Microcapsule with extended release active pharmaceutical ingredient and preparation method thereof

An active pharmaceutical ingredient, prolonged release technology, applied in the direction of organic active ingredients, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. The effect of targeted drug delivery and high encapsulation rate

Inactive Publication Date: 2020-07-10
杭州鹿扬科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it only has a difference in drug release in simulated gastric juice and simulated intestinal fluid, which greatly limits its application range.

Method used

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  • Microcapsule with extended release active pharmaceutical ingredient and preparation method thereof
  • Microcapsule with extended release active pharmaceutical ingredient and preparation method thereof
  • Microcapsule with extended release active pharmaceutical ingredient and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] : a microcapsule with extended release active pharmaceutical ingredient:

[0067] This embodiment provides a microcapsule with prolonged release of active pharmaceutical ingredients, which is prepared through the following steps:

[0068] 1) At a temperature of 50°C, the modified low-substituted arginine 9-mer / chitosan was dissolved in a large amount of 0.5wt% acetic acid solution, and then nano-active bamboo charcoal powder and levofloxacin hydrochloride solution were added successively, and fully mixed;

[0069] 2) Under heat preservation conditions, slowly drop 5.0 wt% sodium pyrophosphate solution into the mixed solution in step 1), filter out after crosslinking for 1 hour, wash the residual solution on the surface, rinse it with ethanol for 5 times, and dry it at room temperature.

[0070] In the present embodiment, the modified low-substituted arginine 9-mer / chitosan is prepared by the following steps:

[0071]1) Slowly add the tetrahydrofuran solution dissolved ...

Embodiment 2

[0085] : Another microcapsule with extended release active pharmaceutical ingredients:

[0086] This embodiment 2 provides another kind of drug-loaded microcapsules, the preparation method of which is basically the same as that of embodiment 1, except that in this embodiment the relative molecular mass is 5 Chitosan replaces the modified low-substituted arginine 9-mer / chitosan, and the rest of the components and steps are the same as in Example 1.

Embodiment 3

[0087] : Another microcapsule with extended release active pharmaceutical ingredients:

[0088] This embodiment 3 provides another kind of drug-loaded microcapsules, the preparation method of which is basically the same as that of embodiment 1, the only difference being that in this embodiment, the relative molecular mass of the arginine 9-mer with a weight ratio of 1:6.0 is 1.2×10 5 The chitosan was simply mixed without double-check modification to replace the modified low-substituted arginine 9-mer / chitosan complex, and the rest of the components and steps were the same as in Example 1.

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Abstract

The invention relates to the technical field of biomedical engineering, and particularly relates to a microcapsule with an extended release active pharmaceutical ingredient. The microcapsule materialcomprises modified low-substitution-degree arginine 9 polymer / chitosan, nano active bamboo charcoal powder and a water-soluble active pharmaceutical ingredient; the weight ratio of the arginine 9 polymer to chitosan is not higher than 1: 5.0 when the arginine 9 polymer / chitosan is prepared; and the modification is to form a disulfide bond between the low-substitution-degree arginine 9 polymer / chitosan. The drug-loaded microcapsule is not added with an anti-sticking agent and a plasticizer, the preparation method is simple and stable, the entrapment rate is high, meanwhile, the microcapsule has excellent pH response characteristics and oxidation-reduction response characteristics, the release time of the active pharmaceutical ingredient from entering the body to the focus is remarkably prolonged, the extended release of the active pharmaceutical ingredient is beneficial to targeted drug delivery of the focus, and the damage of the drug to normal cells of the body is reduced.

Description

technical field [0001] The invention relates to the technical field of biomedical engineering, in particular to a microcapsule material with prolonged release of active pharmaceutical ingredients and a preparation method thereof. Background technique [0002] Microcapsule refers to the use of natural or synthetic polymer capsule wall materials to coat solid, liquid, or even gaseous microencapsulation core substances to form a semipermeable or sealed capsule with a diameter of 1 to 5000 μm. capsule. Microcapsule diameters range from millimeters to microns. Microcapsule preparation technology originated in the 1950s and developed rapidly in the mid-1970s, during which many microencapsulated products and processes appeared. Microcapsules have many functions, such as protecting the core material from the environment, shielding the taste, color, and smell, changing the weight, volume, state or performance of the material, isolating activity, reducing volatility and toxicity, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/36A61K47/34A61K47/04A61K31/5383A61K31/704
CPCA61K9/501A61K9/5031A61K9/5036A61K31/5383A61K31/704
Inventor 不公告发明人
Owner 杭州鹿扬科技有限公司
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