Bioactives LLC

Daniel I Kagan

Doddabele L Madhavi

The present disclosure describes economical processes to improve the bioavailability of nutraceuticals by formulations that induce micronization and sustained release. The inventive process can be used to increase the solubility and bioavailability of lipophilic and moderately water-soluble nutraceuticals by combining excipients that increase the solubility and induce sustained release of the active compounds. The inventive process also can be used to increase the residence time of highly water-soluble nutraceuticals that are metabolized and eliminated quickly from the body, consequently increasing the therapeutic potential. The disclosed formulations advantageously are freely flowing powders that can be used to formulate with other ingredients into tablets, capsules, or the like; or used as bulk powders.

Nutraceuticals having sustained release for improved bioavailability and method of production

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.

Water dispersible policosanol cyclodextrin complex and method of its production

The present invention describes an improved commercial process for the production of carotenoid-cyclodextrin complexes and formulation of the complex for human ingestion. Complexation with cyclodextrins (e.g., &#x3b1;-cyclodextrin, &#x3b2;-cyclodextrin, &#x3b3;-cyclodextrin, or HP-&#x3b2;-cyclodextrin) significantly improves the uptake of carotenoids (e.g., lycopene, lutein, or zeaxanthin) and their mixtures in vitro. The method for making such complexes includes forming a carotenoid/cyclodextrin complex; freezing drying said carotenoid/cyclodextrin complex; and blending said freeze-dried carotenoid/cyclodextrin complex with a mixture of lecithin and a vegetable oil or a vegetable oil suitable for soft gelatin capsules. The cyclodextrin/carotenoid complex can be formed in a molar ratio of between about 0.5:1.0 and 10:1. In vivo, in a human study, the lutein/&#x3b3;-cyclodextrin complex formulated in lecithin-oil or oil showed a better absorption of lutein, as compared to the free lutein-oil formulation.

Bioavailable carotenoid-cyclodextrin formulations for soft-gels and other encapsulation systems

A method for concentrating trans-xanthophyll esters from marigold oleoresin, which includes blending the oleoresin with a solvent and a co-solvent of lower alkanols and recovering a precipitate enriched with trans-xanthophyll esters at a temperature of above 22&#xb0; C. The recovery of the trans-xanthophyll esters is greater when using the alkanol blend than when using only a lower alkanol from the said blend. The said process is most useful using a lower-grade, commercially available oleoresin, thereby helping small producers, who do not have access to higher-grade oleoresin made through backward integration to marigold cultivation and harvest.

Process for the preparation of lutein ester concentrate

A method for concentrating trans-lutein esters from marigold oleoresin, which includes blending the oleoresin with a solvent and a co-solvent of lower alkanols and recovering a precipitate enriched with trans-lutein esters at a temperature of above 22&#xb0; C. The recovery of the trans-lutein esters is greater using the alkanol blend than when using only a lower alkanol in the said blend. The process is most useful using a lower-grade, commercially available oleoresin, thereby helping small producers, who do not have access to higher-grade oleoresin made through backward integration to marigold cultivation and harvest.

The present invention is based on the unexpected discovery that CoQ-10 can be made commercially in a highly bioavailable form suitable for topical, sublingual formulations, or for oral ingestion. One such bioavailable form is a water dispersible freeze-dried CoQ-10/&#x3b3;-cyclodextrin complex. Complexation in general with &#x3b3;- or &#x3b1;-cyclodextrin improved the cellular uptake of CoQ-10 as compared to water dispersible liposomal or micellar forms of CoQ-10. Thus, the present invention includes a highly bioavailable CoQ-10/cyclodextrin complex for use in the nutritional supplement, oral care, and pharmaceutical industry.

Highly bioavailable coenzyme Q-10 cyclodextrin complex

A practical and effective process for isolating and purifying mixed carotenoids containing higher concentrations of specific compounds, such as all-trans lutein, without the use of harmful organic solvents, is disclosed. The process employs hydrolysis of carotenoid esters in a mixture of isopropanol, water, and alkali to separate the carotenoids from other impurities. The carotenoids are purified further using aqueous precipitation, followed by centrifugation and drying under vacuum. The product is a fine crystalline powder with very low residual solvents (hexane 0.22 ppm; isopropanol 0.53 ppm) suitable for human consumption, either in nutritional supplements or as a food additive.

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Belmont, MA, United States of America

Daniel I Kagan