Stanozolol

The basic information

Chinese name: stanzolol

Chinese alias: Kanglilong

English name: Stanozolol

English alias: Tevabolin; Stanozolol; Winstrol; STANAZOL; Estazol; Anabol; STANOZOL; Stromba;

CAS no. : 10418-03-8

MDL number: MFCD00133084

EINECS no. : 233-894-8

RTECS number: BV8741000

PubChem number: 24899733

Molecular formula: C21H32N2O

Formula:

Molecular weight: 328.49200

Accurate quality: 328.25100

PSA: 48.91000

LogP: 4.11810

Physical and chemical properties

Appearance and properties: white to light yellow powder

Density: 1.129 g/cm3

Melting point: 242 DHS C

Boiling point: 490.8ºC at 760 mmHg

Flash: DHS 250.7 C

Stable at normal temperatures and pressures.

Storage condition: 2-8ºC

Steam pressure: 1.89E-10mmHg at 25°C

Safety information

Danger class code: R63

Safety Instructions: 53-22-36/37/39-36-26

Dangerous Goods Mark: Xn [1]

Molecular structure data

1. Molar refractive index: 95.87

2. Molar volume (cm/mol) : 290.8

3, equal tension specific capacity (90.2K) : 769.1

4. Surface tension (DYNE /cm) : 48.8

Computational chemical data

1. Reference value of hydrophobic parameter Calculation (XlogP) : 4.5

2. Number of hydrogen bond donors: 2

3. Number of hydrogen bond receptors: 2

4. Number of rotatable chemical bonds: 0

5. Polar surface area of topological molecules (TPSA) : 48.9

6. Number of heavy atoms: 24

7, surface charge: 0

8. Complexity: 538

9, isotope atomic number: 0

10. Determine the number of atomic centers: 7

11. Number of uncertain atomic centers: 0

12. Determine the number of chemical bond construction centers: 0

13. Number of uncertain chemical bond centers: 0

14. Number of covalent bond units: 1

use

It is used for chronic wasting diseases, serious diseases and weak emaciation after operation, old age, osteoporosis, children's dysplasia, aplastic anemia, etc. [2]

Pharmacopoeia standard pronunciation

Source (Name), content (potency)

This product is 17-methyl-2 'H-5α -androstere-2-ene -[3, 2-C] pyrazole-17 β -alcohol. The content of C21H32N2O shall not be less than 98.0%.

character

This product is white crystalline powder; Odourless; Slightly wetting.

This product is slightly soluble in ethanol or chloroform, slightly soluble in ethyl acetate or acetone, very slightly soluble in benzene, almost insoluble in water or methanol.

Than the curl

The product was precisely weighed, dissolved in anhydrite ethanol and diluted quantitatively to prepare a solution containing about 20mg per 1mL. The specific curl was determined according to law (Appendix ⅵ E, Part II of Pharmacopoeia, 2010 edition) with a range of +34° to +40°.

To identify

(1) Take about 2mg of the product, add 3ml of p-dimethylaminobenzaldehyde test solution, yellow-green color, uv lamp (365nm) under inspection, yellow-green fluorescence.

(2) The product was dissolved in anhydrous ethanol and diluted into A solution containing about 40μg per 1mL. Uv-visible spectrophotometry (Appendix ⅳ A, Part II of Pharmacopoeia, 2010 edition) was used to determine the maximum absorption at the wavelength of 224nm.

(3) The infrared absorption spectrum of the product should be consistent with that of the control spectrum (Figure 597 in Infrared Spectrum of Medicines).

check

About the material

Take this product, add dichloromethane - anhydrous ethanol (9:1) to dissolve and dilute into a solution containing 10mg per 1mL, as the test solution; A proper amount was taken and diluted with dichloromethane and anhydrous ethanol (9:1) to prepare solutions containing 10μg, 30μg and 50μg per 1mL as serial control solutions. In addition, a solution containing 10mg stanzolol and 0.1mg mesonolone per 1mL was prepared by adding methylene chloride and anhydrous ethanol (9:1) to dissolve and dilute stanzolol and mesonolone as the reference solution. According to the TLC test (Appendix ⅴ B, Part II, Pharmacopoeia 2010 edition), 10μ L of each of the above 5 solutions were absorbed, respectively, onto the same silica gel G thin layer plate, and the mixture of chloromethane-methanol (19: 1) as the developing agent, unfold, dry, spray with 20% sulfuric acid ethanol solution, heat at 100℃ for 10 ~ 15 minutes until the spots are clear, place uv lamp (365nm) for inspection. The reference solution should show two clearly separated spots; If the test solution shows impurity spots, the total amount of impurities should not exceed 2.0% compared with the main spots of the series control solution.

Dry weight loss

Take this product and dry it at 105℃ to constant weight, with weight loss of no more than 1.0% (Appendix ⅷ L, Part II, Pharmacopoeia 2010 edition).

On ignition residue

Not more than 0.1% (Appendix ⅷ N, Part II, 2010 Edition of Pharmacopoeia).

Content determination

Take the dry product about 0.27g, weigh accurately, add 30ml glacial acetic acid to dissolve, cool, add 1 drop of crystal violet indicator solution, titrate with perchloric acid titration solution (0.1mol/L) until the solution turns green, and calibrate the titrated result with blank test. Every 1mL perchloric acid titrant (0.1mol/L) is equivalent to 32.85mg C21H32N2O. [3]

Compound related drug description speech

Pharmacological effects

Stanzol is a protein anabolic hormone with strong protein anabolic effect, 30 times of methyl testosterone, 1/4 of androgen activity and 120 differentiation index. It can promote protein synthesis, inhibit the dissimilar decomposition of histone, reduce blood cholesterol and triacylglycerin, promote calcium and phosphorus deposition and reduce bone marrow inhibition, etc. It can enhance physical strength, increase appetite and increase body weight, but the male effect is very weak.

pharmacokinetics

Oral absorption from the gastrointestinal tract, plasma half-life of 4 to 5h, mainly excreted by urine.

indications

Used in chronic wasting diseases, osteoporosis, serious diseases and weak emaciation after operation, old age, dysplasia in children, aplastic anemia, leukopenia, thrombocytopenia, hyperlipidemia, etc. Used for old and sick, postpartum weakness, etc. Also used for prevention and treatment of long-term use of corticosteroids caused by adrenal cortical hypofunction. [4]

contraindicated

Severe liver disease, kidney disease, heart disease, hypertension, pregnant women and prostate cancer patients are prohibited. [5]

Usage and dosage:

1. Commonly used by adults and adolescents

(1) Prevention and treatment of hereditary angoneeurotic edema: orally, 2mg (1 tablet) at the beginning, 3 times a day, 2mg (1 tablet) for women. Dosing should be individualized according to the patient's response. If the therapeutic effect is obvious, the dosage can be reduced every 1 to 3 months until 2mg (1 tablet) daily maintenance. However, in the process of reduction, the condition must be closely observed.

(2) For chronic wasting diseases, post-operation weakness, prolonged trauma treatment: oral, 3 times a day, 2-4mg (1-2 tablets), women moderate.

2. Normal dosage for children

It is used for hereditary angioneurotic edema. Under 6 years of age, 1mg (half tablet) daily orally, only during attacks; 6-12 years old, 2mg (1 tablet) daily orally, only during attacks. [5]

Matters needing attention

1. Patients suffering from gastric ulcer, liver, lung, heart and other dysfunction should be used with caution.

2. If use for a long time, can have liver dysfunction, icteric etc.

3. Discontinue medicine in case of acne and other masculine reactions. [4]

Medication for pregnant and lactating women:

Pregnant women are not allowed.

Medication for children:

Children with caution, precocious, affect growth.

Medication for the elderly:

Easy to cause water and sodium retention, hyperkalemia should be used with caution. [5]

Adverse reactions

1. Women: Long-term use may lead to acne, hairy, clitoral hypertrophy, amenorrhea or menstrual disorders.

2. Men: Long-term use may lead to acne, reduced sperm, reduced semen.

3. Liver: INCREASED GOP, GTP, jaundice.

4. Digestive system: nausea, vomiting, indigestion, diarrhea.

5. Electrolyte: water and sodium retention, edema.

6. Skin: rash, flushing. [5]

Interact with each other

The combination of adrenocorticosteroids, especially corticosteroids, increases the risk of edema. Adrenocorticotropic hormone or glucocorticoid combined with adrenocorticotropic hormone may accelerate the development of acne. The anticoagulant activity is enhanced by androgens and protein anabolic steroids, which reduce the concentration of clotting factor precursors (due to changes in the synthesis and decomposition of clotting factor precursors) and by increasing the affinity of anticoagulants to receptors. The dosage should be reduced when used with dicoumarin or indene diketone derivatives. When used in combination with hepatotoxic agents, liver damage may be exacerbated, especially in long-term use and in patients with pre-existing liver disease.

With barbiturates, carbamazepine, methylalanine, bute, rifamequine can reduce estrogen activity. [4