HPMC

An attempt was made to formulate and evaluate the Nebivolol HCl transdermal drug delivery system. The matrix type films were prepared by using solvent casting technique with polymers HPMC 15cps,PVP K-30,Eudragit RL100 and Methyl cellulose 15cps.Propylene glycol was used as plasticizer. The prepared films were evaluated for physicochemical characteristics such as thickness, weight variation, folding endurance, % moisture uptake and % moisture loss. The drug excipient compatibility was determined by Fourier Transform Infra red Spectroscopy. The results revealed that there were no interaction between drug and selected polymers. In vitro permeation studies were performed in Franz diffusion cell using commercial semi permeable membrane. Ex vivo studies were performed using skin of albino rats. Biological studies such as skin irritation test and % drug diffusion studies were carried out by using rabbits. Drug content varied from 73.72 ± 0.1to 95.4±0.15%. Moisture content and moisture uptake were increased for patches containing higher amount of HPMC due to its hydrophilic nature. The batch F4 (HPMC 1.5%, PVP 0.5%) had shown drug release for 24 h to the extent of 86.87% and drug release followed zero order release kinetics which was of non-Fickaian type of diffusion. The results of ex vivo and in vivo studies were well correlated with in vitro diffusion studies

The present study was carried out in fabricating gastro retentive formulation of an antipsychotic drug using semi synthetic and natural polymers. Floating tablets were prepared by direct compression method using directly compressible microcrystalline cellulose as vehicle. Gum Xanthan and hydroxypropyl methylcellulose (HPMC E4M) were used as polymers for sustaining the drug release and sodium bicarbonate was used as an effervescent agent. Tablets were characterized for their pre compression and post compression parameters. Floating characteristics like floating lag time, floating time were evaluated and were considered as one of the factor for selecting the best formulation. The in vitro release studies were carried out in pH 1.2 buffer for 8hrs. The content uniformity was found to be within the compendial requirements and the release was extended for more than 8hrs. The best fit release kinetics was achieved with zero order followed by higuchi and non-fickian diffusion. The release of Quetiapine fumarate was significantly influenced by the concentration of polymer.

Chitosan, a linear binary heteropolysaccharide, composed of β-1, 4-linked glucosamine (GlcN) with various degrees of N-acetylation of GlcN residues. It is a non-toxic, biocompatible and biodegradable natural polymer of high molecular weight (~500,000 kDa). The degree of deacetylation (DD) and molecular weight (MW) are two fundamental parameters that can affect the properties and functionality of chitosan. HPMC is the dominant hydrophilic vehicle used for the preparation of oral controlled drug delivery systems. Hydrophilic polymers are widely used in controlled release systems due to their favorable functionality. Enhancing the mobility of the polymer chains and diffusing of the drug out from such polymer matrices could be done by inclusion of different types of excipients at different concentrations. The present manuscript describes the attempt undertaken to develop the matrix tablet of Aceclofenac along with different grades of chitosan and HPMC as a copolymer & to study effect of it on the swelling behavior and the drug release pattern.

The present investigation has been undertaken with aim to formulation and evaluation of etoricoxib gel with different gelling agent and different penetration enhancer. Etoricoxib is highly selective cyclooxygenase-2 (COX-2) inhibitor. In this present study gel with carbopol, HPMC and Na-CMC as gelling agent prepared with different penetration enhancer like propyl glycol, oleic acid. Menthol oil. Formulation were evaluated for pH, stability study, spreadibilty, extrudabilty, bioadhesive (ex-vivo), skin irritation, viscosity, appearance and In-vitro drug diffusion. The formulation of Etoricoxib topical gel was prepared using carbopol, HPMC and Na-cmc in three batches A, B and C. With the consideration of all formulation characteristic and parameter we selected batch-A formulation for further study of anti-inflammatory and anti-analgesic activity. It was concluded that the Etoricoxib gel formulation containing carbopol with increase concentration of propyl glycol 10% and 2% oleic acid (OA) was suitable for topical application and it shows comparable result with market product and shows much better result of formulation, anti-inflammatory and anti-analgesic activity.

In the present study, an attempt has been made to prepare floating microspheres of clarithromycin designed as gastroretentive dosage form for the treatment of Heliobacter pylori. The floating microspheres were  prepared using different polymers like HPMC- ethyl cellulose, HPMC, eudragit S-100, eudragit L-100, by solvent evaporation/diffusion methods which offer advantage of short processing time, lack of exposure of the ingredients to high temperature and gives high encapsulation efficiency. Formulations were characterized for their particle size, practical yield, entrapment efficiency, in vitro buoyancy, scanning electron microscopy (SEM) and in vitro drug release. Scanning electron microscopy shows that spherical microspheres with porous surface were formed. The optical microscopic studies revealed that the practical yield was more than 61.78% with a particle size range of 105.61-292.40 µm.  The percent entrapment efficiency is about 62.68% and more in larger particle as compared to smaller particle. The percent buoyancy was more than 74.10% up to 12 hours. The particle size, percent yield, percent drug entrapment and percent was increased significantly with increase in polymer concentration. The in vitro release was significantly decreased with in polymer concentration.  Hence it can be inferred that the floating microsphere of clarithromycin as a gastroretentive dosage form may prolong drug release thereby improving bioavailability and enhance opportunity of drug absorption in stomach to prevent degradation of drug under alkaline pH.

Mosapride citrate a potent anti-histaminic drug, drug which has short half life, makes the development of sustained release (SR) forms extremely advantageous. Therefore, the present investigation of this study was to develop Mosapride citrate SR matrix tablets that provide complete drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain therapeutic effect. Mosapride citrate  showed maximum absorption at wavelength 274 nm in Acetate buffer pH 4.0, Drug-polymer compatibility studies by FTIR gave confirmation about their purity and showed no interaction between drug and selected polymers. Various formulations were developed by using release rate controlling and gel forming polymers like HPMC (K4M, K100M) by direct compression method. From among all the developed formulations, F6 formulation sustained the drug release for longer period of time as compared to other formulations. So, F6 was selected as the best formulation. It was concluded that the release followed zero order kinetics, as the correlation coefficient (R2 value) was higher for zero order release, so the drug release mechanism is controlled release. The best formulation was found to be stable during stability studies for two months. Thus, best formulation satisfied physicochemical parameters and in vitro drug release profile requirements for a sustained drug delivery.

Granisetron hydrochloride is a novel serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. It is well absorbed from the gastrointestinal tract, but its oral bioavailability is low (60%) due to extensive first-pass metabolism which makes it an ideal candidate for rapid release drug delivery system. Hence, an attempt was made to prepare and evaluate fast dissolving oral films containing Granisetron hydrochloride as a model drug by solvent casting method using natural and synthetic polymers. Various formulations were developed with varying concentration of polymers like, CMC, HPMC and Pullulan. Citric acid was used as a disintegrating agent and Propylene glycol as a plasticizer. The prepared oral films were evaluated for their physicochemical and mechanical parameters such as Physical appearance, surface texture, Weight uniformity, surface pH, ,thickness uniformity, percentage moisture absorption, loss on drying, disintegration time, drug content uniformity, folding endurance, tensile strength, percentage elongation, in-vitro drug release, and stability studies. In-vitro release rate of Granisetron hydrochloride was studied in phosphate buffer pH 6.8. F7, F10 showed maximum release rate about 93.95% and 95.29% in 180 seconds respectively, whereas F3 showed 60.98%. The mechanism of drug release of fast dissolving oral film was found to be to be non-fickian diffusion following first order kinetics. The selected fast dissolving oral films were found to be superior to marketed conventional tablet. Short term stability studies of selected films indicated that there is no significant change with respect to physical appearance, disintegration time, drug content and in-vitro drug release.

The aim of this study was to investigate the performance and release behavior of drug from hydroxypropyl methylcellulose (HPMC) matrix tablets prepared using HPMC from three different manufacturers. Three various brands of HPMC used were Methocel, Novocoat, and Zhongbao. A protocol was followed to evaluate these three HPMC samples their physico-mechanical properties such as appearance, particle size distribution, bulk density, tapped density, angle of repose, compressibility index (CI), Hausner’s ratio, swelling and morphology. Formulations were prepared using Carbamazepine (CAR) as a drug molecule, by varying drug loading and polymer concentration to evaluate the physical and comparative performance characteristics. Various drug release kinetic models were evaluated for the best fit of the formulations in order to understand the underlying release mechanisms from the formulations. The best performance with respect to release kinetics was exhibited by Methocel,while Novocoat and Zhongbao were found to have similar performance.

The objective of this research work was to prepare sustained release matrix tablets of doxofylline. Doxofylline is a  xanthine bronchodilator having reduced affinity for A1 & A2 adenosine receptors. Different grades of hydrophilic polymers( HPMC K4M, HPMC K15 cps, HPMC K100 M, Sodium carboxymethylcellulose) and hydrophobic polymer (ethyl cellulose) were used. FTIR study shows that drug and other excipients are compatible with each other. Tablets were prepared by wet granulation technique using non-aqueous solvent IPA and PVP K90D as a binder. Under stage I of preliminary study, tablets were formulated using polymers alone. In stage II polymers were used in combination, with an objective of sustaining release up to 12 hrs. The effect polymer concentration on drug release profile was  investigated. The amounts of HPMC K100 M & NaCMC were selected as independent variables. The results of  final batches indicated that a low concentration of HPMC K100 M & high amount of Sodium CMC favours sustained release of doxofylline from matrix tablets. Accelerated stability study for 8 weeks  confirmed that the best selected formulation F 15 was stable

Different formulation technologies intended for gastro retentive dosage form were investigated and patented over the years. The aim of this study was to formulate, optimize and evaluate the gastro retentive floating tablet of stavudine. The developed technology induces a low density dosage form containing high concentration of active pharmaceutical ingredient (API). In the present work, the in-vitro sustained release of stavudine from matrix of tablet containing HPMC K100M and Xanthan gum as release retardant polymers has been studied. Sodium bi-carbonate and citric acid are used as gas generating agents. The tablets were prepared by direct compression method. The tablets eroded upon contact with the release medium 0.1N HCl and  the relative importance of floating lag time,% swelling index and % drug release patterns varied significantly with the concentration of polymers. Optimization was done by using design expert 8.0.4.1 and optimized formulation F6 of stavudine floating tablet shows no significant change in hardness, drug content, floating lag time and % cumulative drug release pattern after the stability period of 3 months at 400c/75% relative humidity. Key-words- Stavudine, HPMC, Xanthan gum, floating tablet, in vitro buoyancy.