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制备四种释放度相差悬殊的氢氯噻嗪片剂A、B、C、D,用转蓝法测定它们的释放度,并在7名志愿者中,按尿药法测定每种片剂的生物利用度。结果表明四种片剂的体外释放参数(T_d、T_(50)、m),除T_(dA)与T_(dB)、mο与m_D。外,余者间均有显著差异。四种片剂在生物利用度参数(Q、V_(max)、T_(max))方面无显著差异;在志愿者之间,除V_(max)外,其余之间无显著差异。经计算出四种片剂的相对生物利用度分别为100％、89.37％、90.01％、98.24％;在它们的体内、外参数之间无相关性,相关系数为0.3938～0.4489。以上说明四种片剂的体内吸收程度与体外释放速度不一致。根据本文的实验结果,测定氢氯噻嗪片剂的体外释放度不能用来反映此药在体内的生物利用度,这个意见供药典今后制订氢氯噻嗪片剂规格时参考。
Hydrochlorothiazide tablets A, B, C, and D were prepared at four different levels of release, and their release was determined by the turnip blue method. The bioavailability of each tablet was determined by urinalysis in seven volunteers . The results showed that the in vitro release parameters (T_d, T_ (50), m) of four kinds of tablets except T_ (dA) and T_ (dB), mο and m_D. Outside, the remaining were significant differences. The four tablets showed no significant difference in bioavailability parameters (Q, Vmax, Tmax); there was no significant difference among the volunteers except Vmax. The relative bioavailability of the four tablets was calculated to be 100%, 89.37%, 90.01%, 98.24% respectively; there was no correlation between their in vitro and in vivo parameters, and the correlation coefficient was 0.3938-0.4489. The above shows that the in vivo absorption of the four tablets does not agree with the rate of in vitro release. According to the experimental results in this paper, the determination of in vitro release of hydrochlorothiazide tablets can not be used to reflect the bioavailability of the drug in the body, this opinion for the future development of pharmacological hydrochlorothiazide tablet specifications reference.