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Preparation of sublingual administered nalmefene hydrochloride

A technology of sublingual oral administration and nalmefene, which is applied in the field of medicine, can solve problems such as restrictions on occasions of use, and achieve the effects of convenient administration, high bioavailability, and rapid onset of action

Inactive Publication Date: 2007-08-01
薛京 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because injections must be injected to patients by professionally trained medical staff, the occasions for use are greatly limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0009] Embodiment 1: Nalmefene Hydrochloride Dropping Pills

[0010] Prescription Nalmefene Hydrochloride 0.1g

[0011] citric acid 3 g

[0012] Azone 1 g

[0013] Macrogol 6000 30g

[0014] A total of 1000 capsules

[0015] Put 30 grams of polyethylene glycol 6000 in a stainless steel container, heat it in an oil bath at 90-100°C to melt it completely, then add 0.1 gram of nalmefene hydrochloride, 1 gram of azone and 3 grams of citric acid, and stir until Melt it, move it to the liquid storage bottle, keep it warm at 80-90°C, adjust the liquid titration valve, drop it into the liquid paraffin at 10-15°C, drain the formed dripping pills and wipe off the liquid paraffin, dry, that is Can make 1000 nalmefene hydrochloride dropping pills provided by the invention.

Embodiment 2

[0016] Embodiment 2: Nalmefene Hydrochloride Dropping Pills

[0017] Prescription Nalmefene Hydrochloride 2g

[0018] citric acid 10g

[0019] Laurozone 2 grams

[0020] Macrogol 4000 20g

[0021] Macrogol 6000 20g

[0022] A total of 1000 capsules

[0023] Put 20 grams of polyethylene glycol 4000 and 20 grams of polyethylene glycol 6000 in a stainless steel container, heat them in an oil bath at 90-100°C to melt them all, then add 2 grams of nalmefene hydrochloride and 2 grams of laurozone and 10 grams of citric acid, stirred until melted, moved to the liquid storage bottle, and kept at 85±2°C, adjusted the liquid volume metering valve, dropped into the liquid paraffin at 10-15°C, and drained the formed dripping pills. And wipe off liquid paraffin, dry, can make 1000 nalmefene hydrochloride dropping pills provided by the invention.

Embodiment 3

[0024] Embodiment 3: Nalmefene hydrochloride sublingual tablet:

[0025] Prescription: Nalmefene Hydrochloride 0.1g

[0026] citric acid 3 g

[0027] Azone 1 g

[0028] 80g cane sugar

[0029] Sodium carboxymethyl starch 10g

[0030] 10% starch slurry 100g

[0031] Magnesium Stearate 5g

[0032] A total of 1000 pieces

[0033] Grind citric acid and sucrose through a 100-mesh sieve and sodium carboxymethyl starch through a 100-mesh sieve and mix the three evenly, dissolve nalmefene hydrochloride in 10ml of water, add 1 gram of azone, and then add it to 10% starch slurry Mix evenly in medium and use it as a binder to make a soft material, granulate through 14 mesh, dry at 70-80°C, granulate through 16 mesh, add magnesium stearate, mix evenly, and press into tablets to obtain 1000 tablets. The sublingual tablet of nalmefene hydrochloride provided by the invention.

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PUM

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Abstract

The invention disclosed a kind of hydrochloric acid nalmefene sublingually consumed preparation which includes active ingredients and medical accessories at a ratio of 1:1-10000 (by weight), the active ingredients include hydrochloric acid nalmefene, nalmefene liberated alkali or other medically acceptable nalmefene salts. The active ingredients in the invention can enter the vivo circulation through the capillary under patients' mucous membrane of mouth so as to fasten the effects and increase the bioavailability. The invention can be used in any occasions, so it's convenient to use with low taking dosage and less side effects.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a sublingual oral preparation of nalmefene hydrochloride. Background technique [0002] Nalmefene hydrochloride is a new type of opioid receptor antagonist synthesized after naloxone hydrochloride and naltrexone hydrochloride. It is a water-soluble derivative of naltrexone hydrochloride. Can bind, and has the strongest binding effect with μ receptors. Compared with naltrexone hydrochloride, its pharmacological action time is longer, the action intensity is stronger and the toxic and side effects are lower. It is mainly used clinically for the treatment of respiratory depression and heart failure caused by taking narcotic analgesics after surgery, shock, alcohol, etc. Symptoms of poisoning and addiction. The current clinically used nalmefene hydrochloride preparations are injections administered through subcutaneous, intramuscular or intravenous routes. Because injections must be inject...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K9/20A61P25/32A61P25/36
Inventor 薛京赵艳
Owner 薛京
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