Specification
FIELD OF THE INVENTION
[0001] The present invention generally relates to a herbal composition for the treatment of digestive disturbances. Particularly, the present invention relates to a herbal micro-emulsion composition comprising of Pluchealanceolata, Trigonellafoenum-graecum, d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and pharmaceutical^ acceptable carriersfor the treatment of digestive disturbances.
BACKGROUND OF THE INVENTION
[0002] Background description includes information that may be useful in understanding the present invention. It is not an admission that any of the information provided herein is prior art or relevant to the presently claimed invention, or that any publication specifically or implicitly referenced is prior art.
[0003] Drugs usually do not reach the target site easily and may get metabolized at non-target sites which may lead to complications. Delivery of drugs at the target site is dependent on various factors like solubility, thermodynamic stability etc. A lot of study goes into understanding the circulatory system and its interactions with the drug system while developing improved drug delivery systems. The innovative drug delivery systems must ensure targeted delivery in volumes as per the need of the individual. [0004] Micro-emulsions are stable, clear mixtures of oil, water and surfactants, occasionally also comprising co-surfactants and maybe water-in-oil or oil-in-water. They easily form solutions owing to the presence of surfactants which act at the interface of the two phases making them miscible. Micro-emulsions drug delivery system is stable, thermodynamically self-emulsifying delivery systems which could be used to improve efficacy of pharmacological active constituents owing to enhanced intestinal absorption. Micro-emulsions serve as super-solvents of drug which could solubilise hydrophilic as well as lipophilic drugs including drugs that are relatively insoluble in both aqueous and hydrophobic solvents. Micro-emulsions are fascinating and relatively potential formulation owing to superior solubilisation capacity, thermodynamic stability, high rate of diffusion as well as absorption, transparency, and simplicity in production in comparison to solvent without surfactant system (Wu et al., 2009, Jadhav et al., 2006).
[0005] Pluchealanceolata, family Asteracea is a perennial herb found in indo-gangetic plains. Its whole plant was found clinically effective as an ayurvedic medicine for treatment of variety of diseases such as arthritis, chronic inflammation of nervous muscular pains, laxative, analgesic, antipyretic, skin diseases, digestive disturbances like constipation, flatulence, indigestion and abdominal colic, respiratory problems like asthma, bronchitis and chest pain, (Srivastava et al., 2012).
[0006] Another herb, Trigonellafoenum-graecum, family fabaceaehas several therapeutic effects like carminative, gastric stimulant, antiulcer, anti-diabetic, hypocholesterolemic, hepatoprotective, anti-inflammatory, antioxidant, and antibacterial activity. [0007] There is a need in the art to discover novel compositions capable of providing improved efficacy over known pharmaceutical drugs and that can provide a stable, natural and economical alternative to these drugs. The present invention explores this idea using a novel combination of the two herbs Pluchealanceolata and Trigonellafoenum-graecum in a micro-emulsion composition.Development of novel drug delivery system of whole plant extract of Pluchealanceolata and Trigonellafoenum-graecum could successfully augment its therapeutic effects and could serve as versatile remedy for variety of diseases.
OBJECTS OF THE INVENTION
[0008] An object of the present invention is to provide an oral herbal micro-emulsion
composition of whole plant extract of Pluchealanceolata and Trigonellafoenum-graecu.
[0009] Another object of the present invention is to provide aherbal composition
having improved solubility, intestinal absorption, bioavailability and therefore, improved
therapeutic effects of herbal medicine.
[0010] Another object of the present invention is to provide a central composite
design (CCD) optimized composition to produce transparent micro-emulsion with optimum
viscosity and least globule size which could augment intestinal absorption, bioavailability and
therapeutic effects of herbal medicine.
[0011] Another object of the present invention is to provide a micro-emulsion
composition for the effective treatment of digestive ailments.
SUMMARY OF THE INVENTION
[0012] The present invention generally relates to a herbal composition for the treatment of digestive disturbances. Particularly, the present invention relates to a herbal micro-emulsion composition comprising of Pluchealanceolata, Trigonellafoenum-graecum, d-a-
Tocopheryl polyethylene glycol 1000 succinate (TPGS) and optionally pharmaceutically acceptable carriersfor the treatment of digestive disturbances.
[0013] In one aspect, the present invention relates to a herbal micro-emulsion composition comprising:
a) a extract of whole plant of Pluchealanceolata and Trigonellafoenum-
graecum;
b) d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS);
c) surfactant;
d) co-surfactant;
e) oil phase; and
f) optionally pharmaceutically acceptable carriers. In another aspect of the present invention, the surfactant of the herbal composition is selected from poloxamer 188, poloxamer 407 and poloxamer 338.
[0014] In another aspect of the present invention, the co-surfactant is selected from
polyethylene glycol 400 (PEG 400), polyethylene glycol 600 (PEG 600) and the like.
[0015] In yet another aspect of the present invention, the co-surfactant is polyethylene
glycol 400 (PEG 400) and polyethylene glycol 600 (PEG 600) in a ratio of 1:1.
[0016] In yet another aspect of the present invention, the oil phase is selected from
soybean oil.
[0017] In yet another aspect of the present invention, the composition comprises:
a) extract of whole plant of Pluchealanceolata and Trigonellafoenum-graecum in an amount ranges from 5% to 40% by weight by volume of the composition;
b) d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) in an amount ranges from 0.5% to 10% by weight by volume of the composition;
c) surfactant in an amount ranges from 5% to 40% by weight by volume of the composition;
d) co-surfactant in an amount ranges from 5% to 40% by weight by volume of the composition;
e) oil phase in an amount ranges from 5% to 60% by weight by volume of the composition; and
f) optionally pharmaceutically acceptable carriers 10% to 60% by weight of the composition.
[0018] In another aspect of the present invention, the herbal extract is present in a weight range of about 5% to about 20% weight by volume of the composition.
[0019] In another aspect of the present invention, TPGS is present in a weight range of
about 0.5% to about 2% weight by volume of the composition.
[0020] In another aspect of the present invention, the co-surfactant is present in a volume
range of about 7% to about 10% weight by volume of the composition.
[0021] In another aspect of the present invention, the oil phase is present in a weight
range of about 5% to about 40% weight by volume of the composition.
[0022] In another aspect of the present invention, the additional surfactant is present in a
weight range of about 10% to about 12% weight by volume of the composition.
[0023] In yet another aspect, the present invention relates to aherbal micro-emulsion
composition comprising:
a. a extract of whole plant of Pluchealanceolata and Trigonellafoenum-
graecumm 10% weight by volume of the composition;
b. d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) in 1.02% weight
by volume of the composition;
c. poloxamer 407 in 11.676% weight by volume of the composition;
d. soybean oil in 20% weight by volume of the composition; and
e. a 1:1 mixture of PEG 400 and PEG 600 in 9.555% volume by volume of the
composition.
[0024] In another aspect of the present invention, the herbal micro-emulsion composition is formulated in the form of a liquid, syrup, capsule or gel.
[0025] In another aspect of the present invention, the herbal micro-emulsion composition has a viscosity in the range of about 50milipascal second (mPa.s) to about 80 mPa.s. [0026] In another aspect of the present invention, the herbal micro-emulsion composition has a globule size in the range of about 80micrometer (um) to about 100 um. [0027] In another aspect, the present invention relates to a process of preparing a micro-emulsion composition comprising the steps of:
a. preparing an aqueous solution of a herbal extract of whole plant of
Pluchealanceolata and Trigonellafoenum-graecumm distilled water;
b. adding the aqueous solution drop-wise to a mixture of surfactant, co-surfactant
and oil; and
c. stirring the mixture with a magnetic stirrer at 1000 rpm and at a temperature of
37°C to produce a micro-emulsion.
[0028] In still another aspect of the present invention, the micro-emulsion composition is
used for the treatment of digestive ailments including constipation, flatulence, indigestion and
the like.
[0029] Various objects, features, aspects and advantages of the inventive subject matter
will become more apparent from the following detailed description of preferred
embodiments.
BRIEF DESCRIPTION OF THE ACCOMPANYING DRAWINGS
[0030] Figure 1: Contour (2D) and corresponding response surface plot (3D) showing the
effect of independent variables on viscosity (mPa.s) (Yl).
[0031] Figure 2: Contour (2D) and corresponding response surface plot (3D) showing the
effect of independent variables on globule size (um) (Y2).
[0032] Figure 3: Contour (2D) and corresponding response surface plot (3D) showing
desirability value for optimized herbal microemulsion.
[0033] Figure 4: Graphical representation showing composition of optimized herbal
micro-emulsion and values of response variables with desirability = 0.868.
[0034] Figure 5: Overlay and cube plot showing desirability value for optimized herbal
micro-emulsion.
DETAILED DESCRIPTION OF THE INVENTION
[0035] The following is a detailed description of embodiments of the disclosure. The embodiments are in such detail as to clearly communicate the disclosure. However, the amount of detail offered is not intended to limit the anticipated variations of embodiments; on the contrary, the intention is to cover all modifications, equivalents, and alternatives falling within the spirit and scope of the present disclosure as defined by the appended claims. [0036] Unless the context requires otherwise, throughout the specification which follow, the word "comprise" and variations thereof, such as, "comprises" and "comprising" are to be construed in an open, inclusive sense that is as "including, but not limited to." [0037] Reference throughout this specification to "one embodiment" or "an embodiment" means that a particular feature, structure or characteristic described in connection with the embodiment is included in at least one embodiment. Thus, the appearances of the phrases "in one embodiment" or "in an embodiment" in various places throughout this specification are not necessarily all referring to the same embodiment. Furthermore, the particular features,
structures, or characteristics may be combined in any suitable manner in one or more
embodiments.
[0038] As used in this specification and the appended claims, the singular forms "a,"
"an," and "the" include plural referents unless the content clearly dictates otherwise. It should
also be noted that the term "or" is generally employed in its sense including "and/or" unless
the content clearly dictates otherwise.
[0039] In some embodiments, the numbers expressing quantities of ingredients,
properties such as concentration, reaction conditions, and so forth, used to describe and claim
certain embodiments of the invention are to be understood as being modified in some
instances by the term "about." Accordingly, in some embodiments, the numerical parameters
set forth in the written description are approximations that can vary depending upon the
desired properties sought to be obtained by a particular embodiment. In some embodiments,
the numerical parameters should be construed in light of the number of reported significant
digits and by applying ordinary rounding techniques. Notwithstanding that the numerical
ranges and parameters setting forth the broad scope of some embodiments of the invention
are approximations, the numerical values set forth in the specific examples are reported as
precisely as practicable.
[0040] The recitation of ranges of values herein is merely intended to serve as a
shorthand method of referring individually to each separate value falling within the range.
Unless otherwise indicated herein, each individual value is incorporated into the specification
as if it were individually recited herein.
[0041] All processes described herein can be performed in any suitable order unless
otherwise indicated herein or otherwise clearly contradicted by context. The use of any and
all examples, or exemplary language (e.g. "such as") provided with respect to certain
embodiments herein is intended merely to better illuminate the invention and does not pose a
limitation on the scope of the invention otherwise claimed. No language in the specification
should be construed as indicating any non-claimed element essential to the practice of the
invention.
[0042] The headings and abstract of the invention provided herein are for convenience
only and do not interpret the scope or meaning of the embodiments.
[0043] The following discussion provides many example embodiments of the inventive
subject matter. Although each embodiment represents a single combination of inventive
elements, the inventive subject matter is considered to include all possible combinations of
the disclosed elements. Thus if one embodiment comprises elements A, B, and C, and a
second embodiment comprises elements B and D, then the inventive subject matter is also considered to include other remaining combinations of A, B, C, or D, even if not explicitly disclosed.
[0044] All publications herein are incorporated by reference to the same extent as if each individual publication or patent application were specifically and individually indicated to be incorporated by reference. Where a definition or use of a term in an incorporated reference is inconsistent or contrary to the definition of that term provided herein, the definition of that term provided herein applies and the definition of that term in the reference does not apply. [0045] Groupings of alternative elements or embodiments of the invention disclosed herein are not to be construed as limitations. Each group member can be referred to and claimed individually or in any combination with other members of the group or other elements found herein. One or more members of a group can be included in, or deleted from, a group for reasons of convenience and/or patentability. When any such inclusion or deletion occurs, the specification is herein deemed to contain the group as modified thus fulfilling the written description that follows, and the embodiments described herein, is provided by way of illustration of an example, or examples, of particular embodiments of the principles and aspects of the present disclosure. These examples are provided for the purposes of explanation, and not of limitation, of those principles and of the disclosure. [0046] It should also be appreciated that the present invention can be implemented in numerous ways, including as a system, a method or a device. In this specification, these implementations, or any other form that the invention may take, may be referred to as processes. In general, the order of the steps of the disclosed processes may be altered within the scope of the invention.
[0047] Various terms as used herein are shown below. To the extent a term used in a claim is not defined below, it should be given the broadest definition persons in the pertinent art have given that term as reflected in printed publications and issued patents at the time of filing.
[0048] In a general embodiment, the present invention provides a composition, evaluations and quality-by-design optimization of oral herbal micro-emulsion of whole plant extract of Pluchealanceolata and Trigonellafoenum-graecum which could improve solubility, intestinal absorption, bioavailability and therefore, therapeutic effects of herbal medicine specifically for digestive disturbances like constipation, flatulence, indigestion. The herbal micro-emulsions were optimized using central composite design (CCD) to produce
transparent micro-emulsion with optimum viscosity and least globule size which could augment intestinal absorption, bioavailability and therapeutic effects of herbal medicine. [0049] In an embodiment, the present invention relates to a herbal micro-emulsion composition comprising:
f a extract of whole plant of Pluchealanceolata and Trigonellafoenum-graecum; and
g. d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) as surfactant. [0050] In another embodiment, the herbal micro-emulsion composition comprises:
h. a extract of whole plant of Pluchealanceolata and Trigonellafoenum-graecum;
i. d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) as surfactant; and
j. a co-surfactant. [0051] In another embodiment of the present invention, the co-surfactant is selected from polyethylene glycol 400 (PEG 400), polyethylene glycol 600 (PEG 600) and the like. [0052] In another embodiment of the present invention, the co-surfactant is polyethylene glycol 400 (PEG 400) and polyethylene glycol 600 (PEG 600).
[0053] In another embodiment of the present invention, the co-surfactant is polyethylene glycol 400 (PEG 400) and polyethylene glycol 600 (PEG 600) present in a ratio in the range of from about 4:1 to about 1:4, preferably in the range of from about 2:1 to about 1:2, most preferably 1:1.
[0054] In another embodiment of the present invention, the composition further comprises an oil phase.
[0055] In another embodiment of the present invention, the oil phase is selected from soybean oil and the like.
[0056] In another embodiment of the present invention, the composition further comprises distilled water.
[0057] In another embodiment of the present invention, the composition further comprises distilled water in a quantity sufficient to make up the volume of the composition. [0058] In another embodiment of the present invention, the composition comprises an additional surfactant selected from poloxamer 407 and the like.
[0059] In another embodiment of the present invention, the herbal extract is present in a weight range of about 5% to about 20%, preferably in the range of about 5% to about 15% weight, most preferably is 10% by volume of the composition.
[0060] In another embodiment of the present invention, TPGS is present in a weight
range of about 0.5% to about 2%, preferably in the range of about 0.5% to about 1.5%, most
preferably 1.02% by volume of the composition.
[0061] In another embodiment of the present invention, the co-surfactant is present in a
volume range of about 7% to about 10%, preferably in the weight range of about 8% to about
10%), most preferably 9.555%) by volume of the composition.
[0062] In another embodiment of the present invention, the oil phase is present in a
volume range of about 5% to about 40%, preferably in the weight range of about 10% to
about 30%), most preferably 20% by weight of the composition.
[0063] In another embodiment of the present invention, the additional surfactant is
present in a weight range of about 10% to about 12%, preferably in the range of about 11% to
about 12%), most preferably 11.676% by volume of the composition.
[0064] In another embodiment of the present invention, the herbal micro-emulsion
composition comprises:
k. a extract of whole plant of Pluchealanceolata and Trigonellafoenum-graecum;
1. d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS);
m. poloxamer 407;
n. soybean oil; and
o. a 1:1 mixture of PEG 400 and PEG 600. [0065] In yet another embodiment of the present invention, the herbal micro-emulsion composition comprises:
p. a extract of whole plant of Pluchealanceolata and Trigone llafoenum-graecumm the range of about 5% to about 20% weight by volume of the composition;
q. d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) in the range of about 0.5%) to about 2% weight by volume of the composition;
r. poloxamer 407 in the range of 10% to 12% weight by volume of the composition;
s. soybean oil in the range of about 5% to about 40% weight by volume of the composition; and
t. a 1:1 mixture of PEG 400 and PEG 600 in the range of about 7% to about 10% volume by volume of the composition. [0066] In still another embodiment of the present invention, the herbal micro-emulsion composition comprises:
u. a extract of whole plant of Pluchealanceolata and Trigonellafoenum-
graecumm 10% weight by volume of the composition; v. d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) in 1.02% weight
by volume of the composition; w. poloxamer 407 in 11.676%) weight by volume of the composition; x. soybean oil in 20% weight by volume of the composition; and y. a 1:1 mixture of PEG 400 and PEG 600 in 9.555% volume by volume of the composition. [0067] In still another embodiment of the present invention, the herbal micro-emulsion composition comprises:
z. a extract of whole plant of Pluchealanceolata and Trigone llafoenum-
graecumm 10% weight by volume of the composition; aa. d-a-Tocopheryl polyethylene glycol 1000 succinate (TPGS) in 1.02% weight
by volume of the composition; bb.poloxamer 407 in 11.676% weight by volume of the composition; cc. soybean oil in 20% weight by volume of the composition; dd.a 1:1 mixture of PEG 400 and PEG 600 in 9.555% volume by volume of the
composition; and ee. distilled water - lOOmL. [0068] In another embodiment of the present invention, the composition is formulated in the form of a liquid, syrup, capsule or gel.
[0069] In another embodiment of the present invention, the composition has a viscosity in the range of about 50mPa.s to about 80 mPa.s, preferably in the range of about 70 mPa.sto about 80 mPa.s or most preferably about 73.99 mPa.s.
[0070] In another embodiment of the present invention, the composition has a globule size in the range of about 80um to about 100 urn, preferably about 85um to about 95um or most preferably about 90um.
[0071] In yet another embodiment, the present invention relates to a process of preparing a micro-emulsion composition comprising the steps of:
a. preparing an aqueous solution of a herbal extract of whole plant of
Pluchealanceolata and Trigonellafoenum-graecumm distilled water;
b. adding the aqueous solution drop-wise to a mixture of surfactant, co-surfactant
and oil phase; and
c. stirring the mixture with a magnetic stirrer at 1000 rpm and at a temperature of 37
Documents
Application Documents
| # |
Name |
Date |
| 1 |
201911054055-STATEMENT OF UNDERTAKING (FORM 3) [26-12-2019(online)].pdf |
2019-12-26 |
| 2 |
201911054055-FORM FOR STARTUP [26-12-2019(online)].pdf |
2019-12-26 |
| 3 |
201911054055-FORM FOR SMALL ENTITY(FORM-28) [26-12-2019(online)].pdf |
2019-12-26 |
| 4 |
201911054055-FORM 1 [26-12-2019(online)].pdf |
2019-12-26 |
| 5 |
201911054055-EVIDENCE FOR REGISTRATION UNDER SSI(FORM-28) [26-12-2019(online)].pdf |
2019-12-26 |
| 6 |
201911054055-EVIDENCE FOR REGISTRATION UNDER SSI [26-12-2019(online)].pdf |
2019-12-26 |
| 7 |
201911054055-DRAWINGS [26-12-2019(online)].pdf |
2019-12-26 |
| 8 |
201911054055-DECLARATION OF INVENTORSHIP (FORM 5) [26-12-2019(online)].pdf |
2019-12-26 |
| 9 |
201911054055-COMPLETE SPECIFICATION [26-12-2019(online)].pdf |
2019-12-26 |
| 10 |
abstract.jpg |
2020-01-29 |
| 11 |
201911054055-Proof of Right [03-02-2020(online)].pdf |
2020-02-03 |
| 12 |
201911054055-FORM-26 [03-02-2020(online)].pdf |
2020-02-03 |
| 13 |
201911054055-FORM 18 [11-11-2021(online)].pdf |
2021-11-11 |
| 14 |
201911054055-FER.pdf |
2025-06-24 |
| 15 |
201911054055-FORM-5 [17-10-2025(online)].pdf |
2025-10-17 |
| 16 |
201911054055-FORM-26 [17-10-2025(online)].pdf |
2025-10-17 |
| 17 |
201911054055-FER_SER_REPLY [17-10-2025(online)].pdf |
2025-10-17 |
| 18 |
201911054055-DRAWING [17-10-2025(online)].pdf |
2025-10-17 |
| 19 |
201911054055-CORRESPONDENCE [17-10-2025(online)].pdf |
2025-10-17 |
| 20 |
201911054055-CLAIMS [17-10-2025(online)].pdf |
2025-10-17 |
| 21 |
201911054055-US(14)-HearingNotice-(HearingDate-02-12-2025).pdf |
2025-11-17 |
Search Strategy
| 1 |
201911054055_SearchStrategyNew_E_searchE_23-06-2025.pdf |