Interaction between cyclodextrin derivatives and drugs in pharmaceutical preparations
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Interaction between cyclodextrin derivatives and drugs in pharmaceutical preparations

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In order to solve the problems of formulation design and safety and effectiveness caused by the lack of self solubility, stability and bioavailability of drugs, the drug and auxiliary materials can be made into inclusion compound, eutectic, solid dispersion, phospholipid complex, particle delivery system and other formulations, namely, carrier. In recent years, the research on the interaction between drugs and excipients in carrier preparation has been extended to the research direction of the influence of excipients on the formation of carrier preparations and the interaction between other excipients and carriers, and plays an important role in the formulation design and optimization.

Interaction between drugs and cyclodextrin excipients: cyclodextrin inclusion compounds are generally composed of excipients and drug objects. The main interaction among the molecules of the main and objective includes van der Waals force, hydrophobic force, hydrogen bond force, etc. the stronger the interaction between the main and the object molecules, the more likely to form inclusion compounds. Inclusion compounds can cover up the bad taste of the drug, improve the solubility, stability and bioavailability of the drug. For example, the methyl β - cyclodextrin inclusion complex of olanzapine was prepared by rotating evaporation method by de freetas. The infrared spectrum analysis showed that there was hydrogen bond between the hydroxyl group of cyclodextrin and N-H on the o-nitrobenzodiazepine ring, and the hydrophobic interaction between n-ch3 and cyclodextrin cavity was possible. The dissolution rate of the inclusion compound was higher than that of olanzapine at 30 minutes.

cyclodextrin, MBCD, methyl-beta-cyclodextrin

The interaction between the inclusion complex and excipients was observed in the compatibility study of the inclusion complex and excipients. Because the drug is wrapped in the cavity structure, it can avoid direct contact with the excipients, thus reducing the interaction. For example, studies such as sb? Rcea showed that fosinopril was incompatible with MS, but the FT-IR spectrum of the physical mixture of fosinopril sodium and hydroxypropyl - β - cyclodextrin and MS showed that the characteristic peaks of each substance did not move or eliminate, indicating that the inclusion compound improved the compatibility of the drug and MS. Some excipients may compete with the drugs in the inclusion complex, such as propyl p-hydroxybenzoate and benzoic acid, which will replace the drugs in the cavity of cyclodextrin. This not only reduces the solubilization of cyclodextrin to drugs, but also makes the preservatives ineffective. Therefore, it is necessary to consider the competitive effect with drugs in the formulation design of inclusion compounds. Studies have shown that the inclusion efficiency and solubility of cyclodextrin can be increased by adding water-soluble polymers in the preparation process of inclusion compound. For example, sherje et al. Added 0.3% water-soluble polymer polyvinylpyrrolidone (PVP, kollidon-30) to prepare the ternary inclusion complex of paparenone PVP - β - cyclodextrin. The results of phase solubility show that the stability constant and inclusion efficiency of ternary inclusion complexes are higher than those of binary inclusion complexes. FT-IR and DSC analysis showed that the interaction of paparenone with PVP and β - cyclodextrin in the ternary inclusion complex was stronger than that in the binary inclusion complex. In vitro dissolution test showed that the dissolution rate of ternary inclusion complex was 99.0% within 20 min, which was faster than that of binary inclusion complex (82.0%).

Binzhou Zhiyuan biology has been committed to the production and research of cyclodextrin derivatives, and has in-depth cooperation with many domestic universities and scientific research institutions. At present, not only hydroxypropyl beta cyclodextrin, sulfobutyl beta cyclodextrin, but also methyl beta cyclodextrin, hydroxypropyl gamma cyclodextrin and many new cyclodextrins used in scientific research have been industrialized. We are willing to cooperate with colleagues in the pharmaceutical industry To explore the wide application of cyclodextrin inclusion complex in medicine. +86-531-88916568




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