Relative bioavailability estimation of carbamazepine crystal forms using an artificial stomach-duodenum model

• Published in: Journal of pharmaceutical sciences Vol. 95; no. 1; pp. 116 - 125
• Main Authors: Carino, Stephen R., Sperry, David C., Hawley, Michael
• Format: Journal Article
• Language: English
• Published: Hoboken Elsevier Inc 01.01.2006; Wiley Subscription Services, Inc., A Wiley Company; Wiley; American Pharmaceutical Association
• Subjects: Animals; bioavailability; Biological and medical sciences; Biological Availability; carbamazepine; Carbamazepine - analysis; Carbamazepine - chemistry; Carbamazepine - pharmacokinetics; Crystallization; dissolution; Dogs; Duodenum - metabolism; Fasting; General pharmacology; in vitro models; Medical sciences; Models, Biological; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; polymorphs; preformulation; solid forms; solid state; Solubility; Stomach - metabolism; thermodynamics; solid forms; bioavailability; in vitro models; dissolution; polymorphs; thermodynamics; solubility; preformulation; carbamazepine; solid state; Stomach; Crystal form; Pharmaceutical technology; Solubility; Anticonvulsant; Bioavailability; Tricyclic compound; Dissolution; In vitro; Carbamazepine; Solid state; Thermodynamics; Mood stabilizer; Dosage form; Solid form; Pharmacokinetics; Physicochemical properties; Polymorphism
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.20495

The in vitro dissolution of carbamazepine (CBZ) was investigated using an automated artificial stomach-duodenum (ASD) model. Successful simulation of the dog physiology in the fasted state showed that the rank order of the ASD estimated bioavailabilities is as follows: Form III>Form I>dihydrate. This result is in excellent agreement with those found in literature. Additional simulations comparing different gastric transit times during fasted and fed states are also discussed. © 2005 Wiley-Liss, Inc. and the American Pharmacists Association