Slow-releasing polymer microglobe of analgesic and preparation thereof

A technology of polymer microspheres and polymer skeletons, applied in the directions of inactive components of polymer compounds, drug combinations, pharmaceutical formulations, etc., can solve the problems of analgesic drugs, such as tolerance to addiction and consumption, and achieve long analgesic time. , low cost, economical effect

Inactive Publication Date: 2005-10-12
孙永海
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, tolerance, addiction, side effects and huge consumption of analgesic drugs are the difficulties in the treatment of chronic intractable pain drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1, emulsification cross-linking method

[0029] Dissolve 250mg of gelatin in deionized water at 55°C, and ultrasonically mix with 20mg of morphine, take 20ml of liquid paraffin (containing 3% surfactant), and drop the mixed solution into the constantly stirring liquid paraffin at 100ml / h with a micropump , the stirring speed is 1800rpm, the temperature is 60°C, after dispersing for 10min, change to ice bath, continue stirring for 1 hour, add 0.2ml formaldehyde, stir for another 1 hour, add 20ml isopropanol, stir for 10min, centrifuge at 2000rpm, discard the supernatant solution, then 20ml isopropanol, stirred for 10min, centrifuged at 2000rpm, discarded the supernatant, then washed 4 times with 10ml ether and acetone, dried in vacuum, sieved and weighed, packed and capped, 60 The morphine gelatin microspheres of the present invention with a diameter of about 5uM are obtained by Co irradiation sterilization.

Embodiment 2

[0030] Embodiment 2, thermosetting method

[0031] Take 200mg of human serum albumin and 30mg of ropivacaine, mix thoroughly by wet method, add to 30ml of refined cottonseed oil, and ultrasonically homogenize; take another 100mg of refined cottonseed oil and heat it to 115°C, then add the above-mentioned mixed protein-drug oil solution, continuously stirred at 1800rpm for 10min, cooled to room temperature, washed with ether for 3-4 times and then centrifuged, discarded the supernatant (ether), evaporated the precipitate in a dark place, dried, sieved and weighed, packed and capped, 60 Co irradiated and sterilized to obtain the ropivacaine albumin microspheres of the present invention with a diameter of about 6.5uM.

Embodiment 3

[0032] Embodiment 3, solvent volatilization method

[0033] Ultrasonic suspend 250ug sufentanil and 200mg polylactic acid (PLA) in CH 2 CL 2 disperse into colostrum, then slowly add the emulsion to 1ml sufentanil-saturated polyvinyl alcohol (PVA) aqueous solution at a stirring speed of 1500rpm, disperse and emulsify for 3min at room temperature, and then slowly inject 30ml sufentanil In the saturated PVA solution, continue stirring to make CH 2 CL 2 Volatilize completely, filter, wash with a certain amount of deionized water, drain, vacuum dry, sieve and weigh, pack and cap, 60 The Sufentanil polylactic acid microspheres of the present invention with a diameter of about 56uM were obtained by Co irradiation sterilization.

[0034] The morphine-gelatin microspheres made in the above-mentioned Example 1 were implanted into the epidural space of rabbits, and CO 2 The laser stimulates the soles of the feet, and the results show that the pain threshold can be significantly incr...

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PUM

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Abstract

A slow-releasing high-molecular microsphere of analgesic is prepared from high-molecular material and analgesic through emulsifying, cross-linking, thermal setting, and volatilizing solvent. It can be implanted in cavum epidurale or operation incision for slow releasing.

Description

technical field [0001] The invention relates to an analgesic slow-release polymer microsphere and a preparation method thereof. Specifically, analgesic drugs are embedded in polymer microspheres to make analgesic polymer microspheres, which are implanted in the epidural space or surgical incision, and the analgesic drugs are released slowly, so as to achieve long-term Analgesic effect. It can be used for postoperative analgesia and various pain treatments. Background technique [0002] With the rapid development of modern analgesic technology, the advent of patient-controlled analgesia—PCA technology is a milestone in pain treatment methodology. Patient-controlled analgesia (PCA) includes patient-controlled intravenous analgesia (PCIA) and epidural patient-controlled analgesia. (PCEA). Although it is called self-controlled analgesia, there are still some disadvantages, such as poor stability of the instrument, high cost of use, susceptibility to infection, and inconvenien...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K45/00A61K47/34A61K47/42A61P25/04A61P29/00
Inventor 孙永海
Owner 孙永海
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