Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Asenapine maleate sublingual tablet and preparation method thereof

A technology of asenapine maleate and sublingual tablet is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, medical preparations containing active ingredients, etc. The high friability of the process and the reduction of production costs can achieve the effect of avoiding oral sandy feeling, rapid dissolution and wide application.

Inactive Publication Date: 2019-02-15
天津仁生医药科技有限公司
View PDF10 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN 1079670C discloses a rapidly disintegrating sublingual tablet containing medicinal water-soluble or water-dispersible carrier material prepared by freeze-drying process and its preparation method, through sublingual administration, avoiding its oral administration side effects of drugs; freeze-drying technology, although rapid disintegration of preparations can be obtained, but the friability of the product is relatively poor, and increases the production cycle and production costs
[0006] CN103893139B discloses a method for preparing rapidly disintegrating asenapine maleate sublingual tablets by using an easily sublimable porogen, which reduces production costs and improves the brittleness of the freeze-drying process to a certain extent high degree of problem
Porogen sublimation technology, the product obtained is also a loose structure, so it also has a certain impact on the friability, and the preparation process needs to go through high temperature to sublimate the porogen, resulting in the increase of related substances

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Asenapine maleate sublingual tablet and preparation method thereof
  • Asenapine maleate sublingual tablet and preparation method thereof
  • Asenapine maleate sublingual tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] prescription

[0057]

[0058] craft

[0059] 1. Dissolve BHT, povidone and asenapine maleate in methanol;

[0060] 2. Mannitol and low-substituted hydroxypropyl cellulose are passed through a 30-mesh sieve and collected in bags;

[0061] 3. Top-spray the solution of step 1 on the mixed powder 2 with a fluidized bed;

[0062] 4. After spraying, dry until the LOD does not exceed 2.5%;

[0063] 5. Sizing the dry granules with a 35-mesh sieve;

[0064] 6. Mix the sized granules with low-substituted hydroxypropyl cellulose passing through a 30-mesh sieve (10rpm 15min);

[0065] 7. Sodium stearyl fumarate is passed through a 50-mesh sieve, and mixed with step 6 (10rpm 5min);

[0066] 8. Press the tablet with a φ8mm punch.

Embodiment 2

[0068] Prescription is the same as "embodiment 1"

[0069] craft

[0070] 1. Dissolve BHT, povidone and asenapine maleate in methanol;

[0071]2. Mannitol and low-substituted hydroxypropyl cellulose are passed through a 30-mesh sieve and collected in bags;

[0072] 3. Use the wet granulator to add the solution in step 1 to the mixed powder 2 to granulate;

[0073] 4. After granulation, dry until the LOD does not exceed 2.5%;

[0074] 5. Sizing the dry granules with a 35-mesh sieve;

[0075] 6. Mix the sized granules with low-substituted hydroxypropyl cellulose passing through a 30-mesh sieve (10rpm 15min);

[0076] 7. Sodium stearyl fumarate is passed through a 50-mesh sieve, and mixed with step 6 (10rpm 5min);

[0077] 8. Press the tablet with a φ8mm punch.

Embodiment 3

[0079] prescription

[0080]

[0081] craft

[0082] Asenapine maleate is passed through a 100-mesh sieve, and camphor is pulverized through a 60-mesh sieve for subsequent use;

[0083] First mix the prescription amount of camphor and PEG6000 evenly, and then mix with the remaining ingredients in the prescription;

[0084] The mixed powder is directly compressed into tablets, and the hardness is maintained at 4-5kg / cm 2 about;

[0085] Heat the tablet at 80°C;

[0086] After 5 hours, it was taken out and weighed to confirm that the camphor was completely removed.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
hardnessaaaaaaaaaa
Login to View More

Abstract

The invention relates to an asenapine maleate sublingual tablet and a preparation method thereof. The asenapine maleate sublingual tablet comprises a main drug and auxiliary materials, wherein the main drug is asenapine maleate, and the auxiliary materials comprise filler, a disintegrating agent, a binder, an antioxidant and a lubricant. The preparation method comprises the following steps of: dissolving the antioxidant, the binder and the asenapine maleate by using an organic solvent so as to prepare mixed solution; collecting the filler and the disintegrating agent after sieving so as to obtain mixed powder; spraying the mixed solution on the mixed powder and carrying out granulation to obtain wet medicinal granules; drying the wet medicinal granules to ensure that an LOD is not more than 2.5%, and preparing dry medicinal granules; and after the dry medicinal granules are mixed with the sieved disintegrating agent, adding the sieved lubricant for mixing, and carrying out punching andpressing to prepare the asenapine maleate sublingual tablet. The preparation method is capable of realizing rapid disintegration and dissolution and avoiding the friability problem caused by a porousstructure and the related substance increase caused by high temperature, and is simple in process, low in cost and easy to enlarge the production.

Description

technical field [0001] The invention belongs to the technical field of medicament preparation, and relates to a sublingual asenapine maleate tablet and a preparation method thereof. Background technique [0002] Asenapine maleate sublingual tablet, specification 2.5mg\5mg\10mg, original product name SAPHRIS, developed by AllerganUSA, Inc., first approved by FDA in 2009. For the treatment of schizophrenia and bipolar I disorder in adults. At present, this variety (raw material / preparation) is not listed in the domestic market. [0003] According to GoodRx: SAPHRIS US price is 604.75USD / 30 pieces. SAPHRIS' sales in 2017 reached US$155 million, with a large market and large profit margins. [0004] For the production of asenapine maleate sublingual tablets, the existing technologies are mainly divided into freeze-drying technology and porogen sublimation technology: [0005] CN 1079670C discloses a rapidly disintegrating sublingual tablet containing medicinal water-soluble ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/12A61K31/407A61P25/18
CPCA61K9/006A61K9/2013A61K9/2054A61K9/2095A61K31/407A61P25/18
Inventor 孙超左人杰司宗为
Owner 天津仁生医药科技有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com