Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
J Microencapsul. 2009 May;26(3):251-62. doi: 10.1080/02652040802305113. Epub 2008 Oct 20.
The objective of the present study was to prepare multiple-unit formulations of carbamazepine (CBZ) using an emulsion congealing technique. CBZ-hydrogenated castor oil (HCO) (Cutina® HR) wax microparticles were prepared without organic solvents as an alternative to polymeric microparticles. The process involved emulsification and solidification of CBZ-HCO melt at a significantly low temperature (5°C). Five amphiphilic excipients (Pluronic F-68 (PL), Labrasol (LB), Gelucire 44/14 (GL 44/14), D-α-tocopheryl PEG 1000 succinate (TPGS) and Docusate sodium (DOSS) were added with the wax melt. The microparticles were characterized with respect to their particle size distribution, drug loading, morphological character, drug-excipient interaction, differential scanning calorimetry, Fourier-transform infra-red (FT-IR) and release properties. An average value for production yield was 83.45%. Evaluation of the release data indicates that the release mechanism from the prepared Cutina® HR microparticles follows both the Higuchi model of diffusion and anomalous release mechanism. Microparticles containing 5% Labrasol, TPGS and GL 44/14 had the highest extent of dissolution.
本研究的目的是使用乳液凝固技术制备卡马西平（CBZ）的多单位制剂。采用无有机溶剂的方法制备 CBZ-氢化蓖麻油（HCO）（Cutina® HR）蜡质微球，作为聚合物微球的替代品。该过程涉及在显著低温（5°C）下乳化和固化 CBZ-HCO 熔体。加入五种两亲性赋形剂（Pluronic F-68（PL）、Labrasol（LB）、Gelucire 44/14（GL 44/14）、D-α-生育酚聚乙二醇 1000 琥珀酸酯（TPGS）和 Docusate 钠（DOSS）与蜡质熔体混合。对微球进行了粒径分布、载药量、形态特征、药物-赋形剂相互作用、差示扫描量热法、傅里叶变换红外（FT-IR）和释放性能的特征描述。产物收率的平均值为 83.45%。释放数据的评估表明，从制备的 Cutina® HR 微球中释放的机制同时遵循 Higuchi 扩散模型和异常释放机制。含有 5% Labrasol、TPGS 和 GL 44/14 的微球具有最高的溶解程度。
