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High concentration formulations of opioids and opioid derivatives

A technology of opioid substances and derivatives, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, anesthetics, etc., can solve problems such as tissue edema, patient discomfort, and dilute opioid preparations, and achieve Precise dosing, reduced risk of infection and tissue damage, increased compliance

Inactive Publication Date: 2006-02-15
DURECT CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, injecting large volumes of fluid into certain tissues can cause tissue edema, leading to patient discomfort
[0009] Currently available commercial opioid formulations are too dilute to meet the needs of patients requiring long-term treatment or large amounts of pharmaceutical formulations for pain management

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Example 1: Sufentanil formulation in lactic acid solvent

[0103] A sufentanil formulation at a concentration of 600 mg / ml was prepared by adding approximately 30 g of sufentanil to 14 ml of 88% L-lactic acid followed by 15 ml of water and stirring the mixture until all solutes were dissolved. Water was added to the resulting solution to obtain a total volume of 50 ml. The molar ratio of L-lactic acid to drug in the final formulation was approximately 2, and the final pH was 4.1.

Embodiment 2

[0104] Example 2: Sufentanil formulation in acetic acid solvent

[0105] A 500 mg / ml sufentanil formulation was prepared by adding approximately 1.03 g of sufentanil free base to 0.7 ml of a 50:50 mixture of acetic acid:water followed by 0.5 ml of water. Stir the mixture until dissolved. Water was added to the resulting solution to obtain a volume of 2 ml. The molar ratio of acetic acid to drug was about 2.3 and the final pH was 4.5.

Embodiment 3

[0106] Example 3: Hydromorphone Formulation in Acetic Acid Solvent

[0107] A hydromorphone formulation of approximately 600 mg / ml was prepared by adding approximately 15 g of hydromorphone base to 9 ml of glacial acetic acid followed by 0.5 ml of water. Stir the mixture until dissolved. Water was added to the resulting solution to obtain a volume of 25 ml. The molar ratio of acetic acid to drug was about 3 and the final pH was 4.5.

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PUM

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Abstract

The present invention provides opioid formulations suitable for long-term delivery to a subject. The formulation of the invention comprises an opioid or opioid derivative (e.g., morphine, hydromorphone, fentanyl or a fentanyl congener), and an aqueous solvent comprising a low molecular weight carboxylic acid (e.g., C2-4, C2-7). The invention thus provides for formulations comprising morphine, hydromorphone, fentanyl or fentanyl congeners in concentrations significantly in excess of conventional aqueous formulations, e.g., on the order about 2-fold to about 10,000-fold greater than conventional formulations, e.g., currently commercially available formulations.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US application US 10 / 305,252, filed November 25, 2002, the entire contents of which are incorporated herein by reference. technical field [0003] The present invention relates to high concentration aqueous formulations of opioids for pain relief. Background technique [0004] Various forms of opiates, including opium derived from the opium poppy, heroin, and morphine, have potent analgesic properties and have been widely used for anesthesia as well as for the treatment of pain, especially very severe pain. In addition to these natural opiates, a number of synthetic opioids have been synthesized, including hydromorphone, fentanyl, and fentanyl congeners such as sufentanil, alfentanil, profentanil Carfentanil, Remifentanil, etc. These substances are several times more effective than morphine. [0005] Although the most common dosage form used is morphine administered orally, opi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61K31/445A61K9/00A61K9/08A61K31/19A61K47/12
CPCA61K31/19A61K9/0019A61K9/08A61K47/12A61K31/445A61P23/00A61P25/04A61P29/00Y02A50/30
Inventor 陈大华威尔玛·塔姆拉兹李明蓉
Owner DURECT CORP
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