24 results about "Tadalafil" patented technology

The disclosure relates to compositions comprising a phentermine and a unicyclic aminoketone and methods of use thereof. The methods of use include inducing weight loss or reducing weight gain in a human subject. The unicyclic aminoketone may be diethylpropion or bupropion. In some embodiments, the compositions further include tadalafil or naltrexone.

A phosphodiesterase type 5 inhibitor is used in the preparation of a medicament for resisting fibrotic diseases. Experiments in animal models of ischemia-reperfusion (UIRI)-induced renal fibrosis, unilateral ureteral obstruction (UUO)-caused kidney fibrosis and idiopathic pulmonary fibrosis show that a PDE5 inhibitor such as tadalafil, sildenafil and vardenafil can significantly inhibit the expression of multiple fibrosis iconic proteins such as fibronectin, collagen I, renal injury molecule-1, and α-skeletal muscle actin in UIRI and UUO renal fibrosis lesions, improves glomerulopathy, degree of renal tubular distension, renal interstitial collagen fiber deposition and inflammatory cell infiltration, reduces the fibrotic area within the lesion, and significantly inhibits the progression of renal fibrosis; and the PDE5 inhibitor can significantly improve smooth muscle proliferation and inflammatory cell infiltration in bronchioles and pulmonary arterioles of idiopathic pulmonary fibrosis lesion, improve damage condition of alveolar tissue, and significantly inhibit the progression of pulmonary fibrosis.

The present invention relates to a donepezil and tadalafil combination therapy for the prevention, treatment or amelioration of Alzheimer's disease or cognitive dysfunction. The combined administration of donepezil and tadalafil according to the present invention has an improvement effect on Alzheimer's disease or cognitive impairment superior to that of the individual administration of donepezil, and thus can be effectively used as a therapeutic or complexing agent or the like for Alzheimer's disease or cognitive impairment.

There is provided a pharmaceutical composition comprising, as active ingredients: 5 mg of tadalafil or a pharmaceutically acceptable salt thereof; and 0.5 mg of dutasteride or a pharmaceutically acceptable salt thereof, wherein the dissolution rate of tadalafil is 60-75% after 5 minutes and 80% or more after 30 minutes under dissolution conditions of a paddle speed of 50 rpm in 500 mL of a dissolution solution having a pH of 1.2 and containing 0.25% of SLS, and the dissolution rate of dutasteride is 50% or more after 15 minutes and 85% or more after 30 minutes under dissolution conditions of a paddle speed of 50 rpm in 500 mL of a dissolution solution containing water and 0.1% of SLS.

Provided is a pharmaceutical composition comprising as active ingredients: 5 mg of tadalafil or a pharmaceutically acceptable salt thereof; and 0.5 mg of dutasteride or a pharmaceutically acceptable salt thereof, wherein the dissolution rate of tadalafil under the dissolution conditions of a paddle rate of 50 rpm in 500 mL of a dissolution solution having a pH of 1.2 and containing 0.25% of SLS is 60-75% after 5 minutes and 80% or more after 30 minutes, and the dissolution rate of dutasteride under the dissolution conditions of a paddle rate of 50 rpm in 500 mL of a dissolution solution containing water and 0.1% of SLS is 50% or more after 15 minutes and 85% or more after 30 minutes.

The present invention relates immediate-release tablet compositions comprising tadalafil, macitentan and one or more pharmaceutically acceptable excipients.

1. The name of the design product: packaging box (Lei Cao tadalafil tablets). 2. The use of the design product: for product packaging. 3. The design points of the design product: in the combination of shape and pattern. 4. The picture or photo that best indicates the design points: perspective drawing.

1. The name of the design product: packaging box (sildenafil citrate tablet packaging). 2. The use of the design product: packaging box for packaging medicines. 3. The design features of the design product: the combination of shape and pattern. 4. The picture or photo that best indicates the design features: perspective view.

The invention discloses N-nitroso tadalafil and a synthesis method and application thereof, and the synthesis method comprises the following steps: adding tadalafil into a reaction container, then adding a solvent for dissolving, balancing the system at (-20) DEG C to (-2) DEG C for 8-16 minutes, adding a nitrosation reagent for sealed reaction, after the reaction is finished, extracting, drying, concentrating, and carrying out column chromatography to obtain the N-nitroso tadalafil. The target product N-nitroso tadalafil is obtained. The N-nitroso tadalafil synthesis method is simple and convenient in process, the obtained product is high in purity, a reliable standard substance can be provided for tadalafil product quality research and analysis method development and verification, and the method has good popularization value.

The application relates to the technical field of organic synthesis, and discloses a method for preparing tadalafil or epi-tadalafil, which comprises the following steps: reacting N-(1,3-benzodioxol-5-methyl)-D-tryptophan methyl ester with Fomc-Ala-Cl to prepare compound IIa or compound IIb; and performing a deprotection / aminolysis reaction and a cyclization reaction on the compound IIa or the compound IIb in the presence of methylamine to prepare tadalafil or epi-tadalafil. Through the selection of a specific (Fomc-Ala-Cl) acylation reagent, the purity and / or yield of the compound IIa or the compound IIb are improved, so that the yield and / or purity of the tadalafil and / or epi-tadalafil are improved.

A method of treating premature ejaculation in men may include administering a therapeutically effective dosage of a formulation to a patient in need thereof. The formulation for treating male premature ejaculation may include a phosphodiesterase 5 inhibitor (PDE5i), such as Tadalafil; an alpha-1 adrenoreceptor (alpha-1a) selective antagonist, such as Silodosin; and a selective serotonin reuptake inhibitor (SSRI), such as Paroxetine.

Provided are stable, concentrated, and palatable solutions suitable for sublingual and / or transurethral administration containing tadalafil, with or without other active ingredients to address comorbidities, in a liquid vehicle or solvent selected from propylene carbonate, 2-pyrrolidone, dimethyl isosorbide, dimethyl acetamide, n-methyl-2-pyrrolidone, ethanol, water, oleic acid, and isopropyl myristate. The solutions have low irritancy for sublingual tissues and a-are compatible with commercial atomizers. The invention is further directed to methods of treating male erectile dysfunction and / or comorbidities by administering an effective amount of the pharmaceutical formulations comprising tadalafil, with or without other active ingredients, to a patient in need of such treatments.

The invention belongs to the technical field of medicines, and particularly relates to an external tadalafil nano preparation as well as a preparation method and application thereof. Compared with the prior art, the external tadalafil preparation provided by the invention avoids oral administration and local use, drug absorption is not influenced by factors such as pH in the digestive tract and food, the external tadalafil preparation directly acts on the penis to play a drug effect after external use, toxic and side effects on other tissues are reduced, the dosage of the external tadalafil preparation is obviously lower than that of a commercially available oral tadalafil drug, and the external tadalafil preparation has a good application prospect. Meanwhile, the tadalafil pharmaceutical composition is suitable for patients with liver / kidney function impairment, dysphagia and gastrointestinal tract fragility, so that the application scene of tadalafil is further expanded. The external tadalafil preparation provided by the invention can efficiently meet the requirements of erectile dysfunction (ED) patients in China and in the whole world, and has a wide market prospect.

1. The name of the design product: medicine packaging box (tadalafil tablets). 2. The use of the design product: for the packaging of medicines. 3. The design points of the design product: in the combination of shape and pattern. 4. The picture or photo that best indicates the design points: perspective view 3.

1. The name of the design product: package box (tadalafil tablet). 2. The use of the design product: for product packaging. 3. The design points of the design product: in the combination of shape and pattern. 4. The picture or photo that best indicates the design points: perspective view 1.

1. Name of the product in this design: Packaging Box (Tadalafil Tablets). 2. Purpose of this design: For packaging goods. 3. The key design features of this product are the combination of shape and pattern. 4. The image or photograph that best illustrates the design's key points: a 3D model.

The formulation of penile erecting gel comprises biosynthesized silver nanoparticles derived from Kaempferia parviflora extract containing 5,7-Dimethoxyflavone, in combination with sodium hyaluronate, isoprene glycol, phenoxyethanol, glycerin, propylene glycol, and ethylhexylglycerin. The manufacturing process involves blending the specified components, stirring to form a homogeneous gel, adding natural colorants and fragrances, and packaging in single-use plastic vials or aluminum foil sachets. This formulation represents an innovative application of nanotechnology in combination with Thai herbal medicine, enhancing localized vasodilation specifically at the penile region while minimizing systemic side effects such as headaches, nasal congestion, facial flushing, and blue-tinted vision associated with oral phosphodiesterase type 5 inhibitors (PDE5 inhibitors) like sildenafil (Viagra) or tadalafil (Cialis). Additionally, the gel exhibits antimicrobial and antioxidant properties.

The invention provides a compound preparation for treating erectile dysfunction and premature ejaculation and a preparation method thereof.The compound preparation contains a tadalafil inactive part and a fluoxetine hydrochloride active part, and the tadalafil inactive part contains a first stabilizer and a carrier; the tadalafil active part is used for preparing a solid dispersion from an active component tadalafil which is instable in absorption, and the particle size of the solid dispersion needs to be controlled; after the tadalafil active part is prepared into a solid dispersion, the solid dispersion, fluoxetine hydrochloride and auxiliary materials are prepared into a compound preparation, and the auxiliary materials comprise a filler, an adhesive, a disintegrating agent, a second stabilizer and a lubricant. The compound preparation provided by the invention can be used for treating erectile dysfunction and premature ejaculation at the same time. According to the compound preparation prepared by the preparation method provided by the invention, the problem of unstable absorption of tadalafil is reduced, the stability and dissolution rate of tadalafil are improved, the quality of the product is ensured, and the stability and safety of the product are improved.

1. Name of the product in this design: Packaging Box (Tadalafil Tablets). 2. Purpose of this design: For use in packaging boxes. 3. The key design features of this product are the combination of shape and pattern. 4. The image or photograph that best illustrates the design's key features: the front view.

The application belongs to the field of medicine, and specifically discloses application of a PDE5 inhibitor in preparation of a medicine for reducing uric acid and protecting kidneys. Research shows that, through concentration analogy, it is inferred that a PDE5 specific inhibitor is used for reducing uric acid and / or kidney protection, and therefore, the concentration of PDE5 inhibitors such as tadalafil is set to 0.001-0.1 mg / kg. It is found through animal experiments that tadalafil at the dose has a significant effect of reducing uric acid and a kidney protection function, and the dose applied to the human body (adults, body weight 60 kg) is 0.0075 mg-0.75 mg per day. The dose range is far lower than the recommended dosage of the medicine for treating ED, and is also far lower than the use dose of the existing public invention. The application increases the new indication range of the medicine for ED, and is expected to quickly enter clinical use.

The invention discloses a method for measuring the content of a novel epristeride compound sustained-release preparation, which adopts a high performance liquid chromatography to measure the content of epristeride and tadalafil compound, and comprises the following steps: firstly, preparing a reference solution and a test solution for later use; then setting high performance liquid detection conditions: adopting a chromatographic column taking octadecyl bonded silica gel as a filler, taking a 0.1% trifluoroacetic acid aqueous solution as a mobile phase A, taking acetonitrile-tetrahydrofuran (8: 2) as a mobile phase B, and carrying out isocratic elution for 22 minutes by taking the mobile phase A-the mobile phase B (55: 45); respectively sucking the test solution and the contrast solution, injecting the test solution and the contrast solution into a liquid chromatograph, and recording chromatograms. According to the method, the contents of epristeride and tadalafil in the compound sustained release preparation can be rapidly, effectively, accurately and reliably detected, and the medication safety of a patient is further improved by accurately determining the contents of main components.

Formulations of penile erection gel include biosynthetic silver nanoparticles derived from an extract of Kaempferia parviflora comprising 5, 7-dimethoxyflavone, as well as sodium hyaluronate, isoprene glycol, phenoxyethanol, glycerol, propylene glycol, and ethylhexylglycerol. The manufacturing process comprises the following steps: mixing the specified components, stirring to form uniform gel, adding the natural pigment and the essence, and filling into a disposable plastic small bottle or an aluminum foil small bag. The preparation is an innovative application of combining a nanotechnology and Thailand herbal medicines, can specifically enhance local vasodilatation in a penis area, and minimizes side effects of the whole body at the same time; such as headache, nasal obstruction, facial flushing, and hallucination of blue hue associated with oral administration of a type 5 phosphodiesterase inhibitor (PDE5 inhibitor), such as sildenafil (Viagra) or tadalafil (Heli). In addition, the gel also has antibacterial and antioxidant characteristics.

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of a tadalafil nitrosamine impurity. The invention discloses an efficient preparation method of two key nitrosamine impurity compounds of tadalafil. According to the method, nitrosation reaction is performed by adopting a specific reagent, directional synthesis of target impurities is realized under mild and controllable reaction conditions, and the method has the remarkable advantages of simplicity and convenience in operation, high product yield, high purity and the like. According to the method, the problem that related impurities are difficult to obtain is successfully solved, and a key material is provided for toxicological research or qualitative and quantitative research of the tadalafil nitrosamine impurities. The prepared impurity compound can be applied to nitrosamine genotoxic impurity detection and methodological development of tadalafil raw material medicines, preparations and intermediates thereof, and has important value for guaranteeing the safety and compliance of medicines.

The present invention relates immediate-release tablet compositions comprising tadalafil, macitentan and one or more pharmaceutically acceptable excipients.