Hurtado y de la Peña Marcela, Vargas Alvarado Yolanda, Domínguez-Ramírez Adriana Miriam, Cortés Arroyo Alma Rosa
Departamento Sistemas Biológicos, Universidad Autónoma Metropolitana Unidad Xochimilco, Colonia Villa Quietud, México D.F., México.
Drug Dev Ind Pharm. 2003 Aug;29(7):777-84. doi: 10.1081/ddc-120021777.
The in vitro dissolution of albendazole from three different commercially available products (200 mg tablets) was studied using U.S. Pharmacopeia (USP) Apparatus 2 and USP Apparatus 4 in order to compare the release performance of the drug in two essentially different dissolution systems. For both cases, 0.1 N HCl was used as dissolution medium. Only the reference product and one of the generic products studied met the 80% USP 24 specification for albendazole dissolved at 30 min, using USP Apparatus 2. Although the reference product reached 80% of albendazole dissolved at 30 min when Apparatus 4 was used, the generic products' dissolution performance was markedly reduced in this system. Though dissolution rate was slower using Apparatus 4, the total quantity of albendazole dissolved from the reference product, represented by area under the dissolution profile, was practically the same regardless of the system used. Dissolution kinetics of albendazole was adequately described by Weibull's function for all the products. The dissolution time (t(d)) derived from data fitting to this function showed significant differences among the products studied. Data analysis based on analysis of variance (ANOVA) showed nonequivalence among the dissolution profiles of generic products compared with the reference product either with the dissolution vessel system or the flow-through cell, as well as nonequivalence among the dissolution profiles using both apparatuses with the same product. Though differences in the dissolution profiles for generic products against the reference product in both systems were found, USP Apparatus 4 showed higher discriminative capacity in differentiating the release characteristics of the products tested.
为比较阿苯达唑在两种截然不同的溶出系统中的释放性能，采用美国药典（USP）装置2和USP装置4研究了三种不同市售产品（200mg片剂）中阿苯达唑的体外溶出情况。对于这两种情况，均使用0.1N盐酸作为溶出介质。仅参比产品和所研究的一种仿制产品在使用USP装置2时，30分钟时阿苯达唑的溶出量符合80%的USP 24标准。尽管使用装置4时参比产品在30分钟时阿苯达唑的溶出量达到了80%，但在该系统中仿制产品的溶出性能显著降低。尽管使用装置4时溶出速率较慢，但无论使用何种系统，以溶出曲线下面积表示的参比产品中阿苯达唑的总溶出量实际上是相同的。所有产品的阿苯达唑溶出动力学均可用威布尔函数充分描述。根据该函数数据拟合得出的溶出时间（t(d)）在所研究的产品之间存在显著差异。基于方差分析（ANOVA）的数据分析表明，与参比产品相比，仿制产品在溶出容器系统或流通池中的溶出曲线不等效，并且同一产品使用两种装置时的溶出曲线也不等效。尽管在两种系统中均发现仿制产品与参比产品的溶出曲线存在差异，但USP装置4在区分受试产品的释放特性方面显示出更高的鉴别能力。
