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EP0306236A2
Expired / Lapsed
EP
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Controlled release formulations
Assignee: Heron Therapeutics LLC
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Filing: 1988-08-26
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Granted: —
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Expires: 2008-08-26
Abstract
Abstract Active substances intended for topical application are incorporated in novel formulations in which they are retained as impregnants inside the pores of porous solid particles or microspheres. The pores form a continuous network open to the exterior of the particles, permitting outward diffusion of the impregnants at a controlled rate depending on the pore size. The impregnated particles are prepared by the polymerization of monomer droplets which contain the active substance mixed in with the monomers, or by impregnation of preformed particles with the active substance.
Inventors
- 👤 Martin Katz
- 👤 Chung-Heng Cheng
- 👤 Richard Won
- 👤 Helen C. Leong
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-07 14:27
CPC Classifications
A; A61; A61K; A61K8/00; A61K8/18; A61K8/30; A61K8/67; A61K8/671; A61K9/00; A61K9/70; A61K8/02; A61K8/0241; A61K8/0279; A61K8/33; A61K8/38; A61K8/49; A61K8/494; A61K8/4953; A61K8/678; A61K8/72; A61K8/81; A61K8/8141; A61K8/8152; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1635; A61P; A61P17/00; A61Q; A61Q17/00; A61Q7/00; A61K2800/00; A61K2800/40; A61K2800/41; A61K2800/412; A61K2800/56; A61Q19/00; A61Q19/08
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
79 words
A topical composition comprising solid particles containing a substantially continuous non-collapsible network of pores open to the exterior of said particles, and an impregnant retained inside said pores, wherein said impregnant comprises one or more of: a hair growth promotion agent; a therapeutic agent effective in the cosmetic and/or therapeutic treatment of acne; a fragrant substance; one or more substances selected from vitamins, vitamin derivatives and vitamin-containing substances; a counter-irritant substance; an epidermal lipid-replacement agent; optionally in a solvent.
Claim 2
Dependent Claim
79 words
A topical composition comprising solid particles containing a substantially continuous non-collapsible network of pores open to the exterior of said particles, and an impregnant retained inside said pores, wherein said impregnant comprises one or more of: a hair growth promotion agent; a therapeutic agent effective in the cosmetic and/or therapeutic treatment of acne; a fragrant substance; one or more substances selected from vitamins, vitamin derivatives and vitamin-containing substances; a counter-irritant substance; an epidermal lipid-replacement agent; optionally in a solvent.
Claim 3
Dependent Claim
26 words
A topical composition in accordance with claim 1 in which said solvent is a member selected from the group consisting of ethers, alcohols, aromatics and alkanes.
Claim 4
Dependent Claim
23 words
A topical composition in accordance with claim 1 or 2 in which said impregnant comprises a hair growth promotion agent which is Minoxidil.
Claim 5
Dependent Claim
29 words
A topical composition in accordance with any preceding claim in which said impregnant comprises a therapeutic agent for acne selected from benzoyl peroxide, salicylic acid, resorcinol, and mixtures thereof.
Claim 6
Dependent Claim
29 words
A topical composition in accordance with any preceding claim in which said impregnant comprises a fragrant substance selected from flower oils, essential oils, animal substances synthetic fragrances and resinoids.
Claim 7
Dependent Claim
35 words
A topical composition in accordance with any preceding claim in which said impregnant is comprised of a retinoid composition, preferably selected from retinol, 3-dihydroretinol, retinoic acids, retinoic aldehydes, retinoic acid esters, and aromatic derivatives thereof.
Claim 8
Dependent Claim
71 words
A topical composition in accordance with any preceding claim in which said impregnant comprises a counterirritant substance which is a liquid substantially immiscible with water and/or is in the form of a solution of a counterirritant compound in a solvent substantially immiscible with water or in a solvent at least partially miscible with water; the solution optionally being an organic solution of a counterirritant compound which is solid under ambient conditions.
Claim 9
Dependent Claim
30 words
A topical composition in accordance with any preceding claim in which said impregnant comprises a counterirritant substance comprised of a volatile compound, preferably selected from menthol, camphor and methyl salicylate.
Claim 10
Dependent Claim
26 words
A topical composition in accordance with any preceding claim in which said impregnant comprises an epidermal lipid replacement agent selected from squalane, squalene, and mixtures thereof.
Claim 11
Dependent Claim
76 words
A topical composition in accordance with any preceding claim in which said solid particles are substantially spherical in shape, are formed from a cross-linked polymer, have an average diameter of about 10 microns to about 40 microns, have a total pore volume of about 0.1 cc/g to about 2.0 cc/g have a surface area of about 20 m²/g to about 200 m²/g, and have an average pore diameter of about 0.003 micron to about 1.0 micron.
Claim 12
Dependent Claim
38 words
A topical composition in accordance with any preceding claim in which said solid particles are formed of a copolymer of styrene and divinylbenzene; or of methyl methacrylate and ethylene glycol dimethacrylate or of 4-vinylpyridine and ethylene glycol dimethacrylate.
Claim 13
Dependent Claim
30 words
A topical composition in accordance with any preceding claim in which said solid particles are combined with a vehicle to form a composition selected from fluid, semi-solid and solid compositions.
Claim 14
Dependent Claim
21 words
A topical composition in accordance with any preceding claim in which said impregnant comprises from about 5% to about 65% thereof.
Claim 15
Independent Claim
114 words
A method for preparing a topical composition according to any preceding claim comprising: (a) combining a monomer composition capable of forming a crosslinked polymer with an impregnant to form a homogeneous, substantially non-water-miscible liquid solution; (b) dispersing said non-water-miscible liquid solution in an aqueous phase to form a suspension containing said non-water-miscible liquid solution as discrete droplets; (c) polymerizing said monomer composition in said suspension under conditions under which said impregnant is substantially inert to convert said droplets to solid particles containing a non-collapsible, substantially continuous network of pores open to the exterior of said solid particles with said impregnant retained in said pores; and d) recovering said solid particles from said aqueous phase.
Claim 16
Independent Claim
46 words
A method for preparing a topical composition according to any of claims 1 to 13 comprising: (a) forming solid particles containing a substantially continuous network of pores open to the exterior of said particles; and (b) impregnating said pores of said solid particles with an impregnant.
Claim 17
Dependent Claim
91 words
A method in accordance with claim 15 in which step (a) comprises: (i) combining a monomer composition with a substantially water-immiscible liquid species which is inert with respect to said monomer composition to form a homogeneous, substantially water-immiscible liquid solution; (ii) suspending said liquid solution in an aqueous solution to form a dispersion; (iii) polymerizing said monomer composition in said dispersion to form solid beads containing said water-immiscible liquid chemical species; (iv) recovering said solid beads from said dispersion; and (v) extracting said water-immiscible liquid chemical species from said solid beads.
Claim 18
Independent Claim
35 words
A method for cosmetic treatment of an epidermal region, said method comprising applying to said epidermal region a topical composition according to any of claims 1 to 13, said impregnant comprising a cosmetic treatment agent.
References Cited (Backward Citations)
No citation records indexed.
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