中国组织工程研究与临床康复2009，Vol.13Issue(12)：2395-2400,6.DOI:10.3969/j.issn.1673-8225.2009.12.045
氟尿嘧啶植入剂在蛋白变性剂盐酸中的释药行为
Drug-release effect of fluorouracil implants in protein denaturant hydrochloric acid
摘要
Abstract
BACKGROUND: Directly percutaneous injection of protein-denaturant hydrochloric acid (PDHA) into tumors can lead to fast killing of tumor, sustained drug release and prevention of in situ recurrence of tumor. However, whether implants can be used combined with denaturant still remains unknown. OBJECTIVE: To investigate the compatibility of fluorouracil implants and PDHA (6 mol/L). DESIGN, TIME AND SETTING: Observational study was performed in the Hefei Industry University between October 2006 and March 2007. MATERIALS: A total of 78 Wistar rats, weighing (200i20) g, half males and half females, were used for testing drug release in vivo. Drugs fluorouracil implants (H20030345; columniform particle, diameter 0.8 mm, length 4 mm; specifications: Fluorouracil 2 mg/particle; batch number: 20060922; meeting the National Drug Quality Standards [WS1-(X-103)-2005Z]) were provided by Wuhu Zhongren Pharmaceutical Company,Ltd. Hydrochloric acid (37%) was analytical reagent. METHODS: 96 tubes of the implants and PDHA were kept at (37.0± 0.5) ℃. Each time, six samples were collected at 1, 8, 16, 24, 96, 120, 168, 240, 360, 432, 480, 528, 600, 720, and 960 hours after incubation. Appearance of the implants was observed by microscope. Stability of fluorouracil in PDHA was determined by HPLC and ultraviolet absorb method. Based on the entering quantity and residual quantity of fluorouracil, the release rates were calculated. MAIN OUTCOME MEASURES: The approximate solubility, stability and morphological change of fluorouracil in denaturant and the corresponding drug release character in both denaturant and rats in vivo. RESULTS: At (37.0±0,5) ℃, the fluorouracil was stable for 960 hours in PDHA, the saturated concentration of fluorouracil was (22.72±0.04) g/L. The appearance of implants was intact. The surface was porous. Compared with the speed of releasing drug in rats, the speed of releasing drug was faster in the early stage of release process and slower in the later stage. The drug release was incomplete. At 1, 24, 96, 360 and 960 hours, the implants' release rates were (11.9±6.7)%, (37.9±5.3)%, (52.6±4.5)%, (75.3±3.8)%, and (85.5±2.1)%, respectively. CONCLUSION: The fluorouracil implants and hydrochloric acid (6 mol/L) are compatible and no influence is detected during the observation.关键词
氟尿嘧啶/植入剂/变性剂/盐酸/缓释/化疗分类
医药卫生引用本文复制引用
王世亮,王竞,尹情胜,任翠丽,马晓芹,冯梅..氟尿嘧啶植入剂在蛋白变性剂盐酸中的释药行为[J].中国组织工程研究与临床康复,2009,13(12):2395-2400,6.基金项目
国家自然科学基金资助项目(国科基字(2001151号) （国科基字(2001151号）
安徽省"十五"科技攻关计划(01013036) （01013036）
Supported by: the National Natural Science Basic Research Foundation of China, No. [200115] （）
the Tenth Five-Year Plan Science and Technology Research Plan of Anhui Province, No. 01013036 （）
