Title of Invention

A PROCESS FOR THE PERPARATION OF NOVEL MOLECULAR DISPERSIONS OF LIPOPHILIC NUTRIENTS AND A PRODUCT OBTAINED THEREOF

Abstract

The invention disclosed in this application relates to novel water soluble molecular dispersions of lipophilic nutrients such as lutein, zeaxanthin, lycopene, betacarotene, omega-3 fatty acids, tocopherols, many of them being derived from either oils or oleoresins, in water soluble hydrophilic solids or liquid carriers. This invention also provides a process for the preparation of such dispersions. The novel molecular dispersions of the present invention are useful for formulating beverages, capsules, sachets, tablets, lotions, liniments, mouthwashes, and gargles.

Full Text

FORM 2 THE PATENTS ACT 70 (Act 39 of 70 ) PROVISIONAL SPECIFICATION (Section 10) NOVEL MOLECULAR DISPERSIONS OF LIPOPHILIC NUTRIENTS IN LIQUID HYDROPHILIC CARRIERS AND A PROCESS FOR THEIR PREPARATION. OMNIACTIVES HEALTH TECHNOLOGIES PVT LTD., an Indian Company , registered under the Indian company's Act 1957 having its registered office located at Rajan House . Appasaheb Marathe Marg, Prabhadevi, Maharashtra , India 400025 The following specification describes the nature of the invention INTRODUCTION: The present invention relates to novel molecular dispersions of lipophilic nutrients in liquid hydrophilic carriers and a process for their preparation.. The present invention , more particularly, relates to novel molecular dispersion of lipophilic nutrients such as lutein, zeaxanthin, lycopene, betacarotene, omega-3 fatty acids, tocopherols and process for their preparation . The novel molecular dispersions of lipophilic nutrients in liquid hydrophilic carriers of the present invention are useful for formulating beverages, soft gelatin capsules, Heaps,, lotions, liniments, mouthwashes, and gargles. More particularly, the novel free flowing molecular dispersions of lipophilic nutrients of lutein and zeaxanthin in liquid hydrophilic carriers are useful in promoting eye and skin health. PRIOR ART Lipophilic nutrients, by nature, are water insoluble products. Due to their insolubility their bioavailability is very poor. The bioavailability can be enhanced by reducing the particle size, which in turn will enhance their efficiency of micellization, which is an essential step required for absorption in the gastrointestinal tract. Dispersion of nutritional products at molecular level is generally regarded as a technique of reducing the particle size. Such molecular dispersions provide higher efficiency for micellization of nutrients in water and thereby increase the bioavailability. Dispersion of lipophilic nutrients at molecular level will result in converting them in to nano size particles. The particle size of such particles range between 30 nm to 100 nm. In the literature, methods for converting lipophilic nutrients in to molecular dispersion are described. For example, US patent no. 5,286,494 provides a procedure for dispersing poorly water-soluble medicines in to molecular dispersion in in solid carriers such as polyvinyl pyrrolidone, sucrose, etc However, the dispersion is in solid carrier and the resultant product is also in powder form. Such technologies fail to provide high bioavailability in comparison with liquid forms. US patent no. 4,758,427, provides a method for dispersing medicinal products at molecular level . The carrier system used for dispersion, however, is a solid such as polyvinyl pyrrolidone. The resultant product being a solid, has limited aqueous solubility and bioavailability. US patent no. 7,259,186 describes a method for the preparation of molecular dispersion of a medicinal product. However, the carrier used is a solid enteric coating polymer. Such products are in solid form and do not enhance the bioavalability. While technologies exist in the pharmaceutical and nutritional industries for converting lipophilic products in to molecular dispersions such as starch, polyvinyl pyrrolidone, hpmc, sucrose, no such technology provides the dispersion in hydrophilic liquid form All the available prior art references deal with solid dispersion medium, which are not suitable for presenting the nutrients in the forms such as soft gelatin capsules or Heaps. Though the solid dispersions are suitable for incorporation in to beverages, their usage is limited by the solubility of the carrier in water and requirement of an additional step of dissolution. Lipophilic nutrients have limited absoption in the body due to limited solubility in the gastrointestinal tract. Generally, the bioavailabilty of such nutrients is below 40%. Lipophilic nutrients when dispersed in molecular form in hydrophilic liquid carrier, exist in very fine particle size range, particularly in nano range(less than 100 nanometers, whereby the efficiency of micellization is higher and hence, their absorption is enhanced several fold. The bioavailability is increased beyond 85%. OBJECTIVES OF THE PRESENT INVENTION : Therefore, the main objective of the present invention is to provide novel molecular dispersions of lipophilic nutrients in a liquid hydrophilic carrier. Another objective of the present invention is to provide novel molecular dispersions of lipophilic nutrients such as lutein, zeaxanthin, beta carotene and lycopene. in liquid hydrophilic carriers, with nutrients Still another objective of the present invention is to provide novel free flowing molecular dispersions of lipophilic nutrients such as lutein, zeaxanthin, beta carotene and lycopene in liquid hydrophilic which can be formulated further as beverage or soft gelatin capsule or as Heaps. Yet another objective of the present invention is to provide a process for the preparation of novel free flowing molecular dispersions of lipophilic nutrients such as lutein, zeaxanthin, beta carotene and lycopene in liquid hydrophilic which can be formulated further as beverage or soft gelatin capsule or as Heaps. The present invention has been developed based on our finding due to continuous R & undertaken that a solution of lipophilic nutrient in an organic solvent can be dispersed in certain hydrophilic carrier systems. Upon removal of solvent under vacuum, the resultant dispersion remains as a homogenous liquid which is suitable for filling in to soft gel capsules or in to Heaps. Such liquids are also suitable for incorporation in to beverages Accordingly the present invention provides a novel free flowing molecular dispersions of lipophilic nutrients in liquid hydrophilic carriers and which are useful for converting into soft gelatin capsules, Heaps, ointments, pastes, lotions, liniments, mouthwashes, gargles etc. The products are also suitable for incorporation in to beverages. According to the present invention there is provided a process for the preparation of the novel free flowing molecular dispersions of lipophilic nutrients in liquid hydrophilic carriers, soft gelatin capsules, licaps, ointments, pastes, lotions, liniments, mouthwashes, and gargles etc,te products are also suitable for incorporation in to beverages, which comprises, (i) dissolving a lipophilic nutrient in a non polar / polar solvent or a mixture thereof to form a solution and (ii) mixing the resulting solution with a liquid hydrophilic carrier to form a uniform mixture, (iii) blending the above mixture with a one or more stabilizer and optionally with a surfactant, (iv) heating the resulting mixture under reduced pressure at low temperature to remove the solvent to produce a homogenous free flowing liquid dispersion. The lipophilic nutrient product which can be used in the present invention includes lutein, lutein ester, zeaxanthin isomers, lycopene, beta carotene, tocopherols, astaxanthin, omega-3 fatty acids , ubiquinone, phytosterols, lecithins and the mixtures thereof. The hydrophilic liquid carrier used for forming the dispersing solution includes polyethylene glycol 200, polyethylene glycol 400, ethylene glycol, propylene glycol, glycerol, sorbitol In another preferred embodiment the solvent employed for preparing the solution of the lipophilic nutrient product may be selected from Acetone, Hexane, Ethyl Acetate, Isopropyl Alcohol, Ethanol, Dichloromethane, Methanol, etc, ,more preferably form Acetone, Ethanol, Dichloromethane, Isopropyl alcohol, and more preferably Dichloro Methane and Isopropyl Alcohol. The ratio of hydrophilic liquid carrier to the lipophilic nutrient may be in the range of 0.1 to 10, preferably in the range of-0.6 to 5. The stabilizer which may be used in the process may be selected from ascorbic acid, BHA, BHT, ascorbyl palmitate, mixed natural tocopherols, alpha tocopheryl acetate, sodium ascorbate and mixtures thereof: The surfactant which may be used in the process may be selected from polysorbate 20, polysorbate 60, polysorbate 80, sodium lauryl sulfate and mixtures thereof: The vacuum evaporation of the solvent present in the nutrient solution along with the liquid polymer carrier may be carried at a temperature in the range of 25 deg C to 60 deg C, preferably at the range of 35 to 45 deg C. ADVANTAGES OF THE INVENTION 1. Provides free flowing, water soluble/miscible liquid form of lipophilic nutrient. 2. Provides a process for converting lipophilic nutrient in to a molecular dispersion, with particles of said nutrients being in nano range. 3. Provides a suitable method of delivering poorly water soluble, oily, lipophilic nutrient, either as soft gelatin capsules or Heaps or in to beverages.. 4. Provides a dosage form of poorly water soluble, oily, lipophlic nutrient with high bioavailability. 5. Protects the oily, lipophilic nutrient from environmental factors such as light, oxygen & heat.

Documents:

2180-MUM-2007-ABSTRACT(29-10-2008).pdf

2180-MUM-2007-CLAIMS(29-10-2008).pdf

2180-MUM-2007-CLAIMS(AMENDED)-(1-6-2012).pdf

2180-MUM-2007-CLAIMS(AMENDED)-(19-3-2012).pdf

2180-MUM-2007-CLAIMS(GRANTED)-(25-6-2012).pdf

2180-mum-2007-correspondence(1-11-2007).pdf

2180-MUM-2007-CORRESPONDENCE(29-10-2008).pdf

2180-MUM-2007-CORRESPONDENCE(30-3-2012).pdf

2180-MUM-2007-CORRESPONDENCE(IPO)-(25-6-2012).pdf

2180-mum-2007-correspondence-received.pdf

2180-mum-2007-description (provisional).pdf

2180-MUM-2007-DESCRIPTION(COMPLETE)-(29-10-2008).pdf

2180-MUM-2007-DESCRIPTION(GRANTED)-(25-6-2012).pdf

2180-MUM-2007-FORM 13(30-3-2012).pdf

2180-MUM-2007-FORM 18(27-10-2008).pdf

2180-mum-2007-form 2(27-10-2008).pdf

2180-MUM-2007-FORM 2(GRANTED)-(25-6-2012).pdf

2180-MUM-2007-FORM 2(TITLE PAGE)-(1-6-2012).pdf

2180-MUM-2007-FORM 2(TITLE PAGE)-(19-3-2012).pdf

2180-MUM-2007-FORM 2(TITLE PAGE)-(29-10-2008).pdf

2180-MUM-2007-FORM 2(TITLE PAGE)-(GRANTED)-(25-6-2012).pdf

2180-MUM-2007-FORM 3(19-3-2012).pdf

2180-MUM-2007-FORM 5(29-10-2008).pdf

2180-mum-2007-form-1.pdf

2180-mum-2007-form-2.doc

2180-mum-2007-form-2.pdf

2180-MUM-2007-REPLY TO EXAMINATION REPORT(19-3-2012).pdf

2180-MUM-2007-REPLY TO HEARING(1-6-2012).pdf

2180-MUM-2007-SPECIFICATION(AMENDED)-(1-6-2012).pdf

2180-MUM-2007-SPECIFICATION(AMENDED)-(19-3-2012).pdf

2180-MUM-2007-SPECIFICATION(MARKED COPY)-(1-6-2012).pdf

2180-MUM-2007-SPECIFICATION(MARKED COPY)-(19-3-2012).pdf