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Gonadotropin releasing hormone compound carrying sustained-release microsphere and preparation method thereof

A gonadotropin and hormone-releasing technology, applied in sexual diseases, microcapsules, drug combinations, etc., can solve the problems of pain and discomfort of patients, low drug loading rate, increase of microspheres, etc., so as to improve the drug loading rate. , the effect of reducing drug escape and improving stability

Active Publication Date: 2017-11-10
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(2) The drug loading rate of the existing preparation method is low. For example, the imported Dipherene product used clinically has a drug loading rate of only 2%. It is necessary to increase the dose of microspheres in use, and it will bring a lot of pain to the patient during injection. come pain and discomfort

Method used

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  • Gonadotropin releasing hormone compound carrying sustained-release microsphere and preparation method thereof
  • Gonadotropin releasing hormone compound carrying sustained-release microsphere and preparation method thereof
  • Gonadotropin releasing hormone compound carrying sustained-release microsphere and preparation method thereof

Examples

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Effect test

Embodiment 1

[0052] A preparation method for embedding triptorelin acetate long-acting sustained-release microspheres for injection, comprising the steps of:

[0053] 5 mL of triptorelin acetate aqueous solution with a concentration of 20 mg / mL was used as the internal water phase, 10 mg / mL of trehalose was added as a stabilizer, and 1 g of polylactic-co-glycolic acid (PLGA) with a molecular weight of 20,000 was dissolved in 30 mL Acetone, as the oil phase. The inner water phase and the oil phase were mixed, and the homogenizer was emulsified at 15,000 rpm for 1 min to obtain W / O colostrum. Add the colostrum to 300mL of 5wt% PVA and 1wt% sodium chloride aqueous solution, mechanically stir at 300rpm for 5min to prepare double emulsion, solidify at 40°C for 3h, and form embedded triptorelin long-acting sustained-release microspheres , and then centrifuged and washed to obtain the drug-loaded microspheres. Sorbitol was added as a lyoprotectant, and the obtained microspheres were vacuum-drie...

Embodiment 2

[0065] A preparation method for embedding triptorelin long-acting sustained-release microspheres for injection, comprising the steps of:

[0066] 5mL concentration of 10mg / mL triptorelin aqueous solution is used as the inner water phase, 10mg / mL of mannitol is dissolved in the inner water phase, and 500mg of polyethylene glycol-modified polylactic acid-glycolic acid copolymer with a molecular weight of 30,000 (PEG-PLGA) was dissolved in 10 mL of ethyl acetate (EtAc) as the oil phase. The inner water phase and the oil phase were mixed, and the homogenizer was emulsified at 10,000 rpm for 2 minutes to obtain W / O colostrum. Add this colostrum to 400mL of 2%wt PVA and 1%wt sodium chloride aqueous solution, stir mechanically at 500rpm for 5min to prepare double emulsion, and solidify at 42°C for 6h to form embedded triptorelin long-acting sustained release The microspheres are centrifuged and washed to obtain the drug-loaded microspheres. Mannitol was added as a lyoprotectant, an...

Embodiment 3

[0076] A preparation method for embedding triptorelin acetate long-acting sustained-release microspheres for injection, comprising the steps of:

[0077] 1 mL concentration of 10 mg / mL triptorelin acetate aqueous solution was used as the inner water phase, 20 mg / mL trehalose was dissolved in the inner water phase as a stabilizer, and 200 mg of polyethylene glycol-modified polylactic acid (PELA) with a molecular weight of 200 mg was dissolved in 20mL dichloromethane, as the oil phase. Mix the inner water phase and the oil phase, and emulsify for 1 min at a speed of 20,000 rpm in a homogenizer to obtain W / O colostrum. Add the colostrum to 100mL of 1%wt PVA and 2%wt sodium chloride aqueous solution, stir mechanically at 500rpm for 3min to prepare double emulsion, obtain double emulsion, and solidify at 50°C for 6h to form embedding koji Prelin long-acting sustained-release microspheres are centrifuged and washed to obtain drug-loaded microspheres. Sorbitol was added as a lyopro...

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Abstract

The invention disclose a gonadotropin releasing hormone compound carrying sustained-release microsphere and a preparation method thereof. The preparation method comprises: step 1, adding an inner water phase into an oil phase and performing homogenization to obtain a primary emulsion, wherein the inner water phase is a water solution containing a first stabilizer and a gonadotropin releasing hormone compound, the first stabilizer comprises a polysaccharose substance and / or a weakly alkaline inorganic salt, and the oil phase is an organic solvent containing a high-molecular polymer material; step 2, mixing the primary emulsion obtained in step 1 with an outer water phase to obtain a compound emulsion, wherein the outer water phase is a water solution containing a second stabilizer; and step 3, curing, washing and freeze-drying the compound emulsion obtained in step 2 to obtain sustained-release microspheres. The preparation method is simple, and facilitates industrialized production. The sustained-release microsphere prepared by the preparation method can maintain high activity of gonadotropin releasing hormone on the premise of high carrying rate, and has the impurity content less than 2%.

Description

technical field [0001] The invention relates to a preparation method of degradable polymer slow-release microspheres in the field of medicine, and more particularly relates to a slow-release microsphere loaded with gonadotropin-releasing hormone compounds and a preparation method thereof. Background technique [0002] Gonadotropin releasing hormone (GnRH), also known as luteinizing hormone releasing hormone (LHRH), is released through the pituitary portal system and binds to gonadotropins with specific GnRH receptors (GnRH-R) in the anterior pituitary , regulate the synthesis and secretion of pituitary luteinizing hormone (LH) and follicle stimulating hormone (FSH). LH and FSH are released into the blood circulation and act on the gonads to regulate the maturation of germ cells and the synthesis and secretion of sex hormones. Therefore, GnRH plays an important role in controlling and regulating the reproductive function of mammals, and is a key signaling molecule of the hyp...

Claims

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Application Information

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IPC IPC(8): A61K38/09A61K9/52A61K9/50A61K47/36A61K47/02A61K47/26A61P15/00A61P35/00
CPCA61K9/0002A61K9/5031A61K38/09A61K47/02A61K47/26A61K47/36
Inventor 马光辉李勋韦祎周炜清
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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