Study on Pharmacokinetics and Pharmacodynamics of Oral Colon Targeted pH-Sensitive Hydrogel of Hydrocortisone Sodium Succinate
10.13748/j.cnki.issn1007-7693.20223138
- VernacularTitle:氢化可的松琥珀酸钠口服结肠靶向pH敏感型水凝胶的药动学与药效学研究
- Author:
YOU Cuiyu
1
;
SHI Rui
2
;
SUN Jinyao
1
;
DENG Xiang
1
;
WANG Xidan
1
;
DENG Wenting
1
;
ZHANG Wenjuan
1
Author Information
1. Department of Pharmacy, The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an 710061, China;
2. Department of Pharmacy, Yuncheng Central Hospital, Yuncheng 044000, China
- Publication Type:Journal Article
- Keywords:
hydrocortisone sodium succinate;
pH-sensitive;
oral colon-specific drug delivery system;
plasma concentration;
pharmacodynamics
- From:
Chinese Journal of Modern Applied Pharmacy
2023;40(17):2427-2434
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To study the pharmacokinetics and pharmacodynamics of oral colon targeted pH-sensitive hydrogel of hydrocortisone sodium succinate(HSS-GEL). METHODS The plasma concentration changes of HSS-GEL and HSS in the mice were investigated; 2, 4, 6-trinitrobenzene sulfonic acid(TNBS)-induced mouse model of ulcerative colitis(UC) was established, disease activity index(DAI), colon length, myeloperoxidase(MPO) and organ index were used as indicators to investigate the therapeutic effect of HSS-GEL on colitis. RESULTS The results showed that the Tmax, Cmax and AUC of HSS-GEL were significantly different from those of HSS(P<0.01). The Tmax of HSS-GEL was significantly longer than that of HSS, and the time of drug absorption into the blood was significantly delayed. The Cmax of HSS-GEL group was significantly lower than that of HSS. The AUC of the HSS-GEL group was 39.38% of the same dose of HSS, indicating that the amount of the drug absorbed into blood was significantly reduced after the HSS was made into HSS-GEL orally. After modeling, DAI, MPO activity and organ index were increased, while the colon was shortened due to the inflammatory reaction, with the treatment of HSS-GEL, DAI, MPO activity and some organ index of mice were significantly decreased comparing with TNBS group(P<0.05 or P<0.01). The degree of reduction of MPO activity and some organ indexes of the mice in the TNBS+HSS-GEL group were significantly greater than those in the TNBS+HSS group, indicating that HSS-GEL had good therapeutic effect on TNBS-induced ulcerative colitis, and the effect was better than that of HSS. CONCLUSION The HSS-GEL prepared has good colon targeting characteristic and colitis treatment effect.