“POLYHERBAL LIPID-LOWERING THERAPY TO COMBAT HYPERLIPIDAEMIA IN RATS”

Abstract

Hyperlipidaemia is a disorder of lipid metabolism 5 and a significant risk factor for obesity and cardiovascular diseases, affecting millions globally. This study develops and evaluates a polyherbal formulation of Cissus quadrangularis, Picrorhiza kurroa, and Combretum indicum (1:1:1 ratio) for its antihyperlipidemic effects. Preliminary screening identified phenolic acids, flavonoids, and tannins in 10 the formulation. Acute toxicity tests determined safe doses of 200 mg/kg and 400 mg/kg. After inducing hyperlipidaemia in rats with Triton X-100, treatment with the polyherbal elixir for seven days resulted in significant normalization of body weight, BMI, lipid profiles, and liver enzymes. The study supported the antihyperlipidemic effects, indicating the formulation's potential due to its active 15 phytochemicals.

Specification

Description:FIELD OF THE INVENTION
The present invention pertains to herbal medicine, 5 specifically a polyherbal
formulation targeting dyslipidaemia and hyperlipidaemia, major risk factors for
cardiovascular and metabolic disorders. The formulation combines Cissus
quadrangularis, Picrorhiza kurroa, and Combretum indicum to safely and
effectively manage lipid metabolism disorders. Preclinical studies demonstrate its
10 potential to regulate lipid levels, reduce oxidative stress, and support metabolic
health in hyperlipidaemic conditions.
BACKGROUND OF THE INVENTION
Hyperlipidemia, commonly referred to as dyslipidemia, is a metabolic disorder
15 characterized by elevated levels of plasma lipids, including cholesterol, cholesterol
esters, triglycerides, and phospholipids. This condition plays a pivotal role in the
development of obesity and cardiovascular diseases (CVDs), making it a significant
global health concern. Disruptions in lipid metabolism are often at the core of
various chronic health issues, contributing to the multifaceted burden of obesity,
20 cardiovascular illnesses, and metabolic syndromes. These conditions frequently
lead to a decline in the functionality of affected bodily organs and systems, which,
over time, may result in serious complications or even death. Furthermore, the
prevalence of multi-morbidity is alarmingly high worldwide, with approximately
14 million people globally living with multiple chronic diseases. In India alone,
25 around 24.1% of adults are reported to experience such multi-morbidities.
Despite the availability of numerous hypolipidemic medications for the treatment
of hyperlipidemia, these synthetic drugs often come with limitations, including a
3
lack of complete efficacy and safety, as well as a spectrum of side effects. For
example, common hypolipidemic agents like fibrates, bile acid-binding agents, and
statins are known to cause adverse reactions such as dry skin, flushing, myositis,
hyperuricemia, gastrointestinal disturbances, and altered liver functions. Therefore,
there is an increasing demand for alternative 5 therapeutic options that are not only
effective but also safer and free from the undesirable side effects associated with
synthetic medications.
In response to these limitations, our study aims to investigate a natural, plant-based
approach to managing hyperlipidemia through the development and evaluation of
10 a polyherbal elixir. This formulation combines the extracts of three medicinal
plants-Cissus quadrangularis, Picrorhiza kurroa, and Combretum indicum-in
equal proportions (1:1:1). These herbs are well-documented in traditional medicine
for their therapeutic effects and have shown promising results in preclinical studies
related to anti-inflammatory, antioxidant, hepatoprotective, anti-diabetic, and
15 hypolipidemic activities. The synergistic potential of combining these herbs may
provide a more effective, safer, and holistic solution for correcting lipid metabolism
and addressing the root causes of hyperlipidemia.
SUMMARY OF THE INVENTION
20 The present invention pertains to a polyherbal elixir formulated to treat
hyperlipidemia-a condition marked by elevated levels of blood lipids, which can
lead to cardiovascular and metabolic diseases. This elixir combines extracts of
Cissus quadrangularis, Picrorhiza kurroa, and Combretum indicum in equal parts,
aiming to harness their synergistic effects to lower blood lipid levels, improve
25 antioxidant activity, and support liver health.
Key Features of the Invention:
4
1. Composition: The polyherbal formulation includes equal parts of Cissus
quadrangularis (stem), Picrorhiza kurroa (root), and Combretum indicum
(leaves) extracts. These herbs are known for their anti-inflammatory,
antioxidant, and lipid-lowering properties. Additional components include
preservatives and a flavoring agent for 5 enhanced palatability and stability.
2. Mechanism of Action: The herbal extracts target lipid metabolism by reducing
harmful cholesterol levels (LDL, VLDL, triglycerides) and increasing
beneficial HDL cholesterol. They also show hepatoprotective effects by
protecting the liver from lipid-induced oxidative stress and inflammation,
10 potentially reducing the risk of fatty liver disease.
3. Therapeutic Benefits: The elixir aims to provide a natural, effective treatment
for hyperlipidemia with minimal side effects compared to synthetic lipidlowering
drugs, which often have adverse reactions like liver toxicity and
muscle pain. The formulation's antioxidant properties also help counter
15 oxidative stress, which is a contributor to cardiovascular and metabolic
complications.
4. Preclinical Validation: Tested on hyperlipidemic rat models, the elixir
demonstrated significant improvements in lipid profile, liver enzyme activity,
and antioxidant markers.
20 This polyherbal elixir offers a safe, plant-based alternative for lipid management,
potentially suitable for chronic use due to its safety profile and efficacy in lowering
lipid levels and protecting liver health.
DETAILED DESCRIPTION OF THE INVENTION
The following is a detailed description of embodiments of the present disclosure.
25 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
5
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.
Unless the context requires otherwise, throughout the specification which follow,
the word "comprise" and variations thereof, 5 such as, "comprises" and "comprising"
are to be construed in an open, inclusive sense that is as "including, but not limited
to."
Orientation throughout this specification to "one embodiment" or "an embodiment"
means that a particular feature, structure or characteristic described in connection
10 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.
15 The headings and abstract of the invention provided herein are for convenience only
and do not interpret the scope or meaning of the embodiments.
The invention is a polyherbal elixir formulated to treat hyperlipidemia by utilizing
a synergistic blend of Cissus quadrangularis, Picrorhiza kurroa, and Combretum
indicum. These ingredients, traditionally known for their medicinal properties, are
20 combined in specific proportions to create a potent, natural remedy for managing
elevated lipid levels and associated cardiovascular risks. The elixir is designed for
oral administration and formulated to ensure high bioavailability, effectiveness, and
palatability.
EXAMPLES
25 1. Composition and Ingredients
6
The formulation contains equal parts of three primary plant extracts:
 Cissus quadrangularis (Stem Extract): This extract is derived from the stem of
Cissus quadrangularis, a plant well-regarded for its antioxidant, antiinflammatory,
and lipid-lowering properties. 5 It helps reduce LDL and
triglyceride levels, while supporting overall metabolic health.
 Picrorhiza kurroa (Root Extract): Known for its hepatoprotective and antiinflammatory
properties, Picrorhiza kurroa extract supports liver function by
Sr
no
Ingredients F1 F2 F3 F4 F5 F6 F7 F8 F9
1 Combretum indicum
L: Picrorhiza kurroa :
Cissus
quadrangularis
(1:1:1) (gms)
2 2
2
2
2 2 2 2 2
2 Sodium saccharin
(gms)
0.3 0.1 0.3 0.1 0.3 0.1 0.3 0.5 0.3
3 Alcohol (ml) 15 15 15 15 15 15 15 15 15
4 Glycerine (ml) 1.5 1 2.2 2 2 1.5 0.7
92
2 1
5 Methyl paraben (gm) 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2 0.2
6 Propyl paraben (gm) 0.0
2
0.02 0.0
2
0.02 0.0
2
0.0
2
0.0
2
0.0
2
0.0
2
7 Pineapple syrup (ml) 2 2 2 2 2 2 2 2 2
8 Water (ml)
Up to 100 ml
Q.S
.
Q.S. Q.
S.
Q.S. Q.
S.
Q.
S.
Q.
S.
Q.
S.
Q.
S.
7
protecting it from oxidative damage. It plays a crucial role in maintaining a
healthy lipid profile by boosting liver detoxification and metabolic regulation.
 Combretum indicum (Leaf Extract): This leaf extract provides additional
antioxidant and anti-inflammatory effects that aid in reducing high cholesterol
and triglyceride levels. It also 5 exhibits hepatoprotective properties, helping to
prevent fatty liver disease.
Additional excipients may include:
 Preservatives: To ensure the elixir's stability over time, suitable food-grade
preservatives are used.
10  Flavoring Agents: Added to improve taste and make the elixir more
palatable, especially for patients who may need to use it over an extended
period.
2. Preparation Method
The elixir is prepared by a standardized process that ensures the preservation of
15 active phytochemicals in each extract:
 Step 1: Extraction of Plant Components
The stems of Cissus quadrangularis, roots of Picrorhiza kurroa, and leaves of
Combretum indicum are carefully cleaned, dried, and pulverized.
Each plant material undergoes an extraction process (e.g., ethanol or water
20 extraction) to yield concentrated extracts. The choice of solvent is selected based
on its effectiveness in extracting the target phytochemicals, while ensuring safety
and efficacy.
 Step 2: Filtration and Concentration
8
The extracts are filtered to remove any impurities or residual plant material.
After filtration, the extracts are concentrated under reduced pressure to ensure the
potency of active compounds.
 Step 3: Blending and Formulation
The concentrated extracts are mixed 5 in equal parts, and preservatives and flavoring
agents are added.
The final mixture is homogenized and diluted to achieve the desired consistency for
oral administration. The elixir is then bottled under aseptic conditions to maintain
its purity and stability.
10 3. Mechanism of Action
The polyherbal elixir functions through multiple mechanisms to combat
hyperlipidemia:
Lipid Reduction: The extracts work synergistically to inhibit the synthesis of
cholesterol and triglycerides while enhancing the breakdown of lipids. Cissus
15 quadrangularis particularly aids in lowering LDL and VLDL cholesterol, while
increasing HDL levels.
Hepatoprotective Effects: Picrorhiza kurroa and Combretum indicum extracts
protect the liver from oxidative stress caused by excess lipids. This hepatoprotective
action is essential for patients with hyperlipidemia, as they often suffer from non20
alcoholic fatty liver disease.
Antioxidant Activity: The polyherbal formulation is rich in antioxidants, which
scavenge free radicals, thereby reducing oxidative stress and inflammation in blood
9
vessels. This antioxidant effect prevents the formation of plaques in arteries,
reducing the risk of atherosclerosis.
4. Therapeutic Benefits
The elixir offers multiple benefits for patients suffering from hyperlipidemia:
 Improved Lipid Profile: Regular use of 5 the elixir can help significantly
reduce total cholesterol, LDL, VLDL, and triglyceride levels, while
increasing HDL levels, which is beneficial for heart health.
 Enhanced Liver Function: By supporting liver detoxification and reducing
fat deposition, the elixir improves liver health and metabolic functions. This
10 may help prevent conditions like fatty liver and support overall metabolic
balance.
 Natural Antioxidant and Anti-inflammatory Support: The formulation
reduces inflammation and oxidative stress, both of which are common in
patients with hyperlipidemia. This may aid in preventing cardiovascular
15 complications associated with chronic inflammation.
Preclinical Studies and Efficacy
The formulation was tested in preclinical trials using hyperlipidemic animal
models. The following results were observed:
Lipid-Lowering Effects: Animal models treated with the elixir showed a significant
20 decrease in LDL, VLDL, and triglyceride levels, along with an increase in HDL
levels. The improvement in lipid profile was observed within a few weeks of
treatment.
10
Hepatoprotective Effects: Histopathological examinations indicated reduced fat
accumulation and inflammation in the liver tissues of treated models. Liver enzyme
levels (ALT, AST) were also reduced, indicating improved liver health.
Antioxidant Markers: The treated models exhibited increased antioxidant enzyme
activity, including 5 superoxide dismutase (SOD) and glutathione peroxidase, which
help reduce oxidative stress.
Dosage and Administration
The recommended dosage for adults is 10-15 mL, administered twice daily after
meals. The dosage can be adjusted based on the severity of hyperlipidemia and
10 individual response to the treatment. Regular use as prescribed may lead to
significant improvements in lipid profile and liver function over a period of 8 to 12
weeks.
This polyherbal elixir offers a potent, natural solution for managing hyperlipidemia
and its associated risks. With its unique combination of Cissus quadrangularis,
15 Picrorhiza kurroa, and Combretum indicum, the elixir effectively reduces harmful
cholesterol levels, supports liver health, and provides antioxidant protection,
making it an ideal alternative to synthetic lipid-lowering medications.
Hyperlipidemia is an excessive lipid buildup in the blood, increasing risks for heart
attacks and other health issues. High cholesterol can clog arteries, with LDL and
20 VLDL contributing to plaque buildup, while HDL directs cholesterol to the liver
for processing. Lifestyle factors like smoking, alcohol consumption, inactivity, and
stress contribute to hyperlipidemia.
This polyherbal formulation, made from 1:1:1 ethanolic extracts of Combretum
indicum (leaves), Picrorhiza kurroa (roots), and Cissus quadrangularis (stem),
11
contains active phytoconstituents such as alkaloids, terpenoids, saponins, and
flavonoids. Stability tests confirmed the formulation's viscosity, pH, and refractive
index are within acceptable ranges.
Acute oral toxicity studies demonstrated safety at doses up to 2000 mg/kg, with 200
mg/kg (4 ml) and 400 mg/kg (8 ml) established 5 as low and high effective doses,
respectively. Triton X-100 was used to induce hyperlipidemia in animal models,
showing increased lipid profile parameters and oxidative stress. Treatment with the
polyherbal formulation improved HDL-C and glutathione levels while reducing
other lipid parameters, indicating effective antioxidant and lipid-lowering
10 properties.
The proposed mechanism suggests the formulation reduces triglycerides or
enhances lipoprotein uptake by muscle tissues, with saponins, tannins, and phenolic
acids as key compounds in managing hyperlipidemia. Overall, this formulation
demonstrates dose-dependent effectiveness against hyperlipidemia, supporting its
15 potential as a natural therapeutic option. , Claims:1. A polyherbal formulation for the management of hyperlipidemia comprising
equal parts of extracts from Cissus quadrangularis, Picrorhiza kurroa, and
Combretum indicum.
5
2. The polyherbal formulation as claimed in claim 1, wherein the formulation is
designed to lower lipid levels in a subject and support overall metabolic health.
3. The polyherbal formulation as claimed in claim 1, wherein the formulation
10 further comprising one or more preservatives and flavoring agents to enhance
the stability and palatability of the formulation.
4. A method for preparing the polyherbal formulation of claim 1, comprising the
steps of:
15 a. Cleaning, drying, and pulverizing the plant materials;
b. Extracting the active components using a suitable solvent;
c. Filtering and concentrating the extracts;
d. Blending the concentrated extracts in equal proportions;
e. Adding preservatives and flavoring agents; and
20 f. Bottling the final mixture under aseptic conditions.
5. The polyherbal formulation as claimed in claim 1, wherein the dosage of the
formulation is between 10-15 mL administered twice daily after meals.
6. The method for preparing the polyherbal formulation as claimed in claim 4,
25 wherein the administration of the formulation leads to a significant reduction in
plasma levels of low-density lipoprotein (LDL) cholesterol, very low-density
13
lipoprotein (VLDL) cholesterol, and triglycerides, and an increase in highdensity
lipoprotein (HDL) cholesterol levels.
7. The polyherbal formulation as claimed in claim 1, wherein the extracts exert
synergistic effects to enhance 5 lipid metabolism, reduce oxidative stress, and
improve liver function.
8. The polyherbal formulation as claimed in claim 1, wherein the active
ingredients exhibit antioxidant properties, enhancing the antioxidant defense
10 system of the body and mitigating oxidative stress-related complications
associated with hyperlipidemia.

Documents