Iervolino M, Raghavan S L, Hadgraft J
Dipartimento di Chimica Farmaceutica e Tossicologica, Universitá di Napoli 'Federico II', Via D. Montesano 49, Napoli, Italy.
Int J Pharm. 2000 Apr 5;198(2):229-38. doi: 10.1016/s0378-5173(00)00346-x.
Permeation enhancement of ibuprofen from supersaturated solutions formed using the cosolvent technique was investigated using silicone as a model membrane. Hydroxpropyl methyl cellulose and hydroxpropyl-beta-cyclodextrin were used to stabilise the supersaturated states. Physical stability studies showed best results for low drug concentrations in a 40:60 propylene glycol/water cosolvent system. Variations in flux across model silicone membranes from saturated solutions were observed as the PG content was increased. The flux of IBU increased with the degree of saturation for solutions prepared in a 40:60 PG/water cosolvent mixture. HPMC and CD were found to be effective in enhancing the stability of supersaturated solutions of IBU. The mechanisms of action are different for the two additives and are discussed.
以硅酮为模型膜，研究了采用助溶剂技术形成的布洛芬过饱和溶液的渗透增强情况。羟丙基甲基纤维素和羟丙基-β-环糊精用于稳定过饱和状态。物理稳定性研究表明，在40:60的丙二醇/水助溶剂体系中，低药物浓度的效果最佳。随着丙二醇含量的增加，观察到饱和溶液透过模型硅酮膜的通量有所变化。在40:60的丙二醇/水助溶剂混合物中制备的溶液，布洛芬的通量随饱和度的增加而增加。发现羟丙基甲基纤维素和环糊精可有效提高布洛芬过饱和溶液的稳定性。讨论了两种添加剂不同的作用机制。
