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Flucoladine nano-micelle preparation as well as preparation method and application thereof

A nano-micelle and preparation technology, which is applied in the field of medicine, can solve problems such as poor safety, and achieve the effects of increased bioavailability, high bioavailability, and increased blood drug concentration

Pending Publication Date: 2022-03-04
BEIJING SHENOGEN PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the applicant has found that the self-emulsifying agent of the compound of formula A has the disadvantage of poor safety during administration to animals. Therefore, it is necessary to develop a preparation with high safety and high bioavailability

Method used

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  • Flucoladine nano-micelle preparation as well as preparation method and application thereof
  • Flucoladine nano-micelle preparation as well as preparation method and application thereof
  • Flucoladine nano-micelle preparation as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Preparation of Fluocoridine Nanomicelle Oral Liquid

[0071] Flucoridine raw material 2.4g is dissolved in the 0.2mol / L sodium hydroxide aqueous solution of 120mL, and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer 4.8g and 4.8g poloxa Mu 407 was dissolved in 480 mL of 0.05 mol / L hydrochloric acid aqueous solution. Under high-speed stirring at 1000 rpm, the sodium hydroxide solution mixed with flucoridine was added to the hydrochloric acid aqueous solution of the polymer through a peristaltic pump, and then continued to stir for 20 minutes. Then centrifuge at 10,000 rpm for 20 minutes to remove the precipitate, and the supernatant is the fluocoridine micelle solution. The concentration of flucoridine was 3.6 mg / mL. The resulting solution was ultrafiltered in an ultrafiltration cup with a regenerated cellulose filter membrane (100KDa), to obtain a higher concentration of fluocladine micellar solution, the concentration of flucoridine was ...

Embodiment 2

[0076] Preparation of Fluocoridine Micellar Concentrate

[0077] Dissolve 2 g of flucoridine raw material in 140 mL of acetone, and dissolve 20.0 g of polyethylene glycol 15 hydroxystearate and 5.0 g of tocopheryl polyethylene glycol succinate in 500 mL of purified water. Under 1000 rpm high-speed stirring by a peristaltic pump, the acetone solution dissolved with flucoridine is added dropwise to the solution of polyethylene glycol 15 hydroxystearate and tocopheryl polyethylene glycol succinate, dropwise Stirring was then continued for 20 minutes after the addition was complete. Then place the reaction solution in a ventilated place and stir at 200 rpm to volatilize the acetone in the reaction solution for more than 36 hours until the acetone is completely volatilized. The remaining solution is centrifuged at 20°C and 12000 rpm for 20 minutes to remove the precipitate and the supernatant The solution is the micellar solution of flucoridine. The concentration of flucoridine...

Embodiment 3

[0079] Preparation of Fluocoridine Micellar Concentrate

[0080] Dissolve 1.0 g of flucoridine in 70 mL of acetone, and dissolve 20.0 g of polyethylene glycol 15 hydroxystearate and 0.25 g of sodium lauryl sulfate in 200 mL of purified water. Under high-speed stirring at 1000 rpm, the acetone solution dissolved with flucoridine is added dropwise to the solution of polyethylene glycol 15 hydroxystearate and sodium lauryl sulfate through a peristaltic pump. Stirring was then continued for 10 minutes. Then place the reaction solution in a ventilated place and stir at 300 rpm to volatilize the acetone in the reaction solution for more than 24 hours until the acetone is completely volatilized. The remaining solution is centrifuged at 20°C and 12000 rpm for 20 minutes to remove the precipitate and the supernatant That is flucoridine micellar solution. The concentration of flucoridine was 5 mg / mL. Using regenerated cellulose filter membrane (100Kda) for membrane filtration and c...

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Abstract

The invention provides a nano-micelle preparation of flucoradine. The preparation comprises flucoradine and a polymer auxiliary material. The invention also provides a preparation method of the flucoladine nano-micelle preparation. The flucoladine nano-micelle preparation disclosed by the invention has the advantage of high bioavailability.

Description

technical field [0001] The invention relates to a nano-micelle preparation of flucoridine. The preparation method and application of the preparation belong to the field of medicine. Background technique [0002] Flucoladine is a brand-new and effective monomer obtained through structural optimization on the basis of Alcoradine, and its structural formula is shown in the following formula (A): [0003] [0004] The patent of application number 201210573072.6 discloses the compound of the above formula A, and discloses that the compound has the ability to treat tumors, such as breast cancer, colon cancer, endometrial cancer, leukemia, liver cancer, lymphoma, lung cancer, prostate cancer, gastric cancer or role in pancreatic cancer. However, during the research and development process, the applicant found that flucoradine has the disadvantage of poor solubility in water and oil, and it is difficult to make a solvent. [0005] The patent publication number WO2016127925 disc...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/08A61K9/20A61K47/34A61K47/32A61K47/10A61K47/38A61K47/22A61K47/14A61K31/352A61P35/00A61P35/02
CPCA61K9/1075A61K9/0095A61K9/2027A61K47/34A61K47/32A61K47/10A61K47/38A61K47/22A61K47/14A61K31/352A61P35/00A61P35/02
Inventor 汤城陈小明姚华孟坤尹海燕
Owner BEIJING SHENOGEN PHARMA GRP
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