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sak-hv oral controlled release microspheres and preparation method and application thereof

A technology of microspheres and fusion proteins, applied in the intersection of biological preparations and biomedicine, can solve the problems of increased morbidity and mortality, and achieve the effect of reducing immunogenicity and improving patient compliance.

Active Publication Date: 2019-08-23
INST OF BASIC MEDICAL SCI ACAD OF MILITARY MEDICAL SCI OF PLA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Cardiovascular and cerebrovascular diseases are the number one killer of human health. In recent years, its morbidity and mortality have been increasing year by year, and hyperlipidemia is one of its main pathological bases. Currently, statins are the first choice for clinically treating hyperlipidemia. There are few self-developed biological drugs for the treatment of atherosclerosis caused by hyperlipidemia in China, and protein-based drugs for the treatment of hyperlipidemia are still blank in China

Method used

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  • sak-hv oral controlled release microspheres and preparation method and application thereof
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  • sak-hv oral controlled release microspheres and preparation method and application thereof

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Embodiment 1

[0048] Colostrum was obtained by ultrasonic emulsification with SAK-HV PBS solution and oil phase ①. The concentration of SAK-HV solution is 3 mg / ml, and it is added into the oil phase ① at a ratio of 1:10 (water phase: oil phase), and stable W / O colostrum is formed by ultrasonic emulsification and mechanical stirring, and then the colostrum is mixed with colostrum The volume ratio of milk and PVA solution is 1:10 and slowly added to 2wt% PVA (polyvinyl alcohol) solution (containing NaCl0.9wt%), after stirring rapidly at 1000rpm for 10min, stirring at 300rpm at a low speed overnight, solidification , centrifuged, washed with deionized water, and freeze-dried. The SAK-HV encapsulation efficiency of the obtained microspheres was 68%, and the drug loading was 13.1 μg / mg. In artificial gastric juice, the drug release rate is 36.8% in 2 hours, and in the pH7.2 buffer solution, the drug release rate reaches 90.1% in 4 hours. The morphology of the obtained microspheres is as follow...

Embodiment 2

[0050] Colostrum was obtained by ultrasonic emulsification with PBS solution of SAK-HV and oil phase ②. The concentration of SAK-HV solution is 5 mg / ml, and it is added into the oil phase ② at a ratio of 1:10 (water phase: oil phase), and stable W / O colostrum is formed by ultrasonic emulsification and mechanical stirring, and then the colostrum is mixed with colostrum Slowly add milk to PVA solution at a volume ratio of 1:10 to 2% PVA (polyvinyl alcohol) solution (containing 0.9 wt% NaCl), stir rapidly at 1000rpm for 10min, then stir overnight at 300rpm at a low speed, and solidify , centrifuged, washed with deionized water, and freeze-dried. The SAK-HV encapsulation efficiency of the obtained microspheres was 67.3%, and the drug loading was 20.9 μg / mg. 35.8% of the drug was released in 2 hours in artificial gastric juice, and 93% of the drug was released in 4 hours in the pH7.2 buffer solution. The morphology of the obtained microspheres is as follows figure 2 As shown, t...

Embodiment 3

[0052] Colostrum was obtained by ultrasonic emulsification with SAK-HV PBS solution and oil phase ①. The concentration of SAK-HV solution is 6 mg / ml, and it is added into the oil phase ① at a ratio of 1:10 (water phase: oil phase), and a stable W / O colostrum is formed by ultrasonic emulsification and mechanical stirring, and then the colostrum is mixed with colostrum Slowly add milk to PVA solution at a volume ratio of 1:10 to 2% PVA (polyvinyl alcohol) solution (containing 0.9 wt% NaCl), stir rapidly at 1000rpm for 10min, then stir overnight at 300rpm at a low speed, and solidify , centrifuged, washed with deionized water, and freeze-dried. The SAK-HV encapsulation efficiency of the obtained microspheres was 76%, and the drug loading was 26.3 μg / mg. In the artificial gastric juice, the drug release rate is 37.8% in 2 hours, and in the pH7.2 buffer solution, the drug release rate is 91.5% in 4 hours.

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Abstract

The invention provides an SAK-HV oral controlled-release microsphere. The SAK-HV oral controlled-release microsphere contains SAK-HV fusion protein and polylactic acid-glycolic acid copolymer (PLGA); each mg of the SAK-HV oral controlled-release microsphere contains 5 to 30 [mu]g of the SAK-HV fusion protein; and the particle size of the SAK-HV oral controlled-release microsphere is 1 to 100 [mu]m. A preparation method for the SAK-HV oral controlled-release microsphere comprises the following steps: dispersing a solution containing SAK-HV in a dispersion phase--an organic solvent containing a high-molecular material; then dispersing emulsified fine emulsion in another liquid immiscible with the fine emulsion to form a stable W / O / W emulsion; and removing a volatile solvent in the dispersion phase and allowing a skeletal material to form the microsphere through curing. Results of pharmacodynamic experiments with aopE- / -mouse show that the SAK-HV oral controlled-release microsphere has better lipid-lowering effect than the lipid-lowering effect of atorvastatin; and compared with atorvastatin, the SAK-HV oral controlled-release microsphere has smaller side effect on the liver and earlier action time.

Description

technical field [0001] The invention relates to the cross field of biological preparations and biomedicine, in particular to SAK-HV oral controlled-release microspheres and a preparation method and application thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases are the number one killer of human health. In recent years, its morbidity and mortality have been increasing year by year, and hyperlipidemia is one of its main pathological bases. Currently, statins are the first choice for clinically treating hyperlipidemia. There are few self-developed biological drugs for the treatment of atherosclerosis caused by hyperlipidemia in China, and protein-based drugs for the treatment of hyperlipidemia are still blank in China. Therefore, it is of great significance to develop a new type of high-efficiency lipid-lowering biological drug that can be widely accepted by the public. Contents of the invention [0003] One of the objects of the present inven...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/49A61K9/16A61K47/34A61P3/06A61P9/10
Inventor 徐东刚付文亮景浩然邹民吉王旻毛金武徐涛王园园
Owner INST OF BASIC MEDICAL SCI ACAD OF MILITARY MEDICAL SCI OF PLA