DESC:FIELD
The present disclosure relates to an anti-inflammatory composition and a process for its preparation.
DEFINITIONS
As used in the present disclosure, the following terms are generally intended to have the meaning as set forth below, except to the extent that the context in which they are used indicates otherwise.
Bioactive substance refers to a substance when administered will exert an effect upon a living organism, tissue, or cell to provide beneficial physiological, behavioural, and immunological effects.
Galactomannan-rich fenugreek fibers refer to de-bittered fenugreek dietary fiber or fenugreek mucilage or fenugreek gum which is free from phytochemicals, saponins, amino acids, alkaloids, polyphenols, and flavonoids, but rich in galactomannans.
Therapeutically effective amount refers to the amount of the composition which can provide the desired effect when administered to subjects/patients, without leading to undesired adverse effects.
Unformulated physical mixture refers to the preparation of the composition by adding all the components of the composition together followed by simple mixing/blending.
Terpenoids refer to the class of chemical compounds having isoprene units. Terpenoids are terpenes that have had their methyl groups modified by oxygen containing functional groups. Terpenoids are classified into monoterpenoids, diterpenoids, sesquiterpenoids, hemiterpenoids, diterpenoids, sesterterpenoids, triterpenoids, tetraterpenoids, and polyterpenoids depending on their isoprene units. The analogue terpenes are hydrocarbons and include isoprenes, monoterpenes, sesquiterpenes, diterpenes, sesterterpenes, triterpenes, tetraterpenes, and polyterpenes.
Fenugreek mucilage refers to a gel-like substance obtained from soaking fenugreek seeds in water. Rich in polysaccharides, especially galactomannan, it exhibits notable viscosity and adhesive qualities.
BACKGROUND
The background information herein below relates to the present disclosure but is not necessarily prior art.
Inflammation is a key biological response and expression in most acute and chronic disease processes, induced by allergies, infection, tissue injury, metabolic factors, immunologically mediated diseases, malignancies, and the like. It is a protective attempt by the human body to remove harmful stimuli and initiate the healing process. The immunocytes of white blood cells of the body help to protect from micro-organisms (bacteria, viruses, and the like) and foreign substances.
Treatment and management of inflammation is an important and growing area of biomedical research and healthcare, inflammation is one of the primary drivers of many medical disorders and autoimmune diseases.
Several synthetic small molecules are available for the treatment of inflammation. However, these small molecules are associated with adverse effects on prolonged use. Alternatively, several bioactive substances, especially phytochemicals and extracts, are available that possess anti-inflammatory activity. However, these bioactive substances are associated with several drawbacks such as poor solubility, poor bioavailability, and hence requires high amount of dosage. Furthermore, achieving a food-grade status for many bioactive substances becomes challenging due to the frequent necessity of using synthetic ingredients with notable side effects or adverse events. Additionally, majority of these bioactive substances are unsuitable for various dosage forms.
Therefore, there is felt a need to provide an anti-inflammatory formulation that mitigates the drawbacks mentioned herein above or at least provides an alternative solution.
OBJECTS
Some of the objects of the present disclosure, which at least one embodiment herein satisfies, are as follows:
An object of the present disclosure is to ameliorate one or more problems of the background or to at least provide a useful alternative.
Another object of the present disclosure is to provide an anti-inflammatory composition.
Yet another object of the present disclosure is to provide an anti-inflammatory composition that relieves pain in musculoskeletal disorders such as back pain, joint pain, exhaustive exercise, muscle sprain, and to reduce systemic inflammation markers like C-reactive proteins and the like.
Still another object of the present disclosure is to provide a composition that reduces the stiffness of the joints and improves flexibility in subjects suffering from arthritis.
Another object of the present disclosure is to provide an anti-inflammatory composition that is safe and effective.
Another objective of the present invention is to provide a synergetic composition that enhances the efficacy of the bioactive substances.
Yet another object of the present disclosure is to provide an anti-inflammatory composition that is highly soluble, stable and provides enhanced efficacy.
Still another object of the present disclosure is to provide an anti-inflammatory composition that reduces the dosage of the bioactive substance.
Another object of the present disclosure is to provide an anti-inflammatory composition with enhanced bioavailability, and longer elimination half-life for the bioactive substances.
Yet another object of the present disclosure is to provide an anti-inflammatory composition without using synthetic additives.
Still another object of the present disclosure is to provide an anti-inflammatory composition that can be administered orally.
Yet another object of the present disclosure is to provide a process for the preparation of the anti-inflammatory composition that is safe, simple, easy to prepare, easy to scale up, and economical.
Other objects and advantages of the present disclosure will be more apparent from the following description, which is not intended to limit the scope of the present disclosure.
BRIEF DESCRIPTION OF THE ACCOMPANYING DRAWING
The present disclosure will now be described with the help of the accompanying drawing, in which:
Figure 1 illustrates a percent inhibition in paw edema upon treatment with diclofenac, unformulated quercetin (UQ), unformulated Boswellia extract (UB), unformulated physical mixture (Q+B+CL: a blend of Quercetin, Boswellia extract, and 1,8-Cineol), co-delivery formulation of Quercetin and Boswellia extract (F-Q+B) and the co-delivery composition of the present disclosure (F-Q+B+CL); and
Figure 2 illustrates a percent inhibition in paw edema upon treatment with diclofenac, unformulated palmitoylethanolamide (UP), unformulated Boswellia extract (UB), unformulated physical mixture (P+B+CL: blend of palmitoylethanolamide, Boswellia extract, and 1,8-Cineol), co-delivery formulation of Palmitoylethanolamide and Boswellia extract (F-P+B) and the co-delivery composition of the present disclosure (F-P+B+CL).
DETAILED DESCRIPTION
The present disclosure relates to an anti-inflammatory composition and a process for its preparation.
Embodiments, of the present disclosure, will now be described with reference to the accompanying drawing.
Embodiments are provided so as to thoroughly and fully convey the scope of the present disclosure to the person skilled in the art. Numerous details are set forth, relating to specific components, and methods, to provide a complete understanding of embodiments of the present disclosure. It will be apparent to the person skilled in the art that the details provided in the embodiments should not be construed to limit the scope of the present disclosure. In some embodiments, well-known processes, well-known apparatus structures, and well-known techniques are not described in detail.
The terminology used, in the present disclosure, is only for the purpose of explaining a particular embodiment and such terminology shall not be considered to limit the scope of the present disclosure. As used in the present disclosure, the forms "a,” "an," and "the" may be intended to include the plural forms as well, unless the context clearly suggests otherwise. The terms "comprises," "comprising," “including,” and “having,” are open-ended transitional phrases and therefore specify the presence of stated features, integers, steps, operations, elements, modules, units, and/or components, but do not forbid the presence or addition of one or more other features, integers, steps, operations, elements, components, and/or groups thereof. The particular order of steps disclosed in the method and process of the present disclosure is not to be construed as necessarily requiring their performance as described or illustrated. It is also to be understood that additional or alternative steps may be employed.
As used herein, the term "and/or" includes any and all combinations of one or more of the associated listed elements.
The terms first, second, third, etc., should not be construed to limit the scope of the present disclosure as the aforementioned terms may be only used to distinguish one element, component, region, layer or section from another component, region, layer or section. Terms such as first, second, third etc., when used herein do not imply a specific sequence or order unless clearly suggested by the present disclosure.
Several small molecules are available for the treatment of inflammation. However, these small molecules are associated with adverse effects on prolonged use. Alternatively, several bioactive substances are available that possess anti-inflammatory activity. However, these bioactive substances are associated with several drawbacks such as poor solubility, poor bioavailability, requires high amounts of dosage, use of synthetic ingredients, not being available in user-friendly dosage forms, and the like.
The present disclosure envisages an anti-inflammatory composition and a process for its preparation. The anti-inflammatory composition of the present disclosure has enhanced efficacy, avoids adverse effects, and is made of GRAS (Generally Recognized as Safe) ingredients.
In an aspect of the present disclosure, there is provided an anti-inflammatory composition.
The anti-inflammatory composition comprises a) at least one bioactive substance in an amount in the range of 10 wt% to 60 wt% by the total weight of the composition; b) at least one plant extract in an amount in the range of 10 wt% to 60 wt% by the total weight of the composition; c) at least one terpenoid/terpene in an amount in the range of 1 wt% to 5 wt% by the total weight of the composition; d) at least one plant fiber in an amount in the range of 15 wt% to 50 wt% by the total weight of the composition; and e) optionally at least one emulsifying agent in an amount in the range of 5 wt% to 35 wt% by the total weight of the composition.
In an embodiment of the present disclosure, the bioactive substance is at least one selected from quercetin, palmitoylethanolamide (PEA), and curcumin.
In accordance with an embodiment of the present disclosure, the bioactive substances further include flavonoids and flavonols.
In an embodiment of the present disclosure, the plant extract is at least one selected from Boswellia (Boswellia serrata) extract, guggul extract (Commiphora wightii), and Ginger (Zingiber officinale) extract.
In an embodiment of the present disclosure, the terpenoids/terpenes are at least one selected from ß-caryophyllene, 1,8-cineole, a-thujene, turmerones, and carvacrol.
In an embodiment of the present disclosure, the plant fiber is at least one selected from galactomannan rich fenugreek fiber, glucomannan, and arabinoxylan.
In an embodiment of the present disclosure, the galactomannan rich fenugreek fiber is hydrolyzed galactomannan rich fenugreek fiber.
In accordance with the embodiments of the present disclosure, the galactomannan-rich fenugreek fiber can be isolated from dried and matured fenugreek seeds by a mechanical process involving milling, sieving, gravity separation, grinding, and sieving. Fenugreek fiber can be then uniformly powdered to 74 microns to 170 microns size and is used in the composition of the present disclosure.
In accordance with the embodiments of the present disclosure, the galactomannan content in galactomannan rich fenugreek fibers is in the range of 15% to 47%.
In an embodiment of the present disclosure, the galactomannan rich fenugreek fiber is in the form of fenugreek mucilage.
In an embodiment of the present disclosure, the plant fiber can hold water in an amount in the range of 10 mL/g to 50 mL/g.
In an embodiment of the present disclosure, the emulsifying agent is at least one selected from lecithin, quillaja extract, and sugar esters such as polysorbate.
In another aspect of the present disclosure, there is provided a process for the preparation of the anti-inflammatory composition.
The process is described in detail.
In a first step, a predetermined amount of bioactive substance and plant extract are mixed to obtain a first mixture.
In an embodiment of the present disclosure, the bioactive substance is at least one selected from quercetin, palmitoylethanolamide (PEA), and curcumin.
In an embodiment of the present disclosure, the plant extract is at least one selected from Boswellia extract, guggul extract, and Ginger extract.
In an embodiment of the present disclosure, the Boswellia extract comprises boswellic acid in the range of 30% to 60%.
In a second step, the first mixture is mixed with first fluid medium followed by adding emulsifying agent under stirring to obtain a second mixture.
In an embodiment of the present disclosure, the first fluid medium is at least one selected from ethanol, water, ethanol/water.
In an embodiment of the present disclosure, the emulsifying agent is at least one selected from lecithin, quillaja extract, and sugar esters such as polysorbate.
In a third step, the second mixture is homogenized to obtain a third mixture.
In an embodiment of the present disclosure, the homogenization is selected from ultrasound sonication and pressure homogenization.
In a fourth step, the third mixture is mixed with a second fluid medium to obtain a fourth mixture.
In an embodiment of the present disclosure, the second fluid medium is at least one selected from ethanol, water, and ethanol/water.
In a fifth step, the first portion of fiber (hydrolyzed galactomannans) is mixed with a third fluid medium to obtain a fifth mixture.
In an embodiment of the present disclosure, the first portion of fiber comprises hydrolyzed galactomannans.
In a sixth step, the fifth mixture is mixed with the fourth mixture under stirring for a predetermined time period followed by evaporation to obtain a seventh mixture.
In an embodiment of the present disclosure, the evaporation at a temperature in the range of 50° to 60°C at >620 mm of Hg pressure.
In a seventh step, the fenugreek mucilage is mixed with water followed by adding terpene to obtain a eighth mixture.
In a final step, the seventh and eighth mixtures are mixed and followed by drying to obtain anti-inflammatory composition.
In an embodiment of the present disclosure, the drying is selected from spray drying, vacuum drying, and freeze drying.
In an embodiment of the present disclosure, the spray drying is performed at an inlet temperature in the range of 170°C to 190°C and an outlet temperature in the range of 85°C to 95°C.
In an embodiment of the present disclosure, the vacuum drying is performed at a temperature in the range of 50°C to 60°C and a pressure in the range of 620 mm of Hg to 720 mm of Hg.
In an embodiment of the present disclosure, the freeze drying is performed at a temperature in the range of -20°C to -60°C, followed by evaporation of ice by sublimation in the range of 50°C to 60°C and at a pressure in the range of 500 mm of Hg to 900 mm of Hg.
In accordance with the embodiments of the present disclosure, the composition possesses anti-inflammatory activity and analgesic activity.
In accordance with the embodiments of the present disclosure, the anti-inflammatory composition comprising at least one bioactive substance, at least one plant extract, at least one terpenoid/terpenes along with plant fibers, and optionally at least one emulsifier, provides a synergistic effect by enhancing the therapeutic efficacy of the bioactive substance.
In accordance with the embodiments of the present disclosure, the galactomannan rich fenugreek fibers act as a coating over the water insoluble bioactive substances and plant extracts to convert them into soluble dosage forms, thus enhancing stability and bioavailability.
In accordance with the embodiments of the present disclosure, the anti-inflammatory composition of the present disclosure can be in the form of a powder, granule, tablet, solution, gummies, gels, or capsules. Other known suitable forms can also be prepared.
In accordance with the embodiment of the present disclosure, the anti-inflammatory composition of the present disclosure when administered to humans at a therapeutically effective amount provides the desired anti-inflammatory effect.
In accordance with the embodiments of the present disclosure, the anti-inflammatory composition of the present disclosure can be suitably administered orally.
In accordance with the embodiments of the present disclosure, the anti-inflammatory composition of the present disclosure is useful in the treatment of inflammation, pain, joint health, exercise induced pain, dysmenorrhea, headache, body pain, morning sickness, and joint pain due to arthritic conditions.
In another aspect, the present disclosure envisages a process for the preparation of the anti-inflammatory composition.
In accordance with the embodiments of the present disclosure, the process of preparing the anti-inflammatory composition is safe, simple, easy to prepare, easy to scale up, stable, and economical.
The foregoing description of the embodiments has been provided for purposes of illustration and is not intended to limit the scope of the present disclosure. Individual components of a particular embodiment are generally not limited to that particular embodiment but are interchangeable. Such variations are not to be regarded as a departure from the present disclosure, and all such modifications are considered to be within the scope of the present disclosure.
The present disclosure is further described in light of the following experiments, which are set forth for illustration purposes only, and not to be construed as limiting the scope of the disclosure. The following experiments can be tested to scale up to an industrial/commercial scale and the results obtained can be extrapolated to the industrial scale.
EXPERIMENTAL DETAILS
Experiment-1: Preparation of the anti-inflammatory composition in accordance with the present disclosure
36 g of quercetin and 12 g of Boswellia extract are blended to obtain a first mixture. 1000 mL of ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 25 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 to 10 min at 1000 KW with the duration of pulses from 3 to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 10 gm of hydrolyzed galactomannans were mixed with 100 ml of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture (bioactive substance).
Separately, 10 gm of fenugreek mucilage was mixed with 300 ml of water followed by adding 4 gm of 1,8-cineol to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the anti-inflammatory (co-delivery) composition of the present disclosure (F-Q+B+CL).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 35% of quercetin, 10% of boswellic acid, and 3% of 1,8-cineol.
Experiment-2: Preparation of the anti-inflammatory composition in accordance with the present disclosure
41 g of palmitoylethanolamide and 17 g of Boswellia extract are blended to obtain a first mixture. 1000 mL of ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 17 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 to 10 min at 1000 KW with the duration of pulses from 3 to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 10 g of hydrolysed galactomannans were mixed with 100 mL of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture (bioactive substance).
Separately, 10 gm of fenugreek mucilage was mixed with 300 mL of water followed by adding 5 g of 1,8-cineol to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the anti-inflammatory (co-delivery) composition of the present disclosure (F-P+B+CL).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 40% of palmitoylethanolamide, 10% of boswellic acid, and 3% of 1,8-cineol.
Experiment-3: Preparation of the anti-inflammatory composition in accordance with the present disclosure
41 g of palmitoylethanolamide and 17 g of Boswellia extract are blended to obtain a first mixture. 1000 mL of ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 17 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 to 10 min at 1000 KW with the duration of pulses from 3 to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 10 g of hydrolysed galactomannans were mixed with 100 mL of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture (bioactive substance).
Separately, 10 gm of fenugreek mucilage was mixed with 300 mL of water followed by adding 5 g of ß-caryophyllene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the anti-inflammatory (co-delivery) composition of the present disclosure (F-P+B+BC).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 40% of palmitoylethanolamide, 10% of boswellic acid, and 3% of ß-caryophyllene.

Experiment-4: Preparation of the anti-inflammatory composition in accordance with the present disclosure
38 g of quercetin and 22 g of Boswellia extract are blended to obtain a first mixture. 1000 mL ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 15 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to homogenization at 400 to 700 bar pressure to obtain a third mixture. To the third mixture, 100 mL of ethanol was added to obtain a fourth mixture.
Separately 10 g of hydrolysed galactomannans were mixed with 100 mL of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated at 50 oC to 60oC to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture (bioactive substance).
Separately, 10 g of fenugreek mucilage was mixed with 300 mL of water followed by adding 5 g of a –Thujene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the anti-inflammatory (co-delivery) composition of the present disclosure (F-Q+B+aT).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 35% of quercetin, 10% of boswellic acid and 3% of aThujene.
Experiment-5: Preparation of the anti-inflammatory composition in accordance with the present disclosure
38 g of quercetin and 22 g of Boswellia extract are blended to obtain a first mixture. 1000 mL ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 15 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to homogenization at 400 to 700 bar pressure to obtain a third mixture. To the third mixture, 100 mL of ethanol was added to obtain a fourth mixture.
Separately 10 g of hydrolysed galactomannans were mixed with 100 mL of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated at 50oC to 60oC to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture (bioactive substance).
Separately, 10 g of fenugreek mucilage was mixed with 300 mL of water followed by adding 5 g of ß-caryophyllene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the anti-inflammatory (co-delivery) composition of the present disclosure (F-Q+B+BC).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 35% of quercetin, 10% of boswellic acid, and 3% of ß-caryophyllene.
Experiment-6: Preparation of the anti-inflammatory composition in accordance with the present disclosure
41 g of palmitoylethanolamide and 12 g of guggul extract are blended to obtain a first mixture. 1000 mL ethanol/water (90/10 v/v) was mixed with the first mixture followed by adding 22 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 min to 10 min at 1000 KW with the duration of pulses from 3 seconds to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 10 gm of hydrolysed galactomannans were mixed with 100 ml of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture (bioactive substance).
Separately, 10 gm of fenugreek mucilage was mixed with 300 ml of water followed by adding 5 gm of ß-caryophyllene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the co-delivery composition of the present disclosure (F-P+Gu+BC).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 40% of palmitoylethanolamide, 10% of Guggul extract and 3% of ß-caryophyllene.
Experiment-7: Preparation of the anti-inflammatory composition in accordance with the present disclosure
43 g of Quercetin and 20 g of Ginger extract are blended to obtain a first mixture. 1000 mL ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 12 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 to 10 min at 1000 KW with the duration of pulses from 3 to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 10 gm of hydrolysed galactomannans were mixed with 100 ml of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture (bioactive substance).
Separately, 10 gm of fenugreek mucilage was mixed with 300 ml of water followed by adding 5 gm of ß-caryophyllene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the co-delivery composition of the present disclosure (F-Q+Gi+BC).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 40% of quercetin, 10% of Ginger extract, and 3% of ß-caryophyllene.
Experiment-8: Preparation of the anti-inflammatory composition in accordance with the present disclosure
21 g of palmitoylethanolamide and 44 g of Boswellia extract are blended to obtain a first mixture. 1000 mL ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 10 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 to 10 min at 1000 KW with the duration of pulses from 3 to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 10 gm of hydrolysed galactomannans were mixed with 100 ml of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture.
Separately, 10 gm of fenugreek mucilage was mixed with 300 ml of water followed by adding 5 gm of ß-caryophyllene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the co-delivery composition of the present disclosure (F-P+B+BC).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 20% of palmitoylethanolamide, 20% of Boswellic acid and 3% of ß-caryophyllene.

Experiment-9: Preparation of the anti-inflammatory composition in accordance with the present disclosure
21 g of palmitoylethanolamide and 22 g of guggul extract are blended to obtain a first mixture. 1000 mL ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 22 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 to 10 min at 1000 KW with the duration of pulses from 3 to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 15 gm of hydrolysed galactomannans were mixed with 100 ml of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture.
Separately, 15 gm of fenugreek mucilage was mixed with 300 ml of water followed by adding 5 gm of ß-caryophyllene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the co-delivery composition of the present disclosure (F-P+Gu+BC).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 20% of palmitoylethanolamide, 22% of Guggul extract and 3% of ß-caryophyllene.
Experiment-10: Preparation of the anti-inflammatory composition in accordance with the present disclosure
21 g of Quercetin and 44 g of Boswellia extract are blended to obtain a first mixture. 1000 mL ethanol/water (92/8 v/v) was mixed with the first mixture followed by adding 10 g of lecithin under stirring to obtain a second mixture. The so obtained second mixture was subjected to ultrasound sonication for 5 to 10 min at 1000 KW with the duration of pulses from 3 to 5 seconds to obtain a third mixture. To the third mixture, 100 ml of ethanol was added to obtain a fourth mixture.
Separately 10 gm of hydrolysed galactomannans were mixed with 100 ml of water to obtain a fifth mixture. The so obtained fifth mixture was slowly added to the fourth mixture by stirring for 6 hours to obtain a sixth mixture. The sixth mixture was evaporated to obtain a seventh mixture. During the evaporation process, galactomannans form a coating/matrix on the sixth mixture.
Separately, 10 gm of fenugreek mucilage was mixed with 300 ml of water followed by adding 5 gm of ß-caryophyllene to obtain an eighth mixture. The seventh mixture was mixed with the eighth mixture to obtain a homogeneous mixture. The homogeneous mixture was spray-dried to obtain the co-delivery composition of the present disclosure (F-Q+B+BC).
The key ingredients in the final composition were evaluated using HPLC. The composition comprises 20% of quercetin, 10% of Boswellic acid and 3% of ß-caryophyllene.
Experiment-11: Evaluation of the anti-inflammatory composition of the present disclosure
The efficacy of the various anti-inflammatory compositions (Experiments 1 to 10) of the present disclosure was evaluated on Sprague Dawley rats. Carrageenan was administered into the paw of Sprague Dawley rats to induce inflammation. The early phase of inflammation was mediated by histamine, serotonin, and increased synthesis of prostaglandins. The later phase involves prostaglandin release mediated by the tissue macrophages.
The anti-inflammatory effect of the co-delivery composition of the present disclosure (F-Q+B+CL) was evaluated by comparing it with unformulated quercetin (UQ), unformulated Boswellia extract (UB), unformulated physical mixture (Q+B+CL: a blend of Quercetin, Boswellia extract, and 1,8-Cineol), and co-delivery formulation of Quercetin and Boswellia extract (Q+B).
Experimental procedure: Male adult Sprague Dawley rats weighing 200 g to 250 g body weight (b.wt) were divided into six groups [each group has 3 rats (n=3)]. The base volume of the swollen right hind paws was measured by using a plethysmometer. After 40 minutes, a subcutaneous injection of 0.1 ml of 1% carrageenan was injected onto the plantar surface of the right hind paw of all rats. The volume of the swollen right hind paws was measured again. Each group of rats was administered orally with diclofenac (10 mg/Kg b.wt), unformulated quercetin (UQ) (50 mg/Kg b.wt), unformulated Boswellia extract (UB) (50 mg/Kg b.wt), The unformulated physical mixture (Q+B+CL: a blend of Quercetin, Boswellia extract, and 1,8-Cineol), co-delivery formulation of Quercetin and Boswellia extract as presented in this invention (Q+B) and the co-delivery composition of the present disclosure (F-Q+B+CL) were administered at a dose of 10, 25, and 50 mg/Kg b.wt.
Following the administration of respective compositions, the volume of the right hind paws of rats in all groups was measured for 3 hours at 1 hr intervals. The reduction in swelling volume was measured for each treatment group and the efficacy was deduced by measuring the % of inhibition of swelling.
The results among the multiple groups were analysed by using ANOVA. The inter-group comparisons were performed using paired t-tests within unformulated physical mixture Q+B+CL to the co-delivery formulations F-Q+B and F-Q+B+CL; and showed significant differences (P < 0.001) among the 10, 25, and 50 mg/Kg doses. It was observed that the composition of the present disclosure provided better inhibition compared to an unformulated physical mixture (P < 0.001). The results are illustrated in Figure 1.
Experiment-12: Evaluation of the anti-inflammatory composition of the present disclosure
The evaluation of the anti-inflammatory composition was conducted similar to experiment 11, wherein Quercetin was replaced with palmitoylethanolamide.
The results among the multiple groups were analysed by using ANOVA. The inter-group comparisons were performed using paired t-tests within unformulated physical mixture P+B+CL to the co-delivery formulations F-P+B and F-P+B+CL; and showed significant differences (P < 0.001) among the 10, 25, and 50 mg/Kg doses. It was observed that the composition of the present disclosure provided better inhibition compared to an unformulated physical mixture (P < 0.001). The results are illustrated in Figure 2.
Thus, the composition of the present disclosure provides enhanced efficacy in terms of anti-inflammatory action when compared with an unformulated physical mixture, diclofenac, and quercetin.
Experiment-13: Comparative Compositions
The efficacy of the composition of the present disclosure was compared with the compositions by altering the amount of the ingredients in the composition. The comparative compositions were prepared by using the process similar to Experiment 1.
The composition of the present disclosure and the comparative compositions (CP1 to CP8) were evaluated on Sprague Dawley rats by using a similar method to Experiment 11 and the reduction in swelling volume was measured for each treatment group and the efficacy was deduced by measuring the % of inhibition of swelling. The results are provided in Table 1 below

Table 1: Effect of various components and formulations on carrageen- induced paw-oedema inhibition in experimental rats (Anti-inflammatory effect).

TECHNICAL ADVANCEMENTS
The present disclosure described herein above has several technical advantages including, but not limited to, the realization of, an anti-inflammatory composition that:
• is stable, safe, and effective;
• synergistically composition enhances the anti-inflammatory activity of the bioactive substances;
• enhanced solubility in water;
• reduced the dosage of the bioactive substance;
• reduces the inflammation effectively;
• is useful in the treatment of inflammation, pain, and joint health;
• is suitable for the preparation of food substances such as gummies, sachets, gellies, liquid shots, and chocolates;
• is suitable for the preparation of pharmaceutical substances such as tablets, capsules, soft gels, and the like;
• is easy to administer through the oral route;
• contains only GRAS (Generally Recognized as Safe); and
• does not have any adverse effects;
a process for the preparation of the anti-inflammatory composition that is:
• easy to prepare, economical, and easy to scale up.
Throughout this specification, the word “comprise”, or variations such as “comprises” or “comprising, will be understood to imply the inclusion of a stated element, integer or step,” or group of elements, integers, or steps, but not the exclusion of any other element, integer or step, or group of elements, integers or steps.
The use of the expression “at least” or “at least one” suggests the use of one or more elements or ingredients or quantities, as the use may be in the embodiment of the invention to achieve one or more of the desired objects or results. While certain embodiments of the inventions have been described, these embodiments have been presented by way of example only, and are not intended to limit the scope of the inventions. Variations or modifications to the formulation of this invention, within the scope of the invention, may occur to those skilled in the art upon reviewing the disclosure herein. Such variations or modifications are well within the spirit of this invention.
The numerical values given for various physical parameters, dimensions and quantities are only approximate values and it is envisaged that the values higher than the numerical value assigned to the physical parameters, dimensions and quantities fall within the scope of the invention unless there is a statement in the specification to the contrary.
While considerable emphasis has been placed herein on the specific features of the preferred embodiment, it will be appreciated that many additional features can be added and that many changes can be made in the preferred embodiment without departing from the principles of the disclosure. These and other changes in the preferred embodiment of the disclosure will be apparent to those skilled in the art from the disclosure herein, whereby it is to be distinctly understood that the foregoing descriptive matter is to be interpreted merely as illustrative of the disclosure and not as a limitation
,CLAIMS:WE CLAIM
1. An anti-inflammatory composition comprising
a. at least one bioactive substance in an amount in the range of 10 wt% to 60 wt% by the total weight of the composition;
b. at least one plant extract in an amount in the range of 10 wt% to 60 wt% by the total weight of the composition;
c. at least one terpenoid/terpene in an amount in the range of 1 wt% to 5 wt% by the total weight of the composition;
d. at least one plant fiber in an amount in the range of 15 wt% to 50 wt% by the total weight of the composition; and
e. optionally at least one emulsifying agent in an amount in the range of 5 wt% to 35 wt% by the total weight of the composition.
2. The composition as claimed in claim 1, wherein said bioactive substance is at least one selected from quercetin, and palmitoylethanolamide (PEA).
3. The composition as claimed in claim 1, wherein said plant extract is at least one selected from Boswellia extract, guggul extract, and Ginger extract.
4. The composition as claimed in claim 1, wherein said terpenoids/terpenes is at least one selected from ß-caryophyllene, 1,8-cineole, a-thujene, and carvacrol.
5. The composition as claimed in claim 1, wherein said plant fiber is at least one selected from galactomannan rich fenugreek fiber, glucomannan, and arabinoxylan.
6. The composition as claimed in claim 1, wherein said galactomannan rich fenugreek fiber is hydrolyzed galactomannan rich fenugreek fiber.
7. The composition as claimed in claim 1, wherein said galactomannan rich fenugreek fiber is in the form of fenugreek mucilage.
8. The composition as claimed in claim 1, wherein said plant fiber can hold water in an amount in the range of 10 mL/g to 50 mL/g.
9. The composition as claimed in claim 1, wherein emulsifying agent is at least one selected from lecithin, quillaja extract, and sugar esters such as polysorbate.
10. The composition as claimed in claim 1, wherein the ratio of boswellic acid to bioactive substance is in the range of 1:1 to 1:4.
11. A process for the preparation of anti-inflammatory composition as claimed in claim 1, wherein said process comprises the following steps
a. mixing a predetermined amount of bioactive substance and plant extract to obtain a first mixture;
b. mixing said first mixture with a first fluid medium followed by adding emulsifying agent under stirring to obtain a second mixture;
c. homogenising said second mixture to obtain a third mixture;
d. mixing said third mixture with a second fluid medium to obtain a fourth mixture;
e. separately mixing first portion of with third fluid medium to obtain a fifth mixture;
f. mixing said fifth mixture with fourth mixture under stirring for a predetermined time period followed by evaporation to obtain a seventh mixture;
g. separately mixing fenugreek mucilage with water followed by adding terpenoid/terpene to obtain a eighth mixture;
h. mixing said seventh and said eighth mixture followed by drying to obtain the anti-inflammatory composition.
12. The process as claimed in claim 11, wherein said first fluid medium is at least one selected from ethanol, water, ethanol/water.
13. The process as claimed in claim 11, wherein said second fluid medium is at least one selected from ethanol, water, ethanol/water.
14. The process as claimed in claim 11, wherein said second fluid medium is at least one selected from ethanol, and water.
15. The process as claimed in claim 11, wherein the predetermined time period is in the range of 4 hours to 8 hours.
16. The process as claimed in claim 11, wherein the homogenization in step c) is selected from ultrasound sonication and pressure homogenization.
17. The process as claimed in claim 11, wherein said drying is spray drying, vacuum drying, and freeze drying.