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Method For Preparing Of Lipid Based Extracts Having Varying Concentrations Of Active Medicaments And Varying Reduced Levels Of Lipid Content And Products Thereof

Abstract: The invention relates to a method of preparing improved lipid based composition such as formulations of Snehas i.e. Tailams, Kerams, Ghritams, Yamakams, Trivrutams, Mahasnehams and other lipid extracts of the herbs and other materials such that there are ratio of drug to fat can be increased to varying higher percentage. The method of incorporating maximum amount of drug (polar) into a lipid carrier comprises of mixing the lipid formulation of Ayurveda, siddha, Unani systems of medicine with a polar/non-polar solvent fraction and passing it through a column packed with polar/non-polar adsorbent. The eluent containing polar medicament with low fat content is collected. This fraction contains maximum amount of drug in a lower quantity of the lipid base. Administering the improved lipid based composition of the present invention results in very small quantity of the fat being utilized to deliver therapeutically recommended or effective doses of synthetic or natural substance as drugs, cosmetics or nutraceuticals as the case maybe.

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Patent Information

Application #
Filing Date
23 March 2010
Publication Number
15/2016
Publication Type
INA
Invention Field
PHARMACEUTICALS
Status
Email
aamohan@iprightsindia.com
Parent Application

Applicants

AVN AYURVEDA FORMULATIONS PRIVATE LIMITED
175-A VILACHERY MAIN ROAD, MADURAI-625 004

Inventors

1. RAMESH VARIER
175-A VILACHERY MAIN ROAD, MADURAI-625 004
2. DURAIPANDI SELVAKUMAR
175-A VILACHERY MAIN ROAD, MADURAI-625 004

Specification

FIELD OF INVENTION:

The present invention relates to improving the content of extract / active constituents in a lipid based composition and specifically to a method for reducing the lipid level in a lipid based extract. More particularly the invention relates to a composition with maximum amount of active constituents which are in the form of polar drugs / herbal constituents / Nutraceuticals / synthetic chemicals contained in a low quantity of lipid base.

BACKGROUND OF THE INVENTION:

The therapeutic effect of an administered substance is directly related to the quantity and rate at which the substance reaches the blood stream of the animal system including humans. There are many factors that affect the ability of the substance to reach the systemic circulation including; the site of entry into the body, the site of absorption, the nature of the substance, the type of formulation, and other physicochemical parameters of the formulation

Oral delivery of the therapeutic substance is the most common and convenient form of administration. The ability of orally administered substances to reach the systemic circulation and getting absorbed is related to the physicochemical properties of the substance and the physiological factors in the gastro intestinal (Gl) tract. Conventional oral dosage forms consists of solutions, suspensions, powders, granules, two piece gelatin capsules, soft gelatin capsules and compressed tablets. Liquid dosage forms are generally much faster absorbed into the system than solid dosage forms because dissolution is not a rate determining step in the absorption process.

Chemicals (Natural & Synthetic) to be administered into animal systems can be divided into materials that are readily soluble in polar solvents like water, alcohol etc or those soluble in non-polar substances like lipids / fats etc. The different tissues of the body are covered by selectively permeable membranes which select the type of entities that can enter through them to reach the cells. Some of them like the duodenal mucosa readily allow polar substances to pass through while some of them like the blood brain barrier permit lipid based entities to pass through more easily.

Many Pharmaceutical, Nutritional, and Veterinary compounds of Natural and synthetic origin are delivered in to the body through Oral, Parenteral, Rectal, Nasal and
Transdermal and other routes. They are formulated to reach specific target organs by specific techniques and mechanisms. Generally the polar compounds are incorporated in polar solvent systems and made as water / alcohol based formulations and administered.
These compounds either in their original or metabolized form is carried by the body fluids to the different parts of the body and reaches the tissue which are permeable to such substances. Several of these substances do not reach many tissues which are permeable only to lipid based substances.

However, there are several polar substances which are required to penetrate barriers and reach tissues which are permeable to lipid based entities only, to exert their physiological effect. There is growing interest and investment in the use of lipid-based systems in drug discovery and product development to effectively overcome physical and biological barriers. Dosage forms like emulsions (W/O), dry emulsions self-emulsifying lipid formulations etc have the disadvantage of separating into the two phases before reaching systemic circulation. However, the delivery of polar substances in lipid medium up to the target tissue is achieved by liposomes, micro encapsulation etc. Similarly, in the case of liposomic process the main issue is the instability found and the other issues noted are high production cost, leakage and fusion of encapsulated drug / molecules, short half-life, low solubility and sometimes the phospholipids used undergoes oxidation and hydrolysis like reactions creating instability of the product.

On scrutiny of traditional systems like Ayurveda, Siddha and Unani the Indian systems of medicine, it is found that they have a very unique method of formulating aqueous extracts of poly herbal ingredients in fixed oils of plant and animal origin for use in humans and animals. These formulations are called "Sneha Kalpanas" or oil based formulations. The fixed oils of several plants like Sesame, Coconut, Castor, Neem, Mustard and animal fats like ghee, butter, tallow, marrow etc have been formulated to administer nutritional, physiologically active, cosmetic and nutraceutical compounds to humans and animals both externally and internally.

The method of preparation of these formulations is described in traditional literature. The materials to be formulated are added to one or more of the lipids in one or more of the following ways; as an aqueous extract, as a juice or as a paste. The mixture is heated till all the moisture content is evaporated. This leaves an oily extract, which is the part contains the medicaments, and sediment which contains the non-extracted portion. This sediment is filtered out and the resultant oily extract is a fat rich formulation containing the extractable material in a lipid base. This is to be used either internally or externally or both depending on the materials extracted and the purpose for which it is formulated.

These formulations have been in use in these systems of medicines for thousands of years. They are used in varying doses from a few drops in certain cases to 5 ml - 300 ml per dose one or two times a day when used internally. They are also used for external application as medicated oils and cosmetics.

It is to be specifically noted that in these formulation the polar substances are indeed carried by the lipid carrier through the tissues successfully. However, the ratio of the quantity of the extracted material Vis-a-vis the lipid carrier is extremely small and hence large quantities of the carrier are to be administered to deliver therapeutically effective quantities of extracts.

With the changes in the lifestyle of the human race, increased automation is leading to drastic reduction of physical activity. Abundance of food and poor eating habits leading to metabolic diseases like diabetes, dyslipidaemia etc, resulting in cardio-vascular and cerebro-vascular diseases. There is a serious concern among the physicians and the consumers regarding the potential ill-effects of these formulations especially the ones that are given for a long period of time and in doses like 5-15 ml and above per dose (which is the recommended dose in most cases) for continued use. This has lead to the drastic reduction in the use of these formulations for internal administration. The excess fat content of the lipid carrier and the low percentage of extracted matter in these formulation is an undesirable but existing problem in this prior art.

OBJECT OF THE INVENTION:

The object of the invention is designed to address the problems faced in the prior art with particular reference to the process used in the traditional system of lipid based product formulation and offer a solution devoid of the problems described above.

The main object of the present invention is to reduce the quantum of Lipid required to deliver a given amount of the extractable substance to the biological system.

Another object of the present invention is to reduce the dosage of the lipid based compositions used internally in Ayurveda, Siddha and Unani the Indian systems of medicine.

Yet another object of the present invention is to improve the lipid based composition such as formulation of the Snehas i.e., Tailams, kerams, Ghritams, Yamakams, Trivrutams. Mahasnehams and other lipid extracts of the herbs and other materials, such that there is a very high drug is to fat percentage so that a very small quantity of the fat is needed to be administered to deliver therapeutically recommended or effective doses of medicaments.
Yet another object of the present invention is to develop a method to reduce the fat content in the traditional parent lipid based composition.

Yet another object of the present invention is to reduce the overall dose to be administered, so as to be able to present the doses of the extractible matter in easily ingestible form as in soft-gel capsules and thereby improve the patient/consumer's compliance to the regimen.

Yet another object of the present invention is to prevent the associated difficulty in ingesting the recommended doses of the lipid based herbal products for internal administration.

Yet another object of the present invention is to offer highly concentrated versions of the lipid based natural preparations for external use as drugs.

Yet another object of the present invention is to offer highly concentrated versions of the lipid based natural preparations for external use as cosmetics.

Yet another object of the present invention is to offer highly concentrated versions of the lipid based synthetic preparations for external use as drugs.

Yet another object of the present invention is to offer highly concentrated versions of the lipid based synthetic preparations for external use as cosmetics.

Yet another object of the present invention is to ease the transportation of oil based preparations to far away destinations by having concentrated versions for shipping which could then be diluted appropriately.

Yet another object of the present invention is to design a dosage form that optimizes effectiveness, maximizes drug availability and safety of the deliverables.

Yet another object of the present invention is to develop a simple method of formulating and administering non-polar and polar natural and synthetic compounds in lipid medium using natural fixed vegetable and animal oils and fats.

Further object of the present invention is to deliver water soluble drugs to tissues that are permeable to lipids only.

Further object of the present invention is to deliver high concentrations of water soluble drugs and mixtures thereof in lipid base for use in humans as drugs

Further object of the present invention is to deliver high concentrations of water soluble Nutraceuticals or mixtures thereof in lipid base for use in humans as Nutraceuticals.

Further object of the present invention is to deliver high concentrations of water soluble natural products or mixtures thereof in lipid base for use in humans as cosmetics.

Further object of the present invention is to deliver high concentrations of water soluble synthetic compounds or mixtures thereof in lipid base for use in humans as cosmetics.

Further object of the present invention is to deliver high concentrations of water soluble synthetic compounds, natural products, or drugs mixtures thereof in lipid base for use in humans as cosmetics, drugs or Nutraceuticals.

Further object of the present invention is to deliver high concentrations of water soluble drugs or mixtures thereof in lipid base for use in animals as cosmetics.

Further object of the present invention is to deliver high concentrations of water soluble drugs or mixtures thereof in lipid base for use in animals as drugs.

Further object of the present invention is to deliver high concentrations of water soluble nutraceuticals or mixtures thereof in lipid base for use in animals as nutraceuticals.

Further object of the present invention is to deliver high concentrations of water soluble natural or synthetic products or mixtures thereof in lipid base for use in animals, as cosmetics, drugs or nutraceuticals.

SUMMARY OF THE INVENTION:

The invention relates to a method of preparing improved lipid based composition such as formulations of Snehas i.e. Tailams, Kerams, Ghritams, Yamakams, Trivrutams, Mahasnehams and other lipid extracts of the herbs and other materials such that there are ratio of drug to fat can be increased to varying higher percentage. The method of incorporating maximum amount of drug (polar) into a lipid carrier comprises of mixing the lipid formulation of Ayurveda, siddha, Unani systems of medicine with a polar/non-polar solvent fraction and passing it through a column packed with polar/non-polar adsorbent. The eluent containing polar medicament with low fat content is collected. This fraction contains maximum amount of drug in a lower quantity of the lipid base. Administering the improved lipid based composition of the present invention results in very small quantity of the fat being utilized to deliver therapeutically recommended or effective doses of synthetic or natural substance as drugs, cosmetics or nutraceuticals as the case maybe.

DESCRIPTION OF THE INVENTION:

Traditional systems of medicine in India like Ayurveda, Siddha, Unani etc. have been using lipids like ghee, Sesame oil, Coconut oil, Castor oil, animal fat etc. or mixtures thereof as a means of lipid based drug delivery. It is found that these systems of delivery are actually incorporating the aqueous soluble materials into a lipid base. However these preparations have a very low concentration of medicinal substance and the percentage of lipid is very high.

The present invention relates to a method to reduce the fat content in the lipid based compositions such as formulation of Snehas i.e. Tailams, Kerams, Ghritams, Yamakams, Trivrutams. Mahasnehams and other lipid extracts of the herbs and other materials, prepared traditionally using the method described in Ayurveda, Siddha, Unani systems of medicine, with out affecting the medicinal content of the formulation. The above mentioned traditional method of processing is capable of incorporating and delivering aqueous extractions and/or polar substances in a lipid base and has the advantage of stability and effective delivery of the medicaments and extracts across biological barriers which are Non-Polar in nature.

The typical way of preparing the traditional formulations are described in detail below.

STAGE 1:

There are three ways for preparing the aqueous solution in general

The first one being using fresh juices (extracts) of the materials like leaves, fruits, nuts, barks, roots, rhizomes etc ,

The second one being the preparation of decoctions of the materials like leaves, fruits, nuts, barks, roots, rhizomes etc in water or,

The third one being the preparation of pastes from powdered materials like leaves, fruits, nuts, barks, roots, rhizomes etc mixed in water

STAGE 2:

Any or two or all of the preparations of stage 1 are added to a lipid base like Sesame, Coconut, Castor, Neem, Mustard and animal fats like ghee, butter, tallow, marrow or mixtures thereof under continuous boiling and stirred to remove the water content. At the end of the stage, the water is evaporated leaving behind an oily extract which is the formulation, and a portion of solid sediments found at the bottom of the lipid formulation which is rejected.

It is observed that the snehas thus formulated as per the traditional method actually contain two fractions. One fraction with affinity for polar substances called the Polar fraction and another fraction with no affinity for polar substances called Non polar fraction. The Polar fraction contains the polar substances that need to be delivered while the Non-Polar portion does not contain any of the substances that need to be delivered, does not play any significant role and just acts as the filler. So it was proposed that the Polar lipid fraction is separated out and the non-polar portion is discarded as, administering the traditionally prepared Snehas containing the high amount of fat may inadvertently pose a metabolic problem to the system, which in turn may disturb the lipid profile of the patient leading to problems like atherosclerosis, and several other metabolic diseases. This drawback was overcome by improving the ratio of the active constituent to the lipid base.

The method of reducing the lipid level in traditionally prepared lipid based composition to form improved lipid based composition of the present invention is carried out based on the following principle.

The Polar fraction of the traditionally prepared lipid based composition is selectively made to adsorb on a column or alternatively eluted out from the column thereby separating the polar medicament with the Polar lipid fraction from the unwanted Non-polar lipid fraction which does not contain the extract.

The improved lipid based composition comprising of increased concentration of plurality of active constituents and/or decreased concentration of plurality of fat constituent compared to traditionally prepared parent lipid based compositions is prepared by the following process using the above principle.

In one of the preferred embodiment the present invention shall discloses a process for preparing improved lipid based composition by reducing the concentration of plurality of fat constituent from the traditionally prepared parent lipid based compositions, comprises of following steps and sequences:

a. mixing the lipid based composition with atleast one polar or non-polar solvent to form a mixture wherein the lipid based composition is dissolved in the solvent,

b. introducing the mixture of step (a) through a column packed with atleast one adsorbent material having a reversal of polarity with the said solvent of step a, wherein a fraction of the lipid based compositionis adsorbed by the adsorbent material and another fraction remains unadsorbed,

c. eluting the unadsorbed fraction in the column, with alteast one solvent having a reversal of polarity with that of the adsorbent for plurality of runs until the eluate is substantially the solvent,

d. Collecting the eluate of step c from the column in each run,

e. eluting the adsorbed fraction from the column with atleast one solvent having polarity similar to that of the adsorbent for plurality of runs until the eluate is substantially the solvent,

f. collecting the eluate of step (e) from the column in each run,

g. comparing the concentration of active constituents and fat constituents in each of the eluates of step(d) and step (f)

h. selecting the eluate having higher concentration of active constituents from step (g) which eluate may include a part of fat constituents

i. discarding the eluate from step (g) which substantially includes fat constituents

j. evaporating the solvent from the eluate selected in step (h)

In another preferred embodiment the present invention shall discloses a process for preparing improved lipid based composition by reducing the concentration of plurality of fat constituent from the traditionally prepared parent lipid based compositions, utilizing the option of polar adsorbent material in the column, wherein the process comprises of following steps and sequences:

1. An open / closed tubular column of desired dimensions with stop cock at the bottom is packed with atleast one polar adsorbent materials like silica based adsorbents, alumina, (either alkaline, or neutral, or acidic), kieselgur, charcoal, calcium carbonate etc or mixtures thereof.

2. The traditional lipid based composition is mixed with atleast one non-polar solvents like petroleum ether, pentane, cyclopentane, toluene, hexane, cyclohexane, 1,4-dioxane, benzene, chloroform, ethyl acetate, diethyl ether or combinations thereof to form a mixture and introduced at the top of the column

3. More quantity of non-polar solvents like petroleum ether, pentane, cyclopentane, toluene, hexane, cyclohexane, 1,4-dioxane, benzene, chloroform, ethyl acetate, diethyl ether or combinations thereof are added at the top and used for the elution. The eluted portion is collected at the bottom till all the Non-Polar part of the lipid base is separated from the formulation and the eluate is substantially the solvent. The fraction collected is tested by HPTLC chromatogram for the presence of the medicament and is seen to not show any medicament content. Then the column is eluted with ethanol, methanol, dichloromethane, dimethyl formamide, dimethyl sulfoxide, tetrahydrofuran, Acetone,
Acetonitrile, n-butanol, isopropanol, n-Propanol, formic acid, Acetic acid and water or combinations thereof and the eluted portion containing the medicament with the Polar fraction of the lipid is collected at the bottom till the eluate is substantially the solvent, and does not show any medicament content in the HPTLC chromatogram.

4. The eluents collected from the above separation process are heated and the solvents are evaporated and removed.

5. The residual portion contained in the Non-polar solvent fraction is discarded which contains the removed fat and does not contain active medicament and the absence of the medicament in this residue is confirmed by any suitable methods like HPTLC, HPLC or GC

6. The residual portion contained in the Polar fraction contains substantially the active polar material to be incorporated along with minimum lipid content and the presence of the total medicament content is confirmed and relatively quantified by the HPTLC chromatogram in comparison with that of original formulation.
In another preferred embodiment the present invention shall discloses a process for preparing improved lipid based composition by reducing the concentration of plurality of fat constituent from the traditionally prepared parent lipid based compositions, utilizing the option of non-polar adsorbent material in the column, wherein the process comprises of following steps and sequences:

1. An open or closed tubular column of desired dimensions with stop cock at the bottom packed with atleast one non-polar adsorbent material like C18 (octadecylsilane), C8 (octyl), Cyanopropyl, Phenyl C4 (butyl), Hydrophobic interaction, C2 (ethyl), C1 (methyl) (silica based reverse phase columns).

2. The traditional lipid based composition is mixed with polar solvents like ethanol, methanol, dichloromethane, dimethyl formamide, dimethyl sulfoxide, tetrahydrofuran, Acetone, Acetonitrile, n-butanol, isopropanol, n-Propanol, formic acid, Acetic acid and water or combinations thereof to form a mixture and introduced at the top of the column.

3. More quantity of polar solvents, like ethanol, methanol, dichloromethane, dimethyl formamide, dimethyl sulfoxide, tetrahydrofuran, Acetone, Acetonitrile, n-butanol, isopropanol, n-Propanol, formic acid, Acetic acid and water or combinations thereof are used for the elution. The eluted portion is collected at the bottom till all the medicament with the Polar lipid fraction is separated from the traditional formulation and the eluate is substantially the solvent. This is confirmed by the absence of any medicament content in the eluent by suitable methods.

4. Then the column is charged with non-polar solvents to remove the unwanted Non-Polar lipid fraction from the column until the eluate is substantially the solvent.

5. The absence of any medicament content in this fraction is ascertained by suitable methods.

6. The collected eluents of the above separation process are evaporated to remove the solvents.

7. The residual portion contained in the non-polar solvent fraction is discarded which contains the removed Non-Polar lipid fraction and does not contain active medicament and the absence of the medicament in this residue is confirmed by HPTLC, HPLC and GC or other suitable analytical methods.

8. The residual portion contained in the polar fraction contains the active medicament content along with the minimum Polar lipid content and the presence of the total medicament content is confirmed and relatively quantified by the HPTLC chromatogram in comparison with that of original formulation.

As per the invention the column shall be open or closed tubular columns as used in column chromatography or HPLC and the dimension of the column can be of predetermined dimensions used in column chromatography and HPLC. In accordance with the invention the active constituents shall be polar drugs, neutraceuticals, synthetic chemicals, cosmetics or combination thereof. The particle size of the polar/non-polar adsorbent material shall ranges from 30-400 mesh. The flow rate of elution is 1ml per minute to 5000 litres per hour. According to the invention the process of preparing improved lipid based composition further comprises of formulating the collected residue of above processes in to dosage forms such as tablets, soft gel capsules, microencapsules, powders, solutions, suspensions or emulsions.

As per the invention the residue obtained by the above processes can be administered externally or internally as it is, or after formulating suitably into dosage forms such as tablets, soft gel capsules, microencapsules, powders, solutions, suspensions or emulsions.

By the above methods, varying percentages of the Non-Polar lipids are removed by altering the volume of solvents. According to the present invention the lipid content of the lipid based composition can be reduced by any of the above processes to obtain the improved formulations of lipid based composition, as they involve the same principle.

In this invention, the ratio of the material to be delivered vis-a-vis the lipid content is substantially increased. The improved formulation of the lipid based composition with very high drug to fat percentage can be obtained by the above processes.

As per the invention the traditional parent lipid based composition is a formulation prepared out of natural fixed oils of plant and/or animal origin like sesame oil, coconut oil, castor oil, Neem oil, mustard oil, ghee, butter, milk, animal fat etc or mixtures there-of. The active constituent present is herbal constituents (Plant parts) like leaves, barks, roots fruits, seeds, rhizomes or minerals or other natural substances or mixtures thereof (such as in the case of Ayurvedic, Siddha, Unani preparations like Ghritams, Tailams, and other medicated oil and fat preparations described in traditional Indian systems of medicine),In accordance with the invention the active constituent of the lipid based fraction is active medicament.

As per the invention the parent lipid based composition is prepared as per the methods described in traditional medical literature with active constituent comprise of herbal or animal based natural material, synthetic substances, derivatives, cosmetics, neutraceuticals or combination thereof.

In another preferred embodiment the present invention shall discloses an improved lipid based composition produced by the above process, comprising of increased concentration of plurality of active constituents and/or decreased concentration of plurality of fat constituent compared to traditionally prepared parent lipid based compositions.

In another preferred embodiment the present invention shall discloses an improved lipid based formulation prepared using improved lipid based composition.

The improved lipid based composition shall be in solid form such as tablets, soft gel capsules, microencapsules or powders or a liquid form such as solutions, suspensions or emulsions.

According to the invention the ratio of the polar lipid fraction to non-polar lipid fraction of the improved lipid based composition shall ranges from 1:99 to 90:10.

Example 1:

Brahmi Ghritam 100gms 120 ml is taken as the base.

A glass column of 30 cm X 13 cm is taken and packed with silica gel for normal phase chromatography using petroleum ether. The measured quantity of Brahmi Ghritam is added to 50 ml of petroleum ether and charged to the column. 50 ml of Petroleum ether is then charged at the top and is allowed to pass through the column and is collected at the bottom. The column is then flushed with 200 ml of alcohol and the same is collected at the bottom. The two fractions are separately evaporated to remove the solvents. The petroleum ether fraction is seen to weigh 51.70 gm and the alcohol fraction is seen to weigh 45.15 gm. They are subjected to HPTLC examination and the pet ether fraction is seen to contain only the ghee, while the alcohol fraction is seen to contain the medicaments contained in the Ghritam.

The same experiment is repeated with different volumes of Petroleum ether as indicated in the table below and is seen to separate out varying amounts of Non-Polar lipid fractions and leave varying levels of Polar lipid fractions in the column to be further extracted by polar solvents.

The residual fraction A which is unwanted lipid is discarded and fraction B which is medicament with polar lipid is heated with stirring to remove all solvent residues. The final stable product is then tested for absence of solvent residues and the presence of the total medicament content. It may be consumed as it is or in a solid form (e.g., as tablets, or soft gel capsules or microencapsules or powders) or in a liquid form (e.g., as solutions, suspensions or emulsions).

Example 2

Name : ARAGWADHADI GHRITAM.
Experiment No : AVN/R&D/FP/GC001.
Date : 14-Nov-2008.
Batch No : 2495
SEPARATION OF ABIs:
Column : Silica gel (60-120 Mesh) : 130g.
Column Size : Height; 30cm, Diameter; 13 cm. Solvents : Petroleum Ether, Alcohol. Sample size : 120ml or 100gm.

The residual fraction A which is unwanted lipid is discarded and fraction B which is medicament with polar lipid is heated with stirring to remove all solvent residues. The final stable product is then tested for absence of solvent residues and the presence of the total medicament content. It may be consumed as it is or in a solid form (e.g., as tablets or soft gel capsules or microencapsules or powders) or in a liquid form (e.g., as solutions, suspensions or emulsions).

WE CLAIM:

1. A process for preparing improved lipid based composition by reducing the concentration of plurality of fat constituent characterized by increased concentration of plurality of active constituents and/or decreased concentration of plurality of fat constituent compared to traditionally prepared parent lipid based compositions, wherein the said process comprises of following steps and sequences:

a. mixing the said lipid based composition with atleast one solvent to form a mixture wherein the said lipid based composition is dissolved in the said solvent,

b. introducing the said mixture of step (a) through a column packed with atleast one adsorbent material having a reversal of polarity with the said solvent of step a, wherein a fraction of the lipid based composition is adsorbed by the said adsorbent material and another fraction remains unadsorbed,

c. eluting the said unadsorbed fraction in the said column, with alteast one solvent having a reversal of polarity with that of the said adsorbent for plurality of runs until the eluate is substantially the solvent,

d. Collecting the eluate of step c from the column in each run,

e. eluting the said adsorbed fraction from the said column with atleast one solvent having polarity similar to that of the said adsorbent for plurality of runs until the eluate is substantially the solvent,

f. collecting the eluate of step (e) from the column in each run,

g. comparing the concentration of active constituents and fat constituents in each of the eluates of step(d) and step (f)

h. selecting the eluate having higher concentration of active constituents from step (g) which eluate may include a part of fat constituents

i. discarding the eluate from step (g) which substantially includes fat constituents

j. evaporating the solvent from the eluate selected in step (h),

k. Collecting the residue of evaporation of step (j) as the final product

2. A process for preparing improved lipid based composition by reducing the concentration of plurality of fat constituent characterized by increased concentration of plurality of active constituents and/or decreased concentration of plurality of fat constituent compared to traditionally prepared parent lipid based compositions, wherein the said process comprises of following steps and sequences:

a. mixing the said lipid based composition with atleast one non-polar solvent to form a mixture wherein the said lipid based composition is dissolved in the said non-polar solvent,

b. introducing the said mixture of step (a) through a column packed with atleast one polar adsorbent material wherein a fraction of the lipid based composition is adsorbed by the said polar adsorbent material and another fraction remains unadsorbed,

c. eluting the said unadsorbed fraction in the said column, with alteast one non-polar solvent for plurality of runs until the eluate is substantially the solvent,

d. discarding the eluate of step (c) comprising of substantially fat constituents from the column in each run,

e. eluting the said adsorbed fraction from the said column with atleast one polar solvent for plurality of runs until the eluate is substantially the solvent,

f. collecting the eluate of step (e) comprising of substantially active constituents with very lower concentration of fat constituents from the column in each run,

g. evaporating the solvent from the eluate selected in step (f),

h. Collecting the residue of evaporation of step (g) as the final product

3. A process for preparing improved lipid based composition by reducing the concentration of plurality of fat constituent characterized by increased concentration of plurality of active constituents and/or decreased concentration of plurality of fat constituent compared to traditionally prepared parent lipid based compositions, wherein the said process comprises of following steps and sequences:

a. mixing the said lipid based composition with atleast one polar solvent to form a mixture wherein the said lipid based composition is dissolved in the said polar solvent,

b. introducing the said mixture of step (a) through a column packed with atleast one non-polar adsorbent material wherein a fraction of lipid based composition is adsorbed by the said non-polar adsorbent material and an another fraction remains unadsorbed,

c. eluting the said unadsorbed fraction in the said column, with alteast one polar solvent for plurality of runs until the eluate is substantially the solvent,

d. collecting the eluate of step (c) comprising of substantially active constituents with very lower concentration of fat constituents from the column in each run,

e. eluting the said absorbed fraction in the said column, with atleast one non polar solvent for plurality of runs until the eluate is substantially the solvent.

f. discarding the eluate of step (e) comprising of substantially fat constituents from the column in each run

g. evaporating the solvent from the eluate selected in step (d),

h. Collecting the residue of evaporation of step (e) as the final product.

4. The process as claimed in claim 1, 2 and 3 wherein the said active constituent is a polar drugs, Nutraceuticals, synthetic chemicals, cosmetics or combination thereof.

5. The process as claimed in claim 1 wherein the said solvent of step 1a may be a polar solvent or a non-polar solvent.

6. The process as claimed in claim 1 wherein the said adsorbent material may be a polar or non polar adsorbent material.

7. The said polar solvent of claim 2, 3 and 5 is selected from the group comprising of ethanol, methanol, dichloromethane, dimethyl formamide, dimethyl sulfoxide, tetrahydrofuran, Acetone, Acetonitrile, n-butanol, isopropanol, n-Propanol, formic acid, Acetic acid and water or combination thereof.

8. The said non-polar solvent of claim 2, 3 and 5 is selected from the group comprising of petroleum ether, pentane, cyclopentane, toluene, hexane, cyclohexane, 1,4-dioxane, benzene, chloroform, ethyl acetate, diethyl ether or combination thereof.

9. The said polar absorbent material of claim 2 and 6 is selected from the group comprising of silica based adsorbents, alumina, (either alkaline, or neutral, or acidic), kieselgur, charcoal, calcium carbonate or combination thereof.

10. The said non-polar absorbent material of claim 3 and 6 is selected from the group comprising of C18 (octadecylsilane), C8 (octyl), Cyanopropyl, Phenyl C4 (butyl), Hydrophobic interaction, C2 (ethyl), C1 (methyl) (silica based reverse phase columns) or combination thereof

11. The process as claimed in claim 1, 2 and 3 wherein the said column is open or closed tubular columns.

12. The process as claimed in claim 1, 2 and 3 wherein the particle size of the said adsorbent material ranges from 30-400 mesh.

13. The process as claimed in claim 1, 2 and 3 wherein the flow rate of elution is 1ml per minute to 5000 litres per hour.

14. The process as claimed in claim 1, 2 and 3 further comprises of formulating the collected residue of step 1k or 2h or 3h in to dosage forms such as tablets, soft gel capsules, microencapsules, powders, solutions, suspensions or emulsions.

15. A lipid based composition produced using the process of claim 1 or 2 or 3.

16. A lipid based formulation using the claimed lipid based composition of claim15.

Documents

Orders

Section Controller Decision Date

Application Documents

# Name Date
1 0773-che-2010 form-3 23-03-2010.pdf 2010-03-23
1 773-CHE-2010-Correspondence_13-01-2020.pdf 2020-01-13
2 0773-che-2010 form-1 23-03-2010.pdf 2010-03-23
2 773-CHE-2010-ExtendedHearingNoticeLetter-(DateOfHearing-04-12-2019).pdf 2019-11-08
3 773-CHE-2010-Correspondence to notify the Controller (Mandatory) [21-10-2019(online)].pdf 2019-10-21
3 0773-che-2010 description(provisional) 23-03-2010.pdf 2010-03-23
4 773-CHE-2010-Correspondence to notify the Controller (Mandatory) [17-10-2019(online)].pdf 2019-10-17
4 0773-che-2010 power of attorney 23-03-2010.pdf 2010-03-23
5 773-CHE-2010-HearingNoticeLetter-(DateOfHearing-04-12-2019).pdf 2019-10-14
5 0773-che-2010 form-2 23-03-2010.pdf 2010-03-23
6 773-CHE-2010-COMPLETE SPECIFICATION [08-12-2017(online)].pdf 2017-12-08
6 0773-che-2010 correspondence others 23-03-2010.pdf 2010-03-23
7 773-CHE-2010-FER_SER_REPLY [08-12-2017(online)].pdf 2017-12-08
7 0773-CHE-2010 FORM -5 18-08-2010.pdf 2010-08-18
8 Description(Complete) [14-06-2017(online)].pdf 2017-06-14
8 0773-CHE-2010 FORM -3 18-08-2010.pdf 2010-08-18
9 0773-CHE-2010 FORM -2 18-08-2010.pdf 2010-08-18
9 Description(Complete) [14-06-2017(online)].pdf_176.pdf 2017-06-14
10 0773-CHE-2010 FORM -1 18-08-2010.pdf 2010-08-18
10 Examination Report Reply Recieved [14-06-2017(online)].pdf 2017-06-14
11 0773-CHE-2010 DESCRIPTION (COMPLETE) 18-08-2010.pdf 2010-08-18
11 773-CHE-2010-FER.pdf 2017-06-09
12 0773-CHE-2010 CORRESPONDENCE OTHERS 18-08-2010.pdf 2010-08-18
12 773-CHE-2010 CORRESPONDENCE OTHERS 18-05-2012.pdf 2012-05-18
13 0773-CHE-2010 CLAIMS 18-08-2010.pdf 2010-08-18
13 773-CHE-2010 FORM-18 18-05-2012.pdf 2012-05-18
14 0773-CHE-2010 ABSTRACT 18-08-2010.pdf 2010-08-18
15 0773-CHE-2010 CLAIMS 18-08-2010.pdf 2010-08-18
15 773-CHE-2010 FORM-18 18-05-2012.pdf 2012-05-18
16 0773-CHE-2010 CORRESPONDENCE OTHERS 18-08-2010.pdf 2010-08-18
16 773-CHE-2010 CORRESPONDENCE OTHERS 18-05-2012.pdf 2012-05-18
17 773-CHE-2010-FER.pdf 2017-06-09
17 0773-CHE-2010 DESCRIPTION (COMPLETE) 18-08-2010.pdf 2010-08-18
18 Examination Report Reply Recieved [14-06-2017(online)].pdf 2017-06-14
18 0773-CHE-2010 FORM -1 18-08-2010.pdf 2010-08-18
19 0773-CHE-2010 FORM -2 18-08-2010.pdf 2010-08-18
19 Description(Complete) [14-06-2017(online)].pdf_176.pdf 2017-06-14
20 0773-CHE-2010 FORM -3 18-08-2010.pdf 2010-08-18
20 Description(Complete) [14-06-2017(online)].pdf 2017-06-14
21 0773-CHE-2010 FORM -5 18-08-2010.pdf 2010-08-18
21 773-CHE-2010-FER_SER_REPLY [08-12-2017(online)].pdf 2017-12-08
22 0773-che-2010 correspondence others 23-03-2010.pdf 2010-03-23
22 773-CHE-2010-COMPLETE SPECIFICATION [08-12-2017(online)].pdf 2017-12-08
23 0773-che-2010 form-2 23-03-2010.pdf 2010-03-23
23 773-CHE-2010-HearingNoticeLetter-(DateOfHearing-04-12-2019).pdf 2019-10-14
24 0773-che-2010 power of attorney 23-03-2010.pdf 2010-03-23
24 773-CHE-2010-Correspondence to notify the Controller (Mandatory) [17-10-2019(online)].pdf 2019-10-17
25 773-CHE-2010-Correspondence to notify the Controller (Mandatory) [21-10-2019(online)].pdf 2019-10-21
25 0773-che-2010 description(provisional) 23-03-2010.pdf 2010-03-23
26 773-CHE-2010-ExtendedHearingNoticeLetter-(DateOfHearing-04-12-2019).pdf 2019-11-08
26 0773-che-2010 form-1 23-03-2010.pdf 2010-03-23
27 773-CHE-2010-Correspondence_13-01-2020.pdf 2020-01-13
27 0773-che-2010 form-3 23-03-2010.pdf 2010-03-23

Search Strategy

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