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.

Described are nanoparticulate compositions of finasteride, dutasteride, tamsulosin hydrochloride, or a combination thereof. The formulations exhibit unexpectedly prolonged release and can be maintained in a depot for release to a patient for a period of up to six months.

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.

Embodiments of the invention provide patches for the transdermal delivery of compositions to treat an individual suffering from hair loss. Many embodiments provide an iontophoretic patch for the transdermal delivery hair growth stimulating agents for the treatment of hair loss by stimulating the growth of new hair in areas of the scalp exhibiting hair loss. The patch comprises an electrode and a reservoir containing a composition comprising iron containing compound, such as a chelated iron compound for the delivery of the therapeutically effective amount of iron. The patch can be shaped to be placed and remain on the head. Various embodiments provide methods of using embodiments of the iontophoretic patch for delivering a hair growth stimulating agent such as a chelated iron compound, minoxidil and finasteride to the scalp and other areas exhibiting hair loss. Such methods can be used for re-growing hair, and / or preventing or slowing hair loss.

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.

A system for enhancing and promoting hair growth addresses the problem of premature or undesirable hair loss with the use of i) laser energy applied to the scalp in conjunction with ii) certain topical applications that can be applied to the scalp on a periodic basis and iii) certain supplements that are ingested orally. The specific applications and combination of ingredients will be determined, at least in part, by the gender of the patient. The apparatus of the present invention directs laser energy, in an optimal range of wavelengths, directly to the scalp in both residential and clinical environments. The topical application described herein, including the gender-based component, preferably combines some combination of Finasteride with one or more of a DHT inhibitor, primrose oil, a hormone balancing multi-vitamin, and a hair growth vitamin, all administered in accordance with a specific protocol. Finally, the supplements provide for detoxification and nutritional enhancement for an individual receiving hair growth treatment.

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.

The invention relates to the technical field of medicines, disclosing solid lipid nanoparticles of finasteride, which comprise the ingredients according to parts by weight as follows: 1 to 10 parts of finasteride, 3 to 500 parts of solid lipid materials, 10 to 200 parts of phospholipid and 10 to 100 parts of emulsifiers. The invention also discloses a preparation method of the above solid lipid nanoparticles of finasteride. The solid lipid nanoparticles of finasteride primely solve the problems of slightly solubility, low dissolution rate and low bioavailability of the finasteride, being advantageous to fabrication of medicinal preparation and quality improvement.

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.

The invention relates to a drug compound that takes tamsulosin hydrochloride and finasteride as its active ingredients as well as its preparation method and purpose. The invention, which takes tamsulosin hydrochloride and finasteride as its active ingredients and forms drug compound by mixing pharmaceutically acceptable supplementary materials, can be applied for the treatment of benign hyperplasia of prostate. The invention takes tamsulosin hydrochloride and finasteride as its active ingredients and adds the supplementary materials with certain portion and sorts, then develop them into tablet, capsule, dispersible tablet, chewable tablet, toroches and pill via the preparation technology in the invention.

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 present invention is directed to compositions and methods suitable for the treatment of alopecia by topical application include minoxidil sulfate, finasteride, and 17α-estradiol. The combination is characterized by low alcohol content to minimize skin irritation and may be enhanced with the addition of vitamins, minerals, and peptides. The topical use of this combination leads to a lower overall risk of side effects than orally administered drugs.

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.

The present invention aims to provide a pharmaceutical composition for the treatment of alopecia, said composition comprising polymeric nanoparticles, preferably nanocapsules, containing finasteride, additives and a pharmaceutically acceptable carrier, as well as the use of the nanoparticles for preparing said composition for treating alopecia. The invention further includes an appropriate finasteride nanocapsule preparation process suitable for a composition for topical application for treating alopecia.

The invention provides a nano lipid carrier microneedle for treating alopecia. The nano lipid carrier microneedle comprises: a) a needle tip portion, and b) a base portion, wherein the needle tip portion comprises a finasteride nano lipid carrier and a needle tip matrix; and the base portion comprises a base matrix. The invention further provides application of the nano lipid carrier microneedle in preparation of a drug for treating androgen-derived alopecia. The nano lipid carrier microneedle can improve the retention amount of finasteride in hair follicles and a hair follicle targeting effect, and promotes hair follicle development and hair growth by inhibiting 5 alpha-reductase and / or stimulating hair follicle stem cells.