Oral preparation containing ranolazine hydrochloride for treating cardiovascular disease

An oral preparation and cardiovascular technology, which is applied in the field of oral preparations containing ranolazine hydrochloride for the treatment of cardiovascular diseases, can solve the problems of incomplete absorption, incomplete release, and incomplete absorption in the human body, and achieve dose reduction, complete absorption and utilization, The effect of reducing individual differences

Inactive Publication Date: 2005-01-12
HUAZHONG NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The API of the patent formulation is ranolazine free base, and the patent fails to provide definite data to prove that the pH-dependent adhesive promotes the release of ranolazine free base in the intestinal tract, and the AUC of its formulation 0～24 Significantly smaller than immediate-release preparations, suggesting that incomplete release may lead to incomplete absorption by the human body
Since the acrylic resin and ranolazine free base are intimately mixed, the former being swellable in intestinal fluids, and ranolazine free base being slightly soluble to almost insoluble in intestinal fluids, the adhesive prevents the complete release of ranolazine free base resulting in absorption in the body incomplete

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Composition and preparation method of 200mg ranolazine hydrochloride compressed tablet

[0038] Mix 200.0 g of ranolazine hydrochloride, 100.0 g of microcrystalline cellulose, 40.0 g of calcium hydrogen phosphate, and 40.0 g of micropowdered silica gel, use 40 wt% ethanol aqueous solution as a wetting agent to make a soft material, granulate with a 20-mesh sieve, and ventilate and dry at 60°C After 4 hours, granulate, add 5.0 g of sodium carboxymethylcellulose and 5.0 g of magnesium stearate, mix well and press to obtain about 1000 round tablets, each containing 200 mg of ranolazine hydrochloride, to obtain compressed tablets.

Embodiment 2

[0040] Composition and preparation method of 300mg ranolazine hydrochloride compressed tablet

[0041] Mix 300.0g of ranolazine hydrochloride, 100.0g of microcrystalline cellulose, 30.0g of calcium hydrogen phosphate, and 30.0g of micropowdered silica gel, and use 60wt% ethanol aqueous solution containing 5wt% polyvinylpyrrolidone as a wetting agent to make a soft material through a 20-mesh sieve Granulate, ventilate and dry at 60°C for 3 hours, granulate, add 15.0 g of micropowder silica gel and 5.0 g of magnesium stearate, mix evenly, and press to obtain about 1000 capsule-shaped tablets, each containing 300 mg of ranolazine hydrochloride, to obtain compressed tablets.

Embodiment 3

[0043] Composition and preparation method of 500mg ranolazine hydrochloride compressed tablet

[0044] Mix 500.0 g of ranolazine hydrochloride, 60.0 g of microcrystalline cellulose, 50.0 g of calcium hydrogen phosphate, and 40.0 g of micropowdered silica gel, make a soft material with 70 wt % ethanol aqueous solution as a wetting agent, granulate with a 20-mesh sieve, and ventilate and dry at 60 ° C After 3 hours, granulate, add 10.0 g of micropowder silica gel, 15.0 g of polyvinylpyrrolidone, and 5.0 g of magnesium stearate, mix well, and press to obtain capsule-shaped tablets, each containing 500 mg of ranolazine hydrochloride, to obtain compressed tablets.

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PUM

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Abstract

An orally-applied ranolazine hydrochloride for treating cardiovascular disease is prepared from ranolazine hydrochloride, diluent, adhesive, disintegrant, antisticking agent and lubricant through adding wetting agent, preparing soft material, granulating and drying.

Description

Technical field: [0001] The invention relates to an oral preparation containing ranolazine hydrochloride for treating cardiovascular diseases and a preparation method. Administration of this preparation maintains ranolazine in human plasma at a therapeutic level. Background technique: [0002] Ranolazine is (±)-N-(2,6-dimethylphenyl) 4-[2-hydroxy-3-(2-methoxyphenoxy)-propyl]-1-piperazineacetamide It was first disclosed by U.S. Patent US4567264, which explained that ranolazine and its pharmaceutically acceptable salts have superior medical functions, and disclosed that it is used for the treatment of cardiovascular diseases including arrhythmia, variable and exercise-induced angina, and myocardial infarction. disease. [0003] U.S. Patent No. 5,506,229 discloses the use of ranolazine and its pharmaceutically acceptable salts for treating physically and chemically damaged tissues, including cardioplegia, hypoxia or reperfusion injury of heart and skeletal muscle or brain tis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61P9/06A61P9/10
Inventor 杨光富刘祖明卿湘华
Owner HUAZHONG NORMAL UNIV
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