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Pharmaceutical formulation comprising melatonin

A technology of melatonin and pharmaceutical preparations, applied in the field of pharmaceutical preparations containing melatonin and such sleeping pills, capable of solving problems such as poor efficacy, uncomfortable therapeutic application, and poor tolerance of melatonin

Inactive Publication Date: 2005-07-27
NEURIM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] Suhner et al. reported in Aviat.Space Environ.Med.72:638 (2001) that co-administration of zolpidem 10 mg with normal-release melatonin 5 mg was more effective than zolpidem alone for jet lag. Less potent and less well tolerated than melatonin
This co-administration causes various side effects such as nausea, vomiting, amnesia, and sleepwalking to the point of incapacity, suggesting that co-administration of zolpidem and melatonin is useful in the treatment of conditions involving circadian rhythms such as insomnia May not be suitable for practical therapeutic applications

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] method The pharmacokinetics of melatonin (2 mg sustained release formulation), zolpidem (10 mg) and their combinations were evaluated with 16 volunteers (12 males and 4 females). The average age of the recruited individuals was 59.4 years (SD 3.2) and the average body mass index was 25.5 kg / m 2 (SD 2.3), mean body weight was 75.8 kg (SD 11.8) and mean height was 171.8 cm (SD 7.7). In a randomized double-blind crossover study, subjects were given a placebo tablet in the evening to establish a baseline, and then given a melatonin tablet, zolpidem, or a combination dose or placebo (only one tablet) in the evening in a randomized manner. night), with a one-week washout period between these treatments.

[0045] Blood samples were drawn from the individuals at preselected intervals after administration of the tablets.

[0046] result .The pharmacokinetic parameters of the two drugs when administered alone and in combination are listed in Table 1:

[0047] dru...

Embodiment 2

[0050] method . Psychomotor skills and driving behavior were assessed with 16 volunteers (12 males and 4 females) on melatonin (2 mg extended release formulation), zolpidem (10 mg), their combination and placebo. The mean age of the recruited individuals was 59.4 years (SD 3.2) and the mean body mass index was 25.5 kg / m 2 (SD 2.3), mean body weight was 75.8 kg (SD 11.8) and mean height was 171.8 cm (SD 7.7).

[0051] In a randomized double-blind crossover study, subjects were given a placebo tablet in the evening to establish a baseline, and then were randomized to receive a tablet of melatonin, zolpidem, a combination thereof, or placebo in the evening, each treatment There was a week without treatment in between. Patients were administered a battery of behavioral and driving skills tests at preselected intervals following the administration of the tablet. These tests include psychomotor work, alertness, and coordination for reaction testing: ARCI 49, GroovedPegboard, Rive...

Embodiment 3

[0067] In this example, a bilayer tablet was prepared with sustained release of melatonin (inner core) but regular release of a sleeping drug (eg zolpidem) (outer layer). Because the outer layer dissolves directly in the intestinal system, the properties of the zolpidem produced will be similar to those given in Example 1, while the properties of the melatonin produced in the blood will be similar because the core will gradually dissolve. The properties will also be similar to those of Example 1.

[0068] method. First, by mixing the following ingredients, namely, melatonin (2 mg / tablet), Eudragit RSPO acrylic resin carrier (Rohm Pharma), lactose, and calcium hydrogen phosphate in a weight ratio of about 2:1:2.5 and using 2.5 tons of force The mixture was compressed in a 7mm punch to prepare sustained-release melatonin cores.

[0069] Then, suspend acrylic resin (Eudragit RD 100), polysorbate 80 and talc and zolpidem tartrate (5 mg / tablet) in a weight ratio of approximately...

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Abstract

Short-term potentiation of non-barbiturate and non-benzodiazepine hypnotics is effected by use of melatonin.

Description

technical field [0001] The present invention relates to the use of melatonin for the preparation of a medicament for short-term reinforcement of certain hypnotics and pharmaceutical preparations comprising melatonin and such hypnotics. Background technique [0002] Gamma-aminobutyric acid (GABA), acting through GABA-A receptors, is the major inhibitory neurotransmitter system of the brain and plays an important role in regulating brain excitability. The GABA-A receptor includes five subunits. The distinct protein subunits that make up receptors for the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) have been identified and constitute the alpha, beta, gamma, and delta families, with some subtypes present in each group. The subunit composition of a receptor, especially its α-subunit content, determines its pharmacological properties. Many drugs interact with the binding sites of different subunits of the GABA-A receptor, and these drugs inclu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/32A61K9/24A61K31/4045A61K31/437A61K31/496A61K31/4985A61K45/00A61P25/20
CPCA61K31/496A61K31/4045A61K31/4985A61K9/209A61K31/437A61P25/00A61P25/20A61K2300/00A61K9/14
Inventor N·齐萨佩尔
Owner NEURIM PHARMA
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