Title of Invention

HERBAL PHARMACEUTICAL COMPOSITIONS IN JELLY FORMULATIONS

Abstract Herbal pharmaceutical compositions in comprising active ingredients in the form of extracts; one or more water soluble liquid base; jellying agenst like polyacrylamide, thickening agent, chelating agent, food acids, preservative, sweeteners, colorant and flavorants that are spill resistant, palatable and easy to extrude from the container.
Full Text FORM 2
THE PATENTS ACT, 1970
(39 of 1970)
COMPLETE SPECIFICATION
[See section 10; Rule 13]

"HERBAL PHARMACEUTICAL COMPOSITIONS IN JELLY
FORMULATIONS"
(a) M/s LYKA LABS LIMITED.
(b) 77, Nehru Road, Vile Parle (East), Mumbai - 400 099, Maharashtra, India
(c) Indian Company incorporated under the Companies Act 1956
The following specification particularly describes the nature of the invention and the manner in which it is to be performed:
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TECHNICAL FIELD:
The present invention relates to herbal pharmaceutical compositions in semisolid form for oral use. More particularly, the present invention relates to herbal pharmaceutical compositions in j elly forms.
BACKGROUND OF THE INVENTION:
Herbal medicines are widely used today for their advantages like safety and effectiveness. A number of herbal preparations are available in the market of which cough preparations enjoy the largest market share. The extracts of Adulsa (Adhatoda vasica), Jestimadh (Glycerrhiza glabra), Tulsi (Ocimum sanctum), Ginger (Zingiber officinale), Karpura (Cinnamomum camphora), Pudina ka phool (Mentha spicata) being the most popular and highly effective combination. Also Amla (Embelica officinalis), Guduchi (Tinospora cordifolia), Neem (Azadirachta indica), Tulsi (Ocimum sanctum), Pudina (Mentha spicata) are available for treatment of various other conditions like general debility, to boost immunity and for treatment of skin infections. These are available either alone or in various combinations and are available in the form of syrups, elixirs, solution and solid dosage forms like lozenges and pills but not in the jelly form.
US6589543 describes a herbal ointment for soothing aches and pains includes a mixture of clove oil, ginger oil, wintergreen oil, peppermint oil, ginger root powder, cayenne powder and petroleum jelly.
Further GB1077722 discloses the herbal remedy comprising equal quantity of carum copticum, cinnamon camphora and mentha piperita with menthe sylvestria, honey, citric acid, sugar, ginger, alcohol, chicken fat and petroleum jelly for treating wounds and toothache.
CN 1090724 describes addition of Chinese herbal medicines for prevention and cure diseases to conventional raw materials to make jelly, so as to change drug application.
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The extracts of Adulsa (Adhatoda vasica), Jestimadh (Glycerrhiza glabra), Tulsi (Ocimum sanctum), Ginger (Zingiber officinale), Karpura ( Cinnamomum camphora), Pudina ka phool (Mentha spicata) either alone or in combination are available for the treatment of cough and similarly the extracts of Amla (Embelica officinalis), Guduchi (Tinospora cordifolia), Neem (Azadirachta indica), Tulsi (Ocimum sanctum), Pudina (Mentha spicata) either alone or in combination are available for treatment of various conditions like general debility, to boost immunity and for treatment of skin infections. However these are available in the form of syrups, elixirs, solution and solid dosage forms like lozenges and pills but not in the jelly form.
The above mentioned dosage forms in the prior art have several drawbacks.
The liquid dosage forms have the serious drawback of spillage leading to inaccurate dosing besides not being portable. Such dosage forms are also a serious impediment to administering medicine in case of elderly people, children and the infirm. Further solid formulation such as pills, tablets and capsules are difficult for elderly people, children and the infirm to swallow. Lozenge can cause choking in case of small children. Pills though easy to swallow are difficult to manufacture and demand high skill.
In case of herbal products in the liquid form, it has been observed that in some cases coarse particles of the extract settled down and spoil the appearance of the product as also affect efficacy.
In our invention however we use clear aqueous extract of the herb and hence no residue settles down thus maintaining elegance of the product. The extracts are processed such that no coarse particles are found in the product.
Hence there is a need to formulate a dosage form that is spill resistant, easy to administer at the same time being palatable and stable. Considering the drawbacks mentioned in the prior art our main objective is to develop a unique herbal dosage form
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in a semisolid jelly form for oral use and also provided is a squeezable package for administration of the same.
OBJECTIVES:
The main objective of the present invention is to develop a unique herbal pharmaceutical composition in a semisolid dosage form, more particularly jelly form for oral use.
Further objective of the present invention is to develop a herbal pharmaceutical dosage form useful for systemic treatment by the oral route in a form which is convenient to administer to children and convenient for self administration for adults.
Other objective is to develop herbal pharmaceutical dosage form which is transparent / translucent non-greasy semisolids containing the solubilised active substance in a sweetened, flavored base.
Further objective is to develop a novel pleasant tasting herbal pharmaceutical composition.
SUMMARY OF THE INVENTION:
The present invention discloses herbal pharmaceutical compositions comprising extracts of active herbal ingredients; one or more water soluble liquid base; water soluble jellant polymers; thickening agents, bulking agent, food acids, preservatives, sweeteners, colourants and flavourants in a spill resistant, palatable jelly form.
The herbal extracts are extracted from herbs like Adulsa, Jestimadhu, Tulsi, Ginger, Karpura (Camphor), Menthol (Pudina ka Phool), Guduchi, Elattaria cardamom, Cariophyllus aromaticus, Cinnamomum cassia, Cinnamomum iners, Piper longum,
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Helicters isora, Tinospora cardiofolia, Peucedanum graveolens, Apium graveolens, Embelica ribes, Eclipta alba, Cuminum cyminum, Zinger officinalis, Glycerrhiza glabra, Asparagus racemosus, Embellica officinalis, Piper nigrum or combination thereof.
The total concentration of active herbal ingredient in the extract is about 0.01 % to 3.0 % by weight of the total composition.
The one or more of a water soluble liquid base is palatable pharmaceutically acceptable vehicle, which dissolves and carry the active agent. The vehicles are selected from water, Propylene Glycol, Glycerin, Sorbitol solution, Liquid glucose, polyethylene glycol or mixtures thereof. The vehicles when used in combination can acts as co-solvent. The vehicles are added in an amount from 5.0 % to 95.0 % by weight of the total composition. The one or more liquid base comprises Purified water in an amount 10.0 % to 50.0 % by weight; Sorbitol solution in an amount 5.0 % to 25.0 % by weight; Liquid glucose 5.0 % to 25.0 % by weight and Glycerin 5.0 % to 25.0 % by weight of the total composition; polyethylene glycol 5 to 10 % by weight of the total composition or mixture thereof.
The sweeteners are selected from Sucrose, Glucose, Sorbitol, aspartame, sodium glyccerhizinate, cyclamate, sodium saccharin, etc or mixtures thereof. The sweeteners are added in an amount from 0.2 % to 50.0 % by weight of the total composition. The sucrose is added in an amount ranging from 5.0 % to 50.0 % by weight of the total composition. The sorbitol solution is added in an amount ranging from 5.0 % to 25.0 % by weight of the total composition. The liquid Glucose is added in an amount ranging from 5.0 to 25.0 % by weight of the total composition. The aspartame is added in an amount ranging from 0.2 % to 2.0 % by weight of the total composition. The sodium saccharine is added in an amount ranging from 0.2 to 2 % by weight of the total compositions.
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The bulking agents are selected from group comprising polysaccharide such as sucrose, sorbitol, liquid glucose, polyethylene glycol, glycerin and the like. The bulking agent is added in the range of 5.0 % to 50.0 % by weight of total weight of composition.
The jellying agent is selected from a group comprising such as polyacrylamides such as carbopol, xanthan gum, alginates, carageenan, tragacanth, sodium carboxy methyl cellulose, Methyl cellulose, Hydroxy propylmethyl cellulose, as against commonly used jellying agents like starches, gelatin, pectin, and their salts. The jellying agent is preferably carbopol and is added in a concentration ranging from 0.5 % to 2.0 % by weight of the total composition.
The thickening agent is selected from PEG 400, Propylene Glycol, Glycerin, liquid glucose and the like. The thickening agent is added in a concentration of 5 to 25 %.
The food acids are selected from mallic acid, citric acid, fumaric acid, adipic acid, and the like. The food acids are added in a concentration from 0.05 % to 1.0 % by weight of the total composition.
The chelating agent used is sodium EDTA and is added in the range of 0.02 to 1 % by weight of the total composition.
The preservatives are selected from Sodium Benzoate, Methyl Paraben, Propyl Paraben, and the like. The preservatives are added in concentrations 0.02 % to 0.5 % by weight of the total composition.
The colourant are selected from water soluble food colours of F D &C grades. The flavourant are selected from fruit flavours for oral liquid formulation.
The viscosity of the said compositions is in between 7500 to 25,000 cps.
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The composition comprises a combination of herbal extracts Adulsa, Tulsi, Ginger, Jestimadh, Camphor and Menthol at suitable concentrations from about 0.01 % to 2.0 % by weight; liquid base system which comprises purified water 10-50 %; sucrose 10 - 50.0 %; Liquid glucose 5 -25 %; sorbitol solution 5 - 25 %; Glycerin 5 - 25 %; aspartame 0.1-1 %; PEG 400 5-10 %; Carbopol 0.5 - 2.0 %; Disodium EDTA 0.02-1 %; Sodium benzoate 0.05 - 0.5 %, Citric acid 0.05 - 1 %; colour, carmoisine 0.008 %; flavour, mango 0.5 % and peppermint oil 0.04 %. The composition is used for treating cough.
The composition comprises a herbal extract of Guduchi ( Tinospora cordifolia), at concentration 2 % by weight of the total composition; liquid base system which comprises purified water 10 - 50 %; sucrose 10 - 50 %; Liquid glucose 5-25 %; sorbitol solution 5-25 %; Glycerin 5 - 20 %; PEG 400 5-10 %; Carbopol 0.5 -2.0 %; Disodium EDTA 0.02-1 %; Sodium benzoate 0.05 - 0.5 %; and flavour, Chocolate bourbon 0.25 %. The composition is used to boost immunity.
The composition comprises a combination of herbal extracts such as Elattaria cardamom 0.0072 %, Cariophyllus aromaticus 0.625 %, Cinnamomum cassia 0.0375 %, Cinnamomum iners 0.025 %, Piper longum 0.1 %, Helicters isora 0.0375 %, Tinospora cardiofolia 0.0125 %, Peucedanum graveolens 0.1 %, Apium graveolens 0.05 %, Embelica ribes 0.075 %, Eclipta alba 0.0625 %, Cuminum cyminum 0.1 %, Zinger officinalis 0.288 %; Glycerrhiza glabra 0.18 %; Asparagus racemosus 0.36 %; Embellica officinalis 0.36 % and Piper nigrum 0.15 %; liquid base system which comprises purified water 10-50 %; sucrose 10 - 50.0 %; Glycerin 5-20 %; Carbopol 0.5 - 2.0 %; Disodium EDTA 0.02-1 %; Sodium benzoate 0.05 - 0.5 %; methyl paraben 0.05-0.5 %; propyl paraben 0.05 to 0.5 %; flavour mango 0.5 %; Sodium saccharin 0.2 % and Colour Carmoisine, 0.008%. The composition is used to increase appetite.
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The present invention further describes a drug delivery system including a combination of a squeezable container and a semi solid pharmaceutical formulation.
DESCRIPTION OF THE INVENTION:
According to the present invention, there is provided a herbal pharmaceutical compositions in semisolid dosage form, particularly jelly form.
According to the present invention, the herbal pharmaceutical compositions in the form of water soluble jelly comprise active herbal ingredients in the form of extracts; one or more water soluble liquid base; water soluble jellant polymer; thickening agent, bulking agent, preservative; sweeteners, chelating agent, colourant and flavourants.
The compositions were spill resistant and palatable, easy to extrude from the container on to the spoon and easy to administer from spoon.
According to one of the embodiment of the present invention, the herbal pharmaceutical composition of cough in the form of jelly comprises herbal extracts of herbs like Adulsa, Jestimadhu, Tulsi, Ginger, Karpura (Camphor), and Menthol (Pudina ka Phool).
According to another embodiment of the present invention, the herbal pharmaceutical composition of improving immunity in the form of jelly comprises extract of herb, Guduchi.
According to yet another embodiment of the present invention, the herbal pharmaceutical composition for improving appetite in the form of jelly comprises extracts of herbs such as Elattaria cardamom, Cariophyllus aromaticus, Cinnamomum cassia, Cinnamomum iners, Piper longum, Helicters isora, Tinospora cardiofolia, Peucedanum graveolens, Apium graveolens, Embelica ribes, Eclipta alba, Cuminum
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cyminum, Zinger officinalis, Glycerrhiza glabra, Asparagus racemosus, Embellica officinalis and Piper nigrum.
The total concentration of active herbal ingredient in the extract used was about 0.01 % to 3.0 % by weight of the total composition.
The extracts used in the present composition were chosen to contain maximum amount of active ingredient by using only those extract which have specific plant part source, i.e. Adulsa leaf extract, Tulsi leaf extract, Jestimadh rhizome extract, Ginger rhizome extract, Pudina leaf extract, etc.
Also the coarse extracts were processed in such a way as to have maximum activity of herbal active ingredient and also to provide final clear jelly product. Before addition to the bulk the extract were suspended in water and heated at 40°C on water bath then filtered using suitable filtration technique preferably muslin to eliminate any coarse particles or extraneous material. The process was thus optimized to provide for maximum amount of active herbal ingredient for better therapeutic efficacy.
According to the present invention, the herbal pharmaceutical compositions comprise one or more of a water soluble liquid base which is a palatable pharmaceutically acceptable vehicle that dissolves and carry the active pharmaceutical agent. The vehicles were selected from water, Propylene Glycol, Glycerin, Sorbitol solution (70 % w/w), liquid glucose, polyethylene glycol and mixtures thereof.
The vehicles were present in an amount from 5.0 % to 95.0 % by weight of the total composition, preferably 10.0 to 75.0 % of total composition.
Purified water was present in an amount 10 % to 50 % by weight of the total composition; Sorbitol solution (70 %w/w) was present in an amount 5.0 % to 25.0 % by weight of the total composition; Liquid glucose was present in an amount 5.0 % to 25.0
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% by weight of the total composition and Glycerin was present in an amount 5.0 % to 25.0 % by weight of the total composition.
The vehicles were used alone or more preferably in combination to function as co-solvent system to dissolve all active herbal ingredients used thus providing for an elegant and effective formulation.
The present herbal pharmaceutical compositions comprise sweeteners to enhance its palatability. The sweeteners were selected from Sucrose, Glucose, Sorbitol, aspartame, sodium glyccerhizinate, cyclamate, sodium saccharin, etc. They were used either alone or in combination for better palatability by synergistic effect. Sweeteners were used in an amount from 0.2 % to 50 % by weight of the total composition.
The present herbal pharmaceutical compositions comprise preferred sweetener were Sucrose, Sorbitol, Liquid Glucose, Aspartame, sodium saccharine either alone or in combination. Sucrose was used in an amount ranging from 5.0 % to 50 % by weight of the total composition, preferably 20.0 % by weight of the total composition. Sorbitol solution (70 % w/w) was used in an amount ranging from 5.0 % to 25 % by weight of the total composition, preferably 10 % by weight of the total composition. Liquid Glucose was used in an amount ranging from 5.0 to 25 % by weight of the total composition, preferably 20.0 % by weight of the total composition. Aspartame was used in an amount ranging from 0.2 % to 2.0 % by weight of the total composition, preferably 0.4 % by weight of the total composition. Sodium saccharine was used in an amount ranging from 0.2 to 2 % by weight of the total composition, preferably 0.2 % by weight of the total composition.
The present herbal pharmaceutical compositions comprise bulking agent which" add volume to the preparation and were selected from group comprising polysaccharide such as sucrose, sorbitol, liquid glucose, polyethylene glycol 400, glycerin and the like. The bulking agents were added in the range of
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20 % to 70 % by weight of jelly, preferably 40.0 % to 70.0 % by weight of total weight of composition.
The present herbal pharmaceutical compositions comprise a pharmaceutically acceptable jellying agent which is compatible with other ingredients used in the formulation. It was selected from a group of acceptable jellying agents such as polyacrylamides (e.g. carbopol), xanthan gum, alginates, carageenan, tragacanth, sodium carboxy methyl cellulose, Methyl cellulose, Hydroxy propylmethyl cellulose, as against commonly used jellying agents like starches, gelatin, pectin, and their salts. In the present invention the preferred jellying gent was Carbopol. Carbopol gives high viscosity jelly at low concentration. The jellying agent was added in a concentration ranging from 0.5 % to 2.0 % by weight of the total composition, preferably 1.5 % by weight of the total composition.
The carbopol used in this invention was of the grade Carbopol 974P. Alternatively carbopol 971 P was used.
The thickening agents like PEG 400, Propylene Glycol, Glycerin, liquid glucose were used to increase viscosity of the formulation at a concentration of 5 to 25 %. The present invention comprises PEG 400 at a concentration of 5% as viscosity enhancer and glycerin in 5-25 % and liquid glucose in 5 - 25 % as viscosity enhancer and it also imparts sweetness and good mouth feel to the product.
The amount of viscosity enhancer and jellying agent used was optimized to achieve desired viscosity. The jelly should be viscous enough to resist spillage on tilting spoon yet comfortable enough to flow from container onto spoon. The viscosity of the present compositions was generally adjusted between 7500 to 25,000 cps, preferably 7500-9000 cps. The computations of the above viscosity were found most comfortable for administration. Viscosity was determined using Brookfield viscometer at 20 rpm spindle speed.
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The present herbal pharmaceutical compositions comprise food acids to make composition more pallatable. The food acids were selected from mallic acid, citric acid, fumaric acid, adipic acid, etc. These agents impart a certain tart taste to the formulation thus further enhancing palatability. The food acids were used in a concentration from 0.05 % to 1.0 % by weight of the total composition, preferably 0.1 % to 0.2 % by weight of the total composition.
The present herbal pharmaceutical compositions comprise preservatives. The preservatives were added to prevent microbial contamination in this aqueous system. The preservatives were selected from Sodium Benzoate, Methyl Paraben, Propyl Paraben and were added at a concentrations 0.02 % to 0.5 % by weight of the total composition.
Disodium EDTA was used as a chelating agent for improving stability and was used at concentration of 0.02 to 1 % by weight of the total composition.
In order to further enhance palatability and aesthetic value of the formulation, colour and flavor were included. The colourants were selected from water soluble food colourants of F D & C grades and were used at concentrations of 0.005 to 0.2 % by weight of the total composition. The flavourants were selected from fruit flavour for oral liquid formulation. Flavourants were used singly or in combination. Flavourants were added at concentration of 0.01 % to 1.0 % by weight of the total composition.
For the purpose of herbal cough jelly, peppermint oil was added in combination with fruity flavour, preferably mango flavour at a concentration of 0.01 % to 0.6 % w/w
The pH of the final herbal pharmaceutical compositions was kept at 6 to 7 which is found to be comfortable for oral ingestion. pH of the final compositions was adjusted using food acid and / or sodium hydroxide solution. The pH range of the present herbal
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pharmaceutical compositions was from 6.5 to 7.0, preferably 6.5. At this pH, the present compositions were found to be at its optimum palatability and stability.
The present invention thus omits the need for complex mechanical equipments employed in prior art such as pumps, syringes and elaborate measuring vessels without loss of ability and indeed with improved performance. This provides advantages in manufacturing, distribution, waste disposal and other economies as well resulted in a more cost effective formulation.
The invention further encompasses a squeezable plastic container such as tube provided with a cap, the material of the container used was preferably polypropylene. The delivery system may further comprise of a plastic spoon onto which the formulation is extruded. The receptacle, spoon was sized to hold a unit dose, to hold it conveniently without spilling and to be comfortable to hold and provide a good fit into the mouth between the lips for oral administration. The oval sectional shape of a typical teaspoon bowl was the preferred one since it satisfies the above criteria. The spoon was calibrated, was specially designed with two ends; one for 2.5 gm and the other for 5.0 gms.
A process for preparing the present herbal pharmaceutical compositions comprises the following steps:
1. Preparing the liquid base by dissolving sugar and preservatives in water to get syrup;
2. Adding bulking agent like Glycerin, Sorbitol, Liquid Glucose and polyethylene glycol 400 to the syrup;
3. Processing herbal extract by suspending calculated amount of herbal extract in water, heating at 40° C on water bath, filtering the suspension through suitable filter preferably muslin to obtain clear solution of extract, adding the herbal extracts to the syrup (bulk);
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4. Adjusting taste of the bulk by adding sweetener, flavourant, food acid;
5. Adding the colorant for enhancement of appearance to the bulk;
6. Adding volatile ingredients like peppermint oil, menthol and camphor to the bulk;
7. Preparing the smooth thick slurry by hydrating the jellant polymer in required amount of water;
8. Adding the thick slurry to bulk under stirring;
9. Adjusting the final volume and pH to effect final product i.e. jelly
According to the present invention, the herbal pharmaceutical composition in the form of herbal cough jelly comprises a combination of herbal extracts of Adulsa, Tulsi, Ginger, Jestimadh, Camphor and Menthol at suitable concentrations in a sweetened and flavoured aqueous jelly based system.
The herbal extracts comprise 0.4 % w/w Adulsa, 0.02 % w/w Tulsi, 0.24 % w/w Ginger, 0.5 % w/w Jestimadh, 0.004 % w/w Camphor and 0.0015 % w/w Menthol by weight of the total composition.
The jelly base system comprises purified water 10-50 %, sucrose 10 - 50 %, Liquid glucose 5 -25 %, sorbitol solution 5 -25 %, Glycerin 5 - 25 %. The cough jelly comprises aspartame 0.1 - 1.0 %, PEG 400 5-10 %, Carbopol 0.5 - 2.0 %, Disodium EDTA 0.02-2.0 %, Sodium benzoate 0.05 - 1.0 %, Citric acid 0.05 - 1 %. The herbal cough jelly comprises colour carmoisine and flavour mango along with peppermint oil that enhances oraganoleptic properties of the product
The preferred jelly base system comprises purified water 20 - 25 %, sucrose 20.0 %, Liquid glucose 20.0 %, sorbitol solution 20.0 %, Glycerin 10.0 %. The herbal cough jelly comprises aspartame 0.40 %, PEG 400 5.0 %, Carbopol 974 P 1.5 %, Citric acid 0.125 %, colour carmoisine 0.008 %, flavour mango 0.5 % and peppermint oil 0.04 %
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The viscosity of the final herbal cough jelly was around 7500 cps and the pH was 6.5.
According to the present invention, the herbal pharmaceutical composition in the form of herbal jelly to boost immunity comprises a herbal extract of Guduchi (Tinospora cordifolia), at suitable concentrations in a sweetened and flavoured aqueous jelly based system.
The extract of Guduchi was added at concentration 2 % by weight of the total composition.
The jelly base system comprises purified water 10-50 %, sucrose 10 - 30.0 %, Liquid glucose 5-25 %, sorbitol solution 5 -25 %, Glycerin 5-25 %. The herbal jelly comprises PEG 400 5 -10 %, Carbopol 0.5-2.0 %, DisodiumEDTA 0.02-2.0 %, Sodium benzoate 0.05 - 1.0 %. The herbal jelly comprises flavour Chocolate Bourbon.
The preferred jelly base system comprises purified water 20 - 35 %, sucrose 30.0 %, Liquid glucose 10.0 %, sorbitol solution 10.0 %, Glycerin 10.0 %. The herbal cough jelly comprises PEG 400 5.0 %, Carbopol 974 P 1.5 %, flavour Chocolate bourbon, 0.25 %, Sodium benzoate, 0.2 %, Disodium EDTA, 0.05 %.
The viscosity of the final herbal jelly to boost immunity was around 8000 cps and the pH was 6.5.
According to the present invention, the herbal pharmaceutical composition in the form of herbal jelly to increase of appetite comprises a combination of herbal extracts such as Elattaria cardamom; Cariophyllus aromaticus; Cinnamomum cassia; Cinnamomum iners; Piper longum; Helicters isora; Tinospora cardiofolia; Peucedanum graveolens; Apium graveolens; Embelica ribes; Eclipta alba;Cuminum cyminum; Zinger officinalis;
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Glycerrhiza glabra; Asparagus racemosus; Embellica officinalis; and Piper nigrum at suitable concentrations in a sweetened and flavoured aqueous jelly based system.
According to the present invention, the herbal pharmaceutical composition in the form of herbal jelly to increase of appetite comprises a combination of herbal extracts such as Elattaria cardamom at the concentration of 0.0072%; Cariophyllus aromaticus at the concentration of 0.625%; Cinnamomum cassia at the concentration of 0.0375%; Cinnamomum iners at the concentration of 0.025%; Piper longum at the concentration of 0.1%; Helicters isora at the concentration of 0.0375%; Tinospora cardiofolia at the concentration of 0.0125%; Peucedanum graveolens at the concentration of 0.1%; Apium graveolens at the concentration of 0.05%; Embelica ribes at the concentration of 0.075%; Eclipta alba at the concentration of 0.0625%; Cuminum cyminum at the concentration of 0.1%; Zinger officinalis at the concentration of 0.288%; Glycerrhiza glabra at the concentration of 0.18%; Asparagus racemosus at the concentration of 0.36%; Embellica officinalis at the concentration of 0.36%; and Piper nigrum at the concentration of 0.15% in a sweetened and flavoured aqueous jelly based system.
The jelly base system comprises purified water 10-50 %, sucrose 10 - 50.0 %, Glycerin 5-20 %. The herbal jelly comprises Carbopol 0.5 - 2.0 %, Disodium EDTA 0.02-2.0 %, Sodium benzoate 0.05 - 0.5 %, methyl paraben 0.05-1.0 %, propyl paraben 0.05 to 1.0 %. The herbal jelly comprises colour Carmoisine and flavour mango along with sodium sachharine.
The preferred jelly base system comprises purified water 20-35 %, sucrose 50.0 %, Glycerin 10.0 %. The herbal cough jelly comprises Carbopol 974 P 1.5 %; flavour mango, 0.5 %; Sodium saccharin, 0.2%; Sodium benzoate, 0.5 %; methyl paraben, 0.2 %, propyl paraben 0.07 %, Disodium EDTA, 0.05 %; and Colour Carmoisine, 0.008%.
The viscosity of the final herbal jelly was around 8000cps and the pH was 6.5.
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The semisolid oral formulation prepared according to the present invention was not a mere admixture but has properties different from the sum total of the properties of its individual ingredients.
It will be readily apparent to one skilled in the art that varying substitutions and modifications may be made to the invention disclosed herein without departing from the scope and spirit of the invention. Thus, it should be understood that although the present invention has been specifically disclosed by preferred embodiments and optional features, modification and variation of the concepts herein disclosed may be resorted to by those skilled in the art, and that such modifications and variations are considered to be falling within the scope of the invention.
The following examples are for the purpose of illustration of the invention only and are not intended in any way to limit the scope of the invention.
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Example 1
Table 1: Herbal Composition for Cough

Ingredient % by weight
Adulsa extract 0.4
Jestimadh extract 0.5
Tulsi extract 0.02
Ginger extract 0.24
Karpura 0.004
Menthol 0.0015
Peppermint oil 0.04
Sucrose 20
Sorbitol 20
Liquid Glucose 20
Glycerin 10
PEG 400 5
Carbopol 974 P 1.5
Sodium benzoate 0.2
Disodium EDTA 0.05
Aspartame 0.4
Citric acid monohydrate 0.125
Colour: Carmoisine 0.008
Flavour: mango 0.5
Purified water q.s. 100
(q.s.: - quantity sufficient)
The viscosity of the final herbal jelly was around 7500 cps and the pH was 6.5.

The herbal jelly was studied for stability by subjecting it to various conditions of temperature and humidity for suitable period of time i.e. at 40°C / 75 % RH and at room temperature. It was found that the herbal jelly was sufficiently stable at these conditions and hence shelf life of the final herbal jelly can be proposed as three years.
A dose of 2-3 teaspoonfuls per day gives relief from symptoms of cough.
Example 2
Table 2: Herbal Composition to boost immunity

Ingredient % by weight
Guduchi (Tinospora cordifolia) aqueous extract 2
Sucrose 30
Sorbitol 10
Liquid Glucose 10
Glycerin 10
PEG 400 5
Carbopol 974 P 1.5
Flavour: Chocolate bourbon 0.25
Sodium benzoate 0.2
Disodium EDTA 0.05
Purified water q.s. 100
The viscosity of the final herbal jelly was around 8000 cps and the pH was 6.5.
The herbal jelly was studied for stability by subjecting it to various conditions of temperature and humidity for suitable period of time i.e. at 40°C / 75 % RH and at room temperature. It was found that the herbal jelly was sufficiently stable to these conditions and hence shelf life of the final product can be proposed as three years.
The herbal jelly was to boost immunity.
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Example -3
Table 3: Herbal composition for increase of appetite.

Ingredient % by weight
Elattaria cardamom 0.0072
Cariophyllus aromaticus 0.625
Cinnamomum cassia 0.0375
Cinnamomum iners 0.025
Piper longum 0.1
Helicters isora 0.0375
Tinospora cardiofolia 0.0125
Peucedanum graveolens 0.1
Apium graveolens 0.05
Embelica ribes 0.075
Eclipta alba 0.0625
Cuminum cyminum 0.1
Zinger officinalis 0.288
Glycerrhiza glabra 0.18
Asparagus racemosus 0.36
Embellica officinalis 0.36
Piper nigrum 0.15
Sucrose 50
Glycerin 10
Carbopol 974 P 1.5
Sodium benzoate 0-5
Methyl paraben 0.2
Propyl Paraben 0.07
Disodium EDTA 0.05
Sodium saccharin 0.2
Colour :Carmoisine 0.008
Flavour: mango 0.5
Purified water q.s.100
(q.s-quantity sufficient)
The viscosity of the final herbal jelly was arovind 8000cps and the pH was 6.5.
The herbal jelly was studied for stability by subjecting it to various conditions of temperature and humidity for suitable period of time i.e. at 40°C/ 75% RH and at room
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temperature. It was found that the herbal jelly was sufficiently stable to these conditions and hence shelf life of the final product can be proposed as three years.
The herbal jelly was for improving appetite.
The advantages of the present invention are manifold and range from simplicity of processing and greater stability of formulation to better patient compliance and more cost effectiveness. The present invention provides a highly palatable spill resistant and stable jelly formulation for herbal based active ingredient. The formulation and process eliminate the use of expensive equipment. The extraction process was optimized as to ensure maximum activity of herbal ingredients and hence maximum therapeutic efficacy of the final product. The final product thus was more user friendly and more efficacious, thus improving patient compliance especially pediatric compliance.
The present invention describes a drug delivery system which includes a combination of a squeezable container and a semi solid pharmaceutical formulation. Each of these elements of the drug delivery system has certain characteristics which are as follows:
1) Allows easy administration of measured amount of drug.
2) Provides for resistance to spillage
3) Provides suitable storage for stable pharmaceutical composition with compatible components.
4) Provides for a highly palatable formulation which improves patient compliance especially pediatric compliance
The present herbal jelly has a number of advantages over conventional oral dosage forms which are as follows:
1. They were semisolid and hence can be adjusted to suitable viscosity to be spill -resistant
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2. Due to high viscosity they are easy for handling, storing, and easy to carry (portable)
3. Ease of administration and measurement ensures correct dosage in case of children, the elderly and the infirm
4. Storage stable upto 2-3 years at room temperature, i.e. retains its viscosity
5. Ease of extrudability from pack and spreadability onto spoon (but does not spill from the spoon easily). Hence elegant and easy to use in case of children, the elderly and the infirm. This allows for self administration and hence improves patient compliance.
6. Attractive in appearance, suitable texture, delicious in taste and mouth feel hence gives better pediatric compliance.
7. Components are compatible: do not affect bioactivity of active ingredients or physical properties of vehicle
8. Eliminates need for complex mechanical equipment. Requires simple equipments like jacketed S. S. tanks with stirrer
9. It is easier to measure than a liquid and easier to swallow than a solid
10. Due to its high viscosity compared to liquid dosage forms, it remains in contact with the throat for longer time, soothing the throat and providing relief for longer time compared to liquid or solid dosage forms.
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11. In case of herbal products in the liquid form, it has been observed that in some cases coarse particles of the extract settled down and spoil the appearance of the product as also affect efficacy while in our invention we use clear aqueous extract of the herb and hence no residue settles down thus maintaining elegance of the product. The extracts are processed such that no coarse particles are found in the product.
12. The source of herbal extracts chosen is such that it contains maximum active ingredient since extracts are from specific plant parts, e.g. Tulsi leaf extract, Adulsa leaf extract, Ginger rhizome extract, etc.
13. Also processing of herbal extracts is optimized to have its maximum efficacy by heating coarse extract at 40° C in purified water. This ensures better therapeutic efficacy of the product.
14. The other ingredients used in the formulation like propylene glycol, aspartame, glucose further enhance the taste and provide for a extremely pleasant tasting composition. By virtue of its viscosity, the formulation covers the tongue and taste buds for a longer time resulting in improved palatability over conventional liquid / solid dosage forms.
15. The product is presented in a very elegant package of closed squeezable polypropylene tube with replacement cap. Also a calibrated plastic spoon for measuring and administering the product is provided. These features make the product highly consumer friendly.
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We claim,
1. Herbal pharmaceutical compositions comprising one or more extracts of active herbal ingredients; one or more water soluble liquid base; water soluble jelling agents; bulking agents; food acids; preservatives; sweeteners; colourants and flavourants in a spill resistant, palatable jelly form for treating cough, improving immunity and increasing appetite.
2. The compositions as claimed in claim 1, wherein said herbal extracts are selected from Adulsa, Jestimadhu, Tulsi, Ginger, Karpura (Camphor), Menthol (Pudina ka Phool), Guduchi, Elattaria cardamom, Cariophyllus aromaticus, Cinnamomum cassia, Cinnamomum iners, Piper longum, Helicters isora, Tinospora cardiofolia, Peucedanum graveolens, Apium graveolens, Embelica ribes, Eclipta alba, Cuminum cyminum, Zinger officinalis, Glycerrhiza glabra, Asparagus racemosus, Embellica officinalis, Piper nigrum or combination thereof.
3. The compositions as claimed in claims 1 and 2, wherein the total concentration of said active herbal ingredient in said extract is about 0.01 % to 3.0 % by weight of the total composition.
4. The compositions as claimed in claim 1, wherein said one or more of the water soluble liquid base is vehicle.
5. The compositions as claimed in claims 1 and 4, wherein said vehicles are selected from water, Propylene Glycol, Glycerin, Sorbitol solution, Liquid glucose, polyethylene glycol 400 or mixtures thereof.
6. The compositions as claimed in claimsl, 4 and 5, wherein said vehicles are added in an amount from 5.0 % to 95.0 % by weight of the total composition.
7. The compositions as claimed in claims 1 and 4 to 6, wherein said one or more liquid base comprises purified water in an amount 10.0 % to 50.0 % by weight; sorbitol solution in an amount 5.0 % to 25.0 % by weight; liquid glucose 5.0 % to 25.0 % by weight; glycerin .5.0 % to 25.0 % by weight; polyethylene glycol 400 5 to 10 % by weight of the total composition or mixtures thereof.


8. The compositions as claimed in claim 1, wherein said sweeteners are selected from Sucrose, Glucose, Sorbitol, aspartame, sodium glycerhizinate, cyclamate, sodium saccharin or mixtures thereof.
9. The compositions as claimed in claim 8, wherein said sweeteners are added in an amount from 0.2 % to 50.0 % by weight of the total composition.
10. The compositions as claimed in claims 8 and 9, wherein said sucrose is added in an amount ranging from 5.0 % to 50.0 % by weight of the total composition.
11. The compositions as claimed in claims 8 and 9, wherein said sorbitol solution is added in an amount ranging from 5.0 % to 25.0 % by weight of the total composition.
12. The compositions as claimed in claims 8 and 9, wherein said liquid Glucose is added in an amount ranging from 5.0 to 25.0 % by weight of the total composition.
13. The compositions as claimed in claims 8 and 9, wherein said aspartame is added in an amount ranging from 0.2 % to 2.0 % by weight of the total composition.
14. The composition as claimed in claims 8 and 9, wherein said sodium saccharine is added in an amount ranging from 0.2 % to 2.0 % by weight of the total composition.
15. The compositions as claimed in claiml, wherein said bulking agent is selected from group comprising polysaccharides such as sucrose, sorbitol, liquid glucose and polyethylene glycol.
16. The compositions as claimed in claims 1 and 15, wherein said bulking agent is added in the range of 5.0 % to 50.0 % by weight of the total composition.
17. The compositions as claimed in claim 1, wherein said jelling agent is selected from a group of hydrophilic polymers comprising carbopol, xanthan gum, alginates, carageenan, tragacanth, sodium carboxy methyl cellulose, Methyl cellulose, Hydroxy propylmethyl cellulose as against commonly used jelling agents like starches, gelatin, pectin and their salts.
18. The compositions as claimed in claim 17, wherein said jelling agent is preferably carbopol and is added in a concentration ranging from 0.5 % to 2.0 % by weight of the total composition.

19. The compositions as claimed in claim 1, wherein said thickening agent is selected from PEG 400, polyethylene glycol, Glycerin and liquid glucose.
20. The compositions as claimed in claims 1 and 19, wherein said thickening is added in concentration of 5.0 % to 25.0 % by weight.
21. The compositions as claimed in claim 1, wherein said food acid is selected from mallic acid, citric acid, fumaric acid, adipic acid and the like.
22. The compositions as claimed in claims 1 and 21, wherein said food acid is added in a concentration from 0.05 % to 1.0 % by weight of the total composition.
23. The compositions as claimed in claim 1, wherein said preservative is selected from Sodium Benzoate, Methyl Paraben, Propyl Paraben and the like.
24. The compositions as claimed in claims 1 and 23, wherein said preservative is added in concentrations 0.02 % to 0.5 % by weight of the total composition..
25. The compositions as claimed in claims 1, wherein said chelating agent is sodium EDTA and is added in an amount ranging from 0.02 % to 1 % by weight of the total composition.
26. The compositions as claimed in claim 1, wherein said colourant are selected from water soluble food colors of F D &C grades.
27. The compositions as claimed in claims 1, wherein said flavourant are selected from fruit flavours suitable for oral semisolid formulation.
28. The compositions as claimed in claim 1 to 27, wherein the viscosity of the said composition is in the range of 7500 to 25,000 cps.
29. The compositions as claimed in claim 1 to 28, wherein said composition used for the treating cough comprises a combination of herbal extracts Adulsa, Tulsi, Ginger, Jestimadh, Camphor and Menthol at suitable concentrations from about 0.01 % to 3.0 % by weight; liquid base system which comprises purified water 10 - 50 %; sucrose 10 - 50.0 %; Liquid glucose 10 -25.0 %; sorbitol solution 5 -25.0 %; Glycerin 5 - 25 %; aspartame 0.1 - 1. 0 %; PEG 400 5-10 %; Carbopol 0.5 - 2.0 %; Disodium EDTA 0.02-1.0 %; Sodium benzoate 0.05 - 0.5 %, Citric acid 0.05 - 1 %; colour, carmoisine 0.008 %; flavour, mango 0.5 % and peppermint oil 0.04 %.

30. The pharmaceutical compositions as claimed in claim 1 to 28, wherein said composition used for treating boost immunity comprises a herbal extract of Guduchi ( Tinospora cordifolia), at concentration 2 % by weight of the total composition; liquid base system which comprises purified water 10-50 %; sucrose 10 - 50.0 %; Liquid glucose 5 -25.0 %; sorbitol solution 5 - 25.0 %; Glycerin 5 - 25 %; PEG 400 5.0 - 10.0 %; Carbopol 0.5 - 2.0 %; Disodium EDTA 0.02-1.0 %; Sodium benzoate 0.05 - 0.5 %; and flavour Chocolate bourbon, 0.25 %.
31. The pharmaceutical compositions as claimed in claim 1 to 28, wherein said composition used to increase appetite comprises a combination of herbal extracts such as Elattaria cardamom 0.0072 %, Cariophyllus aromaticus 0.625 %, Cinnamomum cassia 0.0375 %, Cinnamomum iners 0.025 %, Piper longum 0.1 %, Helicters isora 0.0375 %, Tinospora cardiofolia 0.0125 %, Peucedanum graveolens 0.1 %, Apium graveolens 0.05 %, Embelica ribes 0.075 %, Eclipta alba 0.0625 %, Cuminum cyminum 0.1 %, Zinger officinalis 0.288 %; Glycerrhiza glabra 0.18 %; Asparagus racemosus 0.36 %; Embellica officinalis 0.36 % and Piper nigrum 0.15 %; liquid base system which comprises purified water 10 - 50 %; sucrose 10 -50.0 %; Glycerin 5 - 25 %; Carbopol 0.5 - 2.0 %; Disodium EDTA 0.02-1.0 %; Sodium benzoate 0.05 - 0.5 %; methyl paraben 0.05-0.5 %; propyl paraben 0.05 to 0.5 %; flavour mango 0.5 %; Sodium saccharin 0.2 % and Colour Carmoisine, 0.008%.
32. Herbal pharmaceutical compositions in ready-to eat jelly form as substantially described herein with reference to the foregoing examples 1 to 3.
Dated this 28th day of December 2004
Dr. Gopakumar G. Nair Agent for the Applicant

Documents:

1333-mum-2003-cancelled pages(03-01-2007).pdf

1333-mum-2003-claims(granted)-(03-01-2007).doc

1333-mum-2003-claims(granted)-(03-01-2007).pdf

1333-mum-2003-correspondence (01-01-2008).pdf

1333-mum-2003-correspondence(ipo)-(19-01-2007).pdf

1333-mum-2003-form 1(30-12-2003).pdf

1333-mum-2003-form 18(25-01-2006).pdf

1333-mum-2003-form 2(granted)-(03-01-2007).doc

1333-mum-2003-form 2(granted)-(03-01-2007).pdf

1333-mum-2003-form 26(09-12-2003).pdf

1333-mum-2003-form 3(30-12-2003).pdf

1333-mum-2003-form 5(29-12-2004).pdf


Patent Number 213402
Indian Patent Application Number 1333/MUM/2003
PG Journal Number 04/2008
Publication Date 25-Jan-2008
Grant Date 01-Jan-2008
Date of Filing 30-Dec-2003
Name of Patentee M/S. LYKA LABS LIMITED
Applicant Address 77, NEHRU ROAD, VILE PARLE(EAST), MUMBAI-400099
Inventors:
# Inventor's Name Inventor's Address
1 SAMANT RAJAN SHANTARAM M/S LYKA LABS LIMITED 77, NEHRU ROAD, VILE PARLE(EAST), MUMBAI-400099
2 SHAH MAHENDRA CHIMANLAL LYKA LABS LIMITED 77, NEHRU ROAD, VILE PARLE(EAST), MUMBAI-400099
3 SHAH HARAKHCHAND KESHAVJI LYKA LABS LIMITED 77, NEHRU ROAD, VILE PARLE(EAST), MUMBAI-400099
4 SANGODKAR SONAL RAJENDRA LYKA LABS LIMITED 77, NEHRU ROAD, VILE PARLE(EAST), MUMBAI-400099
PCT International Classification Number A61K35/78
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA