266 results about "Tadalafil" patented technology

A novel edible polymer based film dosage form manufactured using natural, synthetic, semisynthetic, pharmaceutically acceptable polymers addressing the issues of swallowing difficulties (Dysphagia and Dynaphagia), of tablet or capsule dosage forms and handling and storage difficulties associated with liquid dosage forms, that also includes materials such as emulsifying agents, suspending agents, buffering agents, effervescence agents, colorants, flavorants, sweeteners and specified amounts of bioactive agents, for erectile dysfunction. A flexible film dosage form containing sildenafil citrate, tadalafil or Vardenafil is presented. The film system is enabled to be used in various applications such as oral, mucosal and external environments.

The use of phosphodiesterase 5 (PDE5) inhibitors for treatment of schizophrenia is described. Suitable PDE5 inhibitors for use for treatment of schizophrenia include sildenafil, vardenafil, tadalafil, E-8010, zaprinast, and E-4021. In one embodiment, for example, a method is described for treating schizophrenia in a patient which comprises treating the patient with an effective amount of a PDE5 inhibitor, or a pharmaceutically acceptable salt, solvate, or composition thereof. The PDE5 inhibitor may be administered orally. The PDE5 inhibitor may also be administered together with one or more conventional antipsychotic medications such as risperidone, olanzapine, quetiapine, ziprasidone, aripiprazole, clozapine, haloperidol, and fluphenazine.

Improved pharmaceutical solid oral dosage forms for the buccal and/or sublingual delivery of Tadalafil. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced methods of preparation by the use improved solubilization systems which can maintain the Tadalafil in a buccal and/or sublingual oral dosage form or a polymeric film matrix that provides improved bioavailability and/or absorption of Tadalafil.

The invention discloses an oral quick-dissolving film preparation and a preparation method thereof. The oral quick-dissolving film comprises the following components in percentage by weight: 20 to 40 percent of medicinal active component, 40 to 75 percent of water-soluble film forming material, 10 to 25 percent of plasticizer, 0 to 25 percent of disintegrating agent, and 0.1 to 8 percent of water, wherein the medicinal active component is one of sildenafil, tadalafil, vardenafil or salts thereof. According to the oral quick-dissolving film preparation, the disintegration time limited of the film preparation can be remarkably accelerated, the problem that most oral solid preparations should be taken with water can be solved, medicine taking time cannot be delayed under a condition without water, and the taking compliance of a patient can be improved.

The invention relates to a tadalafil orally disintegrating tablet and a preparation method thereof. Aiming to improve the deficiency of existing tadalafil oral dosage forms, the invention provides the tadalafil orally disintegrating tablet which is convenient to take, is quick in absorption, takes effect quickly and has high bioavailability for doctors and patients to help the patients achieve requirements for natural and satisfactory sexual lives. The tadalafil orally disintegrating tablet takes tadalafil or medicinal salts thereof as an active ingredient, contains pharmaceutically acceptable auxiliary materials such as filling agents, disintegrating agents, flavouring agents and lubricating agents, and when being taken, dispenses with water, can be quickly disintegrated or dissolved in oral cavities only in a few seconds and is ingested along with saliva.

The invention relates to a preparation method of tadalafil. A product is obtained through condensation and cyclization, chloromethylation and aminolysis cyclization reaction based on D-tryptophan methyl ester hydrochloride and heliotropin as starting preparation materials. The simple preparation process is characterized in that condensation and cyclization are used for solving an isomer problem caused by Pictet-Spengler reaction by using isopropanol or nitromethane as a solvent; the yield of ethyl acetate in the aminolysis cyclization reaction is obviously improved; the aminolysis cyclization route includes three preparation steps, wherein the reaction yield of each step is high, the relevant impurities are easy to separate, the reaction conditions are simple, the production period is shorter, and toxic and highly corrosive reagents are not used, and therefore, the simple preparation process is safe and environment-friendly and easy to industrially produce, so that the high-purity qualified products are obtained.

Improved delivery systems and delivery methods for supporting and promoting healthy sexual function, for preventing sexual dysfunction, or for treatment of sexual dysfunction. A compositions including one or more cGMP-specific PDE5 inhibitors and/or dopaminergic agonists is administered in the form of a breath-care strip, mint or lozenge, or a food or beverage product. The cGMP-specific PDE5 inhibitor comprises an ingredient selected from the group consisting of sophoflavescenol, vardenafil, tadalafil, and sildenafil. The dopaminergic agonist comprises apomorphine. Vitex agnus-castus extract, and one or more of lipoic acid, L-Arginine, folic acid, trimethylglycine, policosanol, carnitine, biotin, and acetyl L-Carnitine may also be included in the delivery vehicle.

The invention relates to an oral medicinal preparation of tadalafil and application of the preparation in treatment of male erectile dysfunction. The preparation is characterized in that the main medicne is tadalafil or salt thereof, and the particular formulation can be orally disintegrating tablets, chewable tablets, oral membranes and other preparations capable of being quickly released in the oral cavity; tadalafil is an insoluble medicament, and is low in bioavailability, so that the administrated infective dose is large, multiple adverse responses can be generated, and visual impairment or loss can be caused due to unreasonable administration. Regarding the researches of tadalafil medicinal preparation for improving medicament bioavailability and reducing occurrence of adverse responses, the wide clinical application of tadalafil in treatment of male erectile dysfunction is particularly important. Aiming at the fact that the tadalafil medicinal preparation brings great favor to broad ED patients in improvement of the compliance when the tadalafil medicinal preparation is taken by a patient, particularly in administration in an environment without water and in a non-swallow mode. The oral medicinal preparation is prepared through massive studies based on patients.

A method of sexual enhancement in women includes the steps of identifying a woman requesting sexual enhancement, assuring that the woman's blood includes estradiol within a first predetermined range and testosterone within a second predetermined range, and thereafter administrating a drug selected from the group consisting of vardenafil hydrochloride and tadalafil prior to sexual activity. The selected drug may be loaded into a starch strip which is then applied to the woman's tongue. Sexual enhancement in women can also be achieved by transdermal or subcutaneous application of the steroid hormone DHEA.

Pharmaceutical dosage forms comprising tadalafil are described. Preferred dosage forms are bioequivalent to Cialis® notwithstanding a large particle size.

The invention discloses a method to detect Tadalafil and its derivative. It contains steps: (1) Color reaction. Make color reaction by adding concentrated sulfuric acid. (2) Result estimation. If color reaction presents blue violet, there are Tadalafil and its derivative in test samples. The method has merits of quick, simple, high sensitivity and strong property etc.

The present invention relates to methods of treating multidrug resistance in cancerous cells with phosphodiesterase (PDE) inhibitors, e.g., PDE5 inhibitors. More specifically, the invention relates to methods of treating multidrug resistance that arises, e.g., during administration of chemotherapeutic/antineoplastic (anticancer) agents for treatment of cancer, with a PDE5 inhibitor (e.g., sildenafil, vardenafil, and tadalafil). The invention also relates to methods of treating cancer, e.g., multidrug resistant cancer, using a PDE5 inhibitor in combination with an antineoplastic therapeutic agent. Further, the invention relates to pharmaceutical compositions for treating multidrug resistant cancers comprising a PDE5 inhibitor, or a combination of a PDE5 inhibitor and an antineoplastic agent.

The present invention provides tadalafil of high purity and processes of making such tadalafil by cyclization of TDCl in a solution.

The invention provides a method for refining tadalafil. The method comprises the following steps: 1) dispersing a tadalafil crude product into a mixed solvent of methanol and acetic acid, heating the material to perform dissolved clarification on the crude product; 2) steaming the material to remove a part of the solvent, gradually precipitating crystals; 3) slowly cooling the material, continuously crystallizing the product; and 3) filtering the material, washing the material, and drying the material to obtain the tadalafil crystal form A. Compared with a direct cooling crystallization method, the product yield is obviously increased, production power is increased, recovery and utilization of the mixed solvent are realized, and the method has obvious economic value and environmental protection value.

The invention discloses a method for preparing Tadalafil crystal form A. The method is characterized in that the crystallization solvent is a binary mixed solvent of a C1-C4 alcohol and acetic acid or a ternary mixed solvent of a C1-C4 alcohol, acetic acid and water. The method has the characteristics that: a mixed solvent system is used, thus the dosage of the crystallization solvent can be greatly reduced, the drying process can be simplified and the corrosion of acidic materials to the equipment can be reduced.

This invention relates to compositions, methods and kits for enhancing the permeability of the blood-brain barrier. Particularly, compositions comprising 5-phosphodiesterase inhibitors, such as sildenafil, vardenafil, or tadalafil, when administered to a mammal, will selectively enhance the permeability of the blood-brain barrier in abnormal brain tissue. This selective enhancement allows for selective delivery of therapeutic agents to treat the abnormal brain tissue; for example, a brain tumor.

The present invention provides particulate tadalafil having a particle size of about 200 to about 600 microns and a process for controlling the particle size of tadalafil.