Effect of diethyl-beta-cyclodextrin on the release of nitroglycerin from formulations.

Drug design and delivery Pub Date : 1990-10-01
M Umemura, H Ueda, K Tomono, T Nagai
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Abstract

The complex-forming abilities of 2,6-di-O-ethyl-beta-cyclodextrin (DE-beta-CD), and its effect on the release of nitroglycerin (TNG) from formulations of the compound, were studied and compared with corresponding properties of beta-cyclodextrin (beta-CD) and 2,6-di-O-methyl-beta-cyclodextrin (DM-beta-CD). Complex formation was confirmed by differential scanning calorimetry and infrared absorption spectroscopy. In an accelerator test involving temperature and reduced pressure, marked depression of the volatility of TNG was observed as a result of CD complex formation. Dissolution rates of TNG from powdery TNG/DE-beta-CD complex and its tablets were retarded in comparison with the rates from other CD complexes. The release rate of TNG from ointments was accelerated by complexation with DE-beta-CD, and retarded by complexation with beta-CD. To evaluate their in vivo percutaneous absorption, samples were applied to the inside tip of the cheek pouch of male golden hamsters. The amount of TNG remaining in the cheek pouch was lowest in the case of the TNG/DE-beta-CD complex ointment, and relatively high in the case of the TNG/beta-CD complex ointment, in agreement with the in vitro results. We suggest that the combination of DE-beta-CD complex and beta-CD complex might be applicable to sustained-release preparations for percutaneous administration.

二乙基- β -环糊精对配方中硝酸甘油释放的影响。
研究了2,6-二o -乙基- β -环糊精(de - β - cd)的络合物形成能力及其对制剂中硝酸甘油(TNG)释放的影响,并与β -环糊精(β - cd)和2,6-二o -甲基- β -环糊精(dm - β - cd)的相应性质进行了比较。用差示扫描量热法和红外吸收光谱法证实了络合物的形成。在一项涉及温度和减压的加速器测试中,由于CD络合物的形成,观察到TNG的挥发性明显降低。粉状TNG/ de - β -CD配合物及其片剂中TNG的溶出速度比其他CD配合物慢。与de - β - cd络合可加速TNG在软膏中的释放,与β - cd络合可延缓TNG的释放。为了评估其体内经皮吸收,将样品涂于雄性金仓鼠颊囊内侧尖端。在TNG/ de - β - cd复合物软膏中,脸颊袋中残留的TNG量最低,而在TNG/ β - cd复合物软膏中相对较高,与体外实验结果一致。我们认为de - β - cd复合物和β - cd复合物的组合可能适用于经皮给药的缓释制剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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