Poona College of Pharmacy, Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Erandwane, Pune 411038, Maharashtra, India.
Pharm Res. 2013 Jul;30(7):1906-14. doi: 10.1007/s11095-013-1033-4. Epub 2013 Apr 18.
To investigate influence of ion induced mesophasic transformation on pharmaceutical performance of in situ gelling system consisting of glyceryl monooleate.
The prepared system showed mesophasic transformation during its conversion from sol to gel upon controlled hydration. The process of mesophasic transformation was studied by SAXS, DSC, rheology and plane polarized light microscopy. Further the influence of additives i.e. naproxen salts (sodium and potassium) and naproxen (base) on the process of mesophasic transformation was also elucidated.
It was observed that addition of salt form of naproxen transformed W/O emulsions into cubic mesophase whereas addition of base form of naproxen formed reverse hexagonal (HII) phase upon controlled hydration. The cubic mesophase formed by naproxen salts retarded the drug release for initial 3 h whereas HII phase showed sustained drug release characteristics for naproxen base following Higuchi drug release kinetics.
The current work suggests that formulations with tailor made pharmaceutical performance can be developed by selecting proper additives in the system so as to obtain the desired mesophase 'on demand' thereby controlling drug release characteristics.
研究离子诱导中间相转变对由单油酸甘油酯组成的原位凝胶体系的药物性能的影响。
所制备的体系在受控水合时从溶胶向凝胶转变过程中表现出中间相转变。通过小角 X 射线散射（SAXS）、差示扫描量热法（DSC）、流变学和平面偏振光显微镜研究了中间相转变的过程。此外，还阐明了添加剂（即萘普生盐（钠和钾）和萘普生（碱））对中间相转变过程的影响。
观察到萘普生盐的添加形式将 W/O 乳液转变为立方中间相，而萘普生碱的添加形式在受控水合时形成反向六方（HII）相。萘普生盐形成的立方中间相在最初 3 小时内延缓了药物释放，而 HII 相则遵循 Higuchi 药物释放动力学，表现出萘普生碱的持续药物释放特性。
目前的工作表明，可以通过在体系中选择适当的添加剂来开发具有定制药物性能的制剂，从而获得所需的中间相“按需”，从而控制药物释放特性。
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