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Oral hydroxyl silk peptide nanoparticles and preparation method thereof

A nanoparticle, hydroxyl silk peptide technology, applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, digestive system, etc., can solve the problems of difficult to pass through the biofilm barrier, incomplete oral absorption, poor membrane permeability, etc., to achieve improved Bioavailability, promote gastrointestinal absorption, and improve stability

Inactive Publication Date: 2015-10-28
DALIAN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Hydroxyserin has good water solubility and small molecular weight (about 200 Daltons), which is a drug with low permeability, and the permeability coefficient is about 5.01×10 -6 (cm / sec), that is, the membrane permeability of oral drugs is poor, and it is difficult to pass through the biofilm barrier
In addition, due to the presence of a large number of peptidases and proteolytic enzymes in the gastrointestinal tract, direct oral administration of hydroxyl silk peptide is prone to first-pass effect and is eliminated by liver metabolism.
The result of the experiment was that after the rats were directly orally administered with hydroxylase peptide, t 1 / 2 Only 30~40min, the oral absorption is incomplete, and the bioavailability is about 30%. The therapeutic effect can only be achieved through frequent administration, which is time-consuming and laborious.

Method used

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  • Oral hydroxyl silk peptide nanoparticles and preparation method thereof
  • Oral hydroxyl silk peptide nanoparticles and preparation method thereof
  • Oral hydroxyl silk peptide nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] a. Weigh 10mg of polyvinyl alcohol (PVA), dissolve it in 1ml of deionized water to obtain a PVA solution with a mass volume fraction of 1%, and dissolve 10mg of hydroxyl silk peptide in 0.5ml of the above PVA solution to form an inner water phase; Take 15 mg Tween 80 and 30 mg polyglycolide-lactide copolymer (PLGA, molecular weight 15000, purchased from Singma Company) and dissolve in 1.5 ml ethyl acetate to form an oil phase; take 0.2 ml of the inner water phase and 1.5 ml oil phase mixed, 100W ultrasonic emulsification for 30 sec, to obtain W / O colostrum;

[0026] b. Weigh 150mg of PVA, dissolve in 15ml of deionized water to form an external aqueous phase with a mass volume fraction of 1%; mix 12ml of external aqueous phase with 1.7ml of W / O colostrum obtained in step a, and ultrasonic emulsify at 100W for 60 sec , get W / O / W double milk;

[0027] c. Place the W / O / W double emulsion obtained in step b in a water bath at 40°C, and evaporate under reduced pressure to obt...

Embodiment 2

[0031] a. Weigh 20mg of polyvinyl alcohol (PVA), dissolve it in 1ml of deionized water to obtain a PVA solution with a mass volume fraction of 2%, and dissolve 30mg of hydroxyl silk peptide in 1ml of the above PVA solution to form an inner water phase; weigh 40mg of F68 and 40mg of polylactic acid (PLA, purchased from Jinan Daigang Bioengineering Company) were dissolved in 2ml of ethyl acetate to form an oil phase; 0.5ml of the inner water phase was mixed with 2ml of the oil phase, and ultrasonically emulsified at 200W for 1min to obtain W / O colostrum;

[0032] b. Weigh 300mg of PVA, dissolve it in 15ml of deionized water to form an external water phase with a mass volume fraction of 2%; mix 12ml of the external water phase with 2.5ml of the W / O colostrum obtained in step a, and ultrasonically emulsify at 100W for 2min. Get W / O / W double milk;

[0033] c. Put the W / O / W double emulsion obtained in step b in a water bath at 35°C, and evaporate under reduced pressure to obtain a...

Embodiment 3

[0037] a. Weigh 10mg of polyvinyl alcohol (PVA), dissolve it in 0.5ml of deionized water to obtain a PVA solution with a mass volume fraction of 2%, and dissolve 20mg of hydroxyl silk peptide in 0.5ml of the above PVA solution to form an inner water phase; Weigh 45mg F68 and 60 mg polyglycolide-lactide copolymer (PLGA, molecular weight 47000, purchased from Singma Company) and dissolve in 1.5ml ethyl acetate to form an oil phase; take 0.5ml internal water phase and 1.5ml The oil phase is mixed, 100W ultrasonic emulsification for 1.5min, and W / O colostrum is obtained;

[0038] b. Weigh 200mg of PVA and dissolve it in 20ml of deionized water to form an external aqueous phase with a mass volume fraction of 1%; mix 18ml of the external aqueous phase with 2ml of the W / O colostrum obtained in step a, and ultrasonic emulsify at 100W for 1min to obtain W / O / W complex milk;

[0039] c. Put the W / O / W double emulsion obtained in step b in a water bath at 45°C, and evaporate under reduced...

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Abstract

The invention discloses oral hydroxyl silk peptide nanoparticles capable of prolonging the half-life period of hydroxyl silk peptide and improving the oral bioavailability of the hydroxyl silk peptide and a preparation method thereof. The oral hydroxyl silk peptide nanoparticle comprises the following components in percentage by mass: 5-15% of hydroxyl silk peptide, 20-45% of carrier, 20-45% of polyvinyl alcohol and 5-20% of emulsifier. The preparation method comprises the following steps of: preparing W / O emulsion of the hydroxyl silk peptide and carrier material by an ultrasonic emulsifying method; performing ultrasonic dispersion of the W / O emulsion in a stabilizer solution to form W / O / W multiple emulsion; volatizing the solvent of the W / O / W multiple emulsion to obtain nanoparticle suspension; and purifying and freeze-drying the nanoparticle suspension to obtain the nanoparticle powder.

Description

technical field [0001] The invention relates to a hyseride preparation, in particular to an oral hyseride nanoparticle capable of prolonging the half-life of the hyseride and improving the oral bioavailability of the hyseride and a preparation method thereof. Background technique [0002] Hydroxyserin, whose chemical name is cyclotrans-4 L-hydroxyprolylserine, is an active dipeptide extracted and isolated from the Japanese anti-hepatitis drug Laennec (trade name of human placental hydrolyzate). Its chemical structure is as follows : [0003] [0004] At present, Hydroxyserin is artificially synthesized by Japan Biopharmaceuticals Co., Ltd. and has been sold publicly. Existing experiments have shown that hydroxyl serin has good anti-hepatitis activity and little adverse reaction. However, Hydroxyserin has good water solubility and small molecular weight (about 200 Daltons), which is a drug with low permeability, and the permeability coefficient is about 5.01×10 -6 (cm / ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/4985A61K47/34A61K47/32A61P1/16
Inventor 刘克辛李磊王长远高鹏程田燕
Owner DALIAN MEDICAL UNIVERSITY
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