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GLP-1 analogue and ziconotide composite slow-release microsphere preparation

A technology of sustained-release microsphere preparation and ziconotide, which is applied in the directions of drug combination, drug delivery, peptide/protein composition, etc., can solve the problems of undiscovered combination application

Inactive Publication Date: 2017-05-31
深圳市健翔生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

So far, no reports have been found on the combined application of the two

Method used

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  • GLP-1 analogue and ziconotide composite slow-release microsphere preparation
  • GLP-1 analogue and ziconotide composite slow-release microsphere preparation
  • GLP-1 analogue and ziconotide composite slow-release microsphere preparation

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preparation example Construction

[0049] A preparation method of GLP-1 analog and ziconotide composition sustained-release microsphere preparation, comprising the steps of:

[0050] Step 1) adding water to the GLP-1 analogue and ziconotide to form a drug solution A; adding a biodegradable and biocompatible polymer material to form a solution B;

[0051] Step 2) The solution A and the solution B are mixed and ultrasonicated to form colostrum, and the colostrum is added to an aqueous stabilizer solution saturated with an organic mixed solvent, and homogeneously emulsified to obtain double emulsion;

[0052] Step 3) Stir the double emulsion at room temperature for 1 hour, then raise the temperature to 40°C-45°C and keep it for 1 hour, then lower the temperature to 10°C, add a freeze-drying protective agent, collect the particles by sieving, freeze-dry, and sterilize by radiation.

[0053] Preferably, the organic solvent in step 1) is selected from one of ethyl acetate, benzyl alcohol mixed solution or dichloromet...

Embodiment 1

[0060] Weigh 0.2 mg of liraglutide and 0.2 mg of ziconotide and add water to make a drug solution with a concentration of 40%, dissolve 1 g of polylactide-glycolide with 25 mL of ethyl acetate and 10 mL of benzyl alcohol, and mix the two Ultrasonic for 2 minutes, white homogeneous colostrum is formed. Colostrum was added into 1000 mL of 0.01% (weight to volume ratio) polyvinyl alcohol aqueous solution (containing 1% benzyl alcohol and 1% ethyl acetate) at 6°C through a syringe through a syringe at 1600 rpm, and homogeneously emulsified for 2 minutes to obtain double emulsion . Move the double emulsion to the 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 it to 10°C, add 0.1g of sorbitol to obtain the mixture, filter with a sieve, and freeze-dry to obtain powdery microspheres . Observed by a JSM-5600 scanning electron microscope, the pores of the microspheres are continuous and complete, and the mi...

Embodiment 2

[0062] Weigh 0.25 mg of exenatide and 0.3 mg of ziconotide and add water to make a drug solution with a concentration of 20%, dissolve 1 g of polyhydroxybutyrate valerate with 30 mL of ethyl acetate and 10 mL of benzyl alcohol, and mix the two Ultrasonic for 2 minutes, white homogeneous colostrum is formed. Colostrum was added into 1000 mL of 0.02% polyvinyl alcohol solution (containing 0.5% benzyl alcohol and 1% ethyl acetate) at 6°C through a syringe through a syringe at a homogeneous speed of 1600 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 it to 10°C, add 0.1g of lactose to obtain a mixture, filter through a sieve, and freeze-dry to obtain powdered microspheres. Observed by the JSM-5600 scanning electron microscope, the pores of the microspheres are continuous and complete, and the microsp...

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Abstract

The invention relates to a GLP-1 analogue and ziconotide composite slow-release microsphere preparation and a preparation method thereof. The slow-release microsphere preparation is prepared from a GLP-1 analogue, ziconotide, a biodegradable high polymer material with biocompatibility, a stabilizing agent and a freeze drying protection agent. The preparation method comprises the following steps of (1) adding water for preparing the GLP-1 analogue and the ziconotide into a medicine solution A; adding an organic solvent for preparing the biodegradable high polymer material with biocompatibility into a solution B; (2) mixing the solution A and the solution B; performing ultrasonic processing to form primary emulsion; adding the primary emulsion into a stabilizing agent water solution saturated by an organic mixed solvent; performing homogenizing emulsification to obtain secondary emulsion; (3) performing room-temperature stirring on the secondary emulsion for 1 hour; then, raising the temperature to 40 DEG C to 45 DEG C; maintaining the temperature for one hour; then, lowering the temperature to 10 DEG C; adding the freeze drying protection gent; screening and collecting particles; performing freeze drying; performing radiation sterilization. By using a related technology, the effect of treating diabetes and PDN (painful diabetic neuropathy) complications for a long time can be achieved; the pain of a patient is reduced; the medicine compliance of the patient is improved; the clinic practical significance is realized.

Description

technical field [0001] The invention relates to a slow-release microsphere preparation composed of GLP-1 analogs and ziconotide and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] With the development of society, the incidence of diabetes in the world is increasing significantly. In 2000, it was estimated to be 2.8%, and it is estimated to be 4.3% by 2025. The number of diabetic patients will also increase from 171 million in 2000 to 2025. 380 million. Diabetes has many complications and has become the main cause of death and disability of patients, seriously affecting human health. Diabetic complications include diabetic ketoacidosis, diabetic nephropathy, hypertension, painful diabetic neuropathy (Painful diabetic neuropathy, PDN), among which PDN is one of the most common and serious complications of diabetes. Chronic lesions are common in PDN, mainly involving the extremities and feet. The main manifes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K38/17A61K38/26A61K38/22A61K9/16A61P3/10A61P25/00
CPCA61K45/06A61K9/0002A61K9/1641A61K38/1767A61K38/22A61K38/26A61K2300/00
Inventor 李新宇支钦姚志勇吴丽芬曹演威
Owner 深圳市健翔生物制药有限公司
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