Improvement of chemical instability of carmoful in .BETA.-cyclodextrin solid complex by utilizing some organic acids.

Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and Stabilization

“…This has been shown to be the case with carmofur, an anticancer agent, where the solid-state rate of degradation was increased upon complexation with -cyclodextrin. 93 Under dry conditions cyclodextrin complexation of drugs commonly increases both their chemical (e.g., prostaglandin E 1 94 ) and physical stability (e.g., nifedipine 95,96 ). Large drug molecules like peptides and proteins can also form cyclodextrin complexes, and frequently the complexation results in both enhanced chemical and physical stability of this type of drug.…”

Investigation of Enhancement of Solubility of Norfloxacin β-Cyclodextrin in Presence of Acidic Solubilizing Additives

“…The solid complexes of norfloxacin and β-cyclodextrin were prepared in 1:1 and 1:2 molar ratios and also with various solubilizing additives such as citric acid or ascorbic acid in 1:1:0.5 molar ratio using kneading method [9]and solvent evaporation method.…”

Design and Evaluation of Cyclodextrin-Based Drug Formulation

“…The possible enhancing mechanisms of CyDs on the bioavailability of drugs in various administration routes are summarized as follows: 1) hydrophilic CyDs increase the solubility, dissolution rate, and wettability of poorly watersoluble drugs, [82][83][84][85][86][87][88][89][90][91][92][93][94][95][96][97][98][99][100][101] 2) CyDs prevent the degradation or disposition of chemically unstable drugs in gastrointestinal tracts as well as during storage, [102][103][104][105][106][107][108][109][110][111] 3) CyDs perturb the membrane fluidity to lower the barrier function, which consequently enhances the absorption of drugs including peptide and protein drugs through the nasal and rectal mucosa, [112][113][114][115][116][117][118][119][120][121] 4) competitive inclusion complexation with third components (bile acid, cholesterol, lipids, etc.) to release the included drug, [122][123][124][1...…”