Drug – bio-affecting and body treating compositions – Anti-perspirants or perspiration deodorants
Patent
1992-06-09
1997-11-04
Dodson, Shelley A.
Drug, bio-affecting and body treating compositions
Anti-perspirants or perspiration deodorants
512 1, 574533, A61K 732, A61K 31235
Patent
active
056836821
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
This invention relates to derivatives of aromatic benzoates as inhibitors of esterase-producing micro-organisms, for use primarily in deodorant compositions.
The human skin has a large natural population of micro-organisms. These organisms are nourished by various skin-secreted substances, skin cell debris, breakdown products of the skin and the organisms themselves. The skin secretions are conveniently divided into two groups, those containing water-soluble materials and constituted by eccrine and apocrine sweat, and sebum which contains lipid-soluble materials. These secretions will be referred to as `liquid body-secretions` and they will now be described, as will their functions as they are generally understood.
Eccrine sweat consists mainly of a watery solution of dissolved salts and is produced by glands distributed over the whole skin surface. In conditions of occlusion, e.g. feet enclosed in socks and shoes, the eccrine sweat accumulates, and in these warm damp conditions, the skin debris, together with nutrients from the sweat, provide a medium for micro-organism growth with the possibility of massive overgrowth of one type. This can result, in the first instance, in odorous metabolic products, and in the second, in clinical infection with maceration of the skin and irritation.
Apocrine sweat is produced by the apocrine glands at specific sites on the body, notably the axillae, the anogenital area and around the nipples. Although present at birth, the apocrine glands are not functional until puberty when they are influenced by circulating androgens. Apocrine secretion differs from eccrine sweat in containing lipids (fatty materials) and proteins. In the warm, damp occlusion met in the axillae, certain skin micro-organisms metabolise this secretion, forming free fatty acids and other breakdown products. These materials are odorous and responsible for `body odour`.
The sebaceous glands are distributed over the skin surface except the palms and dorsae. They are most numerous on the scalp, forehead, face, back and chest. The secretion, sebum, consists mainly of fatty materials, wax esters, cholesterol and its esters and squalene. Normally, sebum flows freely from the glands, spreading over the skin surface. In acneic and certain other skin conditions, the sebaceous duct through which the sebum is normally secreted becomes hyperkeratinised and the opening of the duct becomes blocked. The gland continues to produce sebum and the blocked duct distends to form a comedone. Also blocked in the duct, the (normally) commensal micro-organisms produce esterases which hydrolyse the sebum lipids, liberating free fatty acids. These fatty acids are irritant and can result in an inflammatory reaction along the wall of the duct. Leucocytes invade the inflamed area and the comedone develops into a papule and then a pustule. This is a typical acne `spot`.
The scalp is well supplied with sebaceous glands, and the scalp, like all skin, undergoes desquamation. Due to the presence of hair, the squames tend to be retained at the scalp surface. Sebum accumulates beneath these squames and in dandruff conditions is hydrolysed by micro-organism produced esterases to form irritant fatty acids. The irritation causes proliferation of the epidermis and increased formation of the stratum corneum which again desquamates unevenly in large clumps--the dandruff scale or flake.
In our International Application No. PCT/GB87/00323 (Publication No. W087/06827) we disclosed an inhibitor of esterase-producing microorganisms in which the active ingredient comprised an aromatic acid ester of a phenol or of an aromatic alcohol, the phenol or aromatic alcohol being sufficiently water-soluble to impart an anti-microbial action and the aromatic acid being sufficiently water-soluble to impart an anti-microbial action and/or to lower the pH of liquid body-secretion to a level which at least inhibits the growth of micro-organisms in the liquid body-secretions; for use in deodorants the active ingredient may be incorporated
Dodson Shelley A.
Robertet S.A.
Wrya James Creighton
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