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Preparation method of drug-loaded lipid microparticles

A microparticle and drug-loaded technology, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, and medical preparations containing active ingredients, etc. Encapsulation rate and other issues, to achieve the effect of a wide range of dosage forms, reduce the burst release effect, and improve the encapsulation rate

Active Publication Date: 2016-01-20
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The existing lipid particles are generally in a liquid state, and their storage and transportation are relatively difficult, and they are easily affected by changes in environmental conditions, causing problems such as flocculation, agglomeration, precipitation, drug leakage, etc., and the action time in the body is relatively short , affecting the effectiveness, safety and stability of the formulation
In addition, lipid microparticles are better for encapsulating fat-soluble drugs, while the encapsulation efficiency of lipid microparticles is low when encapsulating water-soluble drugs, and usually cannot meet the minimum requirement of 80% encapsulation efficiency
However, the technical operation adopted to improve the encapsulation efficiency of water-soluble drugs is relatively cumbersome and has poor reproducibility, making it difficult to prepare in industrialized batches.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Recombinant Human Growth Hormone Lipid Microparticles

[0027] The first embodiment of the present invention adopts recombinant human growth hormone, a protein drug, as the object, the amphiphilic polymer material selects Poloxamer (Poloxamer188), and the lipid particle film-forming material selects cetyl alcohol, Tween 80 and propylene glycol , to prepare lipid microparticles loaded with recombinant human growth hormone.

[0028] Experimental group: Dissolve 15mg of Poloxamer (Poloxamer188) in 6ml of water, add 1ml of recombinant human growth hormone (3mg / ml) and mix completely, put in a vial, freeze at -30°C for 5 hours, freeze-dry (5×10 -4 Pa, 20h) to obtain a solid-state freeze-dried product of recombinant human growth hormone. Dissolve 5mg of cetyl alcohol, 2mg of Tween 80 and 3mg of propylene glycol in 20ml of tert-butanol, dissolve in a water bath at 65°C, add solid-state lyophilized product of recombinant human growth hormone, dissolve completely, ad...

Embodiment 2

[0033] Embodiment 2: Diclofenac Sodium Lipid Microparticles

[0034] The second embodiment of the present invention adopts diclofenac sodium as the target drug, the amphiphilic macromolecular material selects povidone (PVP), and the lipid particle film-forming material selects stearic acid and Tween 80 to prepare diclofenac sodium entrapped lipid particles.

[0035] Experimental group: 20mg of povidone (PVP) was dissolved in 6ml of water, 8mg of diclofenac sodium was added to dissolve completely, packed in a vial, frozen at -30°C for 5 hours, freeze-dried (5×10 -4 Pa, 20h) to obtain diclofenac sodium solid freeze-dried product. Dissolve 20mg of stearic acid and 4mg of Tween 80 in 20ml of tert-butanol, dissolve in a 65°C water bath, add diclofenac sodium solid-state lyophilized product, dissolve completely, add 200mg of mannitol (PVP), disperse evenly, and put it in a vial Freeze at -30°C for 5 hours, freeze-dry (5×10 -4 Pa, 24h) to obtain a solid-state lyophilized product o...

Embodiment 3

[0041] Embodiment 3: Adriamycin Hydrochloride Lipid Microparticles

[0042] The third embodiment of the present invention adopts doxorubicin hydrochloride as the target drug, the amphiphilic macromolecular material polyethylene glycol (PEG2000), and the lipid particle film-forming material is selected from glycerol monostearate and Span 80 to prepare Lipid microparticles loaded with doxorubicin hydrochloride.

[0043] Experimental group: 15 mg of polyethylene glycol (PEG2000) was dissolved in 6 ml of water, 5 mg of doxorubicin hydrochloride was added to dissolve completely, packed in a vial, frozen at -30°C for 5 hours, and freeze-dried (5×10 -4 Pa, 20h) to obtain adriamycin hydrochloride solid freeze-dried product. Add 15mg glyceryl monostearate and 4mg Span 80 into 20ml tert-butanol, dissolve in a 65°C water bath, add adriamycin hydrochloride solid freeze-dried product, add 180mg polyethylene glycol (PEG2000), disperse evenly, pack Freeze at -30°C for 5 hours in a vial, fr...

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PUM

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Abstract

The invention relates to a preparation method of drug-carrying lipoid particles. In the method, a two-step freeze-drying mode is used for preparing the lipoid particles for coating and carrying water soluble drugs, wherein a primary freeze drying process is performed in a water phase system, and a secondary freeze drying process is performed in an organic phase system. The water soluble drugs are evenly coated and carried in the lipoid particles by the two-step freeze drying method, thus improving the envelopment rate of the drugs and reducing the initial burst release effect of the lipoid particles for coating and carrying the water soluble drugs. The lipoid particles prepared by the preparation method are suitable for coating various kinds of water soluble drugs and have a wide range of applicable dosage forms.

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-loaded 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 the rapi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/32A61K47/34A61K45/00A61K47/10
Inventor 鲁翠涛赵应征
Owner ZHEJIANG HISUN PHARMA CO LTD
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