Tablet containing lamidetan and preparation method thereof
The preparation of lamidin-containing succinate tablets through wet granulation process solves the problem of the unsafeness of existing ‘ditin’ drugs for patients with cardiovascular diseases, and achieves high-quality stability and simple preparation process of the drug, which is suitable for large-scale production.
Patent Information
- Application Number
- CN202311296557.X
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2023-10-09
- Publication Date
- 2025-04-11
AI Technical Summary
The existing migraine treatment drug ‘Ditan’ has a vasoconstrictive effect, which is unsafe for patients with cardiovascular disease, and its preparation form and production process pose certain challenges.
Tablets containing ramiditan succinate are prepared by wet granulation process. By mixing them with equal amounts of pharmaceutically acceptable excipients (such as fillers, disintegrants, lubricants, etc.), stable particles are formed, and treated with binders or wetting agents, and finally tablets are pressed.
This method not only ensures the quality and stability of the drug, but also has a simple preparation process and convenient operation. It is suitable for large-scale production, reducing dust pollution and production costs, and improving economic benefits.
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Abstract
Description
Technical Field
[0001] The invention belongs to the field of medicine and relates to a tablet containing lamiditan and a preparation method thereof. Background Art
[0002] Lasmiditan binds to 5-HT1F receptors with high affinity. Lasmiditan may play its therapeutic role in the treatment of migraine by stimulating 5-HT1F receptors. Its mechanism of action is different from the new drugs of the "ditatan" class currently approved for the treatment of migraine. It does not have a vasoconstrictive effect and is safer for migraine patients with cardiovascular disease or at risk of cardiovascular disease. The tablet is composed of lamiditan succinate and pharmaceutically acceptable excipients and is prepared by wet granulation process, which does not affect the preparation form and ensures the quality and stability of the preparation. The preparation method is simple, easy to operate, has a wide range of applications, is easy to transport and store, and is suitable for large-scale production. Summary of the invention
[0003] To achieve the above object, the technical solution of the present invention is a tablet containing lamiditan and a preparation method thereof. The tablet composition consists of lamiditan succinate and pharmaceutically acceptable excipients.
[0004] The pharmaceutically acceptable excipients include one or more of fillers, binders, disintegrants and lubricants.
[0005] The filler is selected from one or more of microcrystalline cellulose, starch, pre-melted starch, mannitol or sorbitol.
[0006] The disintegrant is selected from one or more of sodium carboxymethyl starch, hydroxypropyl cellulose or cross-linked sodium carboxymethyl cellulose.
[0007] The binder or wetting agent is selected from one or more of water, starch, povidone or hypromellose.
[0008] The lubricant is selected from one or more of magnesium stearate, micro powder silica gel and talc.
[0009] The weight percentage of filler is 10%-70%; the weight percentage of disintegrant is 1%-3%; the weight percentage of lubricant is 0.1%-1%; the weight percentage of binder or wetting agent is 0%-10%.
[0010] The tablets are prepared by a wet method, and the preparation process is: lamiditan hydrochloride and auxiliary materials are added in equal amounts and mixed evenly, a binder or a wetting agent is added, a soft material is prepared, granulated, air-dried, granulated, a prescribed amount of lubricant is added, mixed evenly, and tabletted.
[0011] Compared with the prior art, the present invention has the following beneficial effects: (1) The present invention adopts wet granulation, which has little impact on the environment, has low dust pollution, saves costs, is conducive to industrial production, and improves economic benefits; (2) Compared with dry granulation, the present invention is simple and quick to prepare, has a high one-time forming rate, saves time, has good granule fluidity, strong wear resistance, good compression forming property, and is easy to operate. Implementation
[0012] To facilitate the understanding of the technical solution of the present invention, it is introduced below in conjunction with specific implementation methods. Example
[0013]
[0014] Preparation method: The prescribed amount of succinate lamiditan and mannitol are mixed evenly by equal amounts, and then mixed with microcrystalline cellulose and low-substituted hydroxypropyl cellulose by equal amounts, purified water is added to make a soft material, 16 mesh granules are made, and ventilation drying is carried out at 50°C to a moisture content of 2%-3%, and then 24 mesh granules are made, and the yield is calculated by weighing, and magnesium stearate is added, mixed, and tableted. Example
[0015]
[0016] Preparation method: The prescribed amount of lamiditan and mannitol are mixed evenly by equal amounts, and then mixed with microcrystalline cellulose and low-substituted hydroxypropyl cellulose by the principle of equal amounts, and 10% starch slurry is added to make a soft material, 16 mesh granules are made, and ventilation drying is carried out at 45°C to a moisture content of 2%-3%, and then 24 mesh granules are granulated, and the yield is calculated by weighing, and magnesium stearate is added, mixed, and tableted. Example
[0017]
[0018] Preparation method: The prescribed amount of lamiditan and sucrose are mixed evenly by equal amounts, and then mixed with pre-polymerized starch and low-substituted hydroxypropyl cellulose by the principle of equal amounts, and a polyvidone aqueous solution is added to make a soft material, 16-mesh granules are made, and ventilation drying is carried out at 50°C to a moisture content of 2%-3%, and then granulated with 24-mesh granules. After weighing to calculate the yield, magnesium stearate is added, mixed evenly, and tableted. Example
[0019]
[0020] Preparation method: The prescribed amount of lamiditan and sorbitol are mixed evenly by equal amounts, and then mixed with starch and low-substituted hydroxypropyl cellulose by the principle of equal amounts, purified water is added to make a soft material, 16 mesh granules are made, and ventilation drying is carried out at 50°C to a moisture content of 2%-3%, and then granulated with 24 mesh granules. After weighing to calculate the yield, magnesium stearate is added, mixed evenly, and tableted. Example
[0021] Comparison of related substances: According to the guidelines for the stability of drug preparations in the Appendix of Part II of the 2020 Pharmacopoeia, we accelerated the test of self-made samples and placed them at a temperature of 40℃±2℃ and a relative humidity of 75%±5% for 6 months to compare the related substances:
[0022] As can be seen from the table above, the samples prepared by this prescription process have good stability in terms of relevant substances after 6 months of accelerated testing, and the preparation process is simple, practical and easy to control in production and manufacturing, and the particle fluidity is good, so the overall applicability is very high.
Claims
1. A tablet containing lamiditan, characterized in that: The tablet consists of lamiditan succinate and pharmaceutically acceptable excipients.
2. The tablet of lamiditan succinate according to claim 1, characterized in that The pharmaceutically acceptable excipients include one or more of fillers, binders, disintegrants and lubricants.
3. The tablet of lamiditan succinate according to claim 2, characterized in that: The filler is selected from one or more of microcrystalline cellulose, starch, pre-melted starch, mannitol or sorbitol.
4. The tablet of lamiditan succinate according to claim 2, characterized in that: The disintegrant is selected from one or more of sodium carboxymethyl starch, hydroxypropyl cellulose or cross-linked sodium carboxymethyl cellulose.
5. The tablet of lamiditan succinate according to claim 2, characterized in that: The binder or wetting agent is selected from one or more of water, starch, povidone or hypromellose.
6. The tablet of lamiditan succinate according to claim 2, characterized in that: The lubricant is selected from one or more of magnesium stearate, micro powder silica gel and talcum powder.
7. The tablet of lamiditan succinate according to claim 2, characterized in that: The weight percentage of filler is 10%-70%; the weight percentage of disintegrant is 1%-3%; the weight percentage of lubricant is 0.1%-1%; the weight percentage of binder or wetting agent is 0%-10%.
8. The tablet of lamiditan succinate according to claim 1, characterized in that: The tablets are prepared by wet granulation.