Valnemulin hydrochloride microspheres and preparation method thereof

A technology of warnemulin hydrochloride and microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, block delivery, etc., to achieve high drug loading and encapsulation efficiency, increase blood drug concentration, and improve drug efficacy Effect

Active Publication Date: 2014-09-24
LINYI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the lung-targeted microsphere drug delivery system can also solve the problems of traditional non-targeted drug delivery, such as low solubility, poor stability or malabsorption, short half-life, wide distribution, and small therapeutic index.

Method used

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  • Valnemulin hydrochloride microspheres and preparation method thereof
  • Valnemulin hydrochloride microspheres and preparation method thereof
  • Valnemulin hydrochloride microspheres and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1 preparation example 1

[0033] Weigh 3g of gelatin, put it in a beaker, add 40mL of ultrapure water, and swell completely in a water bath at 60°C, then add 4g of micronized warnemulin hydrochloride (100-300 mesh) and 4g of PVP, mix and dissolve, and then drop into the container In a container with 2.4mL of Span 80 and 240mL of liquid paraffin, at 60°C with a stirring speed of 1000r·min -1 Stir electromagnetically for 20 minutes to make colostrum, quickly put it in an ice-water bath and lower the temperature to below 4°C, continue to emulsify and emulsify for 10 minutes, add 14 mL of 25% glutaraldehyde chemical cross-linking agent in a trickle, stir and cross-link for 1 hour, and use isopropyl Alcohol dehydration, washing, and suction filtration; then wash off the liquid paraffin on the surface of the microspheres with a small amount of petroleum ether, vacuum-dry for 24 hours, and sterilize by cobalt 60 ray irradiation to obtain pale yellow warnimulin hydrochloride lung-targeting microspheres.

[003...

Embodiment 2 preparation example 2

[0036] Weigh 3g of gelatin, put it in a beaker, add 20mL of ultra-pure water, and swell completely in a water bath at 60°C, then add 3g of micronized warnemulin hydrochloride (100-300 mesh) and 4.5g of PVP to mix and dissolve, then drop into the container In a container with 6mL of Span 80 and 240mL of liquid paraffin, at 60°C with a stirring speed of 800r·min -1 Stir electromagnetically for 20 minutes to make colostrum, quickly put it into an ice-water bath and lower the temperature to below 4°C, continue to stir and emulsify for 10 minutes, add 19.5mL of 25% glutaraldehyde chemical cross-linking agent in a trickle, stir and cross-link and solidify for 1 hour, use iso Dehydration with propanol, washing, and suction filtration; then wash off the liquid paraffin on the surface of the microspheres with a small amount of petroleum ether, vacuum-dry for 24 hours, and sterilize with cobalt-60 ray irradiation to obtain pale yellow warnimulin hydrochloride lung-targeting microspheres....

Embodiment 3

[0038] Example 4 Preparation example 4 of warnemulin hydrochloride microspheres

[0039] Weigh 1.5g of gelatin, put it in a beaker, add 20mL of ultrapure water, and swell completely in a water bath at 60°C, then add 2g of micronized warnemulin hydrochloride (100-300 mesh) and 4g of PVP, mix well and dissolve, and then drop into In a container containing 3.0mL of Span 80 and 200mL of liquid paraffin, at 65°C with a stirring speed of 900r·min -1 Stir electromagnetically for 20 minutes to make colostrum, quickly put it in an ice-water bath and lower the temperature to below 4°C, continue to emulsify and emulsify for 10 minutes, add 11 mL of 25% glutaraldehyde chemical cross-linking agent in a trickle, stir and cross-link for 1 hour, and use isopropyl Alcohol dehydration, washing, and suction filtration; then wash off the liquid paraffin on the surface of the microspheres with a small amount of petroleum ether, vacuum-dry for 24 hours, and sterilize by cobalt 60 ray irradiation ...

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Abstract

The invention relates to valnemulin hydrochloride microspheres and preparation method thereof. The valnemulin hydrochloride microspheres are composed of a water phase, an oil phase and a crosslinking agent, wherein a volume ration of the water phase to the oil phase is 1:6-12. The water phase is composed of gelatin, valnemulin hydrochloride, polyvinylpyrrolidone and purified water and the oil phase is composed of an emulsifier and liquid paraffin. The preparation method includes following steps: preparing the water phase and the oil phase, adding the water phase dropwisely to the oil phase, adding the crosslinking agent, washing off the liquid paraffin on surfaces of the microspheres through petroleum ether and performing a vacuum-drying process to obtain the valnemulin hydrochloride microspheres.

Description

technical field [0001] The invention relates to a warnemulin hydrochloride microsphere and a preparation method thereof. Background technique [0002] Valnemulin Hydrochloride (VAL) is a special pleuromutilin derivative for animals. The drug has a broad antibacterial spectrum and strong antibacterial activity. It is sensitive to bacteria, Mycoplasma and spirochetes, etc. , Pasteurella, Mycoplasma arthritis, Mycoplasma bovis, Mycoplasma galliseptica, Mycoplasma pneumoniae, Treponema hyodysenteriae and Treponema colon piliforme all have good antibacterial activity. It has been approved abroad for the prevention and treatment of diseases in pigs, cattle and sheep. However, wernemulin hydrochloride has a bitter taste, strong hygroscopicity, high irritation, relatively poor stability, is not easy to store, absorbs rapidly in the body, has a short half-life, and is widely distributed. At present, there is only one dosage form of warnemulin hydrochloride premix at home and abro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/32A61K31/22A61P31/04
Inventor 李振
Owner LINYI UNIVERSITY
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