Current Issue : January-March Volume : 2015 Issue Number : 1 Articles : 15 Articles
Along with local action of drugs for different purposes such as for the various skin infections, emollients etc and also for cosmetic use topical drug delivery is becoming the area of interest now a days for the systemic delivery of drugs since it is proving to be the alternative for intravenous administration of drugs, due to the advantages like low dose requirement, easy termination of therapy, ease of application. The present review focuses on the details of the skin and its structure with a brief introduction to the barrier properties of the stratum corneum which is an important parameter when topical delivery is under consideration. Also the detail microstructure of the gel formed by different polymers, the method of gel preparation is also discussed....
Drug molecules with poor aqueous solubility are prevalent in research and development work of most of the pharmaceutical companies. Such drugs particularly delivered via oral route, leads to the poor bioavailability and efficacy of drug molecule. Pharmaceutical co-crystals are crystalline molecular complexes containing therapeutic molecules. Co-crystallization alters the molecular interactions and composition of pharmaceutical materials and is considered better alternatives to optimize drug properties. These can be constructed through several types of interaction, including hydrogen bonding, pi-stacking, and van der waals forces. Crystal engineering approaches, which can potentially be applied to a wide range of crystalline materials, offer an alternative and potentially fruitful method for improving the solubility, dissolution rate, hygroscopicity, bioavailability of poorly soluble drugs and the physical stability of moisture liable APIs. This technology is used to identify and develop new proprietary forms of widely prescribed drugs. Co-crystals not only provide a technique for improvement of physiochemical property but also provide opportunity to the researchers of Pharmaceutical companies regarding intellectual property....
Floating microspheres of tramadol hydrochloride was prepared by ionic gelation method with an aim of increasing the gastric residence time and for controlled release. Sodium alginate, polymeric mixture of sodium alginate and gum karaya were used as polymers. Sodium bicarbonate was used as the gas-forming gent. The prepared floating microspheres were evaluated with respect to particle size distribution, floating behaviour, drug content, entrapment efficiency, morphology and in-vitro release study. These results indicated that the release rate was found to decrease with increase in concentration of coating material applied. The wall thickness of microspheres was found to be increased with the increase in concentration of coating material applied. The floating microspheres followed zero order kinetics and the mechanism of drug release was governed by peppas model. For all the microspheres the exponential coefficient values were found to be in between 0.8147 and 0.9188, indicating non fickian diffusion controlled release mechanism....
Valsartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. The drug is having low solubility in biological fluids which results in poor bioavailability after oral administration. Hence present study was carried to enhance dissolution properties of valsartan. Solid dispersions of valsartan were prepared by using PEG-4000 and PEG-6000 as water soluble carriers at various proportions 1:1, 1:1.5, 1:2. The kneading and solvent evaporation methods were used to prepare solid dispersions. The prepared dispersions were made into tablets by direct compression method. The release profile was studied in 0.067M phosphate buffer pH 6.8. It was found that the dissolution rate of tablets containing solid dispersions were higher than those of intact drug. The degree of dissolution rate enhancement depended on the nature and amount of the carrier i.e.; the higher the amount of the carrier used, the higher dissolution rate was obtained. Among the prepared formulations F6 gave highest dissolution. The increase in the dissolution rate of the drug may be due to increase in wettability, hydrophilic nature of the carrier and also possibility due to reduction in drug crystallinity. Formulation F6 was subjected to stability studies. The formulation was found to be stable for 45 days at 40°C without significant change in drug release pattern....
The purpose of the study was to evaluate the suspending property of various suspending agent and to select a cheap, effective alternative natural suspending agent for pharmaceutical suspensions. Comparative study between suspending agents like kollidon CL-M like tragacanth, acacia, hydroxpropyl methylcellulose were done. Different paracetamol suspensions using kollidon CL-M, tragacanth, hydroxpropyl methylcellulose (HPMC) and acacia were prepared and effect of type and concentration of suspending agent on sedimentation volume and redispersibility. Various batches of paracetamol suspension prepared using kollidon CL-M, compound tragacanth, HPMC and acacia were evaluated for sedimentation volume and redispersibility. The sedimentation of the formulation increased with increase in tragacanth concentration and results obtained shows that the tragacanth has good and stable suspending properties. It was concluded that tragacanth can be employed as stabilizer and thickener of choice for paracetamol suspension....
The objective of present study was developing gastro retentive drug delivery system of ofloxacin. Retention of drug delivery system in the stomach prolongs overall GI transit time, there by resulting in improved absorption and bioavailability of ofloxacin. Present investigation highlights the formulation and characterization of floating microspheres of ofloxacin. Ofloxacin is the first generation fluroquinolone. The plasma half-life of drug is approximately 4-5 Hrs. The Floating microspheres of ofloxacin were prepared by solvent diffusion technique using polymer such as ethyl cellulose, HPMC K4M and PVA in a different ratio. The prepare microsphere were subjected to evaluation for physical characteristics like particle size percent drug entrapment, buoyancy test and In-vitro release study. The result of all physicochemical tests for all formulation was found to be satisfactory. The In-vitro drug releases were found to be in the range of 40% to 94% at the end of 6 hrs....
The term mucoadhesion is used specifically when the bond involves mucous coating and an adhesive polymeric device, while cytoadhesion is the cell-specific bioadhesion. The amoxicillin mucoadhesive microspheres, potassium clavulanate mucoadhesive microspheres were prepared by an emulsification/evaporation method. Microspheres were investigated using scanning electron microscopy. The polymer ratio, stirring speed and the temperature affected the particle size, shape and surface morphology of the microspheres. In-vitro release studies were carried out in pH 1.2 HCl buffer medium. Drug release rate was tested on all prepared formulations and marketed product Augmentin-375 (Amoxicillin trihydrate 250 mg + Potassium Clavulanate 125 mg) using basket apparatus on a dissolution apparatus. The test conditions were as follows: marketed tablet and microspheres containing 100 mg of drug were placed in baskets in a vessel containing 900 ml of pH 1.2 HCl buffer medium with the temperature maintained at 37±0.5°C. The rotating rate of the basket was adjusted to 100 rpm. At different intervals, 5 ml of samples were withdrawn and filtered through a whatman’s filter paper. The equivalent volume of the medium with the same temperature was added to the dissolution vessel. The absorbance values of the filtrate at the wavelength of 272 nm for amoxicillin and 205 for potassium clavulanate were determined after suitable dilution. The maximum yield was found to be 78.92% for Amox F-I and 80.89% for Clav F-I. FT-IR spectra of formulated microspheres revealed the drug was compatible with the polymers in the processing conditions....
The aim of present investigation was to develop compression coated tablet of rifampicin and isoniazide to minimize degradation of rifampicin in acidic medium and to modulate the release of rifampicin in the stomach and isoniazide in intestine. Tablets of rifampicin were prepared by wet granulation using PVP K-30, isopropyl alcohol, micro crystalline cellulose, cross carmeloss sodium, talc and magnesium stearate. The powder blend and tablets of rifampicin were characterized. Isoniazide tablets, prepared by wet granulation using dicalcium phosphate, were enteric coated using eudragit S100 and tablets of isoniazide were characterized. Compressed tablets of rifampicin and isoniazide were prepared and characterized for in-vitro drug release and modified dissolution method studies. Rifampicin and isoniazide was released at pH 1.2 up to 2hr from the dosage form. Less than 1% of isoniazide was released at pH 1.2 from dosage form before reaching to intestinal pH 7.4. Complete release of isoniazide was observed within 90 to 120 min at pH 7.4. Also, degradation of rifampicin was less in modified dissolution method compare to USP paddle apparatus....
The objective of the present investigation was to prepare orodispersible tablets of deferasirox by direct compression using sodium starch glycolate and crospovidone as superdisintegrants. Microcrystalline cellulose was used as diluent, mannitol and sodium saccharine to enhance mouth feel. The drug and excipients compatibility study was performed by FTIR and DSC to check purity and to show any possible interaction. The blend of all formulations were evaluated for various precompression parameters such as angle of repose, bulk density, tapped density, compressibility index, Hausner’s ratio. The prepared tablets were evaluated for weight variation, hardness, in-vitro disintegration time, in-vivo disintegration time, wetting time and in-vitro dissolution. Results showed that out of nine formulations studied, D2 showed short dispersion time with maximum drug release in 12 minutes. Combinations of superdisintegrants were found to be better in the formulation to achieve fast dissolution of tablets of deferasirox rather than using them alone in the formulation....
The purpose of present work was to formulate and evaluate metoprolol tartrate floating microspheres. Floating microspheres concept was applied to increase the gastric residence of the dosage form. The floating microspheres were prepared by emulsification solvent diffusion technique. The best batch exhibited excellent floating time as well as release at desired time. The particle size was controlled by changing polymer concentration, rpm and temperature. Polymers used for the preparation were ethyl cellulose and HPMC. This approach suggested the use of floating microsphere to avoid the side effects....
Aim of the present investigation was to formulate and evaluate nebivolol hydrochloride transdermal patch. Patches were prepared by 32 factorial design using solvent evaporation technique with different polymers. Propylene glycol was used as plasticizer. 32 factorial design was employed to explore the effects of eudragit RL100 and HPMC K15M (independent variables) on tensile strength, % cumulative drug release at 6 hours and %cumulative drug release at 24 hours (dependent variables). Patches were evaluated for physicochemical characteristics. Drug-polymer compatibility study was determined by fourier transform infrared spectroscopy and differential scanning calorimetry. The results of compatibility studies revealed that there was no interaction between drug and polymers. Results showed drug release in the range of 79.96±0.31-95.89±0.83 and drug content in the range of 92.65±0.21-98.62±0.17. Moisture content and moisture uptake were increased for the patches containing higher amount of HPMC K15M. Patch containing HPMC K15M in higher proportion gives increase in the drug release. It indicates that as the eudragit RL 100 increases the drug release was decreases. On the basis of in-vitro drug release performance, F7 was selected as the optimized formulation. Ex-vivo drug release study carried out for optimized batch and it showed 91.25±0.62% drug release after 24 hours. F7 showed ideal higuchi release kinetics. Skin irritation study for F7 revealed that it was free of irritation. Optimized batch F7 was found to be stable at 40±0.5°C and 75±5% RH during the test period of 1month. From the results, concluded that transdermal patches of nebivolol hydrochloride with desired characteristics could be prepared for prolonged release....
Most of the sulphonylurea derivatives have poorly water soluble drugs and gliclazide belongs to this class. The antidiabetics are most widely used drugs in the treatment of diabetes mellitus. The aim of current study was to formulate immediate release tablet to solve the problem of dissolution and person to person bio variability due to its poor solubility in water. Initially gliclazide was dissolved/suspended in PEG 400 to get a clear medicated liquid, then this solution poured on carrier material (Avicel PH 102) and subjected for mixing, subsequently coating material (Aerosil 200) was added in the previous mixture. Also 2% croscarmellose was added as a disintegrant. The resulting mixture was then subjected for precompression evaluation, tabletting and post compression evaluation. The precompression evaluation results of liquisolid system showed angle of repose ranging from 23.44-38.56° and dissolution time ranging from 9 minute to 24 minute having drug 98.105-101.58 %. Selected batch showed satisfactory angle of repose and dissolution time....
The purpose of the present investigation was to formulate and evaluate matrix tablets of valsartan sodium using different polymers and study the release of drug depending on the concentration of the polymer. The polymers used for the present investigation were xanthum gum, carbopol 934, HPMC K100M. The tablets were prepared by direct compression method. The drug polymer interaction was investigated by FTIR and their results directed further course of formulation. Valsartan tablets were evaluated for various post compression parameters like tablet hardness, friability, weight variation, drug content and in-vitro dissolution. The results were found to be within the acceptable limits. The time required for 90% (t90%) drug dissolution was selected as dependent variable. The formulations F1, F4, F7 showed that the drug release was concentration dependent and followed first order kinetics. While the formulations F2, F3, F6, F8 and F9 showed that drug release followed zero order kinetics. Formulation F9 was selected as an optimized one where the drug release sustained for a period of 12 hrs. Kinetic treatment to the in-vitro release data revealed that the drug release followed zero order non–fickian diffusion with n value greater than 0.45....
In the present investigation preparation of FDT of model drug (glipizide) by using direct compression. Glipizide was complexed with HPβ-CD by microwave method to improve the solubility and dissolution rate before formulating into a dosage form. Glipizide: HPβCD: poloxamer 188 (molar ratio of 1:1:1) complexed by microwave method which gives marked increased in solubility and selected for formulation of FDT. The prepared complex (GLZ) was characterized by DSC, FTIR and XRD studies. Fast dissolving tablet of solubility enhanced glipizide was prepared by direct compression technique because of its ease of access and contain limited number of unit operations. FDT was formulated with various concentrations of excipients like superdisintegrants, binders which were screened to find the best formulation with good friability, disintegration values and % cumulative drug release. Employing a 23 factorial design, the joint influence of two variables like amount of superdisintegrants (SSG) and binder (MCC) on the disintegration time and % CDR. The formulation batches were evaluated for pre-compressional and post-compressional parameters like weight variation, hardness, friability, thickness, disintegration time and dissolution at gastric pH. The values were of post-compressional parameter were in the prescribed limit and results were within IP acceptable limits. The study reveals that the formulation F3 is found to be optimized formulation with 95.10% drug release within 5 min. The kinetic study shows that the fast dissolving formulation follows the first order kinetic for the drug release mechanism....
Oral Submucus Fibrosis (O.S.M.F.) is associated with juxtaepithelial inflammatory reaction followed by fibroelastic changes of lamina propria which leads to stiffness of oral mucosa. Semecarpus anacardium oil possesses antioxidant, anticancer and anti-inflammatory activity which is relevant for treatment of O.S.M.F. The in-vitro antioxidant, anti-mitotic, anti-proliferative and in-vivo anti-inflammatory and analgesic activity was evaluated for the pharmacological evaluation of oil. Then Hydroalcoholic Gel was formulated using Semecarpus anacardium oil to study its effect on O.S.M.F. The gel was prescribed to patients suffering from O.S.M.F. and parameters such as ulcer size, no. of ulcers and color of mucosa and opening of mouth were studied. The present findings revealed that the hydroalcoholic gel showed promising effects on different parameters of O.S.M.F....
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