دورية أكاديمية
[Validation of in situ single pass perfusion model based on P-gp].
العنوان: | [Validation of in situ single pass perfusion model based on P-gp]. |
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المؤلفون: | Dong YL; Beijing University of Chinese Medicine, Beijing 100102, China., Liu Y; Beijing University of Chinese Medicine, Beijing 100102, China., Yin XW; Beijing University of Chinese Medicine, Beijing 100102, China., Pan M; Beijing University of Chinese Medicine, Beijing 100102, China., Li XL; Beijing University of Chinese Medicine, Beijing 100102, China., Wang ZY; Beijing University of Chinese Medicine, Beijing 100102, China., Dong L; Beijing University of Chinese Medicine, Beijing 100102, China. |
المصدر: | Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica [Zhongguo Zhong Yao Za Zhi] 2017 Apr; Vol. 42 (8), pp. 1539-1544. |
نوع المنشور: | Journal Article; Validation Study |
اللغة: | Chinese |
بيانات الدورية: | Publisher: Zhongguo yao xue hui : Zhongguo Zhong yi yan jiu yuan Zhong yao yan jiu suo Country of Publication: China NLM ID: 8913656 Publication Model: Print Cited Medium: Print ISSN: 1001-5302 (Print) Linking ISSN: 10015302 NLM ISO Abbreviation: Zhongguo Zhong Yao Za Zhi Subsets: MEDLINE |
أسماء مطبوعة: | Publication: Beijing : Zhongguo yao xue hui : Zhongguo Zhong yi yan jiu yuan Zhong yao yan jiu suo Original Publication: [Beijing] : Zhongguo yao xue hui : [Zhongguo Zhong yi yan jiu yuan Zhong yao yan jiu suo, 1989- |
مواضيع طبية MeSH: | Intestinal Absorption* , Perfusion*, ATP Binding Cassette Transporter, Subfamily B, Member 1/*metabolism , Digoxin/*pharmacokinetics , Verapamil/*pharmacokinetics, Animals ; Ileum/drug effects ; Rats |
مستخلص: | To validate in situ rats intestinal single pass perfusion model based on P-glycoprotein (P-gp). Firstly, phenol red perfusion was carried out to verify the close connection structure of intestinal epithelial cells, and the integrity of the intestinal epithelium, with a gravimetric method for correcting water flux. The level of phenol red was determined by high performance liquid chromatography (HPLC) both before and after perfusion. Secondly, the positive drug digoxin specified by FDA was used to validate the model. After different mass concentrations of verapamil were given in the rats, the absorption parameters of digoxin in ileum of rats were observed and compared. The results showed that the phenol red was absorbed in rats ileum segment, with an effective permeability coefficient of (1.09±0.62)×10 ⁻⁶ cm•s ⁻¹. The experiment results indicated that the close connection structure of intestinal epithelial cells was normal, and the integrity of the intestinal epithelium was maintained well. In digoxin perfusion experiment, in case no verapamil was given, digoxin showed certain degree of absorption in rat ileum, with an effective permeability coefficient (Peff) of (1.07±0.59)×10 ⁻⁵ cm•s ⁻¹; after mass concentrations of 0.01,0.1 mmol•L ⁻¹ verapamil were given, the absorption of digoxin was on the rise in rat ileum, with an effective permeability coefficient Peff of (1.58±0.69)×10 ⁻⁵, (3.28±0.95)×10 ⁻⁵ cm•s ⁻¹ respectively (P<0.05). Digoxin perfusion experiment verified that P-gp expression in small intestine epithelium was intact and can be used in the research of P-gp efflux transporter. Competing Interests: The authors of this article and the planning committee members and staff have no relevant financial relationships with commercial interests to disclose. (Copyright© by the Chinese Pharmaceutical Association.) |
فهرسة مساهمة: | Keywords: P-gp; digoxin; in situ rat intestinal perfusion; phenol red |
المشرفين على المادة: | 0 (ATP Binding Cassette Transporter, Subfamily B, Member 1) 73K4184T59 (Digoxin) CJ0O37KU29 (Verapamil) |
تواريخ الأحداث: | Date Created: 20171027 Date Completed: 20180625 Latest Revision: 20191210 |
رمز التحديث: | 20240628 |
DOI: | 10.19540/j.cnki.cjcmm.20170223.007 |
PMID: | 29071859 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1001-5302 |
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DOI: | 10.19540/j.cnki.cjcmm.20170223.007 |