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A kind of camptothecin colon positioning drug release pellet and preparation method thereof

A colon localization, camptothecin technology, applied in the directions of pharmaceutical formulations, drug combinations, antitumor drugs, etc., can solve the problems of reduced curative effect, poor water solubility of camptothecin, enhanced toxicity, etc., to avoid drug waste, great application value, The effect of increasing solubility

Active Publication Date: 2022-07-29
兰州市食品药品检验检测研究院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although it is well known to those skilled in the art that camptothecin has poor water solubility, is irritating to the gastrointestinal mucosa, is easy to open the ring in an alkaline environment, and then reduces the curative effect and enhances the toxicity, etc., but there is still no successful preparation at present. A camptothecin preparation that increases the solubility of camptothecin, reduces the irritation of the gastrointestinal mucosa, and achieves stable drug release in the colon to improve efficacy and reduce toxicity

Method used

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  • A kind of camptothecin colon positioning drug release pellet and preparation method thereof
  • A kind of camptothecin colon positioning drug release pellet and preparation method thereof
  • A kind of camptothecin colon positioning drug release pellet and preparation method thereof

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Embodiment 1

[0030] The preparation of embodiment 1 camptothecin colon positioning drug release pellets 1

[0031] (1) Preparation of camptothecin nanoemulsion: 0.05 g of camptothecin was accurately weighed, 7.5 g of oil-phase propylene glycol monocaprylate (Capryol90) was added, and vortexed and sonicated for about 30 minutes to dissolve it; the emulsifier was polymerized in advance. Oxyethylene 40 hydrogenated castor oil (Kolliphor RH 40) 7.5g was heated in an oven at 60°C, after it was completely melted, an equal amount of co-emulsifier diethylene glycol monoethyl ether (transcutol HP) was added according to the Km value of 1:1 7.5g, use a magnetic stirrer to stir at a constant temperature of 30°C to obtain a mixed emulsifier; add 0.5g of oleic acid to the oil phase containing camptothecin, stir and mix for 5 minutes, add a mixed emulsifier at a constant temperature of 30°C, Continue to stir for about 20 minutes, then sonicate for 30 minutes, then place on a magnetic stirrer with a cons...

Embodiment 2

[0034] The preparation of embodiment 2 camptothecin colon positioning drug release pellets 2

[0035](1) Preparation of camptothecin nanoemulsion: accurately weigh 0.10 g of camptothecin, add 10 g of oil-phase propylene glycol monocaprylate (Capryol90), vortex and oscillate for about 30 minutes to dissolve it; Ethylene 40 hydrogenated castor oil (Kolliphor RH 40) 10.5g was heated in an oven at 60°C, after it was completely melted, an equal amount of co-emulsifier diethylene glycol monoethyl ether (transcutol HP) 10.5 was added according to the Km value of 1:1 g, use a magnetic stirrer to stir at a constant temperature of 30 °C to obtain a mixed emulsifier; add 1.0 g of oleic acid to the oil phase containing camptothecin, stir and mix for 5 minutes, add a mixed emulsifier at a constant temperature of 30 °C, and continue Stir for about 20 minutes, then sonicate for 30 minutes, then place on a magnetic stirrer with a constant temperature of 30°C and slowly add distilled water dro...

Embodiment 3

[0038] The preparation of embodiment 3 camptothecin colon positioning drug release pellets 3

[0039] (1) Preparation of camptothecin nanoemulsion: accurately weigh 0.05 g of camptothecin, add 9.0 g of oil-phase propylene glycol monocaprylate (Capryol90), vortex and oscillate for about 30 minutes to dissolve it; 10.0 g of oxyethylene 40 hydrogenated castor oil (Kolliphor RH 40) was heated in an oven at 60°C. After it was completely melted, an equal amount of co-emulsifier diethylene glycol monoethyl ether (transcutol HP) was added according to the Km value of 1:1. 10.0g, stir with a magnetic stirrer at a constant temperature of 30°C to obtain a mixed emulsifier; add 1.0g of oleic acid to the oil phase containing camptothecin, stir and mix for 5 minutes, add a mixed emulsifier at a constant temperature of 30°C, Continue to stir for about 20min, then sonicate for 30min, then place it on a magnetic stirrer with a constant temperature of 30°C and slowly add distilled water dropwis...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and in particular relates to a colonic positioning drug release pellet of camptothecin and a preparation method thereof. First of all, the present invention provides a camptothecin nanoemulsion / pellet with colon-positioned drug release. The preparation of camptothecin into a nanoemulsion can improve the solubility of camptothecin, and further preparation into a concentrated nanoemulsion / pellet can be used to improve the solubility of camptothecin. The drug-loaded amount is doubled, and the drug-loaded nanoemulsion can be positioned and released in the colon. Camptothecin can be directly absorbed in the form of nanoemulsion, which avoids the problem of the opening of its lactone ring, and increases the solubility of camptothecin. It can smoothly cross the aqueous barrier on the surface of the colon and be taken up by colon cancer tissue, which enhances the curative effect and reduces the toxicity, and has great application value.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a colonic positioning drug release pellet of camptothecin and a preparation method thereof. Background technique [0002] Camptothecin is a water-insoluble pentacyclic pyrroloquinoline alkaloid isolated from the dovetaceae plant Camptotheca, and is also a natural topoisomerase I inhibitor. The treatment of many tumor diseases has good effect. However, camptothecin has poor water solubility and is irritating to the gastrointestinal mucosa. It is easy to open the ring in an alkaline environment, the efficacy is reduced and the toxicity is enhanced, resulting in a greatly reduced drugability. [0003] Micro / nanocarriers have many advantages, such as increased volume / surface area ratio, resulting in a higher contact area for the drug at the same dose and more efficient delivery, by selecting a physiological environment-responsive pharmaceutical polymer material...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/4745A61K47/36A61K47/32A61P35/00A61K9/107A61K47/14A61K47/12
CPCA61K31/4745A61K9/205A61K9/2027A61P35/00A61K9/1075A61K47/14A61K47/12
Inventor 李运史彦斌徐征刘映前邱国玉
Owner 兰州市食品药品检验检测研究院
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