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The effects of organic salts on the cyclodextrin solubilization of drugs
- Source :
- International journal of pharmaceutics. 262(1-2)
- Publication Year :
- 2003
-
Abstract
- Previous studies have indicated that conventional description of drug/cyclodextrin complexes in aqueous solutions as inclusion complexes are not as unambiguous as one might think. It has been shown that in some cases drug/cyclodextrin complexes consist of a mixture of inclusion and non-inclusion complexes. Furthermore it has been shown that drug/cyclodextrin complexes can form aggregates containing up to couple of hundred complexes. In this present study β-cyclodextrin (βCD) solubilization of hydrocortisone is enhanced by including short-chain anionic and cationic species in the aqueous complexation medium. For example, maximum hydrocortisone solubility in pure aqueous βCD solutions or suspensions is 2.2 mg/ml. Addition of 1% (w/v) sodium acetate to the complexation medium increases this value to 7.1 mg/ml (or over 220%). Further addition of 0.25% (w/v) hydroxypropyl methylcellulose to the medium increased the hydrocortisone solubility to over 9 mg/ml. Similar results were obtained when sodium salicylate or benzalkonium chloride were added to the complexation medium. It is also shown that cyclodextrin complexes of lipophilic compounds that have good affinity for the cyclodextrin cavity can be used to enhance cyclodextrin solubilization of drugs that have low affinity for the cavity. All these observations can be explained by formation of drug/cyclodextrin complex aggregates.
- Subjects :
- Anions
Hydrocortisone
Sodium Acetate
Chemistry, Pharmaceutical
Drug Compounding
Pharmaceutical Science
Dosage form
Inclusion compound
chemistry.chemical_compound
Benzalkonium chloride
Cations
polycyclic compounds
medicine
Organic chemistry
Solubility
Sodium salicylate
Chromatography, High Pressure Liquid
chemistry.chemical_classification
Cyclodextrins
Aqueous solution
Cyclodextrin
Alprazolam
beta-Cyclodextrins
Diflunisal
carbohydrates (lipids)
Cholesterol
chemistry
Cyclosporine
Solvents
Benzalkonium Compounds
Sodium acetate
medicine.drug
Nuclear chemistry
Subjects
Details
- ISSN :
- 03785173
- Volume :
- 262
- Issue :
- 1-2
- Database :
- OpenAIRE
- Journal :
- International journal of pharmaceutics
- Accession number :
- edsair.doi.dedup.....c201abf3cf5bf4e02e78b558328c2c7c