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Naloxone hydrochloride crystal form compound

A technology for naloxone hydrochloride and its compounds, which is applied in the field of crystal form compounds of naloxone hydrochloride, can solve problems such as the inability to guarantee the quality of preparation products, the instability of naloxone hydrochloride raw materials, and the lack of preparation methods for three crystal forms

Active Publication Date: 2016-04-20
ZHENGZHOU SIHUAN MEDICINE ARTICLE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, if the naloxone hydrochloride bulk drug deteriorates or degrades during storage, no matter how excellent the synthesis or preparation process is, the quality of the preparation product cannot be guaranteed.
CN103304570A discloses a crystal form of naloxone hydrochloride to solve its solubility problem, but the naloxone hydrochloride product in the prior art has good solubility in aqueous solution, and there is no big problem in the resolubility of the preparation. And this crystal form does not solve the storage stability problem of naloxone hydrochloride in the prior art
Zhang Yajun et al. gave three crystal forms of naloxone hydrochloride in "Naloxone Hydrochloride Crystal Form Analysis" ("Journal of Pharmaceutical Analysis", 2007.27 (02) 169~170 pages), and analyzed the three crystal forms The physical parameters of the three crystal forms were analyzed, but the stability data of the three crystal forms were not given, and the specific preparation methods of the three crystal forms were not given.
Therefore, relevant research still needs to be carried out to solve the instability problem of naloxone hydrochloride bulk drug

Method used

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  • Naloxone hydrochloride crystal form compound
  • Naloxone hydrochloride crystal form compound
  • Naloxone hydrochloride crystal form compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1) Take 60 mg of crude naloxone hydrochloride, add it to 20 mL of aqueous hydrochloric acid solution with a concentration of 1 mol / L, and heat to 50°C~60°C to dissolve to obtain a solution;

[0037] 2) Add activated carbon to the solution obtained in step 1), stir for adsorption, filter for decarbonization and sterilization, and obtain a clear solution;

[0038] 3) Under the condition of stirring at room temperature, add dropwise the mixed solution of ethanol / tetrahydrofuran with a volume ratio of 1:4, wait for the solution to become turbid and let it stand for 24 hours, filter, wash, and dry to obtain a white powder.

[0039] The obtained naloxone hydrochloride crystal form compound is measured using Cu-Kα rays to obtain X-ray powder diffraction patterns, such as figure 1 shown.

[0040] Elemental Analysis Results:

[0041] Measured value (calculated value), C: 62.71 (62.72), H: 6.10 (6.09), Cl: 9.73 (9.74), N: 3.83 (3.85), O: 17.60 (17.59).

Embodiment 2

[0043] 1) Take 50 mg of the crude product of naloxone hydrochloride, add it to 5 mL of aqueous hydrochloric acid solution with a concentration of 1 mol / L, and heat to 50°C~60°C to dissolve to obtain a solution;

[0044] 2) Add activated carbon to the solution obtained in step 1), stir for adsorption, filter for decarbonization and sterilization, and obtain a clear solution;

[0045] 3) Under the condition of stirring at room temperature, add dropwise the mixed solution of ethanol / tetrahydrofuran with a volume ratio of 1:4, wait for the solution to become turbid and let it stand for 24 hours, filter, wash, and dry to obtain a white powder.

[0046] The obtained naloxone hydrochloride crystal form compound is measured using Cu-Kα rays to obtain X-ray powder diffraction patterns, such as figure 1 The results were similar, and the 2θ difference of the spectral data did not exceed ±0.2.

[0047] Elemental Analysis Results:

[0048] Measured value (calculated value), C: 62.73 (62....

Embodiment 3

[0050] 1) Take 100 mg of crude naloxone hydrochloride, add it to 30 mL of aqueous hydrochloric acid solution with a concentration of 1 mol / L, heat to 50°C~60°C to dissolve, and obtain a solution;

[0051] 2) Add activated carbon to the solution obtained in step 1), stir for adsorption, filter for decarbonization and sterilization, and obtain a clear solution;

[0052] 3) Under the condition of stirring at room temperature, add dropwise the mixed solution of ethanol / tetrahydrofuran with a volume ratio of 1:4, wait for the solution to become turbid and let it stand for 24 hours, filter, wash, and dry to obtain a white powder.

[0053] The obtained naloxone hydrochloride crystal form compound is measured using Cu-Kα rays to obtain X-ray powder diffraction patterns, such as figure 1 The results were similar, and the 2θ difference of the spectral data did not exceed ±0.1.

[0054] Elemental Analysis Results:

[0055] Measured value (calculated value), C: 62.70 (62.72), H: 6.10 (6.0...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a naloxone hydrochloride crystal form compound shown as formula (I). The X-ray powder diffraction pattern obtained by measuring the compound with Cu-Ka rays is shown in figure 1. The naloxone hydrochloride crystal form compound provided by the invention has improved stability; compared with the preparation in the prior art, the preparation prepared by adopting the naloxone hydrochloride crystal form compound disclosed by the invention has a better medicinal effect.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a crystal form compound of naloxone hydrochloride. Background technique [0002] Naloxone Hydrochloride (NaloxoneHydrochloride) is a specific morphine receptor antagonist, the chemical name is 17-allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride, synthetic In 1960, the United States began to use it clinically in 1971, and it was recorded in the United States Pharmacopoeia in 1975. The affinity of the drug to opioid receptors is greater than that of morphine and enkephalin, which can competitively block and replace the binding of opioids and receptors, clear the symptoms of opioid drug intoxication, and rapidly induce the withdrawal of opioid addicts symptom. In China, it was first synthesized by the Institute of Toxic Drugs and Drugs of the Academy of Military Medical Sciences in 1985, and obtained the new drug certificate and production number of naloxone in 1990. It is wid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D489/08A61K31/485A61P39/02A61P25/32A61P25/30
CPCA61K9/0019A61K9/08A61K9/19A61K47/10A61K47/183C07B2200/13C07D489/08
Inventor 郭琨
Owner ZHENGZHOU SIHUAN MEDICINE ARTICLE CO LTD
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