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Apatinib polymeric micelle and preparation method thereof

A technology of apatinib and polymer glue, which is applied in the field of apatinib polymer micelles and its preparation, can solve the problems of poor solubility, large side effects, and low bioavailability of apatinib, and improve the curative effect , increased solubility, and high biocompatibility

Inactive Publication Date: 2018-08-03
杭州市肿瘤医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The purpose of the present invention is to overcome the disadvantages of poor solubility, low bioavailability and large side effects of apatinib in the existing oral preparations, and provide a kind of apatinib with high solubility, low side effects, good biocompatibility and simple and feasible preparation process. Tini micelles and preparation method thereof

Method used

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  • Apatinib polymeric micelle and preparation method thereof
  • Apatinib polymeric micelle and preparation method thereof
  • Apatinib polymeric micelle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of a kind of PEG-PLA entrapped apatinib micelles

[0030] 40mgPEG 5K -PLA 10K Dissolve together with 4mg of apatinib in 5ml of acetone solvent as the organic phase; mix 5ml of water and 5ml of ethanol to form the water phase; drop the organic phase into the water phase at a speed of 1ml / min, stir at a low speed of 300r / min to form a shallow The blue nanoemulsion was reacted for 2 minutes, then transferred to a rotary evaporator, and treated for 5 minutes under vacuum rotary evaporation at 37° C., and the acetone solution was removed to obtain apatinib micelles. The average particle size measured by the laser dynamic scattering instrument is 76.53±0.58nm, and the particle size distribution results are as follows: figure 1 shown. The encapsulation efficiency of nanoparticles is 89.11±1.04%, and the dispersion coefficient is 0.361.

[0031] Example 1: Preparation of apatinib micelles loaded with PEG-PLA and TPGS

[0032] 20mgPEG 5K -PLA ...

Embodiment 3

[0033] Embodiment 3: In vitro drug release experiment of micelles containing Apatinib

[0034] Dissolve the prepared Apatinib micelles (Example 1 and Example 2) in an appropriate amount of PBS buffer (pH7.4, containing 0.2% Tween 80), and dilute to Apatinib 0.1 mg / mL , mix well. Take 9mL and put it in the dialysis bag, and tighten the dialysis bag. Put the dialysis bag into 50mL PBS buffer solution (pH7.4, containing Tween 800.2%), 37°C, 100r / min, and take 1.0mL of PBS solution outside the dialysis bag at different time points. Determine the content of Apatinib respectively (chromatographic column: ODS2 (Lichrospher-C18, 250 × 4.6mm, 5 μ m); mobile phase: methanol-acetonitrile-water (30:40:32); flow rate: 1.0mL / min, detection wavelength : 226nm; column temperature: 30°C), see the results figure 2 .

Embodiment 4

[0035] Embodiment 4: In vivo pharmacokinetic experiment of apatinib micelles

[0036] In vivo pharmacokinetic experiments were carried out on the apatinib micelles prepared in Example 1 and Example 2. A total of 8 healthy female SD rats (200±10) grams were taken and randomly divided into 2 groups with 4 rats in each group. The dose of 10 mg / kg was administered to the tail vein of each group of rats, and 200 μL of blood was collected after 5 minutes, 15 minutes, 30 minutes, 45 minutes, 1, 2, 4, 7, 12, and 24 hours, and centrifuged at 5000 rpm. separate. After acetonitrile treatment, the content of apatinib in plasma was detected by high performance liquid chromatography. Figure 5 is the obtained drug-time curve.

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Abstract

The invention discloses apatinib polymeric micelle which is prepared from apatinib as a main medicine and an amphiphilic polymer material as a carrier. A preparation method comprises the following steps: 1) dissolving apatinib and a polymer into an organic solvent so as to obtain a co-solution; 2) dropping the co-solution into stirred water, and stirring at the same time; 3) evaporating off the organic solvent; 4) filtering off medicines which are not packaged and can be separated out by using a filtering membrane, thereby obtaining the apatinib polymeric micelle. The apatinib polymeric micelle disclosed by the invention is low in side effect, high in biocompatibility and simple, convenient and feasible in preparation process.

Description

Technical field: [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an apatinib polymer micelle and a preparation method thereof. Background technique: [0002] Cancer is a major cause of death among Chinese residents, and its morbidity and mortality have continued to rise in recent years. According to statistics, more than 2.8 million people died of cancer in my country in 2016, with an average of 7,500 people every day. Among them, gastric cancer, lung cancer, liver cancer, esophageal cancer and colorectal cancer accounted for 3 / 4 of all cancer deaths. In addition, the five-year survival rate of overall cancer in my country is only 30.9%, which is at a relatively low level. At the 12th International Gastric Cancer Conference (IGCC), Professor Ji Jiafu, chairman of the conference and president of Peking University Cancer Hospital, said that there are about 680,000 new cases of gastric cancer in my country every year, accoun...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K47/22A61K31/444A61P35/00
CPCA61K9/1075A61K31/444A61K47/22A61K47/34A61P35/00
Inventor 王凯峰陈艺丹吴式琇余波张晓敏莫丽钦陈碧龚琳燕杨斐
Owner 杭州市肿瘤医院
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