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4-Amino-2-trifluoromethylphenylretinoate self-microemulsion and preparation method thereof

A technology of trifluoromethyl phenyl retinoic acid ester and self-microemulsion, which is applied in the field of self-microemulsion, can solve the problems of water loss, swelling and softening of capsule shell, influence of preparation stability, storage temperature change, etc., and achieves change in flow rate. The effect of improving solubility, improving solubility, and improving stability

Inactive Publication Date: 2013-10-23
ANHUI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, while studying self-nanometerization to improve bioavailability, researchers often ignore the possible stability of this liquid dosage form: for example, the water in the soft capsule shell can migrate into the nanoemulsion, thereby changing the nanoemulsion. The composition of each phase, and cause the capsule shell to lose water and swell and soften; at the same time, the surfactant and co-surfactant in the nanoemulsion may react with the components of the capsule shell; the storage temperature change may affect the stability of the formulation Wait

Method used

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  • 4-Amino-2-trifluoromethylphenylretinoate self-microemulsion and preparation method thereof
  • 4-Amino-2-trifluoromethylphenylretinoate self-microemulsion and preparation method thereof
  • 4-Amino-2-trifluoromethylphenylretinoate self-microemulsion and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0028] ATPR self-microemulsion consists of the following components by weight:

[0029] Table 1 ATPR self-microemulsion prescription

[0030]

[0031] Mix the surfactant and co-surfactant evenly according to the above prescription, then mix with the oil phase for 30-40 minutes, add the prescribed amount of ATPR, stir until the drug is completely dissolved, and it is obtained from the microemulsion. Dilute with 100 times of distilled water, and the self-emulsification process is completed in 1 minute. After emulsification, the average particle size of the emulsion droplets is measured by a Malvern nanometer particle size analyzer, and the average particle size is between 10-200nm.

Embodiment 2

[0033] Prepare the self-microemulsion according to prescription 3, dilute it with 100 times distilled water, and complete the self-emulsification process in 1 minute. It can be dissolved quickly in the medium, and about 90% can be dissolved in 5 minutes, while only about 10% can be dissolved in 5 minutes for ordinary tablets. See the test results figure 1 .

Embodiment 3

[0035] Weigh the raw materials according to prescription 3, mix them for 40 minutes, make them fully dissolve, and prepare the liquid self-microemulsion. Add the adsorbent prescribed in Table 2 below, stir evenly, and pack into hard capsules. In October, March, and June, no obvious oil leakage and softening of the capsule shell were found in the stability inspection.

[0036] Get 6 capsules of each prescription and carry out dissolution test, dissolution medium is 1000ml of 0.5% sodium lauryl sulfate solution that 25% isopropanol is made, and rotating speed is 100rpm, temperature: (37 ± 0.5) ℃. Sampling 5ml at 5, 10, 20, 30, 45, 60min respectively. After treatment, the dissolution rate of ATPR was detected by high performance liquid chromatography. The HPLC chromatographic conditions are: chromatographic column: Dalian Elite Hypersil ODS column (4.6mm×250mm, 5μm); mobile phase: methanol-water (92:8); flow rate: 1.0ml / min; detection wavelength: 367nm; column temperature: 30°...

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Abstract

The invention relates to a technology of improving the in-vitro dissolution of an indissolvable medicament, discloses a self-microemulsion, and especially discloses an ATPR (4-Amino-2-Trifluoromethyl Phenyl Retinoate) self-microemulsion and a preparation method thereof. The ATPR self-microemulsion is characterized by being prepared from the following components by weight percent: 0.1-20% of ATPR, 1-30% of oil phase, 40-85% of surfactant and 1-40% of cosurfactant. The self-microemulsion and the preparation method provided by the invention have the following beneficial effects: the solubility of the medicament is improved by the ATPR self-microemulsion drug release system, the medicament is dissolved in oil drops and thus protected and the stability of the medicament in vivo is improved, the surfactant is capable of changing the liquidity of the cell membrane and improving the membrane permeability of the medicament, so that the in-vivo absorption of the medicament is increased and the relative bioavailability of the medicament is improved. Besides, the solid self-microemulsion is capable of improving the phenomena of softening and oil leakage of the traditional soft capsules and enhancing the stability of the preparation.

Description

technical field [0001] The invention relates to a self-microemulsion, in particular to a 4-amino-2-trifluoromethylphenyl retinoic acid ester self-microemulsion and a preparation method thereof. Background technique [0002] Malignant tumors are a serious threat to human life. The latest data from the "Sixth China Oncology Academic Conference" shows that more than 2.2 million cancer patients are newly discovered in China every year, and more than 1.6 million people die. The cancer mortality rate has increased by 29.42% in the past 20 years , the medical expenses for tumors can be as high as more than 150 billion yuan per year. Tumor is a disorder of cell differentiation, and its core problem is that the differentiation of normal cells is blocked, and they are similar to undifferentiated embryonic cells in terms of morphology, function, metabolism, and behavior. It has long been believed that once tumor cells are generated, they will remain tumor cells forever, and the non-di...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/232A61K47/44A61K47/34A61P35/00A61K47/10A61K47/26
Inventor 陈飞虎臧洪梅王祺汤继辉石静波吴繁荣
Owner ANHUI MEDICAL UNIV
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