Prepn process of slow release parathyroid hormone microballoon

A technology of parathyroid hormone and slow-release microspheres, applied in the field of medicine, can solve the problem of not achieving the slow-release effect, etc., and achieve the effects of increasing drug loading, reducing adsorption, and improving biocompatibility

Inactive Publication Date: 2006-03-01
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is a serious burst release phenomenon in the in vitro release curve of the obtained microspheres, and 69% is released on the first day, which does not reach the ideal sustained release effect.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Preparation and in vitro release experiment of parathyroid hormone microspheres

[0023] a) dissolving parathyroid hormone (2%, w / w) in 200 mg of an aqueous solution of high molecular weight polysaccharide (2%, w / w) and small molecular sugar (1%, w / w) as the inner water phase;

[0024] b) The inner water phase was added to 400 mg of a dichloromethane solution of poly(lactic-co-glycolic acid) copolymer (95%, w / w), and magnetically stirred at 10,000 rpm for 2 minutes to form W / O colostrum;

[0025] c) Polyvinyl alcohol (0.1%, w / w) and sodium chloride (20%, w / w) aqueous solution at 4°C is used as the external water phase, and the external water phase is first saturated with dichloromethane, and colostrum is added to it, and the Homogenization method, 1500rpm, 50 seconds, the colostrum is further emulsified to form W / O / W double emulsion;

[0026] d) adding the above-mentioned W / O / W double emulsion into 0.5% sodium chloride solution at 4°C and stirring for 3 hours to solidi...

Embodiment 2

[0031] a) dissolving parathyroid hormone (20%, w / w) in 200 mg of an aqueous solution of high molecular weight polysaccharide (2%, w / w) and small molecular sugar (3%, w / w) as the inner water phase;

[0032] b) The inner water phase is added to 10 g of a dichloromethane solution of poly(lactic-co-glycolic acid) (75%, w / w), and magnetically stirred at 2500 rpm for 5 minutes to form W / O colostrum;

[0033] c) Polyvinyl alcohol (5%, w / w) and sodium chloride (0.5%, w / w) aqueous solution at 4°C is used as the external water phase, and the external water phase is first saturated with dichloromethane, and colostrum is added thereto, and the Homogenization method, 3500rpm, 30 seconds, the colostrum is further emulsified to form W / O / W double emulsion;

[0034] d) adding the above-mentioned W / O / W double emulsion into 25% sodium chloride solution at 4°C and stirring for 4 hours to solidify the microspheres;

[0035] e) washing the solidified microspheres with water to remove the polyvinyl...

Embodiment 3

[0037] a) dissolving parathyroid hormone (11%, w / w) in 200 mg of an aqueous solution of high molecular weight polysaccharide (2%, w / w) and small molecular sugar (2%, w / w) as the inner water phase;

[0038] b) The inner water phase was added to 4.2 g of a dichloromethane solution of poly(lactic-co-glycolic acid) copolymer (85%, w / w), and magnetically stirred at 6250 rpm for 3.5 minutes to form W / O colostrum;

[0039] c) Polyvinyl alcohol (2.55%, w / w) and sodium chloride (10.25%, w / w) aqueous solution at 4°C is used as the external water phase, and the external water phase is first saturated with dichloromethane, and colostrum is added to it, and the Homogenization method, 2500rpm, 40 seconds, the colostrum is further emulsified to form W / O / W double emulsion;

[0040] d) Add the above W / O / W double emulsion into 12.75% sodium chloride solution at 4°C, and stir for 3.5 hours to solidify the microspheres;

[0041]e) washing the solidified microspheres with water to remove the poly...

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PUM

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Abstract

The slow release parathyroid hormone microballoon contains parathyroid hormone 2-20 wt%, high molecular weight polysaccharide 2-20 wt%, small molecular weight saccharide 0-10 wt%, and slow release polymer 75-95 wt%. The preparation process includes the following steps: A. dissolving parathyroid hormone in water solution of high molecular weight polysaccharide to form inner water phase; B. adding the inner water phase into the dichloromethane solution of polylactic acid-hydroxy acetic acid copolymer to form initial W/O emulsion; C. emulsifying the initial W/O emulsion into compound W/O/W emulsion via saturating outer water phase of PVA-NaCl aqua with dichloromethane and adding the initial W/O emulsion; D. adding compound W/O/W emulsion to NaCl aqua via stirring to solidify microballoon; and E. water washing the solidified microballoon and freeze drying. The present invention has improved release curve of parathyroid hormone microballoon, high stability of parathyroid hormone and increased medicine carrying amount of the microballoon.

Description

technical field [0001] The invention relates to a method in the technical field of medicines, in particular to a preparation method of parathyroid hormone sustained-release microspheres. Background technique [0002] In 1997, human recombinant parathyroid hormone (1-84 amino acids) was undergoing phase II clinical trials, and Lilly's parathyroid hormone (1-34) product Teriparatide (Teriparatide Forteo) was approved by the US FDA in June 2002. For the treatment of osteoporosis and primary osteoporosis in postmenopausal women. Because the plasma half-life of parathyroid hormone is very short (20-30min), it is not directly absorbed and the treatment cycle is long. At present, the treatment of parathyroid hormone is 40-100 micrograms subcutaneously injected 3-5 times a week, and it is difficult to treat patients for a long time. Tolerance, the above reasons have brought great difficulties to the treatment of parathyroid hormone, so it is necessary to study the sustained release...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/29A61K9/16A61P5/18
Inventor 金拓吴飞
Owner SHANGHAI JIAO TONG UNIV
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