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Home > Products >  Isotretinoin

Isotretinoin CAS NO.4759-48-2

  • Min.Order: 1 Metric Ton
  • Payment Terms: T/T,
  • Product Details

Keywords

  • Isotretinoin
  • 4759-48-2

Quick Details

  • ProName: Isotretinoin
  • CasNo: 4759-48-2
  • Appearance: white powder
  • DeliveryTime: 3 days after payment
  • PackAge: 25kg/plastic drum,200Kg/iron drum
  • Port: Shanghai, Shenzhen, Guangzhou, Hongkon...
  • ProductionCapacity: 1 Metric Ton/Day
  • Purity: 99%
  • Storage: Keep in cool and dry place, away from ...
  • LimitNum: 1 Metric Ton
  • Related Substances: <0.1%
  • Residue on Ignition: <0.1%
  • Heavy Metal: <0.002%
  • Valid Period: 2 years

Superiority

 

  • 【Density】
  • 1.011 g/cm3
  • 【Melting Point】
  • 174-177℃
  • 【Boiling Point】
  • 462.8 °C at 760 mmHg
  • 【Flash Point】
  • 350.6 °C
  • 【Water】
  • insoluble
  • 【Solubilities】
  • insoluble in water
  • 【Color/Form】
  • Reddish-orange plates from isopropyl alcohol
    Yellowish to orange crystalline powder
  • 【Stability】
  • Stable, but probably air and light sensitive. Combustible. Incompatible with strong oxidizing agents.
  • 【Storage temp】
  • ?20°C
  • 【Spectral properties】
  • Max absorption: 354 nm (Epsilon=39,800)
  • 【Computed Properties】
  • Molecular Weight:300.43512 [g/mol]
    Molecular Formula:C20H28O2
    XLogP3:6.3
    H-Bond Donor:1
    H-Bond Acceptor:2
    Rotatable Bond Count:5
    Exact Mass:300.20893
    MonoIsotopic Mass:300.20893
    Topological Polar Surface Area:37.3
    Heavy Atom Count:22
    Formal Charge:0
    Complexity:567
    Isotope Atom Count:0
    Defined Atom Stereocenter Count:0
    Undefined Atom Stereocenter Count:0
    Defined Bond Stereocenter Count:4
    Undefined Bond Stereocenter Count:0
    Covalently-Bonded Unit Count:1
    Feature 3D Acceptor Count:2
    Feature 3D Anion Count:1
    Feature 3D Hydrophobe Count:3
    Feature 3D Ring Count:1
    Effective Rotor Count:5.8
    Conformer Sampling RMSD:0.8
    CID Conformer Count:37

Details

 

Biomedical Effects and Toxicity

  • 【Pharmacological Action】
  • - Drugs used to treat or prevent skin disorders or for the routine care of skin.
    - An agent that causes the production of physical defects in the developing embryo.
  • 【Therapeutic Uses】
  • Keratolytic Agents; Teratogens
    Isotretinoin is indicated in the treatment of severe, recalcitrant nodular acne, where severe is defined as numerous lesions of at least 5 mm in diameter that may be suppurative or hemorrhagic. (Isotretinoin is also indicated for severe, inflammatory acne and acne conglobata. Taking into consideration its potential adverse effects, isotretinoin may be considered in patients with moderately severe acne who are prone to scarring or dyspigmentation. /NOT included in US product labeling/) Because of its potential adverse effects, isotretinoin should be reserved for patients who are unresponsive to or intolerant of conventional therapy, including systemic antibiotics. /Included in US product labeling/
    Isotretinoin is used in the treatment of gram-negative folliculitis and severe rosacea. /NOT included in US product labeling/
    Isotretinoin is used in the treatment of hidradenitis suppurative and is more effective for less established conditions and for those mild in severity (less scarring). Complete suppression or prolonged remission is uncommon. Using isotretinoin as adjunctive therapy to intralesional steroids, systemic antibiotics, or local surgery has proved beneficial for some patients with hidradenitis suppurative. /NOT included in US product labeling/
    Isotretinoin has been used for severe keratinization disorders, such as lamellar ichthyosis, keratosis follicularis (Darier's disease), palmoplantar keratoderma (keratosis palmaris et plantaris), and pityriasis rubra pilaris (PRP). Longer periods of isotretinoin therapy are usually required for keratinization disorders than for acne vulgaris, thus increasing the risk of side effects, including skeletal changes. /NOT included in US product labeling/
    Oral administration of 13-cis-retinoic acid (40 or 160 mg/kg bw daily) significantly reduced the inflammation associated with developing and established adjuvant arthritis, an experimentally induced arthritis in rats that resembles human rheumatoid arthritis. [Brinckerhoff CR et al; Science 221 (AUG 19): 756 (1983)]
  • 【Biomedical Effects and Toxicity】
  • The drug readily crosses the placenta in animals. It is not known if isotretinoin is distributed into milk.
    Radiolabeled doses administered to rats showed high concentrations of radioactivity in many tissues after 15 minutes, maximizing at 1 hour and declining to non detectable concentrations in most tissues after 24 hours. Low radioactive concentrations in rats were still detectable in the liver, ureter, ovary, and adrenal and lacrimal glands after 7 days.
    Rapidly absorbed from the gastrointestinal tract; amount absorbed increase when isotretinoin is taken with food. Data suggest that isotretinoin and 4-oxo-isotretinoin may be reabsorbed from the bile.
    The harmonic mean elimination for the simultaneous iv and oral administration of isotretinoin was approx 5.5 hr. The mean blood clearance, following iv admin, and the intrinsic clearance, following oral administration, were 5.19 and 6.63 ml/min/kg, respectively. The average abs bioavailability was approx 21% indicating an overall 1st-pass effect of approx 80%. Analysis of gut contents for total (14)-C activity suggested that a fraction of the isotretinoin dose was biologically or chemically degraded in the gut lumen prior to absorption. [Cotler S et al; DRUG METAB DISPOS 11 (5): 458-62 (1983)] PubMed Abstract
    Clinical doses of isotretinoin range from 0.5 to 8 mg/kg/day, with acute side effects appearing following doses of 1 mg/kg/day or greater. Plasma concn of isotretinoin following single and multiple doses peak between 2 to 4 hr and exhibit elimination half-lives of 10 to 20 hr. Isotretinoin blood concn-time curves following a single- or multiple-dose regimen are well described by a linear model with biphasic disposition characteristics. ... In most conditions, the retinoids produce a maximal effect in about 8 weeks (at the highest tolerated dose), with a slow recurrence of symptoms usually occurring within several weeks following cessation of treatment - except in the treatment of cystic acne with isotretinoin. Maintenance or intermittent dosing usually results in a prolongation of remission. [Lucek RW, Colburn WA; Clin Pharmacokinet 10 (1): 38-62 (1985)] PubMed Abstract
    A case study involving the disposition of 13-cis retinoic acid in embryonic tissues from a woman who unintentionally took 40 mg/day of isotretinoin from day 8-28 of gestation was discussed. When the pregnancy was terminated on day 31, between 72 and 80 hr after the last dose of isotretinoin, maternal serum samples were obtained. Retinoid concn in the maternal serum, embryonic tissue, and 6 samples of placental tissue were later measured by high performance liquid chromatography. The results showed that in humans, the intake of isotretinoin during pregnancy results in high placental and embryonic concn of all-trans-retoinic acid, in contrast to what was previously discovered in mice experiments. It was concluded that the metabolic activation of isotretinoin to the all-trans isomer could be responsible for the teratogenicity of isotretinoin.
    Elimination: Biliary or feces: 83%; Renal: 65%.
    Distribution of isotretinoin into human body tissues and fluids has not been fully characterized. Following oral administration of isotretinoin in animals, the drug is distributed into many tissues including liver, ureters, adrenals, ovaries, and lacrimal glands. Isotretinoin and its metabolites are distributed into bile in humans, principally as glucuronide conjugates; biliary concentration of the drug is proportional to hepatobiliary function and may be negligible in the presence of obstructive biliary disease. The drug has also been detected in synovial fluid. Unlike vitamin A, isotretinoin is not stored in the liver.
    Isotretinoin and its metabolites are conjugated, possibly with glucuronic acid, before being excreted in urine and feces. Excretion of unchanged isotretinoin in urine appears to be negligible. Isotretinoin appears to be excreted in feces, mainly as unchanged drug. Limited data suggest that isotretinoin and its metabolites are excreted in feces via biliary elimination and that the drug and its metabolites also undergo enterohepatic circulation. In adults with normal renal and hepatic function, 65-85% of a single, radiolabeled 80 mg oral dose of isotretinoin is excreted in urine and feces in approximately equal proportions.

 

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