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Sustained-release preparation for postoperative analgesia and preparation method thereof

A technology of sustained-release preparations and cosolvents, which can be used in non-central analgesics, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., and can solve problems such as inconvenient management, difficult control, and harmful side reactions. , to achieve the effect of easy injection, reduce the frequency of medication, and avoid toxic and side effects

Active Publication Date: 2020-08-21
武汉百纳礼康生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bupivacaine is a non-opioid anesthetic. Conventional injections (0.5%) can only provide pain relief for less than 7 hours, but postoperative pain often lasts for 48-72 hours and is the most difficult to control during this time. Continuous administration of opioids by catheter or infusion pump, resulting in inconvenient administration and multiple adverse side effects

Method used

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  • Sustained-release preparation for postoperative analgesia and preparation method thereof
  • Sustained-release preparation for postoperative analgesia and preparation method thereof
  • Sustained-release preparation for postoperative analgesia and preparation method thereof

Examples

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Effect test

Embodiment 1

[0029] A sustained-release preparation for postoperative analgesia, mainly made of the following raw materials:

[0030] A mixture of 120mg soybean phosphatidylcholine, 50mg diolein, 20mg poloxamer, 30mg absolute ethanol, 12mg cocaine, procaine and lidocaine local anesthetics.

[0031] The preparation method of the sustained-release preparation for postoperative analgesia is as follows:

[0032] Dissolve cocaine, procaine, and lidocaine local anesthetics in absolute ethanol at a ratio of 1:1:4, and mix well to obtain a drug solution; soybean phosphatidylcholine, glyceryl dioleate, porol Sham is heated and melted at 70°C to obtain a molten mixed solution; slowly add the molten mixed solution to the drug solution, vortex and mix, and place it at room temperature to obtain the liquid crystal for postoperative analgesia Gel sustained release formulation precursor formulation. Protect from light, seal, and store in a refrigerator at 4°C.

Embodiment 2

[0034] A sustained-release preparation for postoperative analgesia of this embodiment is mainly made of the following raw materials: 120mg soybean phosphatidylcholine, 50mg diolein, 20mg poloxamer 407, 30mg ethanol, 12mg cocaine, A mixture of lucaine and lidocaine local anesthetics.

[0035] The preparation method of the sustained-release preparation for postoperative analgesia is as follows:

[0036] Dissolve the local anesthetic mixture of cocaine, procaine and lidocaine in absolute ethanol at a ratio of 1:1:5.5, and mix well to obtain a drug solution; soybean phosphatidylcholine, glyceryl dioleate, Loxamer is heated and melted at 70°C to obtain a molten mixed solution; the molten mixed solution is slowly added to the drug solution, vortexed, and placed at room temperature to obtain the above-mentioned drug for postoperative analgesia. Liquid crystal gel sustained release formulation precursor formulation. Protect from light, seal, and store in a refrigerator at 4°C.

Embodiment 3

[0038] A sustained-release preparation for postoperative analgesia provided in this example is mainly made of the following raw materials: 120mg soybean phosphatidylcholine, 50mg diolein, 20mg poloxamer, 30mg ethanol, 12mg cocaine, A mixture of procaine and lidocaine local anesthetics.

[0039] The preparation method of the sustained-release preparation for postoperative analgesia is as follows:

[0040] Dissolve the local anesthetic mixture of cocaine, procaine and lidocaine in absolute ethanol at a ratio of 1:1:6, and mix well to obtain a drug solution; soybean phosphatidylcholine, glyceryl dioleate, Loxamer is heated and melted at 70°C to obtain a molten mixed solution; the molten mixed solution is slowly added to the drug solution, vortexed, and placed at room temperature to obtain the above-mentioned drug for postoperative analgesia. Liquid crystal gel sustained release formulation precursor formulation. Protect from light, seal, and store in a refrigerator at 4°C.

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Abstract

The invention discloses a slow-release preparation for postoperation analgesia and a preparation method of the slow-release preparation. The slow-release preparation is mainly prepared from the following raw materials: 10-15 parts of phospholipid, 4-7 parts of glyceride, 0.3-5 parts of poloxamer, 0.8-5 parts of a cosolvent and 0.5-2 parts of a local anesthetic mixture of cocaine, procaine and lidocaine, wherein the mass ratio of the cocaine to the procaine to the lidocaine in the local anesthetic mixture is 1:1:(4-7.5). The phospholipid is phosphatidylcholine, and preferably soybean phosphatidylcholine; the glyceride is dinolin; the cosolvent is ethanol; the slow-release preparation is easy to inject, and medicines can be slowly released in situ; the action time of the medicines is prolonged, the administration times are reduced, and the bioavailability of the medicines is improved; meanwhile, toxic and side effects caused by too high medicine concentrations can be avoided.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a slow-release preparation for postoperative analgesia and a preparation method thereof. Background technique [0002] Pain is a protective reaction produced by the body after being subjected to noxious stimuli, often accompanied by emotional activities such as fear and nervousness. In addition to feeling pain and emotional uneasiness, pain can also lead to physiological dysfunction, insomnia, and even life-threatening shock. [0003] Among them, postoperative pain (the post-surgical pain) is a common clinical symptom, and there are millions of postoperative patients all over the world suffering from postoperative pain. There are many kinds of operations that cause postoperative pain, such as inguinal defect repair, thoracotomy, and cesarean section. In particular, the acute and chronic pain after thoracotomy for lung cancer has greatly hindered the recove...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/46A61K31/245A61K31/167A61K9/06A61K9/08A61P29/00A61P23/02
CPCA61K9/0019A61K9/06A61K9/08A61K31/167A61K31/245A61K31/46A61K47/24A61P23/02A61P29/00A61K2300/00
Inventor 罗亮黄丽萍孟凡玲
Owner 武汉百纳礼康生物制药有限公司
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