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Enteric composite drug-loading system with halloysite nanotube as skeleton and preparation method thereof

A technology of halloysite nanotubes and skeletons, which is used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. The problems of small strength and high preparation cost can achieve the effect of improving drug loading rate and improving slow-release enteric solubility.

Active Publication Date: 2019-04-09
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In summary, the existing indomethacin drug-loaded sustained-release system has the disadvantages of frequent administration, high preparation cost, and poor enteric-coated sustained-release effect, while halloysite nanotubes are used as targeted functional drug carriers. and less developed

Method used

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  • Enteric composite drug-loading system with halloysite nanotube as skeleton and preparation method thereof
  • Enteric composite drug-loading system with halloysite nanotube as skeleton and preparation method thereof
  • Enteric composite drug-loading system with halloysite nanotube as skeleton and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] (1) Weigh 4g of acetone, 0.025g of indomethacin, and 0.25g of halloysite nanotubes respectively, then add indomethacin into the acetone, stir and mix to form solution A, and slowly drop solution A with a syringe into 0.25g of halloysite nanotubes, stirred evenly at 30°C, dried in a vacuum oven at 50°C, and then placed the dried powder in a tablet press to form tablets with a diameter of 1 cm and a thickness of 0.15 cm. The tablet weighs 0.275g, and each tablet contains 0.025g of indomethacin;

[0018] (2) Weigh 0.5g of hypromellose phthalate, 0.1g of soluble starch, and 0.003g of polyvinylpyrrolidone (Woke, PVP-K30, GR 100g), and add them to 15ml of absolute ethanol and 4ml of In the mixed solution of deionized water, stir for 30 minutes to prepare solution B;

[0019] (3) Use the dipping-pulling method to slowly and uniformly immerse the tablet prepared in step (1) into the solution B of step (2) cooled to 0°C, and slowly take it out after 5 seconds of composite cross...

Embodiment 2

[0021] (1) Weigh 2g of acetone, 0.030g of indomethacin, and 0.35g of halloysite nanotubes respectively, then add indomethacin into the acetone, stir and mix to form solution A, and slowly drop solution A with a syringe into 0.35g of halloysite nanotubes, stirred evenly at 37°C, dried in a vacuum oven at 40°C, and then placed the dry powder in a tablet press to be pressed into tablets with a diameter of 1 cm and a thickness of 0.22 cm. The weight of the tablet is 0.38g, and each tablet contains 0.030g of indomethacin;

[0022] (2) Weigh 0.6g hypromellose phthalate, 0.2g soluble starch, 0.002g polyvinylpyrrolidone (Wokai, PVP-K30, GR 100g), add to 20ml absolute ethanol and 5ml In the mixed solution of deionized water, stir for 60 minutes to prepare solution B;

[0023] (3) Use the dipping-pulling method to slowly and uniformly immerse the tablet prepared in step (1) into the solution B of step (2) cooled to 0°C, and slowly take it out after 3 seconds of composite crosslinking, ...

Embodiment 3

[0025] (1) Weigh 4g of acetone, 0.040g of indomethacin and 0.30g of halloysite nanotubes respectively, then add indomethacin into the acetone, stir and mix to form solution A, and slowly drop solution A with a syringe into 0.30 g of halloysite nanotubes, stirred evenly at 40°C, placed in a vacuum oven at 50°C, and dried, and then the dried powder was placed in a tablet press to be pressed into tablets with a diameter of 1 cm and a thickness of 0.18 cm. The tablet weighs 0.34g, and each tablet contains 0.040g of indomethacin;

[0026] (2) Weigh 0.4g hypromellose phthalate, 0.3g soluble starch, 0.01g polyvinylpyrrolidone (Wokai, PVP-K30, GR 100g), add to 30ml absolute ethanol and 5ml In the mixed solution of deionized water, stir for 60 minutes to prepare solution B;

[0027] (3) Use the dipping-pulling method to slowly and uniformly immerse the tablet prepared in step (1) into the solution B of step (2) cooled to 0°C, and slowly take it out after 3 seconds of composite crossli...

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Abstract

The invention provides an enteric complex drug-loaded system with a halloysite nanotube being a skeleton. A preparation method includes the steps that indomethacin is dissolved in acetone, the obtained solution is dropwise added into the halloysite nanotube and stirred evenly, then powder is obtained through vacuum drying and put into a tabletting machine, and tablets are obtained through pressing; hypromellose phthalate, soluble starch, polyvinylpyrrolidone, absolute ethyl alcohol and deionized water are mixed and stirred evenly to obtain a mixed solution; the obtained tablets are coated with the obtained mixed solution, namely a coating solution, cooled to minus 5-0 DEG C in step2 and pulled and taken out after being subjected to complex crosslinking for 3s-2min, coated tablets are obtained, a coating-pulling-freeze drying process is completed once after freeze drying, the process is repeated 1-10 times, and the finished product is obtained. The drug-loaded ratio of the halloysite nanotube for indometacin is greatly increased, slow-release enteric solubility is greatly improved, and the releasing rate of indometacin in artificially simulated gastric fluid is smaller than 20%.

Description

(1) Technical field [0001] The invention relates to an indomethacin drug-loaded slow-release system and a preparation method thereof, in particular to an enteric-coated composite drug-loading system with halloysite nanotubes as a skeleton and a preparation method thereof. (2) Background technology [0002] Indomethacin has good antipyretic, anti-inflammatory and analgesic effects, but due to its strong medicinal properties, severe adverse reactions such as gastrointestinal reactions, central nervous system symptoms, liver function damage, inhibition of hematopoietic system, and allergic reactions often occur. Currently commercially available indomethacin tablets have the disadvantages of poor sustained release, need for multiple administrations and complicated preparation process. In order to reduce the toxic and side effects of indomethacin and reduce drug accumulation, indomethacin can be loaded on a carrier material for slow release, so as to maintain the effective concen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K31/405A61K47/69A61P29/00
CPCA61K9/2866A61K31/405
Inventor 孙青罗威盛嘉伟张俭
Owner ZHEJIANG UNIV OF TECH
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