Pharmacokinetics of oral amlodipine orotate in vagotomized dogs
| Autor: | Hyun Hee Kwak, Han K. Chung, Seul Min Choi, Joo H. Lee, Myung Gyoon Lee, Jong W. Kwon, Jong O. Kim, Moohi Yoo, Jung H. Kim |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
Male
medicine.medical_specialty Time Factors Metabolic Clearance Rate medicine.medical_treatment Gastric motility Administration Oral Pharmaceutical Science Vagotomy Pharmacology Mass Spectrometry Intestinal absorption Dogs Pharmacokinetics Oral administration Internal medicine medicine Animals Pharmacology (medical) Amlodipine Chromatography High Pressure Liquid business.industry Stomach General Medicine Hydrogen-Ion Concentration Calcium Channel Blockers Endocrinology medicine.anatomical_structure Intestinal Absorption Solubility Area Under Curve Models Animal Gastric acid Gastrointestinal Motility business Tablets medicine.drug |
| Zdroj: | Biopharmaceutics & Drug Disposition. 27:141-145 |
| ISSN: | 1099-081X 0142-2782 |
| DOI: | 10.1002/bdd.495 |
| Popis: | It was reported that gastric motility was delayed and gastric acid secretion was reduced in vagotomized dogs which mimics a low gastric acidity in humans. A delay in gastric motility causes long residence of amlodipine in the stomach. More unionized fractions of amlodipine could exist in less acidic conditions of gastrointestinal fluids, since amlodipine is a weak basic drug with pKa of 8.7. Hence, gastrointestinal absorption of amlodipine is expected to be enhanced and the time to reach a peak plasma concentration of amlodipine (Tmax) is faster in vagotomized dogs. This was proven after oral administration of an amlodipine orotate tablet at a dose of 5 mg as amlodipine in vagotomized dogs. For example, in vagotomized dogs, the total area under the plasma concentration-time curve from time zero to the last measured time, 48 h, in plasma (AUC(0-48 h)) was significantly greater (725 versus 348 ng h/ml) and Tmax was significantly shorter (1.50 versus 5.00 h) than those in dogs without vagotomy. |
| Databáze: | OpenAIRE |
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