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Safinamide mesylate tablet and preparation method thereof

A safinamide mesylate tablet and prescription technology, which is applied in the field of medicine, can solve problems such as inconsistency with the mechanism of action, toxic impurities, and poor powder fluidity, and achieve simple and easy access to excipients, improved dissolution rate, and low requirements for production equipment Effect

Inactive Publication Date: 2018-09-21
NANJING ZENKOM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN106361711 A discloses safinamide mesylate tablets and a preparation method thereof. The powder is directly pressed into tablets, and the dissolution rate is consistent with that of the original research, but there are defects such as poor powder fluidity, large difference in tablet weight, and easy cracking caused by powder compression; CN105456214 A discloses a safinamide mesylate tablet, which adopts the method of adding glutamic acid in the prescription, so that safinamide has a better curative effect and has a significant positive impact on dissolution and disintegration, but safinamide The mechanism of action of fenamide is to inhibit the release of glutamic acid. The addition of glutamic acid in the present invention does not conform to the mechanism of action, and there is no indication of the difference in curative effect before and after adding glutamic acid; CN 106214653 A discloses a safinamide sustained-release tablet and its Preparation method, according to the description, safinamide in this invention should be safinamide methanesulfonate, wet granulation with ethanol may produce toxic impurities, and there is a safety problem

Method used

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  • Safinamide mesylate tablet and preparation method thereof
  • Safinamide mesylate tablet and preparation method thereof
  • Safinamide mesylate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The preparation of embodiment 1 tablet

[0015]

[0016]

[0017] (1) Weighing the ingredients: Weigh the required raw and auxiliary materials according to the prescription amount, and if there are agglomerates, the raw and auxiliary materials are crushed and sieved through 80 sieves;

[0018] (2) Granulation and granulation: Take the prescribed amount of safinamide mesylate, microcrystalline cellulose, hypromellose and crospovidone (internal addition) and put it in a wet mixing granulator (G20 type) , set stirring at 330rpm, chopping at 2500rpm, stirring and mixing for 240s to obtain a dry-mixed material; set stirring at 220rpm, chopping at 1500rpm, add wetting agent while stirring, finish adding within 30s, and then discharge after stirring for 60s. The material is placed in a GZX-9240MBE electric blast drying oven, the drying temperature is set to 60°C, and the drying is carried out until the moisture content is ≤2.0%, and the material is discharged, and the dr...

Embodiment 2

[0021] The preparation of embodiment 2 tablet

[0022]

[0023]

[0024] (1) Weighing the ingredients: Weigh the required raw and auxiliary materials according to the prescription amount, and if there are agglomerates, the raw and auxiliary materials are crushed and sieved through 80 sieves;

[0025](2) Granulation and granulation: Take the prescribed amount of safinamide mesylate, microcrystalline cellulose, hypromellose and crospovidone (internal addition) and put it in a wet mixing granulator (G20 type) , set stirring at 330rpm, chopping at 2500rpm, stirring and mixing for 240s to obtain a dry-mixed material; set stirring at 220rpm, chopping at 1500rpm, add wetting agent while stirring, finish adding within 30s, and then discharge after stirring for 60s. The material is placed in a GZX-9240MBE electric blast drying oven, the drying temperature is set to 60°C, and the drying is carried out until the moisture content is ≤2.0%, and the material is discharged, and the dry...

Embodiment 3

[0028] Embodiment 3 Dissolution Comparison

[0029] Refer to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations" and the relevant guidelines in the second appendix of the 2010 edition of the Chinese Pharmacopoeia. Dissolution measurement method adopts paddle method, with pH1.0 hydrochloric acid solution 1000ml as standard dissolution medium, rotating speed is 50rpm, under this rotating speed condition, embodiment sample and original research sample are in pH6.8 phosphate buffered saline buffer solution, water, pH1.0 In the four dissolution media of hydrochloric acid solution and pH4.5 acetate buffer, the dissolution behavior was similar.

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Abstract

The invention relates to the technical field of medicines, in particularly to a safinamide mesylate tablet and a preparation method thereof. The safinamide mesylate tablet is prepared from the following components in percent by weight: 31.99% of safinamide mesylate, 46.17% of microcrystalline cellulose (M101), 18.44% of crosslinked povidone (internally added), 1.94% of hydroxypropyl methylcellulose (QBJ-E50), 18.44% of crosslinked povidone (externally added), 3.88% of silicon dioxide, 0.49% of magnesium stearate and 2.91% of a film coating premix. The invention further discloses the preparation method of the safinamide mesylate tablet. Wet granulation is adopted, the technical process is stable and mature, equipment is simple, suitability for industrial mass production is achieved, and thedissolution is relatively high.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a safinamide mesylate tablet and a preparation method thereof, which can be used for treating diseases related to Parkinson's disease. Background technique [0002] Safinamide mesylate is jointly developed by Newron, a pharmaceutical company dedicated to developing drugs for central nervous system diseases, and its marketing partner Zambon. Safinamide mesylate is a compound blocker of sodium channel and calcium channel, which inhibits the stimulated release of glutamate, and is also a selective MAO-B inhibitor, which can selectively affect neurons with abnormal discharge without changing the normal activity of neurons. Chemical name: (S)-2-[[4-[(3-fluorobenzyl)oxy]benzyl]amino]propanamide methanesulfonate, the structure is as follows: [0003] [0004] Safinamide mesylate has two advantages over its competitors. First, it is highly specific for MAO-B, so it can limit or el...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/165A61K47/32A61P25/16
CPCA61K9/2866A61K9/2027A61K31/165A61P25/16
Inventor 祁艳徐卓业
Owner NANJING ZENKOM PHARMA
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