Williams R O, Sykora M A, Mahaguna V
Division of Pharmaceutics, College of Pharmacy, The University of Texas, Austin 78712-1074, USA.
AAPS PharmSciTech. 2001 Jun 9;2(2):E8. doi: 10.1208/pt020208.
A reverse-phase high-performance liquid chromatographic (HPLC) method for recovery of the lipophilic drug, alprazolam, from matrix tablets containing the hydrophilic polymer hydroxypropyl methylcellulose (HPMC) was developed. Lipophilic drugs, such as alprazolam, are difficult to completely extract and quantitate from tablets containing HPMC polymer. The percentage of recoveries of alprazolam from placebo powder spiked with alprazolam stock solution and from placebo powder mixed with alprazolam powder were about 100% and 85% to 95%, respectively. The validated method using water to completely dissolve HPMC before the addition of a strong solvent to dissolve and extract the drug from the HPMC solution was shown to be the most reproducible method. Different molecular weight distributions of the HPMC polymer, such as HPMC-K4M and HPMC-K100LV, did not influence the dissolution results of alprazolam using this validated method. Similarly, the excipients composing the matrix tablet formulations, such as dicalcium phosphate dihydrate, dicalcium phosphate anhydrous, calcium sulfate dihydrate, sucrose, dextrose, and lactose monohydrate, did not influence the percent recovery of alprazolam. The recovery method reported herein was shown to be the most efficient to achieve complete recovery of alprazolam from powder blends and tablets containing a variety of excipients and different grades of HPMC.
开发了一种反相高效液相色谱（HPLC）方法，用于从含有亲水性聚合物羟丙基甲基纤维素（HPMC）的基质片剂中回收亲脂性药物阿普唑仑。亲脂性药物，如阿普唑仑，很难从含有HPMC聚合物的片剂中完全提取和定量。从添加了阿普唑仑储备溶液的安慰剂粉末以及与阿普唑仑粉末混合的安慰剂粉末中回收阿普唑仑的回收率分别约为100%和85%至95%。经验证，在添加强溶剂以从HPMC溶液中溶解和提取药物之前，先用水完全溶解HPMC的方法是最可重复的方法。使用这种经过验证的方法，不同分子量分布的HPMC聚合物，如HPMC-K4M和HPMC-K100LV，不会影响阿普唑仑的溶出结果。同样，组成基质片剂配方的辅料，如二水磷酸氢钙、无水磷酸氢钙、二水硫酸钙、蔗糖、葡萄糖和一水乳糖，也不会影响阿普唑仑的回收率。本文报道的回收方法被证明是从含有各种辅料和不同等级HPMC的粉末混合物和片剂中实现阿普唑仑完全回收的最有效方法。
