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Traceable polylactic acid/rifampicin drug-loaded microspheres and preparation method thereof

A technology of drug-loaded microspheres and polylactic acid, which is applied in the field of biomedicine, can solve the problems of patient tolerance, short drug release time, and failure to meet bone repair, and achieve good encapsulation efficiency, good drug loading, and process simple and fast effect

Active Publication Date: 2022-02-15
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In recent years, there are also some methods for the treatment of bone and joint tuberculosis, such as the use of anti-tuberculosis drugs, but they cannot be accurately applied to the lesion, and it is easy for patients to develop tolerance. repair needs

Method used

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  • Traceable polylactic acid/rifampicin drug-loaded microspheres and preparation method thereof
  • Traceable polylactic acid/rifampicin drug-loaded microspheres and preparation method thereof
  • Traceable polylactic acid/rifampicin drug-loaded microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Dissolve about 5g of PLA in about 40mL of dichloromethane until clear and transparent. Then add 0.25g of Span-80 and 10mg of rifampicin for ultrasonic emulsification for 30min to obtain an emulsion; the obtained emulsion is poured into 400mL concentration of 1% PVA (polyvinyl alcohol) aqueous solution, with a rotating speed of 5000r / min Shear and disperse in a high-speed shear emulsifier for 3 minutes to obtain an oil-in-water (O / W) emulsion; magnetically stir the obtained (O / W) emulsion at room temperature, and simultaneously add 5 g of ioversol with a concentration of 1% for imaging After 0.5h, add 1g of sodium tripolyphosphate (TPP) dropwise, and then continue to stir for 3h to completely volatilize the organic solvent, solidify and form the microspheres, and obtain PLA two-layer composite drug-loaded microspheres; place them in 40mL dissolved 5g of PLA in dichloromethane solution, ultrasonically oscillated for 30min at 25°C, and then centrifuged and washed to obtain...

Embodiment 2

[0038] Dissolve about 5g of PLA in about 40mL of dichloromethane until clear and transparent. Then add 0.25 g of Span-80 and 10 mg of rifampicin for ultrasonic emulsification for 30 min to obtain an emulsion; pour the obtained emulsion into 400 mL of 1% PVA (polyvinyl alcohol) aqueous solution at a speed of 5000 r / min Shear and disperse for 3min in a high-speed shear emulsifier to obtain an oil-in-water (O / W) emulsion; the obtained (O / W) emulsion is magnetically stirred at room temperature, and 5g of iodophor with a mass concentration of 1% is added dropwise Alcohol contrast agent solution, add 1g sodium tripolyphosphate (TPP) dropwise after 0.5h, and then continue to stir for 3h to completely volatilize the organic solvent, solidify the microspheres, and obtain PLA two-layer composite drug loading; put it in 40mL dissolved In 5 g of PLA in dichloromethane solution, ultrasonically oscillate at 25°C for 30 min, then centrifuge and wash to obtain three-layer composite drug-loade...

Embodiment 3

[0040] Dissolve about 5g of PLA in about 40mL of dichloromethane until clear and transparent. Then add 0.25g of Span-80 and 10mg of rifampicin for ultrasonic emulsification for 30min to obtain an emulsion; the obtained emulsion is poured into 400mL concentration of 1% PVA (polyvinyl alcohol) aqueous solution, with a rotating speed of 5000r / min In a high-speed shear emulsifier, shear and disperse for 3 minutes to obtain an oil-in-water (O / W) emulsion; the obtained (O / W) emulsion is magnetically stirred at room temperature, and 5 g of ioversol with a mass concentration of 1% is added dropwise Contrast agent solution, add 1g sodium tripolyphosphate (TPP) dropwise after 0.5h, and then continue to stir for 3h to completely volatilize the organic solvent, solidify the microspheres, and obtain PLA two-layer composite drug loading; put it in 40mL and dissolve 5g In the dichloromethane solution of PLA, oscillate ultrasonically at 25°C for 30 minutes, then centrifuge and wash to obtain ...

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Abstract

The invention discloses a preparation method of traceable polylactic acid / rifampicin drug-loaded microspheres, which comprises the following steps: dissolving polylactic acid in dichloromethane, then adding span-80 and rifampicin, and carrying out ultrasonic emulsification to obtain an emulsion; pouring the emulsion into a PVA (Polyvinyl Alcohol) aqueous solution, and shearing and dispersing to obtain an oil-in-water emulsion; stirring the oil-in-water emulsion , adding an ioversol contrast agent solution dropwise, then adding sodium tripolyphosphate dropwise , and curing and forming microspheres to obtain polylactic acid two-layer composite drug loading ; putting the microspheres into a dichloromethane solution dissolved with polylactic acid to obtain three-layer composite drug-loaded microspheres, adding the three-layer composite drug-loaded microspheres into an ioversol contrast agent solution, and dropwise adding TPP to obtain a solution; and centrifuging the obtained solution, and taking out the microspheres at the bottom. The preparation process of the drug-loaded microspheres is simple and rapid, the product has a tracing function, high drug loading rate and encapsulation efficiency and long slow release time, polylactic acid with good biodegradability is used in the preparation process, and the drug-loaded microspheres have wide application prospects.

Description

technical field [0001] The invention relates to a degradable drug carrier material, in particular to a traceable composite drug-loaded microsphere, which belongs to the technical field of biomedicine. Background technique [0002] Bone and joint tuberculosis is often secondary to pulmonary tuberculosis, and is the most common extrapulmonary secondary tuberculosis. The treatment of bone and joint tuberculosis is a comprehensive treatment, including anti-tuberculosis drug treatment, nutritional support, and debridement. Currently, the anti-tuberculosis drug treatment regimen is rifampicin, isoniazid, pyrazinamide triple or a quadruple regimen with streptomycin for intensive treatment for 2 months. However, due to the toxic and side effects of the digestive tract of anti-tuberculosis drugs, many patients still find it difficult to tolerate, and the patient's compliance is poor. And because there is sclerotic bone around the bone and joint tuberculosis lesion, it is difficult f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/32A61K47/34A61K31/496A61P31/06A61K49/00A61K49/04
CPCA61K9/1647A61K9/1635A61K31/496A61P31/06A61K49/00A61K49/04
Inventor 高群刘洋翟淑宁桂辰
Owner SHANGHAI INST OF TECH
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