Injection of ambroxol hydrochloride and preparation method thereof

Abstract

The invention provides an injection of ambroxol hydrochloride and a preparation method thereof; the injection comprises 15 parts by weight of ambroxol hydrochloride, 0.01-0.03 part by weight of citric acid, 2-20 parts by weight of polyethylene glycol 400, 16-18 parts by weight of sodium chloride, and 2000 parts by weight of injection water, and preferably comprises 15 parts by weight of ambroxol hydrochloride, 0.02 part by weight of citric acid, 5 parts by weight of polyethylene glycol 400, 17 parts by weight of sodium chloride, and 2000 parts by weight of injection water. The injection of ambroxol hydrochloride provided by the invention can tolerate hot pressurized sterilization at 121 DEG C for 15 min, is compatible with drug solutions with a pH of more than 10, has good stability, and can better guarantee medication safety for human body.

Description

technical field [0001] The invention relates to ambroxol hydrochloride injection, which belongs to the technical field of pharmaceutical preparations, and more specifically relates to a highly stable ambroxol hydrochloride injection and a preparation method thereof. Background technique [0002] Respiratory diseases are generally manifested as cough, phlegm, wheezing, and inflammation, especially increased sputum volume and difficulty in expectoration are symptoms of many respiratory diseases such as chronic obstructive pulmonary disease (COPD), bronchial asthma, and cystic pulmonary fibrosis (CF). Common symptoms, children and the elderly often have difficulty spitting, which interferes with people's daily life in mild cases, and even endangers the lives of patients in severe cases. At the same time, in the case of thoracic and abdominal operations, patients often produce a large amount of sputum, which can block the respiratory tract, easily cause coughing, wheezing, and e...

AI Technical Summary

Problems solved by technology

It can be seen that there is a pH limit of the liquid medicine when the original research product is used. At the same time, the original research product uses nitrogen gas to protect the product stability. The nitrogen gas filled during production needs to be filtered and sterilized, which increases equipment investment and increases the risk of bacterial contamination during production. At the same time, the product is injected Nitrogen gas dissolved in the medicinal solution will enter the blood and affect the oxygen content of the blood. When the nitrogen content of the blood in the human body increases, it will cause restlessness and mental excitement, so there is a threat of adverse reactions.

[0018] Chinese patent CN101416956B discloses that a kind of ambroxol hydrochloride injection is made up of active ingredient ambroxol hydrochloride, pH regulator, stabilizer, water for injection, osmotic pressure regulator, has used citric acid, sodium dihydrogen phosphate, sodium chloride , water for injection and other components, nitrogen was not used in the preparation process, and the content of related substances in the samples was relatively high (>0.1%), and its stability data showed that the most stable samples at room temperature were kept at room temperature for 36 months. It is higher than 0.2%, which has nearly doubled compared to the data in 0 months, and most samples have nearly tripled. The stability of the samples made by this patented method has serious problems, and it cannot reach the 60-month validity period of the original product.

[0019] Chinese patent CN101836952B discloses a kind of ambroxol hydrochloride injection, which contains ambroxol hydrochloride, disodium hydrogen phosphate, and citric acid in a weight ratio of 1:0.18-0.22:0.12-0.16, and the amount of activated carbon used in the preparation process is 0.2%- 0.3% (W / V), if the amount of activated carbon is too large, it will adsorb the main components in the liquid medicine, causing the loss of active components and affecting the curative effect, and there is also nitrogen filling operation

[0020] Chinese patent CN101836953B discloses a kind of ambroxol hydrochloride injection, comprising 14-16 parts by weight of ambroxol hydrochloride, 2.6-3.2 parts by weight of citric acid, 4.8-6.0 parts by weight of disodium hydrogen phosphate, and 13-16 parts by weight of sodium chloride 1800-2500 parts by weight of water for injection, the pH of the injection is controlled at 5.5-7.0, 0.02%-0.05% of activated carbon is used in the preparation, and a sterilization process of 115 ° C for 20-30 minutes is adopted. Although the injection improves the pH of the liquid, the sample is frozen and placed at room temperature for slow rethawing and has insoluble particles. Once the liquid is transported into the alpine region, it will freeze at low temperature and cannot be rethawed, which will cause inconvenience in transportation and seriously affect the stability of the drug. , the amount of activated carbon used in the patented method is too small, and it is difficult to ensure a low level of bacterial endotoxin. At the same time, the samples obtained by this method cannot withstand the sterilization process at 121 ° C for 15 minutes, and there are hidden dangers in drug safety

[0021] After a lot of systematic creative research work, the inventor has obtained a product with higher quality, simpler production process, lower cost, stable freeze-thaw, no need for nitrogen protection, stable storage at room temperature for 60 months, compatible with pH Ambroxol hydrochloride injection used in combination with a solution higher than 10 creatively solves the problems of the prior art, and has a significant improvement compared with the prior art. Related reports and public use

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