33 results about "Valganciclovir Hydrochloride" patented technology

The invention belongs to the technical field of analytical chemistry, and specifically discloses an HPLC analysis and detection method for valganciclovir hydrochloride impurities, more specifically, relates to an analysis and detection method for guanine, ganciclovir, and methoxymethylguanine Purine, ganciclovir 1‑N‑methylvaline ester, monoacetoxy ganciclovir, monochloroganciclovir, or drugs containing the impurities in the above 6 or their preparations. The solution to be tested is injected into a high-performance liquid chromatography column with phenylsilane-bonded silica gel as a filler, washed and separated with a mobile phase composed of an amine-containing inorganic salt solution and a chromatographically pure organic solvent, and then analyzed and detected by ultraviolet light. For the first time, this method creatively adds a certain concentration of ammonium acetate or ammonium formate into the mobile phase, which completely solves the difficult problem of separation between the main peak and impurity peaks and adjacent impurity peaks. It is easy to operate, high in resolution, high in sensitivity and good in accuracy. , after literature search, there is no similar literature report.

The present invention provides novel solid pharmaceutical dosage forms for oral administration, after being constituted in water. The solid dosage forms comprise a therapeutically effective amount of valganciclovir hydrochloride and a non-hygroscopic organic acid present in an amount sufficient to stabilize the valganciclovir hydrochloride in a predetermined amount of water. The present invention also provides novel liquid pharmaceutical dosage forms for oral administration after constituting the solid pharmaceutical dosage form with water. A non-hygroscopic bulking agent may optionally be included in the above dosage form. These novel pharmaceutical dosage forms are useful in the treatment or control of viruses such as herpes simplex virus and cytomegalovirus. The present invention also provides a method for treating these diseases employing the solid and liquid pharmaceutical dosage forms and a method for preparing these pharmaceutical dosage forms.

The invention belongs to the field of drug analysis, and specifically discloses an HPLC detection method for an enantiomer of a valganciclovir hydrochloride intermediate hydrolyzate. The method uses cellulose-tri(3,5-dichlorophenylamino Formic acid ester) bonded silica gel as a chiral chromatographic column with a mixed solution of alkanes and alcohols as the mobile phase, the column temperature is 20-40°C, the flow rate is 1.0-1.5ml / min, and the wavelength is 250-260nm . The invention realizes the effective separation of four isomers of valganciclovir hydrochloride intermediate hydrolyzate, has good detection result accuracy, high sensitivity, simple operation, low cost and short analysis time, and is valganciclovir hydrochloride The quality control of intermediate hydrolyzate provides guarantee.

The invention discloses a method for preparing valganciclovir hydrochloride I. The method comprises the following steps of: 1, dissolving phosphorus oxychloride into an inert solvent, and performing a reaction of the mixture and the alcoholic liquor to obtain phosphoryl halide II; 2, performing a reaction of ganciclovir and the phosphoryl halide II obtained in the step to obtain ganciclovir monoester III; 3, esterfying the ganciclovir monoester III in the step 2 and N-carbobenzoxy-L-valine to obtain ganciclovir diester IV; 4, acidizing the ganciclovir diester IV in the step 3 for dephosphorylation to obtain N-carbobenzoxy-L-valine ganciclovir monoester V; and 5, performing a hydrogenation reaction on the product in the step 4 to prepare the valganciclovir hydrochloride I. By the method, the ganciclovir monoester with high purity and yield can be produced, the post-processing is easy, and the post-processing difficulty is reduced.

The invention discloses a novel valganciclovir hydrochloride synthesis method. The method includes: taking ganciclovir as a raw material, adopting ortho-ester for protecting a hydroxyl radical, then subjecting to condensation with N-carbobenzoxy-L-valine, and performing hydrolysis reaction to obtain N-carbobenzoxy valganciclovir; performing hydrogenation reduction reaction to obtain valganciclovir hydrochloride. The product purity reaches 99.0% or above and accords with United States Pharmacopeia standards.