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Duloxetine HCl

Duloxetine HCl

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PRODUCT NAME: Duloxetine HCl
CAS NUMBER: 136434-34-9
Duloxetine is a serotonin-norepinephrine reuptake inhibitor. It is effective for major depressive disorder and generalized anxiety disorder. Duloxetine has approval for use in Osteoarthiritis and Musculoskeletal pain. Duloxetine failed the US approval for stress urinary incontinence amidst concerns over liver toxicity and suicidal events; however, it was approved for this indication in Europe, where it is recommended as an add-on medication in stress urinary incontinence instead of surgery. It can also relieve the symptoms of painful peripheral neuropathy, particularly diabetic neuropathy, and it is used to control the symptoms of fibromyalgia.

MP 118-122°C
storage temp.
-20°C Freezer
Pharmacokinetics Absorption and Distribution: oral administration of duloxetine hydrochloride enteric-coated capsules can yield a complete absorption with the average lag being two hours before the drug began to be absorbed (TLag). At 6 hours after oral administration, the duloxetine reaches maximum plasma concentration (Cmax) with eating causing no effects on the Cmax, but will delay the peak time to about 6 to 10 hours with slightly lower degree of absorption at about 10%. Compare the evening administration once with morning administration once, the absorption of duloxetine is delayed by 3 hours; apparent elimination increases by one thirds; the apparent volume of distribution is about 1640 L. Duloxetine has a high affinity (> 90%) to the human plasma proteins which mainly binds with albumin and α- acid glycoprotein. There has been no evaluation of whether there exist interactions between duloxetine with other high affinity protein binding drugs. Liver or renal insufficiency does not affect the binding between plasma protein and duloxetine.
Metabolism and Excretion: oral administration of C14-labeled duloxetine can be used to determine their in vivo biotransformation and degradation. The plasma duloxetine only account for about 3% of the total radiolabel, suggesting that duloxetine is extensively metabolized with many kinds of metabolites. The major biotransformation pathway of duloxetine includes naphthyl epoxidization after the binding and further oxidation. Among in vitro tests, CYP2D6 and CYPIA2 can both catalyze the epoxidation of naphthyl with the plasma product including glucuronide-bound 4-hydroxy duloxetine and sulfate-bound 5-hydroxy 6-methoxy duloxetine. It has been separated of various kinds of other metabolites from urine with some appearing only in the small elimination metabolic bypass. Only a small amount (about 1% of the oral dose) of non-metabolized duloxetine prototype is detected in the urine with the majority (about 70% of the oral dose) existing in the form of duloxetine metabolic product which is excreted
in urine. About 20% of them is excreted through feces.
Indications It is used for the treatment of depression and the treatment of stress urinary incontinence.
In 2004, Japan Shionogi Pharmaceutical Co., Ltd. had obtained the authorization of Eli Lilly Company of US to perform further development on the duloxetine which has dual inhibitory effect on the reuptake of both 5 hydroxy trptamine (5-HT) and norepinephrine (NE). Existing studies have shown that this drug has certain efficacy in treating tension urinary incontinence, depression, and obesity. Currently, clinical trials of the drug for treatment of tension urinary incontinence and depression have all been completed.
Precautions 1. Liver and kidney dysfunction can significantly reduce the metabolism and clearance of duloxetine. Thus it is not recommended for such patients to apply duloxetine.
2. The interaction between duloxetine and alcohol may cause liver damage. Thus it is not generally recommended for the treatment of patients with alcoholism.
3. In the clinical trials, when compared with placebo, duloxetine causes the mean systolic blood pressure increase by 2mmHg, and the average diastolic blood pressure increase by 0.5mmHg. We recommend regular measurement of blood pressure both before and during treatment and therapy.
Drug Interactions Duloxetine is metabolized through CYP2D6 and CYP1A2 metabolism with moderate inhibition of CYP2D6 but no inhibition and induction effects on CYP1A2 and CYP3A4. We should be cautious when apply it together with other drugs which are also metabolized through CYP2D6 and of narrow therapeutic window (such as: TCAs, Ic antiarrhythmic drugs, and phenothiazines).
Medication of Special Populations [Medication of Pregnant women and lactating women] It is not clear whether it is safe when applied this drug for pregnant women of pregnancy category. Therefore, for pregnant women, they should weigh both the advantages and disadvantages to decide whether they should administrate this drug. Only with potential benefits higher than risks can they apply it. Otherwise, they should not administrate this drug during pregnancy and lactation period.
[Pediatric administration] There has been no enough clinical experience on the application on children.
[Elderly people] Clinical studies have not observed a significant difference of the security and efficacy between the elderly population and young population. But it can’t be exclude that the sensitivity of some elderly patients can be increased.
Contraindications 1. It should be contraindicated in patients known to be allergic to duloxetine or any of the inactive ingredients contained in the product.
2. It should be prohibited to apply it in combination with monoamine oxidase inhibitors (MAOIs). It is also not allowed to administrate this drug within 14 days after the withdrawal of MAOIs; According to the half-life of duloxetine, only after the five days of the withdrawal of duloxetine can the patients begin to administrate MAOIs.
3. Clinical trials have shown that duloxetine can increase the risk of mydriasis and therefore the angle-closure glaucoma patients without control should avoid applying duloxetine.
Usage Labelled Duloxetine, which is used as an antidepressant. A dual serotonin and norepinephrine reuptake inhibitor (SNRI). Current lot is 97% d7 with no d0, d1 or d2.
An antidepressant. A dual serotonin and norepinephrine reuptake inhibitor (SNRI). Used in treatment of stress urinary incontinence. Solubility H2O: soluble5 mg/mL (clear solution, warmed)
ITEMS Specification Result
Appearance White to off white colored powder Complies
Identification Meets the requirements Complies
Chloride test Should be positive Complies
Solubility Meets the requirements Complies
Specification rotation +115 °~ +125° +120.52°
Water content by KFR ≤1.0% w/w 0.13%w/w
Sulphated ash ≤0.1% w/w 0.06%w/w
Heavy Metals ≤10ppm 5ppm
Relative Substances
Thiophene amine impurity ≤0.15% N.D.
Naphthol impurity ≤0.15% N.D.
Max single impurity ≤0.1% 0.02%
Total impurity ≤1.0% 0.03%
Assay(HPLC) 98.0% ~ 102.0% w/w 99.36% w/w

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