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Preparation method of encapsulated drug lipid microparticles

A technology of encapsulating drugs and particles, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, powder delivery, etc., to achieve the effects of reducing burst release effects, reducing leakage, and being applicable to a wide range of dosage forms

Active Publication Date: 2014-10-15
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved in the present invention is to provide a solution for the shortcomings of the existing preparation of drug-loaded lipid particles

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: Diclofenac Sodium Lipid Microparticles

[0028] The first embodiment of the present invention adopts the water-soluble drug diclofenac sodium as the target drug, the amphiphilic polymer material selects povidone (PVP), adopts the melting method to prepare the diclofenac sodium-polyvidone solid dispersion, and the lipid particles form Cholesterol, cetyl alcohol, Tween 80 and propylene glycol are selected as membrane materials, and the lipid microparticles encapsulating diclofenac sodium are prepared by a freeze-drying method.

[0029] Experimental group: 30mg of povidone (PVP) was melted in a water bath at 65°C, and 8mg of diclofenac sodium was added to disperse evenly, and transferred to an ice bath at 0°C for quenching treatment to prepare a solid dispersion of diclofenac sodium-povidone. 10mg of cholesterol, 2mg of cetyl alcohol, 2mg of Tween 80 and 4mg of propylene glycol were dissolved in 20ml of tert-butanol, dissolved in a water bath at 65°C, added d...

Embodiment 2

[0035] Example 2: Paclitaxel Lipid Microparticles

[0036]The second embodiment of the present invention adopts fat-soluble drug paclitaxel as target drug, amphiphilic polymer material polyethylene glycol (PEG 2000), adopts solvent-melt method to prepare paclitaxel-polyethylene glycol solid dispersion, lipid Stearic acid and Tween 80 were selected as the microparticle film-forming materials, and lipid microparticles loaded with paclitaxel were prepared by an injection method.

[0037] Experimental group: add 30mg of polyethylene glycol (PEG 2000) into 0.5ml of absolute ethanol, melt in a water bath at 65°C, add 5mg of paclitaxel to disperse evenly, transfer to 0°C for quenching in an ice bath, and make paclitaxel-polyethylene glycol Alcoholic solid dispersion. 10 mg of stearic acid was dissolved in a mixed solvent of 20 ml of chloroform:methanol (3:1, V / V), and paclitaxel-polyethylene glycol solid dispersion was added to disperse evenly to form an organic phase. Take 10 mg o...

Embodiment 3

[0042] Embodiment 3: Irinotecan Hydrochloride Lipid Nanoparticles

[0043] The third embodiment of the present invention adopts irinotecan hydrochloride as the target drug, the amphiphilic polymer material selects poloxamer (Poloxamer 188), and adopts the melting method to prepare irinotecan hydrochloride-poloxamer solid dispersion, The film-forming materials of lipid microparticles were selected from glycerol monostearate, Span 80 and glycerin, and the lipid nanoparticles loaded with irinotecan hydrochloride were prepared by high-pressure homogenization method.

[0044] Experimental group: 55 mg of poloxamer (Poloxamer 188) was melted in a water bath at 65°C, and 5 mg of irinotecan hydrochloride was added to disperse evenly to obtain a solid dispersion of irinotecan hydrochloride-poloxamer. Add 15mg glyceryl monostearate, 3mg Span 80 and 6mg glycerin to 15ml 80°C water, add irinotecan hydrochloride-poloxamer solid dispersion, emulsify four times with a high-pressure homogeniz...

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PUM

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Abstract

The invention relates to a method for preparing medicine-encapsulating lipoid particles, which comprises the following steps of: preparing medicinal solid dispersoid, and dispersing the medicinal solid dispersoid and a film-forming material of the lipoid particles in organic solvent uniformly to prepare the medicine-encapsulating lipoid particles, so that medicines are encapsulated in the lipoid particles uniformly, the envelop rate of the medicines is improved, and the burst effect of the medicine-encapsulating lipoid particles is reduced. The medicine-encapsulating lipoid particles are suitable for encapsulating various medicines, and are wide in range of applicable formulations.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, the invention relates to a preparation method of drug-encapsulated lipid microparticles. 【Background technique】 [0002] Lipid particles are derived from liposomes. Liposomes, also known as niosomes, refer to single-layer or multi-layer new drug carrier single-layer vesicles made of lipid materials such as non-ionic surfactants. Higher than liposomes, it can overcome the toxicity of liposomes caused by phospholipid oxidation, and thus become a promising new drug delivery system. [0003] Liposomes are used to encapsulate drugs, which can reduce or reduce the impact of environmental factors on drugs, prolong the effective time of drugs in vivo, improve the effective bioavailability of drugs in vivo, and reduce the toxic and side effects of drugs, especially for Targeted therapy of biologically active macromolecular drugs and heat-labile drugs. [0004] With th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/32A61K9/14
Inventor 鲁翠涛赵应征
Owner ZHEJIANG HISUN PHARMA CO LTD
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