Pharmaceutical composition for the treatment of acute disorders

Abstract

A pharmaceutical composition for the treatment of acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and / or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.

Description

[0001] The present invention relates to a rapidly acting pharmaceutical composition for sublingual administration of a pharmaceutical agent, to a method for preparing such a composition, and to a method for the treatment of acute disorders by the use of such a composition.[0002] Acute and / or severe disorders are a common cause of emergency treatment or hospitalization. One of the most common disorders of this type is acute or breakthrough pain. In cancer patients, pain is usually treated with non-steroid anti-inflammatory drugs (NSAIDs) and opiates alone or in combination. Opioid-requiring cancer pain patients are usually given slow-release opiates (slow-release morphine or ketobernidone or transdermal fentanyl). A characteristic feature of cancer pain are periods of inadequate analgesia (breakthrough pain). Most often they are due to increased physical activity of the patient. However, treatment of breakthrough pain by administration of increased time contingent doses of long-actin...

AI Technical Summary

Benefits of technology

The composition achieves rapid pharmacologically effective plasma levels with reduced side effects and variability, enabling quick relief for acute disorders without excessive drug accumulation, suitable for repeated dosing and administration of poorly soluble agents.

Problems solved by technology

However, treatment of breakthrough pain by administration of increased time contingent doses of long-acting analgesics causes adverse side effects such an excess sedation, nausea, and constipation.

Presently available oral, rectal, or sublingual formulations have relatively lengthy onset times or erratic absorption characteristics that are not well suited to control acute disorders.

However, many pharmaceutically active agents which would be advantageous to adminster orally are not suitable to be swallowed.

They may, for example, be inactivated by the gastro-intestinal liquids, have a slow action because of a low solubility in the aqueous medium, or be highly susceptible to metabolism by gastrointestinal enzymes and have poor absorptiom properties, as exemplified for peptide hormones.

However, with this way of administration, the risk that the patient swallows the medication by swallowing saliva is well known.

However, compared to these opiates, fentanyl exhibits little hypnotic activity, rarely induces histamine release, and respiratory depression is more short-lived.

In addition, substantial amounts of lozenge-administered fentanyl are swallowed by the patient.

This is not desirable and results in the administration of excessive amounts of the drug, which may give rise to side effects.

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