49 results about "Ubenimex" patented technology

The invention relates to ubenimex disket and its process, a composition disket comprising such as active ubenimex, disintegrating agent, filler, suspending agent bond, glidant, corrigent. Said ubennimex disket is convenient for medication, suitable for the old and small children and patient with swallowing difficulties.

The invention discloses a ubenimex fat emulsion injection, comprising ubenimex, oil for injection, emulsifier, stabilizer, isoosmotic adjusting agent and water, wherein, the concentration of the ubenimex is 0.05-10g / ml, the concentration of the oil for injection is 5-30g / ml, the concentration of the emulsifier is 0.8-3.0g / ml, the concentration of the stabilizer is 0.1-2.0g / ml, and the concentration of the isoosmotic adjusting agent is 2-3g / ml. Through measuring, the quality and the appearance of the fat emulsion injection of the invention are uniform, the average particle diameter is about 300nm, and the pH value is 5.0-9.0, thus, the fat emulsion injection can be used for injection. The ubenimex fat emulsion injection has obvious anti-tumor function. According to the characteristics of common fat emulsion injection, the ubenimex fat emulsion injection as an anti-tumor medicine also has the functions of slow releasing, targeting, providing organisms with energy and the like.

The invention belongs to the technical field of medicines and in particular relates to a method for recrystallizing ubenimex. By adopting the method for recrystallizing ubenimex, the phenomenon that materials can be instantly caked in the existing ubenimex crude product recrystallization process is avoided, hydraulic acid and ammonia water are greatly saved, and the total yield is increased by about 7-8 percent points.

The invention belongs to the field of medicine preparation and provides a completely novel method for synthesizing Ubenimex. The method comprises the steps of firstly, protecting amino of a starting raw material, i.e., (2S,3R)-3-amino-2-hydroxyl-4-phenylbutyric acid (AHPA for short) by using di-tert-butyl dicarbonate so as to form a Boc protective product, then, carrying out condensation with L-leucine tert-butyl ester, and finally, removing the protective group in an organic solution of hydrogen chloride, thereby obtaining Ubenimex. According to the method, reagents used by the adopted synthesis route are all commonly-used reagents, produced industrially and low in cost; reaction solvents are all ordinary solvents, are low in toxicity and little in environmental pollution; and each reaction step is mild in conditions and simple and convenient in operation and does not need special equipment, so that the method is suitable for carrying out industrial production. The purity of the prepared product reaches 99.5% or more.

The invention provides a crystal form of an ubenimex intermediate N-[(2S, 3R)-4-phenyl-3-benzyl-3-formylaminobenzoxy-2-hydroxybutyryl]-L-benzyl leucine. The ubenimex intermediate with the crystal form has high purity and good stability and is suitable for further preparing high-purity ubenimex active pharmaceutical ingredients. The invention also provides a preparation method of the crystal form, wherein according to the method, recrystallization is used for preparation; through HPLC (High Performance Liquid Chromatography), the purity of the obtained crystal is over 98.5%; and moreover, the adopted organic solvent is a common solvent with low price, a single-solvent recrystallization is more convenient for recovery, and the method is suitable for industrial production.

The invention discloses an ubenimex recrystallization device and a method thereof. The recrystallization device comprises a reaction kettle and a driving motor, and the driving motor is connected witha bevel gear transmission mechanism arranged in the reaction kettle through a main stirring shaft; the bevel gear transmission mechanism is composed of a main planet gear, at least one side planet gear and an auxiliary planet gear which are arranged from bottom to top, the side planet gear is connected with the main planet gear and the auxiliary planet gear respectively, and the main planet gearis connected with the main stirring shaft through a shaft; the auxiliary planetary gear is connected with the top end of the reaction kettle through a vertically-arranged auxiliary connecting shaft; and the side planetary gear is connected with the side wall of the reaction kettle through a horizontally-arranged side connecting shaft. According to the ubenimex recrystallization device, six-direction stirring can be achieved, the effect of dispersing gel is achieved, dead corners are greatly reduced, the problem that in the prior art, caking is likely to happen is solved, the production processis easier to control, and the quality is more stable; the product purity is improved, and the yield is also increased.