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Preparation method of magnetically targeted nano INH/HBPE-DDSA/Fe<3>O<4> composite drug carrying microspheres

A technology of drug-loaded microspheres and magnetic targeting, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, antibacterial drugs, etc. Complicated problems, to achieve the effect of low cost, high drug loading and good dispersion

Inactive Publication Date: 2017-11-10
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In view of the above-mentioned technical problems, the purpose of the present invention is to overcome the shortcomings of the current isoniazid sustained-release microspheres, such as complex preparation process, uneven dispersion of microsphere components, low drug loading, poor controlled and sustained release effect, etc., and provide a simple process A one-step preparation method for the preparation of isoniazid composite microspheres, the magnetically targeted isoniazid composite drug-loaded microspheres prepared by this method have narrow particle size distribution, uniform dispersion of components, high drug loading, and sustained release. Good performance and other advantages

Method used

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  • Preparation method of magnetically targeted nano INH/HBPE-DDSA/Fe&lt;3&gt;O&lt;4&gt; composite drug carrying microspheres
  • Preparation method of magnetically targeted nano INH/HBPE-DDSA/Fe&lt;3&gt;O&lt;4&gt; composite drug carrying microspheres
  • Preparation method of magnetically targeted nano INH/HBPE-DDSA/Fe&lt;3&gt;O&lt;4&gt; composite drug carrying microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Dissolve 0.2g INH in 15mL of pure water, dissolve 0.05g of HBPE-DDSA in 15mL of ethanol, pour the two mixed solutions into a 250ml three-neck flask, stir evenly under ultrasonic conditions, and accurately weigh 0.364g of ferric chloride hexahydrate and four Add 0.134 g of ferrous chloride hydrate into the three-necked flask, and seal it. After vacuum treatment, make the vacuum degree reach -0.1MPa, ultrasonically stir for 40min, and the ultrasonic frequency is 80kHz. Then heat to 80°C, slowly add 15ml of ammonia water, continue to react under the above vacuum and ultrasonic conditions for 1 hour, cool to room temperature, wash with deionized water three times, wash with ethanol three times, freeze dry after magnetic separation, and the drying temperature is -50°C , freezing time is 1h, get INH / HBPE-DDSA / Fe 3 o 4 Nanocomposite microspheres. Sample number S-1.

Embodiment 2

[0038] Dissolve 0.1g INH in 15mL pure water, dissolve 0.15g HBPE-DDSA in 15mL ethanol, pour the two mixed solutions into a 250ml three-neck flask, accurately weigh 0.297g of ferric chloride hexahydrate and 0.153g of ferrous sulfate heptahydrate Add to a three-neck flask and seal it. After vacuum treatment, the vacuum degree is -0.08MPa, ultrasonic stirring is performed for 40min, and the ultrasonic frequency is 60kHz. Then heat to 60°C, slowly add 10ml of ammonia water, continue to react under the above-mentioned vacuum and ultrasonic conditions for 60min, cool to room temperature, wash with deionized water three times, wash with ethanol three times, freeze-dry after magnetic separation, the drying temperature is -30°C, The freezing time is 3h to get INH / HBPE-DDSA / Fe 3 o 4 Nanocomposite Microspheres.

Embodiment 3

[0040] Adopt the method identical with embodiment 1, difference only is as follows:

[0041] Contains Fe 3+ The compound is Fe 2 (SO 4 ) 3 ; Contains Fe 2+ The compound is FeSO 4 ; The Fe 3+ and Fe 2+ The molar ratio is 2:1.

[0042] During the mixing process: the concentration of the INH solution is 5 mg / mL; the concentration of HBPE-DDSA is 0.5 mg / mL. The ultrasonic frequency is 20kHz, the ultrasonic time is 100min, and the vacuum degree is -0.01MPa.

[0043] During the reaction process: the ultrasonic frequency is 20kHz, the ultrasonic time is 100min; the vacuum degree is -0.01Mpa; the reaction temperature is 20°C, and the reaction time is 120min.

[0044] During freeze-drying: the freeze-drying temperature is -50°C, and the freezing time is 0.5h.

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Abstract

The invention relates to a preparation method of magnetically targeted nano isoniazid (INH) / functionalized hyperbranched polyester (HBPE-DDSA) / ferrosoferric oxide (INH / HBPE-DDSA / Fe<3>O<4>) composite drug carrying microspheres for tuberculosis treatment, belongs to the technical field of medicine, and relates to a nanocomposite material. The preparation method of the nano INH / HBPE-DDSA / Fe<3>O<4> drug carrying microspheres comprises the steps that by means of a process intensification method, in the conditions of vacuumization and ultrasonic radiation, INH and HBPE-DDSA are added while Fe<3>O<4> is prepared, and the nano INH / HBPE-DDSA / Fe<3>O<4> drug carrying microspheres are preparedin a one-stage process. The preparation method is characterized in that one-stage process is adopted, and intensified reaction processes of the vacuumization and the ultrasonic radiation are introduced. The preparation method has the advantages that the process is simple and controllable; the nano INH / HBPE-DDSA / Fe<3>O<4> drug carrying microspheres prepared have the advantages of being small in particle size, uniform in dispersion and high in drug carrying amount; besides, the nano INH / HBPE-DDSA / Fe<3>O<4> drug carrying microspheres have the properties of superparamagnetism, good biocompatibility and controlled slow release, and can be applicable to drug targeting in the process of tuberculosis treatment.

Description

technical field [0001] The invention relates to a method for preparing isoniazid composite drug-loaded microspheres for treating pulmonary tuberculosis, in particular to a magnetic targeting nano INH / HBPE-DDSA / Fe 3 o 4 The invention relates to a method for preparing composite drug-loaded microspheres, belonging to the technical field of drug carriers for medicine. Background technique [0002] Magnetic nanomaterials refer to solid substances composed of nanoscale ultrafine particles. Magnetic nanomaterials used in the field of biomedicine are called magnetic nanobiological materials. Magnetic nanobiological materials can deliver drugs to the lesion tissue under the action of an external magnetic field, so as to achieve the purpose of targeted drug release in the lesion area. Magnetic nanobiological materials are widely used in the manufacture of magnetic composite microspheres for targeted delivery of medical drugs due to their advantages such as magnetic targeting, contro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/4409A61K47/34A61K41/00A61P31/06A61P11/00
CPCA61K41/00A61K9/0002A61K9/0009A61K9/5153A61K31/4409
Inventor 马振叶陆婷婷赵迟丽张侠韩巧荣苏复
Owner NANJING NORMAL UNIVERSITY