Channeling agent and drug release from a central core matrix tablet

Channeling agent and drug release from a central core matrix tablet
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DOI:
10.1081/ddc-100104319
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发表时间:
2001-01-01
影响因子:
3.4
通讯作者:
Rabasco, AM
Rabasco, AM
中科院分区:
医学4区
文献类型:
--
作者:
González-Rodríguez, ML;Pérez-Martínez, JI;Rabasco, AM

文献摘要

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本发明描述了一种在预定的滞后时间后控制和完全释放药物的新的口服剂型。该系统设计用于利用相对恒定的小肠通过时间,由包被有聚合物基质的含药核心组成,所述聚合物基质由通道形成剂(NaCl、甘露醇和Emdex)和惰性聚合物(Eudragit RS 100)形成。滞后时间被认为是依赖于类型和所使用的通道物质的粒度。此外,二元镜像(通道物质-聚合物)的流变特性也会影响滞后时间。另一方面,发现释放动力学受赋形剂类型和粒度的显著影响。从体外溶出试验中获得的结果表明,该装置可能用于以可控速率口服给药,最多每天给药一次。
A new oral dosage form for controlled and complete release of drug after a predetermined lag time is described. The system designed to exploit the relatively constant small intestine transit rime, consists of a drug-containing core coated with a polymeric matrix formed by a channeling agent (NaCl, mannitol, and Emdex) and an inert polymer (Eudragit RS100). The lag time was found to be dependent on type and particle size of the channeling substances used. Also, rheological properties of the binary mirtures (channeling substance-polymer) can affect the lag time periods. On the other hand the release kinetics were found to be influenced significantly by excipient type and particle size. Results obtained from in vitro dissolution testing demonstrated that this device potentially could be used to deliver drugs orally for up to once-a-day dosing at controllable rates.