A kind of felodipine sustained-release tablet and preparation process thereof

Abstract

The invention discloses a felodipine sustained release tablet and a preparation technology thereof and belongs to the field of chemical drug preparations. The felodipine sustained release tablet comprises a felodipine solid dispersion agent, a filling agent, a disintegrating agent and a lubricating agent. The method comprises the following steps: mixing and suspending felodipine, carbomer resin and sodium alginate in absolute ethyl alcohol, drying and removing ethyl alcohol, thereby acquiring the felodipine solid dispersion agent; uniformly mixing with the filling agent and the disintegratingagent, by taking 60% ethyl alcohol as an adhesive, pelletizing and drying at 45 DEG C, thereby acquiring medicated particles; filtering the medicated particles with a 18-mesh sieve, uniformly mixing with a prescription amount of lubricating agent and preforming. The invention successfully solves the problem of felodipine sustained release; the drugs can be completely released; the effective bloodconcentration can be long-term maintained; the bioavailability is high; the preparation process is simple and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a pharmaceutical preparation, in particular to a sustained-release tablet containing felodipine and a preparation process thereof. Background technique [0002] The chemical name of felodipine is (±)-2,6-dimethyl-4-(2,3-dichlorophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate ethyl ester. White to light yellow crystal or crystalline powder; odorless, tasteless; unstable when exposed to light. This product is soluble in acetone, methanol or ethanol, almost insoluble in water. Molecular formula is C 18 h 19 C l2 NO 4 , the molecular weight is 384.25400, the density is 1.277g / cm3, the boiling point is 471.5℃at 760mmHg, and the flash point is 239℃. [0003] This product is a selective calcium ion antagonist, which mainly inhibits the inflow of extracellular calcium in arteriolar smooth muscle, selectively expands arterioles, has no effect on veins, ...

AI Technical Summary

Problems solved by technology

[0004] CN101953837A discloses a felodipine sustained-release tablet and a preparation method thereof. The cyclodextrin inclusion method is adopted to dissolve the active ingredient felodipine in the macromolecular gap of the cyclodextrin, because the cyclodextrin has good hydrophilicity , so that the release of the preparation is stable, but it takes a long time to prepare the inclusion compound of felodipine cyclodextrin system by this method, and the process is cumbersome and difficult to control

[0005] CN102552200A discloses a felodipine slow-release tablet, which contains felodipine, high-viscosity hypromellose, low-viscosity hypromellose and a water-soluble filler, and also contains other pharmaceutical adjuvants. Hypromellose has poor compressibility and fluidity, making it difficult to form formulations

The felodipine sustained-release tablet comprises the following ingredients: active ingredient felodipine, hydroxypropyl methylcellulose, micropowder silica gel, filler, antioxidant, solubilizer and lubricant, and is prepared by dry granulation and then tableting Defelodipine sustained-release tablets, this invention does not fundamentally solve the stability problem of felodipine, because all the excipients have relatively high hygroscopicity, the degradation products will still increase significantly during storage

At the same time, direct compression has high requirements on the fluidity of excipients, and excipients suitable for direct compression are generally expensive; the most obvious defect of direct compression is poor content uniformity

However, the unevenness of dry granulation particles will lead to problems such as large differences in tablet weight, uneven hardness, and rapid dissolution.

[0012] In summary, the prior art has failed to provide a felodipine sustained-release tablet with good stability, stable dissolution, small side effects, and simple preparation process.

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