NDLI: Effect of Crystal Size on the In Vitro Dissolution and Oral Absorption of Nitrendipine in Rats

Content Provider	Springer Nature Link
Author	Xia, Dengning Cui, Fude Piao, Hongze Cun, Dongmei Piao, Hongyu Jiang, Yanbo Ouyang, Mei Quan, Peng
Copyright Year	2010
Abstract	To investigate the effect of crystal size on the dissolution and oral absorption of nitrendipine, a poorly soluble drug, in rats.Five types of nitrendipine crystal suspensions with different particle sizes (200 nm, 620 nm, 2.7 μm, 4.1 μm, 20.2 μm) were prepared either by the precipitation-ultrasonication or the anti-solvent precipitation method. The simulated intestinal fluid in the fasted state (FaSSIF) was selected as the dissolution medium, and the dissolution behaviors of different nitrendipine crystals were simulated based on a Noyes-Whitney type equation. The in vivo absorption and the absolute bioavailability of the different nitrendipine crystals were evaluated in Wistar rats.The dissolution rate of nitrendipine was significantly increased by a reduction in particle size. The dissolution test in FaSSIF could discriminate between the differences in the dissolution rates of the different particle sizes, and the simulated results were in agreement with the observed dissolution curves. From the simulated T$_{50%}$ values (50% dissolution time), the dissolution rates of crystals with particle sizes of 200 nm, 620 nm, 2.7 μm, 4.1 μm and 20.2 μm were calculated to be 5.1 × 10$^{4}$, 1.0 × 10$^{4}$, 237, 64 and 11-fold greater than that of the raw crystals and resulted in absolute bioavailability of 61.4% 51.5%, 29.4%, 26.7%, 24.7%, respectively. The reduction in the drug particle size correlated well with incremental improvements in oral absorption. A good linear relationship was observed between the Log (T$_{50%}$) and the absolute bioavailability of nitrendipine.The dissolution rate and the oral bioavailability of nitrendipine were significantly affected by the crystal size, and the oral bioavailability could be improved significantly by preparing it as nanocrystals. FaSSIF can be used to predict differences in oral absorption of crystals with different particle sizes.
Starting Page	1965
Ending Page	1976
Page Count	12
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	27
Issue Number	9
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2010-06-29
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Biomedical Engineering Medical Law Biochemistry Pharmacy Pharmacology/Toxicology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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