Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1991-12-12
1995-01-24
Kishore, G. S.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
424 63, 424401, A61K 9127
Patent
active
053841263
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to compositions based on hydrated lipidic lamelar phases or on liposomes containing at least one derivative of labdane, in particular a labd-14-ene, or a plant extract containing it, intended for the preparation of cosmetic or pharmaceutical, particularly dermatological compositions.
Labdanes, and in particular their unsaturated derivatives in 14 position, called labd-14-enes, are diterpenes which are fairly widely distributed in nature.
They are found in particular in different varieties of conifers (particularly pines), tobaccos, cistuses (in particular Cistus ladaniferus, Cistus laurifolius), and Coleus (particularly Coleus forskohlii).
Coleus forskohlii represents one of the two hundred or so known species of Coleus, belonging to the family of Labiaceae and which are found in the tropical and subtropical regions of Asia, Africa, Australia and the Pacific islands. About nine species are catalogued in India. The ten principal varieties of Coleus are catalogued in Indian dictionaries and in particular "The Wealth of India, a dictionary of Indian Raw Materials and Industrial Products, Raw Materials, volume II, Dehli 1950, pages 308-309; the book entitled Indian Materia Medica by Dr. K. M. Nadkarni's, third edition revised and completed by A. K. Nadkarni in two volumes, Volume I, page 372; the book entitled "The Flora of British India" by Sir J. D. Hooker, C.B., K.C., S.I. Volume IV entitled "Asclepiadae to Amarantaceae, pages 624 to 627.
The labdane derivatives to which the present invention refers are in particular derivatives of general formula: ##STR1## in which: R.sub.1 to R.sub.2 are identical or different and each represent a hydroxy group or a --O--COR.sub.6 group in which R.sub.6 represents an alkyl, alcoxy or alkenyl radical possibly substituted, particularly by one or more hydroxy or amino groups, ##STR2## R.sub.5 represents an ethyl or vinyl radical.
Several derivatives of labdane responding to the above formula have been extracted from various plants and in particular from the plant Coleus forskolii. Particular reference will be made to documents FR-2 336 138, FR-2 364 211 and EP-A-1-O 243 646 which describe forskoline (compound of formula I in which R.sub.1 =R.sub.3 =OH; R.sub.2 =OCOCH.sub.3 ; R.sub.4 =O; R.sub.5 =CH.dbd.CH.sub.2), 9-deoxyforskoline (compound of formula I in which R.sub.1 =OH, R.sub.2 =OCOCH.sub.3 ; R.sub.3 =H; R.sub.4 =O; R.sub.5 =CH=CH.sub.2) and coleforsine (compound of formula I In which R.sub.2 =R.sub.3 =OH; R.sub.1 =OCOCH.sub.3 ; R.sub.4 =O; R.sub.5 =CH.dbd.CH.sub.2).
Other derivatives of labdane responding to the above formula have been prepared by synthesis. Particular reference will be made to the following documents: FR-2 372 822; S. V. BHAT et al., J. Chem. Soc., Perkin Trans. 1982, volume 1, page 767; S V. BHAT et al., J. Med. Chem. 1983, volume 26, pages 486-492; EP-A-252 482; EP-A-217 372; E. SEGUIN et al., Planta Medica, 1938, volume 54 No. 1, pages 4-6.
These documents disclose, in addition, that these compounds present certain pharmacological properties and in particular a hypotensive and calming activity on the central nervous system.
Furthermore, document EP-A-O 120 165 describes the local use of associations comprising a .beta.-stimulant and an .alpha..sub.2 -inhibitor, for the treatment of fatty weight. This document cites forskoline by way of example of .beta.-stimulant.
The present invention has for its object to solve the new technical problem consisting in the preparation of a novel formulation of a cosmetic or pharmaceutical, particularly dermatological composition, comprising as active ingredient a labdane or a plant extract containing it and making it possible to potentialize the activity of this ingredient, in particular with respect to the stimulation of regrowth of hair or the reduction in hair loss.
In fact, it has been discovered in totally unexpected manner, and this constitutes the basis of the present invention, that the labdanes or the plant extracts containing them, presented an activity stimulating the regrow
REFERENCES:
patent: 4476140 (1984-10-01), Sears
Bonte Frederic
Marechal Christian
Meybeck Alain
Kishore G. S.
LVMH Recherche
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