Patel Hp, Patel Jk, Patel Mp, Patel Rr
Torrent Research Centre, Gandhinagar, Gujarat, India.
J Young Pharm. 2011 Apr;3(2):90-6. doi: 10.4103/0975-1483.80291.
The present invention relates to produce multiple unit particle system (MUPS) of stabilized ramipril pellets, hydrochlorothiazide, diluents, superdisintegrants, and lubricants which produce better dissolution of the system for better bioavailability with improving stability and bioavailability of ramipril. More particularly, the present invention is directed for stabilized ramipril against decomposition into degradation products, namely ramipril-DKP and ramipril-diacid, during formulation and storage conditions. Simple ramipril formulation shows 15.15% related impurities after 3-month accelerated stability study, which was minimized to the 2.07% related impurities in ramipril pellets after 6 month accelerated stability study. By making MUPS of ramipril pellets, Hydrochlorothiazide and other excipients show better dissolution (100.4% of ramipril and 97.9% of hydrochlorothiazide within 60 min) to produce better bioavailability. So, making MUPS containing ramipril pellets with polymer coating and hydrochlorothiazide and other excipients shows better stability of ramipril along degradation and synergistic effect among hypertension in immediate delivery.
本发明涉及制备稳定的雷米普利微丸、氢氯噻嗪、稀释剂、超级崩解剂和润滑剂的多单元颗粒系统（MUPS），该系统能使药物更好地溶解，从而提高生物利用度，并改善雷米普利的稳定性和生物利用度。更具体地说，本发明旨在使雷米普利在制剂和储存条件下稳定，防止其分解为降解产物，即雷米普利 - DKP和雷米普利二酸。简单的雷米普利制剂在3个月加速稳定性研究后显示出15.15%的相关杂质，而在6个月加速稳定性研究后，雷米普利微丸中的相关杂质降至2.07%。通过制备雷米普利微丸的MUPS，氢氯噻嗪和其他辅料显示出更好的溶解性（60分钟内雷米普利的溶出率为100.4%，氢氯噻嗪的溶出率为97.9%），从而产生更好的生物利用度。因此，制备含有聚合物包衣的雷米普利微丸、氢氯噻嗪和其他辅料的MUPS，在速释剂型中，雷米普利在降解过程中表现出更好的稳定性，并且在高血压治疗中具有协同作用。
