Studies on losartan novel extrudates design and evaluation to treat hypertension.

Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method using Hydroxy propyl methyl cellulose as matrix materials with or without xanthan gum and carbopol, and combination of xanthan gum and carbopol and propylene glycol as plasticizer. The prepared mini matrices were further evaluated for surface texture, uniformity of diameter, thickness, weight, moisture content, drug content uniformity, drug-excipients interaction, relative swelling, mucoadhesive test, in vitro drug release pattern. All the HPMC mini matrices showed good swelling which is proportional to concentration of polymer. The In vitro release of drug was in the range of 64.83% to 93.66%. Formulation H1 prepared with a drug-polymer ratio of 1:0.5 (LSP:HPMC) and 5% propylene glycol by weight of polymer as plasticizer showed promising results as a controlled release dosage form and released approximately 93.66% of the drug in 12 h. This study proves that extrusion method can be used for designing controlled release drug delivery systems providing nearly zero-order drug release over a period of 12 h.

Studies on directly compressed ondansetron hydrochloride mucoadhesive buccal tablets using gelatin, chitosan and xanthan gum along with HPMC K4M.

Mucoadhesive buccal tablets containing ondansetron hydrochloride (ODH) were prepared using polymers like gelatin, chitosan, xanthan gum in varying concentration of 5, 10, 15% w/w and HPMC K4M 40% w/w by direct compression technique. Precompressional studies revealed good micromeritic properties of powder blend for compression and were found as per literature limits. The prepared tablets were evaluated for thickness, hardness, uniformity of weight, drug content, friability, swelling index, mucoadhesion strength, in vitro disintegration, dissolution time and permeation studies. The formulations containing xanthan gum gave better mucoadhesion, release characteristics compared to those containing gelatin and chitosan and the rank order of mucoadhesion and permeation across sheep buccal mucosa was xanthan gum > chitosan> gelatin. The tablets apart from fulfilling all the official specifications, exhibited higher rate of release, in vitro release from all ODH buccal tablets followed Super case II transport due to polymer chain disentanglement and relaxation. and found to be stable upon conducting stability studies as per ICH guidelines at 40ºC/75 % RH. The results revealed that mucoadhesive buccal tablets containing ODH were successfully formulated by direct compression technique as an alternative to conventional tablets for therapy of nausea condition in patients.

Analytical Method Development and Validation of Anti-HIV Drug Abacavir Sulphate.

Analytical method development and validation was useful for estimation of drugs in bulk and biological fluids. They help to improve the reliability, consistency and accuracy of analytical data. Present investigation involves development and validation of UV spectroscopic method for abacavir sulphate as per ICH guidelines. The present work describes sensitive and robust method development of abacavir sulphate by UV spectroscopic method for estimation of abacavir sulphate in bulk and pharmaceutical dosage forms using UV-1700 pharma spec (Shimadzu). The method was validated for accuracy, precision, linearity, ruggedness and robustness to check its consistency. The wavelength scan of UV spectroscopic method showed absorption maxima 249 nm obeying beers law with linearity range of 0-40μg/ml and correlation coefficient of 0.99939. Molar absorptivity and sandell’s sensitivity are found to be 1.2404472 ×10-4 and 0.0208 respectively. The accuracy was found to be 99.94%-100.2% with recovery 99.76%, 100.06%, 100.07% for 50%, 100%, 150% solutions. The obtained results indicated that the developed analytical method was sensitive, accurate, with low standard deviation values for all validation parameters and could be used in day to day regular analysis of abacavir sulphate in bulk and pharmaceutical formulations.

Development and validation of selective UV spectrophotometric analytical method for budesonide pure sample.

Budesonide is a very potent corticosteroid, used for bronchial asthma and inflammatory bowel disease. Objective of the present investigation is to develop the simple and selective UV spectrophotometric method for quantification of budesonide in bulk sample. Absorption maximum of budesonide was found to be 246.0 nm and obeyed the beers law in the concentration range of 1.4 to 25 μ g/ml. Calibration curve shows a linear relationship between the absorbance and concentration in the range of 2 to 10 μ g/ml and the limit of detection is 0.01 μ g/ml. The limit of quantification was found to be 1.4 μg/ml. The method was validated for repeatability, accuracy and precision. The percent amount of recovery was 99 - 100% with minimum standard deviation less than 1%. Obtained results showed there is minimum intra day and inter day variation. The excipients present in the preparation did not interfered during the analysis. Developed analytical UV spectrophotometric method is simple, rapid and reproducible and further it can be used for estimation of drug in bulk and colon matrix tablet dosage form.

Formulation design, in vitro evaluation and stability studies on mucoadhesive buccal films of anti-anginal calcium channel blocker.

Diltiazem hydrochloride has poor oral bioavailability, easily undergo first passage effect in the liver. Hence, an attempt was made to prepare and evaluate mucoadhesive buccal films containing diltiazem hydrochloride by employing HPMC, eudragit, ethyl cellulose alone and in combination with PVP. The I.R and DSC studies showed that there was no interaction between drug and the utilized polymer. The prepared mucoadhesive buccal films showed uniform thickness, weight, folding endurance, surface pH, drug content and swelling index. The drug content of all the formulation was found to be uniform. In vitro drug release studies indicated that the films prepared with HPMC (3%) and ethyl cellulose (4%) has shown fast and slow release respectively. The formulations incorporated with SLS and sodium glycocholate indicated significant drug release from F11 and F15. Later the in-situ diffusion studies using goat cheek pouch showed faster drug release from film with 1% (SLS). About 93.04% and 91.83% of drug release profile were observed during in situ diffusion studies at the end of 9hrs and 18 hrs respectively. The formulated films were stable during stability studies at 45ºC and 75%RH with respect to drug content.

Formulation design of Aceclofenac microcapsules by inotropic gelation technique, characterization studies and release kinetics.

Osteoarthritis predominantly affects the large weight bearing joints and the clinical characteristics include morning stiffness of short duration, stiffness or gelling on rest, pain on use, joint inflammation and bone deformity. Microcapsules of aceclofenac were formulated with methyl cellulose, sodium CMC and hydroxyl propyl methyl cellulose by technique. The microcapsules showed excellent rheological properties for all batches. The formulations showed drug content uniformity with high drug entrapment efficiency. The in vitro wash off test revealed the mucoadhesive ability of the micro capsules. Scanning electron microscopy indicated structural and surface morphology uniformity. The in vitro release studies indicated sustained release of aceclofenac from the formulations. Kinetic study of the release data indicated the zero order release and non fickian sustained release mode of drug release. The microcapsules showed the correlation between wall thickness and drug release pattern.

Enteric coated tablets of novel proton pump inhibitor with super disintegrants design, in-vitro evaluation and stability studies.

The current work evaluate directly compressible esomeprazole magnesium trihydrate enteric coated tablets were prepared to deliver drug in upper GIT. Different tablets were prepared with super disintegrants like Ac-Di-Sol, Crospovidone, sodium starch glycolate and diluents like Pharmatose DCL11, Mannogem EZ. Tablets were enteric coated using Acryl-EZE. The tablets were evaluated for hardness, disintegration time and in vitro drug release. The powder bed showed good rheological properties and enteric coated tablets showed acid uptake value <5 indicates significant protection of acid liable drug. The compressional parameters were within the limits, the drug content in all formulations was found to be uniform and consistent. In vitro dissolution studies indicated there is no drug loss during gastric phase. The tablets with Pharmatose DCL11 released higher than Mannogem EZ which colud be due to its hydrophilicity and due to swelling of the super disintegrant. Stability studies indicated that the prepared formulations were stable for a period of four months of all formulations showed comparable dissolution profiles with similarity factor more than fifty at p<0.05. From the above findings it can conclude that an Esomeprazole magnesium trihydrate enteric coated tablet could be developed to deliver the drug in to proximal small intestine.