Methods of stabilizing azithromycin

Abstract

A method of packaging of azithromycin which provides improved stability of azithromycin upon storage. Additionally, compositions and methods of stabilizing azithromycin compositions are described. Stabilized azithromycin compositions comprise an intimate admixture of azithromycin and a stabilizing-effective amount of an antioxidant to improve the resistance of the azithromycin to degradation. Coprecipitation or co-milling of azithromycin and an antioxidant are particularly preferred means of achieving an intimate admixture. Pharmaceutical formulations comprising a stabilized azithromycin composition and methods of making such formulations are also described.

Description

RELATED APPLICATIONS [0001] This application is a continuation in part of U.S. application Ser. No. 10 / 782,047, filed Feb. 19, 2004, which claims the benefit of priority to U.S. provisional application Ser. No. 60 / 448,946, filed Feb. 19, 2003, herein incorporated by reference. This application is also a continuation in part of U.S. application Ser. No. 10 / 936,075, filed Sep. 7, 2004, which is a continuation of U.S. application Ser. No. 10 / 822,773, filed Apr. 13, 2004, which is a continuation of U.S. application Ser. No. 10 / 247,097, filed Oct. 18, 2002, which claims the benefit of priority to U.S. provisional application Ser. Nos. 60 / 336,346, filed Oct. 18, 2001; 60 / 331,931, filed Nov. 21, 2001; and 60 / 341,295, filed Dec. 17, 2001, herein incorporated by reference.FIELD OF THE INVENTION [0002] The invention encompasses methods of packaging azithromycin to prevent the degradation of azithromycin upon storage. The invention also relates to stabilized azithromycin compositions, methods ...

AI Technical Summary

Benefits of technology

"The patent describes methods for packaging and stabilizing the antibiotic azithromycin. The methods involve storing the azithromycin in a gas impermeable package made of at least one sheet of gas impermeable material, which prevents degradation products from forming. The gas impermeable package may be made of aluminum laminate. The methods also involve adding an antioxidant to the azithromycin, which prevents the transformation of the azithromycin monohydrate to the dihydrate form on storage. The stabilized azithromycin compositions can be used to make pharmaceutical formulations, such as tablets, capsules, and suspensions. The technical effects of the patent include improved stability of azithromycin and the ability to make pharmaceutical formulations with the stabilized azithromycin compositions."

Problems solved by technology

Macrolide antibiotics of the erythromycin class, such as erythromycin A, are known to be unstable in an acidic environment and are inactivated by gastric acids.

Azithromycin is subject to degradation that may occur during manufacture and / or storage.

For example, azithromycin is susceptible to degradation if exposed to elevated temperatures and / or air during manufacturing processes, processes that include formulation of the pharmaceutical dosage form.

The susceptibility of azithromycin to degradation may lead to deviation of the drug product from regulatory purity requirements even prior to the product reaching the patient.

In addition, once formulated, azithromycin tends to degrade under normal storage conditions, which may result in the presence of unacceptable levels of impurities at the time of administration.

Images