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Sustained-release pasireotide microspheres and preparation method thereof

A pasireotide and microsphere technology, applied in microcapsules, cyclic peptide components, pharmaceutical formulations, etc., can solve the problems of long action, short action time, slow release of microspheres, etc., and achieve high encapsulation efficiency and uniform particle size. , the effect of simple preparation process

Active Publication Date: 2020-12-11
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In the prior art, the drug is prepared as an injection, which has a shorter action time in the body; while the microspheres are relatively slow in release and have a longer action time in the body.

Method used

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  • Sustained-release pasireotide microspheres and preparation method thereof
  • Sustained-release pasireotide microspheres and preparation method thereof
  • Sustained-release pasireotide microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of the inner water phase: Weigh 100 mg of pasireotide and water, vortex and shake to dissolve, weigh 100 mg of mannitol in the prescribed amount, add it to the pasireotide aqueous solution to disperse, and dissolve in a water bath to obtain the inner water phase;

[0057] Preparation of the external water phase: Measure an appropriate amount of purified water, add 50 mg of polyvinyl alcohol, heat and stir to dissolve, pass through the gauze to obtain the external water phase solution;

[0058] Preparation of the oil phase: take 0.8g PLGA and dissolve it in 30g of dichloromethane as the oil phase;

[0059] Preparation of colostrum: transfer the dissolved oil phase to the inner water phase and use high-speed stirring (2000rpm) for 20 seconds to obtain colostrum;

[0060] Preparation of double emulsion: Add colostrum to polyvinyl alcohol solution under stirring to obtain double emulsion, continue to stir the double emulsion to remove organic solvent, centrifuge...

Embodiment 2

[0062]Preparation of the inner water phase: Weigh 120 mg of pasireotide and water, vortex shake to dissolve, weigh 180 mg of hypromellose in the prescribed amount, add it to the aqueous solution of pasireotide to disperse, and dissolve in a water bath to obtain the inner water phase ;

[0063] Preparation of the external water phase: Measure an appropriate amount of purified water, add 200 mg of Tween, heat and stir to dissolve, pass through the gauze to obtain the external water phase solution;

[0064] Preparation of the oil phase: Weigh 1.0g PLGA and dissolve it in 30g of ethyl acetate as the oil phase;

[0065] Preparation of colostrum: transfer the dissolved oil phase to the inner water phase and use high-speed stirring (16000rpm) for 30 seconds to obtain colostrum;

[0066] Preparation of double emulsion: Add colostrum to 200 mg Tween solution under stirring to obtain double emulsion, continue to stir the double emulsion to remove organic solvent, centrifuge, wash and c...

Embodiment 3

[0068] Preparation of the inner aqueous phase: Weigh 120 mg of pasireotide and water, vortex shake to dissolve, weigh 180 mg of mannitol in the prescribed amount, add it to the aqueous solution of pasireotide to disperse, dissolve in a water bath, and then add 100 mg of human serum white albumen, add suspending agent gum arabic 100mg simultaneously, obtain inner aqueous phase;

[0069] Preparation of the external water phase: Measure an appropriate amount of purified water, add polyvinyl alcohol with a prescribed amount of 120 mg, heat and stir to dissolve, pass through the gauze to obtain the external water phase solution;

[0070] Preparation of the oil phase: Weigh 1.1g PLGA and dissolve it in 30g of dichloromethane as the oil phase;

[0071] Preparation of colostrum: transfer the dissolved oil phase to the inner water phase and use high-speed stirring (16000rpm) for 30 seconds to obtain colostrum;

[0072] Preparation of double emulsion: Add colostrum to polyvinyl alcohol...

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Abstract

Disclosed are a slow release pasireotide microsphere and a preparation method thereof. The microsphere is prepared using pasireotide as an active ingredient, and a microsphere support polymer, a protecting agent, a surfactant and a suspending agent. The microsphere support polymer is selected from polylactic-co-glycolic acids (PLGA). The suspending agent is selected from one or a combination of any two or more of tragacanth, gum arabic, carbomer and sodium alginate. The preparation method of the microsphere is a multiple emulsion method. Addition of the suspending agent allows for a release time of the pasireotide microsphere of up to 28 days.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a slow-release pasireotide microsphere and a preparation method thereof. Background technique [0002] Pasireotide injection is a somatostatin analogue mainly used to treat patients with Cushing's disease who cannot be treated by surgery. Cushing's disease is pituitary ACTH adenoma or ACTH cell proliferation, which secretes excessive ACTH, causes adrenal cortical hyperplasia, produces hypercortisolism, and leads to a series of substance metabolism disorders and pathological changes. Pasireotide inhibits ACTH secretion, thereby reducing cortisol secretion. [0003] Pasireotide injection has been approved by the US FDA, but due to its short half-life, it needs to be injected subcutaneously twice a day. Compliance is poor, so developing an extended-release microsphere formulation that can be administered once a month could improve patient compliance. [0004] The FDA ap...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K38/12A61K47/34A61P5/02
CPCA61K9/0019A61K9/5031A61K38/12A61P5/02A61K9/16A61K47/34A61P5/38
Inventor 张伟明辛永涛陶安进袁建成
Owner HYBIO PHARMA