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Valaciclovir hydrochloride liposome tablet and preparation method thereof

A technology of valacyclovir hydrochloride and lovir lipid, which is applied in the field of preparation of valacyclovir hydrochloride liposome tablets, can solve problems such as unfavorable stability of valacyclovir hydrochloride, achieve good tabletability, improve The effect of stability, good disintegration performance

Active Publication Date: 2021-01-05
药大制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But adding alkaline substances is more unfavorable for the stability of acidic valacyclovir hydrochloride

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] A preparation method of valacyclovir hydrochloride liposome tablet, comprising the following steps:

[0024] (1) Preparation of valacyclovir hydrochloride liposomes: Weigh 1 g of valacyclovir hydrochloride, 1 g of cholesterol and 8 g of soybean lecithin and dissolve them in a mixed solution of dichloromethane and methanol with a volume ratio of 3:1 , and then remove the solvent under vacuum at 60 °C on a rotary evaporator to obtain a thin film, and continue to evaporate for 2 hours to completely remove all traces of solvent and obtain a dry film; the dry film is added at 45 °C with an appropriate amount of 6g polyethylene. Pyrrolidone-K30 was hydrated in 20 mL of phosphate buffer for 15 minutes to obtain a liposome solution; the obtained liposomes were sonicated for 5 minutes to obtain small and uniform vesicles, and the obtained dried lipids were lyophilized The body powder was sieved through an 80-mesh sieve and stored at 4°C until use;

[0025] (2) Mixing: 1 g of li...

Embodiment 2

[0028] A preparation method of valacyclovir hydrochloride liposome tablet, comprising the following steps:

[0029] (1) Preparation of valacyclovir hydrochloride liposomes: Weigh 1 g of valacyclovir hydrochloride, 1 g of cholesterol and 8 g of soybean lecithin and dissolve them in a mixed solution of dichloromethane and methanol with a volume ratio of 3:1 , and then remove the solvent under vacuum at 60 °C on a rotary evaporator to obtain a thin film, and continue to evaporate for 2 hours to completely remove all traces of solvent and obtain a dry film; the dry film is added at 45 °C with an appropriate amount of 6g polyethylene. Pyrrolidone-K30 was hydrated in 20 mL of phosphate buffer for 15 minutes to obtain a liposome solution; the obtained liposomes were sonicated for 5 minutes to obtain small and uniform vesicles, and the obtained dried lipids were lyophilized The body powder was sieved through an 80-mesh sieve and stored at 4°C until use;

[0030] (2) Mixing: 1 g of li...

Embodiment 3

[0033] A preparation method of valacyclovir hydrochloride liposome tablet, comprising the following steps:

[0034] (1) Preparation of valacyclovir hydrochloride liposomes: Weigh 1 g of valacyclovir hydrochloride, 1 g of cholesterol and 8 g of soybean lecithin and dissolve them in a mixed solution of dichloromethane and methanol with a volume ratio of 3:1 , and then remove the solvent under vacuum at 60 °C on a rotary evaporator to obtain a thin film, and continue to evaporate for 2 hours to completely remove all traces of solvent and obtain a dry film; the dry film is added at 45 °C with an appropriate amount of 6g polyethylene. Pyrrolidone-K30 was hydrated in 20 mL of phosphate buffer for 15 minutes to obtain a liposome solution; the obtained liposomes were sonicated for 5 minutes to obtain small and uniform vesicles, and the obtained dried lipids were lyophilized The body powder was sieved through an 80-mesh sieve and stored at 4°C until use;

[0035](2) Mixing: Add 1 g of...

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PUM

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Abstract

The invention discloses a valaciclovir hydrochloride liposome tablet. The valaciclovir hydrochloride liposome tablet comprises valaciclovir hydrochloride liposome, a filler, an excipient, a disintegrating agent, an adhesive and a lubricant; and the valaciclovir hydrochloride liposome is composed of valaciclovir hydrochloride, cholesterol, soybean lecithin and polyvinylpyrrolidone-K30. The preparation method of the valaciclovir hydrochloride liposome tablet comprises the following steps: (1) preparing the valaciclovir hydrochloride liposome; (2) mixing; and (3) tabletting. The valaciclovir hydrochloride liposome tablet which is good in stability, excellent in disintegration performance and high in bioavailability is obtained by adopting specific auxiliary materials and selecting a proper proportion. The stability and bioavailability of the valaciclovir hydrochloride liposome tablet are far higher than those of the prior art, and great convenience is brought to clinical medication.

Description

technical field [0001] The invention relates to the technical field of medical science and technology, in particular to the preparation and application of a valacyclovir hydrochloride liposome tablet. Background technique [0002] Valacyclovir hydrochloride is L-valine-2-[(6-oxo-2-amino-1,6-dihydro-9H-purin-9-yl)methoxy]ethyl ester hydrochloride , the English name is Valaciclovir Hydrochloride. [0003] Valacyclovir hydrochloride is a prodrug of acyclovir (ACV), which is rapidly absorbed after oral administration and rapidly converted into acyclovir in the body. Its antiviral effect is caused by the action of the parent acyclovir. Ciclovir is an open-chain purine nucleoside that inhibits viral DNA synthesis and has less effect on host cell DNA synthesis. After acyclovir enters into herpes-infected cells, it competes with deoxynucleosides for viral thymidine kinase or cellular kinase, and the drug is phosphorylated into activated acyclovir triphosphate, which acts as a subs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/36A61K47/32A61K9/127A61K31/522A61P31/22
CPCA61K9/205A61K9/2027A61K9/127A61K31/522A61P31/22
Inventor 郝静梅
Owner 药大制药有限公司
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