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以Telfast-D~12H为参比制剂,测定了自制的盐酸伪麻黄碱(2)/盐酸非索非那定(1)(下称伪麻非索)缓释胶囊在不同介质[pH 1.0盐酸、pH 4.0乙酸盐缓冲液、pH 6.8磷酸盐缓冲液(PBS)和水]中的释放行为。根据计算得到的相似因子(f_2)结果,两种制剂中的1和2在各介质中的释放行为都相似。其中,在pH 6.8 PBS和水中,两种制剂中的1在0.25 h的累积释放率均大于85%。自制品中2的体外释放数据用Higuchi方程拟合效果较好(r=0.990)。建立了HPLC-MS/MS法测定20名健康志愿者单剂量口服自制复方胶囊后血浆中1和2的浓度,并采用DAS 2.0软件计算了主要药动学参数。通过比较自制胶囊在不同介质中体外累积释放率和体内吸收分数的相关性,推测当体外释放介质为pH 4.0乙酸盐缓冲液时,体内外相关性较佳。
The self-made sustained release capsules of pseudoephedrine hydrochloride (2) / fexofenadine hydrochloride (1) (hereinafter referred to as pseudo-mafamycin) were tested in different media [hydrochloric acid, pH 1.0, pH 4.0 acetate buffer, pH 6.8 phosphate buffer (PBS), and water]. Based on the calculated similarity factor (f_2) results, 1 and 2 in both formulations showed similar release behavior in each medium. Among them, the cumulative release rates of 1 in both formulations at 0.25 h in pH 6.8 PBS and water were greater than 85%. The in vitro release data of the self-made product 2 was better fitted by the Higuchi equation (r = 0.990). The plasma concentrations of 1 and 2 in 20 healthy volunteers were determined by HPLC-MS / MS. The main pharmacokinetic parameters were calculated by DAS 2.0 software. By comparing the correlation between in vitro cumulative release rate and in vivo absorption fraction of self-made capsules in different media, it is presumed that the in vitro and in vivo correlation is better when in vitro release medium is pH 4.0 acetate buffer.