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Small molecule hydrophilic drug-embedded sustained-release capsule and preparation method thereof

A hydrophilic drug and small molecule technology, 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, improving entrapment rate, and reducing diffusion.

Active Publication Date: 2014-12-24
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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  • Small molecule hydrophilic drug-embedded sustained-release capsule and preparation method thereof
  • Small molecule hydrophilic drug-embedded sustained-release capsule and preparation method thereof
  • Small molecule hydrophilic drug-embedded sustained-release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] A preparation method for embedding small molecule hydrophilic drug slow-release microcapsules, comprising the steps of:

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

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

[0079] (3) will W 1 / O-type primary emulsion is added to the external water phase W 2 , magnetically stirred at 300rpm for 1min to prepare W...

Embodiment 2

[0095] A preparation method for embedding small molecule hydrophilic drug slow-release microcapsules, comprising the steps of:

[0096] (1) Dissolve 20mg of starch in 1mL of water, then dissolve 1mg of recombinant human growth hormone (molecular weight 22kDa) in the above aqueous starch solution as the internal water phase W 1 , a mixture of 1 g 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) was dissolved in 5 mL of carbon disulfide as the oil phase O; with 50 mL of 0.1 wt % of polyglycerol fatty acid ester aqueous solution is the external water phase W 2 ; soak the hydrophilic membrane with a pore size of 0.5 μm in water to fully wet the porous membrane;

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

[009...

Embodiment 3

[0107] A preparation method for embedding small molecule hydrophilic drug slow-release microcapsules, comprising the steps of:

[0108] (1) Dissolve 200mg of a mixture of gum arabic and gelatin (mass ratio: 5:1) in 1mL of water, and then dissolve 50mg of doxorubicin (molecular weight: 543Da) in the above aqueous solution of gum arabic as the internal water phase W 1; The molecular weight of 0.1g is 40,000 polyorthoesters dissolved in 1mL chloroform, as oil phase O; With 4mL of 10wt% polyoxyethylene sorbitan monooleate aqueous solution as external water phase W 2 ; soak the hydrophilic membrane with a pore size of 200 μm in water to fully wet the porous membrane;

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

[0110] (3) will W 1 / O-type primary emulsion is added to the external water phase W 2 , magnetically st...

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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 sustained-release microcapsule embedding a small-molecule hydrophilic drug and a preparation method thereof, and further relates to a small-molecule hydrophilic drug embedded with a controllable size and a high embedding rate Sustained release microcapsules and preparation method thereof. Background technique [0002] Microencapsulation technology is a microcapsule with a diameter of 1-5000 μm formed by wrapping solid or liquid drugs (commonly known as capsule core) in natural or synthetic polymer materials (commonly known as capsule material), called microcapsules for short. (microcapsule). This preparation process is commonly known as microencapsulation (microencapsulation), referred to as microencapsulation. Those whose particle size is in the micrometer range are called microcapsules, and those whose particle size is in the nanometer range are called nanocapsules. [0003] After th...

Claims

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Application Information

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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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