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Medicine composite used for embolotherapy and acesodyne and preparation method thereof

A composition and drug technology, applied in the field of interventional medicine, can solve problems such as inability to maintain pain relief, and achieve the effects of reducing toxic side effects and reducing drug concentration

Active Publication Date: 2010-06-02
HYGEA MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method has limitations. After the local anesthetic is perfused, it quickly spreads outside the administration site, and it cannot maintain the pain relief for a period of time after the operation or even during the operation.

Method used

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  • Medicine composite used for embolotherapy and acesodyne and preparation method thereof
  • Medicine composite used for embolotherapy and acesodyne and preparation method thereof
  • Medicine composite used for embolotherapy and acesodyne and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: microsphere preparation method

[0042] Using the reverse phase suspension polymerization method, add 50ml of liquid paraffin and an appropriate amount of Span80 in a three-necked flask, nitrogen, and then dissolve polyvinyl alcohol, acrylic acid, N, N'-methylenebisacrylamide (crosslinking agent), 12.5 ml of a solution of potassium persulfate (initiator) was added dropwise to the oil phase at 55° C., and after pre-crosslinking for 10 minutes, tetramethylethylenediamine (catalyst) was added and reacted for 4 hours under stirring at 500 rpm. Wash the microspheres, sieve out different specifications according to the particle size, and collect the microspheres in each particle size range.

[0043] By changing the amount of each component, two batches of microspheres were prepared. After sieving, the microspheres with particle sizes ranging from 150-350 μm, 350-560 μm and 560-710 μm were collected for use in the following examples.

Embodiment 2

[0044] Embodiment 2: the mensuration of microsphere exchange capacity

[0045]Accurately weigh 100mg of dry microspheres, fully soak in hydrochloric acid solution, wash with distilled water, blot the surface moisture, place in a 50ml stoppered Erlenmeyer flask, add 25ml of 0.1mol / L sodium hydroxide solution, heat in a water bath at 60°C for 2h, After cooling to room temperature, take out 5ml of the solution, use phenolphthalein as indicator, and titrate with 0.1mol / L hydrochloric acid standard solution; at the same time, conduct blank control test. The volume of consumed hydrochloric acid standard solution is denoted as V 样品 and V 空白 . The formula for calculating the exchange capacity Q is: Q=(V 空白 -V 样品 )×5×0.1 / 100. The two batches of microspheres prepared in Example 1 were measured according to the above method, and their exchange capacities were 10.6 mol / mg and 12.6 mol / mg respectively.

Embodiment 3

[0046] Embodiment 3: microsphere loading lidocaine hydrochloride

[0047] Establishment of the standard curve: Dilute the lidocaine hydrochloride stock solution into 100, 200, 250, 300, 350, 400, 450 and 500 μg / ml sample solutions respectively, and measure the absorbance at the point of maximum absorption at 261 nm. Do linear regression with drug concentration (C) to absorbance (A), and the resulting standard curve equation is: A=0.0015C+0.0025, R 2 = 0.9999.

[0048] Drug loading method: Take 1ml of microspheres with a certain particle size range, put them into a 10ml vial, add 5ml of lidocaine hydrochloride solution of known concentration, and take samples regularly at 0, 10, 30, 60, 90, 120, and 240 minutes 50 μl, the absorbance was measured at 261 nm, and the absorbance value was substituted into the standard curve to calculate the drug concentration contained in the sample.

[0049] Calculation of drug loading: drug loading = (drug content in solution before drug loadin...

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Abstract

The invention provides a medicine composite used for embolotherapy and acesodyne and a preparation method thereof. The medicine composite comprises a biocompatibility macromolecular compound containing hydroxy, a monomer containing unsaturated double bond and anion group, a polymer, and local anesthetic containing amino group, wherein the polymer is generated through a polymerization reaction of an optional vinyl monomer and the polymerization reaction is initiated by free radicals, and the local anesthetic is combined to an anion group of the generated polymer. In the invention, lidocaine hydrochloride is combined to a polymer carrier; which can give full play to the acesodyne effect of the local anesthetic in the embolotherapy; the anion part of the polymer can properly combine with the local anesthetic containing the amino group, which can both realize higher medicine loading capacity and enable the medicine in an emboliaztion agent to be exchanged by cations in vivo and then slowly released. Moreover, the polymer emboliaztion carrier has simple technology, low cost, and suitability for large scale industrial production.

Description

technical field [0001] The invention belongs to the field of interventional medicine, and relates to a pharmaceutical composition for embolization therapy and pain relief and a preparation method thereof, in particular to a pharmaceutical composition of an amino group-containing local anesthetic for embolization therapy and a preparation method thereof. Background technique [0002] Interventional embolization therapy is a minimally invasive treatment method using modern high-tech means. It refers to the introduction of embolic agents into the human body through special precision instruments such as catheters and guide wires for local treatment under the guidance of medical imaging equipment. Embolization therapy has a good effect in the treatment of hemangioma, liver cancer, uterine fibroids, breast cancer, vascular malformation and hemostasis, and has become an alternative therapy for some surgical treatments. [0003] Pain is the main complication after embolization, whic...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/32A61K47/34A61K47/36A61K47/38A61K45/00A61P23/02A61P29/00A61P35/00A61P1/16A61P15/00A61P15/14A61P9/00A61P7/04A61K47/58
Inventor 范田园殷诺雅袁惠燕
Owner HYGEA MEDICAL TECH CO LTD
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