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Oil-phase preparation for opiates medicaments and preparation method thereof

A technology of opioid drugs and preparations, applied in drug combinations, non-active ingredients of oil/fat/wax, nervous system diseases, etc., can solve problems such as drug addiction, reduce opioid drug tolerance and dependence, etc. Achieve dependence and tolerance control, improve analgesic effect, and prolong the effect of analgesic time

Inactive Publication Date: 2011-07-27
泰州市康特生物工程有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After repeated use, tolerance will become stronger and stronger, resulting in a vicious circle, leading to serious drug addiction. Therefore, this type of drug has always been strictly controlled as a drug
Concomitant use of other medications to reduce tolerance and dependence on opioids has long been attempted, but so far without success

Method used

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  • Oil-phase preparation for opiates medicaments and preparation method thereof
  • Oil-phase preparation for opiates medicaments and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: Preparation of morphine oil capsules

[0020] ⑴ Take 6g of morphine, dissolve it into 6ml of pure medical water (or acidic aqueous solution), add 3mg of co-solvent polyvinylpyrrolidone (PVP) to get 6ml of solution ① (morphine content is 1000mg / ml);

[0021] (2) Take 14ml of polyoxyethylene-40 (hydrogenated pyrene sesame oil), stir it magnetically for 10 minutes at a constant temperature of 50-60°C, drop 6ml of solution ① into it, and continue stirring for 1 hour to obtain 20ml of solution ②;

[0022] (3) Take 10g of monoglyceride laurate (GML), stir mechanically for 20 minutes at a constant temperature of 50-60°C, add 20ml of the solution ② dropwise, add perilla seed oil to dilute to 100ml, and continue stirring for 1 hour to obtain the solution③ spare;

[0023] (4) Take 1900ml of perilla seed oil, stir mechanically for 20 minutes at a constant temperature of 40-50°C, add 100ml of the solution ③ dropwise, and continue stirring for 30 minutes to obtain 20...

Embodiment 2

[0025] Embodiment 2: preparation pethidine oil capsule

[0026] ⑴ Take 10g of meperidine and dissolve it in 10ml of pure water (or acidic aqueous solution) to obtain 10ml of solution ① (the content of meperidine is 1000mg / ml);

[0027] ⑵Take 20g of monoglyceride laurate (GML), stir it magnetically for 20 minutes at a constant temperature of 50-60°C, inject 10ml of solution ①, add camellia oil to dilute to 100ml, and continue stirring for 1 hour to obtain solution ② for later use;

[0028] (3) Take 900ml of camellia oil, stir it mechanically for 10 minutes at a constant temperature of 40-50°C, add 100ml of the solution ② gradually dropwise, add 20g of beeswax as a thickener, and continue stirring until the beeswax is completely dissolved to obtain pethidine oil 1000ml (pethidine content 10mg / ml).

[0029] (4) The above-mentioned preparation is made into 2000 soft capsules, and the meperidine content in each capsule is 5 mg.

Embodiment 3

[0030] Embodiment 3: preparation of fentanyl oil capsules

[0031] ⑴ Take 1000mg of fentanyl and dissolve it in 2.5ml of pure water (or acidic aqueous solution) to obtain 2.5ml of solution ① (the content of fentanyl is 400mg / ml);

[0032] (2) Take 12.5ml of polyoxyethylene-40 (hydrogenated oil), stir it magnetically for 10 minutes at a constant temperature of 50-60°C, add 2.5ml of solution ① dropwise, and continue stirring for 1 hour to obtain 15ml of solution ②;

[0033] (3) Take 10g of monoglyceride laurate (GML), stir mechanically for 20 minutes at a constant temperature of 50-60°C, add 15ml of the solution ② gradually dropwise, add fish oil to dilute to 100ml, and continue stirring for 1 hour to obtain the solution ③ for later use;

[0034] (4) Take 4900ml of deep-sea fish oil, stir mechanically for 20 minutes at a constant temperature of 40-50°C, gradually add 100ml of the solution ③, and continue stirring for 30 minutes to obtain 5000ml of fentanyl oil phase preparatio...

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Abstract

The invention relates to an oil-phase preparation for opiates medicaments and a preparation method thereof. The preparation is oral administration oil prepared by fully dissolving the opiates medicaments into medical or edible oil. By changing the formulations and the administration mode of the opiates medicaments, the dependency and tolerance of the opiates medicaments are controlled effectively. The oil-phase preparation is used for easing pain, and can reduce the using dose of the opiates medicaments, prolong the analgesis time, improve the analgesis effect and reduce or eliminate the tolerance, dependency and the toxic and side effect of the opiates medicaments.

Description

technical field [0001] The invention relates to an opioid drug oil-phase preparation and a preparation method thereof, belonging to the technical field of pharmaceutical preparation. Background technique [0002] Pain is the most widespread disease worldwide. According to reports, 1 billion people are in pain every day in the world, and about 1 / 3 of people in our country have experienced chronic pain in the course of their lives. With the quickening pace of life, the incidence of various pains is increasing dramatically. [0003] Currently, the most used analgesics in the world are opioids, including: morphine, pethidine, methadone, fentanyl, codeine, tramadol, dihydroetorphine, buprenorphine, Tazocine, bupivacaine, analgesic new and so on. Although these drugs act quickly and have strong analgesic efficacy, the analgesic time is short, generally only 2 hours, and they all have tolerance, dependence and toxic side effects. After repeated use, the tolerance will become st...

Claims

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Application Information

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IPC IPC(8): A61K47/44A61P25/04
Inventor 赵继红汤波澜
Owner 泰州市康特生物工程有限公司
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