RA Chem Pharma Limited, Road No 18 IDA, Nacharam, Hyderabad-500076, India.
Acta Pharm. 2010 Jun;60(2):185-95. doi: 10.2478/v10007-010-0019-6.
Efavirenz (EFV) tablets of different doses were prepared by a wet granulation process using different superdisintegrants such as crosscarmellose sodium (CCS), sodium starch glycollate (SSG) and crosspovidone (CP) to evaluate the role of different disintegrants on the in vitro release of EFV. Further, the mode of addition of disintegrants on EFV dissolution from tablets containing 600 mg of the drug was evaluated by incorporating the disintegrants extragranularly (EG), intragranularly (IG) or distributing them equally (IG and EG). In vitro dissolution of the prepared tablets was conducted using the recommended medium and a dissolution medium developed in-house, which had the ability to discriminate between the formulations. The t50 and t80 values were indicative of the fact that the drug release was faster from tablet formulations containing CP. CP was able to release the drug faster than the other two disintegrants in both dissolution media and the drug release was unaffected by the mode of CP addition.
采用湿法制粒工艺，使用不同的超级崩解剂，如交联羧甲纤维素钠（CCS）、交联聚维酮（CP）和淀粉甘醇酸钠（SSG），制备了不同剂量的依非韦伦（EFV）片，以评估不同崩解剂对 EFV 体外释放的作用。此外，通过将崩解剂额外添加（EG）、内添加（IG）或等量分配（IG 和 EG）到含有 600mg 药物的片剂中，评估了崩解剂在含药片中的添加方式对 EFV 溶出的影响。采用推荐的介质和自行开发的溶出介质对制备的片剂进行体外溶出度研究，该介质具有区分不同配方的能力。t50 和 t80 值表明，含有 CP 的片剂配方的药物释放速度更快。在两种溶出介质中，CP 均比其他两种崩解剂更快地释放药物，CP 的添加方式对药物释放没有影响。
