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Bioadhesive pellets of astragalosides: preparation and adhesive evaluation based on the physical properties of wet mass / 药学学报
Acta Pharmaceutica Sinica ; (12): 2093-2099, 2019.
Article in Chinese | WPRIM | ID: wpr-780301
ABSTRACT
Bioadhesive preparation can be attached to specific sites to control drug release rate, increase drug concentration and increase efficacy, which is based on natural or synthetic polymer material. In this paper, based on the physical properties of wet mass, a method for screening adhesion formulation was proposed, which was different from conventional way of screening optimal formulation, and astragalosides loaded bioadhesive pellets were prepared by extrusion-spheronization method (extrusion speed 30 r·min-1, spheronization speed 808 r·min-1, spheronization time 7.5 min) based on this formulation screening method, small living animal imaging technology and mucin from porcine stomach model were used to evaluate the in vivo and invitro adhesiveness behaviour of the pellets. According to the relationship between the physical properties of wet mass and the formability and adhesiveness of bioadhesive pellets, five key physical properties hardness (Ha), adhesiveness (Ad), springiness (Sp), cohesiveness (Co), chewiness (Ch) were selected as the index of screening optimal formulation, therefore a comprehensive evaluation model was established, which based on principal component analysis, to did digital ranking for these proposed adhesion formulation, the optimal formulation was determined microcrystalline cellulose (chitosan∶Carbomer 940 = 2∶1), the adhesive material dosage accounted for 20% of the excipient dosage, and the ratio of drugs to excipients was 1 4. All animal experiments have been approved by Ethics Committee of Shanghai University of Traditional Chinese Medicine. The in vivo and in vitro adhesive evaluation results showed the pellets had a clear advantage in intestinal adhesion over normal pellets, its also proved the scientificity and reliability of the method of screening bioadhesive formulation.

Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2019 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2019 Type: Article