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Octreotide sustained-release microspheres with high encapsulation rate and preparation method thereof

A technology of slow-release microspheres and octreotide, which is applied in the direction of pharmaceutical formulations, peptide/protein ingredients, and medical preparations of non-active ingredients, etc., can solve problems such as unsatisfactory results, and achieve round shape, smooth surface, and excellent preparation technology. stable effect

Active Publication Date: 2013-02-27
SHANGHAI SOHO YIMING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A large number of studies and literatures have reported methods to improve the encapsulation efficiency of octreotide microspheres, such as using polyvinyl alcohol as the continuous phase emulsifier, pure water as the continuous phase solvent, and sucrose as the dispersed phase protective agent, but the results are not satisfactory

Method used

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  • Octreotide sustained-release microspheres with high encapsulation rate and preparation method thereof
  • Octreotide sustained-release microspheres with high encapsulation rate and preparation method thereof
  • Octreotide sustained-release microspheres with high encapsulation rate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Prescription process composition:

[0026] Prescription process content or ratio Octreotide: PLGA(w / w) (PLGA Mw=38000, 50:50poly, i.v.=0.61dL / g) 1:5.6 Trehalose: Octreotide (w / w) 1:2 Continuous phase pH 7.92 Polyvinyl alcohol (mg / ml) 10 Polysorbate 80(mg / ml) 0.2

[0027] The preparation method of octreotide sustained-release microspheres is as follows:

[0028] Dissolve 196mg PLGA in dichloromethane as the oil phase; dissolve 35mg octreotide and stabilizer trehalose 17.5mg in water as the dispersed phase; dissolve 400mg polyvinyl alcohol and 8mg polysorbate 80 in 40ml phosphate buffer as the solvent for the continuous phase; mix and oscillate the dispersed phase with the oil phase to form colostrum, add the colostrum to the continuous phase under stirring to form double emulsion; then quickly transfer the double emulsion to phosphate buffer, stir magnetically until the dichloromethane volatilizes Completely, filter and coll...

Embodiment 2

[0040] Prescription process composition:

[0041] Prescription process content or ratio Octreotide: PLGA(w / w) (PLGA Mw=38000, 50:50poly, i.v.=0.61dL / g) 1:8 Trehalose: Octreotide (w / w) 1:3 Continuous phase pH 7.8 Polyvinyl alcohol (mg / ml) 20 Polysorbate 80(mg / ml) 0.4

[0042] The preparation method of octreotide sustained-release microspheres is as follows:

[0043]Dissolve 196mg of PLGA in dichloromethane as the oil phase; dissolve 24.5mg of octreotide in water as the dispersed phase, which contains 2.45mg of stabilizer trehalose; dissolve 800mg of polyvinyl alcohol and 16mg of polysorbate in 40ml of phosphate buffer as the solvent 80 is the continuous phase; the dispersed phase and the oil phase are mixed and shaken to form colostrum, then added to the continuous phase under stirring to form double emulsion, and then quickly transferred to a certain volume of phosphate buffer, magnetically stirred until the dichloromethane volatil...

Embodiment 3

[0046] Prescription process composition:

[0047] Prescription process content or ratio Octreotide: PLGA(w / w) (PLGA Mw=79300, 75:25poly, i.v.=0.55dL / g) 1:10 Trehalose: Octreotide (w / w) 1:5 Continuous phase pH 7.4 Polyvinyl alcohol (mg / ml) 8 Polysorbate 80(mg / ml) 0.16

[0048] The preparation method of octreotide sustained-release microspheres is as follows:

[0049] Dissolve 196mg of PLGA in dichloromethane as the oil phase; dissolve 19.6mg of octreotide in water as the dispersed phase, which contains 3.92mg of stabilizer trehalose; dissolve 320mg of polyvinyl alcohol and 6.4mg of polysorbate in 40ml of phosphate buffer as the solvent Ester 80 is the continuous phase; the dispersed phase and the oil phase are mixed and shaken to form colostrum, then added to the continuous phase under stirring to form double emulsion, and then quickly transferred to a certain volume of phosphate buffer, magnetically stirred until dichloromethane A...

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Abstract

The invention discloses octreotide sustained-release microspheres with high encapsulation rate and a preparation method thereof. The octreotide sustained-release microspheres are characterized in that the weight ratio of octreotide to polylactic-co-glycolic acid (PLGA) is 1:10-1:5; trehalose is used as a dispersion phase stabilizer, and the weight ratio of the trehalose to the octreotide is 1:10-1:1; polyvinyl alcohol and polysorbate 80 are continuous phase emulsifiers, the concentrations of the polyvinyl alcohol and the polysorbate 80 are respectively 5-30mg / ml and 0.1-0.6mg / ml, and the ratio of the polyvinyl alcohol to the polysorbate 80 is 50:1; and the pH value of a continuous phase is 7.0-9.0. The obtained octreotide microspheres are round, uniform in granularity distribution and high in encapsulation rate, the in-vitro medicament release performance accords with the characteristics of long-acting preparations, the medicament release percentage in 24 hours is less than 20 percent, and the accumulated release in 30 days reach over 80 percent.

Description

technical field [0001] The invention relates to a biodegradable controlled-release microsphere of a bioactive drug with a high encapsulation rate and a preparation method thereof, which belongs to the cross research field of a biomedical polymer material and a controlled-release preparation of a bioactive drug. Background technique [0002] Somotostatin (SS) is widely distributed in the body. It is a regulatory polypeptide that mainly acts on the secretion of neuropeptides, cytokines, nutrients, neurotransmitters, growth factors, thyroid and steroid hormones. However, the half-life of natural SS in blood circulation is very short, and some hormone hypersecretion may rebound after drug withdrawal, such as growth hormone, glucagon and insulin. In order to better play the role of SS and minimize its side effects, people have synthesized somatostatin analogues (somotostatin analogue, SSA) in many ways. The half-life of these analogues is longer than natural SS, and its The effe...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/08A61K47/34A61K47/36A61P5/00
Inventor 倪伟磊崔颀徐强强董堃华刘哲鹏包璇周逸明
Owner SHANGHAI SOHO YIMING PHARMA
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