Preparation and Evaluation of Artemether Oral Microemulsion- Gel

XUE Hong-jiao; TANG Hua-zheng; ZHANG Qi; GUO Kun-kun; YANG Zhao-xiang; CAI Zheng

doi:10.13422/j.cnki.syfjx.20180903

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Preparation and Evaluation of Artemether Oral Microemulsion- Gel

更新时间：2024-01-04

- Preparation and Evaluation of Artemether Oral Microemulsion- Gel
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 24, Issue 9, Pages: 29-36(2018)
- 作者机构：
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- DOI：10.13422/j.cnki.syfjx.20180903
  CLC： R283.6
- Published：2018
- 稿件说明：
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XUE Hong-jiao, TANG Hua-zheng, ZHANG Qi, et al. Preparation and Evaluation of Artemether Oral Microemulsion- Gel[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(9): 29-36.
DOI：

XUE Hong-jiao, TANG Hua-zheng, ZHANG Qi, et al. Preparation and Evaluation of Artemether Oral Microemulsion- Gel[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(9): 29-36. DOI： 10.13422/j.cnki.syfjx.20180903.

摘要

目的：优选蒿甲醚口服微乳原位凝胶的处方，并对其性质进行评价。方法：以流动性和凝胶性为指标筛选水相，通过溶解度、相溶性、制剂稳定性和黏附性的考察确定处方组分，采用伪三元相图筛选微乳原位凝胶区域，优选蒿甲醚微乳原位凝胶的最优处方，并对其形态，粒径，Zeta电位，黏度，稳定性，凝胶性以及体内胃滞留时间进行评价。结果：蒿甲醚微乳原位凝胶的最优处方为蒿甲醚-三乙酸甘油酯-聚氧乙烯蓖麻油-二乙二醇单乙基醚-（0.3%结冷胶-0.1%低黏度海藻酸钠）（0.5：4.5：5：5：85），药物浓度约5 g ·L-1，透射电镜下观察乳滴呈球形，平均粒径20.90 nm，多分散指数（PDI）0.172，Zeta电位-19.5 mV，黏度15.32 mPa ·s，在室温条件下稳定。大鼠口服蒿甲醚微乳原位凝胶后，微乳原位凝胶在胃中快速发生相变形成凝胶，6 h后依然能在大鼠的胃中观察到凝胶并检测出蒿甲醚。结论：蒿甲醚微乳原位凝胶改善了蒿甲醚的溶解度，在胃部凝胶性能良好，能有效延长蒿甲醚的胃滞留时间，且黏度适宜，适合口服给药。

Abstract

Objective: To screen the optimal formula for artemether oral microemulsion-in situ gel and evaluate its properties. Method: With liquidity and gelation capacity as indexes

the water phase was determined.The composition was screened by solubility assay

compatibility test

stability and adhesiveness of microemulsion-in situ gel system.Pseudoternary phase diagram was used to optimize the formula.The morphology

particle size

Zeta potential

viscosity

stability

gelation and gastric retention time in vivo of artemether microemulsion-in situ gel were investigated

respectively. Result: The optimal formula was as follows:artemether:glyceryl triacetate:cremophor EL35:transcutol HP:(0.3% gellan gum-0.1% sodium alginate with low viscosity)=0.5:4.5:5:5:85

the concentration of artemether in the microemulsion-in situ gel about 5 g · L-1. Artemether microemulsion-in situ gel in transmission electron microscope consisted of small spherical droplets

mean particle size

polydispersity index (PDI)

Zeta potential

viscosity of the drug delivery system were 20.90 nm

0.172

-19.5 mV and 15.32 mPa · s

respectively.After oral administration

it gelled in the stomach of rats immediately;six hours later

gel could still be observed and artemether could be detected in the stomach. Conclusion: The solubitily of artemether is significantly increased in microemulsion-in situ gel.The artemether microemulsion-in situ gel has characteristics of good gelation in stomach and suitable viscosity

it not only can prolong the gastric retention time of artemether but also is suitable for oral administration.

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