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liquid letrozole

liquid letrozole

Letrozole controls estrogen levels

Aromatase inhibitor that effectively controls estrogen at very low application levels.

  • Agitate bottle before each administration
  • Not for human consumption

Letrozole (also known as Femara) is an oral non-steroidal aromatase inhibitor for the treatment of hormonally-responsive breast cancer after surgery. Letrozole has been used for ovarian stimulation by fertility doctors since 2001 due to less chance of multiple gestation. It also shows promise in studies as a treatment for early onset gynecomastia.

Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Estrogens then bind to an estrogen receptor, which causes cells to divide.Letrozole prevents the aromatase from producing estrogens by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of mineralo- or corticosteroids.

Abstract

A rapid and sensitive reverse phase high performance liquid chromatographic method is depicted for the qualitative and quantitative assay of letrozole in pharmaceutical dosage forms. Letrozole was chromatographed on a reverse phase C18 column with a mobile phase consisting of acetonitrile and phosphate buffer (pH 7.8) in the ratio of 70:30 v/v. The mobile phase was pumped at a flow rate of 1 ml/min. Acenaphthene was used as an internal standard and the eluents were monitored at 232 nm. The retention time of the drug was 3.385 min. With this method, linearity was observed in the range of 10-100 µg/ml. The LOD and LOQ were found to be 0.51 µg/ml and 1.52 µg/ml, respectively. The method was found to be applicable for analysis of drug in tablets. The results of the analysis were validated statistically.

Conclusion

 Our data reveals that letrozole (2.5 mg o.d.) is more effective compared with anastrozole (1.0 mg o.d.) with respect to tissue as well as plasma estrogen suppression in patients with postmenopausal breast cancer.

Contemporary clinical studies have shown that three third-generation aromatase inhibitors (anastrozole, letrozole, and exemestane) improve time to progression in metastatic disease (1–3) and relapse-free as well as overall survival compared with tamoxifen for adjuvant therapy of patients with postmenopausal breast cancer (4–6). These results are most likely related to their improved potency. The third-generation compounds inhibit total body aromatization by ≥98% in vivo (7–10). In contrast, compounds belonging to the first and second generation of inhibitors cause 80% to 90% (11–14) aromatase inhibition and do not improve clinical outcome compared with tamoxifen or megestrol acetate.

Acknowledgements

The authors are grateful to Unimed Technologies Ltd., Baroda, for providing gift sample of pure letrozole. Above all, the authors would like to offer their gratitude to the authorities of College of Pharmaceutical Sciences, Mohuda for providing all the facilities.

Storage

Store Nolvadex between 68 and 77 degrees F (20 and 25 degrees C) in a tightly closed, light-resistant container. Store away from moisture, heat, and light. Do not store in the bathroom. Do not take tablets after the expiration date printed on the label. Keep Nolvadex out of the reach of children and away from pets.

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