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Preparation method of goserelin acetate microspheres

A technology of goserelin acetate and sustained-release microspheres, which is applied in the field of medicine, can solve the problems of increased adverse drug reactions, etc., and achieve the effects of gentle sustained-release curve, reduced diffusion, and small burst release effect

Active Publication Date: 2017-12-01
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 goserelin acetate microspheres. On the one hand, it can overcome the problem of increased adverse drug reactions caused by the sudden release of goserelin acetate microspheres. On the other hand, using the method The blood drug concentration of the prepared microspheres is very smooth and stable, which is conducive to long-term medication

Method used

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  • Preparation method of goserelin acetate microspheres
  • Preparation method of goserelin acetate microspheres
  • Preparation method of goserelin acetate microspheres

Examples

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Effect test

Embodiment 1

[0029] Weigh 1g of goserelin acetate (Relin Bachem Company, 1307003) and add water to make a drug solution with a concentration of 40%. Dissolve 8g of PLGA7525 in 20ml of ethyl acetate and 5ml of benzyl alcohol. Mix the two with ultrasonic for 2min to form a white homogeneous colostrum. The colostrum was added into 1000 ml of 0.5% PVA solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6° C. through a syringe through a syringe at a homogeneous speed of 1500 rpm, and homogeneously emulsified for 2 minutes to obtain double emulsion. Move the double emulsion to a cantilever mixer at a speed of 600rpm, stir for 1 hour, then raise the temperature to 45°C and keep it for 1 hour, then lower the temperature to 10°C for sieve filtration, wash with deionized water, and freeze-dry to obtain powdered microspheres. The drug loading is 10.3%, and the 1-day burst release is 7.67%. The pores of the microspheres are continuous and complete, and they are released smoothly for 28 da...

Embodiment 2

[0031] Weigh 1g of goserelin acetate (Relin Bachem Company, 1307003) and add water to make a drug solution with a concentration of 40%. Dissolve 8g of PLGA7525 in 20ml of ethyl acetate and 5ml of benzyl alcohol. Mix the two with ultrasonic for 2min to form a white homogeneous colostrum. The colostrum was added into 1000 ml of 0.5% PVA solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6° C. through a syringe through a syringe at a homogeneous speed of 1500 rpm, and homogeneously emulsified for 2 minutes to obtain double emulsion. Move the double emulsion to a cantilever mixer at a speed of 600rpm, stir for 1 hour, then raise the temperature to 40°C and keep it for 1 hour, then lower the temperature to 10°C for sieve filtration, wash with deionized water, and freeze-dry to obtain powdery microspheres. The drug loading is 10.1%, and the 1-day burst release is 7.14%. The pores of the microspheres are continuous and complete, and they are released smoothly for 28 day...

Embodiment 3

[0033] Weigh 1g of goserelin acetate (Relin Bachem Company, 1307003) and add water to make a drug solution with a concentration of 40%. Dissolve 8g of PLGA7525 in 24ml of ethyl acetate and 3ml of benzyl alcohol. Mix the two with ultrasonic for 2min to form a white homogeneous colostrum. The colostrum was added into 1000 ml of 0.5% PVA solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6° C. through a syringe through a syringe at a homogeneous speed of 1500 rpm, and homogeneously emulsified for 2 minutes to obtain double emulsion. Move the double emulsion to a cantilever mixer at a speed of 600rpm, stir for 1 hour, then raise the temperature to 40°C and keep it for 1 hour, then lower the temperature to 10°C for sieve filtration, wash with deionized water, and freeze-dry to obtain powdery microspheres. The drug loading is 10.8%, and the 1-day burst release is 4.05%. The pores of the microspheres are continuous and complete, and they are released smoothly for 28 day...

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Abstract

The invention provides a preparation method of acetic acid goserelin microspheres. The preparation method includes: step 1), mixing acetic acid goserelin with water to obtain a drug solution A, and mixing PLGA (polylactic-co-glycolic acid) with an organic solution to obtain a solution B; step 2), mixing the solution A with the solution B to form colostrum through ultrasound, and adding the colostrum to a PVA (polyvinyl acetate) water solution saturated by an organic mixed solution to obtain a compound emulsion through homogeneous emulsification; step 3), stirring the compound emulsion at the room temperature for one hour, increasing the temperature to 40-45 DEG C, keeping the compound emulsion for one hour, reducing the temperature to 10 DEG C, sieving the compound emulsion to collect particles and subjecting the particles to freeze-frying. The preparation method has the advantages that the problem of adverse drug reaction increase caused by high sudden release effect of the acetic acid goserelin microspheres can be solved, and the microspheres prepared by the method have quite smooth and stable blood concentration and are beneficial to long-term medication.

Description

technical field [0001] The invention belongs to the field of medicine, in particular, the invention relates to a preparation method of goserelin acetate sustained-release microspheres and the goserelin acetate sustained-release microspheres prepared therefrom. Background technique [0002] Goserelin acetate is a synthetic 10-peptide of gonadotropin-releasing hormone. Goserelin is used to control the clinical symptoms and signs of endometriosis and adenomyosis, and to prevent the recurrence of endometriosis after surgery, all of which have good results. Long-term use of goserelin acetate can inhibit the synthesis of luteinizing hormone in the pituitary gland, thereby causing a decrease in serum testosterone in men and serum estradiol in women. Increased concentrations of serum testosterone in men and serum estradiol in women. [0003] According to the medication characteristics of the clinical indications of goserelin acetate, patients often need long-term administration. T...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K38/08A61K47/34A61K47/32A61P15/00
Inventor 吴蒙磊刘智慧赵冰
Owner LIVZON PHARM GRP INC
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