28 results about "Finasteride" patented technology

The invention discloses 5 alpha-reductase degradation molecules as well as a preparation method and application thereof, four 5 alpha-reductase degradation molecules can realize thorough removal of zymoprotein by inducing proteasome-dependent degradation of 5 alpha-reductase instead of only inhibiting the activity of the 5 alpha-reductase, so that a more lasting treatment effect is obtained; under the condition of equal dosage, the effect of the 5 alpha-reductase degradation molecule on treating the benign prostatic hyperplasia is superior to that of the traditional inhibitor finasteride; the four kinds of 5 alpha-reductase degrading molecules can effectively degrade 5 alpha-reductase protein and remarkably inhibit development of benign prostatic hyperplasia, have good biological safety and provide new strategies and candidate drugs for treatment of diseases related to 5 alpha-reductase such as benign prostatic hyperplasia, prostatic cancer, androgenetic alopecia and acne.

This disclosure relates to a single pharmaceutical composition comprising a therapeutically effective or prophylactically effective amount of both minoxidil, or a similar antihypertensive vasodilator, and a 5-alpha reductase inhibitor (in some embodiments, the 5-alpha reductase inhibitor is finasteride) for treating or preventing hair loss in a subject. This disclosure also relates to a pharmaceutical package comprising a pharmaceutical composition for oral administration of a therapeutically effective or prophylactically effective amount of minoxidil, or a similar antihypertensive vasodilator, and a pharmaceutical composition for oral administration comprising a therapeutically effective or prophylactically effective amount of a 5-alpha reductase inhibitor (in some embodiments, the 5-alpha reductase inhibitor is finasteride) for treating or preventing hair loss in a subject. The disclosure further provides methods of treating or preventing hair loss in a subject using the disclosed compositions and packages.

The application discloses a method for determining the content of forbidden components in anti-hair-loss cosmetics, and comprises the following steps: after sample treatment, machine determination is carried out, and an HPLC-MS / MS detection method is adopted, wherein: the liquid chromatography conditions are as follows: a chromatographic column is an Agilent ZORBAX SB-C18 (10 cm*4.6 mm, 3.5 um); a mobile phase A is 0.1% formic acid aqueous solution; a mobile phase B is acetonitrile; a flow rate is 0.6 mL / min; a column temperature is 25 DEG C; and a sample injection amount is 5 uL; and the forbidden components are finasteride and / or fluoroandrosterone. The method for determining the forbidden components in the anti-hair-loss cosmetics has high sensitivity, is simple and easy to operate, and has good repeatability, is a kind of detection method capable of accurately determining the nature and quantity, and has important significance for controlling the quality of the anti-hair-loss cosmetics.

A pharmaceutical formulation for treating alopecia, a preparation method therefor and the use thereof are provided. Specifically, a formulation or composition for treating alopecia contains the following active components on the basis of the mass percentage (w / w) or mass / volume percentage (w / v): (a) 5% of minoxidil; and (b) 0.07-0.095% of finasteride. The formulation or the composition is a foaming agent or a liniment. When the formulation is a foaming agent, the total mass in the mass percentage does not contain the mass of a propellant.

The invention provides a sustained-release medicinal preparation for preventing and treating alopecia as well as a preparation method and application of the sustained-release medicinal preparation, and belongs to the technical field of biological medicines. The medicine for preventing and treating alopecia is prepared from the following components: 1 to 2.5 mg of finasteride, 4 to 6 mg of minoxidil, 20 to 60 mg of spirolactone, 10 to 20 mg of isotretinoin, 3 to 8 mg of vitamin B5, 50 to 100 mg of zinc and 5 to 10 mg of vitamin b6. The components cooperate with one another to activate hair follicle stem cells, increase the number of hair follicles and synergistically enhance the ability of promoting hair regeneration, so that a better alopecia prevention and treatment effect is achieved; the pharmaceutical preparation prepared by selecting a specific filler, an adhesive, a sustained-release framework material and a lubricant in a reasonable proportioning range has good sustained-release performance, the dosage and frequency of the medicine are greatly reduced, and the side effect is far lower than that of an oral medicine in a common dosage form.

The invention provides a double-layer photo-thermal drug-loaded hydrogel microneedle, a preparation method thereof and application of the double-layer photo-thermal drug-loaded hydrogel microneedle in preparation of drugs for treating androgenetic alopecia, and belongs to the technical field of microneedle materials. The preparation method comprises the following steps: preparing a first precursor solution from prepared methacrylated hyaluronic acid, a polylactic acid-glycolic acid copolymer loaded with a finasteride drug and lithium phenyl-2, 4, 6-trimethylbenzoyl phosphonate, adding the first precursor solution into a needle body part of a microneedle mold, and performing negative pressure defoaming, heating concentration and light curing to form the needle body part; meanwhile, black phosphorus quantum dots and a methacrylated hyaluronic acid solution are mixed to prepare a second precursor solution, the second precursor solution is added into a needle body part of a microneedle mold to be dried, a substrate part is formed, and the double-layer photo-thermal drug-loading hydrogel microneedle is prepared. According to the double-layer photo-thermal drug-loading hydrogel microneedle, the drug release rate can be regulated and controlled through the photo-thermal effect of the black phosphorus quantum dots, and precise drug delivery is achieved.

According to the preparation method, sodium perborate tetrahydrate is selected as an oxidizing agent, the requirement for preparing the finasteride through an oxidation elimination reaction is met by accurately controlling reaction conditions, the impurity amount is small, a reagent which easily generates a large amount of waste solids or waste liquid is avoided, operation is easy, and the method is suitable for industrial production. Waste liquid generated by post-treatment is easy to treat. Meanwhile, side reactions are reduced, tedious refining steps are avoided, and the yield of the product is increased.

A method for promoting hair regrowth in a subject includes performing microneedling on a region of a scalp of the subject to a depth of 0.5 millimeters (mm) to 1.5 mm, applying at least one therapeutic agent to the microneedled region, wherein the at least one therapeutic agent comprises Minoxidil, Finasteride, and Dutasteride, and implanting non-permanent pigment particles into a superficial dermis of the microneedled region, the microneedling, the applying, and the implanting together synergistically stimulating hair follicle activity.

The invention relates to the technical field of androgen-derived alopecia, and discloses a micro-needle patch based on a hierarchical targeting mechanism as well as a preparation method and application of the micro-needle patch. The finasteride is arranged on the needle tip section of the microneedle, the quercetin is arranged on the needle root section, different cells are targeted through the finasteride and the quercetin in a graded mode, and the microneedle patch with a graded targeting mechanism is formed. After the micro needle pierces into the skin, the water-soluble polymer at the needle tip section is dissolved, finasteride targeted hair papilla cells are released, and then in the process that finasteride acts, the quercetin slowly released at the needle root section gradually acts on endothelial cells in a targeted mode, the proliferation and migration activity of the endothelial cells is promoted, and the effect of the finasteride on the skin is achieved. Endothelial cells are enhanced to form a highly branched capillary network to act on hair papilla cells, the metabolic demand of the hair papilla cells is maintained, and finally the effect of enhancing the finasteride targeting effect is achieved. Therefore, the microneedle patch with the hierarchical targeting mechanism has an excellent AGA curative effect.

Provided is a pharmaceutical composition for preventing or treating benign prostatic hyperplasia or alopecia, comprising lactic acid bacteria of Enterococcus genus as an active ingredient. The pharmaceutical composition of the present invention can replace the conventional therapeutic agents against treating benign prostatic hyperplasia or alopecia, such as finasteride or dutasteride. In particular, by introducing heat-killed probiotics of Enterococcus faecalis, the effect of preventing or treating benign prostatic hyperplasia or alopecia can be further enhanced.

This invention provides a topical finasteride formulation and its preparation method, belonging to the field of pharmaceutical formulation technology. The topical finasteride formulation provided by this invention is a topical dosage form, comprising finasteride and excipients; after scalp administration, the concentration in hair follicles and the epidermis is 999-5021 pg / mL, and the systemic blood concentration is 17.1-178.9 pg / mL; the systemic blood concentration is 1-10% of that of oral finasteride formulations. The method involves preparing finasteride and excipients, followed by steps of dissolving / preparing the matrix, fine filtration / homogenization, and filling to obtain finasteride topical formulations of different dosage forms. This invention effectively solves the shortcomings of existing finasteride formulations, such as high systemic absorption, high risk of adverse reactions, and difficulty in industrializing the process, making it suitable for large-scale clinical application in androgenetic alopecia, combining efficacy and safety.

In one aspect, the disclosure relates to topical formulations, methods of making same, and methods of treating hair loss using same. In an aspect, the present disclosure pertains to topical formulations for treatment of hair loss and / or to increase hair growth, the formulation comprising: a therapeutic composition comprising therapeutically effective amounts of azelaic acid, minoxidil, finasteride, and dutasteride; and one or more compounding agents. In a further aspect, the present disclosure pertains to a method of treating hair loss by applying a disclosed topical formulation. In a further aspect, the present disclosure pertains to a method of enhancing hair grow by applying a disclosed topical formulation. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

The invention discloses a preparation method of a photo-crosslinking hydrogel microneedle loaded with a finasteride drug, which comprises the following three steps: preparing drug nanoparticles, synthesizing a hydrogel precursor and preparing the photo-crosslinking hydrogel microneedle. The preparation method specifically comprises the steps of preparing finasteride (FIN)-loaded polyhydroxyalkanoate (PHA) nanoparticles (F-PHANPs), preparing F-PHANPs-loaded HAMA hydrogel (F-HAMA) and preparing a hydrogel microneedle, introduction of the F-PHANPs enhances the mechanical performance of the hydrogel, meanwhile, the hardness is remarkably enhanced, and the hydrogel has excellent drug release performance and biocompatibility and can be used for preparing the hydrogel microneedle. Potential application prospects are shown in the field of treating androgenetic alopecia through transdermal drug delivery.

A method for the treatment or prevention of the symptoms or effects of hair loss of an animal which comprises treating the animal with a therapeutically effective amount of a combination comprising 7α-Acetylthio-17α-hydroxy-3-oxopregn-4-ene-21-carboxylic acid γ-lactone or a physiologically functional derivative thereof, N-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide or a physiologically functional derivative thereof, 17β-(N-tert-butylcarbamoyl)-4-aza-5α-androst-1-en-3-one or a physiologically functional derivative thereof, and 2,4-pyrimidinediamine, 6-(1-piperidinyl)-, 3-oxide or a physiologically functional derivative thereof. A pharmaceutical formulation comprising the same. A patient pack comprising at least one active ingredient selected from 7α-Acetylthio-17α-hydroxy-3-oxopregn-4-ene-21-carboxylic acid γ-lactone or a physiologically functional derivative thereof, N-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide, 17β-(N-tert-butylcarbamoyl)-4-aza-5α-androst-1-en-3-one, and 2,4-pyrimidinediamine, 6-(1-piperidinyl)-, 3-oxide, and an information insert containing directions on the use of all three active ingredients together in combination.

This invention relates to the field of transdermal microneedle formulation technology, specifically to a chitosan-finasteride nanocrystal microneedle formulation and its preparation method that enhances skin retention. The microneedle formulation includes a needle tip, an extension, and a root. The needle tip and the extension are both composed of chitosan-finasteride nanocrystals, and the root is hyaluronic acid. After being coated with chitosan, the finasteride nanocrystals acquire a positive charge on their surface, forming an electrostatic interaction with the negative charge in the skin's microenvironment. This leads to the adsorption of the chitosan-finasteride nanocrystals onto the skin surface. Simultaneously, the positively charged surface of the chitosan-finasteride nanocrystals increases endocytosis, effectively improving drug entry efficiency and achieving drug accumulation within scalp cells. This dual effect enhances the retention of finasteride nanocrystals on the skin surface and prevents finasteride from entering the bloodstream.

The present invention relates to a composition for alleviating or treating hair loss in which a hair loss drug is loaded in lipid nanoparticles. The lipid nanoparticles contain 0.30 mol% or more of a hydrophobic drug such as finasteride or dutasteride relative to the lipid nanoparticles and are loaded with the hydrophobic drug at an encapsulation rate of 90.0% or more, and thus have the advantage of being able to maintain water dispersibility for a long period of time while increasing transdermal delivery. Therefore, the present invention can more effectively alleviate symptoms of male pattern hair loss on the scalp where localized hair loss or thinning of hair occurs.

Topical compositions and kits are provided for hair regrowth, hair loss prevention, and scalp health improvement. These formulations contain at least one active (e.g., finasteride, minoxidil, dutasteride, and latanoprost), at least one penetration enhancer (e.g., Transcutol®, laurocapram), stabilizers, and anti-inflammatory agents like retinoic acid, hydrocortisone, and aloe vera. They utilize optimized particle sizes (D90 ≤8.5 μm, span ≤1.7) and may include bioadhesive polymers or nanoparticles for enhanced follicular delivery and extended residence. Modular kits offer multi-chambered packaging, calibrated droppers, and app- or sensor-guided dispensing for customizable ingredient mixing and regimen personalization. These innovations improve active stability, minimize irritation, and yield superior clinical outcomes (hair density and quality) over traditional therapies. Methods include treating varied alopecia types, with or without device-assisted delivery (microneedling, light therapy), alongside digital monitoring, compliance tracking, and optional diagnostic or conditioning tools for individualized scalp and hair care.

The invention discloses a finasteride intermediate as well as a preparation method and application thereof, and belongs to the technical field of medicine synthesis. The preparation method of the finasteride intermediate comprises the following steps: mixing progesterone and an organic solvent, continuously introducing ozone at-20 DEG C to-10 DEG C to obtain an intermediate state I, dropwise adding peroxide at-10 DEG C or below, dropwise adding a sodium hydroxide solution, heating to 15-25 DEG C, and reacting to obtain the finasteride intermediate. In addition, the invention also provides the finasteride intermediate which is prepared by the preparation method. In addition, the invention also provides an application of the finasteride intermediate in preparation of finasteride. According to the method, sodium periodate does not need to be used, 4-position double bonds can be cut off through oxidation by adding a small amount of peroxide and a sodium hydroxide solution, the finasteride intermediate is obtained, and the green chemical requirement is met.

In one aspect, the disclosure relates to topical formulations, methods of making same, and methods of treating hair loss using same. In an aspect, the present disclosure pertains to topical formulations for treatment of hair loss and / or to increase hair growth, the formulation comprising: a therapeutic composition comprising therapeutically effective amounts of azelaic acid, minoxidil, finasteride, and dutasteride; and one or more compounding agents. In a further aspect, the present disclosure pertains to a method of treating hair loss by applying a disclosed topical formulation. In a further aspect, the present disclosure pertains to a method of enhancing hair grow by applying a disclosed topical formulation. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

The present invention relates to a pharmaceutical composition for preventing or treating benign prostatic hyperplasia, including mixed extracts of Curcumae radix and Syzygii flos as an effective component. The mixed extracts were found to inhibit the expression of dihydrotestosterone, androgen receptors, prostate-specific antigens, proliferating cell nuclear antigen (PCNA), cyclin B1, and nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB); and to have less adverse side effects compared to an existing benign prostatic hyperplasia drug, finasteride, and thus may be beneficially used for the prevention or treatment of benign prostatic hyperplasia.

This invention provides a plurality of biodegradable microspheres, wherein the microspheres (i) have a d10 value of at least 1 μm and a d90 value of 28 μm or less; (ii) comprise a polylactic-co-glycolic acid copolymer (PLGA) matrix; (iii) carry a therapeutically effective amount of pharmaceutical finasteride; and (iv) when present intradermally, release finasteride for at least one month. This invention also provides related injectable formulations, methods for treating hair loss, and articles of manufacture.

The invention discloses a traditional Chinese medicine essential oil composition for treating alopecia, which comprises traditional Chinese medicine essential oil and a deep eutectic solvent, or the traditional Chinese medicine essential oil composition is a water-based traditional Chinese medicine essential oil transdermal delivery system prepared by dropwise adding the traditional Chinese medicine essential oil into the deep eutectic solvent, uniformly mixing and then uniformly mixing with water. The traditional Chinese medicine essential oil composition is simple in preparation process, can stably entrap essential oil, enhances percutaneous penetration of the essential oil through lipid extraction, effectively delivers the essential oil to hair follicles to play a role in promoting hair regeneration activity, has the effect of treating alopecia, especially androgen-derived alopecia, and has a good application prospect. The adverse reaction caused by applying medicines such as finasteride and minoxidil is avoided. The invention discloses application of the traditional Chinese medicine essential oil composition in preparation of a medicine with hair regeneration promoting activity, preferably application in preparation of a medicine for treating alopecia, and more preferably application in preparation of a medicine for treating androgen-derived alopecia.

The invention discloses a rapidly-dissolved finasteride tablet and a production method thereof, and relates to the technical field of medicine preparation. According to the invention, finasteride is loaded in carboxylated mesoporous silica, so that drug molecules of finasteride are dispersed from a crystalline state to an amorphous state, the dissolution rate is improved, carboxyl maintains a non-ionized state in a gastric juice environment, stimulation of drugs in a gastric acid environment is reduced, carboxyl is ionized in an intestinal solution, and the dissolution rate of the drugs is increased. The quick release of the medicine can be realized; according to the invention, a modified polymer emulsion is also prepared as a material of a coating solution, by utilizing the characteristics of the coating solution, the tablet is insoluble in a gastric acid environment and dissolved in an intestinal juice environment, the irritation to patients with stomach diseases is reduced, and the intestinal absorption area is relatively large, so that the absorption rate of the medicine is improved, and the bioavailability is improved.

The application belongs to the field of medicine, and discloses a composition containing finasteride and use thereof. The composition contains finasteride, graphene and one or more pharmaceutically acceptable excipients. The composition of the application can be used to prevent and / or treat alopecia, seborrheic alopecia, androgenic alopecia, alopecia areata, or promote hair growth, and the amount of active ingredient is greatly reduced compared with finasteride tablets, thereby reducing the side effects associated therewith, and the composition has fast onset, long duration of action and good efficacy.

The application belongs to the field of pharmaceutical preparations, and discloses a cyclodextrin-included finasteride external gel preparation, a preparation method and application thereof. The gel preparation is composed of an inclusion compound of finasteride and a cyclodextrin derivative, a gel matrix and one or more than one pharmaceutically acceptable adjuvant. The finasteride and the cyclodextrin derivative are first prepared into an inclusion compound through an inclusion technology, and then the inclusion compound is uniformly dispersed in the gel matrix to obtain the external gel. In this way, the water solubility and local bioavailability of the finasteride are significantly improved, and the defect of poor water solubility is overcome. Animal experiments show that after local administration, the gel preparation can significantly promote hair regeneration, can effectively limit the drug from entering the systemic circulation through the skin, can avoid the systemic side effects caused by long-term medication, and is safer.

The present application provides a kind of local pharmaceutical composition comprising 5 alpha-reductase inhibitor, penetration agent, hydroxypropyl methyl cellulose and water, and the 5 alpha-reductase inhibitor is finasteride or dutasteride.The composition of the present application has good spraying effect, stable in-vitro skin retention, and shows good hair growth effect on mouse androgenetic alopecia model, and the hair growth effect is better than that of prior art, and the skin feel is better, and is not sticky.

A composition for topical use in the treatment of androgenetic alopecia comprises a nanoemulsion, said nanoemulsion comprising a mixture of oils, at least one surfactant, finasteride and minoxidil. The mixture of oils comprises sandalwood oil, rosemary oil and sweet almond oil.

The invention provides a method for synthesizing a finasteride impurity C. The method comprises the following steps: by taking finasteride (formula F10) as an initial raw material, carrying out electrochemical reaction methoxylation to obtain a methoxyl (formula F11), and then carrying out high-temperature vacuum elimination to obtain the impurity C. The overall yield is 90%. The invention provides a brand-new synthesis method of the impurity C, which can be used for efficiently preparing a reference substance of the finasteride impurity C. Compared with an original obtaining mode of the impurity C reference substance, the method has the advantage that the availability of the impurity reference substance is greatly improved. The invention provides a novel intermediate F11 compound, the impurity C is prepared through high-temperature elimination of the compound, and the compound has the characteristics of high selectivity, high conversion rate and simplicity and easiness in installation of an electrochemical device, and can meet the requirements of laboratories and kilogram-level production. And a new synthesis thought is provided for obtaining the impurity C compound.