A kind of microcapsules for encapsulation of small molecule hydrophilic drug sustained release and preparation method thereof

A technology of hydrophilic drugs and small molecules, which is applied in the field of medicine, can solve the problems of low burst release rate, low drug loading, and high burst release rate, and achieve the effects of reducing drug burst release, increasing embedding rate, and reducing diffusion

Active Publication Date: 2017-02-08
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In view of the fact that the existing microencapsulation technology cannot solve the problems of low embedding rate, low drug loading capacity, high burst release rate, and large side effects of small molecule hydrophilic drugs, a uniform size, high embedding rate, and low Long-acting sustained-release microcapsules embedding small-molecule hydrophilic drugs with burst release rate and preparation method thereof

Method used

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  • A kind of microcapsules for encapsulation of small molecule hydrophilic drug sustained release and preparation method thereof
  • A kind of microcapsules for encapsulation of small molecule hydrophilic drug sustained release and preparation method thereof
  • A kind of microcapsules for encapsulation of small molecule hydrophilic drug sustained release and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] A preparation method of microcapsules with embedded small-molecule hydrophilic drugs, including the following steps:

[0077] (1) Dissolve 300 mg of gelatin in 1 mL of water, and then dissolve 40 mg of triptorelin acetate in the above aqueous gelatin solution as the internal water phase W 1 ; Dissolve 0.1 g of polylactic acid-glycolic acid copolymer (PLGA) with a molecular weight of 60,000 in 10 mL of dichloromethane (MC) as the oil phase O; take 50 mL of 0.1wt% polyvinyl alcohol (PVA) aqueous solution as Outer water phase W 2 ; Place a hydrophilic membrane with a pore size of 50.2μm in water to soak the pore membrane fully;

[0078] (2) The internal water phase W 1 Add to the oil phase O, homogenize and emulsify for 30s to obtain W 1 / O type primary emulsion; among them, the internal water phase W 1 The volume ratio to oil phase O is 1:10;

[0079] (3) Put W 1 / O type primary emulsion is added to the outer water phase W 2 Medium, magnetic stirring 300rpm stirring 1min to prep...

Embodiment 2

[0095] A preparation method of microcapsules with embedded small-molecule hydrophilic drugs, including the following steps:

[0096] (1) Dissolve 20 mg of starch in 1 mL of water, and then dissolve 1 mg of recombinant human growth hormone (molecular weight 22kDa) in the above aqueous starch solution as the internal water phase W 1 , Dissolve 1g of a mixture of polylactic acid with a molecular weight of 10,000 and a polylactic acid-polyglycolic acid copolymer with a molecular weight of 10,000 (mass ratio 1:1) in 5mL of carbon disulfide as the oil phase O; take 50mL of 0.1wt % Of polyglycerol fatty acid ester aqueous solution is the outer water phase W 2 ; Place a hydrophilic membrane with a pore size of 0.5μm in water to soak the pore membrane fully;

[0097] (2) The internal water phase W 1 Add to the oil phase O, homogenize and emulsify for 30s to obtain W 1 / O type primary emulsion; among them, the internal water phase W 1 The volume ratio with oil phase O is 1:5;

[0098] (3) Put ...

Embodiment 3

[0107] A preparation method of microcapsules with embedded small-molecule hydrophilic drugs, including the following steps:

[0108] (1) Dissolve 200 mg of a mixture of gum arabic and gelatin (mass ratio 5:1) in 1 mL of water, and then dissolve 50 mg of adriamycin (molecular weight 543Da) in the above gum arabic aqueous solution as the internal water phase. 1 ; 0.1g of polyorthoester with a molecular weight of 40,000 was dissolved in 1mL of chloroform as the oil phase O; 4mL of 10wt% polyoxyethylene sorbitan monooleate aqueous solution was used as the outer water phase W 2 ; Place a hydrophilic membrane with a pore size of 200μm in water so that the pore membrane is fully wetted;

[0109] (2) The internal water phase W 1 Add to the oil phase O, homogenize and emulsify for 30s to obtain W 1 / O type primary emulsion; among them, the internal water phase W 1 The volume ratio to oil phase O is 1:1;

[0110] (3) Put W 1 / O type primary emulsion is added to the outer water phase W 2 Medium,...

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Abstract

The invention relates to a method for preparing a small molecule hydrophilic drug-embedded sustained-release capsule. The method comprises the following steps: filtering a prepared'internal aqueous phase / oil phase / external aqueous phase' pre-multi-emulsion solution through a microporous membrane; and then removing a solvent, washing and drying to obtain the small molecule hydrophilic drug-embedded sustained-release capsule, wherein the internal aqueous phase comprises a small molecule hydrophilic drug and a thickening agent. The small molecule hydrophilic drug-embedded sustained-release capsule provided by the invention has the advantages of uniform grain diameter, high embedding rate, low burst-release rate, stable drug release and long action.

Description

Technical field [0001] The invention belongs to the field of medicine, and relates to a microcapsule containing small-molecule hydrophilic drugs and a preparation method thereof, and further relates to a small-molecule hydrophilic drug with a controllable size and a high embedding rate. Sustained-release microcapsules and preparation method thereof. Background technique [0002] Microencapsulation technology is to wrap solid or liquid drugs (commonly known as capsule cores) in natural or synthetic polymer materials (commonly referred to as capsules) to form tiny capsules with a diameter of 1 to 5000μm, which are called microcapsules and abbreviated as microcapsules. (Microcapsule). This preparation process is known as microencapsu lation, or microencapsulation for short. Those with a particle size in the micron range are called microcapsules, and those with a particle size in the nanometer range are called nanocapsules. [0003] After the drug is microencapsulated, the following...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K45/00A61K47/42A61K47/36A61K47/40A61K47/38
Inventor 王玉霞马光辉王宁韦祎苏志国
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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