United States Patent:   6,017,963

Assignee:  Euro-Celtique, S.A. (Luxembourg, LU)

Filed:  November 14, 1995

A dosage form for intranasal and/or inhalation administration of an analgesic having low opioid receptor binding activity to a warm blooded animal, that includes a pharmaceutically effective amount of the analgesic. A preferred analgesic is tramadol, a tramadol and/or a pharmaceutically acceptable salt, metabolite or derivative thereof. Methods of making and using the formulation according to the invention are also provided.

SUMMARY OF THE INVENTION

In accordance with the above objects and others which will be apparent from the further reading of the specification and of the appended claims, the present invention is related to the surprising discovery that an analgesic that is a weak opioid receptor binding compound can be effectively administered to a warm blooded animal, including a human patient, by administering a pharmaceutically effective amount of the compound, or a pharmaceutically acceptable salt, to the respiratory tract mucosal surfaces of an animal in need of treatment.

The invention also provides for a dosage form for intranasal and/or inhalation administration of a weak opioid or non-opioid analgesic, to a warm blooded animal.

The invention also provides for a method for producing analgesia in a warm blooded animal, such as a human patient, comprising contacting respiratory tract mucosal surfaces, such as the nasal and/or bronchial mucosal surfaces of a warm blooded animal in need of analgesia, with an analgesically effective amount of a weak opioid or non-opioid analgesic.

The compound can be, for example, the weak opioid analgesic tramadol, either as the free base, and/or as its pharmaceutically acceptable derivatives, salts and active metabolites or in any combination thereof. The compound can be administered to the respiratory tract either intranasally and/or by inhalation.

The dosage form can include a pharmaceutically effective amount of a weak opioid or non-opioid analgesic, such as, e.g., tramadol as described above, together with a pharmaceutically acceptable carrier that is suitable for intranasal and/or inhalation administration. The dosage form can contain, for example, tramadol HCl in an amount ranging from 10 mg to 500 mg.

The dosage form suitable for intranasal and/or inhalation administration can be in the form of, e.g., a liquid solution, suspension, emulsion, liposome or similar such multiphasic composition. Preferably, the dosage form includes a carrier of isotonic saline and a pharmaceutically acceptable buffer. For intranasal administration alone, the dosage form may also include an emulsion, a paste, a cream and/or a gel or gauze packing impregnated with the analgesic to be administered. A useful tramadol metabolite, that is also analgesically active, is for example, mono-O-desmethyltramadol, which can also be so administered at an effective dose intranasally and/or by inhalation alone or in combination with another drug, such as, for example, a tramadol and/or a salt or derivative thereof.

Claim 1 of 11 Claims

1. A method for producing analgesia in a warm blooded animal comprising contacting a nasal tract mucosal surface of a warm blooded animal in need thereof with an intranasal pharmaceutical formulation comprising a pharmaceutically effective amount of tramadol or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable carrier.

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