Determination of aqueous solubility by heating and equilibration:: A technical note

被引：79

作者：

Loftsson, T ^{[1
]}

Hreinsdóttir, D ^{[1
]}

机构：

[1] Univ Iceland, Fac Pharm, IS-107 Reykjavik, Iceland

来源：

AAPS PHARMSCITECH | 2006年 / 7卷 / 01期

关键词：

solubility; solubility determination; shake-flask method;

D O I：

10.1208/pt070104

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A modified shake-flask solubility method, where the equilibration time was shortened through heating, was used to determine the solubility of 48 different drugs and pharmaceutical excipients in pure water at room temperature. The heating process accelerates dissolution of the solid compound and frequently results in supersaturated solution. Seeding with the solid compound after heating and cooling to room temperature promotes precipitation of the solid compound in its original stable form. This modified shake-flask method generates and reproducible and reproducible solubility data. Copyright ©2003. All Rights Reserved.

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页数：4

相关论文

共 22 条

[1]

Amidon G. L., 1986, CHEM STABILITY PHARM

[2] A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY [J].

AMIDON, GL ;

LENNERNAS, H ;

SHAH, VP ;

CRISON, JR .

PHARMACEUTICAL RESEARCH, 1995, 12 (03) :413-420

[3] In silico predictions of drug solubility and permeability:: Two rate-limiting barriers to oral drug absorption [J].

Bergström, CAS .

BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY, 2005, 96 (03) :156-161

[4] Accuracy of calculated pH-dependent aqueous drug solubility [J].

Bergström, CAS ;

Luthman, K ;

Artursson, P .

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2004, 22 (05) :387-398

[5] Experimental and computational screening models for prediction of aqueous drug solubility [J].

Bergström, CAS ;

Norinder, U ;

Luthman, K ;

Artursson, P .

PHARMACEUTICAL RESEARCH, 2002, 19 (02) :182-188

[6] Miniature device for aqueous and non-aqueous solubility measurements during drug discovery [J].

Chen, XQ ;

Venkatesh, S .

PHARMACEUTICAL RESEARCH, 2004, 21 (10) :1758-1761

[7] Automated robotic liquid handling/laser-based nephelometry system for high throughput measurement of kinetic aqueous solubility [J].

Dehring, KA ;

Workman, HL ;

Miller, KD ;

Mandagere, A ;

Poole, SK .

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2004, 36 (03) :447-456

[8] Predicting aqueous solubility from structure [J].

Delaney, JS .

DRUG DISCOVERY TODAY, 2005, 10 (04) :289-295

[9] Comparison of a miniaturized shake-flask solubility method with automated potentiometric acid/base titrations and calculated solubilities [J].

Glomme, A ;

März, J ;

Dressman, JB .

JOURNAL OF PHARMACEUTICAL SCIENCES, 2005, 94 (01) :1-16

[10]

Jain N, 2001, J PHARM SCI, V90, P234, DOI 10.1002/1520-6017(200102)90:2<234::AID-JPS14>3.0.CO