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Einige Anwendungsmöglichkeiten der Cyclodextrine in der Arzneimittelindustrie

1977; Wiley; Volume: 29; Issue: 1 Linguagem: Inglês

10.1002/star.19770290107

2192-4236

J. Szejtli,

Chemical and Physical Properties in Aqueous Solutions

Abstract Some Application Possibilities of Cyclodextrins in Pharmaceutical Industries . The amylose and its cyclic derivatives, the cyclodextrins, these or so‐called “host” molecules, are readily form inclusion complexes with other so‐called “guest” molecules. The complex formation is dependent on chemical and geometrical factors and is a result of partly physical partly chemical‐hydrogen bond formation. Some important physical properties of the entrapped molecules are modified on complex forming, e.g.: — The solubility of some poorly soluble drugs is enhanced, and its resorption from the digestive tract is modified. — The stability of the entrapped molecules is strongly influenced; e.g. the oxygen absorption of complexed unsaturated fatty acids diminishes, or the decomposition rate of hydrolyzable compounds increases. — The volatility of the entrapped molecules also at higher temperatures is strongly reduced, while in aqueous solutions (gastric acid, intestinal juice) the guest molecules will be set free. The internal cavity of the cyclodextrin molecule may be considered as a so‐called “topochemical base”. The rate of such nucleophilic reactions will be enhanced in this cavity in which the nucleophilic attack sensitive part of the reacting molecule is inserted into the cyclodextrin cavity.