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Taxanes medicine preparation for intravenous injection and preparation method thereof

A technology for intravenous administration of taxanes, applied in the field of medicine, can solve problems such as unsatisfactory, hemolytic, and potential safety hazards for patients, and achieve high in vivo tolerance, good biocompatibility, and low toxic and side effects

Active Publication Date: 2011-04-27
JIANGSU TASLY DIYI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the fast infusion speed has certain risks for some patients, which is a defect of the preparation; another defect is that the solubilizer Cremophor EL has high toxicity and side effects, and patients are prone to dyspnea, flushing, rapid heartbeat, rash and other allergies after taking the drug Reactions often bring safety hazards and pain to patients, so anti-allergic drugs are usually taken to prevent them before administration, so this preparation is not ideal
Similar problems also exist in existing docetaxel clinical preparations, the solvent of its drug solution is made up of Tween-80 solution and 13% ethanol solution, solubilizer Tween-80 has certain hemolytic effect, and its After adding normal saline, the stability time is also short, and it needs to be dripped in a short time, so the safety of clinical medication is also poor
[0005] At present, many scholars have reported many emulsion-related preparations of paclitaxel, such as Kan et al. prepared paclitaxel O / W emulsions with non-ionic surfactants and phospholipids (Kan P, et al., Controlled Release, 1999, 58: 271-278) , but the emulsion contains Tween-80, and the patient has hemolysis after intravenous injection, which has a relatively large adverse reaction; B.S. Anderson's "Paclitaxel parenteral stable non-toxic preparation" (patent application No. The pharmaceutical composition for oral administration contains dimethylacetamide and polyethylene glycol, and dimethylacetamide is a solubilizer, which has certain toxicity and hemolytic properties.

Method used

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  • Taxanes medicine preparation for intravenous injection and preparation method thereof
  • Taxanes medicine preparation for intravenous injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1. Preparation of Paclitaxel Intravenous Administration Preparation

[0039] 1. Preparation of drug solution:

[0040] Take 2.5 grams of paclitaxel, add it to 100 ml of polyethylene glycol 400, stir and dissolve at 70°C, adjust the pH to 5.5 with hydrochloric acid and sodium bicarbonate, add 0.2 g of activated carbon for needles, and adsorb for 30 minutes at 25°C, then Filter through a 0.45 μm microporous membrane, aliquot, and sterilize by high-pressure steam at 115° C. for 30 minutes to obtain a drug solution.

[0041] 2. Preparation of emulsion:

[0042] (1) Preparation of the oil phase: take 200 grams of caprylic triglyceride for injection, heat it in a water bath to 70 ° C, add 12 grams of soybean lecithin for injection, stir to dissolve, add 0.5 g of tocopherol, stir and mix to obtain the oil phase ;

[0043] (2) Prepare the water phase: take 640 ml of water for injection, add 22.5 g of glycerin, 18810 g of poloxamer, stir at 70°C to dissolve, and obtai...

Embodiment 2

[0045] Example 2. Preparation of Docetaxel Intravenous Administration Preparation

[0046] 1. Preparation of drug solution:

[0047] Take 3.0 g of docetaxel, add it to 100 ml of polyethylene glycol 300, stir and dissolve at 70°C, adjust the pH to 6.0 with hydrochloric acid and sodium hydroxide, add 0.2 g of activated carbon for needles, and absorb at 25°C for 30 minutes, and then filtered through a 0.45 μm microporous membrane, dispensed, and sterilized by high-pressure steam at 115° C. for 30 minutes to obtain a drug solution.

[0048] 2. Preparation of emulsion:

[0049] (1) Prepare the oil phase: take 200 grams of soybean oil for injection, heat it to 70°C in a water bath, add 12 grams of soybean lecithin for injection, stir to dissolve, add 0.5 g of tocopherol, stir and mix to obtain the oil phase;

[0050] (2) Prepare the water phase: take 640 ml of water for injection, add 22.5 g of glycerin, 18810 g of poloxamer, stir at 70°C to dissolve, and obtain the water phase; ...

Embodiment 3

[0052] Example 3. Preparation of Paclitaxel Intravenous Administration Formulation

[0053] 1. Preparation of drug solution:

[0054] Take 8.0 grams of paclitaxel, add it to 100 ml of absolute ethanol, stir and dissolve it at 55 °C, adjust the pH to 4.5 with hydrochloric acid, add 4.5 g of activated carbon for needles, absorb at 45 °C for 60 minutes, and then use a 0.45 μm micropore Remove charcoal by membrane filtration, then sterilize by filtration through a 0.22 μm microporous membrane, and aseptically dispense to obtain the drug solution.

[0055] 2. Preparation of emulsion:

[0056] (1) Preparation of oil phase: Take 10 grams of elemene oil, 45 grams of capric monoglyceride, 58 grams of capric diglyceride, 47 grams of sunflower oil, and 20 grams of evening primrose oil, mix them, and heat them in a water bath to 75°C , add 65 grams of soybean lecithin for injection, 5 grams of glyceryl monooleate, 3 grams of cholic acid, stir to dissolve, add 3.0 grams of tocopherol, st...

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Abstract

The invention relates to the technical field of medicine, which is a preparation of a taxane drug for intravenous drug delivery, consisting of two parts of drug solution and an emulsion. The drug solution is composed of paclitaxel or docetaxel, a pH regulator and a solvent for injection, wherein, the solvent for injection is an organic solvent; the emulsion comprises a fat emulsion and is composed of oil for injection, an emulsifier, an antioxidant, an isotonic regulator, a stabilizer, a pH regulator and water for injection. When in use, the drug solution can be added and evenly mixed in the emulsion for direct intravenous drip according to the clinical drug dosage and can also be firstly added in the emulsion with the volume that is not less than 5 times of the volume of the drug solution according to the clinical drug dosage and then added with a certain amount of physiological saline or glucose injection for intravenous drip. The preparation of the invention does not contain solubilizer and has the advantages of little toxicity, safety, effectivity, stability and economy. The fat emulsion can also be taken as a nutrition replenisher for a patient, thus achieving better treatment effects. The physiological saline or the glucose injection can also replace a certain amount of the emulsion, so the storage and the transportation are convenient, and the preparation is more economical.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an intravenous administration preparation of taxane drugs and a preparation method thereof. Background technique [0002] Paclitaxel (trade name: Taxol) and docetaxel (trade name: Taxotem) are two taxane anticancer drugs approved by the FDA. Among them, the natural product paclitaxel is an effective anticancer compound extracted from the bark of the plant Yew brevifolia; docetaxel is a semi-synthesized product from the precursor extracted from the needle leaves of the berry yew. [0003] Taxanes are a class of typical cytotoxic agents with broad-spectrum antitumor effects. It has a strong inhibitory effect on malignant and metastatic cancer. Its anti-tumor mechanism is to stimulate the polymerization of cathelicidin, promote the assembly of microtubule dimers into microtubules, and make microtubules ultra-stabilized to inhibit the dynamic reorganization of microtubule network,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/335A61K9/00A61K9/08A61K9/10A61K31/337A61P35/00
Inventor 陈建明高保安孙靖张悦郑肖利李莹郭丹张扬吴忠斌杨秋霞刘薇顾芃
Owner JIANGSU TASLY DIYI PHARMA CO LTD
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