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Opiates painkiller and opiate receptor antagonist-containing medicinal composition

An opioid receptor and composition technology, which is applied in the field of pharmaceutical compositions containing opioid analgesics and opioid receptor antagonists and the field of preparation thereof, can solve the problems of no improvement in analgesic activity of analgesics, and reduce adverse reactions. , enhance the effect of analgesic effect

Active Publication Date: 2011-05-25
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The analgesic activity of naltrexone in the composition does not enhance the analgesic

Method used

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  • Opiates painkiller and opiate receptor antagonist-containing medicinal composition
  • Opiates painkiller and opiate receptor antagonist-containing medicinal composition
  • Opiates painkiller and opiate receptor antagonist-containing medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment l

[0063] Embodiment 1: Opioid analgesic and naloxone hydrochloride injection

[0064] prescription:

[0065]

[0066] Preparation:

[0067] Take 80% of the prescribed amount of water for injection in the batching tank, add the main drug of the prescribed amount, stir until it is completely dissolved, adjust the pH value with sodium hydroxide solution or hydrochloric acid solution, and adjust the volume to the full amount. After the pH value is qualified, add 0.1% Activated carbon was stirred at room temperature for 45 minutes, then decarbonized by coarse filtration, and finely filtered by a 0.22 μm microporous membrane. 2 Potting, sterilizing, light inspection, and packaging.

[0068] Preparation stability investigation test results:

[0069] The fentanyl citrate / naloxone hydrochloride injection prepared according to the above-mentioned prescription process was subjected to accelerated test and long-term test investigation. The results are shown in Table 1 and Table 2.

...

Embodiment 2

[0073] Embodiment 2: Opioid analgesic and nalmefene hydrochloride injection

[0074] prescription:

[0075]

[0076] Preparation:

[0077] Take 80% of the prescribed amount of water for injection in the batching tank, add the main drug of the prescribed amount, stir until it is completely dissolved, adjust the pH value with sodium hydroxide solution or hydrochloric acid solution, and adjust the volume to the full amount. After the pH value is qualified, add 0.1% Activated carbon was stirred at room temperature for 45 minutes, then decarbonized by coarse filtration, and finely filtered by a 0.22 μm microporous membrane. 2 Potting, sterilizing, light inspection, and packing.

Embodiment 3

[0078] Example 3: Generic Tablets of Opioid Analgesics and Naltrexone Hydrochloride

[0079] prescription:

[0080]

[0081] Preparation:

[0082] Premix the opioid analgesics, naloxone hydrochloride, and silicon dioxide in the amounts listed in the above table through 80 mesh for 3 times, add 5 times the amount of lactose for mixing, and then add 10 times the amount of lactose each time Mix, finally add magnesium stearate as a lubricant, compress after total mixing, and pack to get final product.

[0083]Taking fentanyl and naloxone tablets (100μg / 0.5mg) as examples, the dissolution rate was measured. The tablets were tested for drug release by the paddle method in 250 ml of purified water with a paddle speed of 50 rpm. The media samples were taken out periodically, and the samples were analyzed by high performance liquid chromatography, and the dissolution results were listed in Table 3.

[0084] Table 2 Dissolution results of fentanyl and naloxone tablets (100 μg / 0.5...

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PUM

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Abstract

The invention provides an opiates painkiller and opiate receptor antagonist-containing medicinal composition. In the medicinal composition, an opiates painkiller is fentanyl, remifentanil, sufentanil, alfentanil and pharmaceutically acceptable salts thereof; and an opiate receptor antagonist is naloxone, naltrexone, nalmefene and pharmaceutically acceptable salts thereof. The medicinal composition has a pharmacological effect on analgesia. Compared with using the opiates painkiller singly, the composition can prevent and / or lighten side effects in pain treatment, reduce abuse and improve adaptability, and has a reinforcing effect on an analgesic effect of the opiates painkiller.

Description

technical field [0001] The invention relates to the technical field of medicine, and more specifically relates to a pharmaceutical composition containing an opioid analgesic and an opioid receptor antagonist, a preparation method and application thereof. Background technique [0002] Opioid analgesics play an important role in pain management, and fentanyl, remifentanil, sufentanil, and alfentanil are commonly used opioid analgesics. However, after long-term intake, patients suffering from pain must take higher and higher doses to relieve pain, which is prone to drug dependence and addiction. [0003] An opioid receptor antagonist refers to a substance that binds to an opioid receptor with high affinity, but does not cause a decrease in pain reception, and thus counteracts the action of an opioid agonist. Commonly used are naloxone, naltrexone, and nalmefene. [0004] There has long been a need for a method that can both enhance the analgesic (suppressive) effects of opioi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/485A61P25/04A61P29/00A61K31/4468A61K31/4535A61K31/454
Inventor 符义刚杨玉萍叶夏李莉娥李杰
Owner YICHANG HUMANWELL PHARMA
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