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Ranolazine hydrochloride slow-release preparation and its preparing method

A technology for ranolazine hydrochloride and sustained-release preparations, which is applied in the field of oral sustained-release preparations containing ranolazine hydrochloride and its preparation, and can solve problems such as incomplete release of ranolazine base, inability to sustain cardiac protection, incomplete absorption, etc.

Active Publication Date: 2009-08-05
QILU PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since ranolazine base is slightly to very slightly soluble in intestinal fluid, and the patent fails to provide conclusive data demonstrating that the pH-dependent adhesive facilitates release of ranolazine base in the intestinal tract, release of ranolazine base may be incomplete leading to incomplete incomplete absorption
Example 4 of this patent shows that the anti-anginal and anti-ischemic effects of the immediate-release ranolazine formulation will not last throughout the dosing interval, indicating that the common oral formulation of ranolazine is effective and well tolerated, but it cannot provide sustained Protective effects

Method used

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  • Ranolazine hydrochloride slow-release preparation and its preparing method
  • Ranolazine hydrochloride slow-release preparation and its preparing method
  • Ranolazine hydrochloride slow-release preparation and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Ranolazine Hydrochloride Sustained Release Tablets Formula:

[0107] Each 1000 tablets of Ranolazine Hydrochloride Sustained Release Tablets contains

[0108]

[0109] (1) Pass the formulated amount of hydroxypropyl methylcellulose and ethyl cellulose through a 40-mesh sieve 5 times and mix thoroughly.

[0110] (2) Mix ranolazine hydrochloride with the materials in (1) in equal increments, pass through a 40-mesh sieve 5 times and fully mix.

[0111] (3) Add an appropriate amount of 85% ethanol aqueous solution to the uniformly mixed material, mix uniformly, make a soft material, pass through a 20-mesh sieve to granulate, and dry at 40-50° C. for 2 hours.

[0112] (4) Add the prescribed amount of magnesium stearate, pass the dry granules through a 20-mesh sieve for granulation, fully mix, measure the content of the granules, calculate the tablet weight, and compress into tablets.

[0113] (5) A coating layer can be coated on the outer layer of the sustained-release ...

Embodiment 2

[0115] As described in Example 1, the difference is that hydroxypropyl methylcellulose HPMC K100M CR is replaced by hydroxypropyl methylcellulose HPMC K4M CR, The amount of RS PO was increased to 60 g, and the ethyl cellulose EC10CP STD.PREM.FP was replaced with ethyl cellulose EC100CPSTD.PREM.FP and the amount was reduced to 25.8 g.

Embodiment 3

[0117] As described in Example 1, the difference is that the amount of hydroxypropyl methylcellulose (HPMC K100M CR) is increased to 90g, with RL PO instead For RS PO, the amount of ethyl cellulose was reduced to 27g.

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Abstract

The ranolazine hydrochloride sustained-release preparation and a preparation method thereof belong to the technical field of medicine. The ranolazine hydrochloride sustained-release preparation contains 25-95% by weight of ranolazine hydrochloride and one or more pharmaceutically acceptable inert excipients, which include a sustained-release matrix, binder, disintegrant, diluent, lubricant , a glidant or a wetting agent, the sustained-release matrix is ​​a pH-independent substance, and can release medicine for 12 hours. It is used to prepare medicines for treating angina pectoris, acute coronary syndrome, heart failure and other cardiovascular diseases. Each preparation unit of the sustained-release preparation contains 30-600 mg of ranolazine hydrochloride, and the tablet weight is 120-1200 mg. The invention has the characteristics of less times of taking medicine, good sustained-release effect, light tablet weight and the like.

Description

(1) Technical field [0001] The invention relates to a sustained-release preparation of ranolazine hydrochloride and a preparation method thereof, in particular to an oral sustained-release preparation containing ranolazine hydrochloride and a preparation method thereof. (2) Background technology [0002] Ranolazine hydrochloride is N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazinyl}acetamide disalt salt. U.S. Patent No. 4,567,264 discloses ranolazine (±)-N-(2,6-dimethylphenyl)-4-[2-hydroxyl-3-(2-methoxyphenoxy)-propyl]-1 - piperazine acetamide and pharmaceutically acceptable salts thereof, and discloses their use for the treatment of cardiovascular diseases including arrhythmia, variability and exercise angina, and myocardial infarction. [0003] U.S. Patent No. 5,506,229 discloses the use of ranolazine and pharmaceutically acceptable salts and esters thereof for the treatment of physically or chemically damaged tissues, including cardioplegia, h...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/495A61P9/10
Inventor 张宇红杨清敏于艳玲唐玮李颖
Owner QILU PHARMA HAINAN
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