Small intestine transporter targeting nano calcium carbonate composition for improving oral absorption of insoluble drugs

A technology for insoluble drugs and calcium carbonate, which is applied in drug delivery, active ingredients of hydroxyl compounds, and pharmaceutical formulations, and can solve the problems of insufficient absorption and low efficiency of insoluble drugs

Inactive Publication Date: 2020-04-21
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to overcome the deficiencies of convention

Method used

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  • Small intestine transporter targeting nano calcium carbonate composition for improving oral absorption of insoluble drugs
  • Small intestine transporter targeting nano calcium carbonate composition for improving oral absorption of insoluble drugs
  • Small intestine transporter targeting nano calcium carbonate composition for improving oral absorption of insoluble drugs

Examples

Experimental program
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Embodiment 1

[0040] The preparation of embodiment 1 tablet

[0041] Add 45mL of a mixed solvent of ethanol and water (ethanol: water = 1:2, V / V) into a 200mL beaker, and add 1.0mL of 0.5M CaCl2 solution and 1.0mL of 100mg / mL polyacrylic acid dropwise at a speed of 0.5mL / min Sodium solution, stirred for 5min. Then add 1.0mL 0.5M Na dropwise at a rate of 0.5mL / min 2 CO 3 solution, stirred for 5min. Centrifuge at 8000rpm for 10min, and freeze-dry the precipitate to obtain calcium carbonate nanoparticle freeze-dried powder.

[0042] Take 100 mg of freeze-dried calcium carbonate nanoparticles, add 10 mL of 2 mg / mL paclitaxel methanol solution, add 10 mL of 1 mg / mL TPGS1000 methanol solution linked to Sar-Gly, ultrasonicate for 5 min, stir at room temperature for 20 min, and evaporate to dryness at 30 °C under reduced pressure solvent. Add 50mL HBSS buffer solution, ultrasonic 5min, stir at room temperature 10min, filter with 0.8 μm microporous membrane, obtain the calcium carbonate nanopar...

Embodiment 2

[0043] The preparation of embodiment 2 tablet

[0044] Dissolve 60mg of sodium alginate in deionized water at 30°C, then slowly add 7mL of 0.02M CaCl2 solution, and stir for 30min. Then 7 mL of 0.02M Na was added dropwise 2 CO 3 solution, stirred for 3h. Centrifuge at 8000rpm for 10min, wash several times, and freeze-dry the precipitate to obtain calcium carbonate nanoparticle freeze-dried powder.

[0045] Take 10 mg of freeze-dried calcium carbonate nanoparticles, add 1 mL of 0.5 mg / mL doxorubicin aqueous solution, add 1 mL of 1 mg / mL carnitine-linked Pluronic F68 aqueous solution, sonicate for 5 min, stir at room temperature for 10 h, centrifuge, and wash , and lyophilized to obtain a carnitine-modified calcium carbonate nanoparticle composition loaded with doxorubicin. Then pass the freeze-dried powder through a 80-mesh sieve, mix with microcrystalline cellulose, add starch slurry to make a soft material, granulate with a 14-mesh sieve, dry at 40°C, pass through a 12-me...

Embodiment 3

[0046] The preparation of embodiment 3 hard capsules

[0047] Add 10mL of 20mM Na to a 100mL beaker 2 CO 3 solution and polyethylene sulfonic acid, stirred for 1 min. Then slowly add 10mL of 20mM CaCl2 solution, react at room temperature for 10h. After centrifuging at 8000 rpm for 10 min, the precipitate was washed three times with Tris buffer solution of pH 9, and then freeze-dried to obtain freeze-dried powder of calcium carbonate nanoparticles.

[0048] Take 10 mg of freeze-dried calcium carbonate nanoparticles, add 2 mL of 1 mg / mL cyclosporine A methanol solution, add 1 mL of 1 mg / mL methanol solution of PEG2000-PLA1800 linked to deoxycholic acid, ultrasonicate for 5 min, and stir at room temperature for 0.5 h, the solvent was evaporated to dryness under reduced pressure at 30°C. Add 5mL HBSS buffer solution, ultrasonic 5min, stir at room temperature 10min, filter with 0.8 μm microporous membrane, obtain the calcium carbonate nanoparticle composition loaded with cyclos...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to a calcium carbonate nanoparticle composition for improving oral absorption of insoluble drugs, wherein the compositioncomprises an insoluble drug, an amphiphilic polymer, an amphiphilic polymer linked to a substrate of a transporter expressed by small intestinal epithelial cells, calcium carbonate nanoparticles andan optional pharmaceutic adjuvant. According to the invention, the experiment results prove that the composition can obviously improve the oral absorption of insoluble drugs, and provides a novel preparation strategy for oral administration of insoluble drugs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a nano-calcium carbonate composition targeting small intestinal transporters that improves the oral absorption of insoluble drugs, and the composition can also be used for injection administration. Background technique [0002] Oral administration is a convenient, painless, patient-compliant and easy-to-administer route. Nearly 70% of the top 200 orally sold drugs in the Orange Books of the US, UK, Spain, and Japan are poorly soluble. Therefore, for a long time, the dissolution and absorption of poorly soluble drugs has been a problem that plagues people. For this class of drugs with poor curative effect due to less absorption, it is often at the expense of increasing the dose to improve the curative effect, which causes the increase of toxic and side effects and the rise of drug cost. Therefore, improving the oral absorption of poorly soluble drugs is a research hotspo...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K45/00A61K9/19A61K9/20A61K9/48A61K31/05A61K31/337A61K31/704A61K38/13A61K47/54A61K47/64
CPCA61K9/0019A61K9/0053A61K9/0095A61K9/19A61K9/2059A61K9/4808A61K31/05A61K31/337A61K31/704A61K38/13A61K45/00A61K47/542A61K47/549A61K47/554A61K47/64A61K47/6923
Inventor 刘艳邓运强靳尧李馨儒周艳霞
Owner PEKING UNIV
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