Nandi Indranil, Bari Mohammad, Joshi Hemant
Geneva Pharmaceutical Technology Corp, Dayton, NJ 08810, USA.
AAPS PharmSciTech. 2003;4(1):E10. doi: 10.1208/pt040110.
The objectives of this project were to evaluate the effect of alkanols and cyclodextrins on the phase behavior of an isopropyl myristate microemulsion system and to examine the solubility of model drugs. Triangular phase diagrams were developed for the microemulsion systems using the water titration method, and the solubility values of progesterone and indomethacin were determined using a conventional shake-flask method. The water assimilation capacities were determined to evaluate the effective microemulsion formation in different systems. The alkanols showed higher microemulsion formation rates at higher concentrations. A correlation between the carbon numbers of the alkanol and water assimilation capacity in the microemulsions studied was observed; isobutanol and isopentanol produced the best results. The addition of cyclodextrins showed no effect or had a negative effect on the microemulsion formation based on the type of cyclodextrin used. Isopropyl myristate-based microemulsion systems alone could increase the solubility values of progesterone and indomethacin up to 3300-fold and 500-fold, respectively, compared to those in water. However, the addition of cyclodextrins to the microemulsion systems did not show a synergistic effect in increasing the solubility values of the model drugs. In conclusion, microemulsion systems improve the solubility of progesterone and indomethacin. But the two types of cyclodextrins studied affected isopropyl myristate-based microemulsion systems negatively and did not improve the solubilization of 2 model drugs.
本项目的目的是评估链烷醇和环糊精对肉豆蔻酸异丙酯微乳体系相行为的影响，并考察模型药物的溶解度。采用水滴定法绘制了微乳体系的三角相图，并用传统的摇瓶法测定了孕酮和吲哚美辛的溶解度值。通过测定水同化能力来评估不同体系中微乳的有效形成情况。链烷醇在较高浓度下表现出更高的微乳形成速率。在所研究的微乳中，观察到链烷醇的碳原子数与水同化能力之间存在相关性；异丁醇和异戊醇产生的效果最佳。根据所用环糊精的类型，环糊精的添加对微乳形成无影响或有负面影响。与在水中相比，仅基于肉豆蔻酸异丙酯的微乳体系可分别将孕酮和吲哚美辛的溶解度值提高至3300倍和500倍。然而，向微乳体系中添加环糊精在提高模型药物溶解度值方面未显示出协同作用。总之，微乳体系提高了孕酮和吲哚美辛的溶解度。但所研究的两种环糊精对基于肉豆蔻酸异丙酯的微乳体系有负面影响，且未改善两种模型药物的增溶效果。
