A kind of preparation method of triptorelin acetate sustained-release microspheres

A technology of triptorelin acetate and sustained-release microspheres, applied in endocrine system diseases, sexual diseases, powder delivery and other directions, can solve problems such as increase in adverse drug reactions, and achieve long-term drug use, reduce sudden release effects, The effect of slow release curve flattening

Active Publication Date: 2018-05-22
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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  • A kind of preparation method of triptorelin acetate sustained-release microspheres
  • A kind of preparation method of triptorelin acetate sustained-release microspheres
  • A kind of preparation method of triptorelin acetate sustained-release microspheres

Examples

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Embodiment 1

[0030] Take by weighing 1g of triptorelin acetate (Railin Bachem Company, lot number 1209001) and add water to make a drug solution with a concentration of 40%, dissolve 8g of PLGA5050 with 25ml of ethyl acetate and 10ml of benzyl alcohol, mix the two with ultrasound for 2min, and form 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 1500 rpm, and homogeneously emulsified for 2 minutes to obtain double emulsion. Move the double emulsion to a cantilever mixer with a rotation speed of 600 rpm, stir for 1 hour, then raise the temperature to 45° and keep it for 1 hour, then lower the temperature to 10° to filter through a sieve, and freeze-dry to obtain powdered microspheres. The drug loading capacity of the triptorelin acetate microspheres was 10.3%, and the burst release rate was 9% in 1 day. The pores of the microspheres were continuous and c...

Embodiment 2

[0032] Weigh 1g of triptorelin acetate (Railin Bachem Co., lot number 1209001) and add water to make a drug solution with a concentration of 40%. Dissolve 8g of PLGA5050 with 23.5ml of ethyl acetate and 3.3ml of benzyl alcohol, mix the two and sonicate for 2min , forming 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 1500 rpm, and homogeneously emulsified for 2 minutes to obtain double emulsion. Move the double emulsion to a cantilever mixer with a rotation speed of 600 rpm, stir for 1 hour, then raise the temperature to 45° and keep it for 1 hour, then lower the temperature to 10° to filter through a sieve, and freeze-dry to obtain powdered microspheres. The drug-loading capacity of the triptorelin acetate microspheres was 10.8%, and the burst release rate was 8% in 1 day. The pores of the microspheres were continuous and complete, and th...

Embodiment 3

[0034] Take by weighing 1g of triptorelin acetate (Railin Bachem Company, batch number 1209001) and add water to make a drug solution with a concentration of 40%, dissolve 8g of PLGA5050 with 19ml of ethyl acetate and 7.6ml of benzyl alcohol, and mix the two with ultrasound for 2min. Form white homogeneous colostrum. Colostrum is added into 1000ml of 0.5% PVA solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6° C. through a syringe under homogenization at 1500 rpm, and homogeneously emulsified for 2 minutes to obtain double emulsion. Move the double emulsion to a cantilever mixer with a rotation speed of 600 rpm, stir for 1 hour, then raise the temperature to 40° and keep it for 1 hour, then lower the temperature to 10° to filter through a sieve, and freeze-dry to obtain powdery microspheres. The drug loading capacity of the triptorelin acetate microspheres was 10.6%, and the burst release rate was 9% in 1 day. The pores of the microspheres were continuous and com...

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Abstract

The invention relates to a preparation method of triptorelin acetate sustained-release microspheres, comprising the following steps: step 1) adding water to triptorelin acetate to form a drug solution A; adding PLGA to an organic solvent to form a solution B; step 2) mixing Solution A and solution B are mixed and ultrasonicated to form colostrum, and the colostrum is added to a PVA aqueous solution saturated with an organic mixed solvent, and homogeneously emulsified to obtain double emulsion; Step 3) Stir the double emulsion at room temperature for 1 hour and then heat up to 40°C-45°C The temperature was kept at ℃ for 1 hour, and then the temperature was lowered to 10 ℃, and the particles were collected by sieving and freeze-dried. On the one hand, the technology involved in the present invention can overcome the problem of increased adverse drug reactions caused by the sudden release of triptorelin acetate microspheres; on the other hand, the blood drug concentration of the prepared microspheres is very smooth and stable, and is suitable for long-term administration treat.

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 (Triptorelin) is a synthetic decapeptide, which is an analogue of natural GnRH (gonadotropin-releasing hormone). Studies have shown that long-term use of triptorelin acetate can cause the secretion of gonadotropins, thereby inhibiting the function of testes and ovaries. Triptorelin acetate is clinically used in the treatment of metastatic prostate cancer, precocious puberty, and genital and extragenital endometriosis. [0003] According to the medication characteristics of triptorelin acetate clinical indications, patients often need long-term administration, so in order to improve the compliance of patients, a long-acting sustained-release preparation was developed. ...

Claims

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Application Information

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Patent Type & Authority Patents(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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