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Drip pill containing paclitaxel or paclitaxel derivatives and preparation method thereof

A paclitaxel derivative, paclitaxel technology, applied in medical preparations containing active ingredients, medical preparations with non-active ingredients, pill delivery, etc., can solve solvent toxicity, infusion turbidity, allergic reactions and other problems

Inactive Publication Date: 2010-01-27
张鹏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many problems with paclitaxel injection, mainly including: ① Toxicity and sensitization of the solvent: mainly due to the allergic reaction caused by the excipient polyoxyethylated castor oil, which causes bronchospasm, shortness of breath, fatigue, hypotension, etc.
In the production process, containers, syringes and infusion bags in clinical applications are in contact with polyoxyethylated castor oil, which can leach a large amount of plasticizer diethyl ethyl phthalate, causing allergic reactions
Paclitaxel injection is unstable after dilution
③ Compatibility changes: Compatibility of 60 commonly used clinical drugs with paclitaxel injection will cause infusion turbidity, and some drugs will compete with paclitaxel for binding to plasma proteins, which will increase toxicity
The patent application objectively shows the defect of low bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 10 g of paclitaxel and 90 g of soybean lecithin, grind them into 100-mesh fine powder respectively, and mix them for later use.

[0037] Take 200g of polyethylene glycol 4000 and melt it in a constant temperature water bath at 80°C, add the mixed paclitaxel and soybean lecithin fine powder into it, keep warm and stir at 80°C, and continue to stir for 30 minutes to make a liquid medicine, which is passed through the drop pill The machine is directly dropped into the condensate liquid paraffin at 10°C to form pellets, poured out, drained and wiped off the condensate, sealed and stored, and made into drop pills.

Embodiment 2

[0039] Take 20g of paclitaxel and 80g of egg yolk lecithin, grind them into 120-mesh fine powder respectively, and mix them for later use.

[0040] Take 500g of polyethylene glycol 6000 and melt it in a constant temperature water bath at 85-90°C, add the mixed paclitaxel and egg yolk lecithin into it, heat and stir at 85-90°C, and continue to stir for 50 minutes to make a liquid medicine. The dropping pill machine directly drops into the condensate simethicone oil at 10-15°C to form a pill, pour it out, drain it and wipe off the condensate, keep it sealed, and make a drop pill.

Embodiment 3

[0042]Take appropriate amount of branches and leaves of Taxus chinensis, vacuum-dry at 40°C, and measure the water content as 8.5% by the loss-on-drying method. Grind the dried yew branches and leaves into 100-mesh powder, weigh 200g, put it in a cloth bag, add 2000mL of methanol, let it stand overnight (about 15 hours), heat to 40°C and reflux for 3.5 hours, after natural cooling, Filter to obtain filter residue 1, and recover methanol from the filtrate under reduced pressure to obtain concentrated solution 1. Add 1600 mL of methanol to the filter residue 1, reflux and extract at 40°C for 3 hours, let stand overnight (about 15 hours), and filter to obtain the filter residue 2, and recover the methanol from the filtrate under reduced pressure to obtain the concentrate 2. The filter residue 2 was percolated and extracted with 1600 mL of methanol, and the percolated solution was decompressed to recover methanol to obtain the concentrated solution 3. Combine Concentrate 1, Conce...

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PUM

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Abstract

The invention provides a drip pill containing paclitaxel or paclitaxel derivatives, which takes substances containing the paclitaxel or the paclitaxel derivatives as pharmaceutical ingredients, takes lecithin as a pharmaceutical synergist, mixes the pharmaceutical ingredients and the pharmaceutical synergist according to the weight ratio of 1:1-50, adds into a matrix melted at a certain temperature, keeps the temperature, stirs for a certain period of time and prepares the drip pill, and the drip pill is suitable for oral administration for preventing or treating cancers. The invention provides a compound oral preparation of the paclitaxel or the paclitaxel derivatives, the compound oral preparation is suitable for preventing and treating the cancers, and the preparation method is suitable for industrial and scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine and health care, and in particular relates to an oral preparation containing paclitaxel or paclitaxel derivatives and a preparation method thereof. Background technique [0002] Paclitaxel and paclitaxel injection have been recorded in the current United States Pharmacopoeia and Chinese National Drug Standards, and are used for the treatment of metastatic ovarian cancer, breast cancer, lung cancer, and esophageal cancer. According to the United States Pharmacopoeia and China National Drug Standards, paclitaxel is a white crystalline powder, odorless, tasteless, English name Paclitaxel, molecular formula C 47 h 51 NO 14 , molecular weight 853.92. Paclitaxel is soluble in methanol, ethanol or chloroform, slightly soluble in ether, and almost insoluble in water. [0003] At present, the administration route of paclitaxel is mainly intravenous administration, and paclitaxel injection is used clin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/337A61K47/34A61P35/00A61K31/661
Inventor 张鹏
Owner 张鹏