FIELD OF THE INVENTION
The present invention relates to a process for preparing herbal formulations. More
particularly, the present invention relates to a process for preparing granules of
asavarishta.
BACKGROUND OF THE INVENTION
A shift towards a healthy lifestyle has increased the demand for natural products,
such as extracts of herbs, vegetables, fruits, seeds, essential oils and so forth.
Herbal products are complex mixtures of organic chemicals that may come from
any raw or processed part of a plant, including leaves, stems, flowers, roots, and
seeds. As herbs are perceived “natural” and therefore safe, there is a growing
preference for herbal drugs and traditional medicine over synthetic ones.
Ayurveda comprises myriad formulations for different ailments, including the
fermented forms, for example, arishtas (fermented decoctions) and asavas
(fermented infusions). Arishtas are made from decoctions of herbs in boiling
water, whereas asavas are prepared by suspending herbs in pre-boiled water.
Arishtas and asavas are considered distinctive and prized therapeutics in ayurveda
due to their ability to ameliorate a wide range of ailments. Common arishtas and
asavas, collectively called as asavarishtas, include Abhayarishta, Amrita Rishta,
Arjunarishta, Asavagandharishta, Ashokarishta, Babbulyadarishta,
Dashmularishta and Balarishta.
Sushruta Samhita, 44th and 45th Chapter of Sutra Sthana (2 AD), quotes the
process of Sandhana i.e., fermentation with the combination of Kinva or Surabija
(molasses / yeast), Udaka (water) and Pishta (rice flour). Under Sandhana Kalpa
(fermented products), Sarngdhara Samhita Madhyama Khanda (13-14 AD),
mentions naturally self-liberated alcoholic preparations, i.e., asavas and arishtas.
Presence of water and alcohol aids in dissolving active ingredients from the herbs,
thereby enhancing the efficacy of said herbal preparation.
The traditional preparation of Asavarishta, starts with the extraction of bio-active
ingredients from the plant tissues using solvents and standard procedures known
to persons skilled in the art. The part of the plant to be extracted is dried,
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pulvarized and extracted with a suitable solvent. Decoction is concentrated liquor
formed by boiling the pulvarized plant material with water whereas infusion
involves extraction without boiling.
Further, the decoction or the infusion is filtered and the filtrate is mixed with
honey, sugar or jaggery. The filtration step may be carried out after fermentation
in order to increase the extraction of plant metabolite into the decoction or
infusion. After that, the sweetened decoction or infusion is poured in a pot and
inoculum is added to initiate fermentation. The pot is closed and left undisturbed
for a suitable period of time. Thereafter, the pot is opened and the fermented
formulation is further filtered to remove any sediment present therein. Finally, the
filtrate is ready for use in the specified dosage.
Fermentation of the decoction or infusion results in an alcohol content of 10 to
12% v/v, which is also present in quite a few medicinal wines. The presence of
alcohol prolongs the shelf-life of the formulation by inhibiting the growth of
micro-organisms. Hence, asavarishtas are sold as compositions in alcoholic
media. However, presence of alcohol makes traditionally prepared asavarishta
unpalatable for those who dislike the taste of alcohol.
Solutions suggested in the prior art include removing alcohol and water from the
formulation, freeze drying, hot air drying and so forth. Ayurvedic texts quote that
the ideal drug should possess a basic property called bahu kalpa, i.e., presentable
in multiple formats or dosage forms. However, reduction in the alcohol content
has a direct bearing on the shelf life of the product due to its inhibitory effect on
micro-organisms. Further, changing the physical state of the formulation may
have unintended consequences due to the complex chemistries involved in the
physiological mode of action of asavarishta. Moreover, removal of alcohol may
also affect the absorption of active molecules in the gut. Also, high temperatures
required for evaporation of water and alcohol might degrade bio-active molecules
such as anthocyanins, polyphenols, etc present in the formulation. Boiling a
mixture containing ethanol on an industrial scale at its boiling point might create
an explosive mixture.
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Consequently, there is a need for formulating asavarishtas that are not only
devoid of water and alcohol but also retain their physiological activity. Such a
composition would not only appeal to those averse to alcohol but also improve
storage, dosing and handling of said composition. Additionally, there is a need for
for preparing concentrated asavarishtas at low temperatures and pressures to
prevent the degradation of anti-oxidants present therein.
SUMMARY OF THE INVENTION
In accordance with an embodiment of the invention, there is provided a process
for preparing granules of asavarishta, comprising the steps of:
a. preparing asavarishta;
b. concentrating the asavarishta to obtain concentrated asavarishta;
c. adding pharmaceutically acceptable excipients and mixing, thereby
obtaining a plurality of moist granules; and
d. drying the moist granules;
wherein the amount of concentrated asavarishta used in the process is 50 to
61%.
The step of preparing asavarishta comprises the steps of:
a. preparing a herbal infusion or a herbal decoction;
b. adding cane sugar, jaggery, honey, or carbohydrates in the herbal
infusion or herbal decoction;
c. adding inoculum to the composition of step b and fermenting and
maturing in a closed vessel for a pre-determined period of time;
and
d. filtering the composition of step c to obtain asavarishta.
The step for concentrating asavarishta is preferably carried out in an explosion
proof conventional evaporator, a centritherm centrifugal concentrator, a falling
film evaporator, a spinning cone column, a rising film evaporator or a plate
evaporator.
The asavarishta used in the above process contains upto 35% by weight of total
soluble solids.
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The inoculum comprises micro-organisms selected from the group consisting of
Saccharomyces species and novel yeast strains having MTCC accession numbers
DRF-UDS-004/WF, DRF-UDS-016/WF and DRF-UDS-017/WF. Further, the
pre-determined period of time for fermentation and maturation ranges upto 20
days. Still further, the asavarishta is concentrated upto a total soluble solid (TSS)
content of 80% by weight to obtain the concentrated asavarishta.
Preferably, the step of concentrating asavarishta is carried out under reduced
pressure not exceeding -90 kPa and temperature not exceeding 50 °C.
The pharmaceutically acceptable excipients used in the above process are selected
from preservatives, fillers and combinations thereof.
Preferably, the preservatives are selected from the group consisting of potassium
sorbate, sodium benzoate, sodium methylparaben, methylparaben, sodium propyl
paraben, benzoic acid, and sorbic acid, and used in an amount of 0.01 to 0.22%.
Preferably, the fillers are selected from the group consisting of microcrystalline
cellulose (MCC), maltodextrin, silicified microcrystalline cellulose powdered
cellulose, lactose, mannitol, sorbitol, calcium phosphate and calcium hydrogen
phosphate, and used in an amount of 5 to 55%.
The drying of the moist granules is carried out at a temperature not exceeding 60
°C until the loss on drying (LOD) is less than 3%.
The above process for preparing granules of asavarishta, can be used to prepare
granules of Dashmularishta, wherein the granules of Dashmularishta have better
anti-oxidant potential compared to Dashmularishta.
In accordance with another embodiment of the invention there is provided an
herbal composition, prepared by the above process.
DETAILED DESCRIPTION OF THE INVENTION
Discussed below are some representative embodiments of the present invention.
The invention in its broader aspects is not limited to the specific details and
representative methods. The illustrative examples are described in this section in
connection with the embodiments and methods provided. The invention according
to its various aspects is particularly pointed out and distinctly claimed in the
attached claims read in view of this specification.
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It is to be noted that, as used in the specification and the appended claims, the
singular forms "a," "an," and "the" include plural referents unless the context
clearly dictates otherwise. Thus, for example, a reference to a composition
containing “a compound” includes a mixture of two or more compounds. It should
also be noted that the term “or” is generally employed in its sense including
“and/or” unless the content clearly dictates otherwise.
The expression of various quantities in terms of “%” or “% w/w” means the
percentage by weight of the total solution or composition unless otherwise
specified.
All cited references are incorporated herein by reference in their entireties.
Citation of any reference is not an admission regarding any determination as to its
availability as prior art to the claimed invention.
The present invention, in its product and process aspects, is described in detail as
follows:
The inventors of the present invention sought to prepare granules of asavarishta,
which are not only devoid of alcohol and suitable for those averse to alcohol but
also retain their biological efficacy. After much trial and error they optimized a
process for preparing said granules, which are as effective as traditionally
prepared asavarishta. The novel process comprises the following steps.
(a) Preparing asavarishta
Asavarishtas that may be prepared by the process disclosed in the invention
include, but not limited to, Abhayarishta, Amritarishta, Arjunarishta,
Asavagandharishta, Ashokarishta, Babbulyadarishta, Dashmularishta,
Balarishta, Kutajaarishta, Draakshaarishta, Devadaarvaarishta, Jeerakaarishta,
Khadirashta, Karpoorasavam, Pippalyaadi asavam, Punarnavaasavam,
Usiraashtam, Aravindaarishta, and Patrangaasavam. Preferably the asavarishta
contains upto 35% by weight of total soluble solids (TSS).
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The herbal material is dried, pulvarized and extracted with a suitable solvent. The
extract may be in the form of a decoction or an infusion. Decoction differs from
infusion in that the former is made by boiling the herbal material in water whereas
the latter is prepared by pouring pre-boiled water or cold water into a vessel
containing the herbal material.
Herbs useful for use in the present invention depend on the particular asavarishta
being prepared and are known to a person of ordinary skill in the art. The process
provided in the disclosure can be used for the preparation of any asavarishta.
While preparing a decoction, preferably, the ratio of weight of the herbal material
to the volume of the solvent ranges from 1:4 (gm:mL) to 1:16 (gm:mL), which is
reduced to about one fourth of the original volume after boiling. Thereafter, the
decoction so obtained is used as such or filtered and used for further processing.
Further, the decoction or infusion is poured into a suitable vessel for fermentation
and maturation. The term fermentation used herein refers to the conversion of
sugars or carbohydrates into ethyl alcohol and carbon dioxide. Suitable sources of
sugars include, but not limited to cane sugar, honey and jaggery. A suitable source
of sugar or carbohydrate is mixed with the decoction or the infusion.
Carbohydrates useful for the present invention include those that can be fermented
into ethyl alcohol and carbon dioxide by suitable micro-organisms. The term
maturation used herein refers to changes taking place in the decoction after
fermentation.
After that, an inoculum is added to initiate fermentation. The inoculum comprises
organisms selected from the group consisting of Saccharomyces species and novel
yeast strains having MTCC accession numbers DRF-UDS-004/WF, DRF-UDS-
016/WF and DRF-UDS-017/WF. Thereafter the vessel is closed, wherein its
contents are isolated from the external environment, i.e., made air-tight.
Preferably, the processes of fermentation and maturation are together allowed to
proceed for upto 20 days. Finally the fermented decoction or infusion is filtered
and the filtrate is used as asavarishta.
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(b) Concentrating the asavarishta to obtain concentrated asavarishta.
An anti-oxidant is a molecule that inhibits the oxidation of other molecules.
Examples include, but not limited to, anthocyanins, stilbenoids, isoflavone
phytoestrogens, flavanols, flavanones, flavones, and flavonols. Most of them are
short lived; however, some degrade slowly. Anti-oxidant degradation can be due
to light, oxygen, microbes or heat. It is known that anti-oxidants degrade much
slower in the absence of oxygen and at lower temperatures. Accordingly,
maintaining relatively low temperatures and minimizing exposure of the herbal
material to light and oxygen, at all stages of the process of the present invention is
desirable.
The asavarishta prepared by the above process contains upto 35% by weight of
total soluble solids (TSS). It is then subjected to further concentration to provide
concentrated asavarishta. The inventors of the present invention determined that
the concentration step required careful control if the concentrated asvarishta was
to retain its bio-efficacy, as exposure to heat accelerated degradation of the active
components as the concentration of said components increased. Application of
vacuum causes the boiling point of liquids such as water and ethanol to drop,
wherein said liquids start boiling at temperatures at which they would be in
equilibrium with the atmospheric pressure. Evaporating under reduced pressure,
has the additional advantage of reducing the exposure of the herbal material to
atmospheric oxygen, thereby preventing oxidation of desirable anti-oxidants.
Preferably, the step of concentrating asavarishta is carried out under reduced
pressure at a temperature not exceeding 50 °C and more preferably at a
temperature not exceeding 45 °C. Further, the process of concentration is
preferably carried out at a pressure of not exceeding -90 kPa. By evaporation
under reduced pressure, the concentration of total soluble solids may be increased
upto 80%. The concentration may be carried out in an explosion proof
conventional evaporator, in a centritherm centrifugal concentrator, in a falling
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film evaporator, a spinning cone column, a rising film evaporator or a plate
evaporator.
(c) Adding pharmaceutically acceptable excipients and mixing, thereby
forming a plurality of moist granules.
Further, pharmaceutically acceptable excipients are added and mixed with the
concentrated asavarishta to obtain moist granules of asavarishta. The terms
pharmaceutically acceptable excipients, pharmaceutically compatible excipients,
and excipients essentially mean the same thing and are used interchangeably in
this disclosure. They refer to substances such as disintegrators, binders,
preservatives, fillers, and lubricants used in formulating pharmaceutical products
that have no physiological effect on the ailment being treated. They are generally
safe for administering to humans.
Preferably, the excipients used in the present invention are selected from
preservatives, fillers and combinations thereof. The term “preservative” used
herein refers to a substance that inhibits the growth of micro-organisms such as
bacteria, fungi and viruses. The term “filler” used herein refers to a substance that
is used to increase the bulk of the active compound so that it can be provided in
the form of a tablet or a granule of appropriate dose. Non-limiting examples of
fillers that can be used in the present invention include microcrystalline cellulose,
silicified microcrystalline cellulose, powdered cellulose, lactose, mannitol,
sorbitol, calcium phosphate, calcium hydrogen phosphate, maltodextrin and so
forth, each of which can be used individually or in combination. Furthermore, the
preservatives useful in the present invention include, but not limited to, potassium
sorbate, sodium benzoate, sodium methylparaben, methylparaben, sodium propyl
paraben, benzoic acid and sorbic acid.
Preferably, the preservative is used in the range from of 0.01 to 0.22% whereas
the filler is used in the range from 5 to 55%.
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(d) Drying the moist granules to obtain granules of asavarishta
Finally, the moist granules are dried to afford granules of asavarishta. Preferably,
the moist granules are dried at a temperature not exceeding 60 °C until the loss on
drying is less than 3%.
Examples
The present invention is more particularly described in the following examples
that are intended as illustrations only, since numerous modifications and
variations within the scope of the present invention will be apparent to those of
skill in the art. Unless otherwise noted, all parts, percentages and ratios reported in
the following examples are on a weight basis and all reagents used in the
examples were obtained or are available from the chemical suppliers.
Process for preparing Dashmularishta
Wash, dry and powder the Kwatha (decoction) ingredients, i.e. Bilva (Aegle
marmelos), Shayonaka (Oroxylum indicum), Gambhari (Gmelina arborea), Patala
(Stereospermum suaveolans), Agnimantha (Premna integrifolia), Shalaprani
(Desmodium gangeticum), Prishniparni (Uraria picta), Brihati (Solanum
indicum), Kantakari (Solanum surattense), Gokshura (Tribulus terrestris), Yashti
(Glycyrrhiza glabra), Bharangi (Clerodendrum serratum), Kapittha (Feronia
limonia), Bibhitaka (Terminalia belerica), Rakta punarnava (Boerhavia diffusa),
Chavya (Piper chaba), Priyangu (Callicarpa macrophylla), Shveta sariva
(Hemidesmus indicus), Pippali (Piper longum), Puga (Areca catechu), Shati
(Hedychium spicatum), Haridra (Curcuma longa), Shatava (Anethum sowa),
Padmaka (Prunus cerasoides), Nagakesara (Mesua ferrea), Karkatashringi
(Pistacia integrrima), Jivaka (Pueraria tuberosa), Rishbhaka (Pueraria tuberose),
Meda (Asparagus racemosus), Mahameda (Asparagus racemosus), etc
individually and pass through the sieve number 10 to 12 to obtain coarse powder.
Add water, soak overnight, heat, reduce volume to half and filter through muslin
cloth to obtain Kwatha. Wash and crush the Draksha (Vitis vinifera) add water,
soak overnight, heat, reduce to one fourth and filter through muslin cloth to obtain
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Kwatha. Collect the two Kwathas into one clean container and mix to form a
homogenous liquid. Clean, dry and powder the Prakshep dravya ingredients, i.e.,
Kankola (Piper cubeba), Hrivera (Coleus vettiveroides), Shveta chandana
(Santalum album), Jatiphala (Myristica fragrans), Lavanga (Syzygium
aromaticum), Tvak (Cinnamomum zeylanicum), etc individually and pass through
the sieve number 20 to obtain fine powder. Add Guda (Jaggery, 41.7% w/v) to the
Kwatha, dissolve and filter through a muslin cloth. Transfer the filtrate to a clean
container; add Madhu (honey), Dhataki (Woodfordia fruticosa, a known source of
Saccharomyces species) and other finely powdered Praksepa Dravyas and close
the mouth of the container. Shift the container to the fermentation room and
constantly check for the signs of completion of fermentation process. Filter the
fermented material through a clean muslin cloth. Pack in air tight containers and
allow for maturation.
Concentrating Dashmularishta to obtain concentrated Dashmularishta
Dasmularishta obtained by the above process had a TSS content of 25%. After
concentrating in Centritherm® evaporator, Model CT6, for 2 h, its TSS value
increased to 80%. Said evaporator concentrated 291.5 kg of Dasmularishta to
afford 93.3 kg of concentrated Dashmularishta. The instrumental parameters at
various time points in the concentration process are presented in table 1.
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Table 1. Instrumental parameters at different time points in the concentration process
Parameters
Time in minutes
0 15 30 45 60 75 90 105 120
Product inlet temperature (°C) 35.8 39.1 40.2 39.8 39.2 39.2 40.2 40.5 44.8
Chilled water inlet temperature
(°C)
4.5 5.8 10.7 5.3 6.0 8.0 8.8 11.5 13.0
Product outlet temperature (°C) 42.2 40.4 44.8 35.4 40.3 42.1 43.8 45.0 46.2
Chilled water outlet temperature
(°C)
11.6 13.7 16.7 10.4 9.5 10.5 13.5 14.9 16.0
Feed pump rate (kg/h) 1170 1505 1502 1507 1500 1510 1500 1502 1505
Vacuum applied (mm Hg) 700 700 710 700 700 700 700 700 700
Concentration (% TSS) 25 - 35 - 49 - 60 - 80
TSS = Total Soluble Solids
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Process for preparing Dashmularistha granules:
Mix 3000 g of concentrated Dashmularishta prepared by the above process with
1560 g of microcrystalline cellulose and 425 g of maltodextrin to obtain moist
granules of Dashmularishta. Dry the moist granules of Dashmularishta on a tray
dryer, at a temperature of 60 °C, until a loss on drying of less than 3% is obtained.
Pack the granules of Dashmularishta in an air tight high density polyethylene
(HDPE) container.
In-vitro estimation of free radical scavenging activity of Dashmularishta and
Dashmularishta granules
The Dashmularishta and granules of Dashmularishta used in the present study
were prepared by above process. The present study was conducted to evaluate the
free radical scavenging activity of Dashmularishta and Dashmularishta granules
using ABTS (2,2'- azinobis-3-ethylbenzothiozoline-6-sulphonic acid) assay in
vitro. Trolox, a compound with well reported antioxidant properties, was used as a
positive control.
ABTS assay is the most widely reported method for the estimation of antioxidant
activity of test compounds/plant extracts. The radical scavenging activity of
Dashmularishta and Dashmularishta granules was evaluated using PBS solution
of the stable free radical, ABTS. A freshly prepared ABTS solution exhibits green
colour with a maximum absorption at 734 nm, which is decreased in presence of
compounds with antioxidant potential. Antioxidant compounds can quench ARTS
free radicals and convert them to colorless product, resulting in a decrease in
absorbance at 734 nm. Change in absorbance values in presence of
Dashmularishta and Dashmularishta granules was determined with reference to
blank and reflected its anti-oxidant potential.
Dashmularishta, was tested for its anti-oxidant potential at various concentrations
ranging from 0.01%-20% and Dashmularishta granules at concentrations ranging
from 0.01% - 17.5%. It was observed that Dashmularishta and Dashmularishta
granules exhibited strong antioxidant potential with TEAC values of 0.55 and
0.94 respectively. Therefore, it is suggested that Dashmularishta and
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Dashmularishta granules offer protection against various diseases mediated by
oxidative stress. Hence, based on the data obtained in the current study, it can be
suggested that the antioxidant potential of granules of Dashmularishta is greater
than Dashmularishta.
While particular embodiments of the present invention have been illustrated and
described, it would be obvious to those skilled in the art that various other
changes and modifications can be made without departing from the spirit and
scope of the invention. It is thereof intended to cover in the appended claims such
changes and modifications that are within the scope of the invention.

We claim:
1. A process for preparing granules of asavarishta, comprising the steps of:
a. preparing asavarishta;
b. concentrating the asavarishta to obtain concentrated asavarishta;
c. adding pharmaceutically acceptable excipients and mixing, thereby
obtaining a plurality of moist granules; and
d. drying the moist granules;
wherein the amount of concentrated asavarishta used in the process is 50 to
61%.
2. The process for preparing granules of asavarishta, as claimed in claim 1,
wherein the step of preparing asavarishta comprises the steps of:
a. preparing a herbal infusion or a herbal decoction;
b. adding cane sugar, jaggery, honey, or carbohydrates in the herbal
infusion or herbal decoction;
c. adding inoculum to the composition of step b and fermenting and
maturing in a closed vessel for a pre-determined period of time;
and
d. filtering the composition of step c to obtain asavarishta.
3. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the concentration is carried out in an explosion proof conventional
evaporator, a centritherm centrifugal concentrator, a falling film
evaporator, a spinning cone column, a rising film evaporator or a plate
evaporator.
4. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the asavarishta contains upto 35% by weight of total soluble
solids.
5. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the inoculum comprises micro-organisms selected from the group
consisting of Saccharomyces species and novel yeast strains having
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MTCC accession numbers DRF-UDS-004/WF, DRF-UDS-016/WF and
DRF-UDS-017/WF.
6. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the pre-determined period of time ranges upto 20 days.
7. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the asavarishta is concentrated upto a total soluble solid (TSS)
content of 80% by weight to obtain the concentrated asavarishta.
8. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the step of concentrating asavarishta is carried out under reduced
pressure at a temperature not exceeding 50 °C.
9. The process for preparing granules of asavarishta, as claimed in claim 8,
wherein the reduced pressure does not exceeds -90 kPa.
10. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the pharmaceutically acceptable excipients are selected from
preservatives, fillers and combinations thereof.
11. The process for preparing granules of asavarishta, as claimed in claim 10,
wherein the preservatives are selected from the group consisting of
potassium sorbate, sodium benzoate, sodium methylparaben,
methylparaben, sodium propyl paraben, benzoic acid, and sorbic acid, and
used in an amount of 0.01 to 0.22%.
12. The process for preparing granules of asavarishta, as claimed in claim 10,
wherein the fillers are selected from the group consisting of
microcrystalline cellulose (MCC), maltodextrin, silicified microcrystalline
cellulose powdered cellulose, lactose, mannitol, sorbitol, calcium
phosphate and calcium hydrogen phosphate, and used in an amount of 5 to
55%.
13. The process for preparing granules of asavarishta, as claimed in claim 2,
wherein the drying of the moist granules is carried out at a temperature not
exceeding 60 °C until the loss on drying (LOD) is less than 3%.
14. The process for preparing granules of asavarishta, as claimed in claims 1
to 13, wherein the asavarishta is a Dashmularishta, and wherein the
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granules of Dashmularishta have better anti-oxidant potential compared to
Dashmularishta.
15. An herbal composition, prepared by a process as claimed in any of the
claims 1 to 14.