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

Abstract

The invention provides a felodipine sustained-release tablet, which is prepared by wrapping a sustained-release layer with a sustained-release element tablet. The sustained-release element tablet contains the following components in weight percentage: 1-4% of felodipine, 40% polyoxyethylene as a solubilizer Hydrogenated castor oil accounts for 2-8%, filler 63-72.5%, binder 1-5%, skeleton slow-release material 10-25%, absorbent 1-6%, lubricant 0.2-1.5%; slow-release layer The composition contains the following components by weight percentage: the coating material is ethyl cellulose, and the weight gain is 6-12% of the total weight of the sustained-release tablet; the plasticizer, the weight gain is 0-20% of the weight of the coating material; As for the adhesive, the weight gain is 0-50% of the weight of the coating material; for the coloring agent, the weight gain is 0-10% of the weight of the coating material. The present invention realizes the double sustained release of the preparation by constructing the sustained-release tablet and the coating sustained-release material, fully releases the drug, greatly improves the bioavailability, and meets the requirements of consistency evaluation; and has good reproducibility, high uniformity, and reliable quality. control.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, belongs to the sustained-release preparation technology, in particular to a felodipine sustained-release tablet and a preparation method thereof. Background technique [0002] Felodipine, white to light yellow crystal or crystalline powder, odorless and tasteless; unstable in case of light, almost insoluble in water, its chemical name is 2,6-dimethyl-4-(2,3 -Dichlorophenyl)-1,4-dihydro-3,5-methylethylpyridinedicarboxylate, the molecular formula is C 18 h 19 C l2 NO 4 , the molecular weight is 384.2538, and the structural formula is as follows: [0003] [0004] Large-scale clinical trials at home and abroad (such as HOT International Study, HOT China Study, China FEVER Study, etc.) have proved that felodipine can effectively prevent and reduce the occurrence of stroke and other complications caused by hypertension. As a selective dihydropyridine calcium antagonist, fel...

AI Technical Summary

Problems solved by technology

[0005] There are two problems in felodipine preparation: the one, because the water solubility of medicine is poor, dissolution is slow, and bioavailability is low, and first-pass effect is obvious; However, the existing sustained-release preparations have problems such as difficulty in taking effect quickly after oral administration and incomplete drug release, which are common defects of domestic generic drugs

Above-mentioned three kinds of ways can all reach the purpose of improving and improving the solubility and release degree of felodipine in vivo, but the direct addition of anionic surfactant type solvent in the method one has caused the oxidation product of felodipine preparation to increase, and with Oxidation products will continue to increase as time changes, which is not conducive to the quality control of the preparation, and may even cause adverse reactions in severe cases; when the drug release of the preparation made by method two, there will be problems of fast release in the early stage, slow release in the middle and late stages, or even incomplete release; method The prepared preparation solved the problem of fast front and slow slow to a certain extent, but did not solve the problem of low solubility of felodipine in water, and it was difficult to achieve the same dissolution as the original preparation

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