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Oral paclitaxel composite micelle

A technology for compounding micelles and paclitaxel, which is applied in the directions of drug combinations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. Oral dosage forms and other issues, to achieve the effect of improving bioavailability, good stability, and improving drug safety

Pending Publication Date: 2021-06-22
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The most convenient clinical route of administration of paclitaxel is considered to be the oral route, but due to the low solubility of paclitaxel, the efflux of P-glycoprotein in the gastrointestinal tract, and the metabolism of cytochrome P-4503A4 enzymes in the intestine or liver, paclitaxel is very difficult to obtain. Difficulty crossing the GI barrier
Researchers have adopted many strategies to improve the bioavailability of paclitaxel, but there is still no ideal oral dosage form of paclitaxel

Method used

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  • Oral paclitaxel composite micelle
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  • Oral paclitaxel composite micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1) Prescription

[0043] Paclitaxel 1g

[0044] Cyclosporine 0.1g

[0045] mPEG 1000 -POE 4000 5g

[0046] 2) Preparation steps:

[0047] a) Weigh the paclitaxel, cyclosporine and mPEG of the prescribed amount 1000 -POE 4000 , add 21mL of methanol, ultrasonic heating to dissolve;

[0048] b) Rotary evaporation at 30°C until the organic solvent is evaporated to dryness to obtain a mixed film;

[0049] c) Put the prepared mixed film in a water bath at 40°C until it becomes transparent, add ultrapure water or physiological saline, or phosphate buffer solution preheated at the same temperature, and fully hydrate to obtain a transparent drug-loaded micellar solution;

[0050] d) filtering the drug-loaded micellar solution with 0.45 μm and 0.22 μm microporous membranes in sequence;

[0051] e) Refrigerate the prepared composite micelle solution in a refrigerator at 4°C.

Embodiment 2

[0053] 1) Prescription

[0054] Paclitaxel 1g

[0055] Cyclosporin 1g

[0056] mPEG 8000 -PLGA 4000 5g

[0057] 2) Preparation steps:

[0058] a) Weigh the paclitaxel, cyclosporine and mPEG of the prescribed amount 8000 -PLGA 4000 , add 24ml of acetone, ultrasonic heating to dissolve;

[0059] b) Rotary evaporation at 40°C until the organic solvent is evaporated to dryness to obtain a mixed film;

[0060] c) Put the prepared mixed film in a water bath at 50°C until it becomes transparent, add ultrapure water or physiological saline, or phosphate buffer solution preheated at the same temperature, and fully hydrate to obtain a transparent drug-loaded micellar solution;

[0061] d) filtering the drug-loaded micellar solution with 0.45 μm and 0.22 μm microporous membranes in sequence;

[0062] e) Refrigerate the prepared composite micelle solution in a refrigerator at 4°C.

Embodiment 3

[0064] 1) Prescription

[0065] Paclitaxel 1g

[0066] Cyclosporine 0.1g

[0067] mPEG 1000 -PCL 4000 12g

[0068] 2) Preparation steps:

[0069] a) Weigh the paclitaxel, cyclosporine and mPEG of the prescribed amount 1000 -PCL 4000 , add 44mL of ethyl acetate, ultrasonic heating to dissolve;

[0070] b) Rotary evaporation at 30°C until the organic solvent is evaporated to dryness to obtain a mixed film;

[0071] c) Put the prepared mixed film in a water bath at 40°C until it becomes transparent, add ultrapure water or physiological saline, or phosphate buffer solution preheated at the same temperature, and fully hydrate to obtain a transparent drug-loaded micellar solution;

[0072] d) filtering the drug-loaded micellar solution with 0.45 μm and 0.22 μm microporous membranes in sequence;

[0073] e) Refrigerate the prepared composite micelle solution in a refrigerator at 4°C.

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Abstract

The invention relates to an oral paclitaxel composite micelle and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. Wherein the composite micelle contains two active pharmaceutical ingredients, one is paclitaxel, the other is a p-glycoprotein inhibitor, and an amphiphilic polymer is used as a carrier. The nano-scale composite micelle is prepared by optimizing the proportion of polyethylene glycol in an amphiphilic polymer and the proportion of paclitaxel to a p-glycoprotein inhibitor drug. Compared with the prior art, the polymer micelle prepared by the preparation method provided by the invention has the following advantages: firstly, the solubility of paclitaxel is increased; 2, the bioavailability of the paclitaxel is improved; and 3, the stability is good.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a paclitaxel composite micelle for oral administration. Background technique [0002] Paclitaxel is a diterpene isolated from the Pacific yew tree (Taxus brevifolia). Because paclitaxel binds tubulin, paclitaxel has the ability to inhibit cell division. Accordingly, paclitaxel has been approved for the treatment of ovarian, breast, lung, head and neck, and pancreatic cancers. However, the solubility of paclitaxel in water is very low, which makes formulating a safe and effective treatment difficult. [0003] Due to the small solubility of paclitaxel (<1 μg / mL) and the poor permeability of the gastrointestinal barrier, paclitaxel cannot be taken orally, and its bioavailability is low. Paclitaxel preparations currently used in clinical practice are intravenous injections. For example, the commercially available preparation Taxol is a colorless...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61K31/436A61K38/13A61K47/10A61K47/34A61P35/00
CPCA61K31/337A61K38/13A61K31/436A61K9/1075A61K47/10A61K47/34A61P35/00A61K2300/00
Inventor 张贵民尚萍萍徐涛
Owner LUNAN PHARMA GROUP CORPORATION
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