Pharmaceutical formulation

Abstract

Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided.

Description

RELATED APPLICATIONS[0001]This application is a continuation of U.S. patent application Ser. No. 10 / 821,811, filed Apr. 8, 2004, entitled “PHARMACEUTICAL FORMULATION,” which claims priority under 35 U.S.C. §119(e) to U.S. Provisional Application Ser. No. 60 / 461,611, entitled “PHARMACEUTICAL FORMULATION,” filed on Apr. 8, 2003, the contents of which applications are incorporated herein by reference in their entirety.FIELD OF THE INVENTION[0002]This invention relates to methylnaltrexone pharmaceutical preparations, methylnaltrexone formulations, methylnaltrexone kits, and methods of making the same.BACKGROUND OF THE INVENTION[0003]Quaternary amine opioid antagonist derivatives have been shown to have utility in a number of contexts. They are considered peripherally acting only, and, therefore, find particular utility in reducing the side-effects of opioids without reducing the analgesic effect of opioids. Such side effects include nausea, emesis, dysphoria, pruritis, urinary retention...

AI Technical Summary

Benefits of technology

[0015]In any one of the foregoing embodiments, the methylnaltrexone can be present in an amount sufficient to treat nausea, emesis, dysphoria, pruritus, urinary retention, ileus, post-operative ileus, post-partum ileus, paralytic ileus, bowel hypomotility, constipation, gastric hypomotility, delayed gastric emptying, decreased biliary secretion, decreased pancreatic secretion, biliary spasm, increased sphincter tone, cutaneous flushing, impaction, sweating, inhibition of gastrointestinal motility, inhibition of gastric emptying, gastrointestinal dysfunction, incomplete evacuation, bloating, abdominal distention, increased gastroesophageal reflux, hypotension, bradycardia, irritable bowel syndrome, or immunosuppression.

[0016]In any of the foregoing embodiments, the methylnaltrexone can be present in an amount sufficient to accelerate discharge from hospital post-surgery (including abdominal surgeries such as rectal resection, colectomy, stomach, esophageal, duodenal, appendectomy, hysterectomy, or non-abdominal surgeries such as orthopedic, trauma injuries, thoracic or transplantation), for example, by accelerating bowel sounds after surgery, or speeding the time to first food intake or first bowel movement. In other important embodiments, the amount is sufficient to induce laxation. This has particular application where the subject is a chronic opioid user.

[0037]In any of the foregoing embodiments, the methylnaltrexone can be present in an amount sufficient to accelerate discharge from hospital post-surgery, accelerate bowel sounds after surgery, or induce laxation.

Problems solved by technology

The stability of a pharmaceutical composition in solution, however, is not necessarily predictable either over time when stored at room temperature or when autoclaved.

Surprisingly, it has been discovered that methylnaltrexone is unusually unstable.

Images