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目的：观察尼莫地平胃内滞留漂浮型缓释片的胃内漂浮状况及胃内滞留时间，比较其与普通尼莫地平片人体内药物动力学及生物利用度。方法：健康志愿者２名，空腹或饮食后口服掺入放射性活度各为１．８５×１０８Ｂｑ的９９ｍＴｃ漂浮缓释片及普通对照片，体外用ＥＣＴ观察，考察体内滞留情况；６名健康志愿者单剂量交叉口服漂浮片及普通片，描绘药－时曲线，统计矩法计算ＡＵＣ、相对生物利用度及ＭＲＴ。ＨＰＬＣ法测定血浆中尼莫地平含量。结果：漂浮缓释片空腹胃内滞留＜３ｈ，饮食后约５ｈ；对照片空腹２ｈ已排空，饮食后约３ｈ排空。缓释片相对生物利用度为３９１．４６％。结论：自制尼莫地平胃内滞留漂浮型缓释片可以显著延长胃内滞留时间，并能提高生物利用度。
OBJECTIVE: To observe the intragastric floating status and gastric residence time of floating nimodipine sustained-release tablets and compare its pharmacokinetics and bioavailability with nimodipine tablets in vivo. Methods: Two healthy volunteers were orally administered with 99mTc floating sustained-release tablets with radioactivity of 1.85 × 108Bq after oral administration of fasting or normal diet. ECT was used to observe the in vivo retention. Six healthy volunteers One-dose oral floating tablets and common tablets, depicting the drug-time curve, the statistical moment method to calculate AUC, relative bioavailability and MRT. Determination of nimodipine in plasma by. Results: The floating sustained-release tablets in the fasting stomach <3h, about 5h after the diet; the fasting 2h has been emptying the photos, emptying about 3h after the diet. The relative bioavailability of sustained release tablets was 391.46%. Conclusion: Nimodipine intragastric floating sustained-release tablets can significantly prolong gastric residence time and improve bioavailability.