1Nagpur College of Pharmacy, Wanadongri Hingna Road, Nagpur, Maharashtra, India.
2Department of Pharmaceutical Analysis, School of Pharmacy, Faculty of Pharmacy, Parul University, Vadodara, Gujarat, India.
3Department of Pharmaceutical Chemistry, PCET'S Pimpari Chinchwad University, School of Pharmacy, Maval, Pune: 412106, Maharashtra, India.
4Karmayogi Tatyasaheb Bondre Institute of Pharmacy, Chikhali Dist Buldhana, Maharashtra, India.
5Department of Pharmaceutics, Tatyasaheb Kore College of Pharmacy, Warananagar, Dist-Kolhapur: 416113, Maharashtra, India.
6Samrat Prithviraj Chauhan College of Pharmacy, Kashipur, Uttarakhand, India.
7Guru Mishri College of Pharmacy, Shelgaon, Tal Badnapur, Dist Jalna: 431202, Maharashtra, India.
8Department of Pharmaceutical Chemistry, Chettinad School of Pharmaceutical Sciences, Chettinad Hospital and Research Institute, Chettinad Academy of Research and Education, Kelambakkam-603103, Tamil Nadu, India.
Corresponding Author: Mohammad Badrud Duza, Department of Pharmaceutical Chemistry, Chettinad School of Pharmaceutical Sciences, Chettinad Hospital and Research Institute, Chettinad Academy of Research and Education, Kelambakkam-603103, Tamil Nadu, India. E-mail: Badrud@gmail.com
Objective: Bosentan, a biopharmaceutical classification system (BCS) Class II drug (low solubility, high permeability), suffers from poor oral bioavailability due to its limited solubility and extensive first-pass metabolism. The objective of this study was to formulate, develop, and evaluate mouth-dissolving tablets (MDTs) of Bosentan to enhance its dissolution rate, patient compliance, and potentially improve bioavailability by pre-gastric absorption.
Methods: MDTs were prepared by direct compression method using various superdisintegrants such as croscarmellose sodium (CCS), sodium starch glycolate (SSG), and crospovidone (CP) in different concentrations (2%, 4%, 6% w/w). Microcrystalline cellulose and mannitol were used as diluents. The formulated tablets were evaluated for pre-compression parameters (angle of repose, bulk density, tapped density, Carr's index, Hausner's ratio) and post-compression parameters (weight variation, hardness, friability, drug content, wetting time, water absorption ratio, in-vitro disintegration time, and in-vitro dissolution studies).
Results: All formulations showed good pre-compression properties. The post-compression evaluation revealed that all tablets complied with pharmacopoeial standards. Formulation F5, containing 6% w/w crospovidone, exhibited the shortest disintegration time (14.2 ± 1.3 seconds) and the highest drug release (99.45% within 15 minutes), which was significantly higher than the conventional tablet. The results of the optimized formulation (F5) were found to be satisfactory.
Conclusion: The study successfully demonstrated that mouth-dissolving tablets of Bosentan with enhanced dissolution characteristics can be formulated using superdisintegrants by direct compression. Croscarmellose sodium and crospovidone were particularly effective, with crospovidone at a higher concentration yielding the best results, offering a promising approach to improve the therapeutic efficacy of Bosentan.
Keywords: Bosentan, Mouth Dissolving Tablets, Superdisintegrants, Direct Compression, Dissolution Enhancement, Pulmonary Arterial Hypertension, Patient Compliance.
How to cite this article: Mane NS, Sehjad S, Vhankade D, Radke RS, Chopade S, Kumar K, Naik R, Duza MB. Formulation, Development, and Characterization of Mouth Dissolving Tablets Using Bosentan as Model Drug. Int J Drug Deliv Technol. 2026;16(11s): 392-397. DOI: 10.25258/ijddt.16.11s.37
Source of support: Nil.
Conflict of interest: None