5 results about "Clevidipine" patented technology

The invention relates to the technical field of new drugs, in particular to a clevidipine butyrate concentrated solution and a preparation method thereof, and the composition contains clevidipine butyrate, a solubilizer, a cosolvent, a pH regulator and water for injection. Injection oil is abandoned, so that the requirements of lipid metabolism defect patients are met; no phospholipid is used in the prescription, safety risks such as hemolysis, immunoreaction and long-term toxicity and stability problems such as oxidative degradation are avoided, after phospholipid is removed, the clevidipine butyrate preparation can tolerate excessive hot-press sterilization, the sterility level guarantee degree is higher, the state of the clevidipine butyrate preparation is converted into a true solution system from a micelle system, and the stability of the clevidipine butyrate preparation is improved. The solubilizer and the cosolvent are combined, so that the solubility of clevidipine butyrate is greatly improved, dichloromethane, chloroform and other organic solvents with large toxic and side effects are not needed, the toxicity of the medicine is reduced, the stimulation to blood vessels is small, and the adverse reaction of the medicine is reduced; and the preparation method is simple and easy to amplify, and production amplification is facilitated by selecting a production process of a common injection.

Injectable Clevidipine emulsion formulations having enhanced stability and clarity for extended periods of time are disclosed. Methods of making the compositions as well as compositions made by the method and methods of treatment using the compositions are also disclosed.

The invention discloses a preparation method of clevidipine butyrate impurities. Specifically, the invention provides a preparation method of a compound as shown in a formula II, which comprises the following step: in an organic solvent, in the presence of alkali, carrying out hydrolysis reaction on a compound as shown in a formula I. The preparation method provided by the invention has relatively high yield, the purity of the obtained target product can reach 95% or above, and the requirement of NMPA on impurity research in drug declaration is met. The method is simple and convenient to operate, mild in reaction condition and easy in reagent obtaining, and has a good application prospect.

The invention discloses related application of a target compound in treatment of Alzheimer's disease, and relates to the field of biological medicine. In order to solve the problem that an existing autophagy inducer depending on an mTOR signal channel may cause side effects such as immunosuppression or metabolic disorder, the invention provides application of at least one small molecule compound of phytolaccin, 2-hydroxycinnamic acid, clevidipine butyrate or 3 ', 4', 7-trimethoxy quercetin as the autophagy inducer. The compound does not depend on an mTOR signal channel, has the blood-brain barrier penetrating capacity and can effectively induce autophagy. In caenorhabditis elegans and mouse Alzheimer's disease models, the compound shows a remarkable neuroprotective effect, accumulation of toxic protein aggregates such as beta-amyloid protein and over-phosphorylated tau in the brain can be reduced, cognitive impairment and related neuropathological characteristics are improved, and the compound can be used for preventing and treating neurological diseases. A new strategy is provided for treatment and / or prevention of Alzheimer's disease.