Nutraceuticals Having Sustained Release for Improved Bioavailability and Method of Production

摘要

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.

主权项

1. A particulate nutraceutical composition, which comprise:
(a) between about 1% and 60% by weight of a lipophilic nutraceutical having a particle size not substantially larger than about 10μ; (b) between about 0.5% and 20% be weight of a lipid selected from the group consisting essentially of vegetable oils, medium chain triglycerides and isopropyl or ethyl esters of fatty acids; (c) between about 10% and 30% by weight of a surfactant being one or more of a non-ionic type polysorbate, or polyglycerol esters of fatty acids with a hydrophilic-lipophilic balance (HLB) value between 8-16; (d) between about 1% and 50% by weight of a polymer being one or more of carboxymethyl cellulose, ethyl cellulose, hydroxypropyl methyl cellulose, alginic acid sodium salt, or a cyclodextrin; and (e) between about 1% and 50% by weight of an excipient being one or more of a microcrystalline cellulose, silica, maltodextrin, potato starch, bamboo silica, or rice flour; where the amount of said polymer and lipid is insufficient to coat all of the nutraceutical composition particles and where said nutraceutical composition has improved bioavailability and a combination of immediate release and sustained release.