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Magnetic medicament loading method for immunosuppressant

An immunosuppressant and magnetic technology, applied in the fields of polymer materials and biomedicine, can solve the problems of limited application, low encapsulation rate, non-magnetic properties, etc., and achieve the effects of being favorable for popularization, low cost and large drug loading capacity.

Inactive Publication Date: 2010-05-12
SHANXI LIFEGEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation of some lipid-soluble drug encapsulation carriers that have been reported is neither magnetic nor magnetically targeted, and the preparation process is complicated and time-consuming, as reported in Chinese Patent Publication No. CN1736488A and CN1457886A
And the drug loading method of the fat-soluble drug reported in the patent CN1813682A, although it has magnetic properties, the method is complicated, and the encapsulation efficiency is too low (only 30%), which does not meet the requirements of the Pharmacopoeia, which limits its subsequent application

Method used

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  • Magnetic medicament loading method for immunosuppressant
  • Magnetic medicament loading method for immunosuppressant
  • Magnetic medicament loading method for immunosuppressant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A mixture of cyclohexanone and cyclohexane at a volume ratio of 3:1 was added to tacrolimus to prepare a 1 mg / ml immunosuppressant solution. Take 5 mg of magnetic particles and add them into a 10 ml pear-shaped bottle, then add 1 mg of the prepared tacrolimus solution, shake for 48 hours at 25 ° C on a shaking table with a rotation speed of 200 rpm, and reach the balance of drug loading, and then use a rotary evaporator to dissolve the organic The solvent was evaporated and stored at 4°C to obtain magnetic composite particles loaded with tacrolimus. The remaining tacrolimus in the solution was measured by high-performance liquid chromatography, and the following two formulas were used to calculate the drug loading amount to be 20%, and the encapsulation efficiency to be 90%.

[0021]

[0022]

Embodiment 2

[0024] Prepare a 3mg / ml rapamycin solution with methanol. Add 8mg of magnetic particles into a 10ml pear-shaped bottle, add 2.4mg of rapamycin solution, shake at 25°C for 54h on a shaker with a rotation speed of 180rpm, to reach drug loading balance, and use a rotary evaporator to evaporate the organic solvent and stored at 4°C, the magnetic composite microparticles loaded with rapamycin can be obtained. Measure the remaining rapamycin in the solution by high performance liquid chromatography, and then use the following two formulas to calculate the drug loading, encapsulation efficiency, and the resulting drug loading is 25%, see figure 1 , The encapsulation rate is 95%.

[0025]

[0026]

Embodiment 3

[0028] A 5 mg / ml mycophenolate mofetil solution was prepared with tetrahydrofuran and cyclohexane at a volume ratio of 2:3. Take 10 mg of magnetic particles and add them into a 10 ml pear-shaped bottle, add 4 mg of mycophenolate mofetil solution, and shake for 63 h on a shaking table with a rotation speed of 190 rpm at 25 ° C to achieve drug loading balance. Use a rotary evaporator to evaporate the organic solvent. Stored at 4°C, the magnetic composite particles loaded with mycophenolate mofetil can be obtained. The remaining mycophenolate mofetil in the solution was measured by high performance liquid chromatography, and then the drug loading and encapsulation efficiency were calculated by using the following two formulas. The obtained drug loading was 30%, and the encapsulation efficiency was 92%.

[0029]

[0030]

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Abstract

The invention belongs to the technical fields of macromolecular materials and biological medicine, and relates to a medicament loading method for a magnetic macromolecular immunosuppressant with magnetic response performance. The method comprises the steps of adding magnetic particles into immunosuppressant solution to obtain magnetic medicament loading particles of the immunosuppressant by fully and evenly mixing, vibration treatment and the like. The method improves the dispersing state of the immunosuppressant, improves the bioavailability, reduces the dosage, enables the immunosuppressant to have targeting property, reduces the toxic and side effects of the medicament, and can be applied in the targeted treatment. The magnetic medicament loading particles of the immunosuppressant have the advantages of large medicament loading amount, high packing rate, simple method and low cost, and is favorable for popularization.

Description

technical field [0001] The invention belongs to the technical field of polymer materials and biomedicine, and relates to an immunosuppressive magnetic drug loading method with magnetic response performance. Background technique [0002] With the advancement of surgical techniques and the continuous introduction of new immunosuppressants, the short-term survival rate of organ transplantation patients has been significantly improved. For example, the 1-year human / kidney survival rate of kidney transplantation has exceeded 90%, but the long-term survival rate of grafts is still limited. Many factors restrict and stop. In addition to chronic rejection, malignant tumors and functional death of transplanted organs have become two major factors restricting the long-term survival of grafts. Due to the long-term effects of immunosuppressants on the human immune system, the incidence of malignant tumors in organ transplant patients is getting higher and higher as the years of transpl...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K45/00A61K9/14A61P37/06A61K47/36A61K47/40A61K47/34A61K47/04A61K47/02
Inventor 彭明丽刘艳红崔亚丽陈超康文博刘蓓夏炜郭树忠
Owner SHANXI LIFEGEN
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