Preparation of Patchouli Oil Enteric-coated Dropping Pills and Its Efficacy Evaluation on Ulcerative Colitis Rats
10.13748/j.cnki.issn1007-7693.20230377
- VernacularTitle:广藿香油肠溶滴丸制备及其对溃疡性结肠炎大鼠的药效评价
- Author:
Xiaofeng LI
1
;
Weidong CHEN
2
;
Huayuan CHEN
3
;
Weihua XU
4
;
Ergang LIU
3
;
Huan SHEN
5
;
Bing WANG
6
;
Yongzhuo HUANG
5
Author Information
1. School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China；Zhongshan Institute for Drug Discovery, Zhongshan 528400, China；Shanghai Institute of Materia Medica Chinese Academy of Sciences, Shanghai 201203, China；Nantong Haimen Yangtze Delta Drug Advanced Research Institute, Nantong 226133, China
2. School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China
3. Zhongshan Institute for Drug Discovery, Zhongshan 528400, China
4. School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China；
5. Zhongshan Institute for Drug Discovery, Zhongshan 528400, China；Shanghai Institute of Materia Medica Chinese Academy of Sciences, Shanghai 201203, China
6. Shanghai Institute of Materia Medica Chinese Academy of Sciences, Shanghai 201203, China
- Publication Type:Journal Article
- Keywords:
patchouli oil； enteric coated dropping pills； colon-targeted release；ulcerative colitis； Eudragit
- From:
Chinese Journal of Modern Applied Pharmacy
2024;41(12):1621-1630
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE :To prepare patchouli oil enteric-coated dropping pills, evaluate its colon-targeted release behaviors and therapeutic potency against rat ulcerative colitis(UC).
METHODS
The single factor combined with response surface optimization method was used to screen matrix types and optimize preparation process parameters. Formula and thickness of Eudragit coating was selected based on dissolution tendency toward simulated intestinal fluids. Finally, colon targeting release behavior and the therapeutic effect of the preparation were assessed on the rat UC model induced by 2,4,6-trinitrobenzene sulfonic acid(TNBS).
RESULTS
The optimal prescription of patchouli oil dropping pills was patchouli oil∶PEG6000∶PEG8000 ratio of 1∶1∶1; and the optimal condition for preparing patchouli oil pills was keeping nozzle temperature at 9 ℃, and dropping pills at the speed of 33 drops·min−1, with dropping distance set at 6 cm; the optimal ratio of Eudragit L100∶Eudragit S100 was 3∶7 for preferential release in simulate intestinal fluid over simulated gastric fluid. Compared with free patchouli oil, patchouli oil enteric-coated dropping pills significantly alleviated the pathological symptoms such as weight loss, hematochezia and colon shortening in rats; the expression of pro-inflammatory cytokines IL-6, IL-1β, and IL-23 in serum was significantly down-regulated and the expression of anti-inflammatory cytokines IL-10 and TGF-β1 was significantly up-regulated. The mRNA expression of Mucin-1 and Mucin-2 in colon tissue was significantly up-regulated and the mRNA expression of inflammatory cytokines IL-6, IL-1β, and TNF-α was significantly down-regulated.
CONCLUSION
The patchouli oil enteric-coated dropping pills have colon-targeted release ability and improve the anti-inflammatory effect of drugs.
