Pharmaceutical composition containing TBN or salt or hydrate of TBN and preparation method of pharmaceutical composition

A composition and hydrate technology, which is applied in the direction of drug combination, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of high toxicity and side effects, no specific drugs, poor curative effect, etc., and achieve improved bioavailability, Effect of improving stability and improving bioavailability

Active Publication Date: 2020-09-04
GUANGZHOU MAGPIE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, there is still no specific drug for the treatment of cerebral apoplexy clinically, and most of the drugs on the market fail to meet the requirements due to poor curative effect or severe side effects

Method used

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  • Pharmaceutical composition containing TBN or salt or hydrate of TBN and preparation method of pharmaceutical composition
  • Pharmaceutical composition containing TBN or salt or hydrate of TBN and preparation method of pharmaceutical composition
  • Pharmaceutical composition containing TBN or salt or hydrate of TBN and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Pass the TBN crude drug, mannitol, pregelatinized starch, crospovidone, sodium bicarbonate and magnesium stearate through a 40-mesh sieve, and set aside. Weigh 100g TBN raw material, 70g mannitol, 70g pregelatinized starch, 7.5g povidone K30, 5g crospovidone, 10g sodium bicarbonate, mix in a laboratory hopper mixer for 30min, then add 1g stearic acid Magnesium, mixed together for 1min, and directly compressed to obtain 1000 TBN tablet cores with a specification of 100mg and an average tablet weight of 0.2635g.

Embodiment 2

[0057] Pass the TBN crude drug, mannitol, pregelatinized starch, crospovidone, sodium bicarbonate, and magnesium stearate through a 40-mesh sieve, and set aside. Weigh 100g TBN raw material, 70g mannitol, 70g pregelatinized starch, 7.5g povidone K30, 5g crospovidone, 20g sodium bicarbonate, mix in a laboratory hopper mixer for 30min, then add 1g stearic acid Magnesium, mixed together for 1 min, and directly compressed to obtain 1000 TBN core tablets with a specification of 100 mg and an average tablet weight of 0.2735 g.

Embodiment 3

[0059] Pass the TBN crude drug, mannitol, pregelatinized starch, crospovidone, magnesium oxide, and magnesium stearate through a 40-mesh sieve, and set aside. Weigh 100g TBN API, 70g mannitol, 70g pregelatinized starch, 7.5g povidone K30, 5g crospovidone, 20g magnesium oxide, mix in a laboratory hopper mixer for 30min, then add 1g magnesium stearate , mixed together for 1 min, and directly compressed to obtain 1000 TBN tablet cores with a specification of 100 mg and an average tablet weight of 0.2735 g.

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PUM

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Abstract

The invention discloses a pharmaceutical composition containing TBN or salt or a hydrate of the TBN and a preparation method of the pharmaceutical composition. The pharmaceutical composition comprises(1) a tablet core containing an active ingredient TBN or pharmaceutically acceptable salt or hydrate of the TBN, and an alkalizing agent, and (2) an enteric layer outside the tablet core, wherein theenteric layer contains an opacifier and a coating material. The pharmaceutical composition disclosed by the invention is high in enteric coating film-forming property, and the bioavailability of theTBN in vivo can be improved. The pharmaceutical composition can be clinically used as a novel drug for treating diseases caused by excessive free radical generation / thrombosis.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, specifically a pharmaceutical composition containing TBN or its salt or hydrate and a preparation method thereof. Background technique [0002] At present, there is still no specific drug for the treatment of cerebral apoplexy clinically, and most of the drugs on the market fail to meet the requirements due to poor curative effect or severe side effects. [0003] The nitrone compound of the present invention is a kind of nitrone compound TBN that carries out structural modification on the basis of TMP, and its chemical name is (cis)-2-methyl-N-[(3,5,6-trimethyl Basepyrazine-2-)methine]2-propanamine oxide has the chemical structure shown in the following formula: [0004] [0005] TBN improves the antioxidant capacity while maintaining the thrombolytic ability, and can be used clinically for the treatment of neurodegenerative diseases, cardiovascular and cerebrovascular diseases, etc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K9/36A61K9/32A61K47/02A61K47/32A61K47/38A61K31/4965A61P9/10A61P25/00A61P9/00A61P25/08A61P25/16A61P25/14A61P21/00A61P25/28A61P11/00A61P37/02
CPCA61K9/2886A61K9/2009A61K9/2866A61K9/2846A61K31/4965A61P9/10A61P25/00A61P9/00A61P25/08A61P25/16A61P25/14A61P21/00A61P25/28A61P11/00A61P37/02A61K9/2059A61K9/2027A61K9/2018A61K9/2054A61K9/2813A61K9/2086A61K47/02A61K47/10A61K47/32
Inventor 刘伟孙业伟王玉强
Owner GUANGZHOU MAGPIE PHARMA
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