Nasal administered preparation of melatonin

A technology for nasal administration preparations and melatonin, which is applied in the directions of antidote, drug combination, drug delivery, etc., can solve problems such as side reactions of nasal mucosa, and achieve the effect of no special odor.

Inactive Publication Date: 2010-05-26
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Another prescription composition in this patent uses propylene glycol to solubilize, but propylene glycol also has serious side effects on the nasal mucosa

Method used

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  • Nasal administered preparation of melatonin
  • Nasal administered preparation of melatonin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 melatonin nasal spray (15mg melatonin / ml)

[0023] Melatonin 1.5g

[0024] PEG400 15ml

[0025] EDTA-2Na 0.01g

[0026] Sodium bisulfite 0.15g

[0027] Ethyl p-hydroxybenzoate 0.1g

[0028] Sodium chloride 0.9g

[0029] Add water for injection to 100ml

[0030] The clear yellow solution prepared according to the above prescription was divided into quantitative spray pumps to obtain nasal spray T1.

[0031] Also referring to PCT patent WO98 / 42333, the following prescription is designed:

[0032] Melatonin 1.5g

[0033] Hydroxypropyl Beta Cyclodextrin 13g

[0034] EDTA-2Na 0.01g

[0035] Vitamin C 0.2g

[0036] Benzalkonium Chloride 0.1g

[0037] Sodium chloride 0.9g

[0038] Add water for injection to 100ml

[0039] The clear yellow solution prepared according to the above prescription was divided into quantitative spray pumps to obtain nasal spray T2.

[0040] Another 3 mg / ml melatonin intravenous injection preparation R was prepared. Take 6 ...

Embodiment 2

[0048] Example 2 Melatonin nasal powder

[0049] Melatonin 1.5g

[0050] Lactose 30g

[0051] Sodium bisulfite 0.15g

[0052] Distilled water to 100ml

[0053] Add the above-mentioned melatonin and lactose into 100ml of distilled water, stir until completely dissolved, freeze-dry at -35°C overnight, then freeze-dry at -10°C and 0°C for 24 hours, pass through a 100-mesh sieve for nasal inhalation.

Embodiment 3

[0054] Embodiment 3 melatonin microsphere preparation

[0055] Melatonin 1.5g

[0056] Span 80 1.0g

[0057] Gelatin 6.0g

[0058] Medicinal castor oil 100ml

[0059] Toluene solution of saturated glutaraldehyde Appropriate amount

[0060] Take the above gelatin and dissolve it in 30ml of 55°C water, add melatonin to dissolve it. Separately take medicinal castor oil and emulsifier Span80 in a dry beaker, place the beaker in a water bath at 50°C, and slowly add it into the gelatin solution containing the drug under stirring at a stirring speed of 1000 rpm. After stirring for 10 min, a saturated toluene solution of glutaraldehyde was added, stirring was continued for 2 h, and the mixture was washed with n-hexane:isopropanol (1:1). The microspheres obtained by centrifugation were washed with ether, dried, sieved and packaged for use.

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Abstract

The invention relates to a nasal administration preparation comprising melatonin and at least one kind of polyethylene glycol selected from polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, or polyethylene glycol 600.

Description

technical field [0001] The present invention relates to a melatonin-containing nasal administration preparation, which comprises melatonin and at least one of polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 600 polyethylene glycol. Background technique [0002] Melatonin is an indole hormone secreted by the human pineal gland, which has the functions of promoting sleep, delaying aging, enhancing immunity and anti-tumor. As a new type of hypnotic, melatonin has its unique advantages: (1) It has a relatively ideal hypnotic effect at a small dose (0.1-0.3 mg); (2) melatonin is an endogenous The substance works by regulating the endocrine system. It is not a foreign body to the body and has its own metabolic pathway in the body, which will not cause the accumulation of the parent drug and its metabolites in the body; (3) The biological half-life of melatonin is short , after a few hours of oral administration, it will drop to the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/34A61K47/42A61K31/4045A61P25/20A61P35/00A61P37/04A61P39/06
Inventor 梅兴国曹树贵
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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