31 results about "Ganciclovirum" patented technology

The invention provides a ganciclovir preparation method, which comprises: 1, carrying out a condensation reaction process by adopting glycerol acetal ester and diacetyl guanine as raw materials and dioxane as a solvent under the effect of trifluoroacetic acid, and carrying out post-treatment to obtain triacetyl ganciclovir, 2, hydrolyzing the triacetyl ganciclovir obtained in the step 1 to obtaina ganciclovir crude product, and 3, refining the ganciclovir crude product obtained in the step 2 to obtain a ganciclovir finished product. According to the method, based on diacetyl guanine, the total yield reaches 35%-40%, the quality of the prepared bulk drug product is greatly improved, the contents of the impurity C and the impurity F (guanine) are controlled to 0.05% or below, the total impurity content is 0.06%-0.10%, and the product purity is greater than 99.9%.

A process for the preparation of valganciclovir with triacetyl ganciclovir (V) as a starting material, comprising the following steps: selective hydrolysis, reacting with a coupling agent and CBZ valine and a solvent, followed by hydrolysis under basic conditions and hydrogenolysis in the presence of a catalyst.

The invention discloses a preparation method of ganciclovir powder injection and a filter press used therefor, belonging to the technical field of pharmaceutical production. The sodium chloride aqueous solution is mixed evenly, and finally ganciclovir powder injection is obtained by freeze-drying; the filter press includes a bracket, a thrust plate, a pressure plate, a filter plate, a filter cloth and a driving part, and the filter cloth and the filter plate are separated and installed in the On the frame body, the material of the frame body is polypropylene, and the upper and lower edges of the frame body are provided with deep clamping grooves and shallow clamping grooves corresponding to the upper and lower guide rods, which can be easily installed and disassembled on the upper and lower guide rods. The filter plates are respectively provided with the first sealing components, and the opposite surfaces of the two adjacent filter plates are respectively provided with the second sealing components. The impurity content of the ganciclovir powder injection prepared by the method provided by the present invention is relatively small, and the effect of the ganciclovir powder injection can be improved; Clean and replace.

Human cytomegalovirus vectors comprising heterologous antigens are disclosed. The vector derived from the TR strain is ganciclovir-sensitive, contains active US2, US3, US6, US7, and UL131A genes, and has a deleterious or inactivating mutation in the UL82 gene that prevents expression of pp71.

Stereochemically defined dipeptide esters of nucleoside-analogous antiviral agents including acyclovir and ganciclovir are provided. Certain of these stereochemically defined dipeptide esters are found to have unexpectedly enhanced delivery to and uptake by ocular tissues, crossing the blood-ocular barrier more effectively than other stereochemically defined dipeptide esters. For example, (L-Val)-(D-Val)-acyclovir was found to be taken up more effectively into corneal tissue than were underivatized acyclovir, monoesters (L-Val)-acyclovir or (D-Val)-acyclovir, or diester (L-Val)-(L-Val)-acyclovir.

The invention discloses a preparation method of ganciclovir sodium freeze-dried powder for injection, which comprises the following steps in sequence: adding mannitol into water for injection, adding activated carbon, stirring and standing still, and then decarbonizing by coarse filtration; The decarbonized mannitol solution is passed through a sterile mixed cellulose film to obtain a purified mannitol solution; adding ganciclovir sodium to the purified mannitol solution, and then passed through a sterile mixed cellulose film to obtain Ganciclovir sodium solution; Described Ganciclovir sodium solution is carried out temperature control, and with CO 2 Adjusting the pH value; putting the ganciclovir sodium solution in a bottle, half-tamping and then freeze-drying; after the freeze-drying is finished, pressing and re-pressing to obtain the ganciclovir sodium freeze-dried powder for injection. The mannitol of the present invention is more suitable for the storage of the ganciclovir sodium freeze-dried powder as the protective agent of the ganciclovir sodium freeze-dried powder, and can better ensure the purity of the ganciclovir sodium freeze-dried powder.

The invention provides a Gancilorvir dispersable tablet and its preparation, wherein the dispersion tablet comprises 62.5 wt% of Ganciclovir, 10-25% of crystalline cellulose, or calcium hydrogen phosphate and / or starch, 1-10% of sodium carboxymethylstarch, or low substituted methylcellulose propylene glycol ether and / or cross bonding polyvinylpyrrolidone or crosslinked sodium carboxymethylcellulose, 0.1-1.4% of polyvinylpyrrolidone, or methyl hydroxypropylcellulose, 5-15% of lactose, 0.5-1.4% of magnesium stearate. The preparing process comprises sieving, mixing, granulating, drying, and tabletting.

The invention discloses a ganciclovir composition for injection and a freeze drying process of the ganciclovir composition. The ganciclovir composition for injection comprises ganciclovir and sodium hydroxide, and is prepared by freeze drying of a liquid medicine containing 150-180 mg / mL of ganciclovir. The freeze drying process comprises the following steps: sequentially pre-freezing, sublimationdrying and desorption drying of the ganciclovir liquid medicine to obtain a ganciclovir powder injection. The prescription is simple and reasonable, the process is simple and easy to operate, the obtained product has excellent stability and redissolution performance, the problems that moisture is not easy to remove in the freeze drying process and the freeze-dried product structure is easy to collapse and shrink due to high solid content are solved on the premise of not greatly prolonging the freeze drying period, and the quality stability of the product and the safety of clinical medicationare fundamentally ensured.

The invention discloses a ganciclovir related substance detection method, and relates to the field of pharmaceutical analysis. According to the ganciclovir related substance detection method, an octadecyl silane bonded silica gel chromatographic column is used, 0.012 mol / L ammonium dihydrogen phosphate solution-methanol (98-95: 2-5, V / V) is used as a mobile phase A, methanol is used as a mobile phase B, gradient elution is carried out, and the related substances in ganciclovir are detected. The pH value of the ammonium dihydrogen phosphate solution is adjusted to 2.5-3.5 by using a phosphoric acid solution. The method can be used for rapidly and effectively separating various potential trace related substances in ganciclovir raw material medicines, has the advantages of stable base line, attractive peak shape, good separation degree between a main peak and adjacent impurities and between the adjacent impurities, high durability and the like, and can be used for efficiently realizing qualitative and quantitative treatment of various related substances in ganciclovir. The method is suitable for rapid quality monitoring of ganciclovir in industrial mass production, and has important significance for product quality control.

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.

The invention discloses a method for synthesizing valganciclovir hydrochloride. Using 1,3-dichloro-2-acetoxymethoxypropane as a starting material, monochloroganciclovir is prepared by esterification. , hydrolysis, deprotection into salt and finally obtain valganciclovir hydrochloride. The invention provides a method for synthesizing cganciclovir hydrochloride, which avoids the problem of separation and conversion of N-7 and N-9 isomers in the condensation process of diacetylguanine, and directly synthesizes monochlorovir without ganciclovir. Genanciclovir replaces the synthesis of monoacetyl ganciclovir in the prior art, and avoids the difficult problem of separation of diesters caused by residual ganciclovir. The method has short process steps, simple operation, easy purification and low cost. , conducive to industrial production, suitable for the synthesis of valganciclovir hydrochloride.

The present invention relates to an ophthalmic composition, which comprises ganciclovir and olopatadine; wherein, the mass ratio of ganciclovir to olopatadine is (2‑6):1. The present invention also relates to a preparation method of an ophthalmic composition, comprising: step S1, mixing ganciclovir, olopatadine, an osmotic pressure regulator, a pH regulator and water for injection at a temperature of 90-100°C , to obtain a mixed solution; step S2, at a temperature of 70-80° C., adding a solubilizer, a preservative and water for injection to the mixed solution to obtain the ophthalmic composition. In addition, the present invention also relates to the application of the ophthalmic composition in the preparation of medicines for treating keratitis. The eye drops containing the ophthalmic composition provided by the invention not only have good anti-inflammatory and anti-viral effects, but also can avoid adverse reaction symptoms such as eyelid edema, conjunctival hyperemia, pain and burning sensation in patients with long-term use.

The invention discloses a method for synthesizing acyclovir and ganciclovir by carbon-hydrogen bond activation and belongs to the field of organic synthesis. The method comprises that inexpensive guanine as a raw material undergoes methyl protection on 9th NH, a high-valent iodine reagent and monoacetyl-protected ethylene glycol or 1, 2-isopropylidene-protected glycerol are added into the raw material under catalysis of palladium acetate, the mixture undergo a heating reaction to produce acetyl-protected acyclovir or acetyl-protected ganciclovir, and the acetyl group is removed by an inorganicalkali alcohol solution so that acyclovir and ganciclovir are obtained. The method utilizes cheap and easily available raw materials, prevents use risk and corrosive reagents, has the advantages of short reaction route, simple operation, high atomic economy and high total product yield, provides a novel synthesis route of acyclovir and ganciclovir and has a potential application prospect.