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CN-122005480-A - Meloxepin besylate tablet and preparation method thereof

CN122005480ACN 122005480 ACN122005480 ACN 122005480ACN-122005480-A

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and discloses a methoprene besylate tablet and a preparation method thereof. The methoprene besylate tablet comprises a drug tablet core and a coating layer, wherein the drug tablet core comprises, by weight, 4-10 parts of methoprene besylate, 60-120 parts of a filler, 10-20 parts of a disintegrant, 0.5-1.0 parts of an adsorbent and 1.0-2.0 parts of a lubricant. The invention does not add antioxidant, adopts the powder direct tabletting technology, adopts the step gradient mixing and the forced sieving treatment mode to ensure good mixing uniformity of the preparation, simultaneously avoids the unstable risk of the preparation possibly caused by the conventional granulating technology, simplifies the preparation technology and ensures the stable quality of the tablet. The prepared sulbactam besylate tablet has good in vitro dissolution similarity with a reference preparation and is bioequivalent in vivo.

Inventors

  • LIU RUI
  • Wei Jichun
  • SONG QIAN
  • LIU AIJU
  • SHEN JUAN
  • CHEN YUNXIA
  • WANG LI
  • ZHANG NING

Assignees

  • 山东鲁抗医药股份有限公司

Dates

Publication Date
20260512
Application Date
20260318

Claims (10)

  1. 1. The methoprene besylate tablet is characterized by comprising a drug tablet core and a coating layer; The medicine tablet core comprises, by weight, 4-10 parts of melagatran besylate, 60-120 parts of filler, 10-20 parts of disintegrating agent, 0.5-1.0 parts of adsorbent and 1.0-2.0 parts of lubricant.
  2. 2. The methoprene besylate tablet according to claim 1 wherein the particle size of the methoprene besylate is d90:50-200 μm.
  3. 3. A methoprene besylate tablet according to claim 1 wherein the filler is selected from at least one of lactose, starch, mannitol, sorbitol.
  4. 4. The methoprene besylate tablet according to claim 1 wherein the filler is mannitol having a particle size of from 100 to 300 μm.
  5. 5. The methoprene besylate tablet according to claim 1 wherein the disintegrant is selected from at least one of calcium carboxymethyl cellulose, sodium carboxymethyl starch, low substituted hydroxypropyl cellulose, croscarmellose sodium, crospovidone.
  6. 6. A methoprene besylate tablet according to claim 1 wherein the adsorbent is selected from at least one of magnesium aluminum metasilicate, calcium silicate, magnesium silicate.
  7. 7. A methoprene besylate tablet according to claim 1 wherein the lubricant is selected from at least one of magnesium stearate, sodium stearyl fumarate, talc, silica.
  8. 8. The methoprene besylate tablet according to claim 1 wherein the coating layer is a gastric-soluble coating premix comprising, by weight, 3-8 parts of gastric-soluble coating material and 25-100 parts of coating solvent; The coating solvent is water, ethanol or a mixture of water and ethanol.
  9. 9. A process for the preparation of a methoprene besylate tablet according to any of claims 1 to 8 comprising the steps of: s1, pretreatment, namely respectively sieving the bulk drugs and the filler; s2, premixing, namely carrying out multi-step gradient mixing and forced sieving on the sieved bulk drug and the filling agent, and then mixing with the disintegrating agent and the adsorbent to obtain a premixed mixture; s3, mixing the premixed mixture with a lubricant to obtain total mixed powder; s4, tabletting, namely tabletting the total mixed powder, controlling the tablet hardness to be 4-10kg, and obtaining a plain tablet; s5, coating, namely coating the plain tablets by adopting a gastric-soluble coating premix to obtain the melongena barlin besylate tablets.
  10. 10. The method for preparing a tablet of methoprene besylate according to claim 9 wherein the specific mode of operation of step S2 comprises: 1) Placing part of the screened filler and the melagatran besylate into a mixer to be primarily mixed for 3-10 min, forcibly screening after the mixing is finished to obtain a mixture, and flushing a screen with part of the filler; 2) Continuously mixing the mixture and the filler after washing the screen for 3-10 min to obtain mixed powder; 3) Mixing the mixed powder with the rest of filler, the disintegrating agent and the adsorbent for 10-30 min to obtain a premixed mixture.

Description

Meloxepin besylate tablet and preparation method thereof Technical Field The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a sulbactam besylate tablet and a preparation method thereof. Background Melabalin besylate (Mirogabalin Besilate) is a white to yellowish powder with the chemical name [ (1R, 5S, 6S) -6- (aminomethyl) -3-ethylbicyclo [3.2.0] hept-3-en-6-yl ] acetic acid monobenzenesulfonate. The meloidogyne besylate is a novel chronic pain therapeutic drug, and can play an auxiliary role in the function of potential dependent calcium channels in the nervous system, inhibit calcium current and play an analgesic role by combining with Voltage Gate Calcium Channel (VGCC) subunit alpha 2 delta (CACNA 2D). Tarlige (mevalonate tablet) developed by the first co-product of japan (Daiichi Sankyo Company Limited) was first marketed in japan at 2019.01.08 for the treatment of Peripheral Neuropathic Pain (PNP). However, the tablet stability of the original ground product is dependent on the antioxidant and packaging requirements in the prescription, the production cost is high, and no report has been made on the influence of no antioxidant added on the methoxsulfonic acid methoxsalen tablet. Therefore, how to provide an antioxidant-independent methoprene besylate tablet and a preparation method thereof is a technical problem to be solved by the person skilled in the art. Disclosure of Invention In order to overcome the defects and shortcomings in the prior art, the invention provides a melongena besylate tablet and a preparation method thereof. The invention does not add antioxidant, adopts the powder direct tabletting technology, adopts the step gradient mixing and the forced sieving treatment mode to ensure good mixing uniformity of the preparation, simultaneously avoids the unstable risk of the preparation possibly caused by the conventional granulating technology, simplifies the preparation technology and ensures the stable quality of the tablet. The prepared sulbactam besylate tablet has good in vitro dissolution similarity with a reference preparation and is bioequivalent in vivo. In order to achieve the above purpose, the present invention adopts the following technical scheme: A sulbactam besylate tablet, comprising a drug tablet core and a coating layer; The medicine tablet core comprises, by weight, 4-10 parts of melagatran besylate, 60-120 parts of filler, 10-20 parts of disintegrating agent, 0.5-1.0 parts of adsorbent and 1.0-2.0 parts of lubricant. Preferably, the particle size of the sulbactam besylate is D90:50-200 mu m. Preferably, the filler is at least one selected from lactose, starch, mannitol and sorbitol. Preferably, the filler is mannitol, and the granularity is D90:100-300 mu m. Preferably, the disintegrating agent is at least one selected from the group consisting of calcium carboxymethyl cellulose, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, croscarmellose sodium, and crospovidone. Preferably, the adsorbent is at least one selected from the group consisting of magnesium aluminum metasilicate, calcium silicate and magnesium silicate. Preferably, the lubricant is at least one selected from magnesium stearate, sodium stearyl fumarate, talcum powder and silicon dioxide. Preferably, the coating layer is a gastric-soluble coating premix and comprises the following raw materials, by weight, 3-8 parts of gastric-soluble coating materials and 25-100 parts of coating solvents; The coating solvent is water, ethanol or a mixture of water and ethanol. Preferably, the mass of the coating layer is 3-5% of the mass of the drug tablet core. The invention also provides a preparation method of the methoprene besylate tablets, which comprises the following steps: s1, pretreatment, namely respectively sieving the bulk drugs and the filler; s2, premixing, namely carrying out multi-step gradient mixing and forced sieving on the sieved bulk drug and the filling agent, and then mixing with the disintegrating agent and the adsorbent to obtain a premixed mixture; s3, mixing the premixed mixture with a lubricant to obtain total mixed powder; s4, tabletting, namely tabletting the total mixed powder, controlling the tablet hardness to be 4-10kg, and obtaining a plain tablet; s5, coating, namely coating the plain tablets by adopting a gastric-soluble coating premix to obtain the melongena barlin besylate tablets. Preferably, the specific operation manner of step S2 includes: 1) Placing part of the screened filler and the melagatran besylate into a mixer to be primarily mixed for 3-10 min, forcibly screening after the mixing is finished to obtain a mixture, and flushing a screen with part of the filler; 2) Continuously mixing the mixture and the filler after washing the screen for 3-10 min to obtain mixed powder; 3) Mixing the mixed powder with the rest of filler, the disintegrating agent and the adsorbent for 10-30 min to obtain a premixed