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Table of Contents
April-June 2008
Volume 2 | Issue 2
Page Nos. 79-132
Online since Saturday, August 16, 2008
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EDITORIAL
New look, new TRP!
p. 79
VB Gupta
DOI
:10.4103/0973-8398.42491
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REVIEW ARTICLE
Significance of nanotechnology in medical sciences
p. 80
Ajay Gaur, Anil Midha, Arvind L Bhatia
DOI
:10.4103/0973-8398.42492
Nanotechnology refers broadly to a field of applied science and technology whose unifying theme is the control of matter on the molecular level in scales smaller than 1 µm, normally 1-100 nm, and the fabrication of devices within that size range. Two main approaches are used in nanotechnology. In the "bottom-up" approach, materials and devices are built from molecular components, which assemble themselves chemically by principles of molecular recognition. In the "top-down" approach, nano-objects are constructed from larger entities without atomic-level control. In addition, as the need for the development of new medicines is pressing, and given the inherent nanoscale functions of the biological components of living cells, nanotechnology has been applied to diverse medical fields such as oncology, cardiovascular medicine, and in treatment of other chronic diseases. Indeed, nanotechnology is being used to refine discovery of biomarkers, molecular diagnostics, and drug discovery and drug delivery, which could be applicable to management of these patients. In this review, we will focus upon significance of nanotechnology in medical sciences, as well as the plausible side effects related to their use.
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RESEARCH ARTICLES
Effect of casting solvent and polymer on permeability of propranolol hydrochloride through membrane-controlled transdermal drug delivery system
p. 86
Talasila Eswara Gopala Krishna Murthy, Vankayalapati Saikishore
DOI
:10.4103/0973-8398.42493
In the present work, cellulose acetate (CA), ethyl cellulose (EC), and Eudragit RS 100 (ERS100) films were prepared and evaluated as rate-controlling membranes for transdermal drug delivery systems. Acetone-methanol (8:2), chloroform-methanol (8:2), dichloromethane-methanol (8:2), and ethyl acetate-methanol (8:2) were used as solvents in the preparation of films. Dibutyl phthalate or propylene glycol at a concentration of 40% w/w of the polymer was used as a plasticizer in the preparation of CA and EC films. Dibutyl phthalate at a concentration of 15% w/w of the polymer was used as a plasticizer in the preparation of ERS100 films. The solvent evaporation technique was employed for the preparation of CA and EC films, and the casting solvent technique was employed for the preparation of ERS100 films. The dry films were evaluated for physical appearance, thickness uniformity, folding endurance, water vapor transmission (WVT), drug diffusion, and permeability coefficient. Both WVT and drug diffusion rate followed zero-order kinetics. The mechanism of drug release was governed by Peppas model. The diffusion exponent of release profiles (slope) has a value of 1.0360-1.3147 (
n
> 1), which indicates super case II transport diffusion. The results obtained in the present study thus indicated that the polymers and solvents used for the preparation of films have shown significant influence on the WVT, drug diffusion, and permeability of the films.
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Formulation and evaluation of medicated lipstick of allantoin
p. 91
Saba Shaikh, Kiran Bhise
DOI
:10.4103/0973-8398.42494
Cosmetics are incredible in demand since historical time till day. Lipstick formulations are most widely used to enhance the beauty of lips and to add glamor's touch to the makeup. It is difficult to apply lipsticks to the dried, chafed, chapped, cracked lips with sores and lesions. In such cases, one can use medicated lipsticks for the purpose of curing topical infections and beautification of lips. With this aim and objectives, an attempt was made to formulate medicated lipstick by using cow ghee and honey as natural excipients that substituted synthetic ingredients like isopropyl myristate, lanolin, cetyl alcohol, and castor oil. Allantoin was selected a model drug for the local action on lips.
In vitro
evaluation was done on bovine lip membrane, and the data suggested that the drug remained on the membrane only and did not diffuse through the membrane in diffusion studies for 8 h. After 8 h, 0.16% drug release was observed till 12 h. Thus, allantoin can remain topically on lips for 8 h without showing any systemic effects. The lipsticks were evaluated for their organoleptic properties such as spreading, covering property, hardness, shine, and gloss and found to be satisfactory product to give attractive beauty with therapeutic effect on the diseased lips. Thus, the medicated lipsticks with the natural ingredients like cow ghee and honey can serve as economical and effective cosmoseutical product.
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A new approach: Enhancement of solubility of rofecoxib
p. 96
MV Ramana, M Himaja, Kamal Dua, VK Sharma, Kavita Pabreja
DOI
:10.4103/0973-8398.42495
The present study is aimed at improving the dissolution of poorly soluble drug, rofecoxib. Rofecoxib, being a drug, basic in nature shows a better solubility in acidic environment. Hence, an attempt was made to provide an acidic microenvironment around the drug molecules by incorporating various freely soluble acidic substances. Addition of such additives provides a dual effect of not only providing an acidic microenvironment but also imparts solubilizing effects due to the free water-soluble nature of the additives used. In the present work, β -cyclodextrin (β -CD) complexes of rofecoxib were prepared and solubilizing additives such as citric acid and ascorbic acid were incorporated in various proportions. Dissolution studies were performed in both HCl buffer (pH 1.2) and phosphate buffer (pH 7.4). The results have shown an enhanced dissolution rate of rofecoxib in both media from beta-cyclodextrin. complex, and a further enhancement of dissolution was found in presence of ascorbic acid as well as citric acid. Differential scanning calorimetery (DSC) and infrared spectroscopy (IR) spectral studies performed on the solid complexes have shown that there is no interaction of the drug with β -CD and the additives. Hence, β -CD enhances the solubility of rofecoxib, and by creating an acidic microenvironment around the drug molecules, solubility of rofecoxib can be enhanced further, which in turn will enhance the absorption of rofecoxib and produce a better pharmacological activity.
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Development and evaluation of xyloglucan matrix tablets containing naproxen
p. 102
RV Kulkarni, Anirudh Shah, Rashmi Boppana
DOI
:10.4103/0973-8398.42496
The xyloglucan (XGL) matrix tablets containing naproxen were prepared by conventional wet granulation technique and evaluated for its drug release characteristics. Hardness of the tablets was found to be in the range of 5.0-7.0 kg/cm
2
. The tablets showed 98.23-99.12% of the labeled amount of drug, indicating uniformity in drug content. The swelling index increased with the increase in concentration of XGL and with the addition of hydroxypropylmethyl cellulose (HPMC) in the matrices, whereas swelling index decreased with the addition of cellulose acetate phthalate (CAP) and ethyl cellulose (EC). The compaction pressure had no significant effect on the drug release. Increase in polymer content and increased initial drug loading resulted in decreased drug release from the tablets. Addition of HPMC, CAP, and EC to XGL tablets decreased the drug release, and release was extended over a period of 8 h. The mechanism of release from all the tablets deviated from Fickian mode.
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Novel HPLC analysis of cefadroxil in bulk formulation
p. 106
Ravi Shankar Shukla, S Pandey, Rajesh Bargale, Asha Pateland, M Tiwari
DOI
:10.4103/0973-8398.42497
A rapid, accurate, and sensitive method has been developed and validated for the quantitative determination of cefadroxil (first generation) in bulk form. An Inertsil ODS, 4.60 x 250 mm
2
, 5
µ
m analytical column was used with an eluting system consisting of a mixture of phosphate buffer (pH 6.5)-methanol 78-32% (v/v) at a flow-rate 1.5 ml/min. Detection was performed by UV-Vis detector at 210 nm, resulting in limit of detection of 0.06 ppm for cefadroxil per 20-
µ
l injection. A linear relationship was observed up to 0.2 ppm for cefadroxil. Analysis time was less than 10 min. The statistical evaluation of the method was examined by means of within-day repeatability (
n
= 6) and day-to-day precision (
n
= 7) and was found to be satisfactory with high accuracy and precision. The method may be applied for the determination of the cefadroxil in bulk formulation in future.
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Preparation and characterization of aceclofenac microspheres
p. 110
Parul Trivedi, AML Verma, N Garud
DOI
:10.4103/0973-8398.42498
The objective of the present study was to microencapsulate the anti-inflammatory drug (aceclofenac) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track. The drug was targeted to the colon and their aligned area for their local effect. Aceclofenac was microencapsulated with Eudragit (S 100, RL 100, and RS 100), using an O/W emulsion-solvent evaporation technique. Aceclofenac microspheres were subjected to micromeritic properties including angle of repose, bulk density, tapped density, Carr's index, Hausner's ratio, and particle size determination. Microspheres were subjected to drug loading,
in vitro
drug release as well as for scanning electron microscopy. The prepared microspheres were white, free-flowing, and almost spherical in shape. The drug-loaded microspheres show 60-82% drug entrapment, angle of repose was in the range of 16.13 ± 0.621-24 ± 0.590, bulk and tapped densities respectively were in the range of 0.311 ± 0.006-0.562 ± 0.012 and 0.373 ± 0.01-0.735 ± 0.02, Carr's index ranges from 14.04 ± 0.026 to 27.25 ± 1.405, Hausner's ratio was 1.14 ± 0.026-1.37 ± 0.03, and particle size was in the range of 79.7016-144.840 µm.
In vitro
drug release studies were carried out up to 24 h in three different pH media, i.e., 0.1 N HCl (pH 1.2), phosphate buffer (pH 6.8), and phosphate buffer (pH 7.4). The drug-polymer concentration of dispersed phase influences the particle size and drug release properties. All the formulations at higher pH were followed by the Matrix-Higuchi model.
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Formulation and evaluation of dispersible taste masked tablet of roxithromycin
p. 116
AS Mundada, DR Meshram, HB Banbale, MR Bhalekar, JG Avari
DOI
:10.4103/0973-8398.42499
Roxithromycin is a broad spectrum, semisynthetic macrolide antibiotic, having bitter taste. In the present study, an attempt has been made to mask the bitter taste of roxithromycin by complexation technique. Weak cation exchange resins Indion 214 and Amberlite IRP64, polymer carbopol 934P were used in formulation of complexes with the drug. The loading process was optimized for the pH of loading solution and resin or polymer:drug ratio. The complexes were evaluated for bulk density, angle of repose, taste masking, and
in vitro
drug release.
In vitro
drug release studies showed more than 80% drug release from the optimized formulation within 30 min. Amberlite IRP64 was found to be better complexing agent for masking the bitter taste of roxithromycin.
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Development of colorimetric method for cephalexin in dosage forms
p. 120
P Priyanka, P Suresh
DOI
:10.4103/0973-8398.42500
A simple, sensitive, accurate, rapid, and economical colorimetric-spectrophotometric method has been developed for the estimation of cephalexin in capsules. This method is based on the reaction of the drug with ferric chloride and potassium ferricyanide, giving a green-colored chromogen exhibiting maximum absorbance at 791 nm against reagent blank. Beer's law was obeyed in the concentration range of 1-6
µ
g/ml. Results of the analysis were validated statistically and by recovery studies.
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Designing of superporous cross-linked hydrogels containing acrylic-based polymer network
p. 123
Debajyoti Ray, Prafulla Kumar Sahoo, Guru Prasad Mohanta
DOI
:10.4103/0973-8398.42501
Biodegradable cross-linked polymer, 2-hydroxyethyl methacrylate-co-acrylic acid was synthesized by free radical polymerization technique using N,N"-methylene-bis-acrylamide as cross-linker and benzoyl peroxide as reaction initiator. FT-IR,
1
H-NMR, scanning electron microscopy (SEM), and thermogravimetric analysis (TGA) studies of the copolymer along with homopolymers were carried out. FT-IR studies showed no interactions on copolymerization. SEM studies of the copolymer were carried out and mean particle size was found to be 50 µm. TGA analysis indicated an increase in thermal stability by cross-linking the polymer network. Swelling behavior of the copolymer showed more swelling by increasing pH of the medum and the prepared polymer was found to be biodegradable. The prepared cross-linked polymer system holds good for further drug delivery studies in connection to its super swelling and biodegradability.
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Solubility enhancement and development of dispersible tablet of meloxicam
p. 128
Nazma Inamdar, Kiran Bhise, Shakeel Memon
DOI
:10.4103/0973-8398.42502
The present research work investigates enhancement of dissolution profile of meloxicam using solid dispersion (SD) with various polymers. The work also describes the formulation of dispersible tablet (DT) and effervescent tablet of meloxicam. PEG 6000, PEG 8000, PEG 20000, Lutrol F-127, and β -cyclodextrin were selected for the preparation of SD. The SDs were prepared by melting and solvent evaporation methods. Dissolution studies were performed for plain meloxicam, SDs, and tablet formulations. Infrared spectroscopy and differential scanning calorimetry were performed to identify the physicochemical interaction between drug and carriers. Dispersible tablets and effervescent tablets were compared with tablet containing plane drug for dissolution profile. Dissolution of DT improved significantly in SD product (<95% in 1 min).
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