Topical application of opioid analgesic drugs such as morphine
AssigneeEl Khoury and Stein, Ltd.
InventorsGeorge F. El Khoury, Christoph Stein
Life of this patent
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Abstract
The invention is directed to methods and pharmaceutical compositions for the topical administration of opioid analgesic drugs such as morphine. In particular, the invention relates to topical administration of an opioid analgesic agent, e.g., morphine sulfate, to produce a localized analgesic effect in inflamed skin or mucosal tissue, and without a transdermal or transmucosal migration of opioid agent, e.g., into the systemic circulation.
Claims20
A method of inducing analgesia in inflamed skin or mucosal tissue, comprising topically administering to a patient in need of such treatment a topically effective amount of an opioid analgesic agent, which amount is systemically ineffective for induction of analgesia, admixed with a pharmaceutically acceptable excipient for topical administration, wherein said opioid is cyclazocine, piperidine, piperazine, pyrrolidine, morphiceptin, meperidine, trifluadom, benzeneacetamine, diacylacetamide, benzomorphan, hydromorphone, oxymorphone, levophanol, methadone, meperidine, fentanyl, codeine, hydrocodone, oxycodone, propoxyphene, buprenorphine, butorphanol, pentazocine or nalbuphine.
A pharmaceutical composition comprising an admixture of an opioid analgesic agent and a pharmaceutically acceptable excipient for topical administration to inflamed skin or mucosal tissue, wherein
- a unit dosage amount of the admixture contains a systemically ineffective amount of the opioid analgesic agent, and
- the excipient does not enhance transdermal or transmucosal transmission of the opioid analgesic agent,
- with the proviso that, when the admixture is a liquid, it further comprises a component that is pharmaceutically unacceptable for parenteral administration,
- wherein said opioid is cyclazocine, piperidine, piperazine, pyrrolidine, morphiceptin, meperidine, trifluadom, benzeneacetamine, diacylacetamide, benzomorphan, hydromorphone, oxymorphone, levophanol, methadone, meperidine, fentanyl, codeine, hydrocodone, oxycodone, propoxyphene, buprenorphine, butorphanol, pentazocine or nalbuphine.
A pharmaceutical composition comprising an admixture of an opioid analgesic agent and a pharmaceutically acceptable excipient for topical administration, wherein the excipient does not enhance transdermal or transmucosal transmission of the opioid analgesic agent, in a unit dosage form analgesically equivalent to 2-3 mg. of morphine but systemically analgesically ineffective, wherein said opioid is cyclazocine, piperidine, piperazine, pyrrolidine, morphiceptin, meperidine, trifluadom, benzeneacetamine, diacylacetamide, benzamorphan, hydromorphone, oxymorphone, levophanol, methadone, meperidine, fentanyl, codeine, hydrocodone, oxycodone, propoxyphene, buprenorphine, butorphanol, pentazocine or nalbuphine.
A container adapted for spraying a measured amount of a liquid onto skin, and containing a pharmaceutical composition comprising an admixture of an opioid analgesic agent and a pharmaceutically acceptable excipient for topical administration.
A method of inducing analgesia in inflamed skin or mucosal tissue, comprising topically administering to a patient in need of such treatment a topically analgesically effective amount of an opioid analgesic agent, admixed with a pharmaceutically acceptable excipient for topical administration, wherein the amount of opioid analgesic agent is sufficient to directly activate peripheral opioid receptors in the inflamed skin or mucosal tissue, but not sufficient to activate central nervous system opioid receptors, wherein said opioid is cyclazocine, piperidine, piperazine, pyrrolidine, morphiceptin, meperidine, trifluadom, benzeneacetamine, diacylacetamide, benzomorphan, hydromorphone, oxymorphone, levophanol, methadone, meperidine, fentanyl, codeine, hydrocodone, oxycodone, propoxyphene, buprenorphine, butorphanol, pentazocine or nalbuphine.
Dependencies are inferred from the claim text.