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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.
RESUMEN
Objective: To prepare the new diclofenac potassium cataplasms, establish a quality research method and evaluate the preparation quality by the established method. Methods: A high performance liquid chromatography(HPLC)was performed on an ODS column(the column temperature 35℃)using the methanol-4% glacial acetic acid solution(80: 20, V/V)as mobile phase, and the detection wavelength was set at 276 nm. Diclofenac potassium was extracted with methanol, and the adhesion, content and uniformity of potassium diclofenac were measured. The release of diclofenac potassium from the cataplasms was determined in accordance with the fourth method of the XD release methods in the Appendix of the Chinese Pharmacopoeia. Results: The average maximum number of steel ball stuck in the cataplasms in the initial adhesion test was No. 6. Under the HPLC conditions, potassium diclofenac showed good linearity within the concentration range of 400-800 μg/ml, with the average sample recovery rate 1.33 % and RSD< 1.93%(n=6). The methodological studies for the drug release test for the diclofenac potassium cataplasms showed that the diclofenac potassium showed a good linearity within the range of 1-50 μg/ml in the drug release test, and the precision and recovery well satisfied the requirements of Pharmacopoeia. The content uniformity of the cataplasms was in accordance with the Pharmacopoeia. The release amounts of the cataplasms in 2, 5 and 8 hours were 20%-45%, 40%-80% and more than 70% of the labeled amount, respectively, and the release curve followed the first-order release equation. Conclusion: The established HPLC method is sensitive, accurate, easily operable and reproducible, which could be used for the quality control of diclofenac potassium cataplasms. The prepared diclofenac potassium cataplasms were of uniform content and showed characteristics of the sustained release, which is expected to be developed to a new preparation of diclofenac potassium.
RESUMEN
Objective:To investigate the stability of Liuwei Qiangu cataplasms. Methods:The active ingredient( naringin) in the samples was determined by HPLC. Meanwhile, the other indices including character, identification, ointment content, adhesion, mi-crobial limit and so on were detected as well. Results:The results of the accelerated test and long term test showed that Liuwei Qiangu cataplasms were stable. No significant change in each index was found before and after the tests. Conclusion: Liuwei Qiangu cata-plasms are stable at room temperature. The designs of preparation process and package are rational to keep the stability of the prepara-tion.