Pharmaceutical formulations useful in the treatment of insomnia

a technology of pharmaceutical formulations and insomnia, applied in the direction of drug compositions, biocide, heterocyclic compound active ingredients, etc., can solve the problems of function of normal people, affecting the quality of life of people, adverse personal, medical or psychiatric effects, and inability to sleep normally

Inactive Publication Date: 2011-11-03
OREXO AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0022]Thus, as formulations according to the present invention consistently provide measurable plasma concentrations of drug within 10 minutes they are effectively capable of providing for consistent “on demand” sleep induction.

Problems solved by technology

Furthermore, more than 90% of the total population have trouble with sleep at some point during their lives.
Inadequate sleep impairs quality of life and ability to function normally in a general sense.
It often results in adverse personal, medical or psychiatric consequences, in addition to increasing the risk of accidents.
The practitioner also needs to be aware of the potential for undesirable absorption of drug taking place several hours after administration, which may give rise to decreased alertness and impaired psychomotor function during normal activity the following day.
In view of this, onset of action can be delayed in many patients, leading to a frustrating lack of “on demand” sleep, in addition, in many cases, to undesirable residual effects (such as those mentioned hereinbefore) the following day.
In the treatment of insomnia with a short acting hypnotic agent such as zolpidem, such an enhanced rate of absorption might be expected to give rise to potential safety problems in patients that are sensitive to the drug, potentially giving rise to undesirable pharmacological effects, such as a more rapid onset of sleep than is convenient (e.g. when preparing for sleep; see, for example col.

Method used

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  • Pharmaceutical formulations useful in the treatment of insomnia

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Sublingual Tablets

[0080]Sublingual tablets comprising 5 mg and 10 mg of zolpidem hemitartrate were prepared as follows.

[0081]Zolpidem hemitartrate (Boehringer Ingelheim, Germany) was firstly ground for 20 minutes in a ball mill.

[0082]The active ingredient was then accurately weighed out, along with the other excipients (see below), in appropriate proportions that would enable the production of tablets with the absolute amounts of various ingredients mentioned below.

[0083]Pre-weighed quantities of zolpidem hemitartrate and mannitol (Parteck M200; Merck, Germany) were then mixed in a Turbula mixer for 96 hours. Then, pre-weighed quantities of silicified microcrystalline cellulose (ProSolv®; JRS Pharma, Germany), sodium carboxymethylcellulose (Croscarmellose Sodium NF; Ac-Di-Sol®; FMC Corp., USA), Neohesperidin DC (Exquim, Spain) and peppermint powder (Firmenich, Germany) were added and mixing was continued for 30 minutes. Finally, a pre-weighed quantity of magnesium ste...

example 2

Clinical Study

[0087]An open randomized three-period crossover single-centre study was devised to evaluate the pharmacokinetic profile of the sublingual zolpidem 5 mg and 10 mg tablets prepared by way of Example 1 above, as compared to a peroral zolpidem formulation (Stilnoct® 10 mg; Sanofi-Synthélabo, France).

[0088]The trial was a pharmacokinetic study in healthy male and female volunteers to test for dose proportionality as between the two sublingual tablet formulations. The pharmacokinetic profiles were evaluated, focussing on bioavailability and time and rate of absorption. The study also included a subjective assessment of efficacy, i.e. the subjects' perceived degree of sedation.

[0089]18 healthy subjects aged between 18 and 40 were used in this study. Signed informed consents were obtained in all cases.

[0090]Each of the three formulations were given to each of the 18 volunteers, in a random order, at three visits to the study centre (hereinafter “Visits 1, 2 and 3”). Visits 1 a...

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Abstract

There is provided a formulation suitable for transmucosal administration comprising a short acting hypnotic drug, which formulation provides a measurable plasma concentration of drug within 10 minutes of administration. The formulation is capable of providing sleep on demand, and preferably comprises particles of drug, for example zolpidem or a pharmaceutically-acceptable salt thereof and a mucoadhesion promoting agent, such as sodium carboxymethylcellulose, which particles of drug and mucoadhesive are presented upon the surface of larger carrier particles.

Description

RELATED APPLICATIONS[0001]This application is a divisional of co-pending U.S. patent application Ser. No. 11 / 666,361 filed 11 Feb. 2008, which is the U.S. National Phase of PCT / GB2005 / 004147 filed 26 Oct. 2005.BACKGROUND OF THE INVENTION[0002]This invention relates to new, fast acting pharmaceutical formulations comprising short acting hypnotic agents that are useful in the short-term treatment of insomnia, such as transient insomnia.[0003]Insomnia is a common disorder characterised by difficulty in the initiation and / or maintenance of sleep. Insomnia periodically affects 30% of adults. Furthermore, more than 90% of the total population have trouble with sleep at some point during their lives.[0004]Inadequate sleep impairs quality of life and ability to function normally in a general sense. It often results in adverse personal, medical or psychiatric consequences, in addition to increasing the risk of accidents.[0005]The disorder can be transient or chronic. Although isolated incide...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/437A61P25/20A61K9/20A61K9/00A61K31/44
CPCA61K9/0002A61K31/44A61P25/00A61P25/20
Inventor PETTERSSON, ANDERSNYSTROM, CHRISTERBREDENBERG, SUSANNE
Owner OREXO AB
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