氢溴酸加兰他敏口腔崩解片与普通片在健康人体的生物等效性

Bioequivalence of galanthamine hydrobromide orally disintegrating tablets and common tablets in healthy volunteers

目的研究中国健康志愿者单次口服氢溴酸加兰他敏(可逆性胆碱酯酶抑制剂)口腔崩解片的生物等效性。方法 20名健康志愿者随机分成2组,分别接受单次口服2种国产氢溴酸加兰他敏20mg;采用液相色谱-串联质谱法测定给药后不同时间点血浆中的氢溴酸加兰他敏浓度,用DASver2.1软件计算其药代动力学参数。结果氢溴酸加兰他敏的受试制剂与参比制剂主要药代动力学参数:tmax分别为(1.06±0.81),(0.85±0.26)h;t1/2分别为(8.39±1.60),(8.22±1.58)h;Cmax分别为(39.69±8.17),(43.41±11.58)μg·L-1;AUC0-t分别为(384.88±101.75),(407.53±101.12)μg·h·L-1;AUC0-∞分别为(396.92±105.85),(420.10±103.73)μg·h·L-1。氢溴酸加兰他敏的相对生物利用度为(95.5±16.2)%。结论 2种制剂具有生物等效性。

Objective To study the bioequivalence of a single dose galanthamine hydrobromide orally disintegrating tablets in Chinese healthy volunteers. Methods Twenty healthy volunteers were divided into 2 groups. Twenty mg single oral dose of galanthamine hydrobromide orally disintegrating tablets was given to 20 healty volunteers. The concentrations of plasma samples collected from the volunteers respectively were determined by LC - MS/MS. The pharmacokinetic parameters were calaulated by DAS ver 2. 1 software. Results The main pharmacokinetic parameters of galanthamine hydrobromide orally disintegrating test and reference tablets were as follows：tmax were （ 1.06 ±0. 81 ） and （0. 85 ± 0.26） h; t1/2 were （8.39±1.60） and （8.22±1.58） h; Cmax were （39.69±8.17） and （43.41 ± 11.58） ug . L-1; AUC0-t were （384.88 ±101.75） and （407.53±101.12） ug . h . L-1; AUC0-∞ were （396. 92 ± 105.85） and（420. 10 ± 103.73） ug . h. L-1, respectively. The relative bioavailability of drug was （ 95.5 ± 16. 2 ） %. Conclusion The two kinds of galanthamine hydrobromide tablets are bioequivalent.