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Composition for applying active substances to or through the skin

Patent 5716638 Issued on February 10, 1998. Estimated Expiration Date: Icon_subject November 27, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

Multiphase liposomal drug delivery system
Patent #: 4761288
Issued on: 08/02/1988
Inventor: Mezei

Method of preparing lipid structures
Patent #: 4994213
Issued on: 02/19/1991
Inventor: Aitcheson, et al.

Pro-liposome compositions
Patent #: 5004611
Issued on: 04/02/1991
Inventor: Leigh

Preparation of liposome and lipid complex compositions
Patent #: 5077057
Issued on: 12/31/1991
Inventor: Szoka, Jr.

Pharmacological agent-lipid solution preparation
Patent #: 5154930
Issued on: 10/13/1992
Inventor: Popescu, et al.

Compositions for applying active substances to or through the skin Patent #: 5540934
Issued on: 07/30/1996
Inventor: Touitou

Inventor

Assignee

Application

No. 563144 filed on 11/27/1995

US Classes:

424/450, Liposomes264/4.1, Liquid encapsulation utilizing an emulsion or dispersion to form a solid-walled microcapsule (includes liposome)264/4.3, With treatment subsequent to solid wall formation (e.g., coating, hardening, etc.)424/63, LIVE SKIN COLORANT CONTAINING424/401Cosmetic, antiperspirant, dentifrice

Examiners

Primary: Kishore, Gollamudi S.

Attorney, Agent or Firm

International Class

A61K 009/127

Abstract

A cosmetic or medical composition for topical application to the skin. It results in the transdermal passage of an active ingredient, or in the introduction of such agent into the skin. The essential components of such compositions are phospholipids, an aliphatic alcohol of three or four carbon atoms or a combination of these alcohols, water and a compatible active ingredient, optionally with propylene glycol. Compositions advantageously comprise from 0.5% to 10% phospholipids, from 5% to 35% of a C3 - or C4 -alcohol, 15 to 30% ethanol, which contain together at least 20% but not more than 40 wt. % of ethanol and the C3 -alcohol; up to 20 wt. % propylene glycol, at least 20% water and at least one active ingredient. The compositions are suitable for the topical application of a wide variety of cosmetic and pharmaceutically active compounds. Phospholipids of choice are phosphatidylcholine, (P C), hydrogenated P C, phosphatidic acid (P A), phosphatidylserine (P S), phosphatidylethanolamine (P E), phosphatidylglycerol (P P G) and phosphatidylinositol (P I).

Other References

  • Touitou et al., International Journal of Pharmaceutics, Modulation of Cafne Skin . . . , 103 (1994) 131-136
  • Touitou et al., Journal of Pharmaceutical Sciences, Liposomes as Carriers for . . . , vol. 83, No. 9, Sep. 1994
  • Riaz et al., Riaz, Weinr, and Martin, Liposomes, Chapter 16, pp. 568-603
  • Batzri et al., Single Bilayer Liposomes Prepared Without Sonication, Biochim.Biophys.Acta. 298 (1973) 1015-1019
  • Kremer et al., Vesicles of Variable Diameter Prepared By Modified Injection Method, Biochemistry 16 (1977) pp. 3932-3935
  • Barry, V.W. Optimizing Percutaneous Absorption. In Bronaugh, R.L. and Maibach, M.I. (Eds), Percutaneous Absorption, Dekker, New York, 1989, pp. 531-565
  • Touitou et al., Altered Skin Permeation Of Highly Lipophilic Molecule: Tetrahydrocannabinol. Int. J. Pharm. 43 (1988) 17-22
  • Touitou et al. Enhanced Permeation Of Theophylline Through The Skin And Its Effect On Fibroblast Proliferation. Int. J. Pharm. 70 (1991) 159-166
  • Joachim Roding, Natipide II: New Easy Liposome System, Lecture held at In-Cosmetics 6-8 Mar. 1990, Birmingham
  • Eugene R. Cooper, Increased Skin Permeability For Lipophilic Molecules, Journal of Pharmaceutical Sciences, vol. 73, No. 8, Aug. 198
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