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Pharmaceutical composition and its preparation method

A composition and drug technology, applied in the field of pharmaceutical composition and its preparation method, can solve problems such as complicated manufacturing process, poor coating rate, drug leakage, etc.

Active Publication Date: 2019-10-15
SPRING FOUND OF NCTU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, coating the two drugs with multiple shells is prone to problems such as drug leakage, poor coating rate, and complicated manufacturing process.
In addition, if it is desired to coat drugs by polymer self-assembly, it is difficult to coat both hydrophilic and hydrophobic drugs
[0004] Therefore, how to solve the known process problem that multiple steps and multiple environments are required for coating multiple drugs on nanoparticles, and provide a single step to coat hydrophilic and hydrophobic drugs at the same time to prepare drug-loaded particles is really an important step. an important topic

Method used

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  • Pharmaceutical composition and its preparation method
  • Pharmaceutical composition and its preparation method
  • Pharmaceutical composition and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: Preparation of amphiphilic chitosan derivatives modified by hydrophobic hexanoyl group and hydrophilic carboxylic acid

[0041] First, 5 grams (g) of chitosan (Mw = 215,000 g / mol, 80 to 90% deacetylation, purchased from Adrich-Sigma) was suspended in isopropanol (50 milliliters (mL)) at room temperature , and stirred for 30 minutes. The resulting suspension was slowly mixed with aqueous sodium hydroxide solution (12.5 mL) to obtain a mixed solution, and the amount of grafted hydrophilic functional groups could be controlled by adjusting the concentration of sodium hydroxide in the mixed solution. Here, the mixed solution contained 13.3M sodium hydroxide. Next, the mixed solution was reacted with chloroacetic acid to prepare water-soluble hydrophilic carboxymethyl-modified chitosan, and dried.

[0042] 2 g of dried hydrophilic carboxyformic acid-modified chitosan was dissolved in pure water (50 mL), and stirred for 24 hours. Next, the obtained solution w...

Embodiment 2

[0044] Embodiment 2 Utilizes amphiphilic chitosan derivatives to coat medicine

[0045] Take by weighing the amphiphilic chitosan powder prepared in Example 1 of 0.5 milligrams (mg), add 200 microliters (μ L) of 0.1% demethoxycurcumin (dissolved in methanol), and utilize a shaker to mix slightly Finally, add 540 μL of double distilled water, then add 60 μL of pH 10.5 double distilled water, finally add 200 μL of 0.1% cisplatin (cisplatin) (dissolved in water), and stir for 12 hours to prepare the coated double drug (containing demethoxycurcumin and cisplatin) nanoparticles.

Embodiment 3

[0046] The coating rate test of the nanoparticle of embodiment 3 coating double drug

[0047] Put the synthesized double-drug coated nanoparticles into a concentrating centrifuge tube, and centrifuge at 4000 rpm for 30 minutes.

[0048] (1). Cisplatin coverage

[0049] Dilute the supernatant of the concentrated centrifuge tube by 20 times, mix it with 0.14% o-phenylenediamine in dimethylformamide solution at a ratio of 1:1, heat at 100°C for 30 minutes, and put it in a -20°C refrigerator for 10 minutes After cooling, the solution is finally detected by UV-visible light at the peak at a wavelength of 705nm. After conversion, the uncoated cisplatin content is obtained, and then the cisplatin coating rate is obtained.

[0050] (2). Demethoxycurcumin coating rate test

[0051] The nanoparticles on the filter membrane of the concentrated centrifuge tube were redissolved with twice distilled water, and the solution was mixed with methanol at a ratio of 1:1, and analyzed by HPLC. ...

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Abstract

The present invention relates to a pharmaceutical composition and a preparation method thereof. Specifically, a preparation method of a pharmaceutical composition includes: dispersing an amphiphilic chitosan derivative, at least one hydrophobic drug, and at least one hydrophilic drug in a solvent to form a mixed solution, wherein, The amphiphilic chitosan derivative is modified by a plurality of hydrophilic groups and a plurality of hydrophobic groups, and the pH of the mixed solution is adjusted to a range in which the hydrophilic drug and the hydrophobic drug do not precipitate; and stirring the mixture After the solution is at least 12 hours, when the pH of the mixed solution is between 6 and 7, the pharmaceutical composition is collected to simultaneously coat hydrophilic and hydrophobic drugs by a one-pot synthesis method, and perform protein synthesis by a one-pot synthesis method. modified to provide a multifunctional pharmaceutical composition.

Description

technical field [0001] The present invention relates to a pharmaceutical composition and a preparation method thereof, in particular to a pharmaceutical composition in which hydrophobic drugs and hydrophilic drugs are coated with amphiphilic chitosan and a preparation method thereof. Background technique [0002] Chitin is widely distributed in nature. In addition to crustaceans (such as shrimp, crab, and insect shells), it also includes microorganisms (bacterial cell walls or mushrooms) and algae in the plant kingdom. . Chitosan (chitosan) [poly (β-1,4-glucosamine)] [poly (β-1,4-glucosamine)], also known as chitosan, is made of chitin through different degrees of deacetylation reaction resulting heterogeneous aggregates. Chitosan is a copolymer of N-acetylglucosamine and N-glucosamine as structural units, and the content of N-glucosamine structural units in the polymer is usually higher than 60%. Due to chitosan's good biocompatibility (biocompatibility), non-toxicity, b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/68A61K49/00A61K33/24A61P35/00A61K31/12A61K33/243
CPCA61K47/36A61K47/6857A61K47/6939A61K9/5161A61P35/00A61P43/00A61K33/243A61K31/12
Inventor 黄唯婷李翊绮刘典谟
Owner SPRING FOUND OF NCTU
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