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Preparation method of octreotide acetate microspheres

A technology of octreotide acetate and microspheres, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, can solve problems such as hindering the use of drugs, uneven distribution of microspheres, aggregation, etc. Fast distribution, simple operation, and simple method steps

Active Publication Date: 2019-01-01
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the product microspheres obtained by this method are unevenly distributed, and even if they are ready-to-use, they are very prone to aggregation, which seriously hinders the clinical use of the drug

Method used

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  • Preparation method of octreotide acetate microspheres
  • Preparation method of octreotide acetate microspheres
  • Preparation method of octreotide acetate microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The octreotide acetate that takes 0.75g is dissolved in 15g methanol; The PLGA that gets 10g is dissolved in 400g methylene chloride; The above two parts of solutions are stirred and mixed, rated speed 120rpm, form homogeneous solution; Get 640ml silicone oil (viscosity 350cs), in After adding at a constant speed within 13 minutes, continue to stir for 5 minutes, and control the temperature at 8-10°C to form agglomerates; Solidify, solidify for 2 hours; form microspheres after solidification, collect by filtration, wash with n-heptane for 3-4 times, add appropriate amount of mannitol solution, dry in vacuum, and sieve to obtain the product. See SEM image figure 1 and 2 .

[0050] The accelerated release results of the resulting product are as follows:

[0051] Table 1-1

[0052]

[0053]

[0054] Note: The result is the accumulative accelerated release degree of accelerated release 1h, 4h and 24h

[0055] The particle size distribution of the product obtained...

Embodiment 2

[0061] The octreotide acetate that takes 0.75g is dissolved in 15g methanol; The PLGA that gets 10g is dissolved in 345g methylene chloride; The above two parts of solutions are stirred and mixed, rated speed 120rpm, form homogeneous solution; Get 640ml silicone oil (viscosity 350cs), in After adding at a constant speed within 13 minutes, continue to stir for 5 minutes, and control the temperature at 8-10°C to form agglomerates; add a solidifying solution composed of n-heptane (3200ml), water (400ml), Span80 (20ml), and silicone oil (100ml) to solidify , solidified for 2 hours; microspheres formed after solidification, collected by filtration, washed with n-heptane for 3-4 times, added an appropriate amount of mannitol solution, dried in vacuum for 20 hours, and sieved to obtain the product. See SEM image image 3 and 4 .

[0062] The accelerated release results of the resulting product are as follows:

[0063] table 2-1

[0064]

Drug loading

1h

4h

2...

Embodiment 3

[0069] The octreotide acetate that takes 0.75g is dissolved in 15g methanol; The PLGA that gets 10g is dissolved in 400g methylene chloride; The above two parts of solutions are stirred and mixed, rated speed 120rpm, form homogeneous solution; Get 640ml silicone oil (viscosity 600cs), in After adding at a constant speed within 13 minutes, continue to stir for 5 minutes, and control the temperature at 8-10°C to form agglomerates; Solidify, solidify for 2 hours; form microspheres after solidification, collect by filtration, wash with n-heptane for 3-4 times, add appropriate amount of mannitol solution, dry in vacuum for 20 hours, and sieve to obtain the product. See SEM image Figure 5 and 6 .

[0070] The accelerated release results of the resulting product are as follows:

[0071] Table 3-1

[0072]

Drug loading

1

4

24

W03-171113-2-0-1

4.72％

2.51％

28.55％

54.97％

[0073] The particle size distribution of the product obtained is ...

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Abstract

The invention discloses a method for preparing octreotide acetate microsphere preparation. The method comprises the following steps: (1) dissolving octreotide acetate in methanol to form a solution A;(2) dissolving PLGA in dichloromethane to form a solution B; (3) mixing the solution A and the solution B while stirring to form a uniform solution C; (4) adding silicone oil into the solution C at aconstant speed while stirring to form a condensation product; (5) adding the obtained condensation product into curing liquid to form microspheres; (6) filtering the microspheres obtained in step (5), and cleaning; adding a proper amount of solution of mannitol, and performing vacuum drying and sieving. The method is easy to operate, the prepared product has high quality, the octreotide acetate microspheres can be prepared as required, and the microspheres are distributed quickly and uniformly and do not aggregate. According to the method disclosed by the invention, relatively few suspensionsteps are required for preparing the microspheres, the operation is simple, no special requirements are imposed on the preparation personnel, special training is not needed, and convenience in using the medicine by terminal hospitals and patients can be remarkably improved.

Description

technical field [0001] The invention relates to the technical field of microsphere pharmaceutical preparations, in particular to a method for preparing octreotide acetate microspheres by a phase separation method. Background technique [0002] Octreotide is a synthetic octapeptide derivative of natural somatostatin, which was first synthesized by chemist Wilfried Bauer in 1979. It retains the same pharmacological effects as growth hormone and can inhibit many hormones, including gastrin, shrink Secretion of cholecystolin, glucagon, growth hormone (GH), insulin, pancreatic polypeptide, thyrotropin, and vasoactive intestinal peptide. Clinically, it is mainly used for the treatment of acromegaly, gastropancreatic and intestinal endocrine tumors (carcinoid, growth hormone releasing factor adenoma, glucagonoma, gastrinoma / Zollinger-Ellison syndrome, insulinoma, vasoactive intestinal Peptide tumor), clinical application is very extensive. [0003] There are two kinds of octreoti...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/08A61K47/34A61P5/08A61P35/00
CPCA61K9/1641A61K38/08A61P5/08A61P35/00
Inventor 蔡晨辰徐朋蒋刚锋何超梁慧君蒋永康江晓漫
Owner LIVZON PHARM GRP INC
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