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
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[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...
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[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.
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[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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