Triptolide fat emulsion injection and preparation method thereof

A technology of triptolide and emulsion injection, which is applied in the direction of oil/fat/wax non-active ingredients, pharmaceutical formula, emulsion delivery, etc., to achieve the effect of high organ targeting, simple and easy preparation process, and easy acceptance

Inactive Publication Date: 2012-07-11
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Triptolide fat emulsion injection and preparation method thereof
  • Triptolide fat emulsion injection and preparation method thereof
  • Triptolide fat emulsion injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Triptolide fat emulsion, the prescription is as follows: triptolide: 200 mg, soybean oil for injection: 240g, medium chain triglyceride: 60g, egg yolk lecithin: 12g, oleic acid: 2g, vitamin E: 0.5g , Glycerin: 25g, Poloxamer 188: 20g, and water for injection to 1000 mL.

[0032] Preparation:

[0033] (1) Add triptolide to soybean oil, medium-chain triglycerides, egg yolk lecithin, vitamin E and oleic acid, heat to 60°C, stir to dissolve;

[0034] (2) Use a small amount of water for injection, heat to 60°C, add glycerin and poloxamer 188, stir and disperse with a high-speed mixer.

[0035] (3) Under the protection of nitrogen, slowly add the water phase to the oil phase, stir to obtain the initial emulsion, and adjust the pH to 8;

[0036] (4) Transfer the primary emulsion to a high-pressure homogenizer to homogenize, adjust the homogenizing pressure to 20MPa, homogenize and control the temperature, cycle emulsification 5 times, and cool the emulsion to room temperature. Ad...

Embodiment 2

[0038] Triptolide fat emulsion, the prescription is as follows: triptolide: 100 mg, soybean oil for injection: 50g, medium chain triglycerides: 50 g, egg yolk lecithin: 24g, oleic acid: 1.5g, vitamin E: 1g, glycerin: 22.5g, poloxamer 188: 10g, water for injection to 1000 mL.

[0039] Preparation:

[0040] (1) Add triptolide to soybean oil, medium chain triglycerides, egg yolk lecithin, vitamin E and oleic acid, heat to 80°C, stir to dissolve;

[0041] (2) Use appropriate amount of water for injection, heat to 80°C, add glycerin and poloxamer 188, stir and disperse with a high-speed mixer;

[0042] (3) Slowly add the water phase to the oil phase, continue to stir to obtain the initial emulsion, adjust the pH value to 7.5 (full nitrogen protection);

[0043] (1) Transfer the primary emulsion to a high-pressure homogenizer to homogenize, adjust the homogenization pressure to 100MPa, homogenize and control the temperature, cycle emulsification 3 times, and cool the emulsion to room temper...

Embodiment 3

[0045] Triptolide fatty emulsion, the prescription is as follows: triptolide: 20mg, soybean oil for injection: 75g, medium chain triglyceride: 25g, soy lecithin: 120g, oleic acid: 3g, vitamin E: 3g, glycerin : 25g, Poloxamer 188: 200g, water for injection to 1000 mL. The preparation method is as in Example 2. The average particle size is 232.1nm, the polydispersity coefficient is 0.171, and the distribution is uniform.

[0046] Preparation:

[0047] (2) Add triptolide to soybean oil, medium-chain triglycerides, egg yolk lecithin, vitamin E and oleic acid, stir at 80°C to dissolve;

[0048] (3) Use appropriate amount of water for injection, heat to 80°C, add glycerin and poloxamer 188, stir and disperse with a high-speed mixer;

[0049] (4) Slowly add the water phase to the oil phase, continue to stir to obtain the initial emulsion, adjust the pH value to 9 (full nitrogen protection);

[0050] (5) Transfer the primary emulsion to a high-pressure homogenizer for homogenization, adjust...

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Abstract

The invention relates to a fat emulsion of triptolide and a preparation method thereof. The fat emulsion injection comprises an antitumor effective dose of triptolide and pharmaceutically-acceptable auxiliary materials, wherein an oil phase is a mixture prepared from long-chain fat acid triglyceride and middle-chain fat acid triglyceride in the mass ratio of 4:1-1:1. The preparation method comprises the following steps of: mixing triptolide, an emulsifier, fat oil, an isotonic regulator, an anti-oxidizing agent and a stabilizer, and heating to obtain an oil phase; weighing water for injection, adding the isotonic regulator, and heating to obtain a water phase; heating and mixing the oil phase and the water phase under the protection of nitrogen gas, and stirring to obtain a primary emulsion; homogenizing the primary emulsion under a high pressure to form a uniform emulsion; and adjusting the pH value to 6-7, sterilizing rotationally to obtain a product, i.e., the triptolide fat emulsion injection, and sterilizing. The average particle diameter of the fat emulsion is 250.9+/-60.0 nanometers, the polydispersion coefficient is 0.143, dispersion is uniform, a system is stable, the targeting property is high, and vessel irritation is low.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a triptolide fat emulsion injection and a preparation method thereof. Background technique [0002] Triptolide (triptolide, TPL), also known as triptolide, triptolide, triptolide from Euonymus genus Triptolide ( Tripterygium wilfoidiiHook.F ), a diterpene lactone compound containing 3 epoxy groups isolated from Kunming Mountain Begonia [(T.Hy-poglaucum Levl.) Hukeda.] and other plants. The structural formula is as follows: [0003] [0004] Triptolide has strong physiological activity, and has significant anti-inflammatory, anti-tumor, anti-fertility and immune regulation effects. etc.) and kidney, heart transplant rejection also play an important role. Patent application No. 2007100088506 discloses the use of triptolide in the treatment of gastrointestinal tumors. Triptolide has poor water solubility, and needs to be dissolved with organic solvents such as prop...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/585A61K47/44A61P35/00A61K47/14
Inventor 陈元仲邓艳平许建华
Owner FUJIAN MEDICAL UNIV
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