195 results about "Sildenafil" patented technology

The present invention is directed to nanoparticulate compositions comprising sildenafil free base. The sildenafil free base particles of the composition have an effective average particle size of less than about 2000 nm.

A method for treating Tourette's Syndrome and other central nervous system disorders. An effective amount of sildenafil or a pharmaceutically acceptable salt thereof is orally administered to patients suffering from Tourette's Syndrome and other central nervous system disorders to diminish the symptoms associated with such a disorder.

Multiple agent therapy for treatment of sexual dysfunction, including male erectile dysfunction, with sequential administration a type V phosphodiesterase inhibitor (PDE-5), such as sildenafil, preferably wherein the PDE-5 inhibitor is administered by oral dose means, and a melanocortin 3 and / or 4 receptor agonist, such as Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH (PT-141) preferably wherein the PT-141 is formulated for and administered by intranasal means, and further preferably wherein the PDE-5 inhibitor is administered prior to PT-141.

Sildenafil, a known pharmaceutical chemical useful in treatment of male sexual dysfunction, is prepared by processes in which the final chemical intermediate is of significantly lower basicity than sildenafil itself, so that sildenafil can be extracted in substantially pure form from the organic reaction mixture in which it is made by adding an aqueous medium of appropriately chosen acidic pH and causing phase shift of the sildenafil to occur selectively into the aqueous phase.

The invention belongs to the technical field of pharmacy, in particular to an oral disintegrative tablet for treating male erection dysfunction by using sildenafil citrate as an active component and apreparation method thereof. The oral disintegrative tablet of sildenafil citrate comprises the following components in parts by weight: 2.5-10 sildenafil citrate, 10-20 diluent, 0.5-1 disintegrant, 0.1-0.2 lubricant, 0.05-0.1 taste modifier and 0.01-0.02 bonder (accounted by povidone K30), wherein the diluent is a compound jointly formed by chitosan and one or two of lactose and mannitol. The oral disintegrative tablet remarkably improves the humidity resistance and is beneficial to improving the stability of the preparation and ensuring the quality in the production and storage processes.

Provided are processes for the preparation of sildenafil base and the citrate salt sildenafil. Also provided are sildenafil citrate water adduct and a method of preparing pharmaceutical compositions comprising combining the sildenafil citrate and / or sildenafil citrate water adduct with at least one pharmaceutically-acceptable excipient.

A class of cGMP PDE inhibitors, including sidenafil and pharmaceutically acceptable salts thereof, which can be used to treat sexual dysfunction in male and female animals, especially humans, with a spinal cord injury. The invention can be used to treat sexual dysfunction in male animals that exhibit essentially no residual penile function.

The present disclosure is directed to chemically-stable and pharmaceutically-acceptable sildenafil oral spray formulations for the treatment of male erectile dysfunction, wherein the oral spray formulation has a pH of about 1.5 to less than 3.0. The present disclosure is also directed to methods for treating male erectile dysfunction.

Modified release formulations comprising at least one of modafinil and sildenafil, and combinations thereof, and a time-controlled delivery system coating.

The invention discloses a technique for artificially synthesizing antigen of Sildenafil and derivative thereof, which comprises the following steps: generating water-soluble EDC, balancing EDC, NHS, DMF and hapten compound to room temperature, weighting EDC, NHS and hapten compound, adding the weighted sample into a clean round bottomed flask, adding DMF, dissolving and marking the generated solution as No.2 reaction solution, dissolving carrier protein in boric acid buffer solution with a ratio of 1:0.15 to 0.2 in another clean container, turning into another clean round bottomed flask and marking the solution as No.3 reaction solution, adding the No.2 reaction solution into the No.3 reaction solution, dialyzing the samples after finishing reaction, cooling and drying the samples into white flocculent products, namely the artificially synthesized antigen.

The invention provides a synthesis method of a sildenafil analog. The chemical name of the sildenafil analog is 5-[2-ethoxy-5-(4-methylpiperazine-1-yl-thiocarbonyl)]phenyl-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazol[4,3d]pyrimidine-7-thioketone; the sildenafil analog is prepared from 5-(2-ethoxy)phenyl-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazol[4,3-d]pyrimidine-7-one as a raw material through four steps of chemical reactions. The synthesis method of the sildenafil analog is simple in synthesis step operations, economic and environmentally friendly; the yield of each step is above 75% and the total yield is relatively high; the synthesis method is suitable for industrial production.

The invention discloses a method to test Sildenafil citrate and its ramifications. It contains steps: (1) Color reaction. Make color reaction of test sample with bismuth potassium iodide, silico-tungstic acid and Hager's reagent to observe result. (2) Result estimation. If above three color reactions appear deposit, there are Sildenafil citrate and its ramifications in test samples. If just one, two or none color reaction appear deposit, there is no Sildenafil citrate and its ramifications in test samples. The method has merits of quick, simple, strong property, high accuracy, extensive application and testing range.

The invention discloses a medicinal composition containing sildenafil citrate and PD-1 type pregelatinized starch and a preparation method thereof. The medicinal preparation prepared from the medicinal composition containing the sildenafil citrate and the PD-1 type pregelatinized starch and the preparation method provided by the invention can be completely disintegrated in water at a degree of 37 DEG C within 15 to 30 seconds, and can pass through a screen in a size of 600 to 710 mu m.

The invention relates to the technical field of medicine, in particular to a quinazolinone derivative, a preparation method and application thereof. The invention discloses quinazolinone compounds as structural general formula (I) or pharmaceutically acceptable salt thereof. Most of the compounds have stronger PDE5 inhibition activity than that of Sildenafil, and have higher selectivity than thatof PDE 6 distributed on a retina. Therefore, the compounds are expected to show better clinical safety and effectiveness, and have wide clinical application prospect.

The invention provides a stable sildenafil citrate tablet. The sildenafil citrate tablet is prepared from the components in percent by weight: 10-50 percent of sildenafil citrate, 0.01-0.03 percent of antioxidant, 0.3-1.0 percent of acidifying agent, 70-90 percent of filler, 5-10 percent of disintegrant, 0.5-2.5 percent of adhesive, 0.5-1.0 percent of lubricant and 0.5-1.0 percent of flow aid. The invention also provides a method of preparing the tablet. With the adoption of the method, by strictly controlling the moisture of a final finished product, the dosages of the antioxidant and the acidifying agent in the components are remarkably reduced, the product stability is better, and the safety is higher.

A method is provided for the prevention of ischemia / reperfusion injury, for example, in patients undergoing heart surgery, and involves the administration of a phosphodiesterase-5 (PDE-5) inhibitor such as sildenafil. The method may also be used during or after a heart attack to prevent or lessen ischemic heart damage.

The invention discloses a sildenafil citrate sublingual tablet and a preparation method thereof. The sildenafil citrate sublingual tablet is prepared from 1 part by weight of sildenafil citrate and 4 to 8 parts by weight of pharmaceutical adjuvant , wherein the pharmaceutical adjuvant comprises 2 to 4 percent of disintegrant, 94 to 96 percent of diluter, 0.5 to 1.2 percent of lubricator, 0.3 to 1 percent of corrective and 0.1 to 0.2 percent of binder, which are based on the total weight of the pharmaceutical adjuvant. Test results show that the prepared sublingual tablet has shorter disintegration time, higher dissolving speed in vitro and higher body bioavailability than the conventional tablets.

Provided is a fast dissolving film composition comprising a medically active component as an active ingredient, in which the bitter taste of the active ingredient is masked and the fast dissolving film composition has a high content of 50% or higher. More particularly, provided is a pharmaceutical composition which comprises sildenafil or pharmaceutically acceptable salts thereof as an active ingredient, and which comprises a combination of a specific bitter taste masking agent to achieve masking of a bitter taste. Further, provided is a fast dissolving film composition which comprises a combination of a specific plasticizer to mask a bitter taste, and in which the physical properties of the high-content film are excellent.

An improved method of treating male erectile dysfunction by enteral administration of a combination of sildenafil citrate and papavarine hydrochloride. An alternate mode of treatment indicated for individuals with known vascular disease includes the contemporaneous administration of pentoxifylline. Further embodiments include administration of zinc monomethionine aspartate.

The invention provides a preparation method of a sildenafil artificial antigen and antibody, and relates to a preparation method of an artificial hapten, antigen and antibody maximizing the retention of a sildenafil structure. A sildenafil hapten prepared by a chemical synthesis method and a carrier KLH protein are connected and synthesized into an artificial antigen; and an antibody is prepared by the following steps: immunizing animals with the artificial antigen, taking blood, separating out antiserum and purifying. By designing and synthesizing the hapten and artificial antigen having a sildenafil structure, the invention highlights the molecule-specific antigenic determinant, overcomes difficulties in chemical synthesis, and produces the high-affinity antibody through animal immunization inducement. Compared with other similar methods, the invention has the characteristics of specificity, sensitivity, accuracy, high speed, convenience, low cost and the like; and the designed and synthesized hapten lays a foundation for the preparation of the antibody having favorable specificity.

The invention relates to the technical field of medicine analysis, and particularly provides a method of quickly analyzing illegal addition of a sildenafil analogue in yang-reinforcing health care products and a method of screening quick detection conditions for the sildenafil analogue. The method, through molecular docking, generally considers the intensity of interactions between a ligand (micro-molecules) and an acceptor (bio-macro-molecules), thereby finding compounds which have potential pharmacological activity and may be added as an illegal additive; furthermore, with combination of density functional theory, a theoretical Raman peak position is calculated, and theoretical shared peaks, which are obtained after data handling, are deeply developed; the results are used as an evidence for quickly determining illegally added sildenafil compounds in the health care products in on-site detection. The method is free of an artificially synthesized reference substance, has wide application range and low experiment cost, has simple operation, is quick, is suitable for on-site quick detection, and supplies stronger evidence to identification for the illegally added derivatives in the health care foods.

A sildenafil citrate taste-masking preparation and a preparing method thereof are disclosed. The sildenafil citrate taste-masking preparation at least comprises, based on the total weight of tablets, 15-30% of sildenafil citrate, 30-65% of hydroxypropyl cellulose and 15-20% of glyceryl behenate. The preparing method includes: mixing a formula dosage of the sildenafil citrate and a formula dosage of the hydroxypropyl cellulose to prepare melt dispersion, cutting the melt dispersion into particles, grinding the particles together with the glyceryl behenate, fully mixing with other auxiliary materials, and tabletting into tablets for oral administration.

The invention relates to cydiodine buccal tablets and a preparation method thereof. The cydiodine buccal tablets comprise the following components in percentage by mass: 0.1 to 6 percent of cydiodine,0.5 to 5 percent of sildenafil, 0 to 2 percent of lubricant, and 84.4 to 98.5 percent of filler. The filler is one or combination of the following components: mannitol, lactose, xylitol, sorbitol, erythritol, fructose, isomalt, dextrin, microcrystalline cellulose, starch, pregelatinized starch, sodium chloride. The invention also proposes a method for preparing the buccal tablets, which comprisesthe following steps: preparing cydiodine and sildenafil; weighing the components according to proportioning rate, granulating and mixing the components; determining the content of every component inmixed medicaments and calculating the weight difference of products; and tabletting the mixed medicament. In the process of treating oral or other diseases, the cydiodine buccal tablets prepared by the method have the advantages of reducing the amount of sucrose taken in by patients and reducing harm to the patients.

The invention belongs to the field of pharmaceutical preparation and especially relates to a sildenafil film composition. The invention provides a sildenafil rapidly disintegrating film composition with high drug loading capacity. The sildenafil rapidly disintegrating film composition with high drug loading capacity comprises (a) an active pharmaceutical ingredient which is sildenafil or pharmaceutically acceptable salt, and (b) a film forming material which accounts for 5-50%(w / w) of the composition and comprises gelatin which accounts for 10%-100% of the film forming material, (c) a plasticizer and (d) a taste regulator, wherein the biological availability of the active ingredient sildenafil in the film composition is about 60%. The composition disclosed by the invention takes gelatin as a main film forming material, and the obtained sildenafil film agent has the advantages of high drug loading capacity, good physical performance, perfect stability, nice taste and high biological availability, and is capable of rapidly disintegrating in oral cavity. The composition disclosed by the invention is used for treating male erectile dysfunction disease.

Provided are condoms and methods of making and using the same, the condoms having an elastomeric layer and a low melt wax bead which comprises an active ingredient mixed therein, wherein the bead is affixed on the interior surface of the elastomeric layer in the tip of the condom. Active ingredients can include spermicides such as nonoxynol-9 and vasodilators such as niacin, sildenafil citrate, and nitroglycerin and male desensitizing agents such as benzocaine. The bead can comprise a natural wax in combination with polyethylene glycol or it can be a polyethylene glycol-based wax. The exterior surface of the elastomeric layer is substantially free of the active ingredient.

The invention belongs to the technical field of immunodetection and discloses a sildenafil and its analogue immunodetection method. An artificial antigen is prepared from a mercapto-sildenafil hapten, and an antibody is prepared by the artificial antigen and is used for detecting sildenafil and its analogue. The method solves the problems of the existing sildenafil detection technology, has the largest sildenafil detection range of 0.024-1.21ng / mL, sensitivity of 0.17ng / mL, a detection limit of 0.008ng / mL and a recovery rate of 86.0-90.8%, has a fast detection rate, greatly shortens detection time, is not influenced by an operator proficiency degree, can be finished in about 80min, and has a low detection limit and high sensitivity.

The invention belongs to the technical field of medicinal chemistry, relates to a purification method for high-purity sildenafil freebases, particularly to a purification method for removing new impurities from the sildenafil freebases. The method includes adding 1-6 times (v / w) of organic solvents to sildenafil freebase (II) crude products, stirring fully, warming to 40-60DEG C, stirring for 1-6h with temperature preservation, then cooling to the room temperature, filtering and drying to obtain sildenafil freebase (II) fine products.

The invention provides a preparation method of sildenafil, which comprises the following steps: carrying out condensation reaction on initial raw materials 2-ethoxybenzoic acid and N-hydroxysuccinimide to obtain a compound II, and reacting with 1-methyl-3-propyl-4-aminopyrazolyl-5-formamide hydrochloride to obtain a compound III; after cyclizing and chlorinating the compound III, carrying out nucleophilic substitution reaction with alcohol to obtain a compound IV; reacting the compound IV with chlorosulfonic acid to obtain a compound V; reacting the compound V with N-methylpiperazine to obtain a compound VI; and carrying out hydrolysis reaction to obtain the target compound sildenafil. The invention has the advantages of accessible raw material, stable intermediate, high product yield, low production cost and mild reaction conditions, is simple to operate, and can easily control the reaction conditions of the intermediate; compared with the existing method, the invention has fewer side reactions, and enhances the yield and purity of the product; and the product contains fewer impurities, the purification treatment process is simple and convenient, and thus, the invention has high industrial applicability. The reaction route is as follows.