摘要：亲脂性参数在解释药物体内吸收、分布和排泄及预测生物活性等方面的重要性早已被人们认识。几种简单有机溶剂／水分配系统的模型都曾被用于评价药物的亲脂性，但其中取得较为成功的为正辛醇／水系统～([1])。在定量构效关系和药物合理设计上，它已成为标准疏水性参数，构成了药物特征参数的数据库。近年来，研究表明正辛醇／水系统并小能完全模拟所有类型药物在生物膜模型(液晶态脂质体膜)上的分配行为，导致其不能解释由不同化学结构类型药物组成集合的药动学和药效学特征。研究结果表明其分配系数与稳态下脑／血浓度比值或穿透血脑屏障渗透系数间无明显联系～([2])。这主要是因为各向同性、不带电荷中心的正辛醇相并不是呈液晶态生物膜上有序磷脂双分子层的客观模型。

摘要：小肠上皮细胞刷状缘侧的寡肽转运蛋白(PEPT1)以及侧底膜的寡肽转运蛋白是寡肽转运蛋白(PEPT)的2种亚型,它们在寡肽及拟肽类药物(peptidomimetic drug)肠转运中发挥重要作用。通过前体药物(prodrug)设计将一些吸收差的药物修饰成类似二肽或三肽的结构,在PEPT1的介导下吸收,能够提高这些药物的口服生物利用度,这是非常有意义的。

摘要：目的评价氯沙坦钾胶囊与片剂(抗高血压药)在健康人体的生物等效性。方法用随机交叉试验设计,20名健康志愿者分别单剂口服氯沙坦钾受试制剂和参比制剂50mg,测定其血药浓度并进行生物等效性的检验。结果受试制剂和参比制剂的Cmax分别为(317.42±217.05),(295.57±132.16)ng·mL-1;tmax分别为(1.17±0.67),(1.27±0.73)h;AUC0-t分别为(637.63±379.83),(591.05±300.77)ng·h·mL-1,2制剂比较无显著性差异。结论氯沙坦钾胶囊与氯沙坦钾片为生物等效性制剂。

摘要：Aim To evaluate the bioequivalence of two brands of losartan/hydrochlorothiazide （50 mg/12.5 mg） compound tablets in healthy Chinese male volunteers. Methods An open, randomized, single-dose, two-period cross-over study with a wash-out period of 7 d was conducted. Twenty healthy male volunteers were given a single dose 50 mg losartan/12.5 mg hydrochlorothiazide of either test （T） or reference （R） compound tablets, respectively. Blood samples were collected up to 48 h after oral administration. The concentrations of losartan and hydrochlorothiazide in plasma were determined by a validated HPLC-ESI-MS method. Results In the case of losartan, the 90% confidence intervals of two one-side test for percent ratios with a significant level （α） of 0. 05 were 86% - 112% for AUC0-12 and 89% - 134% for Cmax, respectively, which were within the interval proposed in the Chinese Pharmacopoeia, 80% - 125% of AUC and 70% - 143% of Cmax, respectively. Similarly, the 90% confidence intervals for percent ratios were 85% - 100% and 75% - 102% for hydrochlorothiazide, both of which fell into the accepted interval. Conclusion Two immediate-release compound tablets of losartan/hydrochlorothiazide are bioequivalent from a statistical standpoint in the extent and rate of absorption from the single-dose study in healthy Chinese male volunteers.