By Karl-Heinz Frömming
Nearly 3 thousand papers and patents are devoted to the particular or capability makes use of of cyclodextrins in pharmacy and pharmaceutical formulations. this is often the 1st booklet written for pharmacists and pharmaceutical technologists which not just seriously summarizes the large quantity of literature to be had, yet which might be used as a guide whilst searching for options to useful difficulties.
the basics -- chemistry of cyclodextrins and their derivatives -- their actual and chemical houses are condensed to the main appropriate goods in Chapters 1 and a pair of. bankruptcy three offers with the adsorption, metabolism and toxicological homes of cyclodextrins. bankruptcy four explains the formula, constitution, composition and effective results of the cyclodextrin inclusion complexes. bankruptcy five describes the tools for practise and characterization of drug/cyclodextrin complexes. Chapters 6 and seven are devoted to the pharmacokinetics, biopharmaceutical and technological elements of drug/CD complexes. bankruptcy eight treats the appliance and results of cyclodextrins in a number of drug formulations. The Appendix includes a set of recipes for any kind of drug formula.
This ebook is geared toward those that use cyclodextrins in drug formulations, to enhance the homes of present drug formulations, or who are looking to organize rather new formulations.
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Extra info for Cyclodextrins in Pharmacy
Editions de Sant€, Paris (1991). Uekama K. and Irie T. ), Editions de Sant€, Paris (1987). 1. Enzymic Degradation of CDs One of the remarkable properties of CDs is their outstanding resistance towards the usual starch hydrolyzing enzymes. They are completely resistant to ,B-amylase since they do not contain end groups susceptible to the attack of this enzyme. Since they attack inside the molecules and do not require free end groups, a-amylases are capable of hydrolyzing the CDs, though usually at a low rate.
The derived ,B-cyclodextrin products are more soluble than the a-cyclodextrin polymers. These rather heterogeneous products are best characterized by their molecular mass and distribution, determined by gel-permeation chromatography. Cyclodextrin polymers in the 3000-6000 Dalton molecular weight range are readily soluble in water. Solutions of 400-600 gIl polymer concentration are still moderately viscous. When the mass of the crosslinking agent is determined, such solutions contain 160-360 gIl cyclodextrin.
CDs may be regarded as hydrophobic in the sense that their solubility slightly improves when a small amount of a relatively apolar solvent, such as ethanol, is added to water. This shows that the CD cavity is hydrophobic in comparison with water. The solvation of this hydrophobic region is far from ideal. A decrease in the energy of the system is caused by the increase of the solvent! solute interaction, since the contacting surfaces are reduced between the solvent and guest molecule, as well as between the solvent and CD cavity.