In Vitro Pharmacokinetics and Pharmacodynamic Evaluation of Jiaojiang Cataplasms
10.13422/j.cnki.syfjx.20220155
- VernacularTitle:椒姜凝胶贴膏的体外释药动力学与药效学评价
- Author:
Ming-shuo WANG
1
;
Mao-bo DU
2
;
Shuo SHEN
2
;
Rui-hua DANG
3
;
Lan WANG
2
;
Hong YI
2
;
Yao YAO
2
;
Chun-min WANG
4
;
Shu-zhi LIU
2
Author Information
1. Chengde Medical University，Chengde 067000，China
2. Institute of Chinese Materia Medica，China Academy of Chinese Medical Sciences，Beijing 100700，China
3. Jianʹan Pharmaceutical Co. Ltd.，Shenzhen 518000，China
4. Hebei New Exciptients Technology Innovation Center of Traditional Chinese Medicine， Chengde 067000，China
- Publication Type:Journal Article
- Keywords:
Jiaojiang cataplasms;
transdermal absorption;
in vitro release;
hydroxy-α-sanshool;
6-gingerol;
ginsenoside Rb1;
intestinal paralysis
- From:
Chinese Journal of Experimental Traditional Medical Formulae
2022;28(5):141-147
- CountryChina
- Language:Chinese
-
Abstract:
ObjectiveTo study the in vitro kinetics of Jiaojiang cataplasms and evaluate its pharmacodynamics， so as to provide a feasible basis for the development of this preparation. MethodThe improved Franz diffusion cell was used for the in vitro release in semipermeable membrane and transdermal absorption in in vitro mouse skins. The contents of hydroxy-α-sanshool， 6-gingerol， ginsenoside Rb1 were determined by high performance liquid chromatography （HPLC）， to evaluate the in vitro release and transdermal absorption of Jiaojiang cataplasms. The mobile phase of 6-gingerol and hydroxy-α-sanshool was water-acetonitrile-methanol （2∶1∶1） with the detection wavelength of 280 nm. The mobile phase of ginsenoside Rb1 was acetonitrile-0.1% phosphoric acid aqueous solution （31∶69） with the detection wavelength of 203 nm. A mouse intestinal paralysis model was established， and mice were randomly divided into five groups， namely sham operation group， model group， domperidone group （3.9 mg·kg-1） and high- and low-dose groups of Jiaojiang cataplasms （6.2， 3.1 g·kg-1， measured by crude drug dosage）， to observe the effect of this preparation on gastrointestinal propulsion function. ResultAverage release rates of hydroxy-α-sanshool， 6-gingerol and ginsenoside Rb1 at 24 h were 16.41， 4.23， 4.15 μg∙cm-2∙h-1， the average transdermal rates of them at 24 h were 2.31， 0.64， 0.29 μg∙cm-2∙h-1， their skin retention values were 19.56， 3.59， 1.61 μg， respectively. According to the Ritger-Peppas equation， the release of hydroxy-α-sanshool， 6-gingerol， ginsenoside Rb1 was non-Fick diffusion. The high-dose group of Jiaojiang cataplasms could improve intestinal function of model mice after small intestinal friction injury， and promote intestinal peristalsis and small intestinal propulsion rate （P<0.05）. ConclusionJiaojiang cataplasms has in vitro release and transdermal properties， the in vitro release conforms to Higuchi equation， and transdermal absorption behavior conforms to zero-order kinetic equation， which can improve the postoperative function of the small intestine and the propulsion function of small intestine. It preliminarily indicates that the preparation has certain clinical development value.
