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Ramelteon quick-release sustained-release double-release preparation and preparation method thereof

A ramelteon, dual-release technology, applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve the problems of reduced sleep quality, premature awakening of patients, and short duration of drug efficacy, etc. Achieve the effect of avoiding premature awakening, sufficient sleep time, and high release speed

Active Publication Date: 2021-10-22
海南慧谷药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The traditional ramelteon pharmaceutical preparation releases the drug quickly, which can make the patient fall asleep in a short period of time, but at the same time, the drug effect lasts for a short time, and the patient is prone to wake up prematurely, and cannot fall asleep again after waking up, which reduces sleep quality. Quality, which seriously affects the patient's mental state
[0006] Traditional sustained-release formulations can release drugs continuously over a longer period of time to maintain drug efficacy. However, the slow release rate of sustained-release formulations at the initial stage of release means that the curative effect cannot be rapidly exerted, which is a problem for drugs for the treatment of insomnia. Adverse

Method used

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  • Ramelteon quick-release sustained-release double-release preparation and preparation method thereof
  • Ramelteon quick-release sustained-release double-release preparation and preparation method thereof
  • Ramelteon quick-release sustained-release double-release preparation and preparation method thereof

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preparation example Construction

[0085] The present invention also provides a method for preparing the above-mentioned rapid-release sustained-release double-release preparation of ramelteon, comprising the following steps:

[0086] Take ramelteon, the first filler and the disintegrant and mix for the first time, then add the first lubricant and mix to prepare the immediate release part;

[0087] Take ramelteon, the second filler and the sustained-release material and mix them for the second time, then add the second lubricant and mix to prepare the sustained-release part.

[0088] In a specific example, the immediate-release part and the sustained-release part are used for double-layer compression.

[0089] In a specific example, after the first mixing, the following step is further included: performing wet granulation with ethanol or water.

[0090] In a specific example, after the second mixing, the following step is further included: performing wet granulation with ethanol or water.

Embodiment 1

[0093] This embodiment provides a rapid-release sustained-release dual-release formulation of ramelteon, the specific prescription is as follows

[0094]

[0095] Concrete preparation method is as follows:

[0096] Mix ramelteon, lactose, microcrystalline cellulose PH102, hydroxypropyl methylcellulose K4M, and silicon dioxide evenly. Then add magnesium stearate and mix well, as the sustained release part.

[0097] Mix ramelteon, lactose, microcrystalline cellulose PH102, and croscarmellose sodium evenly. Then add magnesium stearate and mix well, as the immediate release part.

[0098] The sustained-release part and the immediate-release part of ramelteon were compressed into tablets using a double-layer tablet press, and the filling amount of the two parts of granules was adjusted. The sustained-release part was 100 mg, and the immediate-release part was 150 mg, and the double-layer tablet was pressed.

Embodiment 2

[0100] The present embodiment provides a rapid-release sustained-release dual-release preparation of ramelteon, and the specific prescription is as follows:

[0101]

[0102] Concrete preparation method is as follows:

[0103] Mix ramelteon, lactose, microcrystalline cellulose PH102, hydroxypropyl methylcellulose K4M, and silicon dioxide evenly. Then add magnesium stearate and mix well, as the sustained release part.

[0104] Mix ramelteon, lactose, microcrystalline cellulose PH102, and croscarmellose sodium evenly. Then add magnesium stearate and mix well, as the immediate release part.

[0105] The sustained-release part and the immediate-release part of ramelteon were compressed into tablets using a double-layer tablet press, and the filling amount of the two parts of granules was adjusted. The sustained-release part was 125 mg, and the immediate-release part was 125 mg, and the double-layer tablet was pressed.

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Abstract

The invention provides a ramelteon immediate-release sustained-release double-release preparation, comprising an immediate-release part and a sustained-release part; the dosage form of the ramelteon immediate-release sustained-release double-release preparation is a double-layer tablet, granule or capsule wherein, in parts by weight, the immediate-release part includes the following raw materials: 1-30 parts of ramelteon, 20-160 parts of the first filler, 0.5-10 parts of disintegrant , 0.1-5 parts of the first lubricant; in parts by weight, the slow-release part includes the following raw materials: 1-30 parts of ramelteon, 20-160 parts of the second filler, 5 parts Parts ~ 30 parts of slow-release material, 0.2 part ~ 10 parts of the second lubricant; the slow-release material is selected from hypromellose, polyvinylpyrrolidone, hypromellose, sodium alginate, calcium alginate, At least one of guar gum and xanthan gum. The preparation has a higher release rate in the initial stage and can prolong the action time of the drug at the same time.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a rapid-release sustained-release double-release preparation of ramelteon and a preparation method thereof. Background technique [0002] Ramelteon, chemical name is (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl] Propionamide, the English name is Ramelteon, the molecular formula is C 16 h 21 NO 2 , the molecular weight is 259.34, and the chemical structural formula is as follows: [0003] [0004] Ramelteon is a drug for the treatment of insomnia developed by Japan's Takeda Pharmaceutical Company. It is the first melatonin receptor agonist used in the clinical treatment of insomnia. type receptors, but not with melatonin type 3 receptors, and has the characteristics of being potent and highly selective. In addition, ramelteon does not bind to neurotransmitter receptors such as GABA receptors, and does not interfere with the activities of most enzymes within a cer...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/24A61K9/16A61K9/52A61K47/38A61K47/36A61K47/32A61K47/26A61K47/02A61K31/343A61P25/20
CPCA61K9/1611A61K9/1623A61K9/1635A61K9/1652A61K9/2009A61K9/2018A61K9/2027A61K9/205A61K9/2054A61K9/209A61K9/485A61K9/4858A61K9/4866A61K9/5084A61K31/343A61P25/20
Inventor 乔飞解健博周晓飞杨礼荣
Owner 海南慧谷药业有限公司
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