Product Name: Estriol
|469 °C at 760 mmHg|
|White crystalline powder|
|as per relevent regulations|
Estriol belongs to natural hormone and is the metabolite of
estradiol in vivo , anti estrogen steroids . It is mainly presented
in the urine . Estrogen has a relative small activity with the oral
activity being 6 times as high as estrone but being weaker than
estradiol with non-carcinogenic effects . After its administration
, the in vivo estradiol levels did not change . Estriol has
selective action on the vaginal and cervical canal but has no
effect on the uterus and endometrium entity .
Estriol,Animal experiments have shown that estriol has a stronger
effect on vaginal epithelial keratosis than estradiol , thus being
able to promote vaginal epithelial hyperplasia , superficial cells
keratosis , mucosal angiogenesis and vaginal epithelial wound
healing , but having a weak effect on the weight gain of mouse
uterus At the same time , estriol can enhance the function of
cervix cell , causing the cervix muscle fiber hyperplasia and
increasing the cervical elasticity and softness . In addition ,
estriol has feedback inhibition on the hypothalamus and pituitary
but does not inhibit ovulation while only having significant impact
on the corpus luteum and therefore can be used as the auxiliary
drug in the medium-term labor induction and artificial abortion and
for the treatment of various kinds of menopathy . Estriol also has
significant effect on the hematopoietic system and can reduce
vascular permeability and fragility. Therefore , it can be used for
the treatment of various kinds of hemorrhage . It also has effect
of rapidly increasing the peripheral leukocytes and generally
begins to take effect at 1 to 3 days after treatment but with a
shorter duration of action and is effective in treatment the
leukopenia induced by radiotherapy and chemotherapy .
Estradiol, or more precisely, 17β-estradiol, is a human sex hormone
and steroid, and the primary female sex hormone. It is named for
and is important in the regulation of the estrous and menstrual
female reproductive cycles. Estradiol is essential for the
development and maintenance of female reproductive tissues but it
also has important effects in many other tissues including bone.
While estrogen levels in men are lower compared to women, estrogens
have essential functions in men as well. Estradiol is found in most
vertebrates as well as many crustaceans, insects, fish, and other
animal species. Estradiol or oestradiol (American or British
English usages), derives from estra-, Gk. οστρο? (oistros,
literally meaning "verve or inspiration") and -diol, a chemical
name and suffix indicating that this form of steroid and sex
hormone is a type of alcohol bearing two hydroxyl groups.
Estradiol is produced especially within the follicles of female
ovaries, but also in other endocrine (i.e., hormone-producing) and
non-endocrine tissues (e.g., including fat, liver, adrenal, breast,
and neural tissues). Estradiol is biosynthesized from progesterone
(arrived at in two steps from cholesterol, via intermediate
pregnenolone). One principle pathway then converts progesterone to
its 17-hydroxy-derivative, and then to androstenedione via
sequential cytochrome P450-catalyzed oxidations.Action of aromatase
on this dione generates estrone, and action of a dehydrogenase on
this gives the title compound, 17β-estradiol.
|Character||White or almost white crystalline powder||White crystalline powder|
|Specific rotation||+54to +62||+59.9|
|Completeness of solution||Clear and free from undissolved solid||Conforms|
|Identification||(1) complies by IR|
(2) complies by UV
|Residue on Ignition||Not more than 0.1%||0.05%|
|Loss on drying||Not more than 0.5||0.1%|
|Total impurities not more than 2.0%||<2.0%|
|Assay||It should contain 97.0% to 102.0% of C18H24O3 calculated on dried
|Particle size||It should be 90% below 30m||Conforms|
|Conclusion||Conforms to USP36|
It can be used for treating cervicitis and especially suitable for
treating menopausal syndrome and senile vaginitis.
It can also be used as the adjuvant drug for middle-term labor
induction and artificial abortion.
It can also be used for treating prostatic hypertrophy and prostate
It still has a rapid role in increasing the peripheral leukocytes.
It generally takes effect at 1 to 3 days after the treatment but
with a short duration period. It also has efficacy in treating
leukopenia caused by chemotherapy or radiotherapy.
It can be used for reducing the vascular permeability and fragility
and can be used for the treatment of various kinds of hemorrhage.
It also has quick hemostasis effect on menorrhagia, hysterectomy or
Indications It can be used for treating cervicitis, especially
suitable for treating menopausal syndrome and senile vaginitis. It
can also be used as the adjuvant drug for middle-term labor
induction and artificial abortion. It can also be used for treating
prostatic hypertrophy and prostate cancer. In addition, it still
has a rapid role in increasing the peripheral leukocytes. It
generally takes effect at 1 to 3 days after the treatment but with
a short duration period. It also has efficacy in treating
leukopenia caused by chemotherapy or radiotherapy as well as
reducing the vascular permeability and fragility and can be used
for the treatment of various kinds of hemorrhage. It also has quick
hemostasis effect on menorrhagia, hysterectomy or tonsillectomy.
A chemical derivative of estradiol, ethinyl estradiol with maximum
dosage 200 µg, is a major component of hormonal contraceptive
devices. Combined forms of hormonal contraception contain ethinyl
estradiol and a progestin, which both contribute to the inhibition
of GnRH, LH, and FSH, which accounts for the ability of these birth
control methods to prevent ovulation and thus prevent pregnancy.
Other types of hormonal birth control contain only progestins and
no ethinyl estradiol.
Hormone replacement therapy:
If severe side effects of low levels of estradiol in a woman's
blood are experienced (commonly at the beginning of menopause or
after oophorectomy), hormone replacement therapy may be prescribed.
Such therapy is usually combined with a progestin to reduce the
risk of endometrial cancer. Estrogen therapy may be used in
treatment of infertility in women when there is a need to develop
sperm-friendly cervical mucus or an appropriate uterine lining.
This is often prescribed in combination with clomifene Estrogen
therapy can also be used to treat advanced prostate cancer, as well
as to relieve symptoms of breast cancer.
Hormone replacement therapy in transgender women:
Estrogen therapy is also used as part of the hormone replacement
therapy for trans women. Either oral or transdermal estradiol is
used in higher concentrations during initial treatment and
transition; estradiol is continued in lower doses to maintain
female-level hormones following gender reassignment surgery.
Inducing a state of hypoestrogenism may be beneficial in certain
situations where estrogens are contributing to unwanted effects,
e.g., certain forms of breast cancer, gynecomastia, premature
closure of epiphyses, and inhibiting feminization in female-to-male
transsexual hormone treatment. Estrogen levels can be reduced by
inhibiting production using gonadotropin-releasing factor agonists
(GnRH agonists) or blocking the aromatase enzyme using an aromatase
inhibitor, or with an estrogen receptor antagonist. Estriol can be
a weak or strong estrogen depending on if it is given acutely or
chronically when given to immature animals, but is an antagonist
when given in combination with estradiol.
Estriol may play a role in the development of breast cancer, but
based on in vitro research, does appea to act as an antagonist to
the G-protein coupled estrogen receptor. Though estriol is used as
part of the primarily North American phenomenon of bioidentical
hormone replacement therapy, it is not approved for use by the FDA
or Health Canada.
Safe and Effective Hormone for Women with Hot Flashes and Vaginal
Protects Against Breast and Uterine Cancers
As a Replacement Estrogen in Breast Cancer Survivors
Prevents Vaginal Atrophy and Urinary Tract Infections
Does Not Cause Blood Clots
Protects the Skin From Aging
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