Title of Invention	A PROCESS OF MANUFACTURE OF AN OPHTHALMIC PREPARATION, AN EYE DROP FROM NATURALLY OCCURRING SUBSTANCES FOR TREATING CERTAIN AILMENTS OF HUMAN EYE
Abstract	. ABSTRACT This invention relates to a process of manufacture of a hebo-mineral medicine- r eye drops' for treating pathogenic conditions of the human eye from naturally occurring substances of herbal and mineral origin containing the active principle namely, an alkaloid and glycerine and preservative. The present invention provides a process for preparation of a herbo-mineral medicine being an eye drop comprising the steps: 1. grinding and crushing and refining of a herb Punarnava/Baskhapra and shoraka/shora kalmi into a fine powder form, or alternatively preparing an aqueous extract of the herb and reduce it to 1/5 th of the ingredient's quantity and 2. mixing the same and dissolving in glycerine with stirrers at laboratory temperature, 3. and thereafter filtering the entire solution through a fine but neutral medium using pressure filtration technique, 4. and storing in a sterile vessel to obtain a crystal clear solution and 5. filling up in sterile bottles or vials as the case may be for use in human eye treatment.

Title of Invention

A PROCESS OF MANUFACTURE OF AN OPHTHALMIC PREPARATION, AN EYE DROP FROM NATURALLY OCCURRING SUBSTANCES FOR TREATING CERTAIN AILMENTS OF HUMAN EYE

Abstract

. ABSTRACT This invention relates to a process of manufacture of a hebo-mineral medicine- r eye drops' for treating pathogenic conditions of the human eye from naturally occurring substances of herbal and mineral origin containing the active principle namely, an alkaloid and glycerine and preservative. The present invention provides a process for preparation of a herbo-mineral medicine being an eye drop comprising the steps: 1. grinding and crushing and refining of a herb Punarnava/Baskhapra and shoraka/shora kalmi into a fine powder form, or alternatively preparing an aqueous extract of the herb and reduce it to 1/5 th of the ingredient's quantity and 2. mixing the same and dissolving in glycerine with stirrers at laboratory temperature, 3. and thereafter filtering the entire solution through a fine but neutral medium using pressure filtration technique, 4. and storing in a sterile vessel to obtain a crystal clear solution and 5. filling up in sterile bottles or vials as the case may be for use in human eye treatment.

Full Text	This invention relates to a process of manufacture of an ophthalmic preparation, an eye drop, from naturally occurring substances in an innovative combination for treating pathogenic, allergic and chemical imbalances of the human eye. INTRODUCTION Medicinal preparations have been classified according to the system of medicines adopted as allopathic. Ayurvedic, Unani, Siddha and Homeopathic etc. In the modern method of treatment by use of eye drops for the ailments of the eyes, there are many allopathic drugs which"* are manufactured and made available in the market. Most of these medicines- allopathic or other suffer from one or the other drawbacks or side effects which may not be apparent immediately and also lead to immunity to the drugs. Furthermore, the manufacture of these drugs requires synthetic raw materials, sophisticated plant and machinery. Whereas in the Indian Systems medicinal manufactury, the equipments are less expensive and less time consuming. In the circumstances, there has been a great interest in natural medicine the world over for safety concerns- namely the occassional adverse reactions and side effects that entail usage of an allopathic formulation. Traditional systems of medicine in India consist mainly of Ayurveda, Unani and Siddha. The medicines made under these systems use drug material of plant, mineral and animal origin which are well documented in the traditional and scientific literature for their healing properties. These systems are very similar in terms of drug material used which is mostly common among them. Some differences can be there in the process of making a medicine, and, the philosophy of treatment. However, the medicines are acknowledged as safe to use, and so spread over a long period. Medicines under the ISM are today manufactured following Good Manufacturing Practices (GMP) norms laid down by the Government of India. THE PRESENT INVENTION The present invention uses active ingredients from nature. A manufacture of the present invention will need to be within the purview of a medicinal system of natural products. Using the active ingredients in the present invention a manufacture of the present invention can be taken up as a proprietary Indian Systems (Ayurvedic/Unani) medicine. There is no eye drops mentioned as such in the traditional reference texts on Indian Systems of Medicine. Any such formulation shall have to be made (1) only from the active pharmaceutical ingredients which figure in the approved lists of drugs of plant, animal and mineral origin in the formularies of Ayurvedic and Unani medicines brought out by the Govt, of India (for use for various ailments), (2) as per the guidelines laid down in the Drugs & Cosmetics Act for allopathic eye drops, (3) and has to be sterile and prepared following a modern scientific methodology. Consequently, the methodology for such preparation has to be developed anew which will evolve as the method of preparation of the invention is perfected. The present invention addresses all the concerns mentioned above. It involves drug material used in the Indian Systems of Medicine in an innovative combination and improves upon them by refining and processing the ingredients with catalysts and use of an effective solvent for treatment of pathogenic, allergic and chemical imbalances of the human eye. The active pharmaceutical ingredients used in the formulation are of natural origin and not synthetic. As single drugs, these are not very useful. The present invention uses herbo-mineral ingredients which are processed so as to have their healing effect well enhanced. The present invention has a herbal component in a form that ensures that its active principle, namely an alkaloid Punarnavine is present. It is processed with a mineral and provided 3 in a known solvent glycerine which further enhances the healing effect of the ingredients. The present invention is preserved with an approved preservative. The end product has been found agreeable to the human eye. The present invention relates to a complete development of the formulation and process of preparation to eventually produce a sterile, user-friendly formulation which can be used over a long period without causing any allergic, adverse reactions or side effects. The method of treatment is topical application of the formulation.'In essence, the primary* object of the present invention is: 1. To provide in particular a process for manufacture of an eye drop from herbo- mineral substances containing an alkaloid as an active principle dissolved in glycerine and an approved preservative; 2. To provide a particular formulation for the treatment of specific eye conditions- pathogenic, allergic and chemical disequilibrium conditions; the treatment is by topical application of the formulation; 3. To provide an ophthalmic preparation which is new, effective and economical. THE INVENTION AND THE PROCESS OF INVENTION According to the present invention a formulation is prepared in a known solvent from active ingredients which have therapeutic properties to which a particular condition being treated is responsive. 1. Form of the invention: eye drops It is a proprietary medicine which is within the Indian Systems {Ayurvedic & Unani) of Medicine. 2. Formula: I. ACTIVE INGREDIENTS Sanskrit/Urdu name Botanical/Latin name Quantity taken 1. Punarnava/ Boerhavia diffusa 100 gm Biskhapra 2. Shoraka/ Potassi Nitras 25 gm shora kalmi II. SOLVENT Glycerine 1000 gm * It is to be emphasized that the process makes the alkaloid Punarnavine act with Potassi Nitras in I above and the solvent mentioned in II above and makes it have greater arid marked effect on the opacities in the lens and cornea, as also their use in this combined form. Method of preparation: The examples of the preparation and the process of manufacture of the present invention provided herein illustrate the scope of the invention and not intended to be limiting. Other applications of aspects of the present invention within the broad scope will be apparent to those skilled in the art. According to the present invention there is provided a process of manufacture of an eye drop for treating certain ailments of the human eye from naturally occurring substances comprising the steps of (a) grinding to a fine powder of a required quantity of shoraka/shora kalmi (Potassi Nitras) (b) crushing and refining punarnava/baskhapra (Boerhaavia diffusa) of an appropriate quantity and, (c) mixing the fine powder of (a) and (b) and (d) dissolving the mixture of the powders of (c) in glycerine with mechanical stirrers (e) at laboratory temperatures for twelve hours and thereafter (f) filtering the entire solution through a fine but neutral medium using pressure filtration technique (g) obtaining a crystal clear solution and store in a sterile vessel; (h) thereafter to fill up the solution in bottles and vials as injectables for dispensation in retail containers. The following examples illustrate the preparation of the eye drop of the present invention. Example I: Take the second ingredient in proportionate measures and grind well to a fine powder. Crush the first ingredient taken in appropriate quantity and properly mix it with shora kalmi dissolved into glycerine with a mechanical stirrer at 180 degree temperature, and allow it to settle down for a time upto 12 hours. Filter the entire solution using the expansion of a compressed gas, to be termed hereafter the pressure filtration technique, through a very fine but neutral medium to obtain a crystal clear solution and store in a sterile vessel. An automatic vial filling is then done in a very clean and secluded area which is airconditioned and fumigated. The purpose of glycerine is to serve as a vehicle for the ingredients. It too has a pharmacological action and acts as a preservative. Example II: It is to be noted that not all the chemical compounds in a plant are of equal interest in the present context. The active principles are alkaloids or glycosides. Other groups such as carbohydrates, fats and proteins are of dietic importance and many others such as starches and gums, though used in pharmacy, lack any marked pharmacological action. This method makes sure that the alkaloid Punarnavine is present in the eye drop of the invention. This is made possible by the use of aqueous extract of the herb. The used extract is taken 1/5 of the ingredient's normal quantity as mentioned above in the formula. This proportion relates to the richness of the alkaloid Punarnavine present in the drug and keeps the water content in the eye drop of the invention to minimum. As in the Example I, the-aqueous extract taken in appropriate quantity is properly mixed with shora kalmi dissolved into glycerine with a mechanical stirrer at 180 degree temperature, and allow the end product to settle down for a time upto 12 hours. Filter the entire solution using the pressure filtration technique through a very fine but neutral medium to obtain a crystal clear solution and store in a sterile vessel. An automatic vial filling is then done in a very clean and secluded area which is airconditioned and fumigated. The purpose of glycerine is to serve as a vehicle for the ingredients. It has its own pharmacological action and acts as a preservative. For the sake of batch consistency, any one of the options about the first ingredient as distinguished in the Example I and Example II can be used. Preservative used in Example I and Example II is Phenyl Mercuric Nitrate. PHARMACOLOGICAL ACTION OF THE DRUGS USED IN THE INVENTION Name of the ingredients Properties Pharmacological action Side Effects and adverse reaction 1. Biskhapra controls oedema. Enhances corneal improves sight. clarity; in immature cataract, it resolves the already coagulated ** protein fibres of the lens and prevents further coagulation or delays it. It has a cooling effect on eyes afflicted with conjunctivitis. Presence of potassium salts in this make the active alkaloid more effective. No side effects or adverse reaction 2. Shora Kalmi cooling, antimicrobial, It cools the eyes and works on infections. Its presence in the solution strenthens the action of the active alkaloid in biskhapra. No side effects or adverse reaction 3. Glycerine A vehicle for It has a softening effect. No side effects the above drugs; draws out watery fluids, or adverse emollient, retains drugs more reaction hygroscopic, effectively, antimicrobial. NOTE: The ingredients and the solvent have been so processed and assimilated that together they synergize to absorb the lens-, corneal and vitreous opacities, Also being moderately hypertonic, the invention reduces fluid collected in the cornea (corneal oedema) through an osmotic action that enhances its clarity. The overall effect is to prevent the formation of cataract or, at the worst, delay the progress of cataract. The present invention has been tested to have a pH value in the range 4.0 -7.0. This is well within the acceptable range of pH values of 3.5 - 10.5 for an eye drop in the allopathic system. The present invention can be stored at room temperature. 7 THERAPEUTIC INDICATIONS The present invention has been found effective in various ailments of the eyes, such as .opacities of the lens, corneal and vitreous opacities, conjunctivitis, watery discharge and headaches resulting from eye ailments. Users have found it useful in dry eyes condition. Clinical tests have shown its effect on the blurred and diminished vision caused by cataract in various stages. It has been found safe to use; its ingredients have antimicrobial property. SPECIFIC EYE AILMENTS ADDRESSED Some specific eye ailments where the present invention has been indicated are described morefully below. Usage in operated eye The present invention has been tried on persons who have an Intra Occular Lens implant after a surgery. This has shown a progressive improvement in the eye condition. As a precaution, in such patients, the use of the present invention {the eye drops) should be recommended only after 6 months or more from the date of operation when the eye is in a state of good health and thereafter continue with the medicine if there is no marked improvement after the surgery. Otherwise, wash the eyes with clean water and stop the usage of the medicine. Dry eyes Human tears are composed of water, electrolytes, carbohydrates, lipids and proteins with many having an enzymic function. The dry eye condition results due to insufficient tear production, excessive tear evaporation or abnormal tear composition. Symptoms of dry eye include itching, irritation, sensitivity to light, blurred vision and contact lens intolerance. As there is not enough support by tears to the ocular epithelium, surface inflammation and eye pain result. An artificial tear is used so that it can provide lubrication to the surface of the eye while offering osmoprotection to the epithelial cells of the cornea. In severe dry eyes and unresponsive surface disease, patients have significant visual impairment and disability. the present invention is very advantageous in the case of dry eyes as it has the viscosity enhancing ingredient of medication - glycerine as a medium. Being a.hyperosmotic, glycerine is suitable in the present ophthalmic preparation in more than one way. It is known to reduce TOP by creating osmotic gradient between plasma and ocular fluids; it reduces oedema and clears corneal haze by attracting water through semipermeable corneal epithelium. There are no well documented drug interactions and laboratory test interactions of glycerine. The only adverse reaction in the ophthalmic solution is ocular pain and irritation. If needed, its elimination is done by flushing. Being more viscous the liquid of the present invention stays on the eye for longer time due to a mucous adhesive property. It will dissolve in the tears, retaining the moisture. Its retention time is longer than that of artificial tears. The liquid of the present invention enters the corneal cells to protect against hypertonic stress. Once exposed to the eye surface pH (7.2), the eye drop liquid having greater viscosity and bioadhesive properties is able to retain its two APIs. The ophthalmic preparation can be used over a long period to help protect the cornea with no side effects. The present invention contains antioxidants to help heal the epithelium and prevent oxidative stress or cell damage caused by the inflammatory process. Cataract The present invention (ophthalmic preparation) has been found to help delay, reduce, reverse and slow the occurrence of senile cataract. Thus it may obviate the need for a surgery, and so, be useful for diabetic persons. The causes of cataract are numerous. Free radicals, the natural byproducts of metabolism, are responsible for most cataracts. These are highly reactive chemicals which cause oxidation and aging. The natural defenses in the form of anti-oxidants decline with advancing age. Consequently the lens of the eye hardens and loses its ability to focus. chronic physical stress that reduces eye movement and increases muscle tension, certain food allergies or sensitivities particularly involving dairy products and poor, nutrition in general can effect nutrition to the eyes. Toxins, steroid or photosensitizing drugs such as gout medications, cholesterol lowering drugs, antibiotics and diuretics, alcoholic consumption all lead to formation of cataract. Smokers have an increase in lipids (both fat and cholesterol) which cause narrowing of the retina blood vessels that carry valuable nutrients to the eye. Diabetics develop cataracts earlier where an accumulation of sorbitol and fructose in the lens can induce osmotic swelling of the lens and cataract. The invisible ultraviolet, e.g., in the sunlight promotes free-radical damage to the lens. Alkaloids have been tested to have a good ability to quench the single oxygen radicals which are damaging to all living organisms. The herb component used in the present ophthalmic preparation has as the active principle Punarnavine alkaloid which in the dry state is 0.01%. Potassium Nitrate in the powdered drug amounts to about 6,41%. Presence of potassium salts in the present invention makes the active alkaloid more effective. As an anti-oxidant, it possesses the ability to protect cells from oxidative stress, both in the lipid phase of cellular membranes and in the aqueous environment. The present ophthalmic preparation works to reduce the content of lipid peroxidation products in the peroxidized lens fibre cells plasma membranes, and to repair their structure accordingly. The anti-oxidant property helps protect structural proteins of the lens from the free-radical induced oxidation process. CLINICAL STUDIES RESULTS The following clinical studies made illustrate the efficacy of the various aspects of the usefulness of the present invention to improve cataract, trachoma, epiphoris, corneal opacity, pterygium, trachiasis, conjuntivitis, difficulty in vision. Patients suffering from the following specific problems were given the treatment: Cataract, Trachoma, Corneal Opacity, Trachiasis, Pterygium, Epiphoris - watery discharge. Acute Catarrhal Conjunctivitis. A clinical trial was conducted by a qualified practitioner of traditional medicines. The following tables give summary of a trial to treat 50 patients p'"! aged 50 and above. The patients were instilled 1 or 2 drops into each eye 3 times a day, for a period of 3 to 6 months. The results presented in the Table 2 speak for themselves. Except for 5, all the patients experienced an improvement in visual acuity. The results were noticeable within 1-2 wee)fe of the application of the present ophthalmic preparation. Only 1 patient reported of an adverse result. There were 5 patients with no symptoms of cataract but with difficulty in vision. The present ophthalmic preparation was found to help them in red eyes, ocular inflammation, blurred vision and dry eyes. This shows that the present ophthalmic preparation is useful both for preventative purposes as also medical applications. From the aforesaid investigations, trials and research conducted a conclusion has been arrived that the present process of manufacture of eye drops from herbal root and mineral is practicable and the results conform to the objectives and advantages mentioned herein above and also conform to the standards laid down in the Ayurvedic and Unani Pharmacoepia of India for the purpose of purity, clarity and conformity. WE CLAIM: 1-. A .process of manufacture of an eye drop for treating certain ailments of th-e human eye from naturally occurring substances comprising the steps of (a) grinding to a fine powder of a required quantity of shoraka/shora kalmi (Potassi Nitras), (b) crushing and refining Punarnava/Baskhapra (Boerhaavia diffusa) of an appropriate quantity and, (c) mixing the fine powder of (a) and (b) and (d) dissolving the mixture of the powders of (c) in glycerine with mechanical stirrers at laboratory temperatures for twelve hours and thereafter filtering the entire solution through a fine but neutral medium using expansion of a compressed gas, the pressure filtration technique obtaining a crystal clear solution and store in a sterile vessel. 2. The process as claimed in Claim 1 wherein the required quantity of shoraka/shora kalmi is 25 gm. 3. The process as claimed in Claim 1 wherein Punarnava/Baskhapra required is 100 gm. 4. The process as claimed in Claim 1 wherein the mixture of shoraka/shora kalmi and Punarnava/Baskhapra are in the ratio of 1:4, or alternatively wherein the mixture of shoraka/shora kalmi and Punarnava/Baskhapra are in the ratio of 1:0.8 to prepare an aqueous extract of the herb and reduce it to 1/5 th of the ingredient's quantity 5. The process as claimed in Claim 1 wherein the mixtures are disolved in glycerine which serves as a vehicle for and also acts as a preservative and leave for a period of 12 hours for it to settle down. 6. The process as claimed in Claim 1 wherein the filtration is done according to pressure filtration technique and the media used is glycerine. 13

Full Text

This invention relates to a process of manufacture of an ophthalmic preparation, an eye drop, from naturally occurring substances in an innovative combination for treating pathogenic, allergic and chemical imbalances of the human eye. INTRODUCTION
Medicinal preparations have been classified according to the system of medicines adopted as allopathic. Ayurvedic, Unani, Siddha and Homeopathic etc. In the modern method of treatment by use of eye drops for the ailments of the eyes, there are many allopathic drugs which"* are manufactured and made available in the market. Most of these medicines- allopathic or other suffer from one or the other drawbacks or side effects which may not be apparent immediately and also lead to immunity to the drugs. Furthermore, the manufacture of these drugs requires synthetic raw materials, sophisticated plant and machinery. Whereas in the Indian Systems medicinal manufactury, the equipments are less expensive and less time consuming. In the circumstances, there has been a great interest in natural medicine the world over for safety concerns- namely the occassional adverse reactions and side effects that entail usage of an allopathic formulation.
Traditional systems of medicine in India consist mainly of Ayurveda, Unani and Siddha. The medicines made under these systems use drug material of plant, mineral and animal origin which are well documented in the traditional and scientific literature for their healing properties. These systems are very similar in terms of drug material used which is mostly common among them. Some differences can be there in the process of making a medicine, and, the philosophy of treatment. However, the medicines are acknowledged as safe to use, and so spread over a long period. Medicines under the ISM are today manufactured following Good Manufacturing Practices (GMP) norms laid down by the Government of India.

THE PRESENT INVENTION
The present invention uses active ingredients from nature. A manufacture
of the present invention will need to be within the purview of a medicinal
system of natural products. Using the active ingredients in the present invention
a manufacture of the present invention can be taken up as a proprietary
Indian Systems (Ayurvedic/Unani) medicine.
There is no eye drops mentioned as such in the traditional reference texts on Indian Systems of Medicine. Any such formulation shall have to be made (1) only from the active pharmaceutical ingredients which figure in the approved lists of drugs of plant, animal and mineral origin in the formularies of Ayurvedic and Unani medicines brought out by the Govt, of India (for use for various ailments), (2) as per the guidelines laid down in the Drugs & Cosmetics Act for allopathic eye drops, (3) and has to be sterile and prepared following a modern scientific methodology. Consequently, the methodology for such preparation has to be developed anew which will evolve as the method of preparation of the invention is perfected.
The present invention addresses all the concerns mentioned above. It involves drug material used in the Indian Systems of Medicine in an innovative combination and improves upon them by refining and processing the ingredients with catalysts and use of an effective solvent for treatment of pathogenic, allergic and chemical imbalances of the human eye. The active pharmaceutical ingredients used in the formulation are of natural origin and not synthetic. As single drugs, these are not very useful. The present invention uses herbo-mineral ingredients which are processed so as to have their healing effect well enhanced. The present invention has a herbal component in a form that ensures that its active principle, namely an alkaloid Punarnavine is present. It is processed with a mineral and provided
3

in a known solvent glycerine which further enhances the healing effect of the ingredients. The present invention is preserved with an approved preservative. The end product has been found agreeable to the human eye.
The present invention relates to a complete development of the formulation and process of preparation to eventually produce a sterile, user-friendly formulation which can be used over a long period without causing any allergic, adverse reactions or side effects. The method of treatment is topical application of the formulation.'In essence, the primary* object of the present invention is:
1. To provide in particular a process for manufacture of an eye drop from herbo- mineral substances containing an alkaloid as an active principle dissolved in glycerine and an approved preservative;
2. To provide a particular formulation for the treatment of specific eye conditions- pathogenic, allergic and chemical disequilibrium conditions; the treatment is by topical application of the formulation;
3. To provide an ophthalmic preparation which is new, effective and economical.
THE INVENTION AND THE PROCESS OF INVENTION
According to the present invention a formulation is prepared in a known solvent from active ingredients which have therapeutic properties to which a particular condition being treated is responsive.
1. Form of the invention: eye drops
It is a proprietary medicine which is within the Indian Systems {Ayurvedic & Unani) of Medicine.
2. Formula:
I. ACTIVE INGREDIENTS
Sanskrit/Urdu name Botanical/Latin name Quantity
taken
1. Punarnava/ Boerhavia diffusa 100 gm Biskhapra
2. Shoraka/ Potassi Nitras 25 gm shora kalmi
II. SOLVENT
Glycerine 1000 gm

* It is to be emphasized that the process makes the alkaloid Punarnavine act with Potassi Nitras in I above and the solvent mentioned in II above and makes it have greater arid marked effect on the opacities in the lens and cornea, as also their use in this combined form. Method of preparation:
The examples of the preparation and the process of manufacture of the present invention provided herein illustrate the scope of the invention and not intended to be limiting. Other applications of aspects of the present invention within the broad scope will be apparent to those skilled in the art.
According to the present invention there is provided a process of manufacture of an eye drop for treating certain ailments of the human eye from naturally occurring substances comprising the steps of
(a) grinding to a fine powder of a required quantity of shoraka/shora kalmi (Potassi Nitras)
(b) crushing and refining punarnava/baskhapra (Boerhaavia diffusa) of an appropriate quantity and,
(c) mixing the fine powder of (a) and (b) and
(d) dissolving the mixture of the powders of (c) in glycerine with mechanical stirrers
(e) at laboratory temperatures for twelve hours and thereafter
(f) filtering the entire solution through a fine but neutral medium using pressure filtration technique
(g) obtaining a crystal clear solution and store in a sterile vessel;
(h) thereafter to fill up the solution in bottles and vials as
injectables for dispensation in retail containers. The following examples illustrate the preparation of the eye drop of the present invention. Example I:
Take the second ingredient in proportionate measures and grind well to a fine powder. Crush the first ingredient taken in appropriate quantity and properly mix it with shora kalmi dissolved into glycerine with a mechanical stirrer at

180 degree temperature, and allow it to settle down for a time upto 12 hours. Filter the entire solution using the expansion of a compressed gas, to be termed hereafter the pressure filtration technique, through a very fine but neutral medium to obtain a crystal clear solution and store in a sterile vessel. An automatic vial filling is then done in a very clean and secluded area which is airconditioned and fumigated. The purpose of glycerine is to serve as a vehicle for the ingredients. It too has a pharmacological action and acts as a preservative. Example II:
It is to be noted that not all the chemical compounds in a plant are of equal interest in the present context. The active principles are alkaloids or glycosides. Other groups such as carbohydrates, fats and proteins are of dietic importance and many others such as starches and gums, though used in pharmacy, lack any marked pharmacological action. This method makes sure that the alkaloid Punarnavine is present in the eye drop of the invention. This is made possible by the use of aqueous extract of the herb. The used extract is taken 1/5 of the ingredient's normal quantity as mentioned above in the formula. This proportion relates to the richness of the alkaloid Punarnavine present in the drug and keeps the water content in the eye drop of the invention to minimum.
As in the Example I, the-aqueous extract taken in appropriate quantity is properly mixed with shora kalmi dissolved into glycerine with a mechanical stirrer at 180 degree temperature, and allow the end product to settle down for a time upto 12 hours. Filter the entire solution using the pressure filtration technique through a very fine but neutral medium to obtain a crystal clear solution and store in a sterile vessel. An automatic vial filling is then done in a very clean and secluded area which is airconditioned and fumigated. The purpose of glycerine is to serve as a vehicle for the ingredients. It has its own pharmacological action and acts as a preservative. For the sake of batch consistency, any one of the options about the first

ingredient as distinguished in the Example I and Example II can be used. Preservative used in Example I and Example II is Phenyl Mercuric Nitrate. PHARMACOLOGICAL ACTION OF THE DRUGS USED IN THE INVENTION

Name of the ingredients

Properties

Pharmacological action

Side Effects and adverse reaction

1. Biskhapra controls oedema. Enhances corneal
improves sight. clarity; in immature
cataract, it resolves the already coagulated ** protein fibres of the
lens and prevents further coagulation or delays it. It has a cooling effect on eyes afflicted with conjunctivitis. Presence of potassium salts in this make the active alkaloid more effective.

No side effects or adverse reaction

2. Shora Kalmi cooling,
antimicrobial,

It cools the eyes and works on infections. Its presence in the solution strenthens the action of the active alkaloid in biskhapra.

No side effects or adverse reaction

3. Glycerine A vehicle for
It has a softening effect. No side effects the above drugs; draws out watery fluids, or adverse emollient, retains drugs more reaction hygroscopic, effectively, antimicrobial.
NOTE: The ingredients and the solvent have been so processed and assimilated
that together they synergize to absorb the lens-, corneal and vitreous opacities,
Also being moderately hypertonic, the invention reduces fluid collected in the
cornea (corneal oedema) through an osmotic action that enhances its clarity.
The overall effect is to prevent the formation of cataract or, at the worst,
delay the progress of cataract. The present invention has been tested to have
a pH value in the range 4.0 -7.0. This is well within the acceptable range of
pH values of 3.5 - 10.5 for an eye drop in the allopathic system.
The present invention can be stored at room temperature.
7

THERAPEUTIC INDICATIONS
The present invention has been found effective in various ailments of the eyes, such as .opacities of the lens, corneal and vitreous opacities, conjunctivitis, watery discharge and headaches resulting from eye ailments. Users have found it useful in dry eyes condition. Clinical tests have shown its effect on the blurred and diminished vision caused by cataract in various stages. It has been found safe to use; its ingredients have antimicrobial property.
SPECIFIC EYE AILMENTS ADDRESSED
Some specific eye ailments where the present invention has been indicated
are described morefully below.
Usage in operated eye
The present invention has been tried on persons who have an Intra Occular
Lens implant after a surgery. This has shown a progressive improvement in the eye
condition. As a precaution, in such patients, the use of the present invention
{the eye drops) should be recommended only after 6 months or more from the date
of operation when the eye is in a state of good health and thereafter continue
with the medicine if there is no marked improvement after the surgery.
Otherwise, wash the eyes with clean water and stop the usage of the medicine.
Dry eyes
Human tears are composed of water, electrolytes, carbohydrates, lipids and
proteins with many having an enzymic function. The dry eye condition results
due to insufficient tear production, excessive tear evaporation or abnormal
tear composition. Symptoms of dry eye include itching, irritation,
sensitivity to light, blurred vision and contact lens intolerance. As there
is not enough support by tears to the ocular epithelium, surface inflammation
and eye pain result. An artificial tear is used so that it can provide
lubrication to the surface of the eye while offering osmoprotection to the
epithelial cells of the cornea. In severe dry eyes and unresponsive surface
disease, patients have significant visual impairment and disability.

the present invention is very advantageous in the case of dry eyes as it has
the viscosity enhancing ingredient of medication - glycerine as a medium.
Being a.hyperosmotic, glycerine is suitable in the present ophthalmic
preparation in more than one way. It is known to reduce TOP by creating
osmotic gradient between plasma and ocular fluids; it reduces oedema and
clears corneal haze by attracting water through semipermeable corneal
epithelium. There are no well documented drug interactions and laboratory
test interactions of glycerine. The only adverse reaction in the ophthalmic
solution is ocular pain and irritation. If needed, its elimination is done
by flushing.
Being more viscous the liquid of the present invention stays on the eye for
longer time due to a mucous adhesive property. It will dissolve in the tears,
retaining the moisture. Its retention time is longer than that of artificial
tears. The liquid of the present invention enters the corneal cells to protect
against hypertonic stress. Once exposed to the eye surface pH (7.2), the
eye drop liquid having greater viscosity and bioadhesive properties is able
to retain its two APIs. The ophthalmic preparation can be used over a long
period to help protect the cornea with no side effects.
The present invention contains antioxidants to help heal the epithelium
and prevent oxidative stress or cell damage caused by the inflammatory
process.
Cataract
The present invention (ophthalmic preparation) has been found to help delay,
reduce, reverse and slow the occurrence of senile cataract. Thus it may obviate
the need for a surgery, and so, be useful for diabetic persons.
The causes of cataract are numerous.
Free radicals, the natural byproducts of metabolism, are responsible for most
cataracts. These are highly reactive chemicals which cause oxidation and
aging. The natural defenses in the form of anti-oxidants decline with advancing
age. Consequently the lens of the eye hardens and loses its ability to focus.

chronic physical stress that reduces eye movement and increases muscle tension, certain food allergies or sensitivities particularly involving dairy products and poor, nutrition in general can effect nutrition to the eyes. Toxins, steroid or photosensitizing drugs such as gout medications, cholesterol lowering drugs, antibiotics and diuretics, alcoholic consumption all lead to formation of cataract. Smokers have an increase in lipids (both fat and cholesterol) which cause narrowing of the retina blood vessels that carry valuable nutrients to the eye. Diabetics develop cataracts earlier where an accumulation of sorbitol and fructose in the lens can induce osmotic swelling of the lens and cataract. The invisible ultraviolet, e.g., in the sunlight promotes free-radical damage to the lens.
Alkaloids have been tested to have a good ability to quench the single oxygen radicals which are damaging to all living organisms. The herb component used in the present ophthalmic preparation has as the active principle Punarnavine alkaloid which in the dry state is 0.01%. Potassium Nitrate in the powdered drug amounts to about 6,41%. Presence of potassium salts in the present invention makes the active alkaloid more effective. As an anti-oxidant, it possesses the ability to protect cells from oxidative stress, both in the lipid phase of cellular membranes and in the aqueous environment. The present ophthalmic preparation works to reduce the content of lipid peroxidation products in the peroxidized lens fibre cells plasma membranes, and to repair their structure accordingly. The anti-oxidant property helps protect structural proteins of the lens from the free-radical induced oxidation process.
CLINICAL STUDIES RESULTS
The following clinical studies made illustrate the efficacy of the various aspects of the usefulness of the present invention to improve cataract, trachoma, epiphoris, corneal opacity, pterygium, trachiasis, conjuntivitis, difficulty in vision. Patients suffering from the following specific problems were given the treatment:

Cataract, Trachoma, Corneal Opacity, Trachiasis, Pterygium, Epiphoris - watery
discharge. Acute Catarrhal Conjunctivitis.
A clinical trial was conducted by a qualified practitioner of traditional
medicines. The following tables give summary of a trial to treat 50 patients p'"!
aged 50 and above. The patients were instilled 1 or 2 drops into each eye 3
times a day, for a period of 3 to 6 months. The results presented in the Table 2
speak for themselves. Except for 5, all the patients experienced an improvement
in visual acuity. The results were noticeable within 1-2 wee)fe of the
application of the present ophthalmic preparation. Only 1 patient reported
of an adverse result.
There were 5 patients with no symptoms of cataract but with difficulty in vision.
The present ophthalmic preparation was found to help them in red eyes, ocular
inflammation, blurred vision and dry eyes. This shows that the present ophthalmic
preparation is useful both for preventative purposes as also medical applications.

From the aforesaid investigations, trials and research conducted a conclusion has been arrived that the present process of manufacture of eye drops from herbal root and mineral is practicable and the results conform to the objectives and advantages mentioned herein above and also conform to the standards laid down in the Ayurvedic and Unani Pharmacoepia of India for the purpose of purity, clarity and conformity.

WE CLAIM:
1-. A .process of manufacture of an eye drop for treating certain ailments
of th-e human eye from naturally occurring substances comprising the steps of
(a) grinding to a fine powder of a required quantity of shoraka/shora kalmi
(Potassi Nitras),
(b) crushing and refining Punarnava/Baskhapra (Boerhaavia diffusa) of an appropriate quantity and,
(c) mixing the fine powder of (a) and (b) and
(d) dissolving the mixture of the powders of (c) in glycerine with mechanical stirrers
at laboratory temperatures for twelve hours and thereafter filtering the entire solution through a fine but neutral medium using expansion of a compressed gas, the pressure filtration technique obtaining a crystal clear solution and store in a sterile vessel.
2. The process as claimed in Claim 1 wherein the required quantity of shoraka/shora kalmi is 25 gm.
3. The process as claimed in Claim 1 wherein Punarnava/Baskhapra required is 100 gm.
4. The process as claimed in Claim 1 wherein the mixture of shoraka/shora kalmi and Punarnava/Baskhapra are in the ratio of 1:4, or alternatively wherein the mixture of shoraka/shora kalmi and Punarnava/Baskhapra are in the ratio of 1:0.8 to prepare an aqueous extract of the herb and reduce it to 1/5 th of the ingredient's quantity
5. The process as claimed in Claim 1 wherein the mixtures are disolved
in glycerine which serves as a vehicle for and also acts as a preservative and leave for a period of 12 hours for it to settle down.
6. The process as claimed in Claim 1 wherein the filtration is done
according to pressure filtration technique and the media used is glycerine.
13

Documents:

0952-che-2005 abstract.pdf

0952-che-2005 claims.pdf

0952-che-2005 correspondence-others.pdf

0952-che-2005 correspondence-po.pdf

0952-che-2005 description (complete).pdf

0952-che-2005 form-1.pdf

0952-che-2005 form-18.pdf

0952-che-2005 form-62.pdf

0952-che-2005 form-9.pdf

« Previous Patent

Next Patent »

Patent Number

228602

Indian Patent Application Number

952/CHE/2005

PG Journal Number

12/2009

Publication Date

20-Mar-2009

Grant Date

05-Feb-2009

Date of Filing

18-Jul-2005

Name of Patentee

RAMESH CHANDER KAPOOR

Applicant Address

31, 4B BLOCK, KORAMANGALA, BANGALORE 560 034,

Inventors:

#	Inventor's Name	Inventor's Address
1	UMA KAPOOR	31, 4B BLOCK, KORAMANGALA, BANGALORE 560 034,
2	RAMESH CHANDER KAPOOR	31, 4B BLOCK, KORAMANGALA, BANGALORE 560 034,

PCT International Classification Number

A61K 35/00

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA