QUAN Jishan,YU Ting,LI Mei,et al.Effect of piperine on oral bioavailability of paclitaxel self emulsifying drug delivery system[J].Journal of Yanbian University,2017,43(02):131-136.
胡椒碱对紫杉醇自乳化给药系统口服生物利用度的影响
- Title:
- Effect of piperine on oral bioavailability of paclitaxel self emulsifying drug delivery system
- Keywords:
- paclitaxel; piperine; self emulsifying drug delivery system(SEDDS); SD rat; pharmacokinetics
- 分类号:
- R944.9
- 文献标志码:
- A
- 摘要:
- 考察胡椒碱对紫杉醇自乳化给药系统(SEDDS)口服生物利用度的影响.首先采用伪三元相图筛选出紫杉醇SEDDS的最优处方,然后利用高效液相色谱法测定SD大鼠口服给药胡椒碱和紫杉醇SEDDS后的血浆中的药物浓度,并考察紫杉醇SEDDS的药物动力学参数.研究结果表明,将P-糖蛋白抑制剂胡椒碱SEDDS与紫杉醇SEDDS联合应用后能显著提高紫杉醇口服生物利用度(P<0.01).
- Abstract:
- We investigate the effect of piperine on oral bioavailability of paclitaxel self emulsifying drug delivery system(SEDDS). First, the optimal formulation of the paclitaxel SEDDS was screened by pseudo-ternary phase diagram design and then the serum concentrations of paclitaxel SEDDS were detected in SD rats after oral delivery piperine and paclitaxel SEDDS by HPLC. The plasma concentration of paclitaxel was determined by high performance liquid chromatography(HPLC). The oral bioavailability of paclitaxel after single dose was significantly increased by SEDDS(P<0.01)and co-administration of piperine(P<0.01).
参考文献/References:
[1] Shah N H, Carvajal M T, Patel C I, et al. Self-emulsifying drug delivery systems(SEDDS)with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs[J]. Int J Pharm, 1994,106(1):15-23.
[2] Esfahani M K M. Cytotoxicity of liposomal paclitaxel in breast cancer cell line MCF-7 [J]. Indian Journal of Clinical Biochemistry, 2013,28(4):358-360.
[3] Haller D G, Misset J L. Docetaxel in advanced gastric cancer[J]. Anticancer Drugs, 2002,13(5):451-460.
[4] Szebeni J, Alving C R, Savay S, et al. Formation of complement-activating particles in aqueous solutions of Taxol: possible role in hypersensitivity reactions[J]. Int Immunopharmacol, 2001,1(4):721-735.
[5] 冯立艳,王成,胡明继.静脉滴注紫杉醇出现过敏性休克1例[J].中国新药与临床杂志,1999,18(5):309-309.
[6] Kemper E M, van Zandbergen A E, Cleypool C, et al. Increased penetration of paclitaxel into to the brain by in hibition of P-glycoprotein[J]. Clin Cancer Res, 2003,9(7):2849-2855.
[7] Schellens J M, Malingre M M. Modulation of oral bioavaibility of anticancer drugs: from mouse to man[J]. Eur J Pharm Sci, 2000,12(2):103-110.
[8] 李峥,庄笑梅,李素云,等.P-糖蛋白中药抑制剂的研究进展[J].解放军药学学报,2009(4):326-329.
[9] 蔡青青.脂质、P-gp抑制剂及自微乳化释药系统对紫杉醇肠淋巴转运的影响研究[D].上海:复旦大学,2014.
[10] 周长征.自微乳化药物传递系统的研究进展[J].内蒙古中医药,2012,31(10):122-122.
[11] Nazzal S, Khan M A. Controlled release of a self-emulaifying formulation from a tablet dosage form: stability assessment and optimization of some processing parameters[J]. Int J Pharm, 2006,315(1/2):110-121.
[12] Swenson E S, Milisen W B, Curatolo W. Intestinal permeability enhancement: efficacy, acute local toxicity, and reversibility[J]. Pharmaceutical Research, 1994,11(8):1132-1142.
[13] 杨蒙蒙,张琰,刘新友,等.中药挥发油微乳与伪三元相图的研究[J].中药材,2011(8):1288-1292.
[14] Moreno M A, Ballesteros M P, Frutos P. Lecithin-based oil-in-water microemulsions for parenteral use: pseudotrnary phase diagrams, characterization and toxicity studies[J]. J Pharm Sci, 2003,92(7):1428-1437.
[15] Pons R, Carrera I, Caelles J, et al. Formation and properties of miniemulsions formed by microemulsions dilution[J]. Adv Colloid Interface Sci, 2003,106(12):129-146.
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备注/Memo
收稿日期: 2017-03-20 基金项目: 延边大学科技发展计划项目(2011第23号)
*通信作者: 孙鹏(1976—),男,副主任药师,研究方向为临床药学.