129 results about "Finasteride" patented technology

This invention provides methods of treating a mammalian subject in need of androgen therapy by orally administering to the subject testosterone, a testosterone ester, or a testosterone precursor in an oil vehicle and by administering to the subject a modulator such as finasteride or dutasteride which increases testosterone bioavailability in the subject.

This invention relates to pharmaceutical formulations of finasteride that include Gelucire®.

The invention discloses a synthesis method of finasteride, which comprises the following steps that: taking inexpensive luteosterone and the like as the raw materials to finally prepare finasteride through 6 steps of synthetic reaction, i.e. the synthesis of 3- carbonyl-4- androstene-17beta-carboxylic acid, the synthesis of N-tertiary-butyl-3- carbonyl-4- androstene-17beta-formamide, the synthesis of N-tertiary-butyl-5- carbonyl-17beta- carbamoyl-A-lost carbon-3,5-cracking- androstane-3-acid, the synthesis of N-tertiary-butyl-3-carbonyl-4- aza-5- androstene-17beta-formamide, the synthesis of N-tertiary-butyl-3- carbonyl-4- aza-5alpha- androstane-17beta- formamide, and the synthesis of finasteride. The synthesis process has the advantages of inexpensive and easily available raw materials and stable yield, is applicable to industrial production, and the product quality meets the pharmacopeia standards.

The invention relates to an injection slow-release micro ball of Finasteride and similar component, wherein said micro ball contains 5-80% Finasteride and biological degradable polymer at 95-20%. The production comprises emulsion disperse (oil/water or oil/oil method), liquid drying method, or atomization drying method. The inventive agent can prolong function time and improve drug utilization.

The present invention relates to a pharmaceutical composition for topical application for the treatment of alopecia, said composition comprising polymeric nanoparticles, preferably nanocapsules containing two active ingredients, finasteride and minoxidil, additives and a pharmaceutically acceptable carrier. The invention further includes a process for the preparation of polymeric nanoparticles, preferably nanocapsules of finasteride and minoxidil, a composition suitable for topical application for the treatment of alopecia, as well as the use of said nanocapsules for the preparation of a pharmaceutical composition.

The invention provides a new synthetic method of finasteride, belonging to the technical field of drug synthesis. The method comprises the following steps of: a. synthesis of dihydro finasteride iodo complex; and b. synthesis of finasteride; the synthesis method can transform dihydrotestosterone finasteride (F9) into the finasteride with a theoretic volume, avoids the use of harmful and toxic chemicals which are sensitive to the environment, has the advantages of total two-step reaction yield of more than 90%, purity of over 99.0%, good product yield, high purity, easy refining, simple operation, low cost, and less three-waste, conforms with the requirements of green chemical synthesis, and can achieve the requirements of high yield, high purity, green cleaning and industrial production of the finasteride.

The invention relates to a finasteride nano-liposome and a preparation method thereof. The finasteride nano-liposome comprises finasteride, phospholipids, a flexible material and a PBS solution, wherein the weight percentage of the finasteride accounting for the phospholipids is 2.5% to 10%, the weight percentage of the flexible material accounting for the phospholipids is 20% to 50%, and the weight percentage of the PBS solution accounting for the phospholipids is 2.5% to 10%. According to the finasteride nano-liposome, the disadvantage, such as poor percutaneous permeability, of the finasteride is improved, the phospholipids and the flexible material are taken as a carrier system, and the prepared finasteride nano-liposome is simple to operate and good in repeatability and prevents from using an organic solvent with large toxicity, drugs are delivered to skin deep layers by using high deformability and efficient permeability of the flexible nano-liposome, and a better therapeutic effect is exerted.

This invention discloses a synthesis technology of finasteride, it takes 3-oxo-4-androstene-17 beta-carboxylic acid methyle as raw material, and synthesizes finasteride through the following five steps, (a). hydrogen peroxide; (b). cyclization; (c). catalyzed hydrogenation reduction; (d). ester-amide condensation into amide; and (e). oxidizing to form double bond. Compare with the existing technology, this technology has short route, high efficiency, simple operation and low cost.

The invention relates to a non-finasteride oral preparation and preparation method, specifically which consists of main drug non-finasteride and medicinal findings. Its contents are oily liquid or semi-solid, and it can be made of soft capsules, liquid-filled capsules and oral emulsion. The important contribution of the invention is preparing the steroidal hormone compounds into liquid or semi-solid in agent preparation early period, avoiding occupational hazard caused by dust flying, protecting workers involving in manufacture;In addition, non-finasteride is the combination of lipophilic compounds, oily liquid or semi-solid drugs and supplies, it can increase the drug dissolution rate, improve bioavailability. The application of the invention can improve labor protection, and also can provide better curative effect in clinical application.

A method for treating hair loss caused by androgenic alopecia and/or male pattern baldness. The method, which not only slows hair loss but causes hair re-growth, includes approximately daily application to a subject's scalp of a novel composition comprising finasteride (Propecia® or Proscar®), dutasteride (Avodart®), and minoxidil (Rogaine®) as active ingredients in a hypoallergenic cream-based vehicle, preferably coupled with daily ingestion of 1 mg per day of finasteride (Propecia® or Proscar®), application to the scalp of 5% minoxidil (Rogaine®) foam approximately once per day, and use of a ketoconazole-containing shampoo (e.g., Nizoral®) approximately 2-3 times per week. The method described herein also resolves scalp dermatitis in atopic subjects suffering therefrom. A method for making the novel composition is also provided.

Processes for preparing polymorphic crystalline Form I and Form III of finasteride.

The invention discloses a finasteride capsule and a preparation method thereof, and belongs to the technical field of medicinal preparations. The content of the finasteride capsule is composed of finasteride and medicinal auxiliaries, wherein the medicinal auxiliaries comprise a filler, a disintegrating agent, a lubricant and a surfactant and does not contain liquid solvent, and the filler comprises pregelatinized starch PC-10. Based on the process of directly filling powder, each component of the medicinal auxiliaries is screened by a 80-mesh screen, while finasteride is screened by a 100-mesh screen; the filler in the medicinal auxiliaries is weighed in the ratio, is subjected to equivalent increasing mixing with finasteride, and is uniformly mixed with other medicinal auxiliary components to fill the capsule. Functional auxiliaries can be screened without liquid solvent by optimizing the formula and the process, the compound solubility can be improved to meet the requirements on dissolution rate and stability, and the quality in accordance with an original development preparation can be achieved, so that the product quality can be guaranteed, and the treatment effect of the finasteride capsule can be relatively effectively played.

The invention discloses an urtica open-loop lignan glycoside D serving as a 5alpha-reductase inhibitor, a preparation method thereof and use thereof. The urtica open-loop lignan glycoside D is prepared by using the underground part of urtica triangularis as a raw material, extracting the raw material with alcohol, mixing an alcohol extract with hot water to obtain a suspension, extracting the extract with petroleum ether, ethyl acetate and water-saturated n-butyl alcohol, separating the extract from a raffinate water layer with macroporous resin, eluting the extract and separating and purifying the extract by silica gel column chromatography. The urtica open-loop lignan glycoside D can obviously inhibit the generation of DHT and has the potential to be used to prevent and treat prostate diseases like finasteride which is a masculine medicament. The open-loop lignan glycoside raw material is pure natural vegetable roots and safe and readily available. The method is simple and easy to operate and avoids introducing toxic materials. The urtica open-loop lignan glycoside D is low in cost, has a remarkable effect in spite of a vegetable source and has a great significance for the researches on and development of anti-benign prostatic hyperplasia medicaments.

The invention belongs to the field of pharmaceutical preparations and discloses a finasteride lyotropic liquid crystal gel preparation precursor. The finasteride lyotropic liquid crystal gel preparation precursor comprises the following raw materials in percentage by mass: 45-80% of phospholipid, 10-50% of glyceride, 5-9% of a cosolvent and 0.1-6% of finasteride. The finasteride in the finasteridelyotropic liquid crystal gel preparation precursor disclosed by the invention is uniformly dispersed; the precursor is low in viscosity and can be used for injection; after entering a human body, theprecursor can act with water to form the lyotropic liquid crystal with an excellent drug sustained release effect; the biocompatibility is excellent, no systemic inflammatory response is caused, andtoxic and side effects of the medicine are avoided; the drug administration frequency can be decreased; the precursor is low in cost, simple in preparation method and capable of easily realizing industrialization; the precursor can be used for treating male hair loss and benign prostatic hyperplasia, so that an enlarged prostate is shrunk, and symptoms brought by urine flow and benign prostatic hyperplasia are improved.

The invention relates to compound tamsulosin and finasteride sustained release capsules and a preparation method thereof. The compound sustained release capsule is prepared by taking tamsulosin and finasteride as medical bioactive ingredients to prepare medicine-containing pellets, coating the medicine-containing pellets by coating materials to prepare sustained release pellets, and placing the sustained release pellets into hard capsule shells. The compound tamsulosin and finasteride sustained release capsules are used for treating benign prostatic hyperplasis (BPH), can be very slowly released to maintain stable plasma concentration and longer action time, and have the advantages of less toxic and side-effects and convenient application.

A composite medicine in the form of form of dispersing tablet, oral disintegrating tablet, capsule, liniment, ointment, etc contains phenandrostamine and additional cyclodextrin or its derivative for higher biologic utilization rate.

Disclosed herein are topical compositions of 5-α reductase inhibitors, such as dutasteride or finasteride, or a pharmaceutically acceptable salt, ester, or derivative thereof and the use of the compositions for the treatment of hair loss secondary to endocrine therapy in patients with breast cancer (Endocrine Therapy-Induced Alopecia or ETIA), androgenetic alopecia (AGA), alopecia areata, and hirsutism. The topical composition is advantageous over the existing oral compositions of 5-α reductase inhibitors because the topical composition is safer and more effective. The topical formulation may allow for a slow release of the active ingredient dutasteride, better penetration at the therapeutically effective amount of dutasteride with an improved safety profile because it does not need to travel through the bloodstream to be efficacious, thereby minimizing the risk of systemic side effects.

The invention relates to a preparation method of a finasteride dispersible tablet. The method comprises the following steps: (i), mixing finasteride, a flow aid and a surfactant to carry out micronization to form a micronized mixture; (ii), uniformly mixing the micronized mixture with a filler and an internally added disintegrating agent, adding a wetting agent for wetting, then, carrying out pelletizing, drying and straightening, adding an externally added disintegrating agent and a lubricating agent for uniformly mixing again, and finally tabletting to prepare the finasteride dispersible tablet. The preparation method is characterized in that in step (i), the grain size of the micronized mixture is less than 5 mu m. The invention further relates to a finasteride dispersible tablet obtained by the preparation method. The preparation process of the finasteride dispersible tablet disclosed by the invention is simple and stable; the obtained finasteride dispersible tablet is good in stability, high in dissolution rate, high in bioavailability and convenient to take, improves medicine-taking compliance of a patient, and is especially suitable for the old, the crowd with difficulty in taking medicine as well as the crowd who travel and are on a business strip.

The present invention relates to a process for producing 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones of formula 1, including Finasteride and Dutasteride.

The present invention relates to an improved process for the preparation of pure Finasteride of Formula I,

which comprises converting dihydrofinasteride to finasteride through novel protected dihydrofinasteride and protected finasteride intermediates.

The invention relates to finasteride-containing orally disintegrating tablets and a preparation method thereof. The orally disintegrating tablets are prepared by jointly grinding a main medicine and a filler; by the preparation process, the particle size of finasteride can be controlled in a certain range, and the finasteride and the filler are fully mixed, so that the bitter taste of the medicine can be effectively masked, and the dissolution rate of the medicine can be effectively improved; and the orally disintegrating tablets have sufficient hardness, can meet the requirements of production, packaging, storage and transportation, and can be used for treating benign prostatic hyperplasia.