Liquid crystal gel microcapsules and preparation method thereof

A technology of gel microcapsules and liquid crystals, applied in the field of medicine, can solve the problems that the preparation method cannot realize the industrialized production of nanoparticle dispersion system, lack of industrialized preparation method, prone to precipitation and aggregation, etc. Effects of storage, improved bioavailability, easy control of process parameters

Active Publication Date: 2018-07-20
武汉百纳礼康生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The industrialization and commercialization of liquid crystal nanoparticle preparations are mainly limited by two bottlenecks: one is the lack of efficient and feasible industrial preparation methods, and the other is the stability of the liquid crystal nanoparticle dispersion system
The huge specific surface area of ​​liquid crystal nanoparticles makes this dispersion system extremely unstable, prone to precipitation and aggregation, and the preparation method cannot realize the industrial production of nanoparticle dispersion sy

Method used

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  • Liquid crystal gel microcapsules and preparation method thereof
  • Liquid crystal gel microcapsules and preparation method thereof
  • Liquid crystal gel microcapsules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] This embodiment provides a liquid crystal gel microcapsule prepared by weight ratio from the following ingredients:

[0037]

[0038] The preparation method is as follows:

[0039] (1) Dissolving phosphatidylcholine, glyceryl dioleate and doxorubicin hydrochloride under the action of anhydrous ethanol as a cosolvent, and evaporated to remove ethanol after dissolving.

[0040] (2) Under stirring conditions, drop the above-mentioned phosphatidylcholine / diolein lipid solution containing doxorubicin hydrochloride into ultrapure water, and then continue to stir for a period of time.

[0041] (3) The solution in the step (2) is sheared at a high speed of 10000r / min for 2min;

[0042] (4) The solution in step (3) was subjected to high-pressure homogenization at a homogenization pressure of 300 bar, and the homogenization cycle was performed 3 times to obtain drug-loaded liquid crystal nanoparticles.

[0043] (5) Add 40 ml of drug-loaded liquid crystal nanoparticle solutio...

Embodiment 2

[0050] This embodiment provides a liquid crystal gel microcapsule prepared by weight ratio from the following ingredients:

[0051]

[0052] According to the preparation method of Example 1, liquid crystal gel microcapsules were prepared. The prepared liquid crystal gel microcapsule is tested, and the encapsulation rate is 80%, the particle size of the microcapsule is 3500-5000nm, and the PDI is less than 0.1.

Embodiment 3

[0054] This embodiment provides a liquid crystal gel microcapsule prepared by weight ratio from the following ingredients:

[0055] Phosphatidylcholine 2.1g

[0056] Glyceryl Dioleate 0.9g

[0057] Vitamin 0.45g

[0058] NSAIDs 0.2g

[0059] Sodium Alginate 2g

[0060] Calcium chloride 1g

[0061] According to the preparation method of Example 1, liquid crystal gel microcapsules were prepared. The prepared liquid crystal gel microcapsules were tested, and the encapsulation rate was 74%, the particle size of the microcapsules was 3000-5000nm, and the PDI was less than 0.15.

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Abstract

The invention discloses liquid crystal gel microcapsules and a preparation method thereof. The liquid crystal gel microcapsules are prepared from alginate, glyceryl dioleate and phosphatidylcholine, wherein glyceryl dioleate and phosphatidylcholine form liquid crystal nanoparticles in water; the microencapsulation preparation method of the liquid crystal nanoparticles comprises the steps of firstly, dissolving and dispersing medicines, phosphatidylcholine and glyceryl dioleate into a liquid crystal precursor solution in presence of a cosolvent, and adopting a high pressure homogenization method to obtain the medicine-loaded liquid crystal nanoparticles; then, evenly mixing the medicine-loaded liquid crystal nanoparticles with a sodium alginate solution, and dropwise adding a cross-linkingagent for carrying out a cross-linking reaction; then, freeze-drying to obtain the spherical alginate gel microcapsules. The method is simple and easy to implement, and is suitable for industrializedproduction; the capsule wall material adopted by the microcapsules is wide in source and low in price, thus being suitable for popularization of products; furthermore, the liquid crystal gel microcapsules has an obvious slow-release effect compared with the liquid crystal nanoparticles, and significantly improves the stability of the liquid crystal nanoparticles, so that the problem that the liquid crystal nanoparticles are difficult to store is solved to a certain extent.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a liquid crystal gel microcapsule and a preparation method thereof. Background technique [0002] Most pharmaceutically active compounds face the problem of low solubility. Research shows that 40% of marketed drugs and 70% of drugs under research are poorly soluble drugs. The slow dissolution rate and low dissolution degree of poorly soluble drugs lead to low bioavailability of drugs and fail to achieve ideal clinical efficacy. The drug must be delivered to the treatment site at a certain speed and reach a therapeutic concentration in order to exert its curative effect in time. This process requires the use of pharmaceutical preparations to increase the dissolution rate and solubility of the drug, thereby increasing the bioavailability of the drug and improving the clinical efficacy. The rate and route of drug dissolution and release from formulations are mainly reg...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/36A61K9/127A61K47/24A61K47/14A61K45/00A61K31/704
CPCA61K9/1274A61K9/5036A61K31/704A61K45/00A61K47/14A61K47/24
Inventor 罗亮王修霞孟凡玲
Owner 武汉百纳礼康生物制药有限公司
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