WO2023201858A1 - Medication for treating androgenetic alopecia - Google Patents
Medication for treating androgenetic alopecia Download PDFInfo
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- WO2023201858A1 WO2023201858A1 PCT/CN2022/097218 CN2022097218W WO2023201858A1 WO 2023201858 A1 WO2023201858 A1 WO 2023201858A1 CN 2022097218 W CN2022097218 W CN 2022097218W WO 2023201858 A1 WO2023201858 A1 WO 2023201858A1
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- Prior art keywords
- aprelite
- medicine
- finasteride
- dutasteride
- treating
- Prior art date
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- 239000003814 drug Substances 0.000 title claims abstract description 47
- 201000004384 Alopecia Diseases 0.000 title claims abstract description 36
- 229940079593 drug Drugs 0.000 title claims abstract description 29
- 201000002996 androgenic alopecia Diseases 0.000 title claims abstract description 28
- 206010068168 androgenetic alopecia Diseases 0.000 title claims abstract description 15
- DBEPLOCGEIEOCV-WSBQPABSSA-N finasteride Chemical compound N([C@@H]1CC2)C(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)NC(C)(C)C)[C@@]2(C)CC1 DBEPLOCGEIEOCV-WSBQPABSSA-N 0.000 claims abstract description 35
- 229960004039 finasteride Drugs 0.000 claims abstract description 35
- JWJOTENAMICLJG-QWBYCMEYSA-N dutasteride Chemical compound O=C([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)N[C@@H]4CC3)C)CC[C@@]21C)NC1=CC(C(F)(F)F)=CC=C1C(F)(F)F JWJOTENAMICLJG-QWBYCMEYSA-N 0.000 claims abstract description 33
- 229960004199 dutasteride Drugs 0.000 claims abstract description 33
- 239000004480 active ingredient Substances 0.000 claims description 16
- 238000002360 preparation method Methods 0.000 claims description 11
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 9
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 6
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 6
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 6
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 claims description 3
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims description 3
- 239000000463 material Substances 0.000 claims description 3
- -1 Or Aprelate Chemical compound 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims description 2
- 239000000203 mixture Substances 0.000 abstract description 33
- 239000002677 5-alpha reductase inhibitor Substances 0.000 abstract description 9
- 230000003779 hair growth Effects 0.000 abstract description 9
- 229940113178 5 Alpha reductase inhibitor Drugs 0.000 abstract description 8
- 210000003780 hair follicle Anatomy 0.000 abstract description 8
- VAPSMQAHNAZRKC-PQWRYPMOSA-N Epristeride Chemical compound C1C=C2C=C(C(O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)NC(C)(C)C)[C@@]1(C)CC2 VAPSMQAHNAZRKC-PQWRYPMOSA-N 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 6
- 229950009537 epristeride Drugs 0.000 abstract description 6
- 238000000034 method Methods 0.000 abstract description 3
- 230000001737 promoting effect Effects 0.000 abstract description 3
- 231100000360 alopecia Toxicity 0.000 abstract description 2
- 230000008569 process Effects 0.000 abstract description 2
- 241000699670 Mus sp. Species 0.000 description 15
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 10
- 239000000243 solution Substances 0.000 description 10
- NVKAWKQGWWIWPM-ABEVXSGRSA-N 17-β-hydroxy-5-α-Androstan-3-one Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 NVKAWKQGWWIWPM-ABEVXSGRSA-N 0.000 description 7
- 229960003473 androstanolone Drugs 0.000 description 6
- 230000003676 hair loss Effects 0.000 description 6
- 208000024963 hair loss Diseases 0.000 description 6
- 229960003604 testosterone Drugs 0.000 description 5
- 102100033875 3-oxo-5-alpha-steroid 4-dehydrogenase 2 Human genes 0.000 description 4
- 101000640851 Homo sapiens 3-oxo-5-alpha-steroid 4-dehydrogenase 2 Proteins 0.000 description 4
- 230000002354 daily effect Effects 0.000 description 4
- 210000004209 hair Anatomy 0.000 description 4
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 description 3
- 208000004403 Prostatic Hyperplasia Diseases 0.000 description 3
- 239000003098 androgen Substances 0.000 description 3
- 210000002307 prostate Anatomy 0.000 description 3
- 210000003491 skin Anatomy 0.000 description 3
- 108010066551 Cholestenone 5 alpha-Reductase Proteins 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000010534 mechanism of action Effects 0.000 description 2
- 229960003632 minoxidil Drugs 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229940068968 polysorbate 80 Drugs 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 230000000750 progressive effect Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- YFDSDPIBEUFTMI-UHFFFAOYSA-N tribromoethanol Chemical compound OCC(Br)(Br)Br YFDSDPIBEUFTMI-UHFFFAOYSA-N 0.000 description 2
- 229950004616 tribromoethanol Drugs 0.000 description 2
- 230000002485 urinary effect Effects 0.000 description 2
- 238000011740 C57BL/6 mouse Methods 0.000 description 1
- XJLXINKUBYWONI-NNYOXOHSSA-O NADP(+) Chemical compound NC(=O)C1=CC=C[N+]([C@H]2[C@@H]([C@H](O)[C@@H](COP(O)(=O)OP(O)(=O)OC[C@@H]3[C@H]([C@@H](OP(O)(O)=O)[C@@H](O3)N3C4=NC=NC(N)=C4N=C3)O)O2)O)=C1 XJLXINKUBYWONI-NNYOXOHSSA-O 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 229930040373 Paraformaldehyde Natural products 0.000 description 1
- 206010046555 Urinary retention Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 238000000540 analysis of variance Methods 0.000 description 1
- 229940030486 androgens Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 230000035617 depilation Effects 0.000 description 1
- 230000002951 depilatory effect Effects 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000003304 gavage Methods 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 230000003681 hair reduction Effects 0.000 description 1
- 238000010832 independent-sample T-test Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 239000007935 oral tablet Substances 0.000 description 1
- 229940096978 oral tablet Drugs 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 229920002866 paraformaldehyde Polymers 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
Definitions
- the present invention belongs to the technical field of hair growth, and more specifically, relates to a medicine for treating androgenic alopecia.
- AGA Androgenetic alopecia
- the prevalence of AGA in men and women in my country is 21.3% and 6.0% respectively. It mostly occurs in adolescence and post-puberty, and is mainly characterized by progressive hair reduction and miniaturization of hair follicles.
- the main causes of AGA are genetic factors and abnormal androgen levels. Among them, abnormal androgen levels are mainly manifested in the type II 5 ⁇ reductase activity in hair loss areas that is significantly higher than in non-hair loss areas. Androgens are converted into dihydrotestosterone under the action of 5 ⁇ reductase. Increased dihydrotestosterone content can make hair follicles miniaturized.
- the thick black terminal hair gradually turns into light-colored vellus hair, and eventually the hair follicles shrink and disappear, clinically manifesting as hair loss.
- the U.S. Food and Drug Administration has approved only two drugs for the treatment of androgenetic alopecia, namely minoxidil topical preparation and finasteride oral preparation.
- minoxidil topical preparation and finasteride oral preparation.
- finasteride is a type II 5 ⁇ reductase inhibitor, thereby inhibiting hair loss, but it can easily cause sex-related side effects.
- Epristeride (chemical name: 17- ⁇ (N-tert-butyl-amino-formyl)androsta-3,5-diene-3-carboxylic acid) is a new type of non-competitive 5 ⁇ reductase Inhibitors.
- Aprelite forms a ternary complex with 5 ⁇ reductase and NADP, which inhibits the conversion of testosterone into dihydrotestosterone (DHT), thereby reducing the content of dihydrotestosterone.
- DHT dihydrotestosterone
- Finasteride is a 4-azasteroid compound and a specific inhibitor of intracellular type II 5 ⁇ reductase. It inhibits the metabolism of testosterone into dihydrotestosterone and can effectively reduce the levels of dihydrotestosterone in the blood, prostate, skin and other tissues. Hydrotestosterone content. It is clinically approved for the treatment of benign prostatic hyperplasia (5 mg strength) and androgenic alopecia (1 mg strength).
- Dutasteride is a type I and type II 5 ⁇ reductase inhibitor. It also inhibits the conversion of testosterone into dihydrotestosterone, thereby inhibiting the growth of the prostate in patients with benign prostatic hyperplasia.
- the dosage form for clinical use is capsule, and the recommended dosage is 0.5mg/day.
- the oral preparation dutasteride at a dose of 0.5 mg/day has been approved by the Korean Ministry of Food and Drug Safety for the treatment of androgenic alopecia.
- the technical problem to be solved by the present invention is to provide a medicine for treating androgenic alopecia.
- a drug for treating androgenic alopecia the active ingredient of which is Apretide, or Apretide and finasteride, or Apretide and dutasteride, or Apretide Specifically, finasteride and dutasteride, the daily dosage of the active ingredient of the medicine is 0.01-1 mg.
- Aplitide single-use drug Aplitide 0.01mg to 1mg;
- Aprelite composition 1 Aprelite 0.01mg to 0.5mg, finasteride 0.01mg to 0.5mg;
- Aprelite composition 2 Aprelite 0.01mg to 0.5mg, Dutasteride 0.01mg to 0.5mg;
- Aprelite composition 3 Aprelite 0.01mg to 0.3mg, finasteride 0.01mg to 0.3mg; dutasteride 0.01mg to 0.3mg.
- the daily dosage of the active ingredient of the drug is 0.05-0.5 mg.
- Aprelite single drug Aprelite 0.05mg to 0.5mg
- Aprelite composition 1 Aprelite 0.05mg to 0.2mg, finasteride 0.01mg to 0.2mg;
- Aprelite composition 2 Aprelite 0.05mg to 0.2mg, dutasteride 0.01mg to 0.2mg;
- Aprelite composition 3 Aprelite 0.05mg to 0.15mg, finasteride 0.01mg to 0.1mg; dutasteride 0.01mg to 0.1mg.
- the daily dosage of the active ingredient of the drug is 0.15 mg.
- Aprelite composition 1 Aprelite 0.1mg, finasteride 0.05mg;
- Aprelite composition 2 Aprelite 0.1 mg, dutasteride 0.05 mg;
- Aprelite composition 3 Aprelite 0.1 mg, finasteride 0.025 mg; dutasteride 0.025 mg.
- the active ingredients of the drug are a three-component compound of aprete, finasteride and dutasteride, and the daily dosage is respectively 0.1 mg of aprete, 0.025 mg of finasteride, and Dutasteride 0.025mg.
- the active ingredient of the drug is diluted with carboxymethyl cellulose sodium solution.
- the active ingredient of the drug is diluted with 0.5 wt.% sodium carboxymethylcellulose solution.
- the preparation method of the drug for treating androgenetic alopecia is as follows: Aprelite, finasteride, and dutasteride weighed according to the formula are dissolved in a 0.5wt.% carboxymethylcellulose sodium solution, Shake well and store at room temperature.
- a pharmaceutical preparation for treating androgenic alopecia is also within the protection scope of this application.
- the pharmaceutical preparation includes the active ingredients of the drug and preparation auxiliary materials.
- the invention provides a new type of 5 ⁇ reductase inhibitor aprelite single-use drug for treating androgenic alopecia and its composition, which can significantly promote the growth of new hair follicles and has significant effects in treating hair loss and promoting hair growth; It has good safety and quick effect; the process is simple and easy to prepare.
- Figure 1 is a diagram of the hair growth on the back of mice of the present invention; in the figure, Day-1 is the day before administration, Day 12 is the 12th day after administration, and Day 18 is the 18th day after administration.
- Testosterone purchased from Beijing Solebao Technology Co., Ltd.
- sodium carboxymethylcellulose and polysorbate 80 purchased from Sinopharm Pharmaceutical Co., Ltd.
- Avertin purchased from Sigma Company
- Aprelite from Jiangsu Lianhuan Pharmaceutical Co., Ltd.
- Finasteride and Dutasteride purchased from Aladdin Reagent Company.
- the 5-alpha reductase inhibitor ipralide is administered alone or in combination with one or both of finasteride or dutasteride. According to the grouping, it is divided into: Aprelite single use group, Aprelite composition 1, Aprelite composition 2 and Aprelite composition 3.
- the specific formula is as follows:
- Aprelite single drug Aprelite 0.01mg to 1mg;
- Aprelite composition 1 Aprelite 0.01mg to 0.5mg, finasteride 0.01mg to 0.5mg;
- Aprelite composition 2 Aprelite 0.01mg to 0.5mg, Dutasteride 0.01mg to 0.5mg;
- Aprelite composition 3 Aprelite 0.01mg to 0.3mg, finasteride 0.01mg to 0.3mg; dutasteride 0.01mg to 0.3mg.
- the 5-alpha reductase inhibitor ipralide is administered alone or in combination with one or both of finasteride or dutasteride. According to the grouping, it is divided into: Aprelite single use group, Aprelite composition 1, Aprelite composition 2 and Aprelite composition 3.
- the specific formula is as follows:
- Aprelite single drug Aprelite 0.05mg to 0.5mg
- Aprelite composition 1 Aprelite 0.05mg to 0.2mg, finasteride 0.01mg to 0.2mg;
- Aprelite composition 2 Aprelite 0.05mg to 0.2mg, dutasteride 0.01mg to 0.2mg;
- Aprelite composition 3 Aprelite 0.05mg to 0.15mg, finasteride 0.01mg to 0.1mg; dutasteride 0.01mg to 0.1mg.
- the 5-alpha reductase inhibitor ipralide is administered alone or in combination with one or both of finasteride or dutasteride. According to the grouping, it is divided into: Aprelite single use group, Aprelite composition 1, Aprelite composition 2 and Aprelite composition 3.
- the specific formula is as follows:
- Aprelite composition 1 Aprelite 0.1mg, finasteride 0.05mg;
- Aprelite composition 2 Aprelite 0.1 mg, dutasteride 0.05 mg;
- Aprelite composition 3 Aprelite 0.1 mg, finasteride 0.025 mg; dutasteride 0.025 mg.
- mice C57BL/6 female mice about 8 weeks old (purchased from Beijing Vitong Lever Company) were adaptively fed in separate cages for 1 week.
- Day-1 of the test (the day before drug administration), they were anesthetized by intraperitoneal injection of Avertin solution. After shaving the hair on the back of the mice with an electric razor, apply depilatory cream to remove the hair.
- mice After all mice were depilated, they were randomly divided into groups according to the condition of their back skin after depilation, with 5 mice in each group.
- the modeling group was subcutaneously injected with a modeling agent (1mg testosterone, suspended in 10% polysorbate 80 solution). Modeling was performed every seven days for five days, and the control group was injected with the corresponding solvent control.
- mice were given 0.1 mL of the corresponding drug by gavage every day as planned.
- mice were weighed twice a week, and photos were taken on Day-1, Day 12, and Day 18 to record the hair growth status on the back of the mice.
- the animal grouping is shown in Table 1 below:
- mice were euthanized according to animal welfare.
- the back skin of mice from each group was soaked in 4% paraformaldehyde and fixed, embedded in paraffin, sectioned, stained with HE, and observed under a light microscope.
- 4 fields of view were selected for counting of hair follicles under a high-power microscope. Each field of view did not overlap. .
- SPSS13.0 statistical software was used for analysis of variance, and the statistical mean ⁇ standard deviation (Mean ⁇ SD) was used.
- the independent sample t test was used for comparison between the two groups, and p ⁇ 0.05 was considered statistically different.
- hair growth scoring index 0 points, no growth; 1 points, ⁇ 20% growth; 2 points, 20–40% growth; 3 points, 40–60% growth; 4 points, 60–80% growth; 5 points, Score 80–100% growth.
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
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- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
The present invention relates to the technical field of hair growth. Disclosed is a medication for treating androgenetic alopecia. The effective components of the medication are epristeride, or epristeride and finasteride, or epristeride and dutasteride, or epristeride, finasteride, and dutasteride; and the daily administration dosage of the effective components of the medication is 0.01-1 mg. The present invention provides a novel 5α reductase inhibitor epristeride single medication for treating androgenetic alopecia, and a composition thereof, being capable of significantly promoting growth of new hair follicles, and having remarkable effects in the aspects of treating alopecia and promoting hair growth. The present invention is good in safety, quick in effect taking, simple in process, and easy to prepare.
Description
本发明属于生发技术领域，更具体地说，涉及一种用于治疗雄激素性脱发的药物。The present invention belongs to the technical field of hair growth, and more specifically, relates to a medicine for treating androgenic alopecia.
雄激素性脱发(androgeneticalopecia，AGA)是最常见的一种渐进性脱发类型。在我国男性和女性AGA的患病率分别为21.3％和6.0％，其多发生于青春期和青春期后，主要表现为毛发进行性减少和毛囊的微小化。AGA发病原因主要为遗传因素和雄激素水平异常。其中，雄激素水平异常主要表现在脱发区II型5α还原酶活性明显高于非脱发区，雄激素在5α还原酶的作用下转化为双氢睾酮，双氢睾酮含量升高可使毛囊微小化，粗黑的终毛逐渐变为淡色的毳毛，最终毛囊萎缩消失，临床上表现为脱发。目前，美国食品和药品监督管理局仅批准了2种用于治疗雄激素性脱发的药物，分别为米诺地尔外用制剂和非那雄胺口服制剂。其中米诺地尔作用机制尚未清晰阐明，且使用起来较为不便；非那雄胺为II型5α还原酶抑制剂，从而抑制脱发，但其易引起性相关副作用。Androgenetic alopecia (AGA) is the most common type of progressive hair loss. The prevalence of AGA in men and women in my country is 21.3% and 6.0% respectively. It mostly occurs in adolescence and post-puberty, and is mainly characterized by progressive hair reduction and miniaturization of hair follicles. The main causes of AGA are genetic factors and abnormal androgen levels. Among them, abnormal androgen levels are mainly manifested in the type II 5α reductase activity in hair loss areas that is significantly higher than in non-hair loss areas. Androgens are converted into dihydrotestosterone under the action of 5α reductase. Increased dihydrotestosterone content can make hair follicles miniaturized. , the thick black terminal hair gradually turns into light-colored vellus hair, and eventually the hair follicles shrink and disappear, clinically manifesting as hair loss. Currently, the U.S. Food and Drug Administration has approved only two drugs for the treatment of androgenetic alopecia, namely minoxidil topical preparation and finasteride oral preparation. Among them, the mechanism of action of minoxidil has not been clearly elucidated, and it is more inconvenient to use; finasteride is a type II 5α reductase inhibitor, thereby inhibiting hair loss, but it can easily cause sex-related side effects.
爱普列特(Epristeride，化学名为17-β(N-叔丁基-氨基-甲酰基)雄甾-3,5-二烯-3-羧酸)是一种新型非竞争性5α还原酶抑制剂。爱普列特与5α还原酶、NADP形成三元复合物，抑制睾酮向双氢睾酮(DHT)的转化，从而使其双氢睾酮含量下降。目前国内临床上用于良性前列腺增生的治疗，为口服片剂，推荐剂量为每天2次，每次5mg。长期服用可使前列腺体积缩小，排尿阻力降低，从而减轻膀胱流出道梗阻以提高尿流率，减少残余尿量，达到症状改善的目的。Epristeride (chemical name: 17-β(N-tert-butyl-amino-formyl)androsta-3,5-diene-3-carboxylic acid) is a new type of non-competitive 5α reductase Inhibitors. Aprelite forms a ternary complex with 5α reductase and NADP, which inhibits the conversion of testosterone into dihydrotestosterone (DHT), thereby reducing the content of dihydrotestosterone. Currently, it is used clinically in China for the treatment of benign prostatic hyperplasia. It is an oral tablet, and the recommended dose is 5 mg twice a day. Long-term use can reduce the size of the prostate and reduce urinary resistance, thereby reducing bladder outflow obstruction, increasing urinary flow rate, reducing residual urine volume, and improving symptoms.
非那雄胺(Finasteride)是一种4-氮杂甾体化合物，细胞内II型5α还原酶特异性抑制剂，抑制睾酮代谢为双氢睾酮，能有效减少血液和前列腺及皮肤等组织中双氢睾酮的含量。临床上被批准用于治疗良性前列腺增生(5mg规格)和雄激素性脱发(1mg规格)。度他雄胺(Dutasteride)为I型和II型5α还原酶抑制剂，同样通过抑制睾酮转化为双氢睾酮，进而抑制良性前列腺增生患者前列腺的生长。临床使用剂型为胶囊剂，推荐用量0.5mg/天。目前，0.5mg/天剂量的口服制剂度他雄胺已被韩国食品药品安全部批准用于雄激素性脱发的治 疗。Finasteride is a 4-azasteroid compound and a specific inhibitor of intracellular type II 5α reductase. It inhibits the metabolism of testosterone into dihydrotestosterone and can effectively reduce the levels of dihydrotestosterone in the blood, prostate, skin and other tissues. Hydrotestosterone content. It is clinically approved for the treatment of benign prostatic hyperplasia (5 mg strength) and androgenic alopecia (1 mg strength). Dutasteride is a type I and type II 5α reductase inhibitor. It also inhibits the conversion of testosterone into dihydrotestosterone, thereby inhibiting the growth of the prostate in patients with benign prostatic hyperplasia. The dosage form for clinical use is capsule, and the recommended dosage is 0.5mg/day. Currently, the oral preparation dutasteride at a dose of 0.5 mg/day has been approved by the Korean Ministry of Food and Drug Safety for the treatment of androgenic alopecia.
结合雄激素性脱发的致病原因及5α还原酶抑制剂非那雄胺已批准用于治疗雄激素性脱发，推测具有相同作用机制的爱普列特具有潜在治疗雄激素性脱发的作用，目前尚未有对含爱普列特的组合物进行药效学考察的报道。Combining the causative factors of androgenetic alopecia and the 5α-reductase inhibitor finasteride has been approved for the treatment of androgenetic alopecia, it is speculated that Aprelite, which has the same mechanism of action, has the potential to treat androgenetic alopecia. Currently, There have been no reports on the pharmacodynamics of compositions containing Aprelite.
发明内容Contents of the invention
针对现有技术存在的上述问题，本发明所要解决的技术问题在于提供一种用于治疗雄激素性脱发的药物。In view of the above-mentioned problems existing in the prior art, the technical problem to be solved by the present invention is to provide a medicine for treating androgenic alopecia.
为了解决上述技术问题，本发明所采用的技术方案如下：In order to solve the above technical problems, the technical solutions adopted by the present invention are as follows:
一种用于治疗雄激素性脱发的药物，所述药物的有效成分为爱普列特，或爱普列特和非那雄胺，或爱普列特和度他雄胺，或爱普列特、非那雄胺和度他雄胺，所述药物的有效成分的每日施用剂量为0.01-1mg。A drug for treating androgenic alopecia, the active ingredient of which is Apretide, or Apretide and finasteride, or Apretide and dutasteride, or Apretide Specifically, finasteride and dutasteride, the daily dosage of the active ingredient of the medicine is 0.01-1 mg.
作为优选：其配方如下：As a preferred option: the formula is as follows:
普列特单用药物：爱普列特0.01mg到1mg；Aplitide single-use drug: Aplitide 0.01mg to 1mg;
爱普列特组合物1：爱普列特0.01mg到0.5mg，非那雄胺0.01mg到0.5mg；Aprelite composition 1: Aprelite 0.01mg to 0.5mg, finasteride 0.01mg to 0.5mg;
爱普列特组合物2：爱普列特0.01mg到0.5mg，度他雄胺0.01mg到0.5mg；Aprelite composition 2: Aprelite 0.01mg to 0.5mg, Dutasteride 0.01mg to 0.5mg;
爱普列特组合物3：爱普列特0.01mg到0.3mg，非那雄胺0.01mg到0.3mg；度他雄胺0.01mg到0.3mg。Aprelite composition 3: Aprelite 0.01mg to 0.3mg, finasteride 0.01mg to 0.3mg; dutasteride 0.01mg to 0.3mg.
进一步的，所述药物的有效成分的每日施用剂量为0.05-0.5mg。Further, the daily dosage of the active ingredient of the drug is 0.05-0.5 mg.
作为优选：其配方如下：As a preferred option: the formula is as follows:
爱普列特单用药物：爱普列特0.05mg到0.5mg；Aprelite single drug: Aprelite 0.05mg to 0.5mg;
爱普列特组合物1：爱普列特0.05mg到0.2mg，非那雄胺0.01mg到0.2mg；Aprelite composition 1: Aprelite 0.05mg to 0.2mg, finasteride 0.01mg to 0.2mg;
爱普列特组合物2：爱普列特0.05mg到0.2mg，度他雄胺0.01mg到0.2mg；Aprelite composition 2: Aprelite 0.05mg to 0.2mg, dutasteride 0.01mg to 0.2mg;
爱普列特组合物3：爱普列特0.05mg到0.15mg，非那雄胺0.01mg到0.1mg；度他雄胺0.01mg到0.1mg。Aprelite composition 3: Aprelite 0.05mg to 0.15mg, finasteride 0.01mg to 0.1mg; dutasteride 0.01mg to 0.1mg.
进一步的，所述药物的有效成分的每日施用剂量为0.15mg。Further, the daily dosage of the active ingredient of the drug is 0.15 mg.
作为优选：其配方如下：As a preferred option: the formula is as follows:
爱普列特单用药物：爱普列特0.15mg；Aprelite single drug: Aprelite 0.15mg;
爱普列特组合物1：爱普列特0.1mg，非那雄胺0.05mg；Aprelite composition 1: Aprelite 0.1mg, finasteride 0.05mg;
爱普列特组合物2：爱普列特0.1mg，度他雄胺0.05mg；Aprelite composition 2: Aprelite 0.1 mg, dutasteride 0.05 mg;
爱普列特组合物3：爱普列特0.1mg，非那雄胺0.025mg；度他雄胺0.025mg。Aprelite composition 3: Aprelite 0.1 mg, finasteride 0.025 mg; dutasteride 0.025 mg.
进一步的，所述药物的有效成分为爱普列特、非那雄胺和度他雄胺三元复配，其每日施用剂量分别为爱普列特0.1mg、非那雄胺0.025mg、度他雄胺0.025mg。Further, the active ingredients of the drug are a three-component compound of aprete, finasteride and dutasteride, and the daily dosage is respectively 0.1 mg of aprete, 0.025 mg of finasteride, and Dutasteride 0.025mg.
进一步的，利用羧甲基纤维素钠溶液稀释所述药物的有效成分。Further, the active ingredient of the drug is diluted with carboxymethyl cellulose sodium solution.
作为优选，利用0.5wt.％羧甲基纤维素钠溶液稀释所述药物的有效成分。Preferably, the active ingredient of the drug is diluted with 0.5 wt.% sodium carboxymethylcellulose solution.
用于治疗雄激素性脱发的药物的制备方法如下：按配方称取的爱普列特及非那雄胺、度他雄胺，溶于的0.5wt.％羧甲基纤维素钠溶液中，震荡摇匀，室温下保存。The preparation method of the drug for treating androgenetic alopecia is as follows: Aprelite, finasteride, and dutasteride weighed according to the formula are dissolved in a 0.5wt.% carboxymethylcellulose sodium solution, Shake well and store at room temperature.
一种用于治疗雄激素性脱发的药物制剂，也在本申请的保护范围内，所述药物制剂包括所述的药物的有效成分和制剂用辅料。A pharmaceutical preparation for treating androgenic alopecia is also within the protection scope of this application. The pharmaceutical preparation includes the active ingredients of the drug and preparation auxiliary materials.
所述的药物或所述的药物制剂在制备预防和/或治疗雄激素性脱发产品中的应用。Application of the described medicine or the described pharmaceutical preparation in the preparation of products for preventing and/or treating androgenic alopecia.
相比于现有技术，本发明的有益效果为：Compared with the existing technology, the beneficial effects of the present invention are:
本发明提供了一种新型用于治疗雄激素性脱发的5α还原酶抑制剂爱普列特单用药物及其组合物，能显著促进新生毛囊生长，在治疗脱发、促进毛发生长方面效果显著；安全性好，见效快；工艺简单，易于制备。The invention provides a new type of 5α reductase inhibitor aprelite single-use drug for treating androgenic alopecia and its composition, which can significantly promote the growth of new hair follicles and has significant effects in treating hair loss and promoting hair growth; It has good safety and quick effect; the process is simple and easy to prepare.
图1为本发明的小鼠背部毛发生长情况图；图中，Day-1为给药前一天，Day 12为给药后的第12天，Day 18为给药后的第18天。Figure 1 is a diagram of the hair growth on the back of mice of the present invention; in the figure, Day-1 is the day before administration, Day 12 is the 12th day after administration, and Day 18 is the 18th day after administration.
下面结合具体实施例对本发明进一步进行描述。The present invention will be further described below with reference to specific embodiments.
以下实施例所使用的试剂和材料为：睾酮：购自北京索莱宝科技有限公司；羧甲基纤维素钠、聚山梨酯80：购自国药集团医药股份有限公司；阿佛丁：购自Sigma公司；爱普列特：来自江苏联环药业股份有限公司；非那雄胺、度他雄胺：购自阿拉丁试剂公司。The reagents and materials used in the following examples are: Testosterone: purchased from Beijing Solebao Technology Co., Ltd.; sodium carboxymethylcellulose and polysorbate 80: purchased from Sinopharm Pharmaceutical Co., Ltd.; Avertin: purchased from Sigma Company; Aprelite: from Jiangsu Lianhuan Pharmaceutical Co., Ltd.; Finasteride and Dutasteride: purchased from Aladdin Reagent Company.
实施例1药物制备方法Example 1 Drug Preparation Method
单用5α还原酶抑制剂爱普列特，或与非那雄胺或度他雄胺中的一种或两种联合施用。按照分组分为：爱普列特单用组、爱普列特组合物1、爱普列特组 合物2和爱普列特组合物3，具体配方如下：The 5-alpha reductase inhibitor ipralide is administered alone or in combination with one or both of finasteride or dutasteride. According to the grouping, it is divided into: Aprelite single use group, Aprelite composition 1, Aprelite composition 2 and Aprelite composition 3. The specific formula is as follows:
爱普列特单用药物：爱普列特0.01mg到1mg；Aprelite single drug: Aprelite 0.01mg to 1mg;
爱普列特组合物1：爱普列特0.01mg到0.5mg，非那雄胺0.01mg到0.5mg；Aprelite composition 1: Aprelite 0.01mg to 0.5mg, finasteride 0.01mg to 0.5mg;
爱普列特组合物2：爱普列特0.01mg到0.5mg，度他雄胺0.01mg到0.5mg；Aprelite composition 2: Aprelite 0.01mg to 0.5mg, Dutasteride 0.01mg to 0.5mg;
爱普列特组合物3：爱普列特0.01mg到0.3mg，非那雄胺0.01mg到0.3mg；度他雄胺0.01mg到0.3mg。Aprelite composition 3: Aprelite 0.01mg to 0.3mg, finasteride 0.01mg to 0.3mg; dutasteride 0.01mg to 0.3mg.
称取适量的爱普列特及非那雄胺、度他雄胺，溶于适量的0.5％羧甲基纤维素钠溶液中，震荡摇匀。配置后使用。Weigh an appropriate amount of Aprelate, finasteride, and dutasteride, dissolve them in an appropriate amount of 0.5% sodium carboxymethyl cellulose solution, and shake well. Use after configuration.
实施例2药物制备方法Example 2 Drug Preparation Method
单用5α还原酶抑制剂爱普列特，或与非那雄胺或度他雄胺中的一种或两种联合施用。按照分组分为：爱普列特单用组、爱普列特组合物1、爱普列特组合物2和爱普列特组合物3，具体配方如下：The 5-alpha reductase inhibitor ipralide is administered alone or in combination with one or both of finasteride or dutasteride. According to the grouping, it is divided into: Aprelite single use group, Aprelite composition 1, Aprelite composition 2 and Aprelite composition 3. The specific formula is as follows:
爱普列特单用药物：爱普列特0.05mg到0.5mg；Aprelite single drug: Aprelite 0.05mg to 0.5mg;
爱普列特组合物1：爱普列特0.05mg到0.2mg，非那雄胺0.01mg到0.2mg；Aprelite composition 1: Aprelite 0.05mg to 0.2mg, finasteride 0.01mg to 0.2mg;
爱普列特组合物2：爱普列特0.05mg到0.2mg，度他雄胺0.01mg到0.2mg；Aprelite composition 2: Aprelite 0.05mg to 0.2mg, dutasteride 0.01mg to 0.2mg;
爱普列特组合物3：爱普列特0.05mg到0.15mg，非那雄胺0.01mg到0.1mg；度他雄胺0.01mg到0.1mg。Aprelite composition 3: Aprelite 0.05mg to 0.15mg, finasteride 0.01mg to 0.1mg; dutasteride 0.01mg to 0.1mg.
称取适量的爱普列特及非那雄胺、度他雄胺，溶于适量的0.5％羧甲基纤维素钠溶液中，震荡摇匀。配置后使用。Weigh an appropriate amount of Aprelate, finasteride, and dutasteride, dissolve them in an appropriate amount of 0.5% sodium carboxymethyl cellulose solution, and shake well. Use after configuration.
实施例3药物制备方法Example 3 Drug Preparation Method
单用5α还原酶抑制剂爱普列特，或与非那雄胺或度他雄胺中的一种或两种联合施用。按照分组分为：爱普列特单用组、爱普列特组合物1、爱普列特组合物2和爱普列特组合物3，具体配方如下：The 5-alpha reductase inhibitor ipralide is administered alone or in combination with one or both of finasteride or dutasteride. According to the grouping, it is divided into: Aprelite single use group, Aprelite composition 1, Aprelite composition 2 and Aprelite composition 3. The specific formula is as follows:
爱普列特单用药物：爱普列特0.15mg；Aprelite single drug: Aprelite 0.15mg;
爱普列特组合物1：爱普列特0.1mg，非那雄胺0.05mg；Aprelite composition 1: Aprelite 0.1mg, finasteride 0.05mg;
爱普列特组合物2：爱普列特0.1mg，度他雄胺0.05mg；Aprelite composition 2: Aprelite 0.1 mg, dutasteride 0.05 mg;
爱普列特组合物3：爱普列特0.1mg，非那雄胺0.025mg；度他雄胺0.025mg。Aprelite composition 3: Aprelite 0.1 mg, finasteride 0.025 mg; dutasteride 0.025 mg.
称取适量的爱普列特及非那雄胺、度他雄胺，溶于适量的0.5％羧甲基纤维素钠溶液中，震荡摇匀。配置后使用。Weigh an appropriate amount of Aprelate, finasteride, and dutasteride, dissolve them in an appropriate amount of 0.5% sodium carboxymethyl cellulose solution, and shake well. Use after configuration.
实施例2药效验证Example 2 Medicinal efficacy verification
8周龄左右的C57BL/6雌鼠(购自北京维通利华公司)分笼适应性喂养1周后，在试验的Day-1(给药前一天)，采用腹腔注射阿佛丁溶液麻醉；电动剃刀剃去小鼠背部毛发后，再涂抹脱毛膏脱毛；所有小鼠脱毛后，按脱毛后背部皮肤情况随机分组，每组5只小鼠。Day 1(给药当天)开始，造模组皮下注射造模剂(1mg睾酮，混悬于10％聚山梨酯80溶液)，每七天造模五天，对照组注射相应溶剂对照。给药组按计划每天灌胃给予小鼠0.1mL相应药物。C57BL/6 female mice about 8 weeks old (purchased from Beijing Vitong Lever Company) were adaptively fed in separate cages for 1 week. On Day-1 of the test (the day before drug administration), they were anesthetized by intraperitoneal injection of Avertin solution. After shaving the hair on the back of the mice with an electric razor, apply depilatory cream to remove the hair. After all mice were depilated, they were randomly divided into groups according to the condition of their back skin after depilation, with 5 mice in each group. Starting from Day 1 (the day of administration), the modeling group was subcutaneously injected with a modeling agent (1mg testosterone, suspended in 10% polysorbate 80 solution). Modeling was performed every seven days for five days, and the control group was injected with the corresponding solvent control. In the drug administration group, mice were given 0.1 mL of the corresponding drug by gavage every day as planned.
小鼠每周称量2次体重，并在Day-1、Day 12、Day 18拍照记录小鼠背部毛发生长状态。The mice were weighed twice a week, and photos were taken on Day-1, Day 12, and Day 18 to record the hair growth status on the back of the mice.
动物分组情况如下表1所示：The animal grouping is shown in Table 1 below:
表1Table 1
结束后根据动物福利将小鼠安乐处死。取各组小鼠背部皮肤浸泡于4％多聚甲醛中固定，石蜡包埋切片，HE染色，光镜下观察，每张片在高倍镜下选取4 个视野进行毛囊计数，每个视野不重叠。After completion, the mice were euthanized according to animal welfare. The back skin of mice from each group was soaked in 4% paraformaldehyde and fixed, embedded in paraffin, sectioned, stained with HE, and observed under a light microscope. For each slice, 4 fields of view were selected for counting of hair follicles under a high-power microscope. Each field of view did not overlap. .
采用SPSS13.0统计软件进行方差分析，统计平均值±标准差(Mean±SD)，两组间比较采用独立样本t检验，p<0.05具有统计学差异。SPSS13.0 statistical software was used for analysis of variance, and the statistical mean ± standard deviation (Mean ± SD) was used. The independent sample t test was used for comparison between the two groups, and p<0.05 was considered statistically different.
根据毛发生长评分指标：0分，no growth；1分，<20％growth；2分，20–40％growth；3分，40–60％growth；4分，60–80％growth；5分，80–100％growth进行评分。According to the hair growth scoring index: 0 points, no growth; 1 points, <20% growth; 2 points, 20–40% growth; 3 points, 40–60% growth; 4 points, 60–80% growth; 5 points, Score 80–100% growth.
各组小鼠背部毛发生长情况如图1和表2所示：The hair growth on the back of mice in each group is shown in Figure 1 and Table 2:
表2Table 2
注：#，p<0.05vs空白对照组；###，p<0.001vs空白对照组；*，p<0.05vs模型组；***，p<0.001vs模型组。Note: #, p<0.05 vs blank control group; ###, p<0.001 vs blank control group; *, p<0.05 vs model group; ***, p<0.001 vs model group.
各组小鼠背部毛囊数如表3所示：The number of hair follicles on the back of mice in each group is shown in Table 3:
表3table 3
| 组别Group | Day 18毛囊计数Day 18 hair follicle count |
| 空白对照组Blank control group | 32.0±2.532.0±2.5 |
| 模型组model group | 23.6±3.1 ## 23.6±3.1 ## |
| 爱普列特单用组Aiplite single use set | 26.0±7.326.0±7.3 |
| 爱普列特组合物1Aiplite composition 1 | 29.6±7.129.6±7.1 |
| 爱普列特组合物2Aiplite composition 2 | 29.0±6.229.0±6.2 |
| 爱普列特组合物3Aiplite Composition 3 | 30.8±5.9*30.8±5.9* |
注：##，p<0.01vs空白对照组；*，p<0.05vs模型组。Note: ##, p<0.01 vs blank control group; *, p<0.05 vs model group.
结果表明，爱普列特单独或与非那雄胺、度他雄胺中的一种或两种联合灌 胃给予野生型小鼠后，能有效促进脱发小鼠毛发的生长；且试验过程中未见小鼠出现任何不良反应，说明药物安全性较好。The results show that after intragastric administration of Aprelite alone or in combination with one or both of finasteride and dutasteride to wild-type mice, it can effectively promote hair growth in alopecia mice; and during the test No adverse reactions were seen in mice, indicating that the drug is safe.
以上详细描述了本发明的优选实施方式，但是，本发明并不局限于此。在本发明的技术构思范围内，可以对本发明的技术方案进行多种简单变型，包括各个技术特征以任何其它的合适方式进行组合，这些简单变型和组合同样应当视为本发明所公开的内容，均属于本发明的保护范围。The preferred embodiments of the present invention are described in detail above, but the present invention is not limited thereto. Within the scope of the technical concept of the present invention, many simple modifications can be made to the technical solution of the present invention, including the combination of various technical features in any other suitable manner. These simple modifications and combinations should also be regarded as the disclosed content of the present invention. All belong to the protection scope of the present invention.
Claims (8)
- 一种用于治疗雄激素性脱发的药物，其特征在于，所述药物的有效成分为爱普列特，或爱普列特和非那雄胺，或爱普列特和度他雄胺，或爱普列特、非那雄胺和度他雄胺，所述药物的有效成分的每日施用剂量为0.01-1mg。A medicine for treating androgenetic alopecia, characterized in that the active ingredient of the medicine is ipremide, or ipremide and finasteride, or ipremide and dutasteride, Or Aprelate, Finasteride and Dutasteride, the daily dosage of the active ingredients of the drugs is 0.01-1 mg.
- 根据权利要求1所述的用于治疗雄激素性脱发的药物，其特征在于，所述药物的有效成分的每日施用剂量为0.05-0.5mg。The medicine for treating androgenic alopecia according to claim 1, wherein the daily dosage of the active ingredient of the medicine is 0.05-0.5 mg.
- 根据权利要求1所述的用于治疗雄激素性脱发的药物，其特征在于，所述药物的有效成分的每日施用剂量为0.15mg。The medicine for treating androgenetic alopecia according to claim 1, wherein the daily dosage of the active ingredient of the medicine is 0.15 mg.
- 根据权利要求1所述的用于治疗雄激素性脱发的药物，其特征在于，所述药物的有效成分为爱普列特、非那雄胺和度他雄胺三元复配，其每日施用剂量分别为爱普列特0.1mg、非那雄胺0.025mg、度他雄胺0.025mg。The medicine for treating androgenetic alopecia according to claim 1, characterized in that the active ingredient of the medicine is a three-component compound of aprete, finasteride and dutasteride, and its daily The dosages used were 0.1 mg of Apremide, 0.025 mg of Finasteride, and 0.025 mg of Dutasteride.
- 根据权利要求1所述的用于治疗雄激素性脱发的药物，其特征在于，利用羧甲基纤维素钠溶液稀释所述药物的有效成分。The medicine for treating androgenic alopecia according to claim 1, characterized in that the active ingredient of the medicine is diluted with sodium carboxymethylcellulose solution.
- 根据权利要求5所述的用于治疗雄激素性脱发的药物，其特征在于，利用0.5wt.％羧甲基纤维素钠溶液稀释所述药物的有效成分。The medicine for treating androgenic alopecia according to claim 5, characterized in that the active ingredient of the medicine is diluted with 0.5wt.% carboxymethylcellulose sodium solution.
- 一种用于治疗雄激素性脱发的药物制剂，其特征在于，所述药物制剂包括权利要求1-6任意一项权利要求所述的药物的有效成分和制剂用辅料。A pharmaceutical preparation for treating androgenic alopecia, characterized in that the pharmaceutical preparation includes the active ingredient of the medicine described in any one of claims 1 to 6 and the auxiliary materials for the preparation.
- 权利要求1至6任一项权利要求所述的药物或权利要求7所述的药物制剂在制备预防和/或治疗雄激素性脱发产品中的应用。Application of the medicine according to any one of claims 1 to 6 or the pharmaceutical preparation according to claim 7 in the preparation of products for preventing and/or treating androgenic alopecia.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210436544.7 | 2022-04-22 | ||
| CN202210436544.7A CN114917234A (en) | 2022-04-22 | 2022-04-22 | Medicine for treating androgenetic alopecia |
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| Publication Number | Publication Date |
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| WO2023201858A1 true WO2023201858A1 (en) | 2023-10-26 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/CN2022/097218 WO2023201858A1 (en) | 2022-04-22 | 2022-06-06 | Medication for treating androgenetic alopecia |
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| Country | Link |
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| CN (1) | CN114917234A (en) |
| WO (1) | WO2023201858A1 (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1899290A (en) * | 2006-07-27 | 2007-01-24 | 江苏联环药业股份有限公司 | Epristeride slow release preparation |
| CN1965839A (en) * | 2005-11-15 | 2007-05-23 | 上海医药工业研究院 | Sustained release microsphere of finasteride and its analogue, preparation process and use thereof |
| CN101596318A (en) * | 2008-06-04 | 2009-12-09 | 北京普润生物科技发展有限公司 | The external preparation of treatment androgens psilosis and seborrheic dermatitis, acne |
| CN102038658A (en) * | 2009-10-20 | 2011-05-04 | 江苏联环药业股份有限公司 | Epristeride tablets with high dissolution rate and preparation method thereof |
-
2022
- 2022-04-22 CN CN202210436544.7A patent/CN114917234A/en active Pending
- 2022-06-06 WO PCT/CN2022/097218 patent/WO2023201858A1/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1965839A (en) * | 2005-11-15 | 2007-05-23 | 上海医药工业研究院 | Sustained release microsphere of finasteride and its analogue, preparation process and use thereof |
| CN1899290A (en) * | 2006-07-27 | 2007-01-24 | 江苏联环药业股份有限公司 | Epristeride slow release preparation |
| CN101596318A (en) * | 2008-06-04 | 2009-12-09 | 北京普润生物科技发展有限公司 | The external preparation of treatment androgens psilosis and seborrheic dermatitis, acne |
| CN102038658A (en) * | 2009-10-20 | 2011-05-04 | 江苏联环药业股份有限公司 | Epristeride tablets with high dissolution rate and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| GANG ZHOU: "How to choose and use the six types of seborrheic alopecia drugs", GOOD DOCTOR ONLINE, 29 August 2018 (2018-08-29), XP093102137, Retrieved from the Internet <URL:https://m.haodf.com/neirong/wenzhang/6708287745.html> [retrieved on 20231116] * |
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| CN114917234A (en) | 2022-08-19 |
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