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

被引：110

作者：

Carino, SR ^{[1
]}

Sperry, DC ^{[1
]}

Hawley, M ^{[1
]}

机构：

[1] Pfizer COrp, Michigan Pharmaceut Sci, Kalamazoo, MI 49001 USA

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 2006年 / 95卷 / 01期

关键词：

carbamazepine; solid forms; dissolution; bioavailability; in vitro models; solubility; solid state; thermodynamics; preformulation; polymorphs;

D O I：

10.1002/jps.20495

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2005 Wiley-Liss, Inc.

引用

页码：116 / 125

页数：10

共 18 条

[11]

KRAHN FU, 1987, PHARM ACTA HELV, V62, P247

[12] PHYSICOCHEMICAL PROPERTIES AND X-RAY STRUCTURAL STUDIES OF THE TRIGONAL POLYMORPH OF CARBAMAZEPINE [J].

LOWES, MMJ ;

CAIRA, MR ;

LOTTER, AP ;

VANDERWATT, JG .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1987, 76 (09) :744-752

[13] Characterization of dihydrates prepared from carbamazepine polymorphs [J].

McMahon, LE ;

Timmins, P ;

Williams, AC ;

York, P .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1996, 85 (10) :1064-1069

[14] The relative bioavailability and in vivo in vitro correlations for four marketed carbamazepine tablets [J].

Meyer, MC ;

Straughn, AB ;

Mhatre, RM ;

Shah, VP ;

Williams, RL ;

Lesko, LJ .

PHARMACEUTICAL RESEARCH, 1998, 15 (11) :1787-1791

[15] THE BIOINEQUIVALENCE OF CARBAMAZEPINE TABLETS WITH A HISTORY OF CLINICAL FAILURES [J].

MEYER, MC ;

STRAUGHN, AB ;

JARVI, EJ ;

WOOD, GC ;

PELSOR, FR ;

SHAH, VP .

PHARMACEUTICAL RESEARCH, 1992, 9 (12) :1612-1616

[16] Solid-state study of polymorphic drugs: carbamazepine [J].

Rustichelli, C ;

Gamberini, G ;

Ferioli, V ;

Gamberini, MC ;

Ficarra, R ;

Tommasini, S .

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2000, 23 (01) :41-54

[17] Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method [J].

Sethia, S ;

Squillante, E .

JOURNAL OF PHARMACEUTICAL SCIENCES, 2002, 91 (09) :1948-1957

[18]

SPERRY DC, 2000, AM CHEM SOC 220 ANYL

← 1 2 →