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Sustained-release analgesic drug

An analgesic drug and slow-release technology, applied in the direction of drug combination, drug delivery, non-central analgesics, etc., can solve the problem of difficult effective control and elimination of pain sensation

Inactive Publication Date: 2012-12-26
伍丽娟
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The pain caused by trauma and surgery is often difficult to effectively control and eliminate, especially the persistent pain is often a huge pain for the patient

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Preparation of Lidocaine Microspheres by Double Emulsion Method

[0023] Dissolve a certain amount of lidocaine hydrochloride in 0.5ml 20mg / ml gelatin solution (containing 10% trehalose), after stirring, add to 1.25ml of dichloromethane solution containing 150mg PLGA, stir for 2 minutes, then add to 20ml In an aqueous solution containing 6% PVA, stirred for 5 minutes, evaporated to remove the solvent, then washed, centrifuged, freeze-dried, and collected. The average diameter of the microspheres is 30 μm, the drug loading rate is 3%, and the encapsulation efficiency is 97.3%.

Embodiment 2

[0024] Embodiment 2 anhydrous method prepares procaine microsphere

[0025] Dissolve about 150 mg of PLGA in 1 ml of acetonitrile, then add about 10 mg of procaine hydrochloride to it, suspend by ultrasonication at 305 in a water bath, and then add it to 200 ml of cottonseed oil (containing poloxamer, etc. as an emulsifier), Stir and emulsify for 2 minutes, use the dispersed phase to continuously extract the acetonitrile solution in the emulsion droplets to solidify into microspheres, then add petroleum ether, continue stirring to completely solidify the microspheres, centrifuge, petroleum ether wash, freeze-dry the procaine Microspheres.

Embodiment 3

[0026] Embodiment 3 low-temperature spray method prepares lidocaine microsphere

[0027] Suspend about 5 mg of lidocaine hydrochloride in 1 ml of dichloromethane solution with 100 mg of PLGA, form small droplets by spraying, freeze in liquid nitrogen, and extract the dichloromethane that dissolves the polymer with ether as an organic co-solvent. Lidocaine microspheres.

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PUM

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Abstract

The invention relates to a sustained-release analgesic drug, which is microsphere of a topical anesthesia agent. The topical anesthesia agent comprises lidocaine, tetracaine, bupivacaine, oxybuprocaine and procaine. The sustained-release microsphere provided by the invention can be prepared into a sterile microsphere injection, a powder, a spray, a tablet, a capsule, a lozenge, a soft capsule, a pill, a syrup, an external ointment, an emulsion, a bandage, a binder and a gauze. The sustained-release microsphere can be prepared by a multiple double emulsion method, a non-aqueous method, a low temperature spray extraction method or a phase coacervation method. The sustained-release analgesic drug provided by the invention can be used for pain killing of skin wounds with small area, such as cuts, abrasions and burns, and operation wounds.

Description

technical field [0001] The invention relates to a sustained-release analgesic drug, which is a sustained-release microsphere of a topical anesthetic. Topical anesthetics are lidocaine, tetracaine, bupivacaine, oxybucaine, and procaine. The sustained-release microspheres of the present invention can be made into sterile microsphere powder injections, powders, sprays, tablets, capsules, buccal tablets, soft capsules, dripping pills, syrups and external ointments, emulsions, bandages, bandages and gauze. Sustained-release microspheres can be prepared by double emulsion method, anhydrous method, low-temperature spray extraction method, and phase coagulation method. The invention relates to a sustained-release analgesic drug which can be used for pain relief of small-area skin wounds such as cuts, abrasions, burns, and surgical wounds. Background technique [0002] Pain caused by trauma and surgery is often difficult to effectively control and eliminate, especially persistent p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/06A61K9/107A61K9/70A61K9/12A61K9/14A61K9/16A61K9/20A61K9/48A61K31/167A61K31/245A61K31/445A61L15/44A61P25/04A61P29/02
Inventor 伍丽娟
Owner 伍丽娟
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