Preparation of enteric microsphere of oleanolic acid dihemiphthalate sodium by salting-out action using spherical crystallization technique
- VernacularTitle:利用球晶造粒技术盐析方法制备齐酞酸钠肠溶微球
- Author:
Yuling FAN
;
Fude CUI
;
Mingshi YANG
;
Yubin JI
- Publication Type:Journal Article
- Keywords:
oleanolic acid dihemiphthalate sodium;
enteric microsphere;
spherical crystallization technique;
salting-out action
- From:
Acta Pharmaceutica Sinica
2005;40(3):267-273
- CountryChina
- Language:Chinese
-
Abstract:
Aim Enteric microspheres were prepared to prevent the interaction of drug with gastric acid and to improve its bioavailability. Methods The enteric microspheres with a matrix structure were successfully produced using a spherical crystallization technique. Hydroxypropyl methylcellulose phthalate ( HP-55 ), an enteric material, was coprecipitated with the drug by salting-out effect during the preparation process. A mixture of water and ethanol was chosen as a good solvent and dichloromethane was used as a the first time to prepare microspheres by making the water-soluble drug and water-insoluble excipient coprecipitated. In vivo test demonstrated that the drug absorption from the enteric oleanolic acid dihemiphthalate sodium (OADHPS) microspheres was significantly prolonged compared to that with OADHPS powder after a lag-time. Furthermore, the drug bioavailability was 181.6% greater than that with the OADHPS powder. Conclusion The microspheres of water soluble drug could be prepared by using water phase replacing organic phase as poor solvent which decrease the quantity of organic solvent and benefit the environment prevention.
