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Long-acting pharmaceutical preparation combination of leuprolide acetate and use method of pharmaceutical preparation combination

A technology for leuprolide acetate and pharmaceutical preparations, applied in directions such as drug combination, drug delivery, and pharmaceutical formulations, can solve the problems such as the inability to increase the drug load, reduce the sudden release, etc., so as to solve the problem that the drug load cannot be increased and reduce the sudden release, cost-saving effect

Active Publication Date: 2020-07-03
SHANDONG GUYUCHUN BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

With the present invention, the glass transition temperature of the polymer is reduced, the burst release of the drug at the beginning of release is reduced, and the yield of biodegradable polymer microspheres is improved; the risk of polymer degradation during storage is also reduced, and the The temperature of storage and transportation saves the cost of storage and transportation; effectively solves the problem that the drug loading of leuprolide acetate microspheres cannot be increased

Method used

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  • Long-acting pharmaceutical preparation combination of leuprolide acetate and use method of pharmaceutical preparation combination
  • Long-acting pharmaceutical preparation combination of leuprolide acetate and use method of pharmaceutical preparation combination
  • Long-acting pharmaceutical preparation combination of leuprolide acetate and use method of pharmaceutical preparation combination

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Effect test

Embodiment 1

[0041] A combination of leuprolide acetate long-acting pharmaceutical preparations, comprising leuprolide acetate, biodegradable polymer microspheres and solvents stored independently; the biodegradable polymer microspheres are microspheres formed from a mixture of PLGA and PCL ball.

[0042] The specific preparation method of the biodegradable polymer microspheres is:

[0043] (1) Dissolve 55 g of PLGA (lactide: glycolide = 50 / 50, self-made, MW: 41000) and 5 g of PCL (self-made, MW: 10000) in 200 ml of dichloromethane, and filter and sterilize to obtain organic Mutually;

[0044] (2) Using a pressure of 1500mpa, the organic phase is squeezed through the membrane tube, the membrane hole is 15 μm, squeezed into the continuous water phase, the flow rate of the water phase is 600ml / min, the microspheres are extruded, the emulsion is volatilized and dried, and the microspheres are solidified and formed. Under GMP conditions, it is aseptically dispensed into vials, 60 mg / bottle; ...

Embodiment 2

[0048] A combination of leuprolide acetate long-acting pharmaceutical preparations, comprising leuprolide acetate, biodegradable polymer microspheres and solvents stored independently; the biodegradable polymer microspheres are microspheres formed from a mixture of PLGA and PCL ball.

[0049] The specific preparation method of the biodegradable polymer microspheres is:

[0050] (1) Dissolve 50 g of PLGA (lactide: glycolide = 75 / 25, self-made, MW: 32000) and 10 g of PCL (self-made, MW: 10000) in 200 mL of dichloromethane, and filter and sterilize to obtain organic Mutually;

[0051] (2) Using a pressure of 500mpa, the organic phase is squeezed through the membrane tube, the membrane hole is 50 μm, squeezed into the continuous water phase, the flow rate of the water phase is 1000ml / min, the microspheres are extruded, the emulsion is volatilized and dried, and the microspheres are solidified and formed. Under GMP conditions, it is aseptically dispensed into vials, 110 mg / bottle...

Embodiment 3

[0055] A combination of leuprolide acetate long-acting pharmaceutical preparations, comprising leuprolide acetate, biodegradable polymer microspheres and solvents stored independently; the biodegradable polymer microspheres are microspheres formed from a mixture of PLGA and PCL ball.

[0056] The specific preparation method of the biodegradable polymer microspheres is:

[0057] (1) Dissolve 50 g of PLGA (lactide: glycolide = 85 / 15, self-made, MW: 41000) and 10 g of PCL (self-made, MW: 10000) in 200 mL of dichloromethane, and filter and sterilize to obtain organic Mutually;

[0058] (2) Using a pressure of 2000mpa, the organic phase is squeezed through the membrane tube, the membrane hole is 30 μm, squeezed into the continuous water phase, the flow rate of the water phase is 5000ml / min, the microspheres are extruded, the emulsion is volatilized and dried, and the microspheres are solidified and formed. Under GMP conditions, it is aseptically dispensed into vials, 130 mg / bottl...

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Abstract

The invention belongs to the technical field of pharmaceutical preparation, and in particular relates to a long-acting pharmaceutical preparation combination of leuprolide acetate and a use method ofthe pharmaceutical preparation combination. The long-acting pharmaceutical preparation combination of leuprolide acetate of the invention comprises separately independently stored leuprolide acetate or analogues of leuprolide acetate, biodegradable polymer microspheres and solvents; and the biodegradable polymer microspheres are microspheres formed by a mixture of PLGA and PCL. According to the present invention, by adopting the pharmaceutical preparation combination, the glass transition temperature of the polymer is reduced, the burst release of the drug at the beginning of release is reduced, and the yield of the biodegradable polymer microspheres is improved; the risk of polymer degradation during storage is reduced, the temperature of storage and transportation is also reduced, and the cost of storage and transportation is saved; and the problems that the drug loading of leuprolide acetate microspheres can not be increased and the burst release of the prior leuprolide acetate gel(Eligard) is too large are solved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparation, and in particular relates to a combination of leuprolide acetate long-acting pharmaceutical preparations and a method for using the same. Background technique [0002] Leuprorelin acetate (Leuprorelin Acetate), is a highly active derivative of artificially synthesized luteinizing hormone-releasing hormone (LH-RH), is a highly active analogue of luteinizing hormone-releasing hormone produced by the hypothalamus, and can treat Or relieve a variety of sex hormone-dependent diseases such as endometriosis, uterine fibroids, precocious puberty, prostate cancer, etc., and are widely used in the treatment of women with precocious puberty, endometriosis, uterine fibroids or premenopausal breast cancer Patients with prostate cancer and other male patients, long-term application can effectively treat endometriosis. [0003] Because leuprolide acetate is a synthetic polypeptide, it is uns...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/10A61K9/06A61K47/34A61P15/00A61P35/00
CPCA61K38/09A61K9/10A61K9/06A61K9/0019A61K47/34A61P15/00A61P35/00
Inventor 苏红清秦昌王栋
Owner SHANDONG GUYUCHUN BIOTECHNOLOGY CO LTD
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