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Preparation method of fluorouracil targeted slow release drugs based on ganoderma spores

A technology of Ganoderma lucidum spores and fluorouracil is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can achieve the effect of stable physical properties and good elasticity

Inactive Publication Date: 2020-01-17
CHANGCHUN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to its insolubility in water, low dissolution rate and bioavailability, frequent medication is required to maintain the therapeutic concentration, and it has a great stimulating effect on the gastrointestinal tract and strong toxic and side effects, which limits its application to a certain extent.

Method used

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  • Preparation method of fluorouracil targeted slow release drugs based on ganoderma spores
  • Preparation method of fluorouracil targeted slow release drugs based on ganoderma spores
  • Preparation method of fluorouracil targeted slow release drugs based on ganoderma spores

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 A preparation method of ganoderma spore-based fluorouracil targeted sustained-release medicament

[0046] (1) Preparation of hollow ganoderma lucidum spores: get 10g ganoderma lucidum spores, heat and stir it with 300ml 85% (v / v) acetone solution in a reflux device at 70°C for 24h, rinse three times with deionized water after reflux ends, degreasing ganoderma spores can be obtained by drying at ℃. Then soak and mix 2g of defatted Ganoderma lucidum spores with 18% (w / v) potassium hydroxide solution (9g of potassium hydroxide particles in 41ml of deionized water) at room temperature for 24h; filter, wash with water and 95% ethanol three times respectively , put it into a lyophilizer and freeze for 12 hours to obtain the ganoderma spores after alkali hydrolysis; finally put it and 60ml 85% (v / v) orthophosphoric acid solution in a reflux device and heat and stir for 6 hours at 70°C, after the reaction , filtered, washed with water and 95% ethanol three times resp...

Embodiment 2

[0060] The impact of different initial concentrations of embodiment 2 on drug loading

[0061] The concentration of the prepared 5-FU solution is 0.5mg / ml, 1mg / ml, 2mg / ml, 3mg / ml, 4mg / ml, 5mg / ml, 6mg / ml, 7mg / ml, 8mg / ml, accurately weigh 0.05g Put MGLS into centrifuge tubes respectively, then add 10ml of the 5-FU solution with the above concentration, place in a constant temperature water bath and shake for 2 hours, after the adsorption balance, use an external magnetic field to separate, and measure the absorbance in the supernatant after separation to calculate Its concentration, get the impact of different 5-FU concentration on the drug loading, the results can be found in Figure 10 .

[0062] Figure 10 The experimental results show that under the same mass of MGLS, the drug loading capacity gradually increases with the increase of the concentration of 5-FU, because the higher the concentration of 5-FU solution, the more molecules in the solution, so that MGLS The highe...

Embodiment 3

[0063] Embodiment 3 The influence of different MGLS dosages on drug loading

[0064] Accurately weigh 0.01g, 0.03g, 0.05g, 0.07g, 0.09g of MGLS and put them into 10ml of 5mg / ml 5-FU solution respectively, place in a constant temperature water bath and shake for 2h, after the adsorption is balanced, use additional Magnetic field separation, and the absorbance in the supernatant after separation was measured to calculate its concentration, and the influence of different microsphere dosage on drug loading was obtained. For the results, see Figure 11 .

[0065] Figure 11 The experimental results showed that in the same concentration of 5-FU solution, the drug loading decreased linearly with the increase of MGLS dosage, because the increase of MGLS dosage provided more loading sites, while the 5-FU solution The concentration is constant, so the amount of drug loaded will decrease with the increase of MGLS dosage.

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Abstract

The invention discloses a preparation method of fluorouracil targeted slow release drugs based on ganoderma spores, and belongs to the technical field of drug carriers and slow release. The preparation method of the fluorouracil targeted slow release drugs based on the ganoderma spores includes the steps: firstly, pretreating natural ganoderma spores to obtain a natural nontoxic internally and externally through ganoderma spore carrier with good biocompatibility; secondly, synthesizing Fe3O4 nanoparticles on the surfaces of the ganoderma spores and inside the ganoderma spores by a chemical coprecipitation method to magnetize the ganoderma spores; thirdly, combining the ganoderma spores with fluorouracil serving as a broad-spectrum anti-tumor drug by the aid of a vacuum loading technique. The preparation method can be used for preparing the fluorouracil oral targeted drugs. The fluorouracil drugs are positioned in a diseased region under the action of an external magnetic field and released, adverse drug reaction is reduced, administration frequency is decreased, maximum drug therapeutic effects are achieved, and a new approach is provided for oral medication and magnetic targeted chemotherapy.

Description

technical field [0001] The invention relates to the technical field of drug carrier and sustained release, and more specifically relates to a preparation method of ganoderma spore-based fluorouracil targeted sustained release medicament. Background technique [0002] When traditional drugs are released in the human body, the blood drug concentration is unstable, the drug utilization rate is low, and the toxicity and side effects are large. Therefore, the study of drug sustained-release carriers has always been a research hotspot of sustained-release pharmaceuticals at home and abroad. The targeted drug therapy technology has also attracted more and more people's attention, especially through the in vitro magnetic permeation targeting technology, because the magnetic nanoparticles have unique physical and chemical properties, which can realize targeted drug delivery, thereby avoiding drug administration. Insufficient or overdose can reduce the damage of drugs to normal tissue...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/52A61K47/46A61K31/513A61P35/00A61K41/00
CPCA61K9/5063A61K31/513A61K41/00A61P35/00
Inventor 李景梅韩斌翁占坤梁开然曲英敏王作斌
Owner CHANGCHUN UNIV OF SCI & TECH
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