A composite nanocarrier to inhibit precipitation of the weakly basic drug in the gastrointestinal tract

Autor: Chunli Zheng, Yun Li, Zhen Peng, Xinyi He, Juan Tao, Liang Ge, Yixin Sun, Yunkai Wu
Jazyk: angličtina
Rok vydání: 2020
Předmět:
Zdroj: Drug Delivery, Vol 27, Iss 1, Pp 712-722 (2020)
Druh dokumentu: article
ISSN: 1071-7544
1521-0464
10717544
DOI: 10.1080/10717544.2020.1760402
Popis: For weakly basic drugs, the sharp decrease of drug solubility and the following drug precipitation after drugs transferring from the gastric fluid to the intestinal fluid in the gastrointestinal (GI) tract is a main reason for the poor oral bioavailability of drugs. Here, an anticoagulant dabigatran etexilate (DE) was used as a model drug, and a composite nanocarrier system of DE was developed to improve the drug dissolution by decreasing the drug leakage in the stomach and inhibiting the drug precipitation in the intestinal tract. With the encapsulation of drugs in nanocarriers, the precipitation percentage of DE in composite nanocarriers was 22.25 ± 3.88% in simulated intestinal fluid, which was far below that of the commercial formulation. Moreover, the relative bioavailability of DE-loaded composite nanocarriers (456.58%) was greatly enhanced and the peak of its activated partial thromboplastin time was also significantly prolonged (p
Databáze: Directory of Open Access Journals
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