Ramelteon sublingual tablet and preparation method thereof

A technology for ramelteon and sublingual tablets, applied in the field of ramelteon sublingual tablets and its preparation, can solve the problems of low drug efficacy, low oral absolute bioavailability, poor content uniformity of low-dose drugs, etc. Achieve high bioavailability, avoid hepatic first-pass effect, and have good taste

Inactive Publication Date: 2019-11-12
HANGZHOU BIO SINCERITY PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to provide a new ramelteon sublingual tablet and the problem of low oral absolute bioavailability and low drug efficacy for drugs with strong first-pass effect and poor content uniformity of low-dose drugs. its preparation method

Method used

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  • Ramelteon sublingual tablet and preparation method thereof
  • Ramelteon sublingual tablet and preparation method thereof
  • Ramelteon sublingual tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Embodiment 1. Ramelteon tablet prescription composition: specification 0.25mg, prescription quantity is 10000 tablets.

[0014] Ramelteon 2.5g Mannitol 956g Crospovidone 40g Magnesium stearate 1g mint flavor 0.5g total 1000g

[0015] Preparation method: Pass ramelteon through a 80-mesh sieve, mannitol, crospovidone and mint essence pass through a 60-mesh sieve; weigh each material in the prescription amount, and set aside; put ramelteon and 1 / 4 prescription amount of manna Alcohol was placed in a ball mill and mixed for 2 hours; the ramelteon-mannitol mixture, the remaining prescription amount of mannitol, crospovidone and peppermint essence were placed in a mixer and mixed evenly; then magnesium stearate was added and mixed evenly; Tablets were compressed on a tablet machine with a 7mm die.

[0016] Comparative Example 1. Ramelteon Tablets Prescription Composition: Specification 0.25 mg, prescription quantity 10,000 tablets....

Embodiment 2

[0025] Example 2. The composition of the prescription of ramelteon tablets: the specification is 0.25 mg, and the prescription quantity is 10,000 tablets.

[0026]

[0027]

[0028] Preparation method: pass ramelteon through a 80-mesh sieve, mannitol, lactose, crospovidone and mint essence pass through a 60-mesh sieve; weigh each material in the prescription amount, and set aside; put ramelteon, mannitol and lactose Grind and mix in a ball mill for 2 hours; put ramelteon-mannitol-lactose mixture, crospovidone and peppermint flavor in a mixer and mix evenly; then add magnesium stearate and mix evenly; Die for tableting.

Embodiment 3

[0029] Example 3. The composition of the prescription of ramelteon tablets: the specification is 0.25 mg, and the prescription quantity is 10,000 tablets.

[0030] Ramelteon 2.5g xylitol 456g sucrose 500g Low-substituted hydroxypropyl cellulose 40g silica 1g Sodium stearyl fumarate 1g mint flavor 0.5g total 1000g

[0031] Preparation method: pass ramelteon through an 80-mesh sieve, sucrose, xylitol, low-substituted hydroxypropyl cellulose and mint flavor through a 60-mesh sieve; weigh each material in the prescription amount, and set aside; put ramelteon, xylose Alcohol and sucrose were ground and mixed in a ball mill for 2 hours; the ramelteon-xylitol-sucrose mixture, low-substituted hydroxypropyl cellulose and mint essence were placed in a mixer and mixed evenly; then silicon dioxide and hard sodium fumarate were added , mix evenly; press on a tablet machine with a 7mm die.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to ramelteon sublingual tablets and a preparation method thereof. The sublingual tablet contains effective amounts of ramelteon, a filler, a disintegrant, a lubricant, and a flavoring agent, and the proportion of a main drug is 0.1 to 0.5%; the filler is selected from one or a combination of mannitol, lactose, sucrose and xylitol; the disintegrant is selected from one or the combination of crospovidone, cross linked sodium carboxymethyl cellulose, and low-substituted hydroxypropyl cellulose; and the lubricant is selected from one or a combination of magnesium stearate, aerosil, and sodium stearyl fumarate; and the flavoring agent is mint flavor. The invention also provides the preparation method of the ramelteonsublingual tablets, that is, ramelteon and the filler are ground and mixed by a ball mill, and mixed with the disintegrating agent, the lubricant, and the flavoring agent, and the materials are pressed to prepare tablets. The ramelteon sublingual tablet of the invention can avoid the first pass effect of the liver and improve the bioavailability.

Description

technical field [0001] The invention relates to a ramelteon sublingual tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Ramelteon (Rozerem) is an oral hypnotic drug developed by Takeda Corporation of Japan, and is the first melatonin receptor agonist to be used and clinically used for the treatment of insomnia. It has high affinity with melatonin receptors MT1 and MT2 receptors, and is specific and fully agonistic to MT1 and MT2 receptors, but does not interact with MT3 receptors. In addition, it does not bind to neurotransmitter receptors such as GABA receptors, and does not interfere with the activities of most enzymes within a certain range. Therefore, it can avoid the distraction associated with GABA drugs (which may cause car accidents, falls, fractures, etc.) and Drug addiction and dependence. Ramelteon has been launched in the United States and Japan in 2005 and 2010 respectively....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/343A61P25/20
CPCA61K9/006A61K9/2027A61K9/2095A61K31/343A61P25/20A61K9/2018A61K9/2059A61K9/2068Y02A50/30
Inventor 陈晓萍沈意康邹永华楼金芳李青青熊卫艳
Owner HANGZHOU BIO SINCERITY PHARMA TECH CO LTD
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