Novel stable beadlets of lipophilic nutrients

Abstract

The invention disclosed in this application relates to novel stable beadlets of lipophilic nutrients comprising an inert core having a coating of stabilizing antioxidants, lipophilic nutrients, or mixtures thereof. The beadlets may be coated with one or more coatings to protect the lipophilic ingredients from the atmosphere, specifically the coatings can be used to protect against moisture and / or oxygen. The invention also relates to a process for the preparation of the stable beadlets. The beadlets can be used in medicines and dietary supplements intended to facilitate the reduced risk of macular degeneration, cataract, and several forms of cancer.

Description

[0001]This application is a Division of application Ser. No. 10 / 901,748, filed Jul. 29, 2004, which application is incorporated herein by reference.[0002]The present invention relates to novel beadlets of lipophilic nutrients and a process for their preparation. The present invention, particularly relates to novel and stable beadlets of lipophilic nutrients, materials, or substances, particularly nutrients like carotenoids, tocopherols, tocotrienols, plant sterols and stanols, and lecithins, select omega-3 fatty acids and poly-unsaturated fatty acids, more particularly novel beadlets of lutein, lutein esters, zeaxanthin, zeaxanthin esters, and a process for their preparation.BACKGROUND OF THE INVENTION[0003]The role of nutrients and phytochemicals in the promotion of good health through nutrition has now been extended to the likely benefits such as prevention of cancer, and protection against many other chronic diseases like arthritis, coronary heart disease, osteoporosis, and possi...

AI Technical Summary

Benefits of technology

"The present invention is about coating an inert core with lipophilic nutrients and stabilizing antioxidants using a fluidized bed technique in an organic solvent medium. The resulting beadlets can be used in pharmaceutical and food industries. The invention has enabled the use of oily lipophilic matter in beadlets, which was previously thought to be difficult. The beadlets are stable, uniform, and have good flow properties for tablet compression. They also have controlled release properties and higher bioavailability. The use of spherical cores avoids degradation of heat-sensitive compounds and the beadlet size range is wider. The invention can be practiced using existing fluid-bed technology and equipment."

Problems solved by technology

Lipophilic substances have a higher solubility in hydrocarbon solvents, such as hexane, and have poor water solubility.

It is a major problem for formulators and manufacturers of such supplements to incorporate lipophilic nutrients such as carotenoids, vitamin E sources like tocopherols and tocotrienols, concentrated forms of PC-rich lecithins, phytosterols and plant stanols, various PUFA rich oils and omega-3 fatty acids singly or in combination with other nutrients into dry forms due to the oily, waxy or viscous nature of these products.

Some options like spray dried powders, granules or gelatin beadlets work only with select products, and do not necessarily function well under tabletting systems.

Some of the challenges in using lipophilic nutrients are explained below:a. Carotenoids tend to be unstable at room temperature, and prone to degradation on exposure to light, heat, air and acidic environment.

Dry delivery forms are considered more difficult to stabilize.c. Tocopherols and tocotrienols are typically found in an oily medium in the presence of vegetable oils.

Such oily products are difficult to use except in the smallest of doses in dry delivery forms such as tablets without the use of specialized technologies to convert them to powders, granules or beadlets.d.

Conventional dry delivery conversion technologies do not provide good solutions for free flowing, directly compressible beadlets.

By nature, carotenoids are unstable at room temperature.

The beadlets obtained by the above known processes do not ensure stability to the active material either in the beadlet form itself, or when formulated into tablets.

In addition, none of the hitherto known methods of making beadlets provide desirable physical characteristics, such as spherical, free flowing beadlets suitable for tabletting or capsule filling.

Further, the beadlets produced by hitherto known methods do not prevent leaching of the active nutrients contained in such beadlets when subjected to compression to form tablets.

In recent times, use of excipients of animal origin in herb-based nutraceuticals is considered undesirable by a large section of users.

Due to poor digestibility, use of gelatin based formulations have a limitation for use among the geriatric population.

Sometimes, lactose is used as an excipient in the main beadlet matrix due to its compressible nature, but its dairy product (animal) origin makes it unacceptable to many, and is therefore considered to be undesirable.

Thus, the formulation of oral delivery systems for lipophilic nutrients, particularly carotenoids such as lutein, lycopene, beta carotene, present a challenge to the pharmaceutical and food industries, due to the oily nature and instability of the carotenoids / lipids.

By nature, carotenoids and lipophilic nutrients are unstable in presence of oxygen and light.

Such processes suffer from drawbacks such as use of high temperature (180.deg.

), which are not suitable for many heat sensitive products such as carotenoids.

Unfortunately, this method using organic solvent medium is not applicable directly for the formation of beadlets of lipophilic nutrients, such as carotenoids, in spite of the above said advantages, due to their oily / waxy nature.

Further these nutrients, when subjected to fluidization, form a cohesive mass, which adversely affects the fluidization.

Therefore a process employing fluid-bed system using a non-aqueous coating medium has hitherto not been considered possible or demonstrated, for the preparation of beadlets of lipophilic nutrients such as carotenoids.