3 min. The mean particle size is 276.6 nm, polydispersity index is 0.329 and zeta potential is -9.54 mV, may prevent aggregation of vesicles and formulation is stable. Ex-vivo absorption studies were done using the rat non-everted intestinal sac model, permeation studies revealed that Papp of the optimized proliposomal formulation and IR tablet found to be 1.19 and 0.995 cm/sec respectively indicates enhanced absorption than the pure IR tablet. Conclusion: The proliposomal formulation indicated a stable formulation with significant improvement in absorption of dolutegravir sodium.

Formulation Development and Characterization of Rapid Mouth Dissolving Film of Frovatriptan Succinate (RETRACTED)

Pankaj Bhatt, Suruchi Singh, Satish Kumar Sharma, Sani Rabiu — Thu, 10 Dec 2020 00:00:00 +0000

NOTE: THE ARTICLE HAS BEEN RETRACTED BASED ON AUTHORS COMMUNICATION.

Objectives: Aim of the present research work is to prepared rapid mouth dissolving film of frovatriptan Succinate. Methods: Rapid Dissolving Film is prepared by Solvent casting method, hydroxypropyl methylcellulose E3 and E15 are helpful in the film-forming polymer, plasticizer in propylene glycol disintegrant is croscarmellose sodium, the artificial sweetener in aspartame as, citric acid as saliva stimulant, xylitol as diluents and natural sweetener, wild cherry as a flavour and Brilliant blue dye for elegance was selected for Rapid Dissolving Film preparation. By prism, software result is obtained and then evaluated using analysis of variance (ANOVA). Results: The result suggested that the formulation containing 20% w/w aspartame, 10% w/w xylitol and 5% citric acid was found to effectively obscure the bitter taste of drug with best overall acceptability. The same composition of aspartame, citric acid and xylitol were used for further optimization using design of an experiment to continue obscuring the bitter taste of frovatriptan Succinate. Simple lattice mixture design which is helpful in drug formulation by using polymer plasticizer and disintegrant concentration for disintegration time-independent variable tensile strength and percentage elongation for the response. Conclusion: The effect of each variable, two and three-factor interactions were studied. The batches were numerically optimized to give a design space. Rapid mouth dissolving films are also found to behave better patient compliance in all the age groups.

NOTE: THE ARTICLE HAS BEEN RETRACTED BASED ON AUTHORS' REQUEST.

Bioengineered Silver Nanoparticle from Spirulina platensis in Attenuating Biofilm Mediated Virulence in Vibrio parahemolyticus: An in vitro and in vivo Approach

Rathna Kumarasamy, Padavala Navyaka, Ekramul Haque — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: In this study, bioengineered AgNPs (silver nanoparticles) from Spirulina platensis was used to counter the biofilm mediated virulence by Vibrio parahemolyticus. Methods: AgNPs were synthesized from crude Spirulina platensis extract and characterized using UV spectrophotometry, Transmission electron microscope (TEM). Antibacterial effect against aquatic pathogen Vibrio parahemolyticus was carried out. Further, the nanoparticle at sub MIC (minimum inhibitory concentration) level were screened for anti-virulence property under in vitro studies which include biofilm inhibition using microtiter plate assay, microscopic analysis under light microscope and SEM (Scanning electron microscope) imaging, EPS (Exopolysaccharide) inhibition, CSH(Cell surface hydrophobicity) inhibition using BATH(Bacterial adhesion to hydrocarbons) assay, swarming and swimming motility inhibition, growth pattern analysis followed by in vivo study in aquatic animal model brine shrimp and its survival percentage along with light microscopic imaging was performed. Results: AgNPs, at 320μg/ml showed bactericidal activity, minimal inhibitory concentration was found to be 160 μg/ml. All anti-virulence assay performed at below sub MIC concentration. Biofilm and EPS showed 63% and 53% inhibition respectively, CSH was found to be decreased 3-fold. Growth pattern at sub MIC compared with non-treated showed similar result. In vivo study increased survival percentage (90%) when treated with AgNPs, compared to untreated (20%). A 7-fold increased resistance to pathogen was found and light microscope also confirms the efficacy of Ag nanoparticle. Conclusion: AgNPs become a substitute to the current commercial antibiotics used in aquaculture against Vibriosis, by functioning as an efficient quorum sensing inhibitor.

α-(1→4)-linked D-galacturonic Acid Based Linear Homopolymer as Drug Release Modulator in HPMC Based Hydrodynamically Balanced System

Amit Verma, Neetu Sacha, Kamla Patha, Anurag Verma — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: Natural polysaccharides are increasingly being used for diverse applications in drug delivery such as controlled release of drugs owing to their wide availability, renewability, biodegradability and biosafety. Furthermore, polysaccharides from plants utilized as food may possibly mitigate regulatory requirement for approval as well. Mung bean (Vigna radiata L. seeds) is a key cereal in India composed of several non-starch polysaccharides. In the present work we have attempted to isolate, characterize and pharmaceutically evaluate the polysaccharide derived from dehusked Mung beans using water-acetone precipitation method. Methods: The obtained polysaccharide was characterized using Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry, Powder X-ray diffraction and ¹³C Nuclear Magnetic Resonance spectroscopy. Further, the polysaccharide derived from Mung beans was carboxymethylated using Williamson Ether Synthesis. The degree of substitution of carboxymethylated Mung bean polysaccharide was determined to be 0.76. The carboxymethylated polysaccharide was then used in combination with hydroxypropyl methylcellulose K4M to fabricate hydrodynamically balanced sustained release capsule dosage form taking moxifloxacin HCl as model drug. Results: The system emerged as a hydrodynamically balanced system that remains floated for 12 hr. The drug release mechanisms involved swelling, dissolution and erosion of polymer matrices. The erosion operated at later times and was sensitive to the osmotic stress exerted by ionic polymer and the drug present in the matrix. Conclusion: The findings of the study suggest that polymer matrices composed of chemically modified Mung bean polysaccharide and hydroxypropyl methylcellulose K4M may form a promising carrier for sustained stomach specific delivery of model drug moxifloxacin Hydrochloride.

Preparation of Topical Nano Gel Loaded With Hesperidin Emusomoes: In vitro and in vivo Studies

Yeramanchi Sarah Sujitha, Yallamali Indira Muzib — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: The objective of the present study was to increase the solubility of poorly soluble drug hesperidin and to increase the efficacy of the drug by loading hesperidin in emulsomal topical gel. Methods: Hesperidin was loaded into emulsomes by using ethanol injection method. The optimized formulation of emulsomes was evaluated by SEM, FT-IR, DSC, P-XRD, in vitro drug release, ex-vivo skin permeation studies, in vivo pharmacokinetic and pharmacodynamic studies. Results: The SEM study shows the emulsomes were tiny and spherical in structure. The particle size and zeta potential of the optimized formulation was found to be 50nm and -1.8mV and in vitro drug release was found to be 98.6% for 6 hrs. The optimized emulgel was prepared by using different gelling agents Carbopol 934 and HPMC. The prepared gels were found to be homogenous and skin permeation studies was found to be 98.9% for 4 hr, with skin permeation efficacy bearing flux value 12.3μg/cm²/h when compared to the pure hesperidin gel. The in vivo pharmacokinetic and pharmacodynamic studies were found to be more efficient for the hesperidin loaded emulsomal gel when compared to the marketed formulation. Conclusion: Hesperidin emulsomal gel has shown a significant increase (p<0.05) in activity when compared to the marketed formulation.

Self Nano-emulsifying Drug Delivery System to Enhance Solubility and Dissolution of Candesartan Cilexetil

Pathuri Raghuveer, Avula Prameela Rani — Thu, 10 Dec 2020 00:00:00 +0000

Aim: Self nano-emulsifying drug delivery system (SNEDDS) of candesartan cilexetil was explored to enhance its oral bioavailability. SNEDDS has tremendous potential in enhancing oral bioavailability of poorly aqueous soluble therapeutic agents. SNEDDS are pre-concentrate mixture of oil, surfactant and co-surfactant produces nanoemulsion after oral administration due to mild agitation produced by gastro motility within the size range of 20-200nm. Methodology: The formulations were developed by selecting capmul MCM^®, triacetin^® and caprylic acid® under the oil phase based on solubility of drug; cremophore RH40^®, brij35^® under surfactants category and transcutol P under co-surfactant on basis of their emulsification property. Optimum concentrations were choosen from the Terinary phase diagrams and evaluated for their properties. Results: From the results of ternary diagrams 16 formulations were selected (A1, A2, A3, A4, B1, B2, C1, C2, C3, C4, D1, D2, E1, E2, F1, F2) and subjected to characterization studies. Best formulations were subjected to particle size analysis and in vitro release studies. Among selected formulations, A1 and C1 have shown high in vitro drug release profiles with less selfemulsification time having grade A dispersibility without any precipitation and phase separation. Discussion: Concentration of surfactant helps in reducing the size of the particle when compared to the co-surfactant concentration. Enhanced dissolution of candesartan cilexitil may be attributed to the spontaneous formation of nanoemulsion in vitro with a decreased particle size that leads to the increased surface area leaving the drug candesartan as finely dispersed particles in dissolution media. Conclusion: Formulation C1 consists of triacetin oil 30% w/w, cremophore RH 40 6%w/w and transcutol P 64%w/w showed best emulsification characteristics like 99% percent transmittance, with increased dissolution profile (98%) than pure drug (45%) with nano range goblet size (165.9nm).

Quality by Design based Development and Validation of RP-HPLC Method for Simultaneous Estimation of Sitagliptin and Metformin in Bulk and Pharmaceutical Dosage Forms

Balamurugan Krishnan, Kirtimaya Mishra — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: This paper portrays a recently developed, optimized and validated isocratic RP-HPLC strategy for the separation of two antidiabetic drugs (sitagliptin and metformin) in bulk and pharmaceutical formulations with the aid of quality by design and multi-criteria decision making approach. Methods: The effective chromatographic separation was accomplished by utilizing the Monolithic C₁₈ segment (100×4.6 mm id, 5μm molecule size) and PDA-UV- detection at 210nm.The scope of independent variables utilized for the streamlining were methanol: 40- 50% v/v, pH: 3.5-4.5 and flow rate:0.3-0.5ml/min. Results: Ideal conditions decided for assay were methanol, acetonitrile, pH 3.5±0.5 balanced with the diluted orthophosphoric acid solution and flow rate of 0.484ml/min and pH 3.946. Peak area ratio of the analyte was utilized for the evaluation of pharmaceutical formulation tests. Total chromatographic analysis time per sample was approximately 4.33 min with metformin and sitagliptin eluting with retention times of 3.3 and 4.4 min respectively. The optimized assay circumstance was validated as per ICH guidelines and applied for the quantitative analysis of marketed tablets containing sitagliptin and metformin. Conclusion: The validation study upheld the determination of the assay conditions by affirming that the assay was specific, accurate and linear, precise and robust. Therefore, this RP-HPLC method can be used as a routine quality control analysis of gliptin derivative like sitagliptin in combination with metformin.

Altitude Variation in Volatile Composition of Blueberry Leaf Analyzed by SPME GC-MS

Thu, 10 Dec 2020 00:00:00 +0000

Background: The present work was aimed to carry out volatile component analyzes in Vaccinium arctostaphlyos L., V. uliginosum L., V. vitis-idaea L. and V. myrtillus L leaf growing at different altitudes of the East Blacksea Region of Turkey. Methods: The leaf of Vaccinium species were harvested from twenty-one different altitudes (748-3035 m) from six cities (Artvin- Ardahan-Rize-Trabzon-Gümüşhane-Giresun) of Turkey. The diversity of volatiles in the leaf was investigated by SPME GC-FID/MS. Results: The major constituents of the Vaccinium leaf showed variation with changes in altitudes. The identified volatile components of V. arctostaphlyos and V. uliginosum were represented mainly by aldehydes in all altitudes, whereas monoterpenes were found the major constituent of V. vitis-idaea at Posof-Ardahan (2376 m) and Artvin (2553 m) samples. In all altitudes, capronaldehyde (7.23-28.96%) and 2(E)-hexenal (8.90-53.59%) in the leaf of V. arctostaphlyos; capronaldehyde (17.04-37.09%) and limonene (16.50- 47.51%) in the leaf of V. vitis-idaea and capronaldehyde (4.55-39.90%), 2(E)-hexenal (25.08-80.99%) and hexadecane (2.97-11.32%) in the leaf of V. uliginosum; and capronaldehyde (14.66-37.26%) and 2(E)-hexenal (18.18-37.59%) at the altitudes of 1912m, 2533 m and 2565 m in the leaf of V. myrtillus were the major constituents with the different percentages, respectively. 2-Bornanone (32.86%) at the altitude of 2613 m and 3-penten- 2-one (93.60%) at the altitude of 2811m in the leaf of V. myrtillus were found to be the major compounds. Conclusion: Comparisons of the volatile components of V. arctostaphlyos, V. uliginosum, V. vitis-idaea and V. myrtillus in different sites showed significant differences among populations at different altitudes.

Stability Indicating LC-MS Method Development and Validation for the Study of the Forced Degradation Behavior of Pimobendan Drug

Thu, 10 Dec 2020 00:00:00 +0000

Objectives: Analytical methods are necessary for the field of pharmaceuticals to discover the drug, determination of drugs and metabolites in biological matrices. The present study aimed to develop liquid chromatography-tandem mass spectrometry (LC-MS) and validation for quantification of Pimobendan in the formulation. Methods: The mobile phase composition was methanol, acetonitrile and 0.1 M phosphate buffers in the ratio of 45:15:40 (v/v) mixtures with isocratic elution. Prontosil ODS C₁₈ column (250 × 4.6 mm, 5μ) was selected for separation with 264nm of LC UV detector wavelength. Ionization mass spectrophotometer was analyzed at nitrogen gas flow at 300 Psi and 300°C of source temperature. Mass spectrometry analysis of Pimobendan drug fragments was performed by introducing column eluting into equipment for Q1 and MS scan. Results: The drug was eluted at 3.56 min retention and the calibration curve was achieved at 0.5-250 μg/ml standard concentration. Different parameters of validation (linearity, specificity, precision, accuracy, selectivity and robustness) were performed and results confirm that all the parameters are in the acceptable limit. In the electrospray ionization spectra of Pimobendan [M+H], positive ions were observed at an m/z value of 335.42. The product-ions of 335.42 were observed at m/z value of 319.18, 287.19, 277.09, 261.08, 250.16, 223.30, 111.47 and 86.05. Conclusion: The proposed method is successfully achieved the acceptance criteria of all validation parameters and stability studies.

Novel Development of RP-HPLC Method to Quantify Amoxicillin, Omeprazole and Rifabutin in Combination

Rama Kumar Kandula, Raja Sundararajan — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: Helicobacter pylori infections are liable for most of the ulcers in the stomach and small intestinal. Talicia capsules was approved to be prescribed for the Helicobacter pylori infections. These capsules have combination of amoxicillin (ACN), omeprazole (OPE) and rifabutin (RFN). In this present study, for the first time, we developed a stability demonstrating RP-HPLC methodology to quantify ACN, OPE and RFN simultaneously. Methods: Assay of this combination was done with Thermo C₁₈ stationary phase column using the mobile phase solvent system of 0.1M KH₂PO₄ buffer (3.5 pH): acetonitrile. Degradation tests were done on ACN, RFN and OPE solution by applying five different conditions, i.e. 0.1N HCl, 0.1N NaOH, 30% H₂O₂, 105°C and sun light. Results: Retention times of ACN, RFN and OPE were 2.539 min, 3.863 and 5.423 min, respectively. Method linearity scope was ranged from 125 – 375 μg/ml for ACN, 5 – 15 μg/ml for OPE and 6.25 – 18.75 μg/ml for RFN. The accuracy was computed in the range of 98.13–101.07% and the precision was between 0.282% and 0.569% relative standard deviation for three drugs. The method can effectively separate the degradation products from ACN, RFN and OPE. Conclusion: The results demonstrated that this method can be employed to quantify ACN, OPE and RFN simultaneously in presence of impurities produced during degradation investigation.

A Novel Ultra Performance Liquid Chromatography-PDA Method Development and Validation for Alectinib in Bulk and its Application to Tablet Dosage Form

HK Sundeep Kumar, Sujit Kumar Sahu, Jitendra Debata — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: To develop a novel ultra-performance liquid chromatographic technique for the estimation of alectinib in a API and tablet. Methods: The chromatographic separation was achieved using DIKMA Endoversil (2.1 x 50mm, 1.7μm) column, mobile phase was phosphate buffer, pH 4.6 and methanol as a mobile phase (45:55) with a flow rate of 0.4 mL/min and eluent was monitored at 265 nm. The method was continued and validated in accordance with International conference on harmonization guidelines. Validation study revealed the specificity and reliability of the method. Results: In this method alectinib was eluted with retention time of 0.418 min. Calibration curve plots were found linear over the concentration ranges 1-100 μg/mL for alectinib. Limit of detection was 0.015μg/ml and limit of quantification was found 0.07μg/mL. The % assay of the marketed dosage form was found 97.80 %, even the present approach was found to be effective in the analysis of alectinib in force degradation condition. Conclusion: The experiential evidences of all the study results revealed the suitability of the estimation of alectinib in API and tablet formulation.

Apoptosis Induction and Anticancer Activity of 2, 4-bis (1-phenylethyl) Phenol from Clerodendrum thomsoniae Balf.f. in vitro

VK Muhammed Ashraf, VK Kalaichelvan, R Ragunathan, V V Venkatachalam — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: Plant phenolic have extended significance as a promising therapeutic candidate for several disorders including cancer. Apoptosis is a well-organized cell death that has importance in cancer research. The present study was aimed to isolate 2, 4-bis (1-phenylethyl) -phenol from Clerodendrum thomsoniae Balf.f. and evaluation of cytotoxicity on human breast cancer cells. Methods: MTT assay was used to estimate cell viability. Apoptosis was analyzed by Annexin V/PI staining, EtBr staining, cell cycle analysis and MMP assay. Results: In this study 2,4-bis (1-phenylethyl) -phenol was separated from aerial parts of C. thomsoniae and its structure was confirmed by different spectroscopic methods. The IC₅₀ value was determined based on cell viability rates and the value was calculated as 12. 58 (μg/mL). Apoptosis analysis by annexin V/PI staining showed that died cells were stained as red fluorescence. The loss of mitochondrial potential as a result of the induction of apoptosis was noted. The EtBr assay showed early apoptotic cells, late apoptotic cells, necrotic cells and, dead cells with characteristic fluorescence. The apoptosis induction of 2, 4-bis (1-phenylethyl) –phenol was also noticed in Cell cycle analysis using flow cytometry. Conclusion: The outcome of this research work, we can conclude that 2, 4-bis (1-phenylethyl)-phenol may be a successful candidate for breast cancer therapy via apoptosis activation and farther in vivo studies are required to evaluate this compound for its safety and efficacy as a potential anticancer candidate.

Effect of Deoxycholic Acid on Immune Cells - An Immunophenotyping Analysis of Peripheral Blood and Splenic Lymphocytes in CD57 Female Mice

Praveen Kumar Reddy Moole, Jagan Mohan Reddy Papireddypalli — Thu, 10 Dec 2020 00:00:00 +0000

Background: Deoxycholic acid has been used in Chinese traditional medicine “Niuhuang” that is known to have Immunoregulatory and anti-inflammatory properties. Preliminary evidences have shown that Deoxycholic acid modulates the immune system by way of stimulation and helps in maintaining a disease-free state within an individual. The aim of this study was to investigate the effect of Deoxycholic acid on immunophenotyping analysis of peripheral blood and splenic lymphocytes in CD57 female mice. Methods: Animals were treated with control, 100, 500 and 1000 mg/kg of Deoxycholic acid for 14 days. The animals were euthanized on Day 15 and blood and intact spleens were collected. The homogenized spleens were collected aseptically and prepared single cell suspension of splenocytes. The whole blood and spleen cells were analyzed by flow cytometry. Results: At 100 mg/kg and 500 mg/kg, 2-fold increase in total lymphocytes (CD45) and significant increases in lymphocyte (T-cell) population and sub-populations of T-cell (Helper T-cell, Cytotoxic T-cell) were observed. Increased (up to 77%) proliferation of B-cells was observed at these doses. Similar trends, but at lesser magnitude as compared to 100 and 500 mg/kg, were observed at 1000 mg/kg, this was due to the toxicity observed at this dose. No treatment related changes in the populations of Lymphocytes of spleen. Conclusion: From the results of the present study, it was suggested that Deoxycholic acid treatment modulates the immune system by activating both cell mediated and humoral immune system.

In vitro Investigation of Conventional, Chitosan Coated and Electrosteric Stealth Liposomes of Rivastigmine Tartrate for the treatment of Alzheimer’s Disease

Srinivas Hebbar, Manasa Poonja, Amitha Shetty, Akhilesh Dubey — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: The main objective of the present investigation was to develop and compared conventional, chitosan-coated and electrosteric stealth liposomes of Rivastigmine Tartrate for the treatment of Alzheimer’s Disease. Methods: The solvent evaporation method was employed to prepare liposomes and optimized by the Design of Experiment approach. The effect of various process parameters was investigated and optimized on for particle size and percentage entrapment efficiency. The compatibility studies were carried out using Fourier Transform Infrared Spectroscopy. The optimized formulations were also characterized by Transmission Electron Microscopy and Atomic Force Microscopy for their surface morphology and in vitro percentage drug release study by comparing it with a standard solution of Rivastigmine Tartrate. The compatibility of drug and excipient mixtures was confirmed by Fourier Transform Infrared Spectroscopy. Results: The optimized formulation of conventional, chitosan-coated, stealth liposome of Rivastigmine Tartrate showed vesicle size of 111.8, 153.3, 136.3 nm respectively and entrapment efficiency of 75.27±0.8 %, 80.33±0.4 % 78.2±0.2 respectively. Clear surface morphology was observed through surface morphological images. The in vitro drug release studies showed a significant difference in percentage cumulative drug release pattern of chitosan-coated and stealth liposomes (81±0.3 % and 76±1.2 %) when compared with the conventional liposomes (69±0.8 %), after 24 h. On subjecting it to stability studies, the liposome preparations did not show any significant changes in particle size and entrapment efficiency. Conclusion: The developed formulations (chitosan-coated and stealth liposomes) can deliver the active moiety on the target site for the treatment of AD.

Antibacterial Activity of Extracts of Solanum xanthocarpum, Aegle marmelos and Capparis spinose Against Antibioticresistant Staphylococcus cohnii

Thu, 10 Dec 2020 00:00:00 +0000

Background: The antibacterial activity of plant extracts and phytochemicals analysis was evaluated with antibiotic susceptible and resistant micro-organisms. In addition, of the possible coefficient effects when associated with antibiotics were studied. Extracts from the following plants Solanum xanthocarpum, Aegle marmelos and Capparis spinose were utilized. Materials and Methods: Collected clinical samples were inoculated in different media and the plates were incubated at 37°C for 48 hr. After incubation to identified Colony Morphology, Microscopic Observation and biochemical characterization and molecular identification of the Selected Bacterial isolate as Staphylococcus cohnii. Extracts from the following plants were Solanum xanthocarpum, Aegle marmelos and Capparis spinose were utilized. Antimicrobial Susceptibility Assay and Minimal inhibitory concentration tests performed. Results: Ethanol, methanol and chloroform extracts of Solanum xanthocarpum, Aegle marmelos and Capparis spinose gave the maximum zones of inhibition of 20 mm, 9 mm in ethanol, 25 mm to17 mm in methanol and 24 mm to 12mm in chloroform extract and MIC values of 1.03 to 0.51 mg/ml, 1.00 to 0.06 mg/ml and 1.03 to 0.60 mg/ml respectively, against Staphylococcus cohnii. Methanol extracts of Solanum xanthocarpum gave the maximum zones of inhibition of 25 mm followed by ethanol 20 mm and 24 mm chloroform extracts. The highest MIC values 0.06 mg/ml in methanol extract respectively and 0.51mg/ml in ethanol and 0.60mg/ml in chloroform extract against Staphylococcus cohnii. The result indicated that all extracts exhibited antibacterial activity against Staphylococcus cohnii. Conclusion: The methanol extract showed greater activity than ethanol and chloroform extracts. Among various extracts, only the methanol extract show potential agents against bacterial Staphylococcus cohnii strain greater than standard Vancomycin test control. Thus, the extract of Solanum xanthocarpum could be used to treat microbial wound infection. Solanum xanthocarpum have the potential to be developed as antibacterial agents, especially against Staphylococcus cohnii strain.

Screening of Antimicrobial and Antioxidant Activity of Acetone Extracts of Heritiera fomes Whole Plant against Pathogens

Thu, 10 Dec 2020 00:00:00 +0000

Background: Phytochemicals are well known to have many important pharmaceutical properties. Heritiera fomes grows in low saline environments. The present study was initiated to explore the biologically beneficial properties of H. fomes. Methods: The crude extracts of H. fomes were extracted in acetone by orbital shaker and concentrated using rota evaporator. Total flavonoid content and Total phenolic content were estimated spectrophotometrically and the in-vitro antioxidant capacity was estimated by DPPH (2,2-diphenyl-1-picrylhydrazyl), Ferric Reducing Antioxidant Power (FRAP) and Hydrogen peroxide (H₂O₂) Scavenging Assays. Anti-microbial activity was determined by Disc diffusion method. Results: Phytochemical screening of acetone extract of H. fomes showed the presence of major classes of phytochemicals like alkaloids, glycosides, flavonoids, saponins, carbohydrates, phenols and sterols in considerable quantity. The total amount of phenolic and flavonoid content was found to be 75.3 mg GAE/g dry weight and 61.3 mg QE/g dry weight respectively. Antioxidant activity of plant extract determined by using different assays like H₂O₂ radical scavenging, DPPH and FRAP. A positive correlation between all the pairs of antioxidant assays was observed. Further, antimicrobial activity against various pathogens was evaluated by disc diffusion method where the zone of inhibitions were found to be in range from 5± 0.35 to 12 ± 0.50 mm. Conclusion: The study concludes that the plant Heritiera fomes has its effect in scavenging free radicals and has a potential to be a power antioxidant. Several in-vitro studies possess significant antioxidant, antimicrobial activities. The present study plays an important tool for new drug discovery.

Antiparkinsonian and Antioxidant Effects of Hydroalcoholic Extract of Camellia sinensis, Asparagus racemosus, Mucuna pruriens and their Combination

Thu, 10 Dec 2020 00:00:00 +0000

Objectives: Because of environmental risk factors Parkinson’s disease rate doubled in last decades. In upcoming decades rate of Parkinson’s disease is expected to be 12 million people in aging population. Present treatments are having huge side effects and requires more combinations. Hence objective of this study is to provide herbal combination for Parkinson’s disease with reduced side and adverse effects. Methods: The antiparkinsonian activity of HECS, HEAR, HEMP and Mixture was evaluated by using haloperidol induced catalepsy, reserpine induced hypolocomotion, tacrine induced vacuous chewing movements and orofacial brusts. Antioxidant activity was assessed by using DPPH radical and H₂O₂ scavenging assay. The results were analyzed by repeated measure ANOVA followed by Dunnett’s test. Results: Significant reduction (P<0.05) in haloperidolinduced catalepsy was observed in the all groups at the doses of 30 and 100 mg/kg when given orally. Mixture 30 mg/kg showed extremely significant (P<0.001) reduction in duration of catalepsy. Pretreatment with Mixture at 100mg/kg was significantly (P<0.05) reduces Reserpine induced hypolocomotion which is more significant as compared with other treatments. Similarly, HECS 30 mg/kg and mixture was more effective (P<0.05) than remaining extracts in reducing tacrine induced Vacuous chewing movements. In tacrine induced orofacial brust Mixture and HEAR 30 mg/kg shows extremely significant (P<0.001) reduction of orofacial brusts. Similarly Mixture and HECS 100 mg/kg is more effective than other treatment in tacrine induced tongue protrusion. In DPPH scavenging assay, all the extracts exhibited free radical scavenging activity. In DPPH assay the IC₅₀ value of ascorbic acid, HECS, HEAR, HEMP and Mixture (1:1:1) was 14.99, 18.44, 26.51, 23.19 and 20.47 μg/ml respectively. Conclusion: 1:1:1 mixture show extremely significant antioxidant and anti-parkinsonian activity as compare with individual hydroalcoholic extract. Thus the studied combination possess potent antiparkinsonian effect.

Pyocyanin Assisting Biosurfactant Mediated Anti-shrimp Pathogen Activity and Crude Oil Recovery

Sriram Shankar, Ekramul Haque, Saqib Hassan — Thu, 10 Dec 2020 00:00:00 +0000

Background: The unflagging engrossing biosurfactant, representing ecological substitute to their synthetic equivalent has gained enormous attention in the 21^st century and their potential applicability in food, medicine and petrochemical industries is being explored and expanding. Objectives: The current study deals with the applicability of pyocyanin and biosurfactant in crude oil recovery and use as a potential anti-shrimp pathogen agent. Materials and Methods: The bacterial strain Pseudomonas aeruginosa ENO-14 was explored for their biosurfactant production using Luria Bertani Broth and Bushnell-Haas Broth supplemented with 1% glucose under shaking condition and pyocyanin production using Luria Bertani Broth under static and shaking conditions. The highest concentration of biosurfactant (11.07±0.15mg/ml) was obtained after 48 h at 37°C in 200 rpm and the maximum production of pyocyanin (70.12±2.11 μg/ml) was observed after 96 h at 37°C under static condition. Further Emulsification activity was evaluated using cell-free supernatant, biosurfactant alone and a combination of pyocyanin (0.01%) and biosurfactant (0.1%). Finally, the produced pyocyanin and biosurfactant were used as anti-shrimp pathogen activity by agar well diffusion assay and in crude oil recovery by sand pack column. Results: 100 % emulsification were observed for the crude oil when treated with pyocyanin and biosurfactant in a union. The noteworthy outcome of this experiment is the prominent role played by pyocyanin in enhancing the emulsification of hydrocarbons. Moreover, as a novel observation, there was an additional significant increase (80%) of residual oil recovered by sand pack column when both pyocyanin and biosurfactant were tested in conjunction as compared to the recovery obtained when biosurfactant was administered alone (65%). Furthermore, both the compounds exhibited significant anti-shrimp pathogen activity. Conclusion: Therefore, biosurfactant and pyocyanin could have promising applications in the aquaculture and petrochemical industries.

Randomized Control Trial to Assess the Efficacy and Safety of NRL/2019/5PNW with Micronutrient Fortification to Promote Health and Well-being in Woman in Fertile Age

Thu, 10 Dec 2020 00:00:00 +0000

Background: Women appear with gender-specific nutritional requirements that may affect their well-being. The nutritional requirements are there for women in rural, suburban and urban regions altogether. Objective: Netsurf Communications Pvt. Ltd. has developed the NRL/2019/5PNW for the women to help manage their health and wellness. The current research is designed to assess safety and efficacy of the test product. Methods and Materials: The trial is randomized, controlled prospective clinical trial. In the present study, 110 subjects were screened. Total 100 subjects were considered evaluable cases at the end of the study 1:1 in test and Marketed product treated group. Results: Test product was better in activity than marketed product in improving energy levels of the subjects throughout the day, elevating mood, improving quality of sleep and reducing stress. Improved glycemic control and reduction in total cholesterol levels were significantly reduced in test group which has preventive potential of metabolic diseases. Less events of recurrent UTI/ RTI in test treated group suggestive of improvement in immune status of females. Conclusion: NRL/2019/5PNW is safe and effective in promoting health and wellbeing in females in fertile age.

A Double-blind, Placebo-controlled, Randomized Comparison of Analgesic Efficacy of Oral Ketorolac Versus Intramuscular Tramadol After Third Molar Surgery

Fazil Arshad Nasyam — Thu, 10 Dec 2020 00:00:00 +0000

Background: Pain due to dental extraction, particularly after the third molar extraction causes discomfort to patients. Different types of analgesics used to manage pain in such cases include nonsteroidal anti-inflammatory drugs and opioids. Objectives: To evaluate the pre-emptive analgesic effectiveness of oral ketorolac and intramuscular (IM) tramadol following lower third molar surgeries. Materials and Methods: A total 60 subjects with impacted mandibular third molars were included in our study. They were randomized into two treatment groups, each with 30 patients. Group A: oral ketorolac 10 mg and IM placebo (1 mL saline solution); Group B: oral placebo (tablet similar to oral ketorolac) and IM tramadol 50 mg diluted in 1 mL saline solution. The treatment regimen were given half an hour before the start the surgery. The parameters evaluated were pain intensity, the time of first analgesic rescue medication and total analgesic consumption. Results: We found that the time of first rescue analgesic medication was longer in oral ketorolac group than IM tramadol group (P=0.01). Group A patients experienced less pain than Group B patients. Conclusion: We found that oral ketorolac group of patients had an enhanced analgesic effectiveness and a longer time of first rescue analgesic than those taking intramuscular tramadol.

Efficacy of Sitagliptin Versus Glimepiride 1-3 mg for Treatment of Type-2 Diabetes Patients

Bhaskar Joshi, Praveen Yadav, Annabathini Geetha Bhavani — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: This study is to compare the effect of Sitagliptin and Glimepiride 1-3mg as a combination therapy for type-2 diabetes mellitus patient’s treatment. It is also concern to evaluate the effect of low dosage on type-2 diabetes mellitus patients as an antidiabetic drug. Methods: The type-2 diabetes patient’s clinical data was analyzed during the treatment through the inclusion and exclusion selection methods. The samples of Sitagliptin (1-3 mg) as add on therapy were chosen by open-label study by randomization on type-2 diabetes mellitus. The total 45 patients (n=45) with age group between 20-60 years was received for statistical analysis. The samples are screened by inclusion with the baseline of HbA_1c was ≥7.0 % and ≤ 10.5 % was selected. The exclusion criteria are restricted to upper age limit of 60 years and having the symptoms of chronic kidney, hepatic, malignancy. Results: The data of combination therapy is compared with initial data and after 14 weeks of treatment data is considered for the effect of antidiabetic drugs. The statistic results show with greater improvement in HbA_1c value and total daily dose of insulin were achieved with Sitagliptin compared to Glimepiride therapy. Conclusion: Finally, Sitagliptin 100mg is an add-on to Metformin treatment shows more adequate results with better tolerance on type-2 diabetes with satisfactory glycemic control is found to be significant reduction with daily dose of insulin in the body.

Synthesis, Docking and Anti-cancerous Activity of Some Novel Thiazole Derivatives of Biological Interest

Anitha Ramalingam, Sarvanan J — Thu, 10 Dec 2020 00:00:00 +0000

Objectives: Heterocyclic compounds are enormously widespread in nature and have attracted research interest because of their pharmaceutical and biological properties. Amongst the heterocyclic rings, the thiazoles are the most important building blocks in today’s drug discovery and are found to have extensive biological activities against different types of diseases. Many potent anti-cancerous drugs like Tiazofurin are having 1,3 thiazole as an active ring structure and based on this theory, a new series of 2, 4 di substituted 1,3 thiazole derivatives were synthesized. Methods: First 2-amino-4-substituted phenyl thiazoles were synthesized by adapting a well-known Hantzsch reaction and subsequently 2-amino substituted derivatives were synthesized using various aryl aldehydes by following established Schiff’s reaction. The synthesized compounds were confirmed by TLC, IR, HNMR, CNMR and Mass Spectral Analysis. Then all the synthesized compounds were docked to RAS p21 receptor using PATCH DOCK Software to study their anti-cancerous activity. Then the compounds were screened for cancer cell line studies. Results: All the synthesized compounds exhibited some degree of anti-cancerous activity both in docking studies and in vitro anti-cancerous cell line studies. Conclusion: Amongst all the 16 synthesized, most compounds showed moderate to good anti-cancerous activity and the compounds S3P1c, S3P2c, S3P2d, S3P3a and S3P4d have shown the best activity.

Correlates of Attitude Towards Amyotrophic Lateral Sclerosis among Health Care Students - A Cross-sectional Study Findings

Muhammad Zahid Iqbal, Salah-Ud-Din Khan, Muhammad Shahid Iqbal — Mon, 16 Nov 2020 00:00:00 +0000

Objectives: To evaluate correlated factors (correlates) of attitude towards Amyotrophic Lateral Sclerosis (ALS) among health care students in a medical university. Methods: A stratified convenient sampling technique was used to calculate the sample size for the current study in three different health care faculties. A pre-validated and self-developed questionnaire was used for data collection of the present study. The Statistical Package for Social Sciences (SPSS) version 24.0 was utilized for data analysis and the interpretation of the results with the help of both descriptive and inferential statistics. Results: A total of 268 health care students from three faculties (medical, pharmacy and dental) participated in the current study. In univariate analysis, a statistical significance (p<0.05) was observed in all of the studied variables. Conversely, in multivariate logistic regression model, gender, faculty, year of education and residence variables were observed as statistically significant (p<0.05). Conclusion: This study confirmed that gender, faculty, year of education and residence were the correlates (pure) of the attitude towards ALS among health care students of a medical university in Malaysia.

Study of Polymorphism on Pargeverine Hydrochloride

Gopal Krishna Rao, Nutan Naik — Sun, 11 Oct 2020 00:00:00 +0000

Objectives: Screening active pharmaceutical ingredients for polymorphs is of utmost importance in drug development to enable stable APIs, robust manufacturing processes and reduction of costs incurred in switching over crystal forms. The current study deals with exploring polymorphism in Pargeverine Hydrochloride using different solvents and solvent systems. Methods: Drug was crystallized by slow solvent evaporation of filtered saturated solution using either single or mixed solvent systems. The resultant crystals were evaluated for physical appearance and by Fourier transform Infrared Spectroscopy, Differential Scanning Calorimetry and Powder X-Ray Diffraction. Results: The physical appearance, melting points, pattern of heat flow for phase transition, peak temperature and the IR spectra and Powder X-Ray Diffraction pattern of the crystals of Pargeverine Hydrochloride in single and mixed solvent systems (50 solvent systems) did not show any marked difference from that of pure drug. Conclusion: From the results, it can be concluded that there were minimal possibilities of polymorph formation for Pargeverine HCl in the solvent/s or combination of solvents attempted, thus need for any specific controls to inhibit transition during its routine manufacturing process may not be required.