Microdroplets of water-insoluble drugs and injectable formulatio

Details Microdroplets of water-insoluble drugs and injectable formulatio Microdroplets of water-insoluble drugs and injectable formulatio

1986-04-22

1988-02-16

Griffin, Ronald W.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424450, 514965, 514801, 514816, 514818, 514906, 514923, 514869, 514822, A61K 910, A61K 952

Patent

active

047254424

ABSTRACT:
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 dimysistoyl phosphatidylcholine are prepared by sonication. The microdroplets so prepared remain stable in physiologically-compatible solution, and are suitable for injection, typically intradermally or intraveneously, into a patient for inducing local anesthesia. These methoxyflurane-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.

REFERENCES:
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patent: 4078052 (1978-03-01), Papahadjopoulos
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patent: 4529561 (1985-07-01), Hunt et al.
patent: 4532089 (1985-07-01), MacDonald
patent: 4622219 (1986-11-01), Haynes

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