Cyclodextrin
 
CycloLab

Research & Development - Pharmaceutical

Cyclodextrins can be used in drugs either for complexation or as auxiliary additives such as carriers, diluents, solubilizers or tablet ingredients.
Inclusion complex formation usually results in advantageous modification of the physico-chemical properties of the complexed drug.

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Improvement of physical and chemical stability:
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• stabilization of volatile compounds against evaporation;
• protection of sensitive compounds against oxidation;
• reduction of sensitivity to light, heat, etc.

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Enhancement of the bioavailability of poorly soluble drugs:
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• increased solubility in water
• transformation of lipophylic substances into a water-soluble formulation
• enhanced rate of dissolution;
• more complete and faster absorption after oral application;
• altered pharmacokinetic profile (higher cmax and shorter tmax) is a usual consequence of complex formation;
• improved bioavailability enables dose reduction with adequate therapeutical effect and of less dose-related side effects;
• decreased interindividual variation of bioavailability;
• improved pH-solubility profile of the complexed, poorly soluble drugs in the physiological pH range;
• enhanced drug absorption independently of the acidity of the gastric juice.

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Alleviation of local irritations or damage induced by drugs:
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• reduced side effects;
• reduced skin irritation and muscular tissue damage;
• reduced kidney damage;
• reduced haemolytic activity;
• masked smell and bitter taste.

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Technological advantages in the formulation of oral drugs:
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• liquids can be transformed into a crystalline form which is suitable for tabletting;
• incompatible compounds can be mixed and used together in complexed form;
• the content uniformity of low dose oral formulations is improved by using complexed actives;
• improved wettability;
• extended release formulations can be prepared.

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Technological advantages in liquid drug formulations, injections, eye drops etc.
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• stable aqueous solutions of insoluble drugs can be prepared without the use of organic co-solvents or surfactants.

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Application as tabletting excipient:
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• βCD can be applied as binder in tablets;
• highly swelling cyclodextrin polymers are effective tablet disintegrants.

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Drugs with dwindling patent life (Life cycle management):
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• strengthening the brand company's patent position by patenting the marketed drug improved by cyclodextrin complexation.
• prolonging the product life for the originator by replacing a top product with its cyclodextrin-complexed form

   
 
Cyclodextrin Laboratory
© 2009 - CycloLab Cyclodextrin Research & Development Laboratory, Ltd. - Hungary
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