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A microemulsion of puerarin-phospholipid complex for improving bioavailability: preparation, in vitro and in vivo evaluations.
Wu, Jun-Yong; Li, Yong-Jiang; Han, Meng; Hu, Xiong-Bin; Yang, Le; Wang, Jie-Min; Xiang, Da-Xiong.
Afiliación
  • Wu JY; a Department of Pharmacy , the Second Xiangya Hospital, Central South University , Changsha , Hunan , China.
  • Li YJ; b Key Laboratory of Traditional Chinese Medicine Preparations of Hunan Province , the Second Xiangya Hospital, Central South University , Changsha , Hunan , China.
  • Han M; c Hunan Provincial Engineering Research Center of Translational Medicine and Innovative Drug , Changsha , Hunan , China.
  • Hu XB; a Department of Pharmacy , the Second Xiangya Hospital, Central South University , Changsha , Hunan , China.
  • Yang L; b Key Laboratory of Traditional Chinese Medicine Preparations of Hunan Province , the Second Xiangya Hospital, Central South University , Changsha , Hunan , China.
  • Wang JM; c Hunan Provincial Engineering Research Center of Translational Medicine and Innovative Drug , Changsha , Hunan , China.
  • Xiang DX; a Department of Pharmacy , the Second Xiangya Hospital, Central South University , Changsha , Hunan , China.
Drug Dev Ind Pharm ; 44(8): 1336-1341, 2018 Aug.
Article en En | MEDLINE | ID: mdl-29513046
Puerarin is a phytochemical with various pharmacological effects, but poor water solubility and low oral bioavailability limited usage of puerarin. The purpose of this study was to develop a new microemulsion (ME) based on phospholipid complex technique to improve the oral bioavailability of puerarin. Puerarin phospholipid complex (PPC) was prepared by a solvent evaporation method and was characterized by X-ray diffraction and infrared spectroscopy. Pseudo-ternary phase diagrams were constructed to investigate the effects of different oil on the emulsifying performance of the blank ME. Intestinal mucosal injury test was conducted to evaluate safety of PPC-ME, and no sign of damage on duodenum, jejunum and ileum of rats was observed using hematoxylin-eosin staining. In pharmacokinetic study of PPC-ME, a significantly greater Cmax (1.33 µg/mL) was observed when compared to puerarin (Cmax 0.55 µg/mL) or PPC (Cmax 0.70 µg/mL); the relative oral bioavailability of PPC-ME was 3.16-fold higher than puerarin. In conclusion, the ME combined with the phospholipid complex technique was a promising strategy to enhance the oral bioavailability of puerarin.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fosfolípidos / Vasodilatadores / Portadores de Fármacos / Composición de Medicamentos / Isoflavonas Tipo de estudio: Evaluation_studies Límite: Animals Idioma: En Revista: Drug Dev Ind Pharm Año: 2018 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fosfolípidos / Vasodilatadores / Portadores de Fármacos / Composición de Medicamentos / Isoflavonas Tipo de estudio: Evaluation_studies Límite: Animals Idioma: En Revista: Drug Dev Ind Pharm Año: 2018 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido