Sekiya Noboru, Nishiwaki Atsushi, Nishiura Akio, Yamamoto Masanobu, Takeda Kazuhisa, Iohara Daisuke, Hirayama Fumitoshi, Arima Hidetoshi, Uekama Kaneto
Pharmaceutical Development Laboratories, Ono Pharmaceutical Co., Ltd.,Osaka, Japan.
Chem Pharm Bull (Tokyo). 2008 Jan;56(1):7-11. doi: 10.1248/cpb.56.7.
We studied the effects of dextran, dextrin, and disintegrants on the chemical stability of Opalmon tablets containing Limaprost-alfadex (Limaprost/alpha-cyclodextrin complex) and found that the addition of dextran or dextrin significantly improved the chemical stability of Opalmon tablets under high humidity, compared to lactose. We also examined how dextran stabilizes Limaprost in Opalmon tablets and studied the formulation of Opalmon tablets in order to achieve higher chemical stability, rapid dissolution and reduced stickiness. The results suggested that dextran increases stabilization after moisture adsorption by decreasing the dissociation of Limaprost-alfadex to the free drug and alpha-cyclodextrin in the dextran matrix, when compared with the lactose matrix. The stickiness of Opalmon tablets containing dextran and dextrin was negligible when dextran and dextrin amounted to less than 20% of the formulation. By selecting a proper disintegrant, we obtained Opalmon tablets with higher chemical stability and rapid dissolution properties.
我们研究了右旋糖酐、糊精和崩解剂对含有利马前列素-α-环糊精（利马前列素/α-环糊精复合物）的Opalmon片剂化学稳定性的影响，发现与乳糖相比，添加右旋糖酐或糊精可显著提高Opalmon片剂在高湿度条件下的化学稳定性。我们还研究了右旋糖酐如何稳定Opalmon片剂中的利马前列素，并研究了Opalmon片剂的配方，以实现更高的化学稳定性、快速溶解和降低粘性。结果表明，与乳糖基质相比，右旋糖酐通过减少利马前列素-α-环糊精在右旋糖酐基质中解离为游离药物和α-环糊精，从而在吸湿后增强稳定性。当右旋糖酐和糊精的含量低于制剂的20%时，含有右旋糖酐和糊精的Opalmon片剂的粘性可忽略不计。通过选择合适的崩解剂，我们获得了具有更高化学稳定性和快速溶解性能的Opalmon片剂。
