Asian Journal of Pharmaceutical Analysis

Nuha Rasheed ¹, Abdul Saleem Mohammad ², Seema Farheen ³, Shaik Zubair ³

Affiliations
1 Department of Pharmaceutics, Nizam Institute of Pharmacy, Deshmukhi (V), Pochampally (M), Behind Mount Opera, Nalgonda (Dist)-508284, Telangana, IN
2 Department of Pharmaceutical Analysis and Quality Assurance, Nizam Institute of Pharmacy, Deshmukhi (V), Pochampally (M), Behind Mount Opera, Nalgonda (Dist)-508284, Telangana, IN
3 Department of Pharmaceutics, Vijaya College of Pharmacy, Munaganur (V), Hayath Nagar (M), Hyderabad, Telangana, IN

Abstract

Bosentan is an endothelial receptor antagonist (ERA) indicated for the treatment of Pulmonary arterial hypertension (PAH). The aim of the present study involves the development of controlled release tablets of bosentan. The tablets were prepared to release the drug for a prolong period of time within the GIT, to enhance the bioavailability, to minimize the dosing frequency, and to improve the patient compliance. The tablets were formulated by using various polymers like hydroxyl propyl methyl cellulose, acacia and xanthum. The formulated tablets were evaluated. The drug release from the optimized formulation (F7) was found to be the best after observing the results of dissolution rate and pre & post formulation studies.

Keywords

Controlled Release, Hydroxyl Propyl Methyl Cellulose (HPMC), Bioavailability, Endothelial Receptor Antagonist (ERA), Pulmonary Arterial Hypertension (PAH), Gastro-Intestinal Tract (GIT).

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Nuha Rasheed ¹, Abdul Saleem Mohammad ², Hajera Hafeez ³, Seema Farheen ¹

Affiliations
1 Department of Pharmaceutics, Nizam Institute of Pharmacy, Deshmukhi (V), Pochampally (M), Behind Mount Opera, Yadadri Bhuvanagiri (Dist)-508284, Telangana, IN
2 Department of Pharmaceutical Analysis and Quality Assurance, Nizam Institute of Pharmacy, Deshmukhi (V), Pochampally (M), Behind Mount Opera, Yadadri Bhuvanagiri (Dist)-508284, Telangana, IN
3 Department of Pharmaceutics, Global College of Pharmacy, Beside to Moinabad Police Station, Moinabad, Rangareddi (Dist)-501504, Telangana, IN

Abstract

The objective of the study was to prepare and evaluate ACS contain pellets by the process of extrusion followed by spheronization for controlled release. The method employed was economical and does not imply the use of toxic solvents. The aqueous SLS which forms micropores on the surface of the pellets. The results of micromeritic properties, Hausner ratio and friability of the pellets were well within the limits which indicate good flow potential for the prepared pellets. Drug contains pellets exhibited spherical nature as evidenced by SEM photomicrographs and sphericity studies. From the FTIR and DSC studies, it was observed that there was no chemical interaction between the drug and polymers used indicates that drug was in stable form. The drug content study revealed uniform distribution of the drug in the pellets. The drug release rate was found vary among the formulations depending on the compositions of polymers used. The obtained dissolution data indicated that the drug release through the microporous polymeric membrane follows Fickian diffusion. Optimized formulation F5 and marketed product Aceton SR100 mg tablet showed similarity in drug release profile. Formulation F5 is an ideal formulation for once daily administration. From the present study, it can be concluded that the prepared matrix pellets demonstrate the potential use of SA/GPS/MCC blend for the development of controlled drug delivery systems for many water insoluble drug.

Keywords

Aceclofenac, NSAID, Surfactants, Formulation, Lipophilic, Hydrophilic, Gastrointestinal Fluid (GIF).

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