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Anti-cancer ent-11 alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid 5F oral emulsion and preparation method thereof

A half-flag, anti-tumor technology, applied in the direction of anti-tumor drugs, emulsion delivery, active ingredients of anhydride/acid/halide, etc. It can solve the problems of poor patient compliance, increased trouble for patients, and inconvenient administration of injections, etc., to achieve Low risk, targeted, good oral bioavailability

Active Publication Date: 2015-02-18
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the drug bioavailability of injections is much higher than that of oral preparations, the administration of injections is inconvenient and needs to be injected in a regular medical place, which adds trouble to patients and causes poor patient compliance.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Dissolve about 50 mg of half-pinner 5F pure product in castor oil, stir and mix to form an oil phase; compound the mixture of 1,2-Propanediol and PEG-400 (mixing mass ratio: 2:1) with Cremorpher EL, the compounded quality The ratio is 1:3; the oil phase and the compound are mixed and stirred according to the mass ratio of 1:9, and water is added while stirring until a transparent emulsion is formed, then filtered and sterilized, and finally put into storage.

[0027] The half-pinner 5F oral microemulsion prepared by the above method includes the following components in mass percentage: water 50%, oil phase 5%, Cremorpher EL and the compound of 1,2-Propanediol and PEG-400 mixture 45%.

Embodiment 2

[0029] Dissolve about 50 mg of half-pinner 5F pure product in castor oil, stir and mix to form an oil phase; compound the mixture of 1,2-Propanediol and PEG-400 (mixing mass ratio: 2:1) with Cremorpher EL, the compounded quality The ratio is 1:2; the oil phase and the compound are mixed and stirred according to the mass ratio of 2:8, and water is added while stirring until a transparent emulsion is formed, then filtered and sterilized, and finally put into storage.

[0030] The half-pinner 5F oral microemulsion prepared by the above method includes the following components in mass percentage: 50% of water, 10% of oil phase, 40% of the compound of Cremorpher EL and 1,2-Propanediol and PEG-400 mixture.

Embodiment 3

[0032] Dissolve about 50 mg of the half-pinner 5F pure product in castor oil, stir and mix to form an oil phase; compound the mixture of 1, 2-Propanediol and PEG-400 (mixing mass ratio: 2:1) with Cremorpher EL, the compounded quality The ratio is 1:1; the oil phase and the compound are mixed and stirred according to the mass ratio of 3:7, and water is added while stirring until a transparent emulsion is formed, then filtered and sterilized, and finally put into storage.

[0033] The half-pinner 5F oral microemulsion prepared by the above method includes the following components in mass percentage: 50% of water, 15% of oil phase, 35% of the compound of Cremorpher EL and 1,2-Propanediol and PEG-400.

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Abstract

The invention discloses an anti-cancer ent-11 alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid 5F oral emulsion and a preparation method thereof. The oral emulsion comprises components in percentage by mass as follows: 5%-45% of an oil phase containing ent-11 alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid 5F, 5%-45% of a compound of a surfactant and a cosurfactant and the balance of water. Compared with the prior art, the anti-cancer ent-11 alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid 5F oral emulsion has the benefits as follows: 1, the oral emulsion is high in solubility, convenient to use and low in risk, the reaction condition is mild, water-insoluble ent-11 alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid 5F is improved to be water-soluble, and the oral emulsion is suitable for being taken orally; and 2, the oral emulsion has good water smoothness, has particle diameter smaller than 50 nm, adopts a controlled release form and has targeting to tumor tissue and good oral bioavailability.

Description

technical field [0001] The invention relates to a half-pinner 5F oral emulsion, which belongs to the technical field of medicine, in particular to an anti-tumor half-pinner 5F oral emulsion and a preparation method thereof. Background technique [0002] Half Banner 5F (English name ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid) is a diterpene acid isolated and purified from the commonly used herbal medicine Pteris genus Half Banner in southern my country The compound, the pure product is white needle-like crystal, has good anti-tumor and anti-inflammatory activities. Half Banner 5F has significant anti-tumor activity against lung cancer and leukemia tumor strains in vitro, and also has anti-tumor activity against liver cancer and ascites tumor in tumor-bearing mice in vivo, and has the potential to be developed into a new drug for clinical use. However, half-pinner 5F is insoluble in water, and it is difficult to reach an effective drug concentration in the lesion after oral...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/19A61P35/00
Inventor 吕应年
Owner GUANGDONG MEDICAL UNIV
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