Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2485099 | Journal of Pharmaceutical Sciences | 2010 | 10 Pages |
Abstract
The purpose of this work was to investigate feasibility of a promising topical drug delivery system (TDDS) for sinomenine hydrochloride (SMH), extracted from the Chinese medicinal plant sinomenine acutum and currently used for the treatment of rheumatoid arthritis. It was found that SMH was a weak base (pKa, 7.98â±â0.04) with pHâdependent solubility and partition coefficient. The result of in vitro permeation studies demonstrated that the permeation enhancer azone was the most effective. In contrast, spray had higher accumulative permeated amounts of SMH than patch, but permeated duration of spray was shorter than that of patch. The efficacy on Freund's complete adjuvantâinduced arthritis suggested that there was near arthritis index for SMH spray with medium dose (i.e., 15âmg/rat) and oral solution at a dose of 12âmg/rat, indicating that topical SMH delivery system could achieve the similar antiâinflammatory efficacy with oral administration. Pharmacokinetic parameters including Cmax and AUC for both topical preparations were lower than those for oral preparation, which hinted that systemic side effect could be ignored. Therefore, the spray and patch were promising formulations for successful topical delivery of SMH through the skin instead of oral administration with side effects. © 2009 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 99: 1790-1799, 2010
Keywords
Related Topics
Health Sciences
Pharmacology, Toxicology and Pharmaceutical Science
Drug Discovery
Authors
Xinru Li, Xiaoyan Li, Yanxia Zhou, Yan Liu, Ming Guo, Qingfen Zhu, Yuanchao Xie, Zhiyun Fan,