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Occurrence of Transformation Products of Pharmaceutical and Personal Care Products in the Aquatic Environment
Published in Leo M. L. Nollet, Dimitra A. Lambropoulou, Chromatographic Analysis of the Environment, 2017
Myrsini Papageorgiou, Eleni Evgenidou, Dimitra A. Lambropoulou
The antihypertensive drugs are used to treat high blood pressure. Valsartan and enalapril have been detected in WWTPs worldwide (Huerta-Fontela et al., 2010; López-Serna et al., 2010; Salgado et al., 2010; Gros et al., 2012; Verlicchi et al., 2012a; Cruz-Morató et al., 2014; Jelic et al., 2015; Kostich et al., 2014; Petrović et al., 2014; Acuña et al., 2015; Moreno-González et al., 2015). Kern et al. (2010) reported that during activated sludge treatment, valsartan undergoes a series of sequential transformations. Firstly, the oxidative dealkylation of valsartan takes place followed by the hydrolysis of the dealkylated valsartan, giving rise to the amino-valsartan, which is finally oxidized to 2-(2H-tetrazol-5-yl)-[1,1-biphenyl]-4-carboxylic acid, referred to as valsartan acid (VALA). The latter appears to be the most stable of the three TPs. VALA was detected in the influents (up to 320 ng L−1) and in the effluents (up to 1053 ng L−1) of WWTPs in Germany and Switzerland (Kern et al., 2010; Nödler et al., 2013). Kern et al. (2010) reported that when 80% of valsartan was removed during treatment with activated sludge, the concentrations of its TP VALA increased about eightfold from 140 to over 1000 ng L−1 due to the formation of the specific TP during treatment, as aforementioned. However, due to structural similarities, this compound could potentially be formed from selected pharmaceuticals different from valsartan but belonging to the same compound class.
Formulation development and evaluation of orodispersible tablet of Azelnidipine by factorial design and its comparison with the marketed formulation
Published in Particulate Science and Technology, 2023
Ramdas T. Dolas, Pooja D. Ware
Hypertension is the most common chronic disease and the calcium channel antagonist is the most popularly used as an antihypertensive drug. Azelnidipine is a third-generation and long-acting dihydropyridine Ca2+ channel antagonist (Kumar et al. 2020). It was first approved in Japan in 2003 for the treatment of hypertension. In India, Azelnidipine was approved for manufacturing and marketing for the treatment of Stage I Hypertension in 2020 by the Central Drugs Standard Control Organization (CDSCO) (Siddiqui and Garg 2010). Azelnidipine is a potent vasodilator that progressively lowers blood pressure in hypertensive patients. Azelnidipine does not cause reflex tachycardia because of vasodilation, in contrast to other drugs in the same family. Due to its high affinity for vascular tissue and antioxidative activity, it also has a sustained hypotensive effect and has been demonstrated to have a significant anti-arteriosclerotic effect in vessels. Azelnidipine shows its activity by inhibiting L-type Ca2+ channels, but it causes a reduction in heart rate in high blood pressure patients as it exhibits inhibitory effects. on sympathetic nervous activity. Azelnidipine shows a long-lasting reduction in systolic as well as diastolic BP when compared with other calcium channels blacker (CCBs) (Chen et al. 2015). Azelnidipine belongs to the BCS II drug with low solubility and high permeability. The drug delivery applications of Azelnidipine are restricted due to low solubility and poor bioavailability. To overcome this severe drawback, fast release with immediate onset of action in a shorter period with improved bioavailability is quite necessary for Azelnidipine.
Improved transdermal delivery of valsartan using combinatorial approach of polymeric transdermal hydrogels and solid microneedles: an ex vivo proof of concept investigation
Published in Journal of Biomaterials Science, Polymer Edition, 2023
Cindy Kristina Enggi, Mega Tri Satria, Nirmayanti Nirmayanti, Jesscia Theodor Usman, Julika Fajrika Nur, Rangga Meidianto Asri, Nana Juniarti Natsir Djide, Andi Dian Permana
Valsartan (VAL) is an antihypertensive drug which belongs to angiotensin II receptor blocker (ARB). The use of VAL does not associate with persistent cough/angioedema due to its ability to not inhibit the breakdown of bradykinin. According to Nixon et al. [5], among other ARB drugs, VAL is found to be more effective at lowering BP and shows comparable efficacy in patients. However, when administrated orally, VAL exhibits low bioavailability (around 10–35%) due to poor absorption in the gastrointestinal tract. Furthermore, food intake is known to affect the pharmacokinetics of VAL by reducing its Cmax and AUC [6, 7]. Therefore, finding an alternative route for delivering VAL is needed.