Formulation and evaluation of a gastroretentive dosage form of labetalol hydrochloride

• Published in: Archives of pharmacal research 2010, 33(3), , pp.405-410
• Main Authors: Garse, Harshal, Vij, Mohit, Yamgar, Manohar, Kadam, Vilasrao, Hirlekar, Rajashree
• Format: Article
• Language: English
• Subjects: Adrenergic Antagonists - chemistry; Antihypertensive Agents - chemistry; Chemistry, Pharmaceutical; Delayed-Action Preparations; Drug Compounding; Hydrogen-Ion Concentration; Hypromellose Derivatives; Kinetics; Labetalol - chemistry; Medicine; Methylcellulose - analogs & derivatives; Methylcellulose - chemistry; Osmolar Concentration; Pharmacology/Toxicology; Pharmacy; Poloxamer - chemistry; Solubility; Tablets; Technology, Pharmaceutical - methods; Water - chemistry; Wetting Agents - chemistry; 약학
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-010-0309-z

Labetalol hydrochloride (LBT), 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl) amino] ethyl]-benzamide, a non-selective α, β-adrenoceptor antagonist is used in the treatment of hypertension. It shows variable bioavailability ranging from 10–80% which may be attributed to its minimum solubility in pH range 6 to 10, the pH conditions prevailing at the major site of absorption i.e. small intestine. Also due to its half life of 3 to 6 hrs it is administered twice daily. In the present work non-effervescent sustained release gastroretentive floating tablets of labetalol hydrochloride have been developed using various grades of HPMC and Poloxamer M127 as wetting agent. The tablets were evaluated for in vitro drug release, floating time, floating lag time, swelling studies etc. The tablets formulated with HPMC K4M CR and HPMC K15M CR along with Poloxamer showed negligible floating lag time with a total floating time over 12 hrs with complete release. Formulation was optimized using Stat-Ease Design Expert 7.1 software. Optimized batch was evaluated for the effect of change of osmolarity and pH on drug release, floating and swelling behaviour.