69 results about "Probucol" patented technology

Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the prevention of thrombosis. The drugs, agents, and/or compounds may also be utilized to treat specific disorders, including vulnerable plaque. Therapeutic agents may also be delivered to the region of a disease site. In regional delivery, liquid formulations may be desirable to increase the efficacy and deliverability of the particular drug. Also, the devices may be modified to promote endothelialization. Various materials and coating methodologies may be utilized to maintain the agents or compounds on the medical device until delivered and positioned. In addition, the devices utilized to deliver the implantable medical devices may be modified to reduce the potential for damaging the implantable medical device during deployment. Medical devices include stents, grafts, anastomotic devices, perivascular wraps, sutures and staples. In addition, various polymer combinations may be utilized to control the elution rates of the therapeutic drugs, agents and/or compounds from the implantable medical devices.

It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

The invention belongs to the technical field of medicine, and in particular relates to probucol solid dispersion prepared by a solvent method. In the total charging amount, probucol accounts for 5 to 20 percent, PVP K30 accounts for 56 to 88.5 percent, tween-80 accounts for 3 to 15 percent, lauryl sodium sulfate accounts for 0.5 to 1 percent, and polyoxyethylene 40 monostearate accounts for 3 to 8 percent. The solid dispersion, 0.15 to 3 percent of superfine silica powder and 0.3 to 0.9 percent of magnesium stearate are mixed fully and evenly, and are subjected to compressing dry granulation and coating. The dissolution of the solid dispersion in 20 months is over 90 percent, and the bioavailability thereof is 580 percent.

The invention relates to a nanometer medicinal elution apparatus in microcellular structure for storing and releasing multiple medicines and a preparation method thereof. The multiple medicines in the invention are selected from medicine therapeutic agents, carrier therapeutic genes and bioactive substances, wherein one or two of the medicine therapeutic agents is/are taxol and/or probucol. The preparation method of the medicinal elution apparatus in the invention mainly comprises the followings: 1) nanometer holes are prepared on the surface of the apparatus body; 2) multiple medicines are coated in the nanometer holes and on the surface of the apparatus body. The apparatus body in the invention does not contain polymers, thereby reducing the risk of long-term thrombus possibly caused by polymers; the nanometer holes on the surface of the apparatus body do not have any influence for mechanical property of the body, thereby being capable of efficiently controlling the releasing rate of medicines and obviously reducing the restenosis rate after surgical operations. The invention can be applied to various medicinal elution implanting apparatuses, particularly having good effects for curing vascular lesion and preventing blood vessel restenosis in vascular stents.

The invention discloses an officinal composition for lowering blood fat. Active ingredients are atorvastatin and probucol. The invention provides a better fat regulating drug for patients clinically suffering from severe lipid metabolism disorders and especially has favorable synergistic effect on patients at high liver function damaging risk level by drug combination; two kinds of drugs complement advantages so as to obviously lower the possibility of side effect occurrence because of increased amount of atorvastatin. The officinal composition for lowering blood fat is prepared from active ingredients and pharmaceutically acceptable supplementary materials, but is not limited in preparations, such as tablets, dispersible tablets, sustained release tablets and the like.

Organic amine salts of compounds of the formula: and their pharmaceutically acceptable salts, and uses in medical therapy are provided.

The invention provides a biodegradable rapamycin-probucol composite medicine coated metal stent, which comprises a metal stent, active ingredients which coat on the surface of the metal stent, and a slow release vector, wherein the active ingredients are rapamycin and probucol; and the slow release vector is in vivo degradable fatty cluster polymers. The coated metal stent not only maintains the advantage of preventing restenosis of the medicine coated stent but also solves the problem of late stent thrombus along with complete release of a slow release coating; and the probucol in the coating has the function of inhibiting local inflammatory reaction caused by the vector and a medicine. The coated metal stent is mainly used for interventional therapy of coronary heart disease, prevention of restenosis, and reduction of formation of late thrombus after the stent is implanted.

A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula

where R₁, R₂, R₃, R₄, R₅, R₆, Z and Z′ are defined herein.

It has been discovered that certain selected probucol monoesters, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

The invention relates to a medicine composition for treating angiocardiopathy. The composition comprises atorvastatin calcium and probucol with therapy dose and pharmaceutically acceptable carriers or excipients.

The invention provides a probucol orally administered nanometer solid preparation, which comprises, by weight, 1 part of probucol, 0.01-0.1 part of additive and 0.05-0.4 part of auxiliary materials. The grain size of the probucol ranges from 10nm to 200nm. The invention further provides a preparation method for the probucol orally administered nanometer solid preparation. The preparation method includes that the probucol and water liquor with 5% of additive are prepared into nanometer suspension with the grain size ranging from 100nm to 600nm by a wet grinding method; the nanometer suspension is homogenized into nanometer grains with the grain sizes ranging from 10nm to 200nm by a high-pressure homogenizing machine; and the nanometer suspension which is homogenized is solidified and is added with the auxiliary materials to be prepared into the orally administered nanometer solid preparation. Compared with a common probucol tablet, the preparation has the advantages that dissolution in vitro of the preparation is increased by 20-30 times, and bioavailability after oral administration is improved by 10-20 times. In addition, the drug loading rate of the preparation is high, and the preparation can meet the requirements of tablet weight clinically needed by high-dose probucol administration. Besides, the preparation is stable, and the dissolution of the preparation can be kept unchanged within two years.

The invention discloses probucol and lovastatin compound composite and a preparation method. The compound composite comprises, by weight, 15-20 parts of probucol, 1-3 parts of lovastatin, 20-30 parts of diluent, 1-3 parts of surfactant, 20-30 parts of disintegrant and 1-3 parts of lubricant. The preparation method includes material preparation, granulation, granule preparation and tableting. Probucol and lovastatin are combined organically, consumption of pharmaceutic adjuvants is reduced to the uttermost degree, and the compound composite can be used for treating hyperlipidemia. The compound composite is high in effective drug proportion, convenient to take, capable of improving compliance of patients and beneficial to reduction of medicine price and industrial production.

A method of treating skin changes and conditions in human skin including applying a topical preparation that includes an active agent including probucol, a derivative of probucol or a combination of probucol and a derivative of probucol.

A process is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds. The process generally includes reacting a probucol compound with a solution of alkali metal oxide, reacting the salt mixture with a solution of an alkyl or aryl halo-substituted carboxylate, hydrolyzing the resulting compound; and separating a crystalline, polymorphic form of the compound from the hydrolyzing mixture. Polymorphic forms of the probucol compounds are also described.

A chitosan nanoparticle able to sequentially release more medicines is proportionally prepared from chitosan, hydrophilic medicine (aspirin), lipophilic medicine (probucol), tween-80 and sodium tripolyphosphate by ion exchange method and microemulsifying method. It features that the aspirin is first released for 24 hr and the probucol is then released for 5 days.

The invention discloses a solid dispersible tab used for curing angiocardiopathy, which contains the constituents with the following part by weight: 250 to 300 shares of probucol mono-succinate, 300 to 800 shares of PVPK30, 60 to 120 shares of Tween 80 and 5000 to 16000 shares of magnesium stearate. The invention also discloses a preparation method of the solid dispersible tab: the probucol mono-succinate is prepared into the solid dispersion tab by adopting the solid dispersing technology, thereby leading the quality of the medicine to be guaranteed and having higher bioavailability. Meanwhile, the material quantity is saved, and the economic burden of the patient is relieved.

The invention relates to a medicament composition for treating cardiovascular diseases. The composition contains Fenofibrate, Probucol and pharmaceutically acceptable carrier or excipient with effective dose for treating.

The invention relates to a synthesis method of probucol. The method comprises the following steps of: reacting 2,6-di-tert-butyl-4-mercaptophenol used as a starting material with allylene through pressurization under the catalysis of alkaline conditions, and then reacting the obtained olefin intermediate with 2,6-di-tert-butyl-4-mercaptophenol under the catalysis of a strong acid so as to obtain a product probucol. The method disclosed by the invention is simple in operation, high in product yield and good in purity.

The invention belongs to the technical field of drug analysis. The invention discloses a high performance liquid chromatography separation and determination method for impurities in a probucol bulk drug and a preparation and application. The method is used for simultaneously separating impurities (2,2',6,6'-tetratert-butyldibenzoquinone), impurities B (4,4'-dithiobis(2,6-di-tert-butylphenol) and impurities C ((4-[(3,5-di-tert-butyl-2-hydroxyphenylthio)isopropyl mercaptan]-2,6-di-tert-butylphenol). According to the method, octadecylsilane chemically bonded silica is adopted as a chromatographiccolumn of a filler to prepare a reference substance solution and a test solution, the reference substance solution and the test solution are injected into a liquid chromatograph, an organic phase anda buffer salt solution in a certain proportion are adopted as mobile phases, and bulk drugs in the bulk drugs and related preparations and probucol, impurities A, impurities B and impurities C in thepreparations can be ensured to be completely separated. The method is short in analysis time, provides an effective quality control method for research, development and production of probucol bulk drugs and related preparations, and has popularization value.

A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula

where R₁, R₂, R₃, R₄, R₅, R₆, Z and Z′ are defined herein.

The preparation process of micron and nanometer probucol supporting ethyl cellulose particle belongs to the field of controlled and slow releasing medicine preparation. The present invention adopts water solution of sodium dodecyl sulfate as the water phase and dichloromethane solution of ethyl cellulose and probucol as the oil phase, adds the oil phase into the water phase, emulsifies and eliminates dichloromethane to obtain micron and nanometer ethyl cellulose particle; and washes the particle with distilled water to neutrality and decompression dries at normal temperature for curing to obtain micron and nanometer probucol supporting ethyl cellulose particle. The present invention has simple operation, and the obtained micron and nanometer probucol supporting ethyl cellulose particle may reach nanometer level size.

The invention provides a porous composite medicine-loaded composition for improving oral absorption for probucol. The porous composite probucol medicine-loaded composition is stable in thermodynamics, capable of improving the stability of medicaments, stable in gastrointestinal tract environment and free of toxic and side effects, uniform in system dispersion, the solubility of the porous composite medicine-loaded composition in water can be improved by 3-12 times, and the bioavailability of the porous composite medicine-loaded composition can be improved by 2-45 times.

Provided is a highly absorbable drug composition including one or more water-soluble compound (A) selected from an enzyme-treated hesperidin, a stevia extract, or an enzyme-treated stevia and a poorly water-soluble drug (B) selected from flurbiprofen or probucol.