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Development of a new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastro-intestinal tract.

Abstract：

:A new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastro-intestinal tract was developed. In this new system, a drug (solid form) is added into a drug-dissolving vessel (pH 1.0) and the dissolved drug is transferred to a pH adjustment vessel (pH 6.0). Then the drug solution is transferred to the apical surface of Caco-2 cells, and the permeation rate of the drug across a Caco-2 monolayer is determined. This system was able to predict the oral absorption ratios of ten water-soluble drugs in humans. Using this system, it was predicted that drugs that permeated Caco-2 at a rate of more than 0.1% of the dose in 200 min would be almost completely absorbed after oral administration in humans. For a drug whose permeation ratio was less than 0.03%, the absorption ratio was predicted to be less than 30%. This system also enabled prediction of the absorption rate and variability in the absorption of albendazole, a drug with poor water solubility. It also enabled assessment of the improvement in absorption using a solid dispersion of albendazole-polymers that improved the water solubility. The results suggest that this system is useful for oral absorption screening of new drugs and pharmaceutical products.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Kobayashi M,Sada N,Sugawara M,Iseki K,Miyazaki K

doi

10.1016/s0378-5173(01)00663-9

keywords:

subject

Has Abstract

pub_date

2001-06-19 00:00:00

pages

87-94

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378517301006639

journal_volume

221

pub_type

杂志文章

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