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Preparation method of triptorelin acetate sustained-release microsphere

A technology of triptorelin acetate and sustained-release microspheres, which can be applied to medical preparations containing active ingredients, pharmaceutical formulas, endocrine system diseases, etc. Reduced diffusion, surface smoothing effects

Active Publication Date: 2015-12-23
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides a preparation method of triptorelin acetate microspheres, which can overcome the problem of increased adverse drug reactions caused by the sudden release of triptorelin acetate microspheres on the one hand, and on the other hand use the method to prepare The surface of the microspheres is smooth, and the blood concentration is stable, which is conducive to long-term medication

Method used

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  • Preparation method of triptorelin acetate sustained-release microsphere
  • Preparation method of triptorelin acetate sustained-release microsphere
  • Preparation method of triptorelin acetate sustained-release microsphere

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Weigh 1 g of triptorelin acetate (Ruilin Bachem company, batch number 1209001) and add water to make a drug solution with a concentration of 40%, dissolve 8 g of PLGA5050 with 25 ml of ethyl acetate and 10 ml of benzyl alcohol, and mix the two with ultrasound for 2 minutes to form a white Homogenized colostrum. The colostrum was added to 1000 ml of 0.5% PVA solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6°C through a syringe at 1500 rpm homogenization, and homogeneously emulsified for 2 min to obtain a double emulsion. The compound emulsion was moved to a cantilever mixer with a rotating speed of 600 rpm, stirred for 1 hour, then heated to 45° for 1 hour, then lowered to 10° for sieve filtration, and freeze-dried to obtain powdered microspheres. The drug loading of triptorelin acetate microspheres was 10.3%, the burst release was 9% in 1 day, and the pores of the microspheres were continuous and intact, and the release was stable for 28 days.

Embodiment 2

[0032] Weigh 1 g of triptorelin acetate (Ruilin Bachem company, batch number 1209001) and add water to make a drug solution with a concentration of 40%, dissolve 8 g of PLGA5050 with 23.5 ml of ethyl acetate and 3.3 ml of benzyl alcohol, and mix the two with ultrasonics for 2 min. A white homogeneous colostrum is formed. The colostrum was added to 1000 ml of 0.5% PVA solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6°C through a syringe at 1500 rpm homogenization, and homogeneously emulsified for 2 min to obtain a double emulsion. The compound emulsion was moved to a cantilever mixer with a rotating speed of 600 rpm, stirred for 1 hour, then heated to 45° for 1 hour, then lowered to 10° for sieve filtration, and freeze-dried to obtain powdered microspheres. The drug loading of triptorelin acetate microspheres was 10.8%, the burst release was 8% in 1 day, the pores of the microspheres were continuous and intact, and the release was stable for 28 days.

Embodiment 3

[0034] Weigh 1 g of triptorelin acetate (Ruilin Bachem company, batch number 1209001) and add water to make a drug solution with a concentration of 40%, dissolve 8 g of PLGA5050 with 19 ml of ethyl acetate and 7.6 ml of benzyl alcohol, and mix the two with ultrasound for 2 min to form The white homogeneous colostrum was added to 1000 ml of 0.5% PVA solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6°C through a syringe at 1500 rpm homogenization, and homogeneously emulsified for 2 minutes to obtain a double emulsion. The compound emulsion was moved to a cantilever mixer with a rotating speed of 600 rpm, stirred for 1 hour, then heated to 40° for 1 hour, then lowered to 10° for sieve filtration, and freeze-dried to obtain powdered microspheres. The drug loading of triptorelin acetate microspheres was 10.6%, the burst release in 1 day was 9%, the pores of the microspheres were continuous and intact, and the release was stable for 28 days.

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Abstract

The invention relates to a preparation method of triptorelin acetate sustained-release microsphere. The preparation method comprises the following steps: (1) adding water into triptorelin acetate to prepare a solution A, and adding PLGA into an organic solvent to prepare a solution B; (2) mixing the solution A and solution B, subjecting the mixed solution to an ultrasonic treatment to form primary emulsion, adding the primary emulsion into a PVA water solution, which has been saturated by an organic mixed solvent, and homogenizing and emulsifying the solution to obtain multiple emulsion; (3) stirring the multiple emulsion at a room temperature for 1 hour, then heating the multiple emulsion to a temperature of 40 to 45 DEG C, maintaining the temperature for 1 hours, cooling to 10 DEG C, sieving, collecting the particles, and freeze-drying the particles. The provided technology can solve the problem that the adverse reactions are enhanced by the burst release of triptorelin acetate, moreover, the blood concentration of the prepared microsphere is very smooth and stable, and thus the sustained-release microsphere is suitable for long-term drug administration.

Description

technical field [0001] The invention belongs to the field of medicine, in particular, the invention relates to a preparation method of triptorelin acetate sustained-release microspheres and triptorelin acetate sustained-release microspheres prepared therefrom. Background technique [0002] Triptorelin acetate is a synthetic decapeptide that is an analog of natural GnRH (gonadotropin-releasing hormone). Studies have shown that long-term use of triptorelin acetate can cause gonadotropin secretion, thereby inhibiting testicular and ovarian function. Triptorelin acetate is clinically used for the treatment of metastatic prostate cancer, precocious puberty, and endometriosis inside and outside the genitals. [0003] According to the medication characteristics of the clinical indications of triptorelin acetate, patients often need long-term administration, so in order to improve the compliance of patients, long-acting sustained-release preparations have been developed. Common sl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/14A61P5/24A61P15/00
Inventor 吴蒙磊刘智慧赵冰
Owner LIVZON PHARM GRP INC
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