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Efficient low-toxicity gambogic acid nanoemulsion preparation and preparation method and application thereof

A high-efficiency, low-toxicity, gambogic acid technology, which can be used in medical preparations containing active ingredients, pharmaceutical formulations, emulsion delivery, etc. , Improve solubility, strong inhibitory effect

Active Publication Date: 2018-08-28
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability of this component is relatively poor, and it is easily decomposed under the influence of conditions such as solvent, humidity, temperature, light and pH value during production and application. Drugs, especially injections, which have high solubility in organic solvents such as alcohols and ketones, have extremely low solubility in water (0.5μg / mL) and poor stability, and the raw materials of gambogic acid reported at present are mainly used Prepared by dissolving borax solution, the method has poor stability and is not safe for clinical use
In order to enhance the feasibility of the development of gambogic acid, it is necessary to solve the problem of poor solubility of gambogic acid

Method used

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  • Efficient low-toxicity gambogic acid nanoemulsion preparation and preparation method and application thereof
  • Efficient low-toxicity gambogic acid nanoemulsion preparation and preparation method and application thereof
  • Efficient low-toxicity gambogic acid nanoemulsion preparation and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1, gambogic acid nanoemulsion preparation

[0042] Prescription 1: Gambogic acid 0.05g, propylene glycol 4.8g, Tween-80 19.6g, IPM 6g, distilled water 69.55g.

[0043] Preparation method: Mix the surfactant and co-surfactant to make a mixed surfactant, then add gambogic acid and oil phase to the mixed surfactant and mix evenly, then stir with a constant temperature magnetic stirrer, and add dropwise while stirring Distilled water until a nanoemulsion with a clear and transparent appearance was formed.

[0044] Prescription 2: Gambogic acid 0.05g, propylene glycol 9g, Tween-80 27g, IPM 9g, distilled water 54.94g. The preparation method is the same as prescription 1.

[0045] Prescription 3: Gambogic acid 0.5g, Tween-80 27g, Span-80 9g, squalene 9g, distilled water 54.5g. The preparation method is the same as prescription 1.

[0046] Prescription 4: Gambogic acid 1.0g, glycerin 3g, EL-35 27g, GTCC 9g, distilled water 60g. The preparation method is the same...

Embodiment 2

[0063] Embodiment 2, the prescription screening of gambogic acid nanoemulsion preparation

[0064] (1) Screening of nanoemulsion formulations

[0065] a. Selection of oil phase:

[0066] The oil phase GTCC, squalene, isopropyl myristate (IPM), paraffin oil, and peanut oil to be selected are selected as the oil phase with relatively high solubility to gambogic acid, and then the gambogic acid is dissolved respectively. The test results show that at room temperature, the solubility of gambogic acid in squalene, GTCC, and isopropyl myristate is better, and squalene in the oil phase is the best, so squalene, GTCC, and isopropyl myristate are selected. Propyl ester is the oil phase.

[0067] b. Surfactant screening

[0068] Surfactants to be selected in this test include EL-35, Tween-80, RH40, Tween 60, and Tween 20. The five surfactants and the screened oil phase were mixed at room temperature in a mass ratio of 9:1, 8:2, 7:3, 6:4, 5:5, 4:6, 3:7, 2 :8 and :9 mix. After mixin...

Embodiment 3

[0102] Embodiment 3, in vitro L929 cytotoxicity evaluation of gambogic acid nanoemulsion

[0103] A. Cell recovery

[0104] 1) Quickly take the cells out of the liquid nitrogen tank, and immediately place them in a 37°C constant temperature water bath and shake vigorously to thaw the cells quickly;

[0105] 2) Wipe the wall of the cryotube with disinfectant alcohol and place it in an ultra-clean workbench. Unscrew the cap of the cryopreservation tube, transfer the cell cryopreservation solution in the tube to a new centrifuge tube with a pipette, then add 4mL of fresh culture medium to the centrifuge tube, centrifuge at 1000rpm for 5 minutes;

[0106] 3) Carefully discard the supernatant, add 5 mL of complete medium containing 10% FBS, blow the cells gently and transfer them to a cell culture flask;

[0107] 4) Shake the culture bottle slightly to make the culture medium evenly cover the bottom of the culture bottle, unscrew the bottle cap, and place at 37°C, 5% CO 2 cultur...

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Abstract

The invention relates to an efficient low-toxicity gambogic acid nanoemulsion preparation and a preparation method and application thereof. The nanoemulsion preparation comprises a surfactant, a cosurfactant, an oil phase, gambogic acid and water, the particle size of the nanoemulsion preparation is 1 to 100 nm, the potential of the nanoemulsion preparation is -30 to 30 mV, and the dispersity is smaller than 0.3, so that the solubility of gambogic acid can be improved obviously, and the nanoemulsion preparation is a preparation with high quality stability. In vivo animal toxicity tests and invitro cytotoxicity indicate that the gambogic acid nanoemulsion preparation can obviously reduce the toxicity of liver and kidney, the nanoemulsion preparation has an obvious slow release effect, thebioavailability is improved, the resistance to multiplication capacity of acute myeloid leukemia cells is strengthened, and the survival time of leukemic mice is prolonged. The novel nanoemulsion preparation has important practical significance for curing leukemia, particularly acute myelogenous leukemia.

Description

technical field [0001] The invention belongs to the field of pharmacy, relates to an insoluble gambogic acid nanoemulsion preparation, and also relates to a preparation method and application of the preparation. Background technique [0002] Leukemia, also known as "blood cancer", is a malignant clonal disease of malignant stem cells in hematopoietic tissues. Serious damage to the body. Among the countries in the world, the incidence of leukemia is the highest in Europe and North America, with a mortality rate of 3.2-7.4 / 100,000 population. The incidence rate in Asia and South America is relatively low, and the mortality rate is 2.8-4.5 / 100,000 population. Among them, acute lymphoblastic leukemia (ALL) is the malignancy with the highest incidence rate in children (accounting for 26% of all cancer cases). According to the survey, the incidence of leukemia in children <10 years old in my country is 3 / 100,000 to 4 / 100,000. Overall survival for acute lymphoblastic leukemi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/352A61P35/02
CPCA61K9/1075A61K31/352A61P35/02
Inventor 孙红武王泽霖冯子琪崔思鑫杜昱志宋振苗宽贾国熙彭六生张怡邹全明
Owner ARMY MEDICAL UNIV