Pharmaceutical compositions of ramelteon and methods of use thereof

A technology of ramelteon and composition, applied in the field of ramelteon pharmaceutical composition for the treatment of insomnia and jet lag syndrome

Inactive Publication Date: 2020-04-10
MAXINASE LIFE SCI LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Another safety concern with oral ramelteon is the active M-II metabolite after hydroxylation

Method used

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  • Pharmaceutical compositions of ramelteon and methods of use thereof
  • Pharmaceutical compositions of ramelteon and methods of use thereof
  • Pharmaceutical compositions of ramelteon and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] ramelteon nasal spray

[0025]In one exemplary composition of the present invention, a nasal composition is prepared using a solubilizing agent such as propylene glycol and sulfobutyl ether-beta-cyclodextrin (SBE-CD). First, 5 g of ramelteon was completely dissolved in 150 mL of propylene glycol, then this solution was gradually added to 5 mL of SBE solution (52%, w / v) containing EDTA.2Na and benzalkonium chloride, and finally an appropriate amount of purified water was added to 1L.

[0026]

[0027] After preparation, the drug solution was filtered through a 0.22 μm filter membrane, and then filled into a glass bottle equipped with a metered dose spray pump for intranasal administration at a volume of 0.10 ml per spray. Each spray will deliver 0.5 mg ramelteon intranasally.

Embodiment 2

[0029] ramelteon sublingual tablet

[0030] Ramelteon sublingual tablets are prepared by two different methods: direct compression and wet granulation. For direct compression, ramelteon is mixed with excipients. The physical mixture was directly compressed with a single punch tablet press (Shanghai Tianfan Pharmaceutical Machinery Factory, model 6A). Wet granulation methods are listed below:

[0031] 1. Weigh the ingredients according to the recipe.

[0032] 2. Dissolve ramelteon and HP-β-cyclodextrin in ethanol under stirring.

[0033] 3. Mix ramelteon-cyclodextrin solution with CL-SF was mixed for granulation. Pass the wet material through a 40 mesh screen.

[0034] 4. Drying: The wet granules were dried in an oven at 60° C. for 120 minutes.

[0035] 5. Dry sieving: The dry granules were ground and sieved through a 60-mesh sieve.

[0036] 6. Final mixing: the extragranular ingredients ( EASYtab SP and magnesium stearate) are added to the dry granules. The final g...

Embodiment 3

[0040] Dissolution test of ramelteon sublingual tablet

[0041] Dissolution tests were performed according to USP 36 / NF 31 Dissolution Test Apparatus II (paddle method) using a dissolution tester (TIANDA TIANFA - Manufacturer of Pharmaceutical Testing Instruments, ZRS-8L). At 37°C, 100 mL of purified water was used as the dissolution medium. The paddle speed was maintained at 50 rpm. 2 mL aliquots were withdrawn at regular intervals and the sample volume was replaced with an equal volume of purified water. Dissolution samples were analyzed by HPLC. The dissolution profiles of ramelteon tablets prepared by direct compression and wet granulation were as follows: figure 1 As shown, the dissolution rate of the wet granulation tablet was faster than that of the tablet prepared by direct compression.

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Abstract

Pharmaceutical compositions of ramelteon for use in the treatment of insomnia or jet lag by transmucosal administration. More specifically, the pharmaceutical composition is formulated into nasal spray or nasal drop for intranasal administration, or formulated into sublingual spray for sublingual administration, or formulated into a solid dosage for sublingual administration.

Description

technical field [0001] The present invention relates to a pharmaceutical composition of ramelteon and a method of use thereof. More specifically, the present invention relates to pharmaceutical compositions of ramelteon for the treatment of insomnia and jet lag by transmucosal administration. The present invention achieves a faster onset of pharmacological action by delivering low doses of ramelteon via intranasal or sublingual routes compared to conventional oral tablet administration. Background technique [0002] About 30% to 40% of the population suffers from mild to severe insomnia. Insomnia can cause impairments in physical and mental health, such as fatigue and reduced alertness, irritability and inability to concentrate, increasing the risk of accidents and reducing productivity. All of these symptoms have a negative impact on quality of life. Appropriate treatment of insomnia includes lifestyle changes, sleep hygiene, and pharmacological intervention with sedativ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61K9/00A61K9/08A61K9/10A61K9/20A61K9/70A61P25/20A61P25/00
CPCA61K9/08A61K9/10A61K31/343A61P25/00A61P25/20A61K9/0043A61K9/0056A61K47/10A61K9/006A61K47/14A61K9/008A61K47/186A61K47/20A61K9/205A61M11/007A61K47/12A61K47/183A61K47/32A61K47/38A61K47/40A61M31/00A61M2210/0618A61M2210/0643A61K9/0073A61K9/20A61K9/50A61K9/51A61K9/70
Inventor 王雁峰许梁陈娟李德晃
Owner MAXINASE LIFE SCI LTD
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