NZ504526A

NZ504526A - Treating herpes simplex symptoms using a mixture of cetyl myristate and cetyl palmitate

Info

Publication number: NZ504526A
Application number: NZ504526A
Authority: NZ
Inventors: Timothy David Meakin; Craig Leonard Heatley; Dianne Cadwallader
Original assignee: Meracol Corp Ltd
Priority date: 2000-05-12
Filing date: 2000-05-12
Publication date: 2003-05-30
Also published as: AU2001260834A1; WO2001085164A1

Abstract

The treatment of humans or other mammals for the prophylaxis of at least the symptoms of herpes simplex or related herpes skin ailments using dosage forms or compositions that include cetyl myristate alone or (in admixture or serially) both cetyl myristate and cetyl palmitate is disclosed.

Description

New Zealand Paient Spedficaiion for Paient Number 504526 No: 504526 Date: 12 May 2000 NEW ZEALAND PATENTS ACT, 1953 Intellectual Property Office of N.2. 1 1 MAY 2001 received COMPLETE SPECIFICATION The Treatment of Herpes We, MERACOL CORPORATION LIMITED, a company duly incorporated under the laws of New Zealand of 19A O'Neills Avenue, Takapuna, Auckland, New Zealand, do hereby declare the invention for which we pray that a patent may be granted to us, and the method by which it is to be performed, to be particularly described in and by the following statement: TECHNICAL FIELD The present invention relates to a method of treatment and/or prophylaxis of at least the symptoms of herpes simplex or related herpes skin ailments.

BACKGROUND Common symptoms of herpes simplex infection can are be recognized by the appearance of small, grouped vesicles showing up under the skin as red spots which then become pustules, which ruptures and breaks the skins surface. This then forms a crust on the outside of the skin. The rupturing can cause deep lesions.

The present invention has surprisingly determined that the administration (particularly by ingestion) of cetyl myristate, and particularly cetyl myristate in conjunction with cetyl palmitate, provides an effective treatment of at least the symptoms of herpes simplex and related herpes skin ailments.

Cetyl myristate and cetyl palmitate can each be sourced from animals or vegetables. Cetyl myristate is not to be mistaken for cetyl myristoleate which is also a fatty acid derived traditionally from spermaceti by saponification and more recently from the tallow of bovine(s).

Reference is made to US Patent No.4,113,881 where it is disclosed that the administration of an effective amount of cetyl myristoleate to a mammal is useful in inhibiting or relieving the symptoms of inflammatory rheumatoid arthritis in mammals. Also in US 5,569,676 there is disclosure of the use of cetyl myristoleate in the treatment of osteo-arthritis.

It is thought that cetyl myristate has a negligible anti-arthritic activity in laboratory experiments and reference is made to the website www.gcinutrients.com/Newletter.com. However this point is arguable and a product known as cetyl myristate sold by Amerex Corporation of 770 Sycamore Avenue, Suite J148, Vista, CA 92083, USA purports that cetyl myristate is useful for the treatment of arthritis.

Cetyl myristate is derived from the saturated fatty acid, myristic acid. This acid is found in nutmeg butter, in the fats of Myristicaceae, in palm seed fats, milk fats and also sperm whale oil. Reference is made to US 2,481,365 which discloses the preparation of myristic acid from tall-oil fatty acids. It is to be noted that Amerex Corporation source the cetyl myristate used in their products from sunflower oil. See their website at www.hollinet.com.

Cetyl palmitate is derived from the fatty acid, palmitic acid which occurs as the glycerol ester in many oils and fats such as palm oil or Chinese vegetable tallow. A synthetic method of preparation is to react palmitoyl chloride and cetyl alcohol in the presence of magnesium. See the Merck Index, 12th edition at page 336. Reference is also made to US patent 3,169,099 which discloses a biosynthetic method of producing cetyl palmitate.

It is an objection of the present invention to provide a medicament to aid in the treatment of herpes and at least herpes simplex which will provide an alternative to existing treatments or to provide the public with a useful choice.

DISCLOSURE OF INVENTION As indicated earlier the present invention is directed to the treatment and/or prophylaxis of at least the symptoms of herpes reliant upon administration (whether by self administration or otherwise) of either cetyl myristate or cetyl myristate and cetyl palmitate (whether given simultaneously in admixture or not or given serially).

The present invention also encompasses the prospect of dosage forms that in some instances might contain cetyl myristate alone and in other instances both cetyl myristate and cetyl palmitate and dosage regimes that might use one dosage form or both.

In another aspect the invention is a method of treatment and/or prophylaxis of a mammal for at least the symptoms of herpes simplex which comprises or includes administering or having self administered to such mammal an effective amount of either (a) cetyl myristate, or (b) cetyl myristate and cetyl palmitate.

Preferably said administration is orally of (b) whether as a mixture of both cetyl myristate and cetyl palmitate, or serially.

Preferably the effective amount is of (b).

Preferably said administration is with a mixture of cetyl myristate in conjunction with cetyl palmitate where the cetyl myristate comprises from 50 to 98% w/w of the mixture.

Preferably said effective amount of (a) or (b) is by means of one or more capsules.

The method also extends to related conditions, eg; accelerated wound healing where a composition as disclosed in US Patent 4,775,291 can at least sometimes be supplemented by use of the present invention methodology.

In another aspect the invention is an oral pharmaceutical composition for treating herpes which comprises or includes both cetyl myristate and cetyl palmitate.

In still another aspect the invention is an oral pharmaceutical composition for treating herpes simplex which comprises or includes both cetyl myristate and cetyl palmitate.

Preferably said cetyl myristate comprises at least 50% by weight of the composition.

Preferably said composition also includes at least one pharmaceutically acceptable excipient and/or diluent.

In still another aspect the invention is an oral dosage unit effective in the treatment of herpes simplex, said dosage unit having either (a) cetyl myristate, or (b) a mixture of cetyl myristate and cetyl palmitate.

Preferably said dosage unit has (b) and said cetyl myristate in any such mixture comprises from 50 to 98% w/w of the mixture.

In another variant the dosage unit has (a) only and there is between 5 to 400 mg of cetyl myristate.

Preferably in the dosage use, where (b) is present, there is from 5 to 400 mg of the mixture of cetyl myristate and cetyl palmitate.

Preferably (a) or (b) is in a capsule.

Preferably said capsule also includes a pharmaceutically acceptable excipient and/or diluent.

Preferably the dosage unit includes silicon dioxide.

Preferably the dosage unit also contains calcium phosphate and/or magnesium oxide.

Preferably the dosage unit also includes additionally at one trace element.

In another aspect the invention is a liquid dosage unit being also an oral dosage unit as aforesaid.

In another aspect the invention is the use, in the manufacture of oral dosage units for the treatment or prophylaxis of at least the symptoms of herpes simplex or related herpes skin ailments in a mammal, of (a) cetyl myristate, or (b) a mixture of cetyl myristate and cetyl palmitate, or (c) cetyl palmitate.

In another aspect the invention is the use, in the manufacture of oral dosage units for the treatment or prophylaxis of at least the symptoms of herpes simplex or related herpes skin ailments in a mammal, of (i) cetyl myristate and (ii) cetyl palmitate.

The mixture can use cetyl myristate available from a commercial source such as EHP Products Inc., PO Box 20727, Mt Pleasant, SC 29465 or at Amerex Corporation, 770 Sycamore Avenue Suite J148 Vista, California 92083.

The mixture can use cetyl palmitate derived from a source such as, for example, Quimica Croda, S.A. de C.V, Circuito Medicos No.47. Apdo. Postal 71-A Cd. Satelite, 53100 Naucalpan, Edo. de Mexico, Mexico or online at www.butterburandsage.com.

Most ideally however the mixture is synthetised from starting materials utilising the procedures as disclosed in New Zealand Patent Specification No. 332959 which involves reacting both myristic acid and palmitic acid with a cetyl alcohol at an elevated temperature in the presence of at least one acid catalyst and at least one aromatic hydrocarbon. The aromatic hydrocarbon fraction then contains the cetyl myristate and cetyl palmitate from whence it can be crystallised.

The full content of NZ 332959 is here incorporated by way of reference.

This crystallised form can then be ground up, dissolved and mixed with a suitable general pharmacy liquid to be administered to a person. The crystals are usually dissolved in hot water before adding to the pharmacy liquid which is usually a sugar syrup available from most pharmaceutical companies. The liquid is made up to a concentration of 70 w/v.

Alternatively the crystals may be ground up into a powder and combined with magnesium oxide, silicon oxide and fine di-calcium phosphate. This powder can then be transferred into capsules for oral ingestion into the body. The capsules used are VEGICAP™ that are non-gelatin containing.

The mode of administration is preferably oral. The dosage unit can be either a swallowable capsule or some alternative (preferably having the active ingredient(s) as a waxlike solid or can be an orally consumable liquid composition (eg; made up with a general pharmacy type carrier such as methyl cellulose)).

Other modes of administration can include transdermal, sublingual, parenteral, and suppository delivery.

The oral administration for the treatment of herpes can be in addition to any other medicament administered for such ailment whether administered orally, topically, parenterally, sublingually, etc.

In practice the present invention will involve ideally oral self administration of effective quantities of cetyl myristate alone or more preferably as a mixture of both cetyl myristate and cetyl palmitate.

Preferably in any such mixture the cetyl myristate comprises at least about half of the mixture or the serial application on a weight to weight basis. It is envisaged that daily doses will vary depending on patient needs and may range from 1 to 20 capsules per day. A capsule ideally contains between 5 to 370 mg of the mixture or cetyl myristate.

Trials with a variety of patients reliant upon dosage forms of cetyl myristate alone have shown favourable responses insofar as relief from the symptoms of herpes simplex is concerned. It has been found however that enhanced benefits occur where there is at least a small proportion of cetyl palmitate in addition to the cetyl myristate and it is to the use of one such ratio of these active ingredients that the following trial examples relate.

Examples of use follows. Each briefly describes the patient's condition before and after the stated treatment using dosage forms (ie; "of the invention") each having about 350 mg of the mixture of cetyl myristate and cetyl palmitate. That mixture comprises by weight 95% cetyl myristate and 5% cetyl palmitate by weight manufactured by the process as disclosed in

Claims

-6- NZ Patent Specification No. 332959. In addition added excipients were present in the non gelatin two part capsule case. Trial Examples: • Patient 1 is female and is 42 years of age. Patient 1 suffers an acute flair of herpes simplex on her upper lip which results in deep lesions developing on her lip which is triggered by cold wind or sun exposure to her lips. In the past, this patient had used ZOVIRAX™ ointment. At the first appointment Patient 1 was provided with capsules of a dosage unit as described in this invention for a dosage regime of 4 capsules, 3 times daily. After two days Patient 1 noted that the lesion did not develop further and the tissue that did become affected was only superficial. The lesion then disappeared in about three days after taking the treatment. • Patient 2 is female and is 39 years of age. Patient 2 suffers acute herpes simplex virus on her lips. Again, this is triggered by cold wind or sun exposure to her lips. Again like patient 1, this patient has used ZOVIRAX™ ointment. At the first appointment Patient 2 was provided with capsules of a dosage unit as described in this invention for a dosage regime of 4 capsules, 3 times daily. After one day the lesion did not develop any further and was also superficial as far as the lesion was concerned. • Patient 3 is male and is 43 years of age. Patient 3 has suffered from Herpes simplex virus for 20 years. The virus attacks when the patient is run down and this is usually every 2-3 months. The symptoms begin with a common, itchy pain on the lip with the development of a lesion that can last up to 10-12 days. His treatment has included taking lysine amino acid as a dietary supplement. At the first appointment Patient 3 was provided with capsules of a dosage unit as described in this invention for a dosage regime of 6 capsules, 3 times daily. This dosage begins when he sees the first symptoms of a herpes "pimple" and he continues with this dosage until the acute signs have disappeared. After taking this dosage at a sufficiently early stage, the lesion in most cases had not" developed. However, if it is taken at a later stage, such a large dose appears to interrupt the development of the lesion so that it is less extensive. Further the lesion caused disappeared after 4 days rather than the usual 10-12 days. -7- CLAIMS: 0 3 MAR 2Q03 RECEIVED

I. An oral pharmaceutical composition for treating the symptoms of herpes simplex which comprises cetyl myristate and cetyl palmitate.
2 A composition of claim 1 wherein said cetyl myristate comprises at least 50% by weight of composition.
3 A composition of claim 1 or 2 wherein said composition also includes at least one pharmaceutically acceptable excipient and/or diluent.
4. An oral dosage unit effective in the treatment of the symptoms of herpes simplex, said dosage unit having a mixture of cetyl myristate and cetyl palmitate.
5. A dosage unit as claimed in claim 4 wherein said cetyl myristate comprises from 50 to 98 w/w of the mixture.
6. A dosage unit of any one claim 4 or 5 wherein there is from 5 to 400 mg of the mixture of cetyl myristate and cetyl palmitate.
7. A dosage unit of any one of claims 4 to 6 wherein said mixture is in a capsule.
8. A dosage unit as claimed in anyone of claim 4 to 7 wherein said dosage unit also includes a pharmaceutically acceptable excipient and/or diluent.
9. A dosage unit of claim 8 wherein said excipient and/or diluent is selected from any one of the following silicon dioxide calcium phosphate magnesium oxide, and/or one trace element.
10. A liquid dosage composition or unit being also an oral composition of any one of claims 1 to 3 or an oral dosage unit as claimed in any one of claims 4 to 9 respectively.
II. The use, in the manufacture of an oral dosage composition or unit for the treatment or prophylaxis of the symptoms of herpes simplex or related herpes skin ailments in a mammal, wherein said composition or unit is a mixture of cetyl myristate and cetyl palmitate.
12. The use of claim 11 wherein the ratio by weight of cetyl myristate to cetyl palmitate is
13. A composition of any one of the claims 1 to 3 substantially as hereinbefore described. 14 A dosage unit of any of claims 4 to 9 substantially as hereinbefore described. 95:5. DATED THIS 3rd DAY OF (farcin AJ Park per AGENTS FOR THE APPLICANT