ChemInform Abstract: 4‐(1,3‐Dimethoxyprop‐2‐ylamino)‐2,7‐dimethyl‐8‐ (2,4‐dichlorophenyl)pyrazolo[1,5‐a]‐1,3,5‐triazine: A Potent, Orally Bioavailable CRF1 Receptor Antagonist.
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Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.Keywords:
Triazine
The health effects of flavonoids which are highly found in fruits and vegetables were mostly investigated by in vitro studies and the topics of metabolic changes and bioavailability of these compounds in humans were ignored. However, it is of great importance to provide information on the absorption, bioavailability and metabolism of flavonoids in order to evaluate their health effects. Current literature showed that the factors affecting the bioavailability of flavonoids are related with the flavonoid class, its chemical structure, and the glycoside group attached to its structure. In addition, dosage, vehicle of administration, diet, sex differences, individual genetic properties, microbial population of the colon, and other compounds present in the food material were also found to affect absorption and bioavailability. In this study, the research studies which investigated the bioavailability of flavonoids and the factors affecting it were investigated.
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Caco-2
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The absolute bioavailability of 8-methoxypsoralen in gelatin capsules and as a solution was studied in dogs. A dose of 2 mg kg-1 was given. Both for the solution and the gelatin capsules, a large variation in bioavailability was found between the different dogs. For the gelatin capsules in 1 dog out of 4 an absolute bioavailability of more than 100 per cent was found; for the solution a bioavailability of more than 100 per cent was found in all 4 dogs. Resorption was more rapid and bioavailability higher for the solution than for the gelatin capsules. Relative bioavailability of an emulsion and of a solution of 8-methoxypsoralen was studied in 2 dogs. A faster resorption and a higher bioavailability were found for the solution.
Gelatin
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Crossover study
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This chapter contains sections titled: Introduction Oral Bioavailability Definition Cassette Dosing Across-species Prediction of Bioavailability In silico Models for Estimating Human Oral Bioavailability Quantitative Structure–Activity Relationship (QSAR) Approaches Molecular Properties Influencing Bioavailability Estimation of Bioavailability from Calculated Absorption ACE Inhibitors β-Blockers Calcium Antagonists In vitro Model for Predicting Oral Bioavailability in Human and other Species In vivo Method for Estimating Human Oral Bioavailability from Animal Pharmacokinetic Studies Factors to Consider in Optimizing Oral Bioavailability
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Several factors affecting the bioavailability of 5,5-diphenylhydantoin (I) and its sodium salt (I-Na) were examined in dogs in relation to meal and following results were obtained. The bioavailability of I was not appreciably affected by the volume of coadministered water in the range of 30-120 ml. The bioavailability of I was most excellent when I was administered 0.5 h after meal. Food intake 0.5 h after drug administration enhanced appreciably the bioavailability, but that 2 h after drug administration did hardly affect the bioavailability. The extent of bioavailability of I-Na was almost 100% of the dose in the range of 100-400 mg/dog when it was administered 0.5 h after meal. While, when I-Na was administered in the fasting state, the extent of bioavailability was about 60% of the dose. Food-induced enhancement of the bioavailability of I was independent of the food constituents. The bioavailability of I was increased about 1.5-fold and 2-fold with 10-fold increase in the specific surface area of I, in the nonfasting and the fasting states, respectively. In the experiments using the dogs with the chronically implanted fistula in the common bile duct, it was found that the bile was not a major factor contributing to the food-induced enhancement of the bioavailability of I. There was a good correlation between the bioavailability of I in dog and that in man.
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The bioavailability in beagle dogs and the dissolution rates of cyclandelate from five capsule preparations commercially available in Japan were measured. One of the capsules that showed an extremely low bioavailability in humans also showed the lowest bioavailability in beagle dogs, although the difference in bioavailability with the highest preparation was smaller than in humans. A significant correlation was obtained between the results of the studies in humans and beagles. However, the power of the test using beagles was extremely low in comparison with that in the human study. Food enhanced the bioavailability of cyclandelate from the capsules having the highest and lowest bioavailability in the fasted state in beagles as observed in the human study previously. The bioinequivalence of the cyclandelate capsules detected in the fasted state disappeared in the fed state in the beagle dog study, while the bioinequivalence still remained in the non-fasted state in human subjects. Thus bioequivalence testing in the fed state led to different results in both species. The most poorly bioavailable capsule in both species in the fasted state showed a slow dissolution rate by several dissolution methods with moderate stirring. In order to obtain a good correlation with in vivo bioavailability, a large volume of test solution and addition of Tween 80 were required. Extensive growth of whiskers (needle-like crystals) was observed in the entire capsule mass having the lowest bioavailability.
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Biopharmaceutics
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