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Preparation method of protein drug long-acting preparation using polyketal as matrix

A polyketal and drug technology, applied in the field of medicine, can solve the problems of incomplete release and low bioavailability of long-acting sustained-release preparations, and achieve low bioavailability, improved stability, improved release and bioavailability degree of effect

Inactive Publication Date: 2014-08-13
李又欣 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides a preparation method of a long-acting preparation of protein drugs using polyketal as a matrix. The polyketal is used as a matrix to avoid the disadvantages of acidic degradation products to protein activity during storage and release of common protein long-acting preparations. Impact, solves the problem of incomplete release and low bioavailability of long-acting sustained-release formulations of protein drugs

Method used

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  • Preparation method of protein drug long-acting preparation using polyketal as matrix
  • Preparation method of protein drug long-acting preparation using polyketal as matrix
  • Preparation method of protein drug long-acting preparation using polyketal as matrix

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Experimental program
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Effect test

Embodiment 1

[0029] Weigh 60mg of BSA protein, dissolve it in 150ul 1%PVA, this is the inner water phase; weigh 400mg of PLGA50507A and polyketal PCADK 100mg, dissolve it in 2.25ml of dichloromethane, this is the oil phase; add the inner water phase to the oil phase In the process, homogenize at 10000rpm for 30s to form colostrum, slowly and uniformly add colostrum into 100ml 1%NaCl 1%PVA solution, and homogenize with a homogenizer at 7500rpm for 30s to form double milk. Stir the double emulsion for 3 hours, wait for the organic solvent to evaporate completely, wash and collect the microspheres, freeze-dry and store at 4°C to obtain a long-acting preparation of BSA protein drugs. figure 1 . Its fluorescence spectrum see figure 2 ; In vitro release rate-time curve of microspheres see image 3 , conclusion: the shape of the microspheres is round and uniform, the mechanical properties are strong, and the release is relatively complete.

Embodiment 2

[0031] Weigh 60mg of BSA, dissolve in 150ul 1%PVA, this is the internal water phase; weigh 350mg of PLGA75257E and polyketal PCADK 150mg, dissolve in 2.25ml of dichloromethane, this is the oil phase; add the internal water phase to the oil phase , perform homogenization at 10000rpm for 30s to form colostrum, slowly and uniformly add colostrum into 100ml 1%NaCl 1%PVA solution, and homogenize at 10000rpm for 30s with a homogenizer to form double emulsion. Stir the double emulsion for 3 hours, wait for the organic solvent to evaporate completely, wash and collect the microspheres, freeze-dry and store at 4°C to obtain a long-acting preparation of BSA protein drugs. Figure 4 . Its fluorescence spectrum see Figure 5 ; In vitro release rate-time curve of microspheres see Figure 6 , conclusion: the shape of the microspheres is round and uniform, the mechanical properties are strong, and the release is relatively complete.

Embodiment 3

[0033] 200ul 65mg / ml desalted recombinant human growth hormone (rHGH) solution is the inner water phase; weigh PLGA5050 3A 400mg and polyketal PCADK 100mg and dissolve it in 2ml dichloromethane, this is the oil phase; add the inner water phase to the oil phase In the process, homogenize at 4000rpm for 90s to form colostrum, slowly and uniformly add colostrum into 100ml 4%NaCl 1%PVA solution, and homogenize with a homogenizer at 4000rpm for 120s to form double milk. Stir the double emulsion for 3 hours, wait for the organic solvent to evaporate completely, wash and collect the microspheres, freeze-dry and store at 4°C to obtain a long-acting preparation of recombinant human growth hormone (rHGH). Figure 7 . Its fluorescence spectrum see Figure 8 ; In vitro release rate-time curve of microspheres see Figure 9 , conclusion: the shape of the microspheres is round and uniform, the mechanical properties are strong, and the release is relatively complete.

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Abstract

The invention discloses a preparation method of a protein drug long-acting preparation using polyketal as a matrix; the polyketal as the matrix is mixed with a biodegradable polymer material to prepare the protein-drug-packaging long-acting preparation, wherein the mass ratio of polyketal to other biodegradable polymer material is 9:1-1:9, and the mass ratio is preferably 4:6-2:8; the polyketal is used as the matrix to avoid adverse effects of acidic degradation products on protein activity in the storage and release process of a common protein long-acting preparation, and the problems of incomplete release and low bioavailability of the protein drug long-acting sustained-release preparation can be solved, addition of other biodegradable polymer material provides mechanical support and ensures molding of the protein drug long-acting sustained-release preparation. The protein drug long-acting preparation is rounding and uniform in micro spherical morphology, strong in mechanical properties and more complete in release.

Description

technical field [0001] The invention provides a preparation method of a protein drug long-acting preparation with a polyketal as a matrix, belonging to the technical field of medicine. Background technique [0002] With the development of genomics and proteomics, protein drugs can be produced in large quantities through recombination, and the use of transgenic animals and plants also makes mass production possible. At present, more than 40 important therapeutic drugs have been launched, and more than 720 biotechnology drugs are undergoing phase I-III clinical trials or undergoing FDA review, of which more than 200 drugs are entering the final approval stage. However, due to the limitations of protein drugs themselves, their clinical therapeutic effects are limited. How to effectively and stably deliver protein drugs to the site of action is a worldwide problem. Therefore, the effective delivery system of protein drugs is one of the most promising fields, but also the most c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K38/27A61K38/38
Inventor 李又欣孙凤英王晨晖余昌会
Owner 李又欣
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