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文献信息

Octenylsuccinate hydroxypropyl phytoglycogen, a dendrimer-like biopolymer, solubilizes poorly water-soluble active pharmaceutical ingredients

期刊名:Carbohydrate Polymers
文献编号:
文献地址: http://www.sciencedirect.com/science/article/pii/S0144861717311505
发表日期:3 October 2017
Effective solubilizers for poorly water-soluble active pharmaceutical ingredients (APIs) are highly desirable. This study introduced an amphiphilic dendrimer-like biopolymer, octenylsuccinate hydroxypropyl phytoglycogen (OHPP) as a new solubilizer. The molar substitution degree of octenylsuccinate and hydroxypropyl groups of OHPP was 0.51 and 1.69, respectively. The weight-average molecular weight, Z-average root mean square radius, and Zeta-potential of OHPP were 1.507 × 107 g/mol, 22.6 nm, and ?23.6 mV, respectively. OHPP was highly soluble in polar organic solvents and aqueous buffers with pH ≥ 5.0. To evaluate its solubilization capability, each of five APIs (celecoxib, docetaxel, fenofibrate, griseofulvin, and resveratrol) was incorporated with OHPP to form solid dispersions (API-OHPP SD). API-OHPP SD reduced API crystallinity and increased API solubility by up to 1,755 times. Over the 3 h dissolution, the cumulative dissolved API with API-OHPP SD was in the range of 6.8 ~ 84.9%. Evidently, OHPP was a potent and non-specific polymeric solubilizer of poorly water-soluble APIs.



... St. Louis, MO). Resveratrol was obtained from TCI America (USA). Docetaxel was purchased from Chengdu Biopurify Phytochemicals Ltd. (China). Celecoxib was
purchased from Hangzhou dayangchem Co., Ltd. (China). Hypromellose ...
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