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Protein polypeptide drug long-acting microspheres and preparation method thereof

A protein polypeptide and polypeptide technology, which is applied in pharmaceutical formulations, peptide/protein components, medical preparations with non-active ingredients, etc. problem, to achieve the effect of stable and long-lasting drug release rate, good reproducibility and low burst release rate

Active Publication Date: 2018-08-17
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The steps of this process are cumbersome, and due to the addition of the external water phase, it is easy to cause protein and polypeptide drugs to migrate out of the internal water phase, resulting in low microsphere encapsulation efficiency and high burst release rate.

Method used

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  • Protein polypeptide drug long-acting microspheres and preparation method thereof
  • Protein polypeptide drug long-acting microspheres and preparation method thereof
  • Protein polypeptide drug long-acting microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1: Preparation of bovine serum albumin microspheres

[0053] The preparation method of the bovine serum albumin microspheres of the present embodiment may further comprise the steps:

[0054] (1) Bovine serum albumin is dissolved in the aqueous solution that contains 20mg / mL mannitol, obtains the aqueous phase (W) that contains bovine serum albumin concentration and is 20mg / mL, the polylactic acid-glycolic acid copolymer ( PLGA, LA:GA=50:50, molecular weight 40000Da) was dissolved in a mixed solvent of dichloromethane and dimethyl carbonate 2:1 (v:v) to obtain an oil phase (O) with a polymer concentration of 50mg / mL ;

[0055] (2) Add the prepared water phase (bovine serum albumin aqueous solution) into the oil phase (PLGA organic solution) (the volume ratio of oil to water is 20:1), and use a cell disruptor in an ice bath with a power of 400W and a duration of 30s. Under the conditions, the two are emulsified to prepare W / O emulsion;

[0056] (3) The abov...

Embodiment 2

[0060] Embodiment 2: Preparation of bovine serum albumin microspheres

[0061] The preparation method of the bovine serum albumin microspheres of the present embodiment may further comprise the steps:

[0062] (1) Dissolve bovine serum albumin in an aqueous solution containing 20 mg / mL mannitol to obtain a water phase (W) containing bovine serum albumin at a concentration of 20 mg / mL. Polylactic acid-glycolic acid copolymer (PLGA , molecular weight 20000Da, LA:GA=50:50) is dissolved in the mixed solvent of dichloromethane and dimethyl carbonate 2:1 (v:v), obtains the oily phase (O) that polymer concentration is 50mg / mL;

[0063] (2) Add the prepared water phase (bovine serum albumin aqueous solution) into the oil phase (PLGA organic solution) (the volume ratio of oil to water is 20:1), and use a cell disruptor in an ice bath with a power of 400W and a duration of 30s. Under the conditions, the two are emulsified to prepare W / O emulsion;

[0064] (3) The above-mentioned W / O e...

Embodiment 3

[0066] Embodiment 3: Preparation of salmon calcitonin microspheres

[0067] The preparation method of the salmon calcitonin microspheres of the present embodiment comprises the steps:

[0068] (1) Dissolve salmon calcitonin in an aqueous solution containing 20 mg / mL mannitol to obtain a water phase (W) containing salmon calcitonin at a concentration of 20 mg / mL, polylactic acid-glycolic acid copolymer (PLGA, molecular weight 40000Da) was dissolved in a mixed solvent of dichloromethane and dimethyl carbonate 2:1 (v:v), to obtain an oil phase (O) with a polymer concentration of 50 mg / mL;

[0069] (2) Add the prepared water phase (salmon calcitonin aqueous solution) into the oil phase (addition of PLGA organic solution) (the volume ratio of oil to water is 20:1), and use the cell disruptor in an ice bath with a power of 400W and a duration of 30s Under certain conditions, the two are emulsified to prepare a W / O emulsion;

[0070] (3) The above-mentioned W / O emulsion is supplied...

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Abstract

The invention relates to protein polypeptide drug long-acting microspheres and a preparation method thereof. The preparation method comprises the steps of (1) dissolving a protein or polypeptide water-soluble drug and a protein protectant to obtain an aqueous drug solution; dissolving a macromolecular carrier material in an organic solvent to obtain an oil phase macromolecular solution; (2) addingthe aqueous drug solution into the oil phase macromolecular solution, and using a cell disrupter or a high-speed shear apparatus to prepare W / O emulsion; (3) feeding the W / O emulsion into a superfineparticle preparation system through a peristaltic pump so as to obtain the protein polypeptide drug long-acting microspheres. The protein polypeptide drug long-acting microspheres prepared via the preparation method have the advantages of good preparation process simplicity, controllable parameters, good reproducibility, and high production efficiency. The protein polypeptide drug long-acting microspheres prepared herein have the advantages of high drug encapsulating rate, low sudden release agent, stable and lasting release speed of drug, smooth microsphere surface, good spherical shape integrity, and homogenous particle size.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a long-acting microsphere of protein and polypeptide drugs and a preparation method thereof. Background technique [0002] Protein peptide drugs are currently the most widely used biological macromolecules. Because of their high potency, good biocompatibility, and low dose, they play an increasingly important role in the prevention, diagnosis, and treatment of diseases. As active substances with metabolic functions in organisms, protein and polypeptide drugs involve various fields such as hormones, nerves, cell growth and reproduction. Compared with traditional small molecule chemical drugs, protein peptide drugs have clear intrinsic effects, less toxic side effects, stronger pharmacological effects, fewer adverse reactions, and higher safety. Therefore, their research and development work has become one of the hot spots in the field of pharmaceutical research and devel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/113A61K38/00A61K39/00A61K38/38A61K38/23A61K47/34
CPCA61K9/113A61K9/16A61K38/00A61K38/23A61K38/385A61K39/00A61K47/34
Inventor 吴传斌李静朱春娥潘昕杨莉董妮
Owner SUN YAT SEN UNIV
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