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Medicine composition for improving docetaxel oral bioavailability

A technology of docetaxel and composition, which is applied in the direction of drug combination, drug delivery, antineoplastic drugs, etc., can solve the problems of low blood drug concentration, difficulty in oral absorption, low oral bioavailability of docetaxel, etc., to improve oral administration Absorption and reduction of toxic and side effects

Inactive Publication Date: 2016-06-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Since docetaxel is the substrate of the efflux transporter P-gp and the cytochrome P450 isoenzyme CYP3A4, its oral absorption is limited by the efflux transporter P-gp and it is difficult to be absorbed orally. Causes its lower plasma concentration, thus makes docetaxel oral bioavailability low
There are no related reports on the combined use of docetaxel and flavonoids to improve the in vivo absorption of docetaxel

Method used

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  • Medicine composition for improving docetaxel oral bioavailability
  • Medicine composition for improving docetaxel oral bioavailability
  • Medicine composition for improving docetaxel oral bioavailability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1 The pharmacokinetic experiment that myricetin promotes the oral absorption of docetaxel

[0019] Experimental scheme: SD rats, 250-300 grams, male, were randomly divided into docetaxel group and myricetin + docetaxel group, with 6 rats in each group, and the administration method of the two groups of rats was as follows:

[0020] Docetaxel group: Docetaxel (40 mg / kg) was administered alone.

[0021] Myricetin + docetaxel group: myricetin (2.5 mg / kg) and docetaxel (40 mg / kg) were administered in combination.

[0022] After oral administration, take 0.4ml of blood at 5min, 15min, 30min, 45min, 60min, 90min, 2h, 3h, 4h, 6h, and 8h, centrifuge to get the upper plasma, detect the blood concentration of docetaxel, and calculate its drug concentration - Area under the time curve and relative bioavailability.

[0023] Experimental results:

[0024] According to the results of pharmacokinetic experiments, the plasma drug concentration-time curve of myricetin-prom...

Embodiment 2

[0029] Embodiment 2 The pharmacokinetic experiment that myricetin promotes the oral absorption of docetaxel

[0030] Experimental scheme: SD rats, 250-300 grams, male, were randomly divided into docetaxel group and myricetin + docetaxel group, with 6 rats in each group, and the administration method of the two groups of rats was as follows:

[0031] Docetaxel group: Docetaxel (40 mg / kg) was administered alone.

[0032] Myricetin + docetaxel group: myricetin (10 mg / kg) and docetaxel (40 mg / kg) were administered in combination.

[0033] After oral administration, take 0.4ml of blood at 5min, 15min, 30min, 45min, 60min, 90min, 2h, 3h, 4h, 6h, and 8h, centrifuge to get the upper plasma, detect the blood concentration of docetaxel, and calculate its drug concentration - Area under the time curve and relative bioavailability.

[0034] Experimental results:

[0035] According to the results of pharmacokinetic experiments, the plasma drug concentration-time curve of myricetin-promo...

Embodiment 3

[0040] Embodiment 3 The pharmacokinetic experiment that myricetin promotes the oral absorption of docetaxel

[0041] Experimental scheme: SD rats, 250-300 grams, male, were randomly divided into docetaxel group and myricetin + docetaxel group, with 6 rats in each group, and the administration method of the two groups of rats was as follows:

[0042] Docetaxel group: Docetaxel (40 mg / kg) was administered alone.

[0043] Myricetin + docetaxel group: myricetin (40 mg / kg) and docetaxel (40 mg / kg) were administered in combination.

[0044] After oral administration, take 0.4ml of blood at 5min, 15min, 30min, 45min, 60min, 90min, 2h, 3h, 4h, 6h, and 8h, centrifuge to get the upper plasma, detect the blood concentration of docetaxel, and calculate its drug concentration - Area under the time curve and relative bioavailability.

[0045] Experimental results:

[0046] According to the results of pharmacokinetic experiments, the plasma drug concentration-time curve of myricetin-promo...

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Abstract

The invention provides a medicine composition for improving docetaxel oral bioavailability and belongs to the technical field of medicine. Flavone compounds comprising quercetin, myricetin and baicalein are combined with docetaxel according to a certain proportion, so that oral bioavailability of docetaxel is improved.

Description

technical field [0001] The invention relates to a pharmaceutical composition for improving the oral bioavailability of docetaxel, which belongs to the technical field of medicines. Background technique [0002] Docetaxel is a compound with significant anticancer activity. It belongs to mitosis inhibitor. By promoting the formation of microtubules and inhibiting the depolymerization of microtubules, it stabilizes microtubules, blocks cells in G2 and M phases, and finally inhibits cancer cells. Mitosis and proliferation of cells. Docetaxel has good effects on ovarian cancer, prostate cancer, liver cancer, advanced breast cancer and gastric cancer. [0003] Docetaxel is poorly soluble in water, and its solubility in water at room temperature is only 0.5 μg / mL. At present, the commercially available preparation of docetaxel is injection, and the preparation contains high concentration of Tween 80. Because Tween 80 is hemolytic, it will cause severe allergic reactions after inj...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K31/352A61P35/00
CPCA61K31/337A61K9/0056A61K31/352A61K2300/00
Inventor 钱帅郝天云高缘张建军
Owner CHINA PHARM UNIV