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Naloxone hydrochloride dropping pills

A technology of naloxone hydrochloride and naloxone, which is applied in the field of medicine, can solve problems such as unstable chemical properties, limited use occasions, drug decomposition, etc., and achieve the effects of quick onset, convenient administration, and controllable dosage

Inactive Publication Date: 2007-09-19
薛京 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although naloxone hydrochloride injection has the advantages of fast onset of action, high bioavailability, and easy dose adjustment and control, but because the molecular structure of naloxone hydrochloride contains a phenolic hydroxyl structure, its chemical properties are unstable, so when it is prepared In the process of forming aqueous injection preparations, the drug may be decomposed due to heat sterilization
Although the powder injection preparation can avoid the decomposition and deterioration of the drug caused by high temperature and has a relatively long storage period, it needs to be injected by professionally trained medical staff to the patient just like the water injection preparation, so the occasion of use is limited. extremely restrictive

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0008] Example 1: Naloxone Hydrochloride Dropping Pills

[0009] Prescription Naloxone Hydrochloride 0.4g

[0010] 3 g citric acid

[0011] Azone 0.04g

[0012] Macrogol 6000 30g

[0013] 1000 capsules in total

[0014] Put 30 grams of polyethylene glycol 6000 in a stainless steel container, heat it in an oil bath at 90 to 100 °C to melt it all, then add 0.4 grams of naloxone hydrochloride, 0.04 grams of azone and 3 grams of citric acid, and stir until Melt it, move it to a liquid storage bottle, keep the temperature at 80-90°C, adjust the droplet metering valve, drop it into the liquid paraffin at 10-15°C, drain the formed drop pellets and wipe the liquid paraffin, dry, namely 1000 naloxone hydrochloride dropping pills provided by the present invention can be prepared.

Embodiment 2

[0015] Example 2: Naloxone Hydrochloride Dropping Pills

[0016] Prescription Naloxone Hydrochloride 2g

[0017] 6g citric acid

[0018] Azone 2g

[0019] Macrogol 4000 20g

[0020] Macrogol 6000 20g

[0021] 1000 capsules in total

[0022] Place 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 to 100 ° C to melt them all, then add 2 grams of naloxone hydrochloride, 2 grams of azone and 6 grams of citric acid, stirred until melted, transferred to a liquid storage bottle, and kept at 85±2°C, adjusted the droplet metering valve, dropped into liquid paraffin at 10 to 15°C, and drained the formed drop pellets. The liquid paraffin is wiped off and dried to obtain 1000 naloxone hydrochloride dropping pills provided by the present invention.

Embodiment 3

[0023] Embodiment 3: Naloxone hydrochloride dropping pills:

[0024] Prescription: Naloxone Hydrochloride 2g

[0025] 3 g citric acid

[0026] 2 g mint

[0027] Azone 2g

[0028] Sodium stearate 100g

[0029] Bug wax 25g

[0030] 1000 capsules in total

[0031] Add 100 grams of sodium stearate and 25 grams of insect wax into the container in turn, dissolve in water, mix well, reflux at 100°C to melt them all, then add 2 grams of naloxone hydrochloride, 2 grams of peppermint, and 2 grams of lauryl azone and 3 grams of citric acid, stir until melted, transfer to a liquid storage bottle, and keep the temperature at 85±2 °C, adjust the droplet metering valve, drop into a 1% sulfuric acid solution at 10 to 15 °C, and put the formed dropping pills. Drain and wipe off the cooling liquid, and dry to obtain 1000 naloxone hydrochloride dropping pills provided by the present invention.

[0032] The naloxone hydrochloride dropping pills provided ...

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PUM

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Abstract

A naloxone hydrochloride pill is disclosed in the invention, which is formed by naloxone hydrochloride, naloxone free alkali or the other naloxone acceptable in medicine having a ratio by weight of 1:5~10000 with pharmaceutic edjuvant based on general pill preparation process. Active ingredient of the naloxone hydrochloride pill in the invention can directly participate intracorporeal circulation after absorbed by capillary tube under oral mucosa of a patient, thus has advantages of fast absorption and high bioavailability, additionally, suffering of intramuscular injection of the patient is prevented. In particular, the drugs of the invention can be taken with no requirement of use situation, so that it is convenient for taking the medicine which dosage is controllable and has little side effect.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a naloxone hydrochloride dropping pill. Background technique [0002] The chemical name for naloxone hydrochloride is 17-allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride anhydrate, monohydrate or dihydrate. It is an opioid receptor antagonist. It has no intrinsic activity, but can competitively antagonize various opioid receptors. It has a strong affinity for μ receptors, and has the characteristics of rapid effect and strong antagonistic effect. It is mainly used clinically. It is used for the treatment of respiratory depression and coma caused by overdose of narcotic analgesics, which causes patients to be highly excited, so that their cardiovascular function is hyperactive. The current clinically used naloxone hydrochloride preparations are injections and tablets administered through subcutaneous, intramuscular or intravenous routes. Although naloxone hydrochloride inject...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K9/20A61P39/02
Inventor 薛京赵艳
Owner 薛京
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