What Is Testosterone Undecanoate?

Testosterone Undecanoate chemical name is 17-hydroxyandrost-4-en-3-one undecanoate, white crystal or crystalline powder; odorless, easily soluble in chloroform, It is soluble in ethanol, slightly soluble in methanol and vegetable oil, and insoluble in water. The molecular formula is C30H48O3, molecular weight is 456.70000, density is 1.038g / cm3, melting point is 39-42 ° C, and boiling point is 260-262 ° C.

Testosterone Undecanoate chemical name is 17-hydroxyandrost-4-en-3-one undecanoate, white crystal or crystalline powder; odorless, easily soluble in chloroform, It is soluble in ethanol, slightly soluble in methanol and vegetable oil, and insoluble in water. The molecular formula is C30H48O3, molecular weight is 456.70000, density is 1.038g / cm3, melting point is 39-42 ° C, and boiling point is 260-262 ° C.

Chinese name

Testosterone undecanoate

Foreign name

Testosterone Undecanoate

CAS number

5949-44-0

Molecular formula

C30H48O3

About Testosterone Undecanoate

Testosterone Undecanoate Basic Information

Chinese name: testosterone undecanoate

Chinese alias: testosterone undecanoate; testosterone undecanoate;

English name: Testosterone Undecanoate

English alias: Testosterone undecanoate

CAS number: 5949-44-0

Molecular formula: C ₃₀ H ₄₈ O ₃

Molecular weight: 456.70000

Structural formula:

Exact mass: 456.36000

PSA: 43.37000 ^[1]

LogP: 7.96090

Testosterone Undecanoate Properties

Appearance and properties: white crystalline powder

Density: 1.038g / cm ³

Melting point: 39-42 ° C (lit.)

Boiling point: 260-262 ° C (lit.)

Flash point: 150 ° F

Refractive index: 1.5836

Storage conditions: controlled substance, minus 20ºC refrigerator ^[1]

Testosterone undecanoate uses

API ^[1]

Testosterone Undecanoate Pharmacopoeia Standard

The main active ingredient of testosterone undecanoate

17-hydroxyandrost-4-en-3-one undecanoate. Calculated on dry basis, containing C30H48O3 should be 97.0% to 103.0%.

Testosterone undecanoate

White crystal or crystalline powder; odorless. It is extremely soluble in chloroform, soluble in ethanol, slightly soluble in methanol and vegetable oil, and insoluble in water. The melting point is 60-63 ° C. ^[2]

Testosterone undecanoate specific rotation

Take this product, weigh it accurately, add dioxane to dissolve and quantitatively dilute it to make a solution containing about 14mg per 1ml. According to the law, the specific rotation is + 68 ° to + 72 °. ^[2]

Testosterone undecanoate identification

(1) Take about 5mg of this product, add 1ml of sulfuric acid-ethanol (2: l) to dissolve, that is yellowish with yellow-green fluorescence.

(2) In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.

(3) The infrared light absorption spectrum of this product should be the same as that of the control ("Infrared Spectra of Medicine" 584). ^[2]

Testosterone undecanoate

relative substance

Take this product, dissolve and dilute it with mobile phase to make a solution containing about 2mg per 1ml as the test solution; take 1ml precisely, place it in a 50ml measuring flask, dilute to the mark with mobile phase, shake well, and use it as a control Solution. Except the mobile phase is acetonitrile-isopropanol-water (40:40:20), and other chromatographic conditions under the content determination, take 20l of the control solution into the liquid chromatograph, adjust the detection sensitivity, and make the main component chromatographic peaks The peak height is approximately 20% of full scale. Precisely measure 20 l each of the test solution and the reference solution, and inject them into the liquid chromatograph respectively, and record the chromatogram to 3 times the peak retention time of the main component. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak must not be greater than 0.25 times (0.5%) the area of the main peak of the control solution, and the sum of the area of each impurity peak must not be greater than the area of the main peak of the control solution (2.0%). Any peak that is less than 0.02 times the area of the main peak of the control solution in the chromatogram of the test solution can be ignored. ^[2]

Loss on drying

Take this product, use phosphorus pentoxide as desiccant, dry under reduced pressure to constant weight, and lose less than 0.5% of weight.

Determination of testosterone undecanoate

As determined by high performance liquid chromatography.

Chromatographic conditions and system suitability tests

Octadecylsilane-bonded silica gel was used as the filler; acetonitrile-isopropanol-water (43:43:14) was used as the mobile phase; the detection wavelength was 240nm. The number of theoretical plates is not less than 4000 calculated from the peak of testosterone undecanoate. ^[2]

Assay

Take this product, weigh it accurately, add methanol to dissolve and quantitatively dilute it to make a solution containing about 0.5mg per 1ml. Precisely measure 10l into the liquid chromatograph and record the chromatogram; take another testosterone undecanoate reference substance, the same The determination is based on the peak area calculated by the external standard method. ^[2]

Testosterone Undecanoate Drug Analysis

Principle introduction

Method name: Testosterone Undecanoate API-Determination of Testosterone Undecanoate-Spectrophotometry

Scope of application: This method uses spectrophotometry to determine the content of testosterone undecanoate in raw materials of testosterone undecanoate.

This method is suitable for testosterone undecanoate raw materials.

Principle of the method: A test solution is prepared by adding a test solution with absolute ethanol, and an ultraviolet-visible spectrophotometer is set, and the absorbance is measured at a wavelength of 240 nm, and the content is calculated.

Reagent production

Reagent: absolute ethanol

Equipment: UV-visible spectrophotometer

Sample preparation: 1. Preparation of reference solution

An appropriate amount of a testosterone undecanoate reference was accurately weighed, dissolved in anhydrous ethanol, and quantitatively diluted to prepare a solution containing about 10 g per microliter of the reference solution.

2. Preparation of test solution

Accurately weigh an appropriate amount of testosterone undecanoate, add absolute ethanol to dissolve and quantitatively dilute it to make a solution containing about 10 g / micron per 1 mL, to obtain a test solution.

Note: "Precision weighing" means that the weighing weight should be accurate to one thousandth of the weighing weight. "Precision measurement" means that the accuracy of measuring the volume should meet the accuracy requirements of the volume pipette in national standards.

Operation steps: Take the reference solution and the test solution according to ultraviolet spectrophotometry, and measure the absorbance at a wavelength of 240nm.

Note: The spectrophotometric method should be based on the same batch of solvent prepared as the test product, using a 1cm quartz absorption cell. The wavelength with the largest absorbance is used as the measurement wavelength. Generally, the error of the absorbance reading of the test product is between 0.3-0.7. The slit band width of the instrument should be less than half the width of the absorption band of the test product, otherwise the measured absorbance is low. The selection of the slit width should be based on reducing the absorption of the test article when the slit width is reduced. Because the absorption cell and the solvent may have blank absorption, the blank reading should be subtracted after measuring the absorbance of the test product, and the content should be calculated. ^[2]

Testosterone undecanoate pharmacology and toxicology

This product is an androgen, an undecanoate of testosterone, and a derivative of testosterone. Can promote male growth, male secondary sexual characteristics and development of testis, paragonadal structure. Promote protein synthesis and reduce breakdown, enhance immune function, and promote bone growth. Promote red blood cell production, feedback inhibit gonadotropin secretion, and inhibit estrogen secretion. ^[3]

Testosterone undecanoate pharmacokinetics

After oral administration, the drug is absorbed in the small intestine lymphatics in the form of chylomicrons, enters the systemic circulation through the chest duct, and releases testosterone after the ester bond is broken. This form of absorption avoids first-pass effects of the liver and hepatotoxicity. There are obvious individual differences in serum peak time after oral administration, with an average of about 4 hours. After continuous administration, serum testosterone levels gradually increased and reached a steady state after 2 to 3 weeks. The peak time of serum testosterone after a single intramuscular injection On day 7, it returned to the level before intramuscular injection after 21 days. This product is a lipophilic drug, which is absorbed by the lymphatic system together with lipids after oral administration. The individual difference is large, the tmax is 1 to 8 hours, and the average is 4 hours. Excreted by the urine, the total amount of urine in the 1 week after taking the drug is 45% to 48%, within 24 hours of the absorbed dose appears in the urine. ^[3]

Testosterone undecanoate

1. Primary or secondary testicular hypofunction;

2. Delayed physical puberty in boys;

3. Palliative treatment of breast cancer metastasis;

4. Adjuvant treatment of aplastic anemia;

5. Androgen deficiency syndrome in middle-aged and elderly people;

6. Rheumatoid arthritis. ^[3]

Testosterone undecanoate

The diagnosis and possible prostate cancer, breast cancer patients and suspicious persons are disabled. ^[3]

Testosterone undecanoate dosage

oral. Must be used under the guidance of a specialist. The initial dose is maintained at 120-160 mg (3 to 4 capsules) per day. After two weeks of administration, the daily dose is maintained at 40 to 120 mg (1 to 3 capsules). Twice morning and evening, orally after meals. If you take a single capsule daily, you can take an extra capsule in the morning or as directed by your doctor. ^[3]

Testosterone undecanoate adverse reactions

The following adverse reactions have been found in androgen therapy: Prepubertal boys: precocious puberty, increased erection frequency, enlarged penis, and premature sacral closure. Men: abnormal penile erections and other signs of sexual irritation, long-term high-dose use may cause reduced sperm and decreased ejaculation. All patients: urinary problems in elderly men; water and sodium retention. ^[3]

Testosterone undecanoate notes

1. When serious adverse reactions occur, treatment should be stopped immediately, and after the symptoms disappear, restart from a lower dose.

2. Patients with heart failure (including asymptomatic), renal failure, prostate hypertrophy, hypertension, epilepsy or trigeminal neuralgia (or those with a history of the above diseases) should be used with caution, and should be closely observed because androgens may cause , Sodium retention.

3. Preadolescent boys should be used with caution to avoid premature closure of the epiphysis or precocious puberty.

4. Patients with edema-prone kidney disease and heart disease should be used with caution. ^[3]

5. Use with caution by athletes

Testosterone undecanoate for pregnant and lactating women:

Pregnant women lactating women are prohibited.

Testosterone undecanoate for children:

Long-term application in children can cause precocity, premature bone closure, and affect growth and development, and should be used with caution.

Testosterone undecanoate for elderly:

Elderly patients with low metabolic function, prone to hypertrophy should be used with caution. ^[3]

Testosterone undecanoate drug interactions

To improve the effect, you can take appropriate amount of protein sugar and vitamins at the same time. ^[3]

Testosterone undecanoate expert review

This product is the undecanoate ester of the natural androgen testosterone, androgen medicine for the treatment of testosterone deficiency. After oral absorption, it is absorbed in the small intestine lymphatics in the form of chylomicrons, enters the systemic circulation through the thoracic duct, and is converted into testosterone in the body to play the role of androgen, supplementing the endogenous androgen deficiency. It is suitable for alternative treatments for male sexual insufficiency, such as after orchiectomy, no testis, hypopituitarism, and endocrine impotence. Also used in middle-aged and older men with decreased libido. This product is absorbed by the lymphatic system, thereby avoiding liver inactivation, so that the therapeutic amount of active testosterone reaches the peripheral circulation, so the plasma testosterone level is constant, the male effect is complete, does not affect liver function, and does not inhibit the pituitary function. The effect is the same as testosterone. After oral absorption, it is converted into testosterone in the body to play an androgenic effect, supplementing the endogenous androgen deficiency. It is suitable for alternative treatment of male sexual dysfunction, such as after orchiectomy, testicular arrhythmia, etc. It is also used in middle-aged and elderly men with hyposexuality, mental and physical weakness, and osteoporosis caused by androgen deficiency, or some men are Infertility. It is also used for aplastic anemia. ^[4]