Abstract
Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose (NaCMC) or carbopol 934P was added to alter the drug release profile or the dimensional stability of the formulation. Dicalcium phosphate (DCP) was used as filler. Formulations were evaluated for floating lag time, duration of floating, dimensional stability, drug content and in vitro drug release profile. The formulations were found to have floating lag time less than 1min. It was found that the dimensional stability of the formulations increase with increasing concentration of the swelling agent. The release mechanism of propranolol hydrochloride from floating tablets was evaluated on the basis of Peppas and Higuchi model. The ‘n’ value of the formulations ranged from 0.5201 to 0.7367 (0.5<n<1.0) which indicated anomalous (non-Fickian) transport mechanism. Formulation containing 27.5% HPMC K15M, 29% DCP, 3.75% citric acid and 18.75% sodium bicarbonate seemed most desirable. FTIR, DSC and XRPD studies indicated the absence of any significant chemical interaction within dug and excipients. Stability study of optimized formulation revealed no significant change and found to be stable.
Highlights
IntroductionShort and variable gastric emptying time can result in incomplete drug release from the delivery system above the absorption zone (stomach or upper part of small intestine), leading to diminished efficacy of the administered dose [1]
Gastric emptying of dosage forms is an extremely variable process
Our preliminary study indicated that ≥ 27.5% concentration of HPMC K15M was needed as the swelling agent in order to maintain sufficient matrix integrity of the tablets when citric acid and sodium bicarbonate were used in amount of 15 mg and 75 mg respectively, as the effervescent base and Dicalcium phosphate (DCP) as the diluents
Summary
Short and variable gastric emptying time can result in incomplete drug release from the delivery system above the absorption zone (stomach or upper part of small intestine), leading to diminished efficacy of the administered dose [1]. Improved bioavailability is expected for drugs that are readily absorbed upon release in the GI tract. These drugs can be delivered ideally by slow release from the stomach [2]. The lasting intragastric buoyancy of a controlled release dosage form might provide a suitable manner to constantly deliver a drug locally into the stomach and achieve a sustained site-specific therapeutic action
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