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Pharmaceutical composition for the treatment of acute disorders

a technology for acute disorders and pharmaceutical compositions, applied in the direction of drug compositions, immunological disorders, metabolism disorders, etc., can solve the problems of many pharmaceutically active agents, long onset times of rectal or sublingual formulations, and inability to control acute disorders

Inactive Publication Date: 2004-10-28
OREXO AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009] It is one object of the invention to provide for the treatment of acute disorders by perorally administering at least one pharmaceutically active agent in a manner giving rise to pharmacologically effective plasma levels of said agent or agents within a short time after administration.

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.

Method used

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  • Pharmaceutical composition for the treatment of acute disorders

Examples

Experimental program
Comparison scheme
Effect test

example 2

Preparation of a Rapidly Disintegrating Tablet with Bio / Mucoadhesion Promoting Properties

[0059] A batch of 1000 tablets was produced from the following composition: 91.0 g of mannitol (granular quality of a particle size from 250 to 450 .mu.m) and 1.0 g of sodium lauryl sulfate and 500 mg of micronized fentanyl were mixed in a V-mixer over a period of 24 hours. Thereafter, 5.0 g of Avicel.RTM. PH101 and 2.0 g of Ac-Di-Sol.RTM. (here used both as a disintegrant and as a bio / mucoadhesion promoting agent) was admixed for an additional 2 hours. Finally, 0.5 g of magnesium stearate was admixed for 2 minutes. The resulting tablet mass was compacted into tablets at a compaction pressure of 130 Mpa, each tablet containing 0.5 mg of fentanyl.

[0060] The disintegration time was tested with the use of the apparatus described in Ph.Eur. (latest edition)

[0061] It was found that the disintegration time was less than 15 seconds.

[0062] For comparison, conventional rapidly dissolving tablets were als...

example 3

Evaluation of Uptake in Sublingual Administration

[0064] To one patient suffering from breakthrough pain due to cancer was administered 400 .mu.g of fentanyl as a sublingual tablet formulated as described in Examole 1. The plasma concentration of fentanyl was monitored for a time of 240 minutes after the administration, and the results are shown in the accompanying figure. It will be seen that the uptake of fentanyl was rapid, with the maximum value attained already after 5 minutes. This shows that a sublingual preparation according to the invention gives a rapid uptake of the active agent, even though a very small volume of liquid is available for dissolution in this route of administration.

example 4

Evaluation of Bio / Mucoadhesive Properties

[0065] For in vitro evaluation of the bio / mucoadhesive properties of the formulation according to the present invention, a method permitting evaluation of bio / mucoadhesion promoting properties directly on finished dosage forms (Sala, G. E. et al., Proc. Int. Symp. Contr. Release Bioact. Mat. 16:420, 1989) was used. The evaluation was based on measurements of the flow of water required to remove the active substance from a rabbit intestinal membrane. A strip of rabbit mucosa was placed horizontally in a suitable temperature controlled chamber set at 37.degree. C. The tissue was first washed with predetermined volumes of water by means of a peristaltic pump. Pre-compressed compositions according to Example 1 (5-15 mg) were then placed on the tissue and allowed to remain there for 2 minutes to ensure proper dissolution. Upon this followed an elution with water fed by a peristaltic pump during 10 minutes. Rinsed-off fentanyl was collected, and it...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/46A61K9/00A61K9/16A61K31/445A61K31/4468A61K38/12A61K38/22A61K47/20A61K47/24A61K47/26A61K47/28A61K47/32A61K47/34A61K47/36A61K47/38A61P25/04A61P43/00
CPCA61K9/0056A61K9/006A61K9/2866A61K31/19A61K38/00A61K31/44A61K31/445A61K31/4468A61K38/2242A61K31/34A61K9/145A61K9/2018A61K9/2054A61K31/136A61K31/341A61K31/4745A61K31/4985A61K31/5415A61K31/5513A61K36/84A61P11/00A61P25/04A61P25/20A61P29/00A61P3/00A61P37/00A61P43/00A61P7/00A61P7/10A61P9/00A61K9/16A61K31/485A61K9/146A61K31/196A61K31/4439A61K31/635
Inventor PETTERSSON, ANDERSNYSTROM, CHRISTER
Owner OREXO AB
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