Abstract：
:The effect of the oral dosing volume (DV) on both gastric emptying and intestinal absorption was examined by analyzing the gastrointestinal disposition of a model solute, L-glucose, in rats. The amount of 14C-labeled L-glucose in the gastric and intestinal contents of sacrificed rats was measured at various times after administration, and the data were analyzed with a linear model, assuming first-order gastric emptying followed by first-order intestinal absorption. The gastric emptying rate constant (kg) rose from 0.025 to 0.072 min-1 by increasing DV from 0.1 to 3 mL/rat, whereas the intestinal absorption rate constant (ka) decreased from 0.031 to 0.015 min-1. This decrease in ka was attributed to an increase in the average intestinal lumen volume (Vav) from 24 to 39 microL/cm, assuming that the relationship ka = CLa,app/Vav holds (where CLa,app is the apparent intestinal membrane permeability clearance or the product of the apparent membrane permeability coefficient and surface area). The CLa,app (= kaVav), a measure of the in vivo intestinal membrane permeability, was 0.74 microL/cm/min for a DV value of 0.1 mL/rat and decreased only marginally by 20% for larger values of DV, suggesting an insignificant effect of DV on CLa,app. These results suggest that the accelerating effect of the increased kg, produced by the increased DV on the gastrointestinal absorption, may be canceled by the decrease in ka. A decrease in ka may lead to a decrease in the fraction absorbed. Finally, this study also provides a means for carrying out physiological modeling of drug absorption following oral administration.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Yuasa H,Numata W,Ozeki S,Watanabe Jdoi
10.1002/jps.2600840417subject
Has Abstractpub_date
1995-04-01 00:00:00pages
476-81issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49773-4journal_volume
84pub_type
杂志文章abstract：:Recently developed techniques were applied in a preformulation program to select a compound and a suitable salt for use in a one-month toxicological test. The program showed that valuable information can be obtained prior to the choice of a compound as a candidate for a solid-dosage form. Information about the physica...
journal_title：Journal of pharmaceutical sciences
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更新日期：1977-12-01 00:00:00
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更新日期：2013-05-01 00:00:00
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更新日期：2001-12-01 00:00:00
abstract：:Alzheimer's disease (AD) is historically difficult to treat, in part because of the inaccessible nature of brain pathology. Amyloid beta and tau proteins drive pathology by forming toxic oligomers that eventually deposit as insoluble amyloid plaques and neurofibrillary tangles. Recent clinical studies suggest that eff...
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740509
更新日期：1985-05-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js950304x
更新日期：1996-04-01 00:00:00
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更新日期：2000-05-01 00:00:00
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更新日期：1984-01-01 00:00:00
abstract：:Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms. This study aimed to determine the types of drugs that could adopt a stable amorphous form in SD. Twenty compounds with various melting points (70-218 degrees C), molecular weights (135-504) a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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更新日期：2007-06-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
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更新日期：2013-01-01 00:00:00
abstract：:A stability-indicating assay procedure for the determination of norethindrone on the surface of Red Delicious apple slices was developed. The apple slice is homogenized in pH 10 borate buffer solution and norethindrone is then partitioned into chloroform using a diffusion chamber that has a membrane that is permeable ...
journal_title：Journal of pharmaceutical sciences
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更新日期：1990-08-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
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更新日期：2017-08-01 00:00:00
abstract：:Intestinal transport of the type III phosphodiesterase inhibitor cilostazol was characterized to evaluate the influence of secretory transporter. Intestinal absorption of cilostazol measured by the in situ closed loop method, showed regional differences, with high permeability in the upper part of the small intestine....
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10490
更新日期：2003-11-01 00:00:00
