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用于持续递送香豆素的羟基磷灰石陶瓷基质的研发。

Development of a hydroxyapatite ceramic matrix for the continuous delivery of coumadin.

作者信息

Mileti I F, Bajpai P K

机构信息

University of Dayton, Ohio 45469-2320, USA.

出版信息

Biomed Sci Instrum. 1995;31:177-82.

PMID:7654958
Abstract

Coumadin [Warfarin Sodium, 3-(alpha-Acytonylbenzyl-4-hydroxy coumarin)] has been associated with severe side affects such as excessive hemorrhaging and necrosis when given in dosages to maintain the plasma concentration above the effective threshold level. Periodic administration of drugs induces large, fluctuating concentrations in the body A ceramic drug delivery system (CDDS) consisting of hydroxyapatite resorbable ceramic matrix (HA) and coumadin could release coumadin in a sustained manner. Thus, the dosage of coumadin could be decreased while maintaining an effective threshold level of the drug. In this investigation, a hydroxyapatite ceramic delivery system was developed to continuously release coumadin. Data obtained in this investigation suggest that ceramic-coumadin devices compressed at loads of 9000 pounds with cysteine as a binder could deliver coumadin continuously for several days.

摘要

香豆素(华法林钠,3-(α-丙酮基苄基)-4-羟基香豆素)在给予维持血浆浓度高于有效阈值水平的剂量时,会出现严重的副作用,如过度出血和坏死。定期给药会在体内引起浓度大幅波动。一种由羟基磷灰石可吸收陶瓷基质(HA)和香豆素组成的陶瓷药物递送系统(CDDS)能够持续释放香豆素。因此,在维持药物有效阈值水平的同时,可以减少香豆素的剂量。在本研究中,开发了一种羟基磷灰石陶瓷递送系统来持续释放香豆素。本研究获得的数据表明,以半胱氨酸作为粘合剂在9000磅压力下压制的陶瓷-香豆素装置能够连续数天递送香豆素。

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