Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1992-07-23
1995-01-17
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424DIG5, 424 64, 424445, 4241951, 514934, 514944, 514951, A61K 3152
Patent
active
053824369
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
This invention relates to pharmaceutical compositions for use in the treatment of lesions resulting from Herpes Simplex Virus (HSV) infections.
Herpes simplex is an enveloped, Class I Double Stranded DNA Virus. It infects vertebrates and it is thought that by the age 21, up to 80% of the population are infected with the so-called Type I virus or Herpes simplex labialis hereinafter referred to as HSVI. The vital infection begins when a virion comes into contact with a host cell and attaches to it. The vital DNA and proteins then cross the membrane into the cytoplasm of the cell ending up in the nucleus where the vital nucleic acid interacts with the host cell's nucleic acid synthesising machinery to direct its own replication and the synthesis of vital proteins. The multiple components of the herpes virions assemble in stages resulting in the production of a new round of virus particles and the death of the cell.
Primary HSVI infection occurs normally as a result of direct mouth to mouth or hand to mouth contact with a carrier. The primary infection is widespread (e.g. a rash inside the mouth) and often goes unnoticed. Following infection, the virus particles travel by axonal flow to nerve ganglia within the maxillary branch of the trigeminal nerve (which supplies the muscles around the mouth) where they remain dormant.
The dormant virus can undergo reactivation at any time resulting in localized lesions--the characteristic "cold-sore". Reactivation factors include any occurences causing immunosuppression such as infection, stress, pregnancy, drugs etc.
The second strain of HSV is HSV II--(Herpes simplex genitalis) which give rise to lesions in the genital regions. HSV II is sexually transmitted and although HSV types I and II were originally separate they have become interchangeable due to aberrant sexual practices.
Infants can become infected with HSV II as a result of passage through the birth canal of an infected mother. Following infection with HSV II the virus remains dormant in the sacral ganglia.
A current treatment for HSV infections is use of the drug Acyclovir which acts to prevent viral replication by blocking the action of the vital DNA polymerase. Though very effective, this drug is expensive, available only on prescription, and is generally recommended for use only under close medical supervision.
SUMMARY OF THE INVENTION
An object of this invention is to provide a pharmaceutical composition in a form which can be applied topically for the treatment of lesions resulting from HSV infections which is less expensive than Acyclovir and is available without prescription.
Methyl xanthines such as caffeine, theophylline and theobromine have been shown to have an inhibitory effect in vitro on the growth of Hela, Veto and human diploid skin fibroblasts in tissue culture (Lino et al., 1976. Shaw et al., 1981). These authors have described inhibitory effects on proliferation at concentrations about 4 mM. Damon and Raouth (1969) found that caffeine inhibits or delays mitosis in mouse L cells and at a concentration of 2 mM causes a delay in progression of cells in the G.sub.1 phase of growth to the S phase where cells are engaged in DNA synthesis. Beetham and Tolmach (1982) working with Hela cells, found that caffeine at concentrations below 15 mM kills only cells replicating DNA. That caffeine suppresses the growth of certain viruses including polio, influenza and vaccinia virus but has no effect on JEV or NDV has been demonstrated by Yamoviaki and Tagaya (1980).
It has further been suggested (Morgan et al., (1968), Smith (1964) and Nil et al., (1968)) that caffeine may act to prevent proper assembly of the virion in the nucleus namely be disrupting the budding process through the nuclear membrane so that those particles which do bud through the membrane collect malformed envelopes and are rendered non-infective.
None of these prior art references discloses or suggests that caffeine might possess anti-vital activity when administered topically to cells infected with HSV, n
REFERENCES:
patent: 4132782 (1979-01-01), Bean
patent: 4684522 (1987-08-01), Marissal et al.
patent: 4945094 (1990-07-01), Salim
patent: 5030451 (1991-07-01), Trebosc et al.
Chemical Abstracts, vol. 109, No. 25, 19 Dec. 1988, W. P. P. Leary et al., Xanthines in Treatment of Herpes Blisters, p. 72.
Page Thurman K.
Spear James M.
Surtech International Limited
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