盐酸索他洛尔爆破型脉冲片的制备及释放度研究

Preparation and in vitro study of explosion pulsatile-release tablets of sotalol hydrochloride

目的:以盐酸索他洛尔为模型药物,研制爆破型脉冲片并考察其体外释药特性。方法:通过体外释放实验,考察片芯崩解剂种类、包衣组成与厚度、增塑剂种类与用量、致孔剂种类与用量等处方因素对脉冲片体外释放的影响;并通过吸水实验分析脉冲片的释药机制。结果:以乙基纤维素(EC)为包衣材料,邻苯二甲酸二乙酯(DEP)为增塑剂,聚乙二醇6000(PEG6000)为致孔剂,采用薄膜包衣法,制备含盐酸索他洛尔30 mg的脉冲片。该制剂在体外延迟释放时间为4 h^6 h,时滞后1.5 h累积释药达90%。结论:盐酸索他洛尔爆破型脉冲片在体外具有脉冲释放特性。

Objective： To prepare the explosion pulsatile-release tablets of sotalol hydrochloride （SH） and to investigate the release characteristics in vitro. Methods： The release characters of the SH pulsatile-release tablets were related to the varieties and amounts of pore-forming agent, the composition and the thickness of the coating films as well as the varieties and amounts of plasticizer. The relationship between the formulation composition and the releasing rate of this pulsatile-release tablets was investigated. The pulsatile-release mechanism of the tablets was proved by the water take-up experiments. Results： The pulsatile-release tablets containing SH 30mg was prepared by film-coated methods using ethylcellulose （EC） as coating materials, DEP as plasticizer and PEG6000 as pore-forming agent. The delayed-release time was 4 h - 6 h in vitro, the accumulated amouts of release was 90% when the pulse-release time was 1.5 h. Conclution： The pulsatile-release character of the SH pulsatile-release tablets is confirmed in vitro.