Pharmaceutical composition containing nalmefene hydrochloride and preparation method of same

Abstract

The invention relates to a pharmaceutical composition containing nalmefene hydrochloride. Nalmefene hydrochloride injection is a product of the pharmaceutical composition. 1ml injection consists of 0.1mg or 1mg nalmefene hydrochloride, 9.0 mg sodium chloride, 0.3mg ethylene diamine tetraacetic acid, hydrochloric acid and the remaining of water for injection, wherein the hydrochloric acid is used for regulating pH of the injection to 3.75-3.85. A preparation method of the pharmaceutical composition comprises the following steps of: mixing the nalmefene hydrochloride, the sodium chloride and the ethylene diamine tetraacetic acid, dissolving the mixture in the water for injection, uniformly mixing the mixture, and adding the water for injection to full; adding 0.1mol / L hydrochloric acid in to the mixture to regulate the pH value of medicine liquid to 3.75-3.85; filtering the medicine liquid by using a microporous filtering film with the thickness of 0.22 microns; and sterilizing the medicine liquid in a water bath with the temperature of 121 DEG C for 15 minutes to obtain the nalmefene hydrochloride injection. The pharmaceutical composition containing the nalmefene hydrochloride is simple components; and the product has the advantages of less foreign matters as well as high stability and safety based on tests on influencing factors, long-term stability and safety.

Description

[0001] technical field [0002] The invention belongs to the technical field of medicine, and in particular relates to a nalmefene hydrochloride pharmaceutical composition and a preparation method thereof. [0003] Background technique [0004] Opioid receptor antagonists are mainly used clinically for first aid for opioid drug overdose or poisoning, anesthesia awakening after surgery, first aid for alcoholism, anti-relapse after detoxification, adjuvant treatment for shock, adjuvant treatment for alcohol dependence, etc. . Indications that are still under investigation include weight loss, smoking cessation, childhood autism, self-harm, interstitial cystitis, and more. With the continuous expansion of clinical applications, the consumption of opioid receptor antagonists has increased dramatically in recent years. [0005] The existing varieties of opioid receptor antagonists in China cannot fully meet various clinical needs in terms of pharmacokinetic parameters, alterna...

AI Technical Summary

Problems solved by technology

However, adding new components will not only affect the medicinal effect of nalmefene, but also bring new problems (such as impurity content and stability after storage)

The Chinese patent with the authorized notification number CN101406474B pointed out in the background technology that "the nalmefene injection prepared with reference to the technical solution disclosed in the specification of CN895251, although the dimer is reduced, produces more polar impurities after sterilization. , still can not fully meet the quality stability requirements", for this reason, CN101406474B patent provides a kind of nalmefene hydrochloride injection, it comprises the nalmefene hydrochloride of therapeutically effective amount and pharmaceutical carrier, and described pharmaceutical carrier comprises isotonic Regulators, antioxidants and pH regulators, optionally containing chelating agents, wherein said antioxidant is tryptophan (see claim 1 of this patent)

The patent can improve the stability of the injection by using tryptophan as an antioxidant. After being placed under high temperature conditions for 10 days and accelerated testing at 40°C for 6 months, the appearance, pH, content of active ingredients and related substances of the sample are not obvious. Changes; but no more than one year of stability tests and data

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