Taxol-cholesterin complex

Abstract

The invention discloses a taxol-cholesterin complex which is prepared by compounding taxol and cholesterin, wherein the weight ratio of the taxol to the cholesterin is between 1:0.09 and 1:0.90; the preferred weight ratio of the taxol to the cholesterin is between 1:0.15 and 1:0.60; and the more preferred weight ratio of the taxol to the cholesterin is between 1:0.23 and 1:0.45. The invention also discloses a preparation method and application thereof in the preparation of submicron emulsion, dry emulsion, self-microemulsion and solid oral preparation. The complex is prepared from the taxol and the cholesterin through the bonding of non-chemical bonds among molecules, thus the solubility of drugs in vegetable oil and n-octyl alcohol is greatly improved, and the taxol-cholesterin complex provides a good intermediate carrier for the preparation of a novel emulsion with high encapsulation rate, good safety and stable quality and an oral preparation with high bioavailability.

Description

technical field [0001] The invention relates to a paclitaxel-cholesterol complex and a preparation method thereof, and also relates to the use of the paclitaxel-cholesterol complex, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Paclitaxel (Taxol) has important antitumor activity and is widely used clinically in the treatment of ovarian cancer, breast cancer, non-small cell lung cancer, head cancer and neck cancer. Because it is almost insoluble in water (0.006μg / ml), paclitaxel injection is currently used clinically It is prepared by dissolving 30 mg of paclitaxel in 5 ml of Cremopher EL (polyoxyethyl castor oil) / ethanol (50:50, V / V) mixed solution. Since the prescription contains a large amount of Cremopher EL, it is easy to cause the release of histamine in the body, leading to severe allergic reactions. For this reason, the following desensitization treatment is required in clinical use: oral administration of dexamethas...

AI Technical Summary

Problems solved by technology

For example, for cholesterol as a lipid material, it is generally believed that the daily intake of cholesterol for healthy adults should not exceed 300 mg (equivalent to the amount of cholesterol contained in one egg yolk), but the compound involved in the existing patent and its preparations, calculated according to the ratio of the two 1:1-19, the maximum intake is equivalent to 19 egg yolks, which is obviously high and has potential safety hazards

[0010] 3) It is unfavorable for the preparation and storage of the submicroemulsion in the later stage: when the compound is used as an intermediate carrier to prepare the submicroemulsion, according to the clinical treatment dose and the specific paclitaxel concentration, the higher the amount of lipid material in the compound is, the more the submicroemulsion will be. The total amount of complexes wrapped in the inner oil phase of the

Limited by the volume of oil droplets in the internal oil phase and the oil-water interface, the more the total amount of encapsulated complexes, the lower the encapsulation efficiency and the worse the stability of the prepared submicroemulsion

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