Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1997-08-05
1999-03-30
Weddington, Kevin E.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
514647, 514654, 514661, A61K 9127, A61K 31135, A61K 3113
Patent
active
058885366
DESCRIPTION:
BRIEF SUMMARY
This appln. is a 371 of PCT/HU95/00052, filed Oct. 20, 1995.
The invention relates to liposomic compositions containing as active ingredient selegilin (-)-(N-.alpha.-dimethyl-N-(2-propynylphenylethylaniine) and/or a salt thereof. Further, the invention relates to their preparation, pharmaceutical compositions containing them and their therapeutical use.
Nowadays a great number of liposomic compositions and processes for their preparation is known in the art.
Such compositions are, as a matter of fact, "drug delivery systems" (DDS), as described by G. Gregoriadis et al (Receptor-mediated targeting of drugs, Plenum Press, New York. 243-266, 1980). They contain the active ingredient similarly to encapsulated status in one or more lamellar membranes comprising lipids, i.e. in liposomes. The good absorption and biodisposition of the active ingredient(s) can be influenced among others by the composition and method of preparation of the liposomes so that it can deliver the active ingredient into a specified area. In the liposomic compositions the active ingredient is encompassed by one or more lipid lamella(s) which also serve as a carrier of the active ingredient.
Multilamellar lipid vehicles (MLV) were first prepared and described by Bangham et al (J. Mol. Biol. 13, 238-252, 1965).When biologically active substances are encapsulated in small, unilamillar lipid vesicles, water-soluble substances can be encapsulated by poor efficiency due to the small volume of water encapsulated into the SUV (small unilamellar lipid vesicles) (U.S. Pat. No. 4,089,801).
Unilamellar lipid vesicles were prepared by other methods, i.e. by Biophys. Acta 443, 629-634, (1976)! so that the solution of lipids in an organic solvent was injected quickly into a buffer solution and thus unilamellar liposomes were formed spontaneously. The method is rapid and generally used but results in diluted liposomic preparations and poor encapsulating effectivity.
Unilamellar liposomes can be formed also by the so-called detergent Gregoriadis, CRC Press Inc., Boca Raton, Fla., Vol. 1. Ch 7, pp. 79-107, (1984)!, in the course of which the lipids and other substances are dissolved together with detergents and then the detergents are removed by dialysis.
Multilamellar liposoinic encapsulation is carried out according to U.S. Pat. No. 4,234,871 (Papahadjopoulos) by the so-called reverse phase evaporation (REV) technique and according to U.S. Pat. No. 4,016,100 (Suzuki) by lyophilizing the aqueous-lipidic dispersion of lipids and the biologically active substance.
In the published patent specification No. WO 93/20934 the preparation of a stable, aqueous liposomic suspension is disclosed which can be stored for 6 months at 40.degree. C.
In the course of the preparation of the above liposomic compositions the dispersion of the lipids and the aqueous phase is carried out in contact Pat. No. 4,485,054!.
According to U.S. Pat. No. 4,761,288 which is expressly incorporated herein by reference, multiphase systems are prepared for improving the absorption of the biologically active substances having poor water-solubility, which contain the active ingredient in super-satureted solution form, in solid form and encapsulated in multilamellar lipid vesicles. The vesicles, the solution and the solid form of the biologically active compound are dispersed in a hydrocolloidal gel. The hydrocolloidal gel is prepared by utilizing the method for preparing multilamellar lipid vesicles described in U.S. Pat. No. 4,485,054 expressly incorporated herein by reference. Thus, liposomic compositions can be prepared, in which the active ingredient is present in higher concentrations than could be expected on the basis of its water- and/or liposolubility.
In U.S. Pat. No. 4,937,078 liposomic compositions of locally applied anesthetic and analgesic active ingredients are disclosed. It was found that locally applied active ingredients are more effective in liposomal encapsulated state than the usual ointment, cream or liquid compositions. The liposoma formation itself has been carried out
REFERENCES:
patent: 4089801 (1978-05-01), Schneider
patent: 4485054 (1984-11-01), Mezei et al.
patent: 4761288 (1988-08-01), Mezei
patent: 4937078 (1990-06-01), Mezei et al.
Windholz et al., T6 Merck Index, 10th Ed. p. 419 abstract No. 2876 (Selegilin).
Gaal Jozsef
Lengyel Jozsef
Magyar Kalman
Marmarosi Katalin
Mezei Michael
Chinoin Ltd.
Weddington Kevin E.
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