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Water dispersible policosanol cyclodextrin complex and method of its production

a technology of cyclodextrin complex and water dispersible policosanol, which is applied in the field of water dispersible policosanolcyclodextrin complexes, can solve the problems of poor bioavailability of policosanol in human studies, poor bioavailability of policosanol in humans, and low and variable efficacy of policosanol in human studies, so as to improv

Inactive Publication Date: 2008-09-04
BIO ACTIVES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0007]The present disclosure is a formulation of policosanol with natural cyclodextrins resulting in a water dispersible form of policosanol, thereby improving bioavailability. The disclosed process provides an economical commercial method for making the policosanol complex. The complex is suitable for incorporation into oral dosage forms and also in functional foods.

Problems solved by technology

Policosanol is a highly lipophilic material, insoluble in water and has poor bioavailability in humans.
However, in human studies the results have been variable with minimal uptake of policosanol.
It has been suggested that the lower and variable efficacy of poilcosanols in human studies can be due to their poor absorption from conventional delivery systems used in the industry.

Method used

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  • Water dispersible policosanol cyclodextrin complex and method of its production
  • Water dispersible policosanol cyclodextrin complex and method of its production
  • Water dispersible policosanol cyclodextrin complex and method of its production

Examples

Experimental program
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Effect test

example 1

[0020]51 g alpha-CD was dissolved in 300 ml of water by heating to 70° C. 10 g of sugarcane Policosanol was mixed with 1.5 g of Tween-80 (also known as Polysorbate 80, is a mixture oleate esters of sorbitan polyethoxylates) and melted by heating to 70° C. The oily mixture was added to the CD solution under homogenization. After 30 min of homogenization, the complex started to precipitate out of solution. The mixture was cooled to room temperature and stirred overnight using an overhead stirrer. The slurry was freeze-dried to obtain a white water dispersible powder containing 16% policosanol.

[0021]The DSC analysis was conducted using TA Instruments 2920 in an inert atmosphere. FIGS. 1-4 present the DSC profiles of Policosanol, alpha-CD, policosanol+alpha-CD physical mixture and the complex respectively. Policosanol showed a major melting endotherm at 81.9° C. The area of the endotherm, which is proportional to the free Policosanol, makes it possible to quantify the complexing. Polico...

example 2

[0022]62 g beta-CD was dissolved in 300 ml of water by heating to 70° C. 10 g of sugarcane Policosanol was mixed with 1.5 g of Tween-80 and melted by heating to 70° C. The oily mixture was added to the CD solution under homogenization. After 30 min of homogenization, the complex started to precipitate out of solution. The mixture was cooled to room temperature and stirred overnight using an overhead stirrer. The slurry was freeze-dried to obtain a white water dispersible powder containing 14% policosanol. The DSC analysis indicated the uncomplexed Policosanol as 9%.

example 3

[0023]69.5 g gamma-CD was dissolved in 300 ml of water by heating to 70° C. 10 g of sugarcane Policosanol was mixed with 1.5 g of Tween-80 and melted by heating to 70° C. The oily mixture was added to the CD solution under homogenization. After 30 min of homogenization, the complex started to precipitate out of solution. The mixture was cooled to room temperature and stirred overnight using a overhead stirrer. The slurry was freeze-dried to obtain a white water dispersible powder containing 12.5% policosanol. The DSC analysis indicated the uncomplexed Policosanol as 11%.

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Abstract

Disclosed is a formulation of policosanol with natural cyclodextrins resulting in a water dispersible form of policosanol. The disclosed process provides an economical commercial method for making the policosanol complex. The complex is suitable for incorporation into oral dosage forms and also in functional foods. One aspect of the present disclosure is a process for making a water dispersible policosanol cyclodextrin complex for animal ingestion. This method includes preparing a policosanol cyclodextrin complex and administering said complex to an animal. The preferred animal is a human with the route of administration being oral ingestion. The form of the complex for ingestion can be a hard gelatin capsule, tablet or wafers, which may contain other ingredients, both active and inactive. The complex also can be further formulated with excipients suitable for soft gelatin capsules, such as, for example, vegetable oils, waxes, lecithin, and surfactants such as Tween-80.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims benefit of provisional application Ser. No. 60 / 901,533 filed on Feb. 15, 2007, the disclosure of which is expressly incorporated herein by reference.STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH[0002]Not applicable.BACKGROUND[0003]The present disclosure generally relates to development of water dispersible policosanol-cyclodextrin complexes for use in nutritional supplements and functional foods.[0004]Cyclodextrins (sometimes abbreviated herein as “CD” or “CD's”) are cyclic oligosaccharides composed of 6, 7, or 8 α-(1-4)-linked anhydroglucose units. The α-, β-, and γ-cyclodextrins prepared from starch are considered natural and are GRAS according to the USFDA. The cyclodextrins are widely used in the pharmaceutical industry to improve dissolution, stability and uptake of lipophilic molecules.[0005]Policosanol is a complex mixture of lipophilic very long-chain alcohols (C24-C34) isolated from waxes, such as, for ...

Claims

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Application Information

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IPC IPC(8): A61K31/724
CPCA61K31/045B82Y5/00A61K47/48969A61K47/6951A61P3/00
Inventor MADHAVI, DODDABELE L.KAGAN, DANIEL I.
Owner BIO ACTIVES