By Karl-Heinz Frömming
Nearly 3 thousand papers and patents are devoted to the particular or power makes use of of cyclodextrins in pharmacy and pharmaceutical formulations. this is often the 1st ebook written for pharmacists and pharmaceutical technologists which not just severely summarizes the big volume of literature to be had, yet which are used as a instruction manual while trying to find options to functional difficulties.
the basics -- chemistry of cyclodextrins and their derivatives -- their actual and chemical houses are condensed to the main correct goods in Chapters 1 and a couple of. bankruptcy three offers with the adsorption, metabolism and toxicological homes of cyclodextrins. bankruptcy four explains the formula, constitution, composition and positive results of the cyclodextrin inclusion complexes. bankruptcy five describes the equipment for training and characterization of drug/cyclodextrin complexes. Chapters 6 and seven are devoted to the pharmacokinetics, biopharmaceutical and technological facets of drug/CD complexes. bankruptcy eight treats the applying and results of cyclodextrins in quite a few drug formulations. The Appendix contains a suite of recipes for any form of drug formula.
This publication is aimed toward those that use cyclodextrins in drug formulations, to enhance the homes of present drug formulations, or who are looking to organize relatively new formulations.
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Extra resources for Cyclodextrins in Pharmacy
Intact CD in the blood was determined by HPLC. 5 mg/kg) PHARMACOKINETICS AND TOXICOLOGY OF CYCLODEXTRINS 0'.. : 90 > u 0 35 .. 0 "2 60 14C - GlU CaSE "2 0 CD 30 • ~ ~14C_~CD S 0 12 18 21, h 12 18 24 h 01. : 14C-GLUCOSE ~v 0 ~ 2 20 ""~ .. a. a: 10 6 Fig. 3-1. (a) Blood radioactivity level following oral administration of 14C-glucose or 14C-,BCD in starved rats. (b) Radioactivity exhaled by rats after oral administration of 14C_,BCD (36 mg-I) or 14C-glucose (13 mg kg-I). of 14C-,BCD. The radiochromatogram obtained by HPLC revealed the presence of 3-50 ppm ,BCD in the blood.
Thomas and D. French fed rats a diet in which a part of the carbohydrate was supplied by highly purified j3-dextrin. The animals refused to eat the test diet except in very small quantities and within a week all animals on the ration were dead. Postmortem examination did not reveal the cause of death. Since then many animals have been fed CD but none have refused it. ) since recent toxicological studies have definitely disproved these results. 1. ORAL TOXICITY No definite acute toxicity values can be determined, because the highest possible dose does not result mortality in the animals.
There are some further names used in the literature, such as adduct, clathrate, molecular compound, cryptate and complex. Considering that no covalent bond is established between the host and guest, and moreover the dissociation-association equilibrium in solution is one of the most characteristic features of the host-guest association, the name 'inclusion complex' (or CD complex) seems to be the most appropriate. Figure 4-2 is a schematic representation of the CD inclusion complex formation. e.