LHRH (luteinizing hormone releasing hormone) analogue and ziconotide composition sustained-release microsphere preparation and preparation method thereof

A slow-release microsphere preparation, technology of ziconotide, applied in the direction of drug combination, anti-inflammatory agent, pharmaceutical formula, etc., can solve the problems of inconvenient administration of ziconotide, and achieve clinical drug administration inconvenience and good curative effect Effect

Active Publication Date: 2014-07-09
南京星银药业集团有限公司 +1
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

[0006] Based on this, it is necessary to provide a sustained-release microsphere preparation of LHRH analogue and ziconotide composition with sustained-release effect,

Method used

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  • LHRH (luteinizing hormone releasing hormone) analogue and ziconotide composition sustained-release microsphere preparation and preparation method thereof
  • LHRH (luteinizing hormone releasing hormone) analogue and ziconotide composition sustained-release microsphere preparation and preparation method thereof
  • LHRH (luteinizing hormone releasing hormone) analogue and ziconotide composition sustained-release microsphere preparation and preparation method thereof

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preparation example Construction

[0048] see figure 1 , the preparation method of the slow-release microspheres of LHRH analogue and ziconotide composition according to one embodiment, comprising the following steps S110 to S130.

[0049] Step S110: dissolving the LHRH analog and ziconotide in water to obtain an aqueous phase; dissolving a pharmaceutically acceptable polymer material in an organic solvent to obtain an oil phase.

[0050] The LHRH analogue and ziconotide were dissolved in water to obtain an aqueous phase. Water is sterile water. The mass ratio of LHRH analogs to ziconotide is preferably 0.1-30:60-90. In the aqueous phase, the mass concentration of LHRH analogs and ziconotide was 60 mg / L.

[0051] In other embodiments, the aqueous phase also includes gelatin and glycerin. In this case, an aqueous solution containing gelatin and glycerin is prepared first, and then LHRH analogues and ziconotide are dissolved in the aqueous solution containing gelatin and glycerin to obtain water box.

[0052...

Embodiment 1

[0067] 1. Dissolve gelatin and glycerin of equal quality in sterile water to prepare an aqueous solution containing gelatin and glycerin, wherein the mass concentrations of gelatin and glycerin are both 5 mg / L, and dissolve goserelin acetate and ziconotide in In the aqueous solution that contains gelatin and glycerol, the total mass concentration that obtains goserelin acetate and ziconotide is the water phase of 60mg / L; Add PVP in the water phase, obtain mixture; Polylactide that molecular weight is 5000— Glycolide was dissolved in dichloromethane to obtain an oil phase with a mass concentration of 2400 mg / L; wherein, the mass ratio of goserelin acetate and ziconotide was 1:1, polylactide and polylactide-B The mass ratio of lactide is 1:3;

[0068] 2. Put the above mixture and the oil phase in the mixer, and mix evenly at a speed of 12000r / min to form a water-in-oil emulsion. Add the water-in-oil emulsion to water and mix evenly to obtain a water-in-oil-in-water emulsion. Do...

Embodiment 2

[0072] 1. Dissolve gelatin and glycerin of equal quality in sterile water to prepare an aqueous solution containing gelatin and glycerin, wherein the mass concentrations of gelatin and glycerin are both 5 mg / L, and dissolve goserelin acetate and ziconotide in In the aqueous solution that contains gelatin and glycerin, the total mass concentration that obtains goserelin acetate and ziconotide is the aqueous phase of 60mg / L; Add PVA in the aqueous phase, obtain mixture; Polylactide and the polylactide that molecular weight is 20000 and Polylactide-glycolide with a molecular weight of 20,000 is dissolved in ether to obtain an oil phase with a mass concentration of 540 mg / L; wherein, the mass ratio of goserelin acetate and ziconotide is 1:10, and the polylactide The mass ratio of polylactide to glycolide is 3:2;

[0073] 2. Put the above mixture and the oil phase in the mixer, and mix evenly at a speed of 12000r / min to form a water-in-oil emulsion. Add water to the water-in-oil em...

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Abstract

The invention relates to an LHRH (luteinizing hormone releasing hormone) analogue and ziconotide composition sustained-release microsphere preparation and a preparation method thereof. The LHRH analogue and ziconotide composition sustained-release microsphere preparation comprises sustained-release microspheres, wherein the sustained-release microspheres comprise an LHRH analogue, ziconotide and a pharmaceutically acceptable high polymer material. The LHRH analogue and ziconotide composition sustained-release microsphere preparation can effectively bring synergistic effect of the LHRH analogue and the ziconotide into play; experiments prove that the LHRH analogue and ziconotide composition sustained-release microsphere preparation has a sustained-release effect, has a better curative effect in treating cancers, is capable of achieving an analgesic effect at the same time, is administrated by regular injection, and can be used for solving a problem that the ziconotide is inconvenient for clinical administration.

Description

technical field [0001] The invention relates to the technical field of sustained-release microsphere preparations, in particular to a sustained-release microsphere preparation composed of LHRH analogues and ziconotide and a preparation method thereof. Background technique [0002] Whether it is the tumor itself or the treatment methods of radiotherapy and chemotherapy, tumor patients will always be accompanied by severe pain, which has a serious impact on the quality of life of the patient. The present invention inhibits the pain of the patient for a long time Pain, and can improve the efficacy of tumor therapy drugs. [0003] Gonadotropin-releasing hormone, also known as luteinizing hormone-releasing hormone (LHRH), is synthesized in the hypothalamus. It is a polypeptide hormone whose main function is to cause the pituitary gland to release follicle stimulating hormone (FSH) and luteinizing hormone (LH), which can be used to treat certain cancers. LHRH analogues that are ...

Claims

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Application Information

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IPC IPC(8): A61K38/17A61K9/16A61P35/00A61P29/00A61K38/09
Inventor 刘凯豪赵文华何红锋姚志勇支钦李新宇
Owner 南京星银药业集团有限公司
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