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2017| January-March | Volume 7 | Issue 1
Online since
March 17, 2017
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ORIGINAL RESEARCH ARTICLES
Formulation and evaluation of transdermal drug delivery of topiramate
Suneetha Cherukuri, Uma Rajeswari Batchu, Kiranmai Mandava, Vidhyullatha Cherukuri, Koteswara Rao Ganapuram
January-March 2017, 7(1):10-17
DOI
:10.4103/jphi.JPHI_35_16
PMID
:28405574
Background:
Transdermal drug delivery system (TDDS) was designed to sustain the release and improve the bioavailability of drug and patient compliance. Among the various types of transdermal patches, matrix dispersion type systems disperse the drug in the solvent along with the polymers and solvent is allowed to evaporate forming a homogeneous drug-polymer matrix. The objective of the present study was to design and formulate TDDS of topiramate (TPM) and to evaluate their extended release
in vitro
and
ex vivo
.
Materials and Methods:
In the present study, an attempt has been made to develop a matrix-type transdermal therapeutic system comprising TPM with different ratios of hydrophilic and hydrophobic polymeric combinations using solvent casting technique.
Results:
The physicochemical compatibility of the drug and the polymers was studied by Fourier transform infrared spectroscopy. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. The patches were further subjected to various physical evaluations along with the
ex vivo
permeation studies using pig ear skin.
Conclusions:
On the basis of results obtained from the physical evaluation and
ex vivo
studies the patches containing the polymers, that is, Eudragit L 100 and polyvinylpyrrolidone, with oleic acid as the penetration enhancer were considered as the best formulations for the transdermal delivery of TPM.
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REVIEW ARTICLE
Spherical crystallization: A technique use to reform solubility and flow property of active pharmaceutical ingredients
Arindam Chatterjee, Madan Mohan Gupta, Birendra Srivastava
January-March 2017, 7(1):4-9
DOI
:10.4103/jphi.JPHI_36_16
PMID
:28405573
Tablets have been choice of manufacturers over the years due to their comparatively low cost of manufacturing, packaging, shipping, and ease of administration; also have better stability and can be considered virtually tamper proof. A major challenge in formulation development of the tablets extends from lower solubility of the active agent to the elaborated manufacturing procedures for obtaining a compressible granular material. Moreover, the validation and documentation increases, as the numbers of steps increases for an industrially acceptable granulation process. Spherical crystallization (SC) is a promising technique, which encompass the crystallization, agglomeration, and spheronization phenomenon in a single step. Initially, two methods, spherical agglomeration, and emulsion solvent diffusion, were suggested to get a desired result. Later on, the introduction of modified methods such as crystallo-co-agglomeration, ammonia diffusion system, and neutralization techniques overcame the limitations of the older techniques. Under controlled conditions such as solvent composition, mixing rate and temperature, spherical dense agglomerates cluster from particles. Application of the SC technique includes production of compacted spherical particles of drug having improved uniformity in shape and size of particles, good bulk density, better flow properties as well as better solubility so SC when used on commercial scale will bring down the production costs of pharmaceutical tablet and will increase revenue for the pharmaceutical industries in the competitive market. This review summarizes the technologies available for SC and also suggests the parameters for evaluation of a viable product.
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ORIGINAL RESEARCH ARTICLES
A comprehensive physicochemical, thermal, and spectroscopic characterization of zinc (II) chloride using X-ray diffraction, particle size distribution, differential scanning calorimetry, thermogravimetric analysis/differential thermogravimetric analysis, ultraviolet-visible, and Fourier transform-infrared spectroscopy
Mahendra Kumar Trivedi, Kalyan Kumar Sethi, Parthasarathi Panda, Snehasis Jana
January-March 2017, 7(1):33-40
DOI
:10.4103/jphi.JPHI_2_17
PMID
:28405577
Objective:
Zinc chloride is an important inorganic compound used as a source of zinc and has other numerous industrial applications. Unfortunately, it lacks reliable and accurate physicochemical, thermal, and spectral characterization information altogether. Hence, the authors tried to explore in-depth characterization of zinc chloride using the modern analytical technique.
Materials and Methods:
The analysis of zinc chloride was performed using powder X-ray diffraction (PXRD), particle size distribution, differential scanning calorimetry (DSC), thermogravimetric analysis/differential thermogravimetric analysis (TGA/DTG), ultraviolet-visible spectroscopy (UV-vis), and Fourier transform-infrared (FT-IR) analytical techniques.
Results:
The PXRD patterns showed well-defined, narrow, sharp, and the significant peaks. The crystallite size was found in the range of 14.70–55.40 nm and showed average crystallite size of 41.34 nm. The average particle size was found to be of 1.123 (
d
10
), 3.025 (
d
50
), and 6.712 (
d
90
) μm and average surface area of 2.71 m
2
/g. The span and relative span values were 5.849 μm and 1.93, respectively. The DSC thermogram showed a small endothermic inflation at 308.10°C with the latent heat (ΔH) of fusion 28.52 J/g. An exothermic reaction was observed at 449.32°C with the ΔH of decomposition 66.10 J/g. The TGA revealed two steps of the thermal degradation and lost 8.207 and 89.72% of weight in the first and second step of degradation, respectively. Similarly, the DTG analysis disclosed T
max
at 508.21°C. The UV-vis spectrum showed absorbance maxima at 197.60 nm (λ
max
), and FT-IR spectrum showed a peak at 511/cm might be due to the Zn–Cl stretching.
Conclusions:
These in-depth, comprehensive data would be very much useful in all stages of nutraceuticals/pharmaceuticals formulation research and development and other industrial applications.
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EDITORIAL
Emerging role of nanoemulsions in oral health management
Jasjeet Kaur Narang, Ramandeep Singh Narang
January-March 2017, 7(1):1-3
DOI
:10.4103/jphi.JPHI_32_16
PMID
:28405572
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1
ORIGINAL RESEARCH ARTICLES
Evaluation of anti-diabetic activity of AHPL/AYTAB/0513 tablet in streptozotocin induced diabetes in rats
Sanjay U Nipanikar, Soham S Chitlange, Dheeraj Nagore
January-March 2017, 7(1):25-32
DOI
:10.4103/jphi.JPHI_34_16
PMID
:28405576
Background:
Diabetes is a chronic, progressive disease associated with several complications leading to significant mortality and morbidity. Limitations and drawbacks of the conventional treatment generate need for safer, effective complimentary therapies to prevent complications, and maintain normoglycemic status.
Aim and Objectives:
The aim of this study is to to evaluate antidiabetic activity of AHPL/AYTAB/0513 tablet alone, oral hypoglycemic agents (OHA[s]), and combination of AHPL/AYTAB/0513 tablet and OHA(s) in streptozotocin-induced diabetes in rats.
Materials and Methods:
Totally, ten groups of animals were studied comparatively to evaluate antidiabetic activity of AHPL/AYTAB/0513 tablet, OHA(s), and combination of AHPL/AYTAB/0513 tablet and OHA(s). Blood glucose level (BGL), lipid profile, serum creatinine, serum insulin level, and histopathological characteristics of pancreas were studied to evaluate the efficacy of various formulations. Histopathological examination of kidney and heart was carried out to assess the ability of various formulations in preventing complications of diabetes.
Results:
There was a significant decrease in mean BGL, serum triglycerides, serum total cholesterol, low-density lipoprotein (LDL), very LDL, and serum creatinine levels in all formulations groups. Significant increase in mean serum insulin level and high-density lipoprotein level was observed when compared to diabetic control (DC) group. Recovery of pancreatic beta cells and prevention of damage to heart and kidney cells was significant in all the formulation groups as compared to DC group. None of the formulations tested in nondiabetic rat showed hypoglycemia suggesting safety of all the formulations.
Conclusion:
AHPL/AYTAB/0513 tablet alone and in combination with OHA(s) can be effectively used in the management of diabetes mellitus. In addition, AHPL/AYTAB/0513 tablet alone and in combination with OHA(s) help in prevention of diabetic complications. As an adjuvant to OHA(s), AHPL/AYTAB/0513 tablet can be more effective.
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Factorial analysis of the binding properties of acetylated ginger starch in metronidazole tablet formulations
Oluyemisi Adebowale Bamiro, Abioye Josephina Duro-Emanuel
January-March 2017, 7(1):18-24
DOI
:10.4103/jphi.JPHI_31_16
PMID
:28405575
Introduction:
The delivery of drug is often affected by formulation processes and the excipients used in the formulation.
Materials and Methods:
A 2
3
factorial analysis was used in this study to evaluate the effect of acetylated ginger starch (AGS) (
Zingiber officinale
) as a binder in metronidazole tablets, in comparison to corn starch (CS) BP. The individual and interacting effects of variables (binder type X
1
, binder concentration X
2
, and compression pressure X
3
) used on tablet properties such as friability, crushing strength, crushing strength friability ratio (CSFR), disintegration and crushing strength friability/disintegration time ratio (CSFR/DT) were determined. The effect of these binders on the granule properties using Hausner's ratio, Carr's index (CI), angle of repose, and densities as response parameters was also determined.
Results:
Granules prepared with AGS had high densities and small granule sizes when compared with those containing CS. Granules containing CS have better flow properties. X
1
(binder type) has a significant effect on the crushing strength of the tablet. It also had the highest effects on CSFR and CSFR/DT. The combination of X
I
X
3
had the highest effect on crushing strength and DT.
Conclusion:
This study shows that, in formulations, care must be taken in choosing the excipients and the process parameters required for the formulation since these can affect the delivery of the drug individually or in combination. AGS could be useful as a binder when a tablet with low crushing strength and fast disintegration is desired.
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