WO1992019233A3 - Sustained release composition and methods of use thereof - Google Patents

Sustained release composition and methods of use thereof Download PDF

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Publication number
WO1992019233A3
WO1992019233A3 PCT/US1992/003555 US9203555W WO9219233A3 WO 1992019233 A3 WO1992019233 A3 WO 1992019233A3 US 9203555 W US9203555 W US 9203555W WO 9219233 A3 WO9219233 A3 WO 9219233A3
Authority
WO
WIPO (PCT)
Prior art keywords
related compounds
compounds
pharmaceutical
agents
chains
Prior art date
Application number
PCT/US1992/003555
Other languages
French (fr)
Other versions
WO1992019233A2 (en
Inventor
Anders Buur
Bente Steffansen
Original Assignee
Control Delivery Sys Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Control Delivery Sys Inc filed Critical Control Delivery Sys Inc
Publication of WO1992019233A2 publication Critical patent/WO1992019233A2/en
Publication of WO1992019233A3 publication Critical patent/WO1992019233A3/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/695—Silicon compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/58—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin

Abstract

The present application relates to lipophilic conjugates of pharmaceutical compounds in admixture with a pharmaceutical vehicle not soluble in an aqueous solvent, such as a silicone oil useful as a sustained released pharmaceutical composition and methods for the treatment of medical disorders by administering an effective amount of such a sustained release pharmaceutical composition. In this invention a wide variety of pharmaceutical compounds are conjugated with the carrier and placed in admixture with a silicone oil. Acceptable compounds for conjugation with the carrier in this release delivery system include, for example, steroids (e.g., dexamethasone, prednisolone and related compounds), anti-neoplastic agents and/or ophthalmic agents (5-Fluorouracil, adriamycin and related compounds), anti-viral agents (ganciclovir, trifluorothymidine and related compounds), nonsteroidal anti-inflammatory agents (flurbiprofen, indomethacin and related compounds), anti-mitotic drugs (colchicine taxol and related compounds), drugs that act on actin polymerization (phalloidin, cytochlasin B and related compounds). Suitable lipophilic carrier molecules include long branched or unbranched alkyl chains. These chains may be saturated or unsaturated and may contain heteroatoms. Silicone chains may also be used.
PCT/US1992/003555 1991-04-29 1992-04-29 Sustained release composition and methods of use thereof WO1992019233A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US69322891A 1991-04-29 1991-04-29
US693,228 1991-04-29

Publications (2)

Publication Number Publication Date
WO1992019233A2 WO1992019233A2 (en) 1992-11-12
WO1992019233A3 true WO1992019233A3 (en) 1993-01-07

Family

ID=24783833

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1992/003555 WO1992019233A2 (en) 1991-04-29 1992-04-29 Sustained release composition and methods of use thereof

Country Status (2)

Country Link
AU (1) AU2025092A (en)
WO (1) WO1992019233A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5411947A (en) * 1989-06-28 1995-05-02 Vestar, Inc. Method of converting a drug to an orally available form by covalently bonding a lipid to the drug
DE4437502A1 (en) * 1993-12-02 1995-06-08 Basf Ag Conjugates of hirudin with lipophilic cpds.
ES2910987T3 (en) * 2016-08-09 2022-05-17 Univ Liverpool Ophthalmic compositions

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ARCHIVES OF OPHTHAMOLOGY, Vol. 104, March 1986, pp. 431-434. *

Also Published As

Publication number Publication date
AU2025092A (en) 1992-12-21
WO1992019233A2 (en) 1992-11-12

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