Vardenafil HCl Trihydrate - CAS 224785-90-4
Catalog number: 224785-90-4
Category: Inhibitor
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Phosphodiesterase (PDE)
Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Vardenafil was co-marketed by Bayer Pharmaceuticals, GlaxoSmithKline, and Schering-Plough under the trade name Levitra. As of 2005, the co-promotion rights of GSK on Levitra have been returned to Bayer in many markets outside the U.S. In Italy, Bayer sells vardenafil as Levitra and GSK sells it as Vivanza.
Vardenafil; Levitra; Staxyn; Vivanza; BAY 38-9456; BAY-38-9456; BAY38-9456;
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1.Dual β-cyclodextrin functionalized Au@SiC nanohybrids for the electrochemical determination of tadalafil in the presence of acetonitrile.
Yang L;Zhao H;Li CP;Fan S;Li B Biosens Bioelectron. 2015 Feb 15;64:126-30. doi: 10.1016/j.bios.2014.08.068. Epub 2014 Sep 2.
This finding described the electrochemical detection of tadalafil based on CM-β-cyclodextrin and SH-β-cyclodextrin functionalized Au@SiC nanohybrids film. The tadalafil electrochemical signal could be dramatically amplified by introducing 40% of acetonitrile in buffer medium and further enhanced by the host-guest molecular recognition capacity of β-cyclodextrin. Uniform and monodispersed ~5.0 nm Au NPs were anchored on the SiC-NH2 surface via a chemical reduction process by using polyethylene glycol and sodium citrate as dispersant and stabilizing agent. CM-β-CD was covalently bound on Au@SiC by combining the amine group of SiC-NH2 with the carboxyl group of CM-β-CD with the aid of EDC/NHS coupling agent. SH-β-CD could tightly attach to the surface of Au@SiC by the strong coordinating capability between Au and thiol. Differential pulse voltammetry was successfully used to quantify tadalafil within the concentration range of 0.01-100 µM under optimal conditions with a detection limit (S/N = 3) of 2.5 nM. In addition, the β-CD-Au@SiC nanohybrid electrochemical sensor showed high selectivity to two other erectile dysfunction drugs sildenafil and vardenafil. The proposed electrochemical sensing platform was successfully used to determine tadalafil in raw materials, herbal sexual health products, and spiked human serum samples.
2.An LC-MS/MS method for the determination of five erectile dysfunction drugs and their selected metabolites in hair.
Lee S;Choi B;Kim J;In S;Baeck S;Oh SM;Chung KH J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Jan 26;978-979:1-10. doi: 10.1016/j.jchromb.2014.11.024. Epub 2014 Dec 5.
The abuse of sildenafil and its analogous, accelerated by their inappropriate or illegal distribution, is a serious social issue globally. However, no studies have been conducted to monitor these drugs simultaneously in hair, which can provide valuable information on chronic drug use. In the present study, an LC-MS/MS method was developed for the simultaneous determination in hair of five erectile dysfunction drugs having a high risk for abuse (mirodenafil, sildenafil, tadalafil, udenafil and vardenafil) and their selected metabolites (SK3541, desmethylsildenafil, DA8164 and desethylvardenafil). The novel method was fully validated after optimizing matrix effects and extraction efficiency. The optimized sample preparation included acidic methanol extraction followed by solid phase extraction using C18 mixed mode strong cation exchange polymeric cartridges. The prepared samples were analyzed by LC-MS/MS with electrospray ion source in the positive ionization mode. The validation results proved the method to be selective, sensitive, accurate and precise, with acceptable linearity within calibration ranges. LODs ranged from 0.05 (DA8164) to 1 ng/10 mg hair (tadalafil). LOQs were 1 ng/10 mg hair except for DA8164 and vardenafil, of which they were 2.
3.Preparation and characterization of intravaginal vardenafil suppositories targeting a complementary treatment to boost in vitro fertilization process.
Gomaa E;Abu Lila AS;Hasan AA;Ghazy FS Eur J Pharm Sci. 2018 Jan 1;111:113-120. doi: 10.1016/j.ejps.2017.09.044. Epub 2017 Sep 28.
Vaginal route has been recently considered as a potential route for systemic delivery of drugs with poor oral bioavailability. Vardenafil (VDF) is a relatively new phosphodiesterase-5 inhibitor that exhibits a limited oral bioavailability (≈15%) due to extensive first-pass metabolism. In this study, we attempted to enhance the systemic bioavailability of VDF via its formulation within vaginal suppositories. Witepsol H15 and Suppocire NA50 were adopted as lipophilic suppository bases while polyethylene glycol 4000/400 and glycerogelatin were used as hydrophilic suppository bases. The effect of different base types and/or the incorporation of bioadhesive polymer on in vitro release of VDF were evaluated. The in vivo fate and organ biodistribution of VDF following intravaginal (IVG) administration were also investigated. VDF release from water-soluble bases was higher than that from lipophilic bases. The incorporation of bioadhesive polymers, such as Na alginate, remarkably sustained drug release from suppository base. The organ biodistribution study showed a higher C;max; (32 times) and AUC;0-4h; (20 times) of VDF in uterus following IVG administration of conventional suppositories, compared to oral administration of VDF suspension.
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CAS 224785-90-4 Vardenafil HCl Trihydrate

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