CN107362131A - A kind of Estradilum and preparation method - Google Patents

A kind of Estradilum and preparation method Download PDF

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Publication number
CN107362131A
CN107362131A CN201710769456.8A CN201710769456A CN107362131A CN 107362131 A CN107362131 A CN 107362131A CN 201710769456 A CN201710769456 A CN 201710769456A CN 107362131 A CN107362131 A CN 107362131A
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CN
China
Prior art keywords
estradilum
auxiliary material
estradiol
major ingredient
ingredient
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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CN201710769456.8A
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Chinese (zh)
Inventor
刘晓霞
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Beijing Hai Xia Run Menopause Syndrome Medical Research Institute
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Beijing Hai Xia Run Menopause Syndrome Medical Research Institute
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Priority to CN201710769456.8A priority Critical patent/CN107362131A/en
Publication of CN107362131A publication Critical patent/CN107362131A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to skin care products technical field, more particularly to a kind of Estradilum and preparation method, the Estradilum includes major ingredient and auxiliary material;Major ingredient includes, estradiol;L40 or azone;Carbomer;Auxiliary material includes:Ethanol, propane diols, distilled water and triethanolamine.The invention has the advantages that:Major ingredient is basic material and important part in gel, it plays a key effect when in use, can nurse one's health menstrual disorder, chest enlarge, postpartum maintains, assisted reproduction, improve life quality, beautifying and anti-aging, prevent climacteric metancholia and regulation menopause symptom, improve metabolism, slim the abdomen accumulation, and transdermal effect is good.

Description

A kind of Estradilum and preparation method
Technical field
The present invention relates to skin care products technical field, more particularly to a kind of Estradilum and preparation method.
Background technology
One of greatest discovery of twentieth century preventive medicine is to find that female climacteric syndrome is a lack of estrogen and drawn Rise, can prevent and treat.With the quickening of Chinese population aging process, the growth rate of climacteric women population It will also further speed up.Current Chinese climacteric women has reached 1.6 hundred million, and it is deep by climacteric to have more than 100,000,000 2 thousand ten thousand women every year Syndrome troubles, and Chinese climacteric women number leaps to the first in the world.The climacteric of women quality of life is had a strong impact at present Phase problem does not obtain safe and effective treatment not only, let alone prevents, but owner both knows about, and prevention overweights treatment.
The content of the invention
Weak point present in regarding to the issue above, the present invention provide a kind of Estradilum and preparation method.
To achieve the above object, first aspect present invention provides a kind of Estradilum, including major ingredient and auxiliary material;
The major ingredient includes:
Estradiol;
L40 or azone;
Carbomer;
The auxiliary material includes:Ethanol, propane diols, distilled water and triethanolamine.
In above-mentioned Estradilum, it is preferable that each Ingredient Wt number proportioning is in the major ingredient:
The estradiol:0.02~0.2 part;
The L40 or described azones:0.5~3 part:
The carbomer:0.3~2 part.
In above-mentioned Estradilum, it is preferable that each Ingredient Wt number proportioning is in the major ingredient:
The estradiol:0.06~0.16 part;
The L40 or azone:1~2.5 part:
The carbomer:0.6~1.7 part.
In above-mentioned Estradilum, it is preferable that each Ingredient Wt number proportioning is in the major ingredient:
The estradiol:0.08~0.12 part;
The L40 or azone:1.5~2 parts:
The carbomer:0.8~1.4 part.
In above-mentioned Estradilum, it is preferable that each Ingredient Wt number proportioning is in the major ingredient:
The estradiol:0.1 part;
The L40 or azone:1.8 part:
The carbomer:1 part.
In above-mentioned Estradilum, it is preferable that Ingredient Wt number proportioning is in the auxiliary material:
10~40 parts of the ethanol;
1~10 part of the propane diols;
55~75 parts of the distilled water;
0.5~3.5 part of the triethanolamine.
In above-mentioned Estradilum, it is preferable that Ingredient Wt number proportioning is in the auxiliary material:
15~35 parts of the ethanol;
2~8 parts of the propane diols;
60~70 parts of the distilled water;
1~3 part of the triethanolamine.
In above-mentioned Estradilum, it is preferable that each Ingredient Wt number proportioning is in the auxiliary material:
20~30 parts of the ethanol;
4~6 parts of the propane diols;
65 parts of the distilled water;
2 parts of the triethanolamine.
In above-mentioned Estradilum, it is preferable that each Ingredient Wt number proportioning is in the auxiliary material:
25 parts of the ethanol;
5 parts of the propane diols.
Compared with prior art, the invention has the advantages that:
Major ingredient is basic material and important part in gel, and it plays a key effect when in use, can nurse one's health the moon Through imbalance, chest enlarge, postpartum maintenance, assisted reproduction, life quality is improved, beautifying and anti-aging, prevents climacteric metancholia and tune Menopause symptom is saved, improves metabolism, slim the abdomen accumulation, and transdermal effect is good.
Second aspect of the present invention provides a kind of preparation method of Estradilum, comprises the following steps:
(1) ethanol in the estradiol and auxiliary material in major ingredient is made into the first solution, it is standby;
(2) propane diols in the L40 or azone and auxiliary material in major ingredient is made into the first solution, it is standby;
(3) distilled water in the carbomer and auxiliary material in major ingredient, and triethanolamine are made into the first solution, it is standby;
(4) first solution, first solution and first solution are sufficiently mixed into bottling to seal, shape after standing Into required Estradilum.
The preparation side for the Estradilum that embodiment provides according to a second aspect of the present invention, by the way that major ingredient and auxiliary material are blended together First, second and third kind of solution, then three kinds of solution are mixed, it is more fully mixed, can preferably realizes the effect of Estradilum Fruit, prepare convenient and swift.
The additional aspect and advantage of the present invention will provide in following description section, partly will become bright from following description It is aobvious, or recognized by the practice of the present invention.
Brief description of the drawings
Fig. 1 is the flow chart of the preparation method of Estradilum in one embodiment of the invention.
Embodiment
To make the purpose, technical scheme and advantage of the embodiment of the present invention clearer, below in conjunction with the embodiment of the present invention In accompanying drawing, the technical scheme in the embodiment of the present invention is clearly and completely described, it is clear that described embodiment is The part of the embodiment of the present invention, rather than whole embodiments.Based on the embodiment in the present invention, ordinary skill people The every other embodiment that member is obtained on the premise of creative work is not made, belongs to the scope of protection of the invention.
First aspect present invention provides a kind of Estradilum, including major ingredient and auxiliary material;Major ingredient includes:Estradiol;L40 Or azone;Carbomer;Auxiliary material includes:Ethanol, propane diols, distilled water and triethanolamine.
The Estradilum that embodiment provides according to a first aspect of the present invention by major ingredient is formed with auxiliary material, and wherein major ingredient is Basic material and important part in gel, when in use it play a key effect, can nurse one's health menstrual disorder, chest enlarge, production After maintain, assisted reproduction, improve life quality, beautifying and anti-aging, prevent climacteric metancholia and regulation menopause symptom, change Kind metabolism, slim the abdomen accumulation.This product is that women maintains the transdermal new category of nutritional agents, the percutaneous female estrogen of estradiol Gel, special efficacy (prevention overweights treatment) especially in terms of climacteric metancholia is prevented, instead of hypofunction and the ovary work of exhaustion Make, allow women never to lack estrogen, it is good away from climacteric and disease of old people, transdermal effect.
Preferred embodiment list:
Present invention also provides the method for preparing Estradilum, comprise the following steps:
S1:Ethanol in estradiol and auxiliary material in major ingredient is made into the first solution, it is standby;
S2:Propane diols in L40 or azone and auxiliary material in major ingredient is made into the first solution, it is standby;
S3:Distilled water in carbomer and auxiliary material in major ingredient, and triethanolamine are made into the first solution, it is standby;
S4:First solution, first solution and first solution are sufficiently mixed bottling sealing, then stands and stops Put to form required Estradilum after 60-120 minutes.
The preparation side for the Estradilum that embodiment provides according to a second aspect of the present invention, by the way that major ingredient and auxiliary material are blended together First, second and third kind of solution, then three kinds of solution are mixed, it is more fully mixed, can preferably embodies the effect of Estradilum Fruit, it can preferably embody the effect of Estradilum.
First, this Estradilum acts on and is applicable crowd:
1. regulating menstruation is lacked of proper care:Menstruation is few, cycle time, extension etc. (coordinating balanced nutritious vegetarian diet).
2. chest enlarge:Good estrogen is enriched, helps chest enlarge, but is not only to be applied to chest to work (smearing), but percutaneously Be absorbed to blood and improve estradiol level function of breast augmentation in blood (applying amount and area are more important).
3. assisted reproduction and prenatal and postnatal care:Appropriate this product coordinates balanced nutritious vegetarian diet to improve ovarian follicle quality, and increase pregnancy is several Rate (Ovulation barrier sterile), increase endometrium thickness, anti-miscarriage (including biochemical miscarriage);Supplementary reproduction, test-tube baby, people Work fertilization etc. improves endometrium receptivity, improves success rate.
4. postpartum conserves:Alopecia, puerperal melancholia etc. caused by prevention postpartum estradiol is low suddenly.
5. sexual life:Increase female libido and love liquid secretion, improve life quality.
6. beautifying and anti-aging:Increase skin blood circulation, increase hyaluronic acid and collagen synthesis, increase skin thickness And elasticity, there is wrinkle resistant effect (cooperation basal nutrient).
7. prevent climacteric metancholia:Starting within 35 years old preventative use lasting on a small quantity can be with whole bodies such as rich female nourishing ovaries 400 Various Tissues cells, delay menopause, estrogen estradiol are never lacked, without climacteric.
8. treat climacteric metancholia special efficacy:Insomnia, Tidal fever with perspiration is melancholy, vexed, has palpitation, short-tempered etc..
9. ovarian dysfunction caused by a variety of causes, low estrogen level performance:Immunologic hypofunction, repeatedly vagina Inflammation, aedoeatrophia, caruncula etc..
10. the women of pair decrease in estrogen has prevention urinary calcium to lose, protects bone amount, reduces osteoporosis generation and drop The effect of low fracture rates.
11. repairing inner membrance hemostasis after medicine incomplete abortion, do and reduce the palace of the Qing Dynasty operability artificial menstrual cycle.
12. improving metabolism, (osteoporosis, senile dementia, cardiovascular and cerebrovascular diseases, three is high, colon for prevention disease of old people Cancer, the prolapse of uterus, the urinary incontinence, apparatus urogenitalis caruncula etc.).
13. slim the abdomen accumulation, recover women S type curves.
2nd, contrasted with similar effect product on the market, the advantages of this product:
1. the concentration of a female Estradilum improves (0.2%), it is ensured that its validity, improves estradiol definite effect. Estradilum before is because concentration is low (0.06%), and specification dosage is small, and daily 0.75mg estradiol dosage can not be effective Relief of symptoms, it is also easy to cause paramenia, because climacteric women ovarian function declines, estradiol production fluctuation is big, when it Endometrial growth can not be maintained when being reduced to low spot, causes the bleeding that comes off, paramenia, while inner membrance to be repaired difficult, does not allow Easily hemostasis, menostaxis reaches about 80pg/ml not to the utmost, by the supplement dosage for improving estradiol, when estradiol fluctuates in vivo Remain to supplement by external source and maintain endometrial growth, and menstruation latter stage, supplement can repair endometrium hemostasis in time in time, Effectively recover menorrhea and alleviate menopause symptom.Just because of Estradilum before has the defects of such, just fail by Doctor receives, and just fails to popularize in clinic, is improved by above-mentioned content, greatly improve its validity, doctors and patients gladly receive, non- Often it is beneficial to popularizing for the good product of such a change women's health destiny.
2. technological change:Promote transdermal agent (to refer to using pure plant bleeding agent L40:CN201310027667.6), promote Transdermal effect is 3 times of azone, the effect of more improving product.
L40:Product Status is liquid, faint yellow, slight fragrance.On the basis of S6 after 10 years constantly improve and Clinical verification, Jie Ruikang latest generation profit compatibility transdermal agents L-40 is magnificent to emerge.Top transdermal (infiltration) agent of L-40 is entirely with essence Product raw material and auxiliary material are made, and the guarantee of superelevation standard has been obtained from food-grade original, auxiliary material, security completely on the basis of S6; From the further perfect water soluble characteristic of newest supplementary material, it has the effect of oozing of good rush, water to hydrophilic and hydrophobic drug Molten effect and capacity have obtained more preferable lifting;S6 has been current optimal transdermal agent, but the technology constantly reformed causes L40 It is even better.
Packaging:500g/ bottles, characteristic:The organic solvents such as soluble in water and alcohols, lipid, it is widely used in various external preparations Type:Such as solution, emulsion, creme, essential oil, suppository, film, ointment, plaster, washing lotion, wet tissue, cosmetics.
1st, made and formed by food grade materials and auxiliary material, safest water-soluble transdermal agent.
2nd, the skin of face that is particularly suitable for use in uses, no allergic reaction.
3rd, outstanding compatibility, water, alcohols are dissolvable in water, in organic reagent.
4th, transdermal effect is optimal.
Application method:
1st, cosmetics or, the liquid material such as medicine and L-40 transdermal agents be according to 98:2 ratio is mixed evenly i.e. Can.
2nd, emulsifiable paste class bulk drug and L-40 transdermal agents are according to 98:2 ratio mixing, stirs.
3rd, it can be added in water or be used in alcohol as solution.
4th, ProductName weighs up female Estradilum, and percutaneous estradiol is rare without intestines and stomach and the first pass effect of liver Side effect, good estrogen allow women no longer to fear estrogen, are more beneficial for product promotion and numerous women are benefited.
Work out has the reason for many side effects as bad estrogen oestrone of the estradiol substitute in Clinical practice for many years; Moreover, the estradiol being orally esterified passes through after first pass effect and non-supplemental estradiol, is still a large amount of oestrone of increase, band Carry out side effect;Definition to textbook estrogen for the first time proposes objection, and women is by scientific management and suitably supplement does not have The percutaneous good estrogen estradiol gel of side effect, can promote longevity, and without climacteric, prevent and treat disease of old people, old improve comprehensively in Year women bioplasm amount;Specify medical field and detour has been walked during complementing estrogen:Past does not know what body really needed Estrogen only has estradiol, and the metabolism rubbish oestrone and estriol of estradiol are also mistakenly considered estrogen (because having a little 10-3% estrogen active because can oral absorption, alleviate menopause symptom), because estradiol be unable to oral absorption just move back and Look for second solution and develop rubbish estrogen.Past is all the time by oral estrogen come to supplement the estrogen estradiol that body loses be one Kind incorrect selection because oral estrogen (either oestrone, or esterification estradiol), it is oral after due to by hydrochloric acid in gastric juice, Enteric microorganism and the effect of liver, what is covered is not the estradiol that body lacks and really needed, but human body need not Oestrone, oestrone is directly referred to as " bad estrogen " and " female poison " by some scientists in the world, and various secondary make can occur certainly With.If percutaneously supplementing Estradilum because needing not move through stomach, enteron aisle and liver, will not by hydrochloric acid in gastric juice, enteric microorganism and Liver etc. destroys, and what is directly mended is itself natural estradiol (molecular structure and the ovarian secretion estradiol one that human body needs Sample), therefore the side effect of oestrone is not had.
Make menstruation rule normal by using Estradilum, high-quality eugenic fertility, the health in postpartum, plentiful chest Portion, the curve of S types, the sexual life of high-quality, high-quality sleep, happy mood, vigorous energy, away from involutional tired Disturb, the reduction of disease of old people.
The preferred embodiments of the present invention are these are only, are not intended to limit the invention, for those skilled in the art For member, the present invention can have various modifications and variations.Any modification within the spirit and principles of the invention, being made, Equivalent substitution, improvement etc., should be included in the scope of the protection.

Claims (10)

1. Estradilum, including major ingredient and auxiliary material;
The major ingredient includes:
Estradiol;
L40 or azone;
Carbomer;
The auxiliary material includes:Ethanol, propane diols, distilled water and triethanolamine.
2. Estradilum according to claim 1, it is characterised in that each Ingredient Wt number proportioning in the major ingredient For:
The estradiol:0.02~0.2 part;
The L40 or described azones:0.5~3 part:
The carbomer:0.3~2 part.
3. Estradilum according to claim 2, it is characterised in that each Ingredient Wt number proportioning in the major ingredient For:
The estradiol:0.06~0.16 part;
The L40 or azone:1~2.5 part:
The carbomer:0.6~1.7 part.
4. Estradilum according to claim 3, it is characterised in that each Ingredient Wt number proportioning in the major ingredient For:
The estradiol:0.08~0.12 part;
The L40 or azone:1.5~2 parts:
The carbomer:0.8~1.4 part.
5. Estradilum according to claim 4, it is characterised in that each Ingredient Wt number proportioning in the major ingredient For:
The estradiol:0.1 part;
The L40 or azone:1.8 part:
The carbomer:1 part.
6. according to the Estradilum described in claim any one of 1-5, it is characterised in that Ingredient Wt number in the auxiliary material Match and be:
10~40 parts of the ethanol;
1~10 part of the propane diols;
55~75 parts of the distilled water;
0.5~3.5 part of the triethanolamine.
7. Estradilum according to claim 6, it is characterised in that Ingredient Wt number proportioning is in the auxiliary material:
15~35 parts of the ethanol;
2~8 parts of the propane diols;
60~70 parts of the distilled water;
1~3 part of the triethanolamine.
8. Estradilum according to claim 7, it is characterised in that each Ingredient Wt number proportioning in the auxiliary material For:
20~30 parts of the ethanol;
4~6 parts of the propane diols;
65 parts of the distilled water;
2 parts of the triethanolamine.
9. Estradilum according to claim 8, it is characterised in that each Ingredient Wt number proportioning in the auxiliary material For:
25 parts of the ethanol;
5 parts of the propane diols.
10. a kind of method for preparing the Estradilum any one of claim 1-9, comprises the following steps:
(1) ethanol in the estradiol and auxiliary material in major ingredient is made into the first solution, it is standby;
(2) propane diols in the L40 or azone and auxiliary material in major ingredient is made into the first solution, it is standby;
(3) distilled water in the carbomer and auxiliary material in major ingredient, and triethanolamine are made into the first solution, it is standby;
(4) first solution, first solution and first solution are sufficiently mixed bottling sealing, institute is formed after standing The Estradilum needed.
CN201710769456.8A 2017-08-31 2017-08-31 A kind of Estradilum and preparation method Pending CN107362131A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109276539A (en) * 2018-11-08 2019-01-29 北京海霞润月更年期综合症医学研究院 A kind of testosterone gel and preparation method
CN110755370A (en) * 2019-11-07 2020-02-07 刘晓霞 Progesterone transdermal gel and its preparation method
CN110876713A (en) * 2019-11-26 2020-03-13 健民药业集团股份有限公司 Estradiol gel

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0435200A2 (en) * 1989-12-28 1991-07-03 Nitto Denko Corporation Estrogen-containing gel preparation
CN101036660A (en) * 2006-03-17 2007-09-19 武汉健民集团随州药业有限公司 Estrogen gelatin medicine and the method for preparing the same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0435200A2 (en) * 1989-12-28 1991-07-03 Nitto Denko Corporation Estrogen-containing gel preparation
CN101036660A (en) * 2006-03-17 2007-09-19 武汉健民集团随州药业有限公司 Estrogen gelatin medicine and the method for preparing the same

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
北京杰瑞康透皮剂官方: "透皮剂-化妆品用透皮剂促渗辅料", 《HTTP://BLOG.SINA.COM.CN/S/BLOG_65DC1C5B0102X95K.HTML》 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109276539A (en) * 2018-11-08 2019-01-29 北京海霞润月更年期综合症医学研究院 A kind of testosterone gel and preparation method
CN110755370A (en) * 2019-11-07 2020-02-07 刘晓霞 Progesterone transdermal gel and its preparation method
CN110876713A (en) * 2019-11-26 2020-03-13 健民药业集团股份有限公司 Estradiol gel

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Application publication date: 20171121