85 results about "Fasudil" patented technology

Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT_2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.

The invention provides a fasudil salt injection for improving stability. The injection consists of the following components based on a weight ratio: the fasudil salt and medical sodium chloride are blended with water to 2,000ml according to a ratio of 100:1 to 1:100 to prepare 1,000 injections. The stability of the fasudil salt injection to light and heat is improved by reducing the oxygen content in the injection and introducing inert gas, so that the preserving period of injection products can be prolonged, and the injection has higher industrial application value. The invention provides a preparation method.

The invention relates to a fasudil hydrochloride compound and a novel method thereof. The method comprises the following steps of: in the presence of a solvent, performing sulfonation reaction on a chlorosulfonic acid serving as a sulfonating agent and isoquinoline to generate a 5-isoquinolinesulfonic acid; reacting the 5-isoquinolinesulfonic acid with thionyl chloride under a heating condition to generate isoquinoline-5-sulfonyl chloride hydrochloride; and dissolving the isoquinoline-5-sulfonyl chloride hydrochloride with ice water, adjusting the pH value of the solution with sodium bicarbonate, reacting the solution with homopiperazine, adjusting the pH value again with a hydrochloric acid, and concentrating under reduced pressure and recrystallizing to prepare the fasudil hydrochloride compound. The synthesis method of the invention has the advantages of mild reaction conditions, high yield and easy industrial production.

The invention discloses hydrochloric acid Fasudil liposome injection and new application thereof. The injection mainly comprises the following components according to parts by weight: 1 part of hydrochloric acid Fasudil, 2 to 20 parts of phospholipid, 0.5 to 10 parts of cholesterol and 1 to 8 parts of polysorbate 80. Simultaneously, the hydrochloric acid Fasudil liposome injection also can be used for treating vertebral artery type cervical spondylosis.

The invention relates to a preparation method of fasudil hydrochloride. In the method, 1-(5-isoquinoline sulfonyl) homopiperazine does not undergo chromatographic column separation and purification, lots of organic solvent for elution is omitted, and multiple concentration under reduced pressure becomes unnecessary, thus the process is no longer tedious and time consuming. The crude product of fasudil hydrochloride adopts methanol as the recrystallization solvent, so that the preparation steps are reduced, the energy can be saved and the cost can be reduced. The undried 5-isoquinoline sulfonyl chloride hydrochloride that is subjected to a Karl Fischer moisture test and purified solved in water and dichloromethane, and sodium bicarbonate is added for neutralization followed by layering. The split dichloromethane solution of 5-isoquinoline sulfonyl chloride and the dichloromethane solution of homopiperazine are condensed, and water is added for washing. When the dichloromethane layer isseparated and dried, dry hydrogen chloride gas is introduced into the dichloromethane, so that the fasudil hydrochloride crude product can be obtained. The crude product is then recrystallized in methanol, thus obtaining a competitive product which is white or almost white crystalline powder. The yield of 5-isoquinoline sulfonic acid as the competitive product is calculated as 66.3%.

This invention relates to alcaine telfairic injection liquid quality control method, which comprises the following steps: property observing, content identifying; content testing and testing component volume.

The invention provides a method for determination of the content of a related impurity (5-methyl isoquinolinesulfonic acid) of fasudil hydrochloride. The method is characterized in that a reversed-phase high-performance liquid chromatographic peak area normalization method is adopted for quantitative analysis; for the chromatographic conditions, the chromatographic column is an ACCHROM XAmide column; the flow speed is 0.9-1.1ml/min; the detection wavelength is 238nm; the column temperature is 28-32 DEG C; the sample injection amount is 20mu l; a mobile phase A is 0.05mol/l ammonium dihydrogenphosphate aqueous solution; a mobile phase B is methanol; A:B is equal to (91-94): (6-9) (V:V). The method provided by the invention is convenient to control the product quality in the processes of production and quality control, and has the advantages of low cost, simpleness, easy implementation, high accuracy and precision, good stability and reproducibility and high sensitivity.

The invention relates to a freeze dried powder injection of Fasudil hydrochloride and its preparation, which comprises (by weight percent) Fasudil hydrochloride 1-5%, excipient 4-40%. The excipient can be mannitol, lactose, sodium chloride, glucose, glycine, and / or other pharmaceutically acceptable excipient.

The invention relates to the application of Fasudil in preparing medicaments for treating glaucoma through ophthalmic drug delivery, which belongs to the technical field of medicines. The Fasudil comprises pharmaceutically acceptable saline forms such as hydrochloride, nitrate, sulfate, phosphate, hydrobromide, mesylate, citrate and the like as well as pharmaceutically acceptable forms such as crystallization form, hydrate form and the like. The medicament is a pharmaceutic preparation composition prepared by using the Fasudil as an active pharmaceutical ingredient.

The invention discloses a quality control method for fasudil hydrochloride. The quality control method comprises the following steps: observation of properties; identification of contents; inspection of the contents; and determination of the contents of components included in the contents; wherein inspection of the contents comprises determination of the contents of related substances and determination of the content of homopiperazine. In the process of a synthesis reaction, fasudil hydrochloride is prone to generation of degradation impurities and to a side reaction for production of a dimer impurity and a starting reaction material homopiperazine is hard to thoroughly remove, so purity and security of fasudil hydrochloride are influenced; thus, the contents of impurities in fasudil hydrochloride should be determined in time in the production process so as to control product quality in the production process. The method provided by the invention has additional steps of determination of dimer content and determination of homopiperazine content on the basis of conventional control method, so the quality control method further improves the quality of fasudil hydrochloride, perfects current industrial standards, has the advantages of simplicity, easy practicability and high precision and accuracy and is of great significance to improvement of product quality.

The invention belongs to the technical field of drug preparation, and particularly relates to fasudil hydrochloride injection and a preparing method thereof. The fasudil hydrochloride injection is prepared from, by mass, 30 parts of fasudil hydrochloride, 5-15 parts of sodium citrate, 0.1-0.4 part of ethylenediamine tetraacetic acid disodium, and 1500-2500 parts of injection water. Compared with the prior art, the fasudil hydrochloride injection has the advantages that the ph value, content and related material results of every embodiment are still qualified after the fasudil hydrochloride injection is exposed to high temperature, illumination and acceleration for 6 months and 24 months, and therefore the quality of the whole product is stable; furthermore, the preparing process is simple, cost is quite low, and industrialized production is facilitated.

This invention provides a therapeutic target for pancreatic cancer. The invention further provides methods of screening of new therapeutic agents using the target. The invention also provides a pharmaceutical composition comprising fasudil or derivatives thereof for pancreatic cancer treatment, and a kit comprising such a pharmaceutical composition.

The invention discloses a method for detecting homopiperazine in fasudil hydrochloride, which uses gas chromatography to qualitatively or quantitatively detect the homopiperazine in the fasudil hydrochloride. The diluent used in the sampling detection solution in the gas chromatography comprises DBU and organic solvent. According to the method for detecting the homopiperazine in the fasudil hydrochloride, the homopiperazine in the fasudil hydrochloride can be detected effectively and veritably, and the quality and the safety of fasudil hydrochloride are guaranteed.

The invention discloses a stable large-capacity fasudil hydrochloride injection, which comprises 30-120mg of fasudil hydrochloride and 5%-20% of glucose, or comprises 30-120mg of fasudil hydrochloride, 5%-10% of glucose and 0.9% of sodium chloride, wherein the pH (potential of hydrogen) value of the solution is 3.5-4.0, and the pH value is regulated through hydrochloric acid or NaOH.

The invention belongs to the pharmaceutical field and relates to a compound preparation of Fasudil and Beraprost as well as a preparation method and application thereof to treating pulmonary hypertension. The compound preparation in the invention comprises Fasudil, Beraprost and auxiliary materials chosen from auxiliary materials acceptable in pharmacy, such as a disintegrating agent, an adhesive, an excipient, diluents, a lubricant, framework materials used for controlling the release of active ingredients in slow and controlled release agents, and the like. Proper carriers are chosen according to different types of drugs.