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目的：比较自制的盐酸尼卡地平缓释微丸（ Ｎ Ｉ Ｃ Ｓ Ｐ）与普通市售盐酸尼卡地平片剂、进口缓释尼卡地平胶囊（ Ｐｅｒｄｉｐｉｎｅ Ｌ Ａ）的药代动力学及生物利用度。方法：采用拉丁方试验设计，将志愿者６ 人随机分为３ 组，交叉口服 Ｎ Ｉ Ｃ Ｓ Ｐ、普通市售片剂和 Ｐｅｒｄｉｐｉｎｅ Ｌ Ａ，以普通片剂和 Ｐｅｒｄｉｐｉｎｅ Ｌ Ａ 为对照制剂，计算 Ｎ Ｉ Ｃ Ｓ Ｐ的相对生物利用度。结果： Ｎ Ｉ Ｃ Ｓ Ｐ相对于 Ｐｅｒｄｉｐｉｎｅ Ｌ Ａ 的生物利用度为１１６．０９％ ；两种制剂的 Ａ Ｕ Ｃ及体内平均驻留时间（ Ｍ Ｒ Ｔ）有显著性差异（ Ｐ＜ ０．０５）；达峰时间，峰浓度，消除速率常数和吸收速率常数均没有显著性差异（ Ｐ＞ ０．０５）。 Ｎ Ｉ Ｃ Ｓ Ｐ和 Ｐｅｒｄｉｐｉｎｅ Ｌ Ａ 相对于普通片剂的生物利用度分别为８６．５３％ 和 ７４．５４％ 。结论： Ｎ Ｉ Ｃ Ｓ Ｐ体内缓释效果优于进口的 Ｐｅｒｄｉｐｉｎｅ Ｌ Ａ，达到设计要求。
OBJECTIVE: To compare the pharmacokinetics of homemade sustained-release nicardipine hydrochloride pellets (N I C-S P) with nicardipine hydrochloride tablets and the imported sustained-release nicardipine capsules (Perdipine L A) bioavailability. Methods: Sixteen volunteers were randomly divided into three groups according to the Latin square design. N I C S P, common commercial tablets and Perdipine L A at the crossover point were taken as control tablets and Perdipine L A as control. Calculate the relative bioavailability of NIC-SP. RESULTS: The bioavailability of N I CS P relative to Perdipine L A was 116.09%. There was a significant difference between the two preparations in terms of A U C and mean in vivo residence time (M R T) (P <0. 05). There was no significant difference in peak time, peak concentration, elimination rate constant and absorption rate constant (P> 0.05). Bioavailability of NIC-P and Perdipine L-A relative to conventional tablets were 86.53% and 74.54%, respectively. Conclusion: N I C S P sustained release in vivo better than imported Perdipine L A, to meet the design requirements.