Development of domestic infusion drugs based on paracetamol

Abstract

The intravenous form of paracetamol compared with oral more reliably supports effective drug concentration in blood plasma that promotes a higher therapeutic effect.Recent studies have confirmed that the use of the intravenous form of paracetamol to deal with postoperative pain multimodal analgesia modes results in reducing the frequency and quantity of opioids administered , and, as a consequence, its associated side effects. The drug Paracetamol , infusion solution 10 mg / ml to 100 ml glass bottles is a drug - generic . His qualitative and quantitative composition is developed from the study of literature data about the drug - similar to " Perfalhan , 10 mg / ml solution for infusion in 100 mL " company Bristol - Myers Squibb, France and experimental work.The aim of our study is development and support of the national composition of the infusion of the drug on the basis of paracetamol, selection of excipients that provide stability of the active substances. Materials and methods. The object of the study was the substance of paracetamol manufactured by Zhejiang Kangle Pharmaceutical Co. , Ltd, China. During the work conducted qualitative and quantitative monitoring sample preparation for indicators of stability: pH content of the active ingredient , transparency, color, impurities , contamination by the methods described in the SFU [and nor- ral documentation to the drug . One potential factor of instability is the effect of paracetamol oxygen, due to the presence in the molecule of paracetamol and -NH possibility of oxidation.Results and Discussion. Paracetamol is derived atsetamina . Substance acetylation are p - aminophenol with acetic anhydride . Saturated aqueous solution has a pH of paracetamol - ment about 6 .Paracetamol is a crystalline white powder , sparingly soluble in water, soluble in 96% alcohol, very slightly soluble in metilenhloride . . Active substance enters in comparison drug in the concentration of 10 mg/ml. Stable aqueous solution decreases in acidic and alkaline environments where paratse - tamol gradually destroyed to acetic acid or p - aminophenol To prevent oxidation of the drug administered antioxidant - sodium metabisulfite in concentrations generally 1.0 g / l. In order to prevent the negative - tive impact of oxygen on paracetamol solution 10 mg / mL drug preparation was conducted under nitrogen gas protection . It is established that the use of nitrogen gas protection affects the quality of the drug. Prepared sample preparation without nitrogen gas protection did not meet project MKYA in terms of " 4 - aminophenol " and " color ", besides a slight tendency pH change and reducing quantitative content of active ingredient. Therefore, the production of the drug " Paracetamol , infusion solution 10 mg / ml. in bottles of 100 ml " necessary solution prepared bubbling nitrogen for 20 minutes. It is established that the use of nitrogen gas protection affects the quality of the drug. the manufacture of the drug " Paracetamol , infusion solution 10 mg / ml. in bottles of 100 ml " necessary solution prepared bubbling nitrogen for 20 minutes. Calculated theoretical osmolarity of the drug- 299,47 мОsм / l. Solution osmolarity close to osmolarity of blood, which is an important criterion when used in injection therapy. Conclusions. Theoretically grounded and experimentally confirmed rational composition drug infusion composition based on paracetamol.Selected auxiliaries and processing methods in the preparation of the solution , prevents oxidation of the main active ingredient , and also provide the optimum level of osmolarity solution. Results of this development are used during compile of registration dossier of preparation, analytical and technological normative documents on his production and control of quality of intermediate products and prepared products.