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Ultrasonically controlled-release target medicinal preparation and production method thereof

A technology of ultrasonic control and pharmaceutical preparations, which is applied in the directions of pharmaceutical formulations, medical preparations with non-active ingredients, non-active ingredients of polymer compounds, etc. Dosing and other issues

Inactive Publication Date: 2010-02-24
INST OF CHEM CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, although the above "active-guiding" and "passive-guiding" targeted drug delivery preparations can deliver the drug directly to the target drug site and limit the step-by-step distribution of the drug in the body, they cannot control the release of the drug , with no control over when or how much to administer

Method used

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  • Ultrasonically controlled-release target medicinal preparation and production method thereof
  • Ultrasonically controlled-release target medicinal preparation and production method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Embodiment 1, preparation and performance of PLGE porous microsomes loaded with 5-fluorouracil

[0045] 1) Preparation of PLGE porous microsomes loaded with 5-fluorouracil

[0046] At 15°C, 200 mg of poly(lactide-glycolide-polyethylene glycol ether) copolymer with a molecular weight of 10,000 (the molar ratio of each monomer in PLGE is 60 / 30 / 10, and the molecular weight of PEG is 1000) Dissolve in 10ml dichloromethane (CH 2 Cl 2 ), solution A was obtained after complete dissolution. The solution A was poured into 1 ml of an aqueous solution in which 10 mg of 5-fluorouracil was dissolved, and ultrasonically emulsified for 30 seconds (polymers containing PEG components do not need to add emulsifiers) to form a water-in-oil emulsion. Then this water-in-oil emulsion is slowly added dropwise to 150ml containing the aqueous solution that mass volume concentration is 1% (g / 100ml) polyvinyl alcohol (PVA) to form water-in-oil-in-water emulsion, then continue to stir for 2 hou...

Embodiment 2

[0052] Example 2, preparation and performance of paclitaxel-loaded PGCE porous microsomes

[0053] The preparation method is basically the same as in Example 1. The difference is that the preparation temperature is 23°C, and the carrier used is 200 mg of poly(glycolide-caprolactone-polyethylene glycol ether) copolymer with a molecular weight of 15,000 (the molar ratio of each monomer in PGCE is 30 / 50 in sequence). / 20, the molecular weight of PEG is 2000), the drug is 5 mg paclitaxel, and finally the paclitaxel-loaded PGCE porous microsomes with a particle size of 1 to 8 microns and a porous structure (micropore diameter of 100-1000 nm) are obtained.

[0054] To culture human liver cancer cells, add paclitaxel-loaded PGCE microsomes to the culture medium, and at the same time, apply ultrasonic sound intensity of 0.5W / cm to the cell culture medium 2 After irradiating for 30s, cell apoptosis was measured by fluorescent staining. The results showed that paclitaxel-loaded PGCE 3...

Embodiment 3

[0055] Embodiment 3, preparation and performance of PGCE porous microsomes loaded with heparin

[0056] The preparation method is basically the same as in Example 1. The difference is that the preparation temperature is 20°C, and the carrier used is 180 mg of poly(glycolide-caprolactone-polyethylene glycol ether) copolymer with a molecular weight of 12,000 (the molar ratio of each monomer in PGCE is 30 / 60 in sequence). / 10, the molecular weight of PEG is 1000), the drug is 8 mg heparin, and finally the heparin-loaded PGCE microsomes with a particle size of 1-8 microns and a porous structure (micropore diameter of 100-1000 nm) are obtained.

[0057] The same method as in Example 1 and the results of intravenous infusion with dogs as simulated animals show that the heparin-loaded PGCE microsomes have excellent in vivo ultrasound imaging functions.

[0058] The heparin-loaded PGCE microparticles were made into a suspension and injected into the rat body through the femoral vein ...

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Abstract

The invention discloses a biologically degradable ultrasonically controlled target granular medicinal preparation and a production method thereof. The ultrasonically controlled target granular medicinal preparations are 0.5-0.8 microns wide granules made from biologically degradable macromolecules and medicines; the granules are a) porous particulates with pore diameters of 10-1000nm or b) a hollow capsule. The ultrasonically controlled (passively guided) target medicinal release preparation can be transported into human blood cycle system or the diseased part of a human body through injectionor venous perfusion; ultrasonic transmission characteristic on part of a human body with preparation can be changed through the physical theory of ultrasonic waves to generate featured ultrasonic image, thereby increasing the contrasts degree between diseased part and normal tissue as well as between movable part and static part, and carrying out ultrasonic development; simultaneously, the irradiating energy of the ultrasonic waves can promote the release of medicine so as to control the release of medicine by ultrasonic waves.

Description

technical field [0001] The invention relates to an ultrasonic controlled release targeted drug preparation and a preparation method thereof, in particular to a biodegradable ultrasonic controlled release particle targeted drug preparation and a preparation method thereof. Background technique [0002] A pharmaceutical preparation is a collection of drugs and excipients, in which the drug is the real therapeutic component of the drug preparation, and the excipients are used to stabilize, solubilize, aid in dissolution, slow release, control release, or facilitate the preparation of the drug. The general term for various ingredients other than drugs added during administration and processing; it is precisely because of the combination of drugs and excipients that pharmaceutical preparations can be applied and achieve certain curative effects. [0003] However, under normal circumstances, only a small part of the medicine is delivered to the patient site through the blood circu...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/50A61K47/34A61K47/36A61K47/42
Inventor 王身国智光郭兴林徐勇杨飞周肖
Owner INST OF CHEM CHINESE ACAD OF SCI
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