摘要
目的:研究复方对乙酰氨基酚Ⅱ胶囊的溶出度,并考察其与上市片剂的人体生物等效性。方法:溶出度测定方法采用2010年版《中国药典》(二部)附录ⅩC第一法,以盐酸溶液为溶出介质,转速100r/min,检测波长273nm;生物等效性采用随机双交叉试验,18名健康受试者分别单剂量口服复方对乙酰氨基酚Ⅱ胶囊(受试制剂)与片剂(参比制剂)后,用高效液相色谱串联质谱电喷雾(HPLC-MS/MS)法测定血药浓度,计算药动学参数,评价生物等效性。结果:受试制剂与参比制剂中对乙酰氨基酚和咖啡因在15min时的累积溶出量>85%,异丙安替比林相似因子(f2)=85;受试制剂相对于参比制剂的生物利用度分别为对乙酰氨基酚(103.2±11.3)%、异丙安替比林(108.0±29.5)%、咖啡因(110.1±48.3)%。结论:两种制剂的体外溶出行为相似,体内生物等效。
OBJECTIVE: To study the dissolution of Compound paracetamol Ⅱ capsules and bioequivalence of it and tablet on the market. METHODS: First method of appendix in 2010 edition of Chinese Pharmacopoeia (part ⅡX C) was adopted in the de- termination of dissolution, which was as follows: hydrochloric acid slontion as medium; rotation speed of 100 r/min; detection wavelength of 273 nm. By randomized crossover study of bioequivalence, 18 healthy volunteers were given Compound paracetamol lI capsules (test preparation) and Compound paracetamol Ⅱ tabelts (reference peparation). The blood concentration of paracetamol was determined by HPLC-MS/MS. RESULTS: The accumulative dissolution of paracetamol and caffeine in two prepa- rations exceeded 85 % in 15 mins; similarity factor (f2) of propyphenazone was 85; the relative bioavailability of test preparation to reference preparation were (103.2 ±11.3)% for paracetamol, (108.0± 29.5)% for propyphenazone and (110.1 ±48.3)% for caf- feine. CONCLUSIONS : In vitro dissolution behavior of two preparations is similar, and two preparations are bioequivalent in vivo.
出处
《中国药房》
CAS
CSCD
2013年第14期1274-1276,共3页
China Pharmacy
基金
国家重大新药创制专项"大品种技术改造"资助项目(No.2011ZX09201-101-26)