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Drug composition for targeted release of trace elements and preparation method and application thereof

A technology of trace elements and compositions, which is applied in the field of anti-tumor pharmaceutical compositions and inducing tissue regeneration, and can solve the problems of low content and intake, restricted trace elements, difficulty in reaching therapeutic concentrations and biological physiological effects, etc.

Active Publication Date: 2012-01-25
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Any trace element must be subject to the "trace" requirements for the body. Although this type of metal element is very important to the body, the body content and intake are extremely low, which often leads to The body's uptake and utilization of such elements is inefficient, and it is prone to trace metal element poisoning
2. Contradictions between the non-specificity of routine intake and distribution in the body and the specific concentration requirements of disease sites
However, such methods are still subject to the functional status of specific organs. For example, if the function of related organs has been damaged, it is still difficult to achieve the therapeutic concentration and biophysiological effect of trace elements even through a large amount of dietary supplementation.

Method used

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  • Drug composition for targeted release of trace elements and preparation method and application thereof
  • Drug composition for targeted release of trace elements and preparation method and application thereof
  • Drug composition for targeted release of trace elements and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1 confirms that copper ions stimulate cell regeneration in vitro and stem cell mobilization experiments and the physiological effects of local film-controlled release of copper ions in the body

[0099] In vitro cell experiments have confirmed that trace element copper ions can effectively enhance the proliferation and differentiation of human umbilical vein endothelial cells (HUVEC). HUVECs were cultured and passaged in vitro. HUVEC in 5×10 3 Cells / well density were seeded in 96-well plates, and the cells were randomly divided into 3 groups according to the concentration of solutions added to the well plates, and the cells in group A were 5 μmol / L CuSO 4 , group B 25μmol / L CuSO 4 , group C is a blank control, each group has 4 duplicate wells, the basal medium is MCDB131, the cell proliferation is detected by MTT method and the growth curve is drawn. Take another HUVEC with 2×10 5 The cells / well density were seeded in 6-well plates, and the grouping was the ...

Embodiment 2

[0103] Example 2 confirms that copper ions stimulate cell regeneration and stem cell mobilization experiments in vitro and the physiological effects of local membrane-applied controlled release of copper ions in the body.

[0104] In order to determine the local effect of copper ions on the activation of scars and stimulate the regeneration of blood vessels in scars, the animal model of local myocardial infarction was pasted with copper ion gel to verify the physiological effect of local slow release of copper ions.

[0105] 1. Preparation of calcium alginate + CuSO 4 film. 10 ml of a 2% mass fraction of sodium alginate solution containing 10 mg of CuSO 4 The solution was mixed well, and 5ml CaCl was added dropwise 2 film after solution.

[0106] 2. Preparation of the myocardial infarction model: under anesthesia, the left anterior descending coronary artery of the rabbit heart was opened and ligated to prepare the rabbit left myocardial infarction model. In the state of t...

Embodiment 3

[0110] Example 3 Copper ion and albumin binding experiment (preparation of copper ion chelated albumin microbubbles)

[0111] The solution used in the experiment was prepared with deionized water, using 0.1mol L -1 NaCl maintains the ionic strength, uses Tris-HCl as the buffer solution, the pH value is 7.4, prepares HSA and copper sulfate solutions, the concentration is 8.76×10 -6 mol·L-1 and 6.48×10 -4 mol·L-1. Using a 1cm cuvette, measure (1) fix the excitation wavelength at 280nm, titrate HSA with copper sulfate, and observe the change of the fluorescence emission peak of HSA. It can be seen from the figure that Cu 2+ The addition of the copper sulfate did not significantly change the position of the excitation peak and the maximum fluorescence peak, but the fluorescence intensity weakened to varying degrees with the increase of the amount of copper sulfate. Since the volume of the HSA solution is much larger than the volume of the metal ion solution added dropwise, the...

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Abstract

The invention discloses a drug composition with a function of ultrasonic targeted release of the trace elements. The drug composition comprises hollow microspheres the concentration of which is greater than 1*106 / ml and the particle size of which is less than 10 mu m, at least one trace element the dosage of which is less than or equal to ten times higher than that of the physiological dose of human body and pharmaceutically acceptable carriers or auxiliaries, wherein the trace element and the hollow microspheres exist in the form of combination or dissociation; and the hollow microspheres are prepared by a pharmaceutically acceptable film-forming material. The drug composition of the invention is stable and safe; and the trace element ions can be directionally introduced into the body under the ultrasonic irradiation effect so as to effectively realize the biological effects of regeneration of blood vessels of the tissue, regeneration of the tissue or tumor resistance for the parts irradiated by the ultrasound, thereby having wide clinical prospect.

Description

technical field [0001] The invention discloses a pharmaceutical composition for directional and controlled release of trace elements, in particular a pharmaceutical composition capable of directional and controlled release by ultrasound, capable of inducing tissue regeneration and anti-tumor. technical background [0002] Trace elements play a fundamental role in maintaining human health. The main physiological function is to play a catalytic role in various enzyme systems, play a role as an essential component or cofactor of hormones or vitamins, and form metalloproteins with special functions. The significance of the physiological effects of trace elements can be compared with that of vitamins, but the body can synthesize some vitamins by itself but cannot synthesize any elements. From this point of view, essential trace elements are more important to the human body than vitamins. The basic definition of essential trace elements refers to those elements that have obvious n...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/00A61K9/50A61K47/48A61K47/42A61K47/30A61K47/24A61K33/30A61K33/32A61P35/00A61P9/00
CPCA61K9/0019A61K33/00A61K9/1275A61K9/1658A61K9/0009A61K9/127A61K9/5052A61K41/0028A61P9/00A61P35/00
Inventor 周翔解慧琪康裕建
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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