氨酚曲马多缓释片的研制及体外释放度考察

Preparation and in Vitro Drug Release of Paracetamol and Tramadol Hydrochloride Substained Release Tablets

目的制备氨酚曲马多缓释片,并进行体外释放度考察。方法以羟丙甲纤维素(HPMC K4M)为骨架材料制备对乙酰氨基酚(PT)颗粒,以HPMC K4M及乙基纤维素(EC)为骨架材料制备盐酸曲马多(TH)颗粒,并分别用单因素考察法确定两种颗粒的组成。两种颗粒以适当比例混合后(每片含PT 250 mg及TH 60 mg),压片制备氨酚曲马多缓释片。采用高效液相色谱(HPLC)法同时测定两种主药的含量,用转篮法对其体外释药特性进行考察,对其质量进行初步考察,并与市售氨酚曲马多片进行比较。结果氨酚曲马多缓释片各项检查指标均符合药典规定,建立的HPLC法可同时测定两种主药的含量,体外释药特性均符合一级释药方程,与市售普通片比较,该缓释片具有明显的缓释特性。结论氨酚曲马多酚缓释片制备工艺简单,质量理想,含量测定方法可靠,具有较好的缓释特性。

Objective To prepare paracetamol（ PT） and tramadol hydrochloride（ TH） sustained release tablets and study the in vitro drug release. Methods Hydroxypropyl methylcellulose（ HPMC K4M） was used as the matrix to prepare PT granules,and ethyl cellulose（ EC） combined with HPMC4 M was applied as the matrix to prepare tramadol hydrochloride granules,and single factor investigation was used to optimize the granules. The above two granules were mixed in the proper proportion（ respectively 250 mg and 60 mg per tablet）and compressed for the preparation of paracetamol and tramadol hydrochloride sustained release tablets. The quality of the tablets was investigated, and an HPLC method was used to determine the two drugs simultaneously. The in vitro release behavior of the sustained release tablets was studied using a basket method, and compared with that of the marketed common tablets. Results The quality of paracetamol and tramadol hydrochloride sustained release tablets met the requirements in Chinese pharmacopeia. The established HPLC method could be used for the simultaneous determination of the two drugs. The in vitro release behavior of the sustained release tablets fitted first- order equation, suggesting notable sustained release property when compared with that of the common tablets. Conclusion The preparation of paracetamol and tramadol sustained release tablets is simple with promising quality, reliable content determination method and notable sustained release property.