34 results about "Vidarabine Monophosphate" patented technology

The invention discloses a refining method of vidarabine monophosphate. The refining method is characterized by comprising the following steps of: regulating the pH of a vidarabine monophosphate crude product and an antioxidant to 8-10 by using alkali, and heating and dissolving; then adding a right amount of active carbon, and filtering while hot; regulating pH to 3-5; and crystallizing. The refining method disclosed by the invention can achieve high yield and can be used for refining the high-purity vidarabine monophosphate.

The invention relates to a vidarabine monophosphate freeze-dried powder injection and a preparation method thereof, and the vidarabine monophosphate freeze-dried powder injection is prepared by freeze-drying vidarabine monophosphate, sodium hydroxide solution and water for injection, wherein the sodium hydroxide solution is used as a pH regulator, and the sodium hydroxide solution is used until the pH value of liquid medicine is 7.0-7.5. The vidarabine monophosphate freeze-dried powder injection provided by the invention is few in types of auxiliary materials, low in using amount, good in forming property of a freeze-dried product, good in re-dissolving property, clear in appearance of the solution before freezing, good in clarity after being freeze-dried, low in content of impurities, good in stability and controllable in quality, and can reduce the potential safety hazard of the vidarabine monophosphate freeze-dried powder injection, and improve the efficacy of the vidarabine monophosphate freeze-dried powder injection.

The invention provides a phosphorylation method for preparing vidarabine monophosphate. The method is specifically as below: using vidarabine as a starting material; conducting phosphorylation on the material under the protection of inert gas and under the effect of catalyst; and conducting active carbon decoloration treatment to obtain a vidarabine monophosphate crude product. The process route is simple, low-cost and high-yield; and compared with the prior art, the production process has significantly reduced toxicity, and is suitable for process production.

The invention relates to a chitosan microsphere drug delivery system of vidarabine and a preparation method. The method is characterized by acquiring the the medicinal microsphere drug delivery system with a complete spherical shape, a uniform particle size, a high embedding rate, good dispersity and a sustained release property. The specific technical scheme is that: chitosan is taken as a membrane material, polyethylene glycol is adopted as a pore-forming agent, glutaraldehyde is employed as a crosslinking agent, and inverse emulsification-crosslinking method is used to prepare the drug carrying microspheres. The preparation method includes: dissolving the drug in an acidic aqueous solution of chitosan, adding polyethylene glycol and stirring them uniformly, and taking the mixture as an aqueous phase; adding the aqueous phase slowly into an oil phase containing a surface active agent and a dispersing agent, carrying out stirring and emulsifying to uniformity, and adding the crosslinking agent to undergo crosslinking solidification; and washing and drying the obtained product. The invention provides the vidarabine chitosan microsphere drug delivery system with a sustained-release property.

The invention relates to a vidarabine monophosphate freeze-dried powder injection for injection and a preparation method thereof. The freeze-dried powder injection is obtained by freeze-drying a vidarabine monophosphate drug solution. The formula is: 100 g of vidarabine monophosphate, 25 g of mannitol, 3 g of disodium hydrogen phosphate, 0.3 g of sodium dihydrogen phosphate, 1 g of disodium edetate, and add water for injection to 2000 mL. The freeze-drying process in the preparation method of the freeze-dried powder injection includes three processes of pre-freezing, sublimation and temperature-rising drying. The freeze-dried powder injection and the preparation method thereof of the present invention have significant advantages in storage and transportation compared with the commonly used water injection in the prior art.

The invention relates to an officinal composition of vidarabine monophosphate for injection, wherein the main active components of the composition comprise vidarabine monophosphate and lysine.

The present invention relates to a vidarabine monophosphate pharmaceutical composition and a preparation method thereof. The pharmaceutical composition consists of vidarabine monophosphate, vidarabine, sodium chloride and water-soluble cyclodextrin or a water-soluble cyclodextrin derivative, wherein the mass ratio of vidarabine monophosphate, vidarabine, sodium chloride and water-soluble cyclodextrin or the water-soluble cyclodextrin derivative is 25-35:1-3:1:10-20, preferably 30:2:1:15. The vidarabine monophosphate pharmaceutical composition provided by the present invention has significantly reduced irritation to muscle and blood vessels, and better long-term storage stability. Meanwhile, the vidarabine monophosphate pharmaceutical composition provided by the present invention contains both vidarabine monophosphate and vidarabine, thereby having more significant efficacy. The preparation method for the vidarabine monophosphate pharmaceutical composition is simple and feasible, suitable for industrial production.

The invention discloses a synthesis technology of vidarabine monophosphate. The synthesis technology comprises the following steps: suspension dissolving vidarabine into an aprotic polar solvent firstly, carrying out reaction on a reactant and pyrophosphoryl chloride at low temperature, then carrying out hydrolysis quenching, regulating a pH value to 2.5-3, and precipitating the vidarabine monophosphate, wherein the purity of a crude product is 95 percent or above; and finally, carrying out recrystallization treatment on the vidarabine monophosphate to improve the purity of the vidarabine monophosphate to 99 percent or above with the maximum single impurity content controlled to be 0.2 percent or below. The synthesis technology of the invention has the advantages of high yield and less impurities and is suitable for industrial production.

The invention discloses a preparation method of vidarabine monophosphate. The preparation method comprises the following two steps: crude product synthesis and crude product refining. In a crude product synthesis stage, reaction conditions are controlled severely, side reaction and production of related substances are reduced effectively, and high percent conversion of a target product is ensured.Meanwhile, because most of side products of reaction are dissolved in the reaction system and the target product is not dissolved in the reaction system basically, aftertreatment is facilitated to improve the purity of the product. The method is simple in process, high in product yield, high in purity and high in reaction selectivity; any special equipment is not used during production; and the preparation method is suitable for industrial production.