Arbidol hydrochloride injection emulsion and preparation method thereof

A technology of arbidol hydrochloride and emulsion, which is applied in the field of medicine and can solve the problems of poor stability and low solubility

Active Publication Date: 2021-06-11
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the problems of low solubility and poor stability of arbidol hydrochloride injection, the invention p...

Method used

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  • Arbidol hydrochloride injection emulsion and preparation method thereof
  • Arbidol hydrochloride injection emulsion and preparation method thereof
  • Arbidol hydrochloride injection emulsion and preparation method thereof

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Embodiment 1

[0038] The embodiment of the present invention provides an arbidol hydrochloride injection emulsion, which consists of the following components:

[0039] Arbidol hydrochloride 1.2g, soybean lecithin 3g, Tween 80 1g, gum arabic 1g, n-propanol 2g, soybean oil 80g, glucose 15g, vitamin C 2g, appropriate amount of citric acid, and water for injection to 1000mL;

[0040] The above-mentioned Arbidol hydrochloride injection emulsion preparation method is as follows:

[0041] Weigh each component according to the above ratio, add arbidol hydrochloride, soybean lecithin, Tween 80, gum arabic, and n-propanol into soybean oil, heat and stir to dissolve as an oil phase; add glucose and vitamin C In 200mL of water for injection, heat and stir to dissolve as the water phase; add the oil phase to the water phase under shear and mix to make colostrum, the shear speed is 5000r / min, and the shear time is 7min; add water for injection to 1000ml and use citron Adjust the pH to 2.2 with acid, and...

Embodiment 2

[0043] The embodiment of the present invention provides an arbidol hydrochloride injection emulsion, which consists of the following components:

[0044]Arbidol hydrochloride 4.8, soybean lecithin 15g, Tween 80 15g, gum arabic 15g, n-propanol 15g, soybean oil 300g, glycerin 45g, vitamin C 5g, acetic acid-sodium acetate buffer solution, and water for injection 1000mL;

[0045] The above-mentioned Arbidol hydrochloride injection emulsion preparation method is as follows:

[0046] Weigh each component according to the above ratio, add arbidol hydrochloride, soybean lecithin, Tween 80, gum arabic, and n-propanol into soybean oil, heat and stir to dissolve as an oil phase; add glycerin and vitamin C In 500mL of water for injection, heat and stir to dissolve it as the water phase; add the oil phase to the water phase under shear and mix to make colostrum, the shear speed is 10000r / min, and the shear time is 20min; add water for injection to 1000ml and use acetic acid- Adjust the p...

Embodiment 3

[0048] The embodiment of the present invention provides an arbidol hydrochloride injection emulsion, which consists of the following components:

[0049] Arbidol hydrochloride 3g, soybean lecithin 10g, Tween 80 5g, gum arabic 7g, n-propanol 7g, soybean oil 150g, glycerin 30g, vitamin C 3g, acetic acid-sodium acetate buffer solution, and water for injection 1000mL;

[0050] The above-mentioned Arbidol hydrochloride injection emulsion preparation method is as follows:

[0051] Weigh each component according to the above ratio, add arbidol hydrochloride, soybean lecithin, Tween 80, gum arabic, and n-propanol into soybean oil, heat and stir to dissolve as an oil phase; add glycerin and vitamin C In 350mL of water for injection, heat and stir to dissolve as the water phase; add the oil phase to the water phase under shear and mix to make colostrum, the shear speed is 7000r / min, and the shear time is 15min; add water for injection to 1000ml and use acetic acid- Adjust the pH to 3 ...

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Abstract

The invention relates to the technical field of medicines, in particular to an arbidol hydrochloride injection emulsion and a preparation method thereof. The arbidol hydrochloride injection emulsion comprises the following components: arbidol hydrochloride, an emulsifier, a co-emulsifier, oil for injection, an isoosmotic adjusting agent, a pH adjusting agent, an antioxidant and water for injection, wherein the emulsifier is soybean lecithin and Tween 80, and the co-emulsifier is Arabic gum and n-propyl alcohol. According to the preparation method of the arbidol hydrochloride injection emulsion provided by the invention, a high-pressure homogenization process is adopted, and the drug is entrapped in the emulsion droplets, so that the drug loading capacity of the preparation is improved, the solubility and bioavailability of arbidol hydrochloride are improved, the administration frequency is reduced, the toxic and side effects and irritation are reduced, and the preparation is high in stability. The problem that the medicine is easy to separate out in the storage and use processes of the conventional injection emulsion is solved; and meanwhile, administration is convenient, effect taking is fast, the preparation technology is simple, and the preparation method can be used for industrial large-scale production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an arbidol hydrochloride injection emulsion and a preparation method thereof. Background technique [0002] Arbidol hydrochloride (also known as Arbidol hydrochloride, Arbidol), its chemical name is: 6-bromo-4-(dimethylaminomethyl)-5-hydroxyl-1-methyl-2-(phenylthio Methyl)-1H-indole-3-carboxylic acid ethyl ester hydrochloride is an antiviral drug developed by the former Soviet Medicinal Chemistry Research Center as a treatment for A and B influenza viruses and other acute respiratory virus infections Preventive and therapeutic drugs can significantly improve the clinical symptoms of patients. [0003] Arbidol hydrochloride is a drug that is insoluble in water. Arbidol hydrochloride injection prepared by conventional preparation methods has low bioavailability due to its low water solubility and short half-life. And during use, the drug is prone to precipitation, and the drug s...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/4045A61K47/10A61K47/24A61K47/26A61K47/36A61K47/44A61P11/00A61P31/12A61P31/16
CPCA61K31/4045A61K9/1075A61K9/0019A61K47/44A61K47/36A61K47/24A61K47/26A61K47/10A61P11/00A61P31/16A61P31/12
Inventor 王立江赵勇征崔永斌刘敬涛安志远刘苗尹灏轩
Owner SHIJIAZHUANG NO 4 PHARMA
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