| Atenolol is a selective β1-epinephrine potential receptor antigonist which has been used in the treatment of a range of cardio vasculardisorders, hypertension, anginapectoris, myocardial infarction, arrhythmic and glaucoma. Tablet, gutta and injection of atenolol are used in clinic now. In this paper, monolithic osmotic pump tablet (MOPT) of atenolol was prepared by a simple method. The method for the preparation of monolithic osmotic pump tablet was obtained by coating the indented core tablet compressed by the punch with a needle. Sodium chloride as osmotic agent and polyethylene oxide as suspending agent, and the core tablet was prepared by wet method. Ethyl cellulose was employed as semipermeable membrane containing polyethylene glycol 400 as plasticizer for controlling membrane permeability. We prepared 9 kinds of Atenolol osmotic pump tablets, and measured their release characteristics in vitro. The formulation of atenolol osmotic pump tablet was optimized by orthogonal design and evaluated by similarity factor (f2). The optimal formulation was as follows: atenolol:25.0 mg, NaCl:100.0 mg, PEO(Mr5 × 105):58.3 mg, PEO(Mr2 × 105):66.7 mg. Thickness of coating membrane was 0.198 mm.The optimal formulation was evaluated in various environmental media and agitation rates. Indention size of core tablet hardly affected drug release in the range of (1.001.14) mm. The optimal osmotic tablet was found to be able to deliver atenolol at an approximately constant rate up to 24 h, independent on both environmental media and agitation rate.In-vivo pharmacokinetics of Atenolol OPT was studied on in dogs with Atenolol normal tablet used as reference preparation. The pharmacokinetic parameters of the Atenolol MOPT and the Atenolol normal tablets were as follows: Tmax were (8.4±3.29)... |
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