Soluble Excipients Assisting Dissolution of Drugs: Importance of Amorphous State
The absorption of drugs from solid state preparations can be improved by additives which increase their rates of dissolution. Three new classes of additives/solubilizers were developed. (1) Polymethionine sulfoxide: this polymer has all the structural elements of the powerful solvent dimethyl sulfoxide and some of its solubilizing power; the undesired bioeffects of the dimethyl sulfoxide were suppressed. (2) Hydroxyalkyldigitonin: the saponin, digitonin, was condensed with epoxides and this substitution increased the solubility and suppressed the toxicity of the parent compound. (3) Cy-clodextrins substituted with alkyl or 2-hydroxyalkyl groups: these compounds had considerably higher water solubility than the parent cyclodextrins; also, their inclusion complexes with drugs were very soluble.
KeywordsBile Acid Dimethyl Sulfoxide Inclusion Complex Propylene Oxide High Water Solubility
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