Nano-drug sustained release preparation for treating malignant tumor and preparation method thereof

A technology of sustained-release preparations and nano-drugs, applied in the field of medicine, can solve problems such as greater influence on solubility, many adverse reactions, slow oral absorption, etc., and achieve the effects of prolonging survival time, simple preparation method, and preventing agglomeration and precipitation

Inactive Publication Date: 2017-10-17
THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But along with the widespread application of gefitinib and more and more studies show, gefitinib oral formulations have following defects: poor water solubility, solubility is greatly affected by pH; maximum bioavailability is only 59% ; slow oral abso

Method used

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  • Nano-drug sustained release preparation for treating malignant tumor and preparation method thereof
  • Nano-drug sustained release preparation for treating malignant tumor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Preparation and application of PLA (polylactic acid) nano-sustained-release preparations loaded with gefitinib:

[0029] Prepared by emulsification volatilization method: Weigh 10 mg of gefitinib and 90 mg of PLA (polylactic acid) polymers and dissolve them in 5 ml of dichloromethane, then add 50 ml of 1% poloxamer F68 aqueous solution, and mix at high speed The mass machine was cut at a speed of 6000-15000 rpm for 5-20 minutes, and then the organic solvent was removed by rotary evaporation under reduced pressure at room temperature for 1 hour to obtain a nanoparticle suspension. The above-mentioned prepared nanoparticles were filtered and centrifuged. After several times, add a freeze-drying protection agent for freeze-drying storage, and the particle size of the nanoparticles prepared above is controlled within the range of 10-1000 nanometers.

[0030] Redissolve the above-mentioned gefitinib nano drug powder after freeze-drying in normal saline or glucose injection t...

Embodiment 2

[0032] Preparation and application of PEG-PCL (polymer of polyethylene glycol and polycaprolactone) nano-sustained-release preparations loaded with gefitinib:

[0033] Prepared by film emulsification method: Weigh 10 mg of gefitinib and 90 mg of PEG-PCL polymer and dissolve them in 5 ml of absolute ethanol, then remove the organic solvent by rotary evaporation under reduced pressure at room temperature for 1 hour, and the addition temperature is 10-65 Oscillating and redissolving in deionized water at ℃ to obtain a nanoparticle suspension. After filtering the above-mentioned nanoparticles, add a freeze-drying protective agent and freeze-dry them for storage. The particle size of the above-mentioned nanoparticles is controlled within the range of 10-1000 nanometers .

[0034] The gefitinib nano-drug freeze-dried powder prepared above was redissolved in normal saline or glucose injection to obtain the sustained-release injection of gefitinib nano-drug, and a mouse liver cancer m...

Embodiment 3

[0036]Preparation and application of Pluronic-PLGA (a polymer of poloxamer and polylactic-glycolic acid) nano-sustained-release formulation loaded with icotinib:

[0037] Prepared by self-assembly method: Weigh 20 mg of Icotinib and 80 mg of Pluronic-PLGA polymer dissolved in 5 ml of acetone, then slowly add dropwise to 50 ml of 1% poloxamer F68 aqueous solution, and then reduce at room temperature Press rotary evaporation for 1 hour to remove the organic solvent to obtain a nanoparticle suspension. After the above-mentioned nanoparticles are filtered and centrifuged for several times, they are added with a freeze-drying protective agent and freeze-dried. The particle size of the above-mentioned nanoparticles is controlled at In the range of 10-1000 nanometers.

[0038] The above-mentioned icotinib nano-medicine powder after freeze-drying was redissolved in normal saline or glucose injection to prepare gefitinib nano-medicine sustained-release injection, and a rat gastric canc...

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Abstract

The invention discloses a nano-drug sustained release preparation for treating a malignant tumor and a preparation method thereof. The preparation is formed by an epidermal growth factor receptor tyrosine kinase inhibitor with the tumor growth inhibition effect, a high-molecular polymer and a freeze-drying protective additive. The preparation method is simple, suitable for the large-scale production, and particularly suitable for preparing an antitumor drug nano-preparation with the characteristics of long blood circulation time, biodegradation in vivo, slow release of drugs, and passive targeting. The antitumor nano-drug sustained release preparation prepared by the method is suitable for the management by using modes, such as intravenous injection, intramuscular injection, intratumor injection and peritumoral injection, and applied to the treatment of the malignant solid tumors, such as lung cancer, liver cancer, gastric cancer, intestinal cancer, esophagus cancer, nasopharyngeal cancer, uterus cancer, breast cancer, glioma cancer, ovarian cancer, and prostate cancer, and has the good application prospect.

Description

technical field [0001] The invention relates to the field of medical technology, and relates to a sustained-release nano drug preparation for treating malignant tumors and a preparation method thereof Background technique [0002] In recent years, the incidence and mortality of malignant tumors in my country have remained high, and the situation has become more and more serious. In particular, the incidence and mortality of lung cancer have been rising year by year, ranking first among malignant tumors and seriously threatening human health. For the treatment of lung cancer, there are mainly surgical treatment, chemotherapy, radiotherapy, targeted therapy, etc. Among various treatment methods, targeted therapy is an important means for the treatment of lung adenocarcinoma. In recent years, based on the study of the molecular level of tumor lesions, many new therapeutic targets have been discovered, which provides the possibility for the development of new drugs with high eff...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/34A61K47/10A61K31/5377A61K31/519A61K31/517A61K49/00A61P35/00
CPCA61K9/0002A61K9/0019A61K9/08A61K31/517A61K31/519A61K31/5377A61K47/10A61K47/34A61K49/0008
Inventor 傅少志倪晓玲吴敬波
Owner THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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