System for positioning delivery of medicament and quantitatively controlling and releasing

A drug and delivery carrier technology, applied in the field of biomedical engineering, can solve the problems of small cavitation effect, unfavorable microbubble reperfusion, and reduced cavitation effect

Inactive Publication Date: 2008-08-20
许川山
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, at present, there is no specialized device for ultrasonically irradiating microbubbles to deliver drugs at home and abroad.
However, diagnostic ultrasound has some obvious deficiencies in ultrasonic irradiation of microbubbles, which are mainly manifested in: ① What diagnostic ultrasound emits is high-frequency ultrasound, which can improve the gray-scale imaging of tissues, but it destroys the microbubbles produced However, the cavitation effect is significantly reduced. The study found that the cavitation effect is inversely proportional to the ultrasonic frequency used. The higher the ultrasonic frequency, the s...

Method used

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  • System for positioning delivery of medicament and quantitatively controlling and releasing
  • System for positioning delivery of medicament and quantitatively controlling and releasing
  • System for positioning delivery of medicament and quantitatively controlling and releasing

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0028] Example 1: Preparation of drug-microbubble conjugate

[0029] Mix phosphatidylcholine (DPPC), phosphatidylethanolamine (DPPE), dipalmitoylphosphatidic acid (DPPA) and hypocretin 2 mg into 400 μl of soybean oil in a mass ratio of 5:2:1, and add poloxa The drug-microbubble combination was obtained after 50 μl of mol, 0.5 mg of glycerol and perfluoropropane gas were shaken mechanically for 60 seconds. The prepared drug-microbubble combination was rinsed several times with phosphate buffer, and the particle size distribution was measured with a Malvern measuring instrument, and the morphology and structure of the drug-microbubble combination were observed under light and electron microscopes. The test results showed that the concentration was 1.4×10 9 ~4.5×10 9 / ml, 90% of its particle size is between 1 and 5 μm, and the size distribution of the drug-microbubble combination is uniform and stable as observed by light and electron microscopes. (Figure 1, Figure 2)

example 2

[0030] Example 2: Determination of drug entrapment efficiency in drug-microbubble conjugates

[0031] Adopt density gradient centrifugation to separate free drug and encapsulated drug, use blank soybean oil microbubble as control group, adopt density gradient centrifugation, use 10%-20% sucrose to dilute the drug and microbubble combination to 4ml, 3000 Centrifuge at rpm for 5 minutes, take 40 μl of the gradient layer and dilute it to 2 ml with double distilled water to detect the free drug content by ultraviolet spectrophotometry. (2) Calculation of Encapsulation Efficiency: Calculate Encapsulation Efficiency as follows: Encapsulation Efficiency (%)=[(input drug amount-free drug amount) / input drug amount]×100; (3) drug loading Calculation: The following formula is used to calculate the drug loading: drug loading=(Wt-Wi) / Vc×100%, where Wt is the total drug content in the drug-microbubble complex, Wi is the free drug amount, and Vc is the total solution amount. The results...

example 3

[0032] Example 3: In Vitro Ultrasound Imaging of Drug-Microbubble Conjugates

[0033] Add 0.2ml of drug and microbubble combination into degassed water and mix well, use GEVivid 7 color ultrasonic diagnostic instrument, 12L linear array probe. All conditions of the instrument are set to the same standard: the mechanical index (MI) is set to 0.24 for the second harmonic, the gain is -14dB, the imaging depth is fixed at 3cm, and parameters such as TGC and focus range are adjusted to the best state. Use the internal workstation of the ultrasonic instrument to store the imaging data before and after adding the combination of drugs and microbubbles. It was found that there was a significant difference before and after contrast (Figure 3).

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Abstract

The invention relates to a location delivery and quantity controlled release system of medicine, comprising a medicine delivery carrier and the location and quantity controlled release device; wherein, the medicine delivery carrier is a combination of the medicine and the microvesicle, the location and quantity controlled release device comprises a microvesicle location unit, a triggering unit, a drive unit connecting the triggering unit and a quantity and estimate unit; the triggering unit is pulse focus ultrasonic the focal region of which is adjustable, the focal region of the triggering unit is adjusted by changing the frequency of the focus ultrasonic, controlling the original phase size and the emission power of each ring of the annular array transducer or controlling the phase size and the emission power of each array unit of the two-dimensional planar or the multi-dimensional array ultrasonic phased controlled array transducer. The location delivery and quantity controlled release system of medicine has an advantage that the invention can realize the integration of the location delivery, quantity controlled release and therapeutic effect estimate of medicine.

Description

technical field [0001] The invention belongs to the technical field of biomedical engineering, and in particular relates to a drug positioning delivery and quantitative controlled release system. Background technique [0002] Drugs in conventional dosage forms are distributed throughout the body after intravenous, oral or local injection, and the amount of drugs that actually reach the treatment target area is only a small part of the dose, and the distribution of most drugs in non-target areas not only has no therapeutic effect, It can also cause toxic side effects. Therefore, the development of new drug dosage forms has become a direction of modern pharmacy development. In recent years, with the development and infiltration of molecular pharmacology, biopharmaceutical analysis, cell medicinal chemistry, drug molecular delivery and system engineering, and the continuous emergence of new technologies, the research on drug dosage forms and preparations has entered the drug d...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K49/22A61K47/32A61K47/24A61K47/34A61K47/36A61K47/42
Inventor 许川山夏新蜀于廷和王志刚王华
Owner 许川山
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