42 results about "Finasteride" patented technology

The present invention relates to a novel long-acting injectable composition comprising finasteride for the prevention or treatment of androgenetic alopecia. The composition inhibits type II 5α-reductase with a single injection lasting over one month, thereby suppressing the conversion of testosterone to DHT and reducing androgen-mediated follicular miniaturization. In addition, after injection into the body, the average elimination half-life (T1 / 2el) of finasteride can be increased to enhance stability and provide more predictable and uniform therapeutic effects compared to oral formulations.

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 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 invention belongs to the technical field of pharmaceutical analysis, and particularly relates to a biological analysis method for detecting the concentration of hydrocortisone butyrate in blood plasma, which is used for analyzing a compound to be detected in the blood plasma through an LC-MS / MS (Liquid Chromatography-Mass Spectrometry / Mass Spectrometry) method. According to the detection method, a liquid-liquid extraction pretreatment method is preferably adopted, finasteride serves as an internal standard substance, a Shim-pack Velox SP-C18 chromatographic column is adopted, gradient elution and electrospray ionization source tandem mass spectrometry detection are carried out, and the detection method is high in sensitivity, precise, accurate, high in analysis speed, high in sensitivity, high in sensitivity, high in sensitivity, high in sensitivity, high in sensitivity, high in sensitivity, high in sensitivity, high in sensitivity and high in sensitivity. The sample analysis requirement in the clinical research of the hydrocortisone butyrate is met.

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 present invention discloses a preparation process and application of a compound preparation of astaxanthin, lycopene and proanthocyanidins for anti-aging and prevention of prostate diseases, belonging to the field of biomedicine. The preparation is composed of astaxanthin (1-10 parts), proanthocyanidins (5-30 parts), lycopene (2-15 parts), black cumin seed oil (0.5-3 parts), Phyllanthus emblica extract (3-8 parts) and Withania somnifera extract (1-5 parts), and is prepared by high-efficiency wet granulation technology. The components act synergistically to significantly enhance antioxidant, anti-inflammatory and anti-cancer activities, and have dual effects of anti-aging and prevention and treatment of prostate diseases. Experiments show that the hydroxyl radical scavenging rate of the compound preparation is 2.3 times higher than that of the single ingredient, the inflammatory factors in the prostatitis model are reduced by 68%, the skin antioxidant capacity is increased by 55%, and the combination with finasteride can reduce the dosage of chemical drugs by 80% and reduce the risk of sexual dysfunction. Black cumin seed oil significantly improves the bioavailability of lycopene (29.7%), and the drug concentration in the prostate tissue reaches 6.5 times that in the blood, achieving high efficiency with low dosage.

The invention relates to the field of biological medicine, in particular to application of finasteride in preparation of a medicine for treating triple negative breast cancer. In-vitro experiments prove that by up-regulating ZBTB20 gene expression, finasteride significantly inhibits polarization of macrophages to M2 type and promotes M1 type differentiation; a mouse triple-negative breast cancer transplantation tumor model further proves that the treatment of finasteride combined with adriamycin has an anti-tumor effect and can significantly inhibit tumor growth, so that the combination of finasteride and adriamycin can significantly enhance the anti-tumor effect and is superior to single-drug treatment. The invention discloses the application of finasteride in treatment of triple negative breast cancer for the first time, proposes the ZBTB20 gene as a main action target of finasteride in inhibition of triple negative breast cancer tumor, and proposes that the ZBTB20 protein or the ZBTB20 gene as a treatment target has great potential in treatment of triple negative breast cancer, drug screening and other aspects.

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 belongs to the field of medicines, and discloses a finasteride-containing composition and application thereof. The composition comprises finasteride, graphene and more than one pharmaceutically acceptable auxiliary material. The composition can well prevent and / or treat alopecia, alopecia seborrhoeica, androgenetic alopecia and alopecia areata or promote hair growth, compared with finasteride tablets, the dosage of active ingredients of the composition is greatly reduced, related side effects of the active ingredients are relieved, and the composition is quick in effect taking, long in drug effect lasting time and good in curative effect.

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.

The invention relates to the related field of treatment of alopecia, in particular to a compound preparation for treating alopecia and a preparation technology of the compound preparation for treating alopecia. The first active component accounts for 1-10% by mass of the compound preparation, the second active component accounts for 0.1-5% by mass of the compound preparation, the first active component is minoxidil, and the second active component is finasteride. The compound preparation is a gel, plays a local role and is free of irritation, and the medicine can be better reserved to act on the scalp, so that the effect of treating alopecia is achieved.

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.

An embodiment relates to a novel long-acting injectable composition for preventing or treating androgenetic alopecia containing finasteride. The injectable composition is capable of inhibiting type II 5α-reductase for one month or more with a single injection, thereby limiting the conversion of testosterone to DHT and inhibiting androgen-mediated hair follicle miniaturization. In addition, the injectable composition may increase the mean elimination half-life (t1 / 2el) of finasteride after in vivo injection, thereby increasing the stability of finasteride, and exhibiting a more predictable and uniform therapeutic effect compared to oral dosage forms.

The invention belongs to the field of transdermal drug delivery preparations, and particularly relates to a finasteride transdermal patch. The finasteride transdermal patch is provided with a backing layer, a drug-containing layer and an anti-sticking layer in a laminated manner, the drug-containing layer comprises a main drug, a pressure-sensitive adhesive and a penetration enhancer, and the main drug is selected from finasteride or a finasteride-organic acid ion pair; and the pressure-sensitive adhesive is selected from hydroxyl polyacrylate pressure-sensitive adhesive. The finasteride pressure-sensitive adhesive dispersible patch which is simple in composition, gentle in blood concentration, good in in-vivo and in-vitro permeability and high in safety is prepared by adopting a strategy of combining an ion pair technology and a chemical penetration enhancer, is administered once a day, has the same drug effect as oral finasteride, and is suitable for clinical application. The traditional Chinese medicine composition can be used for treating androgen alopecia.

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.

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 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 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.

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 pharmaceutical composition for treating alopecia, which contains minoxidil, optionally finasteride and / or dutasteride, and a specific kind of carbohydrates. The specific type of carbohydrates can effectively improve the stability of the pharmaceutical composition, including reducing the generation of impurities in the pharmaceutical composition and prolonging the stable storage period of the pharmaceutical composition at low temperature or high temperature. The invention further discloses a preparation for treating alopecia, and the preparation can be widely applied clinically.

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.