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THE PHARMA REVIEW (MAY - JUNE 2011)

Formulation and Evaluation of Inlay Tablets of Propranolol Hydrochloride with Hydrochlorthiazide

Chitra.P*,Elango.K,. Ramesh kumar. K,. Senthil Kumari .K

Abstract: The purpose of present investigation was to develop and optimize once daily sustained release inlay tablets of Propranolol hydrochloride (PRO) and Hydrochlorthiazide (HCTZ). An objective of the present invention is to provide a dosage form comprising PRO as sustained release (SR) layer and HCTZ as immediate release (IR) layer, wherein the SR active ingredient is selected from high dose active ingredient and IR active ingredient is selected from low dose active ingredient. PRO is known to have low bioavailability due to first pass effect. Its short half life of 3-6 hrs makes it an appropriate candidate for being a sustained release formulation. The (IR) tablets were formulated by Direct Compression Method using the superdisintegrant Cross povidone and the (SR) tablets were formulated by Wet Granulation Method using Hydroxy Propyl Methyl Cellulose ( HPMC K 100M & HPMC K 4M ) in various concentrations. Inlay tablets compressing was done with core rod tooling in which only one surface of core is exposed to outside and other drug is incorporated in cup portion. The inlay tablets were evaluated for hardness, thickness, uniformity of weight, friability, content uniformity, in- vitro drug release, disintegration and swelling. The formulation P5 could extend the release of PRO for 24 hrs and HCTZ for 15 mins. Stability studies were performed at 400C and 75% Relative humidity for 90 days and the formulation was evaluated every 30 days.
Introduction
The main objective of any therapy is to achieve desired therapeutic concentration of the drug in blood and tissues. Anti hypertensive medications can be used alone or in combination. The goal of therapy for hypertension is to bring the blood pressure down to normal levels for people having certain chronic kidney disease.(1) The rationale for combination therapy in treating hypertension is based on improved blood pressure values and improve tolerability. Combination therapy with antihypertensives that have multiple and complementary mechanisms of action may provide additive or synergistic antihypertensive effects while allowing for the use of lower dosages and reducing adverse events(2). The combination of β blockers with thiazide diuretics produce the additive effects. Inlay tablet dosage form comprises two parts like immediate release and sustained release(3). Sustained release dosage forms are designed to reduce the frequency of dosing and improve the patient compliance. Present study is undertaken to combine the additive effect of β blocker (PRO) with (HCTZ) as inlay tablets for sustained release dosage form, which will prolong the drug release , better control of hypertension by maintaining the plasma/ blood level of the drug consistently.
Propranolol is a non-selective beta-adrenergic receptor blocking agent. It has no other autonomic nervous system activity. Propranolol is a competitive antagonist which specifically competes with beta-adrenergic receptor stimulating agents for available beta-receptor sites. The propranolol has decreased cardiac output, inhibition of renin release by the kidneys, and diminution of tonic sympathetic nerve outflow from vasomotor centers in the brain. It has been suggested, but not established, that propranolol may achieve a better antihypertensive effect in patients with normal or elevated plasma renin activity than those with low plasma rennin activity.

 

 

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