Ternary composite microsphere formulation and its preparation method

A technology of composite microspheres and preparations, applied in the field of pharmacy, can solve the problems of activity change and difficulty in improving the encapsulation rate, and achieve the effect of improving the encapsulation rate, good drug release mode, and reducing incomplete release

Inactive Publication Date: 2004-12-29
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, hydrophobic materials have a slow-release effect, but they are incompatible with water-soluble proteins and polypeptide drugs, which will cause the stretching of the natural protein structure in the folded state, resulting in a change in activity, and the encapsulation efficiency is also very low. Difficult to improve

Method used

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  • Ternary composite microsphere formulation and its preparation method
  • Ternary composite microsphere formulation and its preparation method
  • Ternary composite microsphere formulation and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 A kind of preparation method of composite microsphere of the present invention

[0031] (1) Preparation of calcium alginate microcapsules: using BSA as a model drug, dissolve BSA with a small amount of distilled water and mix well with 1% sodium alginate solution. The first emulsifier is Span 80, which is soluble in isooctane 5% (w / v), the volume ratio of the two phases is 1:2, the high-speed milking speed is 12000rpm, and the time is 3 minutes, then add the second emulsifier, namely Tween 80, and the concentration is 30% (w / w) , the dosage is 45% of Span 80, and then milk for 3 minutes, add cross-linking agent calcium chloride solution, the concentration is 8% (w / v), and then milk for 3 minutes, add isopropanol to separate out the extraction of microcapsules The time is 2 minutes. Calcium alginate microcapsules were prepared after centrifugation.

[0032] (2) Preparation of calcium alginate-chitosan microspheres: the above-mentioned calcium alginate micr...

Embodiment 2

[0035] Embodiment 2 The second preparation method of composite microspheres of the present invention

[0036] The rotational speed of the two-phase high-speed emulsion in the first step is 5000rpm; the particle size of the double-layer composite microcapsules obtained in the second step is <8 μm; the particle size of the microspheres obtained in the third step is <50 μm; the rest of the steps are the same as in Example 1.

Embodiment 3

[0037] Embodiment 3 The 3rd kind of preparation method of composite microsphere of the present invention

[0038] In the first step, the rotation speed of the two-phase high-speed emulsion is 20000rpm, the particle size of the double-layer composite microcapsules obtained in the second step is <2 μm, and the particle size of the microspheres obtained in the third step is <30 μm, and the rest of the steps are the same as in Example 1.

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Abstract

The triple composite microsphere preparation consists of mainly model medicine, calcium alginate, chitosan, and diglycolide-lactide copolymer. The preparation process includes W / O emulsification, washing with isopropanol to prepare small calcium alginate microcapsule, coating with chitosan to form compact double-layered alginic acid-chitonsan microcapsule, the subsequent emulsifying and solvent volatilization step to coat the double-layered alginic acid-chitonsan microcapsule into diglycolide-lactide copolymer to form the three-layered composite microsphere. The present invention can protect protein and polypeptide medicine in hydrophilic sodium alginate-chitonsan microcapsule environment to reduce abrupt release and incomplete release, prolong the medicine release time, and regulate the medicine releasing mode via altering PLGA composition.

Description

Technical field [0001] The invention belongs to the field of pharmacy, and relates to a biodegradable microcapsule and microsphere preparation and a preparation method thereof, in particular to a calcium alginate-chitosan-glycolide-lactide copolymer triple composite microsphere preparation and a preparation method thereof. This new compound preparation is of great significance to solving the bottleneck problem of protein vaccine administration. technical background [0002] Vaccination is the most effective public health measure against infectious diseases other than the provision of purified water. It’s just that some vaccines such as hepatitis B vaccine and tetanus vaccine often need to be inoculated 2-3 times to achieve the expected immune effect. Therefore, complete immunization upon first vaccination is one of the main goals of the World Health Organization's vaccine development programme. The development of a single-dose vaccine that provides full immunity with a sin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/62B01J13/02
Inventor 梁文权郑彩虹
Owner ZHEJIANG UNIV
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