Preparation And Quality Standard Of Naloxone Hydrochloride For Injection

Naloxone synthesized in1963, clinical applicationed in1971in the United States. China officially listed it in1990. This medicine is used to treat morphine overdose or acute poisoning, against respiratory depression and other central nervous system depression symptoms, enables coma recovering quickly. In recent years, there are varieties of naloxone hydrochloride on the market, including injection, ocular drug delivery formulations, transdermal formulations, sublingual tablets, and so on. This paper based on the study of literature research, according to the situation of the modern research, reference to the same drug and other drugs in the same dosage form of the research program, Established prescription and the study of the preparation process, use HPLC and other modern analytical techniques, developed quality standards,and the stability of the preparation of a preliminary study for future drug research and production of large-scale experimental basis.Preparation Process aspects:design three kinds of different specifications of the prescription, Production of the product in accordance with the preparation process, the resulting product traits dispersion as the evaluation index, screening of excipients; In order to verify the preparation to the relevant standards of the medication, its pH value was measured, the results between3.0and5.0, it can meet the Medication standards and provide a basis for the development of its quality standards;pyrogen (bacterial endotoxin) injection inspection is an important indicator of the need to control the injection of the preparation、usually adding an appropriate amount of activated carbon using the method in addition to pyrogen (bacterial endotoxin);But the activated carbon adsorption of drugs, often make content decreased, therefore, examine the amount and use of activated carbon, minimize the adsorption of the main drug in the premise of reach depyrogenation (bacterial endotoxin). The indexes of the product plus activated carbon content before and after the change (adsorbed amount) and bacterial endotoxin inspection to determine the the recipients species, the pH value and the amount of active carbon production products with different specifications, in accordance with the design process.Quality standards aspects:the six batches of test products for the trait, identification, acidity, clarity and color, moisture, related substances, bacterial toxins, load difference, and the determination of compatibility and other related research. Based on the findings, and combined with the stability of the findings to develop quality standards naloxone hydrochloride for injectionPreliminary stability test:Stability inspection.the two specifications of the products of the three batches of samples, results of two specifications of the study sample was consistent, The concrete conclusion are as follows:The light (45001x), high temperature (40℃), high humidity under10days test, Product traits and acidity are almost no change, clarity, and clarity of the solution are required, related substances which under light10days increased by about0.9%, the content will decrease, under heat10days increased by about0.3%, the content of a corresponding decline, under humidity10days material and content are almost unchanged. Show that the goods of high humidity and high temperature is relatively stable, slightly worse on the light stability.Accelerated test (40℃)6months, product traits and acidity little change, the clarity and the clarity of the solution are required, related substances increased by about0.5%, and a corresponding decline in content.Stability of long-term retention samples in a12-month, the sample characteristics and acidity are little change, clarity and clarity of solution are required, related substances increased by about0.2%, the content decreased accordingly. Bacterial endotoxin and sterility to12months comply with regulations. Room temperature stability investigation is still in progress. Based on the above test results, this product should be shading, sealed, and the storage conditions, the validity of this product is tentatively scheduled for2years.