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Loperamide hydrochloride-casein composite nanoparticles, as well as preparation method and application thereof

A technology of loperamide hydrochloride and casein, which is applied in the directions of drug combinations, pharmaceutical formulations, inactive components of polymer compounds, etc., can solve the problems of low oral bioavailability, poor compliance, and affecting therapeutic effects.

Inactive Publication Date: 2017-12-08
SICHUAN AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, at present, due to the low oral bioavailability and extremely bitter taste of LOP, the compliance of clinical treatment of children with dysentery is poor, which seriously affects the therapeutic effect. Therefore, it is necessary to find effective ways to improve the solubility of LOP, cover up its bitter taste, and increase its oral intake. bioavailability

Method used

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  • Loperamide hydrochloride-casein composite nanoparticles, as well as preparation method and application thereof
  • Loperamide hydrochloride-casein composite nanoparticles, as well as preparation method and application thereof
  • Loperamide hydrochloride-casein composite nanoparticles, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Encapsulation efficiency and drug loading of LOP-Cas (mass ratio of the two substances Cas:LOP=50:1)

[0035] 1 Experimental materials

[0036]

[0037] 2 Experimental methods

[0038] 1) Preparation of LOP-Cas

[0039] ①Precisely measure 50ml of double-distilled water in a 100ml beaker, accurately weigh 1g of Cas, pour it into the beaker, make it float on the double-distilled water, and seal it overnight to obtain a 2% Cas aqueous solution.

[0040] ②Weigh 16mg of LOP and dissolve in 20ml of redistilled water to obtain 0.8mg / ml LOP aqueous solution.

[0041] ③ Measure 20 mL of Cas aqueous solution with a concentration of 2% (w / v) in a 50 mL beaker, slowly add 10 mL of 0.8 mg / mL LOP aqueous solution dropwise, and continue stirring for 30 min.

[0042] ④ Adjust the pH of the resulting mixed solution to 5.5 with 1M HCl.

[0043] ⑤Put the pH-adjusted mixed solution in a cell ultrasonicator with a power of 130W, pulse on for 10s, pulse off for 10s, and pulv...

Embodiment 2

[0054] Example 2 Effects of Different Drug-Carrier Mass Ratio on LOP-Cas Particle Size, PDI, Zeta Potential, Encapsulation Efficiency and Drug Loading Capacity

[0055] 1 Experimental materials

[0056]

[0057] 2 Experimental methods

[0058] The LOP-Cas solution was prepared, and other conditions were fixed (adjust the pH of the solution to 5.5, 130W probe sonicated 10 times), and the influence of different drug-carrier mass ratios on LOP-Cas was investigated. The drug-carrier mass ratios were selected as 25:1, 33:1, 50:1, 75:1, and 100:1 for the experiment.

[0059] The particle size, polydispersity index (PDI) and potential of LOP-Cas were measured with a Nano ZS90 laser particle size and potential analyzer produced by Malvern Company in the United Kingdom, and the measured samples were put into the sample cell for direct measurement.

[0060] The encapsulation efficiency and drug loading of LOP-Cas were determined by ultrafiltration.

[0061] Effect of drug-drug loa...

Embodiment 4

[0072] Example 4 Effect of Ultrasound on LOP-Cas Particle Size, PDI, Zeta Potential, Encapsulation Efficiency and Drug Loading Capacity

[0073] 1 Experimental materials

[0074]

[0075] 2 Experimental methods

[0076] Prepare LOP-Cas nanoparticles, fix other conditions unchanged (carrier-drug mass ratio is 50:1, adjust pH=5.5), and investigate the effect of probe ultrasound on LOP-Cas. Choose whether to perform ultrasonic treatment, repeat ultrasonic treatment 10 times, 20 times and 30 times (130W, pulse on for 10s, pulse off for 10s) to carry out the experiment.

[0077] The particle size, polydispersity index (PDI) and potential of LOP-Cas were measured with a Nano ZS90 laser particle size and potential analyzer produced by Malvern Company in the United Kingdom, and the measured samples were put into the sample cell for direct measurement.

[0078] The encapsulation efficiency and drug loading of LOP-Cas were determined by ultrafiltration.

[0079] Effects of ultraso...

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Abstract

The invention relates to loperamide hydrochloride-casein composite nanoparticles, as well as a preparation method and application thereof, and particularly discloses loperamide hydrochloride-casein composite nanoparticles, wherein loperamide hydrochloride is dispersed into nano-carriers formed by casein in an amorphous form. The preparation method comprises the following steps: 1) preparing a casein solution; 2) preparing a loperamide hydrochloride solution; 3) adding the loperamide hydrochloride solution obtained in the step 2) into the casein solution; 4) adjusting the pH value of the solution obtained in the steps 3) to be 5.5 to 8.5; 5) performing ultrasonic dispersion on the solution obtained in the step 4) to obtain the loperamide hydrochloride-casein composite nanoparticles. The loperamide hydrochloride-casein composite nanoparticles has the effects of improving the solubility of the loperamide hydrochloride, covering up the bitter taste of the loperamide hydrochloride, selectively releasing in gastric juice and improving the bioavailability, so as to achieve higher compliance and achieve the curative effect of treating gastrointestinal inflammation and dysentery.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method and application of a loperamide hydrochloride-casein composite nanoparticle antidiarrheal agent. Background technique [0002] Loperamide hydrochloride (LOP) is an opioid receptor antidiarrheal agent that acts on intestinal wall opioid receptors, it can prevent the release of acetylcholine and prostaglandins, thereby inhibiting intestinal peristalsis and prolonging the residence time of intestinal contents, It is mostly used in the treatment of acute and chronic dysentery in children and adults. The major metabolic pathway of loperamide hydrochloride is through oxidative N-demethylation and is regulated primarily by the cytochrome oxidases CYP3A4 and CYP2C8. Although loperamide hydrochloride is mostly absorbed by the intestinal wall, its bioavailability is only about 0.3% due to the obvious first-pass effect. In the current market, dif...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/42A61K31/451A61P1/12A61P1/00A61P1/04A61P29/00
CPCA61K9/5052A61K31/451Y02A50/30
Inventor 袁志翔何铭卉蒋婷婷周佳敏尹莹符华林舒刚张伟
Owner SICHUAN AGRI UNIV
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