WO2006003383A1

WO2006003383A1 - Ophthalmic eye preparation

Info

Publication number: WO2006003383A1
Application number: PCT/GB2005/002537
Authority: WO
Inventors: Pravin G. Patel
Original assignee: ACCUMED Ltd
Current assignee: ACCUMED Ltd
Priority date: 2004-07-01
Filing date: 2005-06-29
Publication date: 2006-01-12
Anticipated expiration: 2007-01-01
Also published as: GB0414772D0; GB2415902A

Abstract

This invention relates to an ophthalmic eye preparation comprising herbal extracts or their synthetic equivalents and a method for its production. The preparation comprises ocimum sanctum (5-20%), curcuma longa (5-18%), carum copticum (0.5-5%), terminala belerica (2-7.5%), embilica officinalis (3-10%), terminala chebula (2-7.5%), camphora officinarum (1-5%), mentha sylvestries (0.5-5%), Eletteria Cardamomum (2-7.5%), santalum album (2-7.5%), santalum rubrum (2-7.5%), azadirachta indica (2-7.5%), vitex negundo (2-7.5%), moringa pterygosperma (2-7.5%), eclipta alba (2-7.5%), boerhaavia diffusa (5-10 %) and rosa damascena (5 -10 %) , the preferred amounts of the herbal extracts in percentage by volume being given in brackets.

Description

OPHTHALMIC EYE PREPARATION

This invention relates to^' ophthalmic eye preparations comprising herbal extracts or their synthetic equivalents.

Ophthalmic eye preparations are well known in the art and are generally formulated using pharmaceutical chemicals and drugs for the treatment of eye diseases. In recent years there has been an increasing demand for alternative medical treatment of such eye diseases using herbal formulations. In addition, the extensive use of contact lenses and refractive surgery has created a demand for eye drops that are safer to use in the long term.

The use of synthesised chemicals and drugs as eye drops tends to result in increased side effects and can also cause immunity towards these drugs. The present invention seeks to solve these problems by providing herbal formulations that can be used daily without any significant side effects or adverse interactions with existing medication.

An example of previously known herbal ophthalmic eye preparations is the product "Ophthacare" , eye drops sold by the Himalaya Drug Company of India. According to Himalaya's product literature Ophthacare possesses antimicrobial, anti-inflammatory and analgesic qualities and is effective in the management of infective and inflammatory eye disorders. It also claims to relieve congestion and asserts to be beneficial in eyestrain. The ingredients of Ophthacare are stated to be extracts of Carum copticum (6.00%), Terminalia belerica (6.50%) , Emblica officinalis (13.00%), Curcuma longa (13.00%), Ocimum Sanctum (13.00%), Rosa Datnascena (11.00%), Cinnamomum camphora (0.50%) and Meldespumatum (37.-00%)

The ophthalmic eye preparations of the present invention improve on the prior art by comprising a novel combination of the extracts from 17 herbs, or the synthetic equivalents of the extracts, in therapeutically effective amounts. The preparations result in unexpectedly improved treatment of various eye diseases dry eye syndrome and the wetting and lubricating of eyes. The preparations are suitable for use with or without contact lenses. In the process for the production of the preparations using the herbs themselves, the herbs are picked, washed and weighed for processing. The weighed herbs are then enclosed in a high-pressure vessel, through which steam is passed, thereby extracting the herbal oils. The steam extraction procedure produces the oils in the form of concentrated oil/water mixtures. The extract is then checked for its composition and sterility.

The herbs used in the preparations, their preferred levels as a percentage by volume and their activity are given below:

Ocimum sanctum (Tulsi) - anti-inflammatory and anti¬ microbial, 5-20%

Curcuma longa (Haridra) - anti-inflammatory (comparable to hydrocortisone acetate and phenylbutazone) and anti¬ microbial (comparable to penicillin and streptomycin on gram +ve and gram -ve bacteria) , 5-18% Carum copticum (Yamani) - anti -bacterial (against

Salmonella typhi , Micrococcus pyogenes and Escherichia coli) , 0 . 5-5%

Terminalia belerica (Vibhitaka) - anti-bacterial (against Micrococcus pyogenes and E. coli) , 2-7.5%

Embilica officinalis (Dhatriphala) - anti-inflammatory and cooling effect, 3-10%

Terminalia chebula (Haritaki) - astringent and anti¬ inflammatory, 2-7.5% Camphora officinarum (Kapoor) - anti-bacterial (against several gram +ve and gram -ve bacteria) , 1-5%

Mentha sylvestries (Pudina) - antiseptic and analgesic,

0.5-5%

Eletteria Cardamomum (EIa) - anti-irritant, 2-7.5% Santalum album (Swet Chandan) - soothing, 2-7.5%

Santalum rubrum (Rakta Chandan) - soothing, 2-7.5%

Azadirachta indica (Nimba) - antiseptic and anodyne, 2-

7.5%

Vitex negundo (Nirgundi) - antiseptic and anodyne, 2-7.5% Moringa pterygosperma (Sobhajana) - analgesic, 2-7.5%

Eclipta alba (Bhringaraj) - anodyne and antiseptic, 2-

7.5%

Boerhaavia diffusa (Punarnava) - anti-inflammatory, 5-10%

Rosa damascena (Satapatri) - astringent and cooling, 5- 10%

The formulations also include a sequestering or chelating agent, which is preferably present at approximately 0.01- 2% by volume. The preferred sequestering agents are ethylenediaminetetraacetic acid (EDTA) and its salts, with the disodium salt, disodium edetate, being especially preferred. The preparations may also include buffering agents and tonicity adjusting agents. The buffering agents can be used to buffer or adjust the pH of the solution. Examples of suitable buffering agents include alkali metal salts such as potassium or sodium carbonates, acetates, borates, phosphates, citrates and hydroxides or weak acids such as acetic, boric and phosphoric acids. Preferably, buffering agents are present at approximately 0.01-2.5% by volume. Examples of tonicity adjusting agents include sodium and potassium chloride, and those materials listed as buffering agents. Tonicity agents may be employed in an amount effective to adjust the osmotic value of the final solution to approximate that of human tears, generally at about 0.01-2.5%.

Additionally, the preparations may include wetting agents or viscosity modifiers. Examples of suitable wetting agents and viscosity modifiers include sodium hyluronate; cellulose derivatives such as cationic cellulosic polymers, hydroxypropyl methylcellulose, hydroxyethylcellulose and methylcellulose; and polyols such as polyethylene glycol, glycerine, polyethylene oxide containing polymers, polyvinyl alcohol and polyvinyl pyrrolidone. Such additives are preferably present at approximately 0.01-1.5% by volume.

Preservatives may also be added to the formulation. Examples of suitable preservatives include polyhexamethylene biguanide, sorbic acid, benzalkonium chloride and phenyl mercuric nitrate.

The remainder of the composition is water.

Claims

CLAIMS :

1. An ophthalmic eye preparation comprising a mixture of herbal extracts from ocimum sanctum, curcuma longa, carum copticum, terminalia belerica, embilica officinalis, terminalia chebula, camphora officinarum, mentha sylvestries, Eletteria Cardamomum, santalum album, santalum rubrum, azadirachta indica, vitex negundo, moringa pterygosperma, eclipta alba, boerhaavia diffusa and from rosa damascena, or of one or more synthetic equivalent of such extracts.

2. A preparation as claimed in claim 1, wherein each of the herbal extracts have been obtained by a process comprising the steps of

-picking a herb recited in claim 1, optionally washing and weighing it,

-placing the herb in a high pressure vessel and passing steam through the vessel, -extracting oil from the herb in the form of a concentrated oil/water mixture, and

-optionally checking the extract for its composition and sterility.

3. A preparation as claimed in either claim 1 or claim 2, wherein the mixture comprises the following herbal extracts:

5-20% by volume ocimum sanctum

5-18% by volume curcuma longa 0.5-5% by volume carum copticum

2-7.5% by volume terminalia belerica

3-10% by volume embilica officinalis

2-7.5% by volume terminalia chebula

1-5% by volume camphora officinarum 0.5-5% by volume mentha sylvestries 2-7.5% by volume eletteria cardamoraum 2-7.5% by volume santalum album 2-7.5% by volume santalum rub>rum 5 2-7.5% by volume azadirachta indica

2-7.5% by volume vitex negun&o 2-7.5% by volume moringa pter-ygosperma 2-7.5% by_.volume eclipta alba 5-10% by volume boerhaavia diffusa ]_0 5-10% by volume rosa damascena.

4. A preparation as claimed in any one of the preceding claims, wherein the preparation includes a sequestering agent or chelating agent.

15

5. A preparation as claimed in claim 4, wherein the sequestering agent or chelating agent is EDTA or one of its salts.

20 6. A preparation as claimed in claim 5, wherein the EDTA is in the form of its disodium salt.

7. A preparation as claimed in any one of the preceding claims, wherein the preparation includes a buffering

25 agent.

8. A preparation as claimed in claim 7, wherein the buffering agent is an alkali metal salt.

30 9. A preparation as claimed in claim 8, wherein the alkali metal salt is potassium or sodium carbonate, potassium or sodium acetate, potassium or sodium borate, potassium or sodium phosphate, potassium or sodium citrate, or potassium or sodium hydroxide.

10. A preparation as claimed in claim 7, wherein the buffering agent is a weak acid.

11. A preparation as claimed in claim 10, wherein the weak acid is either acetic acid, boric acid or phosphoric acid.

12. A preparation as claimed in any one of claims 7 to 11, wherein the buffering agent is present in an amount of 0.01% to 2.5% by volume.

13. A preparation as claimed in any one of the preceding claims, wherein the preparation includes a tonicity agent.

14. A preparation as claimed in claim 13, wherein the tonicity agent is an alkali metal salt.

15. A preparation as claimed in claim 14, wherein the alkali metal salt is potassium or sodium chloride, potassium or sodium carbonate, potassium or sodium acetate, potassium or sodium borate, potassium or sodium phosphate, potassium or sodium citrate, or potassium or sodium hydroxide.

16. A preparation as claimed in any one of claims 13 to

15. wherein the tonicity agent is present in an amount of 0.01% to 2.5% by volume.

17. A preparation as claimed in any one of the preceding claims, wherein the preparation includes a wetting agent or viscosity modifier.

18. A preparation as claimed in claim 17, wherein the wetting agent or viscosity modifier is a cellulose derivative, a polyol or sodium hyluronate.

19. A preparation as claimed in claim 18, wherein the cellulose derivative is a cationic cellulosic polymer, hydroxypropyl methylcellulose, hydroxyethylcellulose or methylcellulose.

20. A preparation as claimed in claim 18, wherein the polyol is polyethylene glycol, glycerine, a polyethylene oxide containing polymer, polyvinyl alcohol or polyvinyl pyrrolidone.

21. A preparation as claimed in any one of claims 17 to 20, wherein the wetting agent or viscosity modifier is present in an amount of 0.01% to 1.5% by volume.

22. A preparation as claimed in any one of the preceding claims, wherein the preparation includes a preservative.

23. A preparation as claimed in claim 22, wherein the preservative is polyhexamethylene biguanide, sorbic acid, benzalkonium chloride and phenyl mercuric nitrate.

24. A preparation as claimed in any one of the preceding claims, wherein any remainder of the composition is added water.

25. A process for the production of an ophthalmic eye preparation comprising the steps of:

-picking the herbs ocimum sanctum, curcuma longa, carum copticum, terminalia belerica, embilica officinalis, terminalia chebula, camphora officinarum, rαentha sylvestries, Eletteria Cardamoraum, santalum album, santalum rubrum, azadirachta indica, vitex negundo, moringa pterygosperma, eclipta alba, boerhaavia diffusa and rosa damascena, optionally washing and weighing them,

-placing the herbs in a high pressure vessel and passing steam through the vessel,

-extracting the herbal oils in the form of concentrated oil/water mixtures,

-optionally checking the extract for its composition and sterility, and

-formulating the preparation according to the desired composition.