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1. WO1985000011 - MICRODROPLETS OF WATER-INSOLUBLE DRUGS

Publication Number WO/1985/000011
Publication Date 03.01.1985
International Application No. PCT/US1984/000906
International Filing Date 14.06.1984
IPC
A61K 9/107 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions
A61K 9/127 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
CPC
A61K 9/1075
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions ; ; Emulsion preconcentrates; Micelles
1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
A61K 9/127
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
Y10S 514/816
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
10TECHNICAL SUBJECTS COVERED BY FORMER USPC
STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
514Drug, bio-affecting and body treating compositions
816Anesthetic, general
Y10S 514/817
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
10TECHNICAL SUBJECTS COVERED BY FORMER USPC
STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
514Drug, bio-affecting and body treating compositions
817Anesthetic, topical
Y10S 514/818
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
10TECHNICAL SUBJECTS COVERED BY FORMER USPC
STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
514Drug, bio-affecting and body treating compositions
818Anesthetic, local
Y10S 514/937
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
10TECHNICAL SUBJECTS COVERED BY FORMER USPC
STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
514Drug, bio-affecting and body treating compositions
937Dispersion or emulsion
Applicants
  • HAYNES, DUNCAN, HAROLD [US]/[US]
Inventors
  • HAYNES, DUNCAN, HAROLD
Agents
  • CRAWFORD, Arthur, R. @
Priority Data
505,32617.06.1983US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MICRODROPLETS OF WATER-INSOLUBLE DRUGS
(FR) MICRO-GOUTTELETTES DE MEDICAMENTS INSOLUBLES DANS L'EAU
Abstract
(EN)
Microdroplets of water-insoluble drugs coated with a phospholipid are prepared by sonication. As an example, microdroplets of the general anesthetic methoxyfluorane coated by a unimolecular layer of dimyRistoyl phosphatidylcholine are prepared by sonication. The microdroplets so prepared remain stable in physiologically-compatible solution, and are suitable for injection, typically intradermal or intraveneously, into a patient for inducing local anesthesia. These methoxyfluorane-containing microdroplets have been demonstrated to cause long-term local anesthesia when injected intradermally, giving duration of anesthesia 28 times longer than with other anesthetics, such as lidocaine and 11 times longer than with bupivacaine. The latter is considered longest acting conventional local anesthetic. The microdroplet is also capable of solubilizing and delivering benzocaine and other water-insoluble drugs, and thus represents a novel drug delivery system and general method for delivery of water-insoluble drugs, lowering the necessary dose and providing a more direct and timed release.
(FR)
Des micro-gouttelettes de médicaments insolubles dans l'eau enrobées d'un phospholipide sont préparées par traitement sonore. Par exemple, des micro-gouttelettes de l'anesthétique général métoxyfluorane enduites d'une couche unimoléculaire de dimyRistoyl phosphatidylcholine sont préparées par traitement sonore. Les micro-gouttelettes ainsi produites restents stables dans une solution physiologiquement compatible, et sont indiquées pour l'injection, en général par la voie intradermique ou intraveineuse, dans un patient dans le but d'obtenir une anesthésie locale. On a pu démontrer que ces micro-gouttelettes contenant du métoxyfluorane provoquent une anesthésie locale prolongée lorsqu'elles sont injectées par la voie intradermique, produisant une anesthésie d'une durée vingt fois plus longue que celle provoquée par d'autres anesthétiques, tels que la lidocaïne et onze fois plus longue que celle provoquée par la bupivacaïne. La bupivacaïne est considérée comme étant l'anesthétique local conventionnel ayant l'action la plus longue. La micro-gouttelette peut également solubiliser et libérer de la benzocaïne et d'autres médicaments insolubles dans l'eau, et représente par conséquent un nouveau système d'administration de médicaments et un procédé général d'administration de médicaments insolubles dans l'eau, permettant de diminuer la dose nécessaire et d'obtenir une libération plus directe et étalée dans le temps.
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