对乙酰氨基酚体外和体内释放的a/ spl β /-磷酸三钙陶瓷体系的研制

D. Mudra, K.M. Moldovan, P. K. Bajpai
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引用次数: 0

摘要

对乙酰氨基酚常被用作兽药止痛剂。常规给药方法可能导致药物水平周期性地超过和/或低于治疗水平。本研究考察了a/ spl β /-磷酸三钙陶瓷给药体系对乙酰氨基酚的体内体外释放能力。为了应对使用Tris-HCl遇到的困难,我们使用乙醇作为体外培养基。一项为期12小时和7天的研究检查了压缩负荷对陶瓷装置释放对乙酰氨基酚的影响。压缩载荷的差异不影响对乙酰氨基酚从陶瓷装置的释放谱。在一个12小时和一个4天的研究中,研究了不同剂量的对乙酰氨基酚的影响。陶瓷装置中初始载药量显著改变了对乙酰氨基酚的释放谱。一项体内研究调查了陶瓷基质装置(cmd)释放对乙酰氨基酚至少7天的能力。测试疼痛耐受水平,并测定循环镇痛水平。植入含有对乙酰氨基酚的陶瓷装置的动物表现出明显更高的循环镇痛水平和疼痛耐受性。这些研究表明,通过a/ spl β /-磷酸三钙陶瓷装置在体外和体内都可以有效地递送对乙酰氨基酚。
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Development of a /spl beta/-tricalcium phosphate ceramic system for in vitro and in vivo release of acetaminophen
Acetaminophen is often used as a veterinary analgesic. Conventional methods of drug administration may lead to drug levels that periodically exceed and/or fall below therapeutic levels. This study investigated the ability of a /spl beta/-tricalcium phosphate ceramic delivery system to release acetaminophen in vitro and in vivo. In response to difficulties experienced with the use of Tris-HCl, ethanol was used as the in vitro media. One 12 hour and one seven day study examined the effects of compression load on the acetaminophen release profile from the ceramic device. Differences in compression loads did not affect the release profiles of acetaminophen from the ceramic device. The effects of different acetaminophen dosages were investigated in one 12 hour and one four day study. The initial amount of drug loaded in the ceramic device significantly changed release profiles of acetaminophen. An in vivo study investigated the ability of the ceramic matrix devices (CMDs) to release acetaminophen for a minimum of seven days. Pain tolerance levels were tested and circulating analgesic levels were determined. Animals implanted with ceramic devices containing acetaminophen displayed significantly higher levels of circulating analgesic and pain tolerance. These studies suggest that it is possible to effectively deliver acetaminophen by means of a /spl beta/-tricalcium phosphate ceramic device, both in vitro and in vivo.
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