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Protein-medicament-carrying PLGA composite microspheres and preparation method thereof

A technology of composite microspheres and proteins, which is applied in the fields of peptide/protein components, pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve the problems of difficult to meet treatment needs, obvious drug burst release phenomenon, and low blood drug concentration levels. , to prolong the action time of the drug, the preparation process is stable, and the fluidity is good.

Inactive Publication Date: 2012-10-17
THE THIRD AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The most commonly used preparation process is the solvent evaporation method. The microspheres prepared by this method have a better encapsulation efficiency and are easy to release the drug, but the drug release phenomenon is obvious, showing a two-phase release, that is, only a very low blood drug concentration can be maintained in the later stage. Difficulty meeting treatment needs

Method used

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  • Protein-medicament-carrying PLGA composite microspheres and preparation method thereof
  • Protein-medicament-carrying PLGA composite microspheres and preparation method thereof
  • Protein-medicament-carrying PLGA composite microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of embodiment 1 interferon PLGA composite microsphere

[0046] (1) Preparation of PLGA solution

[0047] 600 mg PLGA was dissolved in 4 ml dichloromethane to form an organic phase (15% g / ml).

[0048] (2) Preparation of interferon sodium alginate solution

[0049] Dissolve 6 mg of lyophilized recombinant human interferon-α in 300 ul of a solution containing 1% poloxamer 188 and 1.5% (g / ml) sodium alginate to form an inner aqueous phase;

[0050] (3) Preparation of colostrum

[0051] Inject the inner aqueous phase into the organic phase, stir and emulsify for 1 minute at 10,000 rpm to form colostrum (W / O);

[0052] (4) Preparation of double emulsion

[0053] Add colostrum to the mixture containing 2.5% (g / ml) PVA and 3.0% (g / ml) CaCl under the condition of stirring at 1800rpm 2 In the solution (outer water phase 1), emulsify for 10 minutes to form double emulsion (W / O / W); wherein the ratio of colostrum to outer water phase 1 is 1:40;

[0054] (5) Fo...

Embodiment 2

[0061] Example 2 Preparation of Interferon PLGA Composite Microspheres

[0062] (1) Preparation of PLGA solution

[0063] 600 mg PLGA was dissolved in 4 ml dichloromethane to form an organic phase (15% g / ml).

[0064] (2) Preparation of interferon sodium alginate (Sa) solution

[0065] Dissolve 6 mg of lyophilized recombinant human interferon-α in 300 ul of a solution containing 1% poloxamer 407 and 0.8% (g / ml) sodium alginate to form an inner aqueous phase;

[0066] (3) Preparation of colostrum

[0067] Inject the inner aqueous phase into the organic phase, stir and emulsify at 5000rpm for 10 minutes to form colostrum (W / O);

[0068] (4) Preparation of double emulsion

[0069] Add colostrum to the mixture containing 2.5% (g / ml) PVA and 1.5% (g / ml) CaCl under the condition of stirring at 1600rpm 2 In the solution (outer water phase 1), emulsify for 10 minutes to form double emulsion (W / O / W); wherein the ratio of colostrum to outer water phase 1 is 1:60;

[0070] (5) Form...

Embodiment 3

[0076] Example 3 Preparation of Interferon PLGA Composite Microspheres

[0077] (1) Preparation of PLGA solution

[0078] 800 mg PLGA was dissolved in 4 ml dichloromethane to form the organic phase (20% g / ml).

[0079] (2) Preparation of interferon sodium alginate solution

[0080] Dissolve 6 mg of lyophilized recombinant human interferon-α in 300 ul of a solution containing 1% poloxamer 188 and 0.5% (g / ml) sodium alginate to form an inner aqueous phase;

[0081] (3) Preparation of colostrum

[0082] Inject the above-mentioned internal aqueous phase into the above-mentioned organic phase, stir and emulsify at 18000rpm for 1 minute to form colostrum (W / O);

[0083] (4) Preparation of double emulsion

[0084] Add colostrum to the mixture containing 2.5% (g / ml) PVA and 1.5% (g / ml) CaCl under the condition of stirring at 2500rpm 2 In the solution (outer water phase 1), emulsify for 15 minutes to form double emulsion (W / O / W); wherein the ratio of colostrum to outer water phase...

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Abstract

The invention discloses protein-medicament-carrying PLGA composite microspheres and a preparation method thereof. According to the invention, an improved multiple emulsion-solvent evaporation method is adopted. On the basis of a multiple emulsion method, a principle that sodium alginate and calcium ions are subjected to chelating and form sustained-release gel is adopted; PLGA is adopted as a microsphere carrier; lyophilized injection-use recombinant human interferon-alpha, bovine serum albumin and the like are adopted as encapsulation objects; and the medicament-carrying microspheres are prepared. The microspheres are advantaged in round appearance, and uniform particle size distribution. An average particle size distribution is 70 micrometers, a medicament-carrying rate is above 0.6%, an encapsulation rate reaches approximately 50%, and an in-vitro medicament releasing performance satisfies the characteristic of prolonged-action preparations.

Description

technical field [0001] The invention relates to a polylactic acid-glycolic acid copolymer (PLGA) composite microsphere loaded with protein drugs and a preparation method thereof, which belongs to the cross research field of biomedical polymer materials and bioactive drug controlled release preparations. Background technique [0002] In recent years, with the development of genetic engineering recombination technology and proteomics, peptide and protein drugs have become the most active and fastest-growing part of the current pharmaceutical research and development field. Many new peptide and protein drugs are used in the treatment of AIDS, cancer, It is effective in diseases such as hepatitis, diabetes, and chronic pain, and it also plays an important role in diagnosis and vaccine prevention of diseases. Due to the instability of such drugs in vivo and in vitro, the main clinical dosage forms are solution injections and freeze-dried powder injections. After injection, the d...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K47/34A61K47/04A61K38/21A61K38/38A61K9/19
Inventor 张永明罗宇燕李姝瑾
Owner THE THIRD AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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