Opioid formulations

Abstract

The present invention provides high-concentration formulations of opioids such as fentanyl or fentanyl congeners. The formulation of the invention comprises fentanyl or a fentanyl congener in concentrations significantly in excess of conventional formulations, e.g., on the order about 2-fold to about 10,000-fold greater than conventional formulations, e.g., currently commercially available formulations. These formulations are particularly useful for long-term delivery to a subject suffering from pain. The invention further provides drug delivery devices comprising the high-concentration opioid formulations, and further provides methods of alleviating pain in a subject, comprising administering the high-concentration formulations to a subject in need thereof.

Description

FIELD OF THE INVENTION [0001] The invention relates to high-concentration formulations of opioids to alleviate pain. BACKGROUND OF THE INVENTION [0002] Opiates in various forms, including opium, heroine and morphine which derive from the opium poppy, have very powerful analgesic properties and have seen widespread use for anesthesia as well the treatment of pain, especially where the pain is very severe. In addition to these natural opiates, many synthetic opioids have since been synthesized including fentanyl and congeners of fentanyl such as sufentanil, alfentanil, lofentanil, carfentanil, remifentanil, etc., which are many times more potent than morphine. [0003] At present, the dosage form with the most widespread use is still morphine administered orally, although opioids can also be delivered by intravenous infusion (see, e.g., Scholz et al. 1996 Clin. Pharmacokinet. 31:275-92; White 1989 Anesth. Analg. 68:161-71), oral administration, (see, e.g., U.S. Pat. Nos. 4,769,372; 5,20...

AI Technical Summary

Benefits of technology

Enables consistent, long-term delivery of therapeutic amounts of opioids with reduced risk of infection and tissue damage, improving patient compliance and maintaining accurate dosing without the need for frequent device refills or replacements.

Problems solved by technology

An aqueous formulation would thus not provide sufficient drug concentration to meet the desired dosing requirements for a system with a small drug reservoir, e.g., an implantable system, without the need for frequent re-filling of the drug reservoir or providing a new implant.