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Method for preparing nanocapsule and nanocapsule composite microsphere

A technology of composite microspheres and nanocapsules, which is applied in the direction of medical preparations containing active ingredients, drug combinations, and pharmaceutical formulas, can solve the problems of drug sustained release time and sustained drug concentration, and achieve uniform size and preparation Simple process, less toxic and side effects

Inactive Publication Date: 2009-04-08
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There have been a variety of sustained-release dosage forms of chemotherapy drugs, but they have not been widely used clinically because the drug sustained-release time and drug concentration do not meet the requirements of local sustained-release drugs for bone tumors.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 (preparation of nanocapsule)

[0028] The preparation process of the nanocapsule of the present embodiment is specifically as follows:

[0029] Step 1: Add 100mg of methotrexate to 2ml of 0.25M NaOH solution to obtain a 50mg / ml alkaline solution of methotrexate; dissolve 100mg of PLGA (polylactic acid-glycolic acid copolymer) in 5ml of dichloromethane , fully dissolved after stirring to make (polylactic acid-glycolic acid copolymer)-CH with a concentration of 20mg / ml 2 Cl 2 solution;

[0030] Step 2: Take 20μl of MTX alkaline solution and inject 0.5ml of PLGA-CH 2 Cl 2 The solution was emulsified with a 120w ultrasonic cell pulverizer for 15s of continuous ultrasonication to obtain W / O colostrum;

[0031] Step 3: Add the above-mentioned colostrum into 0.5ml of 1at% sodium cholate, use an ultrasonic cell pulverizer at 120w to pulse ultrasonically for 15s, emulsify with an interval of 1s each time, and obtain W / O / W double emulsion;

[0032] Step 4: Plac...

Embodiment 2

[0035] Embodiment 2 (preparation of nanocapsule)

[0036] The preparation process of the nanocapsule of the present embodiment is specifically as follows:

[0037]Step 1: Add 100mg of methotrexate to 2ml of 0.25M NaOH solution to obtain a 50mg / ml alkaline solution of methotrexate; dissolve 150mg of PLGA (polylactic acid-glycolic acid copolymer) in 5ml of dichloromethane , fully dissolved after stirring to make (polylactic acid-glycolic acid copolymer)-CH with a concentration of 30mg / ml 2 Cl 2 solution;

[0038] Step 2: Take 50μl of MTX alkaline solution and inject 0.5ml of PLGA-CH 2 Cl 2 The solution was emulsified with a 120w ultrasonic cell pulverizer for 15s of continuous ultrasonication to obtain W / O colostrum;

[0039] Step 3: Add the above-mentioned colostrum into 2ml of 1at% sodium cholate, use an ultrasonic cell pulverizer 120w pulse ultrasonic for 15s, emulsify at intervals of 1s each time, and obtain W / O / W double emulsion;

[0040] Step 4: Place the obtained do...

Embodiment 3

[0043] Embodiment 3 (preparation of nanocapsule)

[0044] The preparation process of the nanocapsule of the present embodiment is specifically as follows:

[0045] Step 1: Add 100mg of methotrexate to 2ml of 0.25M NaOH solution to obtain a 50mg / ml alkaline solution of methotrexate; dissolve 200mg of PLGA (polylactic acid-glycolic acid copolymer) in 5ml of dichloromethane , fully dissolved after stirring to make (polylactic acid-glycolic acid copolymer)-CH with a concentration of 40mg / ml 2 Cl 2 solution;

[0046] Step 2: Take 100μl of MTX alkaline solution and inject 0.5ml of 40mg / ml PLGA (polylactic acid-glycolic acid copolymer)-CH 2 Cl 2 The solution was emulsified with a 120w ultrasonic cell pulverizer for 15s of continuous ultrasonication to obtain W / O colostrum;

[0047] Step 3: Add the above-mentioned colostrum into 4ml of 1at% sodium cholate, use an ultrasonic cell pulverizer at 120w for pulse ultrasound for 15s, emulsify with an interval of 1s each time, and obtain...

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Abstract

The invention discloses a method for preparing a nanometer capsule and a method for preparing a nanometer capsule composite microsphere. The method for preparing the nanometer capsule comprises the following: step 1, preparing a methotrexate alkaline solution and a PLGA-CH2Cl2 solution; step 2, injecting the methotrexate alkaline solution into the PLGA-CH2Cl2 solution to obtain a W / O colostrum after ultrasonic emulsification; step 3, adding the colostrum into sodium cholate to obtain a W / O / W multiple emulsion after the ultrasonic emulsification; and step 4, placing the obtained multiple emulsion in the sodium cholate to be evaporated through decompression to remove CH2Cl2 so as to obtain a nanometer capsule particle suspension. The method for preparing the nanometer capsule composite microsphere comprises the following: step a, preparing a nanometer capsule; and step b, preparing the nanometer capsule composite microsphere. The nanometer capsule particle prepared by the invention has the characteristics of even size, higher drug loading and encapsulation efficiency, peak value drug release, and smooth drug release.

Description

technical field [0001] The invention relates to a method for preparing nanocapsules and nanocapsule composite microspheres for treating bone tumors. Background technique [0002] Bone tumor treatment is a comprehensive treatment that combines surgery, chemotherapy and radiotherapy. Due to the limb-salvage treatment of malignant bone tumors in the limbs, the adjacent structures of malignant bone tumors in the spine are complicated, and it is difficult to completely remove the lesion. Preventing recurrence after surgery has become more and more important. However, this problem and the lack of a large amount of bone graft materials required for bone reconstruction after tumor resection are still difficult problems for surgeons. They are the bottleneck affecting the treatment effect of bone tumors and the development of treatment concepts. [0003] At present, the research on the treatment of bone tumors mainly focuses on two aspects: reconstruction materials after tumor resecti...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/127A61K31/519A61P35/00
Inventor 许国华徐一帆叶晓健蔡舒袁文吴建峰徐虹
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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