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Oseltamivir phosphate oral liquid and preparation method thereof

A technology of oseltamivir phosphate and Wei oral liquid, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of inability to ensure the safety of drug administration and unsuitable capsule dosage forms. , difficult to accurately administer and other problems, to achieve the effect of convenient carrying and taking, easy storage, and stable quality

Inactive Publication Date: 2016-05-04
SHANGHAI TAOHONG CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, in my country, the commercially available dosage form of oseltamivir phosphate is capsule, and its unit dose is 98.5 mg / capsule (containing 75 mg of oseltamivir). It can be seen that the dose of capsule is too large, which is not suitable for children, especially young children. It is not easy for patients to administer medicines accurately, and the safety of administration cannot be ensured; on the other hand, due to inconvenient swallowing or difficulty in swallowing by the elderly, children and patients with severe influenza, the capsule dosage form is not suitable for these specific groups of people

Method used

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  • Oseltamivir phosphate oral liquid and preparation method thereof
  • Oseltamivir phosphate oral liquid and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0028] Raw materials for oseltamivir phosphate oral liquid: 0.3g oseltamivir phosphate, 0.044g co-solvent, 0.03g aspartame, 0.03g stabilizer, 0.03g ethyl p-hydroxybenzoate, 90g distilled water.

[0029] The co-solvent is prepared by mixing 0.11g sodium carboxymethylcellulose, 0.11g propylene glycol, 0.11g maltitol, and 0.11g poloxamer 188.

[0030] The stabilizer is prepared by mixing 0.02g of hydroxypropylmethylcellulose, 0.005g of sodium alginate and 0.005g of disodium glutarate.

[0031] Oseltamivir phosphate oral liquid is prepared by the following method:

[0032] Add the cosolvent into distilled water and stir evenly; then add oseltamivir phosphate and stir evenly; then add aspartame, stabilizer and ethyl p-hydroxybenzoate, mix evenly to obtain a mixed solution; finally mix the mixed solution at 115 Sterilize at ℃ for 18 minutes to obtain the oseltamivir phosphate oral liquid, which is divided into 15ml / bottle after cooling.

Embodiment 2

[0034] Prepare by the method of embodiment 1, difference is only in:

[0035] The co-solvent is replaced by a mixture of propylene glycol, maltitol and poloxamer 188 in a mass ratio of 1:1:1.

Embodiment 3

[0037] Prepare by the method of embodiment 1, difference is only in:

[0038] The co-solvent is replaced by a mixture of sodium carboxymethylcellulose, maltitol and poloxamer 188 in a mass ratio of 1:1:1.

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Abstract

The invention discloses oseltamivir phosphate oral liquid and a preparation method thereof. The oseltamivir phosphate oral liquid is prepared from, by weight, 0.2-0.4 part of oseltamivir phosphate, 0.03-0.05 part of a cosolvent, 0.03-0.05 part of aspartame, 0.03-0.05 part of a stabilizing agent, 0.03-0.05 part of ethyl p-hydroxybenzoate and 75-95 parts of water. The prepared oseltamivir phosphate oral liquid has the advantages of being small in taking dosage, rapid to absorb, stable in quality, convenient to carry and take, easy to preserve, good in stability, high in clearity and the like and is particularly suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an oseltamivir phosphate preparation and a preparation method thereof, in particular to an oseltamivir phosphate oral liquid and a preparation method thereof. Background technique [0002] Oseltamivir Phosphate, Chemical Name: (3R,4R,5S)-4-Acetamido-5-Amino-3(1-Ethylpropoxy)-1-Cyclohexene-1-Carboxylic Acid Ethyl Phosphate . [0003] Oseltamivir phosphate is the prodrug of its active metabolite, and its active metabolite (oseltamivir carboxylate) is a selective influenza virus neuraminidase inhibitor. The activity of neuraminidase, a glycoproteinase on the surface of viruses, is critical for the release of newly formed virus particles from infected cells and the further dissemination of infectious virus in humans. [0004] The active metabolite of oseltamivir phosphate inhibits the neuraminidase activity of influenza A and B viruses. The half-inhibitory concentration of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/38A61K47/10A61K47/26A61K47/36A61K47/12A61K31/215A61P31/16
CPCA61K9/0053A61K9/08A61K31/215A61K47/10A61K47/12A61K47/26A61K47/36A61K47/38
Inventor 黄毅
Owner SHANGHAI TAOHONG CHEM TECH
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