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舌下硝酸甘油。II. 耐绞宁片和硝酸异山梨酯片的体外和体内生物利用度。

Sublingual nitroglycerin. II. In vitro and in vivo availability of Nitrostat and Nitrobaat tablets.

作者信息

Lagas M, Duchateau A M

机构信息

Laboratory for Pharmaceutical Research, Roden, The Netherlands.

出版信息

Pharm Weekbl Sci. 1988 Dec 9;10(6):254-8. doi: 10.1007/BF02219664.

Abstract

The in vitro and in vivo availability of nitroglycerin from three compressed and one stabilized molded tablet have been studied. Compressed nitroglycerin tablets have to disintegrate before the drug is released. The disintegration and release of nitroglycerin from these tablets appeared to be strongly dependent upon conditions in the in vitro dissolution tests, such as the degree of agitation, and in vivo factors, such as tongue pressure and/or movement. The stabilized molded nitroglycerin tablet did not disintegrate but dissolved completely. Because the dissolution of the molded tablet was fast, the release rate of nitroglycerin was far less influenced by the in vitro and in vivo factors described above. The potency and in vitro and in vivo availability of fresh tablets and tablets which had been stored in tightly closed glass containers for over one year did not differ significantly. It is conjectured that the supposed potency loss of properly stored compressed nitroglycerin tablets is rather a release problem than a stability problem.

摘要

对三种压制片和一种稳定化模制片中硝酸甘油的体外和体内可用性进行了研究。压制的硝酸甘油片在药物释放前必须崩解。硝酸甘油从这些片剂中的崩解和释放似乎强烈依赖于体外溶出试验的条件,如搅拌程度,以及体内因素,如舌压和/或运动。稳定化模制硝酸甘油片不会崩解而是完全溶解。由于模制片的溶解很快,硝酸甘油的释放速率受上述体外和体内因素的影响要小得多。新鲜片剂以及在密闭玻璃容器中储存一年以上的片剂的效力、体外和体内可用性没有显著差异。据推测,妥善储存的压制硝酸甘油片所谓的效力损失与其说是稳定性问题,不如说是释放问题。

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