HPMC E15

Depressive Disorder medications are pharmacological agents that are used to treat Major Depressive Disorder disease. The intention of the present study is to design and characterization of fast dissolving buccal films of Paroxetin.  Films were prepared by using different polymers like HPMC E15, PVA, PVP and Glycerol as plasticizer and saccharin as a sweetening agent and vanillin as a flavoring agent. Buccal films were prepared using solvent casting technique. The major problem with Paroxetine was it belongs to class ? in BCS classification and have low solubility in biological fluids. In order to enhance the solubility of Paroxetine solid dispersion of Paroxetine   were prepared by melting technique at different drug carrier (PEG 4000) weight ratios and evaluated. No interaction was found between the drug and the polymers which was obtained by FTIR studies. The buccal films were evaluated for Folding endurance, weight variation, Drug content, Thickness, permeation study and in-vitro drug release study. Dissolution profile were studied by using USP dissolution apparatus type I, pH 6.8 simulated saliva were used as dissolution media. The influence of variable like polymer type, and their concentration, on Paroxetine release profile was studied. The formulation was optimized on the basis of various evaluation parameters like drug content and In-vitro drug release. Formulation F3 successfully gave the fast release of drug within 12 minutes. Stability studies were as per ICH guide lines and result indicated that the selected formulation was stable.

Oral fast disintegrating films (OFDF) is an emerging technology brings out “formulations taken without water” with quick onset of action and improved patient compliance. The present aim of study is to enhance the dissolution rate of the dosage form by using the different superdisintegrants and co-processed superdisintegrants. The films were prepared by solvent casting method using hydrophilic polymers that rapidly dissolves on the tongue or buccal cavity, delivering the drug to the systemic circulation. The polymer was used  HPMC E15, PEG 6000 as plasticizer, citric acid as the saliva stimulating agent, sucrose as the sweetening agents and sodium starch glycolate, crosscarmelose sodium and crospovidone as the superdisintegrants and tween 80 as surfactant . The FTIR reports suggest that drug and excipients were compatible. These oral disintegrating films were evaluated for various evaluation parameters. The in-vitro dissolution studies were conducted as per USP II with sinker. There were three ODFs prepared by using different types of the superdisintegrants, two were prepared by using the co-processed superdisintegrants and one was without any superdisintegrants. Among all formulation, the F6 shown the better in-vitro drug release profile which was prepared by using co-procesed superdisintegrants. It can be concluded that the co-processed superdisintegrants enhances the dissolution rate by comparing with other formulation.

Nebivolol Hydrochloride is a third generation beta blocker used for the treatment of hypertention and heart failure. Nebivolol is rapidly absorbed following oral administration, reaching peak plasma concentrations in 0.5 – 4.0 hrs. The present study was designed to develop a suitable matrix type transdermal drug delivery system (TDDS) for Nebivolol Hydrochloride employing various ratios of hydrophilic and hydrophobic polymers by solvent casting technique. The developed patches were then evaluated for physicochemical characterization, ex-vivo permeation and skin irritation studies. The compatibility of drug with other ingredients was checked by FTIR studies. FTIR results revealed that there was no interaction between dug and other excipients. The transdermal patches obtained were transparent, smooth, uniform and flexible. The results of physicochemical properties were within the pharmacopoeial limits. All the formulations were subjected to ex-vivo skin permeation study by means of Franz’s diffusion cell in order to optimize the suitable formulation. Two formulations with the polymeric blend 3:2 (HPMC E50: ERL 100 and HPMC E15: ERL100 respectively) showed an increase in permeation of drug via skin when compared with the formulations having less proportion of hydrophilic polymer (HPMC), however the formulation with HPMC E50 : ERL 100 showed overall improvement in flux and permeation, hence it was optimized as suitable matrix system. The drug release follows zero order kinetics with diffusion mechanism. The average steady state flux obtained with HPMC E50: ERL 100 (3:2) was 43.3 µg/cm2/hr and the same was increased to 59.2 µg/cm2/hr with the incorporation of 5% v/w of DMSO as permeation enhancer. In conclusion, the present data confirm the feasibility of developing Nebivolol Hydrochloride transdermal system. The release rate of drug through patches increased when the concentration of hydrophilic polymer was increased. 

The purpose of the present study was to design, characterize and evaluate extended release coated tablets of Metoprolol Succinate (MS) to reduce its dosing frequency. Core tablets were prepared using various matrix forming agents like HPMC, HPC, and HEC, and further subjected for coating using blend of aqueous dispersion of a hydrophobic and hydrophilic polymer, (Surelease®: HPMC E15) to control the drug release of the highly water soluble drug Metoprolol Succinate. Varying the matrix forming agent concentrations in the core tablets and percentage coating build up on core tablets showed range of drug release patterns in phosphate buffer pH 6.8. The present study dealt with the suitable grade of cellulose polymer and optimized coating composition which can modify the drug release to match up with the USP dissolution specifications and marketed product for the MS. The optimized formulation containing Metolose 90 SH 100000 and 3% coating with plasticized Surelease: hydroxypropyl methylcellulose (HPMC E15) showed extended drug release up to 24hrs and the drug release pattern was similar with the specifications. The in-vitro dissolution studies revealed that the release rate is inversely proportional to the concentration of matrix former in the core tablet and percent of coating thickness. The kinetic treatment illustrate that the optimized formulation HMC5 followed zero order kinetics with diffusion mediated drug release which is evidenced from n value of (0.73) Peppas equation. FT-IR and DSC studies indicated no interaction between the drug and excipients and prepared formulations showed good stability as per ICH guidelines. Key words: Metoprolol Succinate, Extended Release, HPMC E15, Surelease, Coated Tablet