陈 鹰 李 高 黄建耿 王瑞华 刘 宏 汤 韧. 自微乳化技术与固体分散技术在改善长春西汀溶出度和生物利用度上的比较(英文)J. 药学学报, 2009,44(6): 658-666.
引用本文: 陈 鹰 李 高 黄建耿 王瑞华 刘 宏 汤 韧. 自微乳化技术与固体分散技术在改善长春西汀溶出度和生物利用度上的比较(英文)J. 药学学报, 2009,44(6): 658-666.
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CHEN Ying, Li- Gao, Huang-Jian-Geng, Wang-Rui-Hua, Liu- Hong, Tang- Ren. Comparison of self-microemulsifying drug delivery system versus solid dispersion technology used in the improvement of dissolution rate and bioavailability of vinpocetineJ. 药学学报, 2009,44(6): 658-666.
Citation: CHEN Ying, Li- Gao, Huang-Jian-Geng, Wang-Rui-Hua, Liu- Hong, Tang- Ren. Comparison of self-microemulsifying drug delivery system versus solid dispersion technology used in the improvement of dissolution rate and bioavailability of vinpocetineJ. 药学学报, 2009,44(6): 658-666.
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自微乳化技术与固体分散技术在改善长春西汀溶出度和生物利用度上的比较(英文)

Comparison of self-microemulsifying drug delivery system versus solid dispersion technology used in the improvement of dissolution rate and bioavailability of vinpocetine

    摘要
  • 摘要:

    探讨与比较自微乳化释药系统 (self-microemulsifying drug delivery systems, SMEDDS) 与固体分散体 (solid dispersion, SD) 在改善难溶性药物长春西汀 (vinpocetine, VIP) 溶出度和生物利用度方面的差异。本文选用中链甘油三酯 (Labrafac)、油酸、聚氧乙烯氢化蓖麻油 (Cremophor EL) 和二乙二醇单乙基醚 (Transcutol P) 为材料, 以微粉硅胶吸附制备长春西汀固体自微乳化释药系统 (VIP-SMEDDS); 采用泊洛沙姆188 (F68) 为载体制备长春西汀固体分散体 (VIP-SD)。溶解度实验结果表明, VIP在SMEDDS中的溶解度是SD载体中的17.3倍; 体外溶出度实验表明, VIP-SMEDDS的溶出效果和稳定性比VIP-SD更好; 大鼠体内生物利用度实验表明VIP-SMEDDS是VIP原料的1.89倍, 且不受食物影响, 而VIP-SD的生物利用度与VIP原料相比不具有显著性差异。给药2 h后组织分布结果表明, VIP-SMEDDS在Peyer’s节、肠道、肝脏的药物浓度分别是VIP-SD的3.7、2.2和1.5倍。Caco-2细胞转运实验表明VIP-SMEDDS的表观渗透系数 (Papp, cm·s−1) 是VIP-SD的2.65倍。透射电镜下观察, VIP-SMEDDS组Caco-2细胞间隙是空白对照组的9.6倍, 而VIP-SD组与空白组比较无显著性差异。由此可见, 自微乳化技术在改善长春西汀溶解度、溶出度、肠黏膜透过率、淋巴吸收和生物利用度以及减少食物影响方面优于固体分散技术。

     

    Abstract:

    The objective of this study is to compare the differences between self-microemulsifying drug  delivery system (SMEDDS) and solid dispersion (SD) technology used to improve the dissolution rate and bioavailability of vinpocetine (VIP).  The formulation of VIP-SMEDDS was composed of Labrafac, oleic acid, Cremophor EL, Transcutol P, and gum acacia which was used as solid absorbent. VIP-SD was prepared using  poloxamer F68 as the carrier.  In the solubility test, the solubility of VIP in SMEDDS was 17.3 times as much as that in SD.  In the dissolution test, SMEDDS had shown better enhancement and stability in dissolving VIP than SD.  When compared to VIP crude powder, the bioavailability of VIP in SMEDDS (VIP-SMEDDS) was 1.89-fold higher, and was less affected by food intake.  However, the bioavailability of VIP in SD (VIP-SD) was bioequivalent to that of VIP crude powder.  The tissue uptake of VIP-SMEDDS in Peyer’s patches, intestine  and liver after administration for 2 hours was more favorable than that of VIP-SD, which was 3.7 times higher  in Peyer’s patches, 2.2 times higher in intestine and 1.5 times higher in liver.  In Caco-2 tests, the apparent  permeability (Papp) of VIP-SMEDDS was 2.65 times of that of VIP-SD.  The width of the cell tight junctions of Caco-2 cell monolayer treated with VIP-SMEDDS were 9.6-fold wider, but there was no significant change after treatment with VIP-SD, when compared to the blank control.  In conclusion, SMEDDS was more efficient than the traditional SD technology in increasing solubility, dissolution, intestinal permeability, lymphatic absorption and bioavailability of the insoluble drugs such as VIP, which is less affected by food intake.

     

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