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KR-102964698-B1 - A compound for the use of subcutaneous injection in the scalp dermis for the improvement of male hair loss and a method of manufacturing the compound

KR102964698B1KR 102964698 B1KR102964698 B1KR 102964698B1KR-102964698-B1

Abstract

The present invention relates to a composition for subcutaneous injection into the dermis of the scalp for improving male pattern baldness, and more specifically, to a composition for subcutaneous injection into the dermis of the scalp for improving male pattern baldness that is characterized by having a significantly higher absorption rate in the body than the method through oral administration by configuring the composition for subcutaneous injection differently from conventional compositions (oral administration form) using finasteride or dutasteride for preventing hair loss or stimulating hair growth, while eliminating side effects by eliminating cytotoxic reactions by using less than 2% of ethanol.

Inventors

  • 유화정

Dates

Publication Date
20260513
Application Date
20250515

Claims (7)

  1. As a composition for subcutaneous injection, The above composition is, Based on the total weight of the above composition, it comprises 0.01 wt% to 0.1 wt% of dutasteride, 0.5 wt% to 2 wt% of polysorbate 80, 0.01 wt% to 2 wt% of ethanol, and 95.9 wt% to 99.48 wt% of normal saline. The above dutasteride is dissolved in ethanol, polysorbate 80 is added to the resulting solution, and physiological saline is added in small amounts to the additive containing polysorbate 80 while mixing to prepare the product. A composition for intradermal subcutaneous injection of the scalp for improving male pattern baldness, characterized in that the above mixing is performed for 4 to 6 minutes so as not to destroy micelles through a sonicator.
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  3. In a method for preparing a composition for subcutaneous injection, A dissolution step (100) in which dutasteride is first dissolved in ethanol so that micelles can be formed; An addition step (200) of adding polysorbate 80 to the dissolved product produced through the above dissolution step (100); and A mixing step (300) comprising adding small amounts of physiological saline to the additive to which Polysorbate 80 has been added through the above addition step (200), and mixing for 4 to 6 minutes using a sonicator so as not to destroy the micelles; wherein A method for preparing a composition for intradermal subcutaneous injection of the scalp for improving male pattern baldness, characterized in that, based on the total weight of the composition, the dutasteride, ethanol, polysorbate 80, and physiological saline used in the dissolution, addition, and mixing steps are 0.01% to 0.1% by weight, the ethanol is 0.01% to 2% by weight, the polysorbate 80 is 0.5% to 2% by weight, and the physiological saline is 95.9% to 99.48% by weight.
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Description

A compound for the use of subcutaneous injection in the scalp dermis for the improvement of male hair loss and a method of manufacturing the compound The present invention relates to a composition for subcutaneous injection into the dermis of the scalp for improving male pattern baldness, and more specifically, to a composition for subcutaneous injection into the dermis of the scalp for improving male pattern baldness that is characterized by having a significantly higher absorption rate in the body than the method through oral administration by configuring the composition for subcutaneous injection differently from conventional compositions (oral administration form) using finasteride or dutasteride for preventing hair loss or stimulating hair growth, while eliminating side effects by eliminating cytotoxic reactions by using less than 2% of ethanol. According to studies conducted to date, the causes of hair loss have been identified as including endocrine disorders such as hormonal imbalances, autoimmune nervous system disorders, excessive sebum production caused by circulatory system disorders such as blood circulation disorders, nutritional deficiencies of hair roots, allergies, bacterial infections, genetic factors, psychological stress, environmental factors such as air pollution or food, and aging. Products sold as hair growth stimulants or anti-hair loss agents for hair include growth cycle induction effects, hair growth cycle extension effects, 5α-reductase inhibition effects, blood circulation promotion effects, antiseptic effects, anti-dandruff effects, moisturizing effects, antioxidant effects, etc., but the anti-hair loss and hair growth stimulating effects of conventional formulations are not sufficient. Male pattern baldness is influenced by male hormones and is therefore directly related to the amount of male hormones. In particular, 5α-reductase is the enzyme responsible for the conversion of testosterone, a male sex hormone, into dihydrotestosterone (DHT). DHT is an androgenic compound that causes hyperandrogenic conditions, such as the enlargement of the prostate gland—known as "benign prostatic hyperplasia"—in men as they age. Another consequence of increased DHT levels is androgenic alopecia (AA), commonly referred to as "male pattern baldness." The cause of male pattern baldness is the excessive synthesis of DHT by the action of 5α-reductase, and therefore, it is possible to effectively prevent and treat male pattern baldness by inhibiting the activity of 5α-reductase. Currently, two treatments are approved by the U.S. Food and Drug Administration for the treatment of androgenetic alopecia (AA) in men: topical minoxidil and oral finasteride. Minoxidil (which has the chemical name 6-piperidin-1-ilpyrimidine-2,4-diamine3-oxide) is an arterial vasodilator, and finasteride is a type II 5α-reductase inhibitor. In this case, minoxidil was developed to lower blood pressure in hypertensive patients, but it is most widely used as a hair growth drug because its use changed due to hair growth side effects that occurred during use. The mechanism of action of minoxidil has not been clearly elucidated. However, the mechanism of action of minoxidil has been explained by the hypothesis that minoxidil stimulates hair growth by increasing blood flow to the hair follicles to induce increased blood flow, and the hypothesis that minoxidil acts directly on the hair follicle epithelium to induce hair growth. However, hair growth products containing minoxidil must be applied several times a day to maintain the hair growth effect, which is very cumbersome and easy to forget. Therefore, in many cases, the hair growth effect is not sufficiently achieved due to irregular application and arbitrary discontinuation of treatment. Finasteride is a drug that inhibits type II 5α-reductase, which converts testosterone, one of the male hormones, into DHT, which causes hair loss. Oral finasteride 1 mg used for androgenetic alopecia may cause sexual side effects even after discontinuation of use. Therefore, the USFDA has advised caution for healthcare professionals and patients. As a result of reviewing post-marketing cases reported to the FDA’s Adverse Event Reporting System (AERS) and the safety database of marketed products, it was found that some sexual function-related adverse reactions (e.g., decreased libido, ejaculatory dysfunction, orgasmic dysfunction) persisted after discontinuation of use. Another compound in the aforementioned class of 5α-reductase inhibitors is dutasteride. Dutasteride has the chemical name (5α,17β)-N-{2,5-bis(trifluoromethyl)phenyl}-3-oxo-4-azaanthrost-1-en-17-carboxamide. The structural formula is shown as follows. Dutasteride is a selective inhibitor of both type I and type II isoforms of the steroid 5α-reductase (5AR), an intracellular enzyme that converts testosterone into 5α-dihydrotestosterone (DHT), and is a synthetic 4-azosteroid compound indicated for the treatment of symptomatic beni