Views:0 Author:Site Editor Publish Time: 2021-05-25 Origin:Site
The compound Remdesivir is relatively insoluble in aqueous media and chemically unstable. It is most stable in solutions with a pH of about 4 to 5. At a pH of 4 or below, the solubility of the compound increases.
Remdesivir lyophilized preparation for injection is a white to off-white or yellow lyophilized solid without preservatives. In addition to the active ingredients, the lyophilized preparation also contains the following inactive ingredients: water for injection, sodium sulfobutyl beta cyclodextrin (SBECD) and hydrochloric acid and/or sodium hydroxide. SBECD is an anionic, highly water-soluble cyclodextrin derivative, which can be well included with drug molecules to form non-covalent complexes, thereby improving drug stability, water solubility, safety, and reducing nephrotoxicity.
Preparation method of freeze-dried composition:
The cyclodextrin was dissolved in water, acid was added to the solvent to adjust the pH to less than 2, the compound Remdesivir was added to the acidified mixture to form a suspension of the complex, and alkali was added to the solution to adjust the pH to about 3.5 to form a supersaturated solution . Water is added to it as needed to adjust the concentration of the compound, and the mixture is lyophilized.
Remdesivir for injection has started a Phase III clinical study of anti-new coronavirus (2019-nCoV) in Beijing China-Japan Friendship Hospital. Gilead has done a lot of research on the dosage and safety of Remdesivir. At clinical doses, Remdesivir (Remdesivir) exhibits good overall safety in addition to its effects on liver function.
Remdesivir freeze-dried formulations also contain the following inactive ingredients: water for injection, sodium sulfobutyl-β-cyclodextrin (SBECD), use HCL and/or NAOH to adjust the pH of the formulation to 3.0-4.0, and then freeze-dry . According to the current stability data, the freeze-dried agent can be stored below 30 degrees for three years.
Shandong Binzhou Zhiyuan Biological Technology Co., Ltd. is committed to the professional production of pharmaceutical excipients: sulfobutyl beta cyclodextrin sodium, which has been filed in CDE. It has solubilizing and solubilizing properties, which can improve the stability and water solubility of Radixivir Sex, safety, reducing nephrotoxicity, etc.