Beta
7110

THE EFFECT OF BETACYCLODEXTRIN ON THE SOLUBILITY AND DISSOLUTION OF SPIRONOLACTONE USING PHYSICAL MIXING AND CO-EVAPORATION METHODS

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Last updated: 22 Jan 2023

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Abstract

Spironolactone is a steroidal drug acting as a specific aldosterone antagonist used as potassium sparing diuretic.  It shows variable absorption and bioavailability due to its poor solubility.  The objective of this study was to investigate the effect of betacyclodextrin (BCD) on the solubility and dissolution of spironolactone using physical mixing and co-evaporation methods.  The physical mixtures of different w/w drug/carrier ratios (1:1, 1:2 and 1:3) were prepared by simple mixing.  Also co-evaporate systems containing (1:1, 1:2 and 1:3) w/w drug/carrier ratios were prepared.  The physicochemical characterization of the systems using differential scanning calorimetry (DSC) and powder X-ray diffraction was carried out to detect the interaction between the drug and the carrier, moreover, quantitative solubility and in-vitro dissolution studies of spironolactone alone and in physical mixtures or co-evaporates were studied in simulated gastric fluid (SGF) of pH 1.2 and in simulated intestinal fluid (SIF) of pH 7.5. The reduction of drug peaks in X-ray diffraction pattern of the co-evaparate and the absence or reduction of drug peaks in DSC profile of the physical mixture and the co-evaporate suggest the transformation of crystalline spironolactone into an amorphous form due to the inclusion complexation with betacyclodextrin.  The study showed an increase in the solubility values and an improvement in the dissolution pattern of the drug in case of the physical mixtures and the co-evaporates.

DOI

10.21608/ajps.2013.7110

Authors

First Name

Khaled

Last Name

Saleh

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Affiliation

Dept. of Pharmaceutics and Industrial Pharamcy, Faculty of Pharmacy, Al-Azhar University, Assiut Branch.

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Volume

47

Article Issue

1

Related Issue

1346

Issue Date

2013-03-01

Receive Date

2018-05-14

Publish Date

2013-03-01

Page Start

83

Page End

94

Print ISSN

1110-1644

Online ISSN

2535-1958

Link

https://ajps.journals.ekb.eg/article_7110.html

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https://ajps.journals.ekb.eg/service?article_code=7110

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7

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Original Article

Type Code

518

Publication Type

Journal

Publication Title

Al-Azhar Journal of Pharmaceutical Sciences

Publication Link

https://ajps.journals.ekb.eg/

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Article

Created At

22 Jan 2023