Pain reducing parenteral liposome formulation

A - Human Necessities – 61 – K

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Details

A61K 9/127 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2279259

Disclosed is an invention directed towards pain-reducing parenteral formulations comprising a macrolide drug entrapped in a liposome vesicle. The macrolide drug is selected from the group consisting of derivatives of erythromycins A, B, C and D; clarithromycin; azithromycin; dirithromycin; josamycin; midecamycin; kitasamycin; roxithromycin; rokitamycin; oleandomycin; miocamycin; flurithromycin; rosaramicin; 8,9-anhydro-4''-deoxy-3'-N-desmethyl- 3'-N-ethylerythromycin B 6,9-hemiacetal; 8,9-anhydro-4''-deoxy-3'-N-desmethyl- 3'-N-ethylerythromycin A 6,9-hemiacetal; and 11-amino-11-deoxy-3-oxo-5-O- desosaminyl-6-O-[1'-3'-quinolyl-2'-propenyl]-erythronolide A 11,12-cyclic carbamate. The formulations of the invention are effective in substantially reducing the pain at the injection site typically associated with the injection of macrolide antibiotics.

Cette invention a trait à des formulations à administration parentérale analgésiques comprenant un macrolide enfermé dans un liposome. Le macrolide est issu du groupe constitué par des dérivés d'érythromycines A, B, C et D, la clarithromycine, l'azithromycine, la dirithromycine, la josamycine, la midécamycine, la kitasamycine, la roxithromycine, la rokitamycine, l'oléandomycine, la miocamycine, la flurithromycine, la rosaramycine ainsi que par 8,9-anhydro-4''-désoxy-3'-N-desméthyl-3'-N-éthylérythromycine B 6,9-hémi-acétal, 8,9-anhydro-4''-désoxy-3'-N-desméthyl-3'-N-éthylérythromycine B 6,9-hémi-acétal et 11-amino-11-désoxy-3-oxo-5-O-désosaminyl-6-O-[1'-3'-quinolyl-2'-propényl]-érythronolide A 11,12-carbamate cyclique. Les formulations de l'invention soulagent efficacement les douleurs sur le site d'injection, d'ordinaire en association avec une injections d'antibiotiques consistant en des macrolides.

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