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P-toluene sulfonic acid edoxaban oral solution and preparing method thereof

A technology of p-toluenesulfonic acid and edoxaban, which is applied in the fields of blood diseases, pharmaceutical formulas, and extracellular fluid diseases, and can solve the problems of poor patient compliance and low bioavailability

Inactive Publication Date: 2016-03-30
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Whether it is a common tablet or a sustained-release tablet, there are deficiencies, that is, poor patient compliance and relatively low bioavailability. For stroke patients, a more suitable drug dosage form is needed clinically.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Edoxaban p-toluenesulfonate 20.20g

[0032] Citric acid 0.8g

[0033] Sodium citrate 1.6g

[0034] Propylene glycol 100g

[0035] Ethylparaben 0.3g

[0036] Sorbitol 200g

[0037] Strawberry essence 1g

[0038] Preparation method: Dissolve edoxaban p-toluenesulfonate and ethylparaben in propylene glycol, slowly add to the aqueous solution containing sorbitol, citric acid, and sodium citrate, mix well, adjust the pH, add purified water to nearly 900ml About; add strawberry essence, add purified water to 1000ml, constant volume, mix evenly, filter; test, subpackage, and sterilize.

[0039] Evaluation: The sample is a colorless clear liquid, slightly sweet, with a good taste.

Embodiment 2

[0041] Edoxaban p-toluenesulfonate 40.41g

[0042] Lactic acid 10g

[0043] Sodium Lactate 18g

[0044] Glycerin 150g

[0045] Benzoic acid 0.5g

[0046] Mannitol 180g

[0047] Lemon essence 1.5g

[0048] Preparation method: Dissolve edoxaban p-toluenesulfonate and benzoic acid in glycerin, slowly add to the aqueous solution containing mannitol, lactic acid, and sodium lactate, mix well, adjust the pH, add purified water to about 900ml; then add lemon Essence, add purified water to 1000ml, constant volume, mix evenly, filter; test, subpackage, and sterilize.

[0049] Evaluation: The sample is a colorless clear liquid, slightly acidic, and has a good mouthfeel, but not as good as that of Example 1.

Embodiment 3

[0051] Edoxaban p-toluenesulfonate 80.82g

[0052] Malic acid 1.0g

[0053] Polyethylene glycol 120g

[0054] Sodium Benzoate 1.0g

[0055] Maltitol 300g

[0056] Orange flavor 2g

[0057] Preparation method: dissolve edoxaban p-toluenesulfonate and sodium benzoate in polyethylene glycol, slowly add to the aqueous solution containing maltitol and malic acid, mix well, adjust the pH, add purified water to about 900ml; then Add orange essence, add purified water to 1000ml, constant volume, mix evenly, filter; test, subpackage, and sterilize.

[0058] Evaluation: The sample is a colorless clear liquid, slightly acidic, and has a good mouthfeel, but not as good as that of Example 1.

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PUM

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Abstract

The invention provides a p-toluene sulfonic acid edoxaban oral solution and a preparing method thereof; the preparation can treat phlebothrombosis, deep venous thrombosis and pulmonary embolism after adult patient elective hip joint or knee joint replacement surgery, and reduces risks of stroke and systemic embolism of patients with nonvalvular atrial fibrillation. The p-toluene sulfonic acid edoxaban oral solution has the advantages that the drug is dispersed in a medium in a molecular state, has large dispersion degree and fast absorption, can quickly play a drug effect, is beneficial for improving the bioavailability of the drug, can improve patient medication compliance, is convenient to take, easy dosage division, and is especially suitable for senile patients.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a pharmaceutical preparation containing edoxaban p-toluenesulfonate used for treating venous thrombosis, deep vein thrombosis and pulmonary embolism (VTE) after elective hip joint or knee joint replacement surgery in adult patients and its The preparation method has the advantages that the drug is dispersed in the medium in a molecular state, has a large degree of dispersion, is absorbed quickly, can quickly exert the drug effect, and is beneficial to improving the bioavailability of the drug; and can improve the drug compliance of patients, and is convenient to take and distribute. Dosage, especially for elderly patients. technical background: [0002] Atrial fibrillation (AF) is a cardiovascular "epidemic". As many as 3 million people around the world suffer from atrial fibrillation-related strokes every year. Atrial fibrillation-related strokes are more disabling and...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/444A61K47/26A61P7/02
CPCA61K9/0053A61K9/08A61K31/444A61K47/26
Inventor 张芳张庭
Owner BEIJING VENTUREPHARM BIOTECH
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