Department of Pharmaceutics, Bharati Vidyapeeth University Poona College of Pharmacy, Erandwane, Pune, 411 038, Maharashtra, India.
Pharm Res. 2012 Aug;29(8):2180-8. doi: 10.1007/s11095-012-0746-0. Epub 2012 Apr 4.
Self-emulsifying systems (SES) emulsify spontaneously to produce fine oil-in-water emulsion when introduced into aqueous phase. The self-emulsification process plays an important role during formation of emulsion. The objective of current work was to understand and explore the inner structuration of SES through controlled hydration and further to study the influence of additive on the same which ultimately governs performance of final formulation in terms of droplet size.
Droplet size of final formulations containing structural analogues of ibuprofen was determined. Microstructural properties of intermediate hydrated regimes of SES were investigated using techniques such as small angle X-ray scattering, differential scanning calorimetry and rheology.
The current work established inverse relationship between droplet size of the formulations containing structural analogues of ibuprofen and their Log P values. Microstructural analysis of intermediate hydrated regimes of the prepared samples showed formation of local lamellar structure. Structural analogues of ibuprofen significantly altered microstructure of lamellae which was well correlated with the droplet size of final formulations. In vitro drug release study showed increase in dissolution rate of lipophillic drugs when formulated as SES.
The current work emphasizes the fact that tailor-made formulations can be prepared by controlling the properties of intermediate regimes.
自乳化系统（SES）在引入水相时会自发乳化，产生细小的油包水乳液。自乳化过程在乳液形成过程中起着重要作用。目前的工作旨在通过控制水合作用来了解和探索 SES 的内部结构，并进一步研究添加剂对其的影响，这最终会影响最终配方的性能，包括粒径。
测定含有布洛芬结构类似物的最终配方的粒径。使用小角度 X 射线散射、差示扫描量热法和流变学等技术研究 SES 中间水合阶段的微观结构特性。
本工作建立了含有布洛芬结构类似物的制剂的粒径与其 Log P 值之间的反比关系。对制备样品中间水合阶段的微观结构分析表明，局部层状结构的形成。布洛芬的结构类似物显著改变了层状结构的微观结构，这与最终制剂的粒径很好地相关。体外药物释放研究表明，将亲脂性药物制成 SES 可提高其溶解速率。
本工作强调了通过控制中间阶段的性质可以制备定制配方的事实。
