49 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.

The invention provides a pharmaceutical composition and application thereof in preparation of a compound preparation, and belongs to the field of medicines. The pharmaceutical composition comprises a potassium ion channel opener, a 5 alpha-reductase inhibitor and a phosphodiesterase 5 inhibitor. The pharmaceutical composition can synergistically promote treatment of androgen dependent diseases or prevention of complications, and by taking the pharmaceutical composition of minoxidil, finasteride and tadalafil as an example, the effects in a benign prostatic hyperplasia rat model and an androgenic alopecia mouse model are verified, which indicates that the minoxidil, finasteride and tadalafil have a synergistic interaction effect, and the pharmaceutical composition can be used for treating the androgen dependent diseases or preventing the complications. Good clinical application prospects are realized.

The present invention relates an improved process for the preparation of piperonal (2), which is useful as an intermediate for the preparation of Tadalafil of formula (1).

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.

1. Name of the design product: Packaging box (Tadalafil tablets). 2. Use of the design product: For product packaging boxes. 3. Design key points of the design product: The combination of shape and pattern. 4. Picture or photograph that best shows the design key points: Front view.

The invention relates to the technical field of inspection and detection, in particular to a method for detecting tadalafil analogues. According to the method disclosed by the invention, the tadalafil impurity O, the EP impurity 1 and the impurity 82 in the sample are rapidly screened and quantitatively detected by adopting UPLC-MS / MS (Ultra Performance Liquid Chromatography-Mass Spectrometry). Extracting and purifying the sample by adopting a four-salt dispersion solid-phase extraction method; a C18 chromatographic column is adopted, 5-20 mM ammonium formate-acetonitrile is used as a mobile phase for gradient elution, and an MRM mode is combined for detection. A verification result of the method shows that the linear relation of target impurities is good, the quantitation limit of oral liquid is 0.02 mg / kg, the detection limit is as low as 0.007 mg / kg, the quantitation limit of a semi-solid preparation and a solid preparation is 0.05 mg / kg, the detection limit is as low as 0.02 mg / kg, and the average recovery rate reaches 80%-116% (RSDlt; 5.3%).

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 invention discloses a microneedle patch for treating male erectile dysfunction as well as preparation and application of the microneedle patch. The microneedle patch comprises a soluble matrix carrier and a needle-shaped array, wherein the needle-shaped array is formed by ED treatment medicines and is wrapped in the soluble matrix carrier; the matrix carrier comprises a polymer or polysaccharide with high mechanical strength, high biocompatibility and high water solubility; the ED treatment medicine is prepared from tadalafil, sildenafil and vardenafil; the micro-needle patch is used for rapidly delivering a drug for treating male erectile dysfunction in a percutaneous manner, and the effect of treating male erectile dysfunction is achieved.

The invention belongs to the technical field of analysis and detection, and discloses a method for detecting impurities in a tadalafil bulk drug and / or a tadalafil intermediate. The method for detecting the impurities in the tadalafil bulk drug and / or the tadalafil intermediate comprises the following steps: taking the tadalafil bulk drug and / or the tadalafil intermediate to be detected, and preparing a sample solution; taking an impurity standard substance, and preparing a standard sample solution; and detecting the impurities in the sample solution by adopting an ultra-high performance liquid chromatography-mass spectrometry method. According to the detection method, two N-nitroso genotoxic impurities and ten other process impurities in tadalafil raw materials and / or tadalafil intermediates can be determined at the same time, the specificity is high, the sensitivity is high, results of multiple different types of impurities can be obtained at the same time in one-time determination, the analysis efficiency is effectively improved, and the method is suitable for popularization and application. Powerful guarantee is provided for analyzing generation factors influencing impurities, effectively controlling medicine quality and guaranteeing medicine use safety.

The application discloses a preparation method of an amino tadalafil succinic acid derivative, and comprises the following steps: S1, synthesizing compound 1, i.e. 4-hydrazinyl-4-oxobutanoic acid, by reacting hydrazine with succinic anhydride; S2, synthesizing compound 3, i.e. the amino tadalafil succinic acid derivative, by carrying out a hydrazinolysis cyclization reaction of compound 2 with compound 1. In the amino tadalafil succinic acid derivative prepared by the application, the solubility of the amino tadalafil derivative is greatly improved by introducing succinic acid, and the drug administration mode is expanded; meanwhile, the existence of the carboxyl group as a reactive site can be used to derive other functional groups or to be connected with other active groups to form a synergistic active group, so that more possibilities are provided for preparing other related products based on the amino tadalafil derivative.

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

The invention discloses a tadalafil oral soluble film and a preparation method thereof. The oral soluble film comprises the following components in parts by weight on a dry basis; the pharmaceutical composition comprises 20-35 parts of a deep eutectic drug carrier, 50-65 parts of a film-forming matrix, 1-3 parts of a polymer anti-devitrification agent, 3-5 parts of a disintegration accelerator, 4-8 parts of a plasticizer and 3-6 parts of a flavoring agent. An amphiphilic natural deep eutectic solvent technology is adopted, choline chloride, dicarboxylic acid and a hydrophobic donor are used for constructing a ternary system according to a specific molar ratio, the hydrophobic donor remarkably improves the solubility of tadalafil through hydrophobic interaction, a strong hydrogen bond of the deep eutectic solvent inhibits drug crystallization, and a high-speed shearing micro-domain dispersion technology is combined, so that the solubility of tadalafil is remarkably improved. The high-efficiency solubilization of insoluble drugs, excellent anti-crystallization stability, rapid disintegration performance and good taste are realized, mucous membrane irritation of a traditional surfactant is avoided, and in-vivo absorption and patient compliance are expected to be improved.

1. Name of the product of this design: Pharmaceutical packaging box (Ailijin Tadalafil tablets). 2. Purpose of this design product: This design product is used for packaging of medicines. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The picture or photo that best illustrates the key points of the design: main view.

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.

The present disclosure relates to an injectable composition comprising tadalafil or a pharmaceutically acceptable salt thereof, a lipid, and a co-solvent. The injectable composition according to the present disclosure has the advantages of achieving a constant level of drug blood concentration over a long period of time, thereby reducing the number of drug administration, having excellent long-term safety due to absence of local tolerance and minimal side effects due to absence of initial rapid drug release, and providing high formulation stability.

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.

To provide an agent for the treatment of a patient suffering from pulmonary arterial hypertension (PAH).SOLUTION: An agent for initial triple combination therapy with macitentan, tadalafil, and selexipag for treating a patient having PAH, the agent containing macitentan, tadalafil, and selexipag, wherein the patient has, at initiation of the initial triple combination therapy, a resting mean pulmonary arterial pressure (mPAP) of about 25 mmHg or more, a mean pulmonary arterial wedge pressure (PAWP) of about 15 mmHg or less, and a pulmonary vascular resistance (PVR) of about 240 dyne sec / cm5 or more, and wherein the macitentan and the tadalafil are administered on day 1, and the selexipag is administered within 4 weeks.SELECTED DRAWING: None

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.

The invention belongs to the field of medicines, and particularly discloses application of a PDE5 inhibitor in preparation of medicines for reducing uric acid and protecting kidneys. The research shows that the uric acid reduction mouse experiment of EGCG and the in-vitro PDE5 inhibition activity speculate the use dosage of the PDE5 specific inhibitor for uric acid reduction and / or kidney protection through concentration analogy, so that the concentration of the PDE5 inhibitor such as tadalafil is set to be 0.001-0.1 mg / kg, and the use dosage of the PDE5 specific inhibitor for kidney protection is set to be 0.01-0.1 mg / kg. Animal experiments find that tadalafil under the dosage has a remarkable uric acid reducing effect and a remarkable kidney protection function, the dosage of tadalafil applied to human bodies (adults with the weight of 60 kg) is 0.0075 mg-0. 75 mg, and the dosage range is far lower than the recommended dosage of drugs for treating ED and far lower than the use dosage of existing inventions. According to the invention, a new indication range of the ED medicine is increased, and the ED medicine can be expected to be quickly used clinically.

1. Name of the Design Product: Packaging Box (Tadalafil Tablets). 2. Use of the Design Product: For the outer packaging box of drugs. 3. Design Key Points of the Design Product: Lies in the combination of shape, pattern and color. 4. Picture or Photograph that Best Illustrates the Design Key Points: Three-dimensional view. 5. The claimed design includes color.

The present application belongs to the technical field of traditional Chinese medicine, and particularly relates to a traditional Chinese medicine composition with the function of improving male sexual function, and a preparation method and application thereof. The traditional Chinese medicine composition is prepared from the following raw medicinal materials: centipede, angelica, fried white peony root, chuanxiong, cyperus rotundus, bupleurum, honey ephedra, notopterygium, baishu, cassia twig, cypress seed, epimedium, and western ginseng. The traditional Chinese medicine composition has the functions of soothing liver stagnation and promoting yang and erection. Experimental results show that the traditional Chinese medicine composition has a significant improvement effect on the erectile dysfunction of vascular ED model rats, and the levels of NO and ET-1 are also improved. The improvement effect of the traditional Chinese medicine composition on the above indexes is close to that of tadalafil, and is obviously superior to that of Yishenling granules which is a commonly used medicine for improving male sexual function. Therefore, the traditional Chinese medicine composition is particularly suitable for being prepared into a medicine for improving male sexual function, and has a wide clinical application prospect and commercial value.

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.

The present invention discloses a tadalafil tablet comprising a tadalafil liquid self-emulsifying drug delivery system, a solid adsorbent, and tablet excipients; the tadalafil liquid self-emulsifying drug delivery system and the solid adsorbent have a content ratio of 1:1-2; the tadalafil liquid self-emulsifying drug delivery system comprises a tadalafil API, an oil phase solvent, a nonionic surfactant, and a co-surfactant; the tadalafil content is 15-25%; the oil phase solvent content is 40-50%; the nonionic surfactant content is 30-40%; and the co-surfactant content is 5-15%. The tadalafil tablets prepared by the present invention have good uniformity, high solubility, and few impurities.

1. Name of the product of this design: Packaging box (tadalafil tablets). 2. Purpose of this product with design: This product with design is used to pack various items. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The picture or photo that best illustrates the design points: Stereoscopic drawing 1.

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.

The invention provides a tadalafil and fasudil pharmaceutical composition as well as a preparation method and application thereof, and belongs to the technical field of preparation of pharmaceutical preparations. Through research, the applicant finds that when the tadalafil and the fasudil are combined for treating the pulmonary arterial hypertension, a synergistic effect can be generated, and the improvement effect is superior to that of single use of one of the medicines. Moreover, the invention provides a preparation process of a tablet of the pharmaceutical composition, and the tablet comprises the following components: 1-5% of tadalafil, 10-25% of fasudil, 60-75% of a filler, 1-4% of an adhesive, 5-8% of a disintegrating agent, 0.5-2.0% of a lubricant and 0.1-0.5% of a solubilizer. According to the preparation process, auxiliary materials are cheap and easy to obtain, the process is simple, large-scale production is easy, the prepared pharmaceutical composition is an oral tablet, and the problems that the fasudil injection is inconvenient to take and the solution is easy to degrade under illumination are solved.