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A kind of triflusalol pharmaceutical composition with high bioavailability

A technology of availability and trifluxalol, which is applied in the field of trifluxalon pharmaceutical compositions, can solve the problems of low bioavailability and non-bioequivalence, and achieve the effect of high bioavailability and high dissolution rate

Active Publication Date: 2017-04-19
HAINAN ZHONGYU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventors have found through a large number of studies that although the dissolution rate of some prior art triflusalol oral solid preparations has been improved to a certain extent, there are still problems of low bioavailability and inability to be bioequivalent to the original product.

Method used

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  • A kind of triflusalol pharmaceutical composition with high bioavailability
  • A kind of triflusalol pharmaceutical composition with high bioavailability
  • A kind of triflusalol pharmaceutical composition with high bioavailability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1, triflusal capsules

[0055] prescription:

[0056]

[0057] Preparation Process:

[0058] 1) Preparation of adhesive: Take 15g of hypromellose, add appropriate amount of 80% ethanol solution, stir to dissolve, and use 80% ethanol solution to make up to 1000ml;

[0059] 2) Grind triflusalox through a 120-mesh sieve, and crush lactose, tartaric acid, and sodium carboxymethyl starch through a 100-mesh sieve respectively, weigh the prescription amount of trifluxal, lactose, tartaric acid, and sodium starch glycolate and mix well ;

[0060] 3) Add an appropriate amount of binder to make a soft material; granulate with a 24-mesh sieve, and ventilate and dry at 60°C;

[0061] 4) Add the prescription amount of talcum powder and mix, use a 22-mesh sieve to granulate, and mix evenly to get the product;

[0062] 5) Measure the main drug content of the granules;

[0063] 6) Pack capsules and polish;

[0064] 7) Packaging.

Embodiment 2

[0065] Embodiment 2, triflusalol tablet

[0066] prescription:

[0067]

[0068] Preparation Process:

[0069] 1) Preparation of adhesive: Take 15g of hypromellose, add appropriate amount of 80% ethanol solution, stir to dissolve, and use 80% ethanol solution to make up to 1000ml;

[0070] 2) Grind triflusalox through a 120-mesh sieve, and crush lactose, tartaric acid, and sodium starch glycolate through a 100-mesh sieve respectively, and weigh the prescribed amount of triflusal, lactose, tartaric acid and 2 / 3 of the prescribed amount of carboxymethyl starch Starch sodium is fully mixed evenly;

[0071] 3) Add an appropriate amount of binder to make a soft material; granulate with a 16-mesh sieve, and ventilate and dry at 60°C;

[0072] 4) Add the remaining 1 / 3 amount of sodium carboxymethyl starch and talcum powder to mix, use a 14-mesh sieve to sieve the granules, and mix well to get the product;

[0073] 5) Measure the content, determine the tablet weight, and compress...

Embodiment 3

[0076] Embodiment 3, triflusal capsules

[0077] prescription:

[0078]

[0079] Preparation method: with embodiment 1.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a triflusal pharmaceutical composition with high bioavailability. The pharmaceutical composition comprises the following components in parts by weight: 250-350 parts of triflusal, 35-65 parts of lactose, 45-55 parts of tartaric acid, 75-105 parts of sodium carboxymethyl starch, 3-8 parts of talcum powder and a proper amount of 1.5% hydroxy propyl cellulose and 80% ethanol solution. According to the triflusal pharmaceutical composition disclosed by the invention, the triflusal is high in dissolution rate and high in bioavailability in a preparation, and has bioequivalence with an original product; and the problems that a triflusal solid preparation in the prior art is low in bioavailability and cannot be biologically equivalent to the original product are solved.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a triflusalon pharmaceutical composition with high bioavailability. Background technique [0002] Triflusal, English name: Triflusal, chemical name: 2-acetoxy-4-[trifluoromethyl]-benzoic acid, molecular formula: C 10 h 7 f 3 o 4 , molecular weight: 248.15, the chemical structure is as follows: [0003] [0004] Triflusal is another anti-platelet aggregation drug similar in structure to aspirin. Its mechanism of action is similar to that of aspirin but different. Its mechanism of action is to inhibit cyclooxygenase and block thromboxane ( Thromboxane) formation. However, triflusal has little effect on inhibiting endothelial cell cyclooxygenase and does not affect the synthesis of prostaglandins. In addition, triflusal and its metabolite 2-hydroxy-4-trifluoromethylbenzoic acid (HTB) can inhibit phosphodiesterase, increase the concentration of cAMP in platelet...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/616A61K47/38A61K47/36A61K47/26A61K47/12A61K47/04A61P7/02A61P9/10A61K9/20A61K9/48
Inventor 石均平
Owner HAINAN ZHONGYU PHARMA CO LTD
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