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 administra

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

Example Embodiment

[0041] Example 1: Preparation method of microspheres

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

[0043] By changing the dosage of each component, two batches of microspheres were prepared. After sieving, microspheres with particle sizes ranging from 150 to 350 μm, 350 to 560 μm, and 560 to 710 μm were collected and used in the f...

Example Embodiment

[0044] Example 2: Measurement of microsphere exchange capacity

[0045] Precisely weighed 100mg dry microspheres, fully soaked in hydrochloric acid solution, washed with distilled water, absorbed the surface moisture, placed in a 50ml flask with stopper, added 25ml of 0.1mol / L sodium hydroxide solution, heated in a 60℃ water bath for 2h, After cooling to room temperature, take out 5ml of the solution, use phenolphthalein as an indicator, and titrate with 0.1mol / L hydrochloric acid standard solution; at the same time, perform a blank control test. The volume of consumed hydrochloric acid standard solution is recorded as V sample And V blank . The formula for calculating the exchange capacity Q is: Q = (V blank -V sample )×5×0.1 / 100. According to the above method, the exchange capacity of the two batches of microspheres prepared in Example 1 were 10.6 mol / mg and 12.6 mol / mg, respectively.

Example Embodiment

[0046] Example 3: Microspheres loaded with lidocaine hydrochloride

[0047] The establishment of the standard curve: The lidocaine hydrochloride stock solution was diluted into 100, 200, 250, 300, 350, 400, 450 and 500μg / ml sample solutions, and the absorbance was measured at the maximum absorption at 261nm. Take the drug concentration (C) to the absorbance (A) for linear regression, the standard curve equation obtained 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 it into a 10ml vial, add 5ml lidocaine hydrochloride solution of known concentration, and sample regularly at 0, 10, 30, 60, 90, 120, and 240 minutes 50μl, measure the absorbance at 261nm, and substitute the absorbance value into the standard curve to calculate the drug concentration in the sample.

[0049] Calculation of drug loading: drug loading = (drug content of solution before drug loading-drug content of solution after drug loa...

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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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