Formulation and Evaluation of Gastroretentive Drug Delivery System of Propranolol Hydrochloride |
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Authors: | Swati C Jagdale Amit J Agavekar Sudhir V Pandya Bhanudas S Kuchekar Aniruddha R Chabukswar |
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Institution: | (1) Department of Pharmaceutics, MAEER’s Maharashtra Institute of Pharmacy, Pune, 411 038, Maharashtra, India;(2) MAEER’s Maharashtra Institute of Pharmacy, Pune, 411 038, Maharashtra, India;(3) Quality Assurance, Nulife Pharmaceuticals, Pimpri, 411 018 Pune, Maharashtra, India;(4) Department of Pharmaceutical Chemistry, MAEER’s Maharashtra Institute of Pharmacy, Pune, 411 038, Maharashtra, India |
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Abstract: | The objective of present study was to develop a gastroretentive drug delivery system of propranolol hydrochloride. The biggest
problem in oral drug delivery is low and erratic drug bioavailability. The ability of various polymers to retain the drug
when used in different concentrations was investigated. Hydroxypropyl methylcellulose (HPMC) K4 M, HPMC E 15 LV, hydroxypropyl
cellulose (HPC; Klucel HF), xanthan gum, and sodium alginate (Keltose) were evaluated for their gel-forming abilities. One
of the disadvantages in using propranolol is extensive first pass metabolism of drug and only 25% reaches systemic circulation.
The bioavailability of propranolol increases in presence of food. Also, the absorption of various drugs such as propranolol
through P-glycoprotein (P-gp) efflux transporter is low and erratic. The density of P-gp increases toward the distal part
of the gastrointestinal tract (GIT). Therefore, it was decided to formulate floating tablet of propranolol so that it remains
in the upper part of GIT for longer time. They were evaluated for physical properties, in vitro release as well as in vivo behavior. In preliminary trials, tablets formulated with HPC, sodium alginate, and HPMC E 15 LV failed to produce matrix
of required strength, whereas formulation containing xanthan gum showed good drug retaining abilities but floating abilities
were found to be poor. Finally, floating tablets were formulated with HPMC K4 M and HPC. |
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