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Nano suspension containing hydroxycamptothecin and preparation method of nano suspension

A nanosuspension, hydroxycamptothecin technology, applied in the directions of liquid delivery, antitumor drugs, emulsion delivery, etc., can solve the problem of high manufacturing cost of nanoparticles and liposomes, unfavorable industrial production, and unsuitable for intravenous injection, etc. problems, to achieve high drug loading, improve bioavailability, and facilitate the clinical application of large doses

Inactive Publication Date: 2015-01-07
中盛特医食品(汕头)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above nano dosage forms have their own defects. The synthesis of prodrugs is cumbersome and costly; the prepared microspheres have a large particle size and may not be uniformly distributed in the body, so they are not suitable for intravenous injection; the manufacturing costs of nanoparticles and liposomes are high. , high process requirements, stability is a major problem, and its drug loading is generally lower than 20%, and the dosage is large at the same concentration
[0005] In summary, although the drug delivery systems currently developed can stabilize the active site of the lactone ring of HCPI' to varying degrees and improve solubility, they all have their own problems, which are not conducive to industrial production

Method used

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  • Nano suspension containing hydroxycamptothecin and preparation method of nano suspension
  • Nano suspension containing hydroxycamptothecin and preparation method of nano suspension
  • Nano suspension containing hydroxycamptothecin and preparation method of nano suspension

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Take 50 mg of hydroxycamptothecin and put it in a beaker, add 4 ml of dichloromethane to dissolve it, and use it as an oil phase; then take 50 mg of poloxamer, 25 mg of hypromellose and 2 g of mannitol in another beaker, and add it to the beaker. 50ml of distilled water was added into it, and magnetic stirring was performed to make it fully dissolved to serve as the water phase. At room temperature, the oil phase was slowly injected into the water phase, and at the same time, the high-shear emulsifier was used for stirring at 10,000 rpm for 10 minutes. The initial suspension was rotary evaporated for 1 hour to remove the organic solvent, added to a high-pressure homogenizer, and homogenized at 1000 bar for 5 minutes. , the nanosuspension with opalescence was obtained, the particle size was 196nm measured by Malvern 2000 nanometer particle size analyzer, the zeta potential was -28.5mv, and the polydispersity coefficient was 0.11.

[0038] The prepared nanosuspension was ...

Embodiment 2

[0040] Take 50 mg of hydroxycamptothecin and place it in a beaker, add 4 ml of ethyl acetate to dissolve it as an oil phase; then take 50 mg of poloxamer and 25 mg of hypromellose in another beaker, add 50 ml of distilled water to it , magnetic stirring to make it fully dissolved, as the water phase. At room temperature, the oil phase was slowly injected into the water phase, and at the same time, the high-shear emulsifier was used for stirring at 10,000 rpm for 10 minutes, the initial suspension was rotary evaporated for 1 hour to remove the organic solvent, added to the high-pressure homogenizer, and the homogenization cycle was performed at 1000 bar. 20 times, a nanosuspension was obtained, and the particle size was 298 nm as measured by a Malvern 2000 nanometer particle size analyzer, the zeta potential was -25.6 mv, and the polydispersity coefficient was 0.25.

Embodiment 3

[0042] Take 100 mg of hydroxycamptothecin and place it in a beaker, add 4 ml of dichloromethane to dissolve it, and use it as an oil phase; then take 100 mg of poloxamer and 100 mg of hypromellose in another beaker, and add 50 ml of distilled water to it , magnetic stirring to make it fully dissolved, as the water phase. At room temperature, the oil phase was slowly injected into the water phase, and at the same time, the high-shear emulsifier was used for stirring at 10,000 rpm for 10 min. The initial suspension was rotary evaporated for 1 h to remove the organic solvent, and added to a high-pressure homogenizer. The homogenization condition was 500 bar. After 10 cycles, 5 cycles at 500bar and 5 cycles at 1000bar, the particle size of the prepared nanosuspension was 254nm, the zeta potential was -26.6mv, and the polydispersity coefficient was 0.15 as measured by a Malvern 2000 nanometer particle size analyzer.

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Abstract

The invention discloses a nano suspension containing hydroxycamptothecin and a preparation method of the nano suspension, and relates to the field of pharmaceutical preparation, in particular to a nano suspension containing hydroxycamptothecine and a preparation method of liensinine freeze-dried powder of the nano suspension. The suspension comprises components in percentage by weight as follows: 2%-45% of hydroxycamptothecine, 8%-55% of a stabilizer and 0%-90% of a freezing and drying protecting agent, wherein the proportion of hydroxycamptothecine and the stabilizer is (1:1.5)-(1:4), and the particle size ranges from 180 nm to 300 nm. The invention further relates to a preparation method of the suspension. The suspension is prepared through combination of an emulsion method and a high-pressure homogenization method, and the preparation method is suitable for industrial production; and compared with hydroxycamptothecine injection sold in the market, the suspension has the advantages that the dissolution speed of hydroxycamptothecine is increased while a lactonic ring of the nano suspension is not damaged, and the pesticide effect can be increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a hydroxycamptothecin nano-suspension and a preparation method thereof. Background technique [0002] Camptothecin (CPT) is an alkaloid with anti-tumor effect isolated and extracted from the unique plant Camptotheca chinensis in my country in the 1960s and 1970s, but its application is limited due to its high toxicity. Hydroxycamptothecin (HCPT) is a semi-synthetic derivative. In vivo and animal experiments have shown that it has a strong anti-tumor effect and a broad anti-tumor spectrum, and its anti-cancer effect is 30 times that of camptothecin. Animal experiments have proved that HCPT is a cell cycle-specific drug, and its effect on the S phase is more obvious than that of the G phase. At a higher concentration, it has an inhibitory effect on nuclear division and can prevent cells from entering the division phase. Unlike antimetabolites and alkylating agents, HCPT...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4745A61K47/38A61K47/34A61K47/26A61P35/00
Inventor 孙小虎张永丰陈卫陈丹瑾
Owner 中盛特医食品(汕头)有限公司
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