By Karl-Heinz Frömming
Nearly 3 thousand papers and patents are devoted to the particular or strength 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 quantity of literature on hand, yet which might be used as a instruction manual whilst trying to find options to sensible difficulties.
the basics -- chemistry of cyclodextrins and their derivatives -- their actual and chemical homes are condensed to the main appropriate goods in Chapters 1 and a couple of. bankruptcy three offers with the adsorption, metabolism and toxicological houses of cyclodextrins. bankruptcy four explains the formula, constitution, composition and helpful results of the cyclodextrin inclusion complexes. bankruptcy five describes the equipment for instruction 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 numerous drug formulations. The Appendix contains a set of recipes for any form of drug formula.
This e-book is geared toward those that use cyclodextrins in drug formulations, to enhance the houses of current drug formulations, or who are looking to organize particularly new formulations.
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Additional resources for Cyclodextrins in Pharmacy
Extremely high doses of (JCD (up to 78% of the nutrition), for a longer period (110 days) in rats, resulted in a retarded body weight gain and reduced body fat deposition. The rats could hardly digest the pure aCD; only the (JCD was digested. If, however, aCD was only part of a cyclic and acyclic dextrin mixture, it could be digested. ,CD was studied in rabbit and dog after intravenous administration. ,CD administered directly into the circulatory system is either metabolized or excreted within 4 h.
The results prove that HPBCD is scarcely absorbed from the gastrointestinal tract. The total amount absorbed is below 10 dose-%. 25% of the administered dose is metabolized, according to the radioactivity exhaled by the animals. The toxicity of HPBCD has been assessed in both rats and monkeys in acute, subacute (14 days) and subchronic (90 days) treatments with no overt manifestation. Doses as high as 10 000 mg/kg in monkeys were not lethal. In mice acute intraperitoneal administration up to 10000 mg/kg and intravenous administration up to 2000 mg/kg did not cause death.
A similar substituent in the para position has a relatively weak effect. Hydroxyl groups hinder complex formation, but their hydrophilic effects decrease in the order ortho > meta> para. In the case of amino groups it is important whether they are present in the -NH2 or -[NH3]+ form. Ionic species are usually, but not always, unfavoured in complex formation. Excessively strong cohesive forces between the molecules of the guest impede their separation, which is a precondition for the inclusion. A measure of the cohesion between the molecules of a crystalline substance is the melting point.