Delving into the Latest Updates on Nebivolol Hydrochloride/Valsartan with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Byvalson, Nebivolol/valsartan, Valsartan/nebivolol

Target

AT1R x β1-adrenergic receptor

Mechanism

AT1R antagonists(Angiotensin II Receptor Type 1 antagonists), β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

Allergan Ltd. (Ireland)

Active Organization

Prinston Pharmaceutical, Inc.

Inactive Organization

AbbVie, Inc.

Drug Highest PhaseApproved

First Approval Date

US (03 Jun 2016),

Hypertension

Regulation-

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Structure

Molecular FormulaC46H54F2N6O7

InChIKeySCTCSYRLAUPSSW-KXUDKMLBSA-N

CAS Registry1562428-72-1

BACKGROUNDNebivolol and valsartan (VAL) in combination with each other successfully control blood pressure and improve hypertension patient outcomes.OBJECTIVETo develop and validate innovative, simple, and sustainable spectrophotometric methods for the simultaneous analysis of nebivolol and valsartan.METHODThe new modified difference amplitude modulation (MD-AM) method uses only unified regression equation and does not require any resolution techniques. Other different approaches were also applied for the determination of the same mixture including univariate and multivariate spectrophotometric methods. The multivariate methods were PLS and PCR, whereas the univariate methods were derivative ratio (DD1), ratio difference (RD), constant center (CC), constant center spectrum subtraction (CC-SS), constant value coupled with amplitude difference (CV-AD), advanced concentration value (ACV), and amplitude difference (AD). The proposed methods use a green solvent; thus, the environmental impact of the presented procedures was evaluated qualitatively and quantitatively using six well-known evaluation tools.RESULTSAll methods were applied successfully for the analysis of the studied drugs in their bulk powder, pharmaceutical dosage form Byvalson®, and in vitro release at intestinal pH (7.4) using a USP dissolution tester. Results obtained were compared statistically with the reported method and with each other using a one-way ANOVA statistical test, and no significant differences were found.CONCLUSIONSAll green and white analytical chemistry evaluation tools results confirm the safety, sustainability, and cost-effectiveness of the approaches, indicating that the methods are regarded green and sustainable. Results were agreeable, encouraging their applicability in quality control laboratories for dosage form and making these methods an eco-friendly substitute for the analysis of this combined dosage form and for evaluating the dissolution profile.HIGHLIGHTSFor the first time, a severely overlapped spectrum was determined using a unified regression equation without the need of extended part or zero contribution regions by the novel method MD-AM. The proposed methods are the first study of in vitro dissolution profiling of nebivolol hydrochloride (NEB) and VAL and the first sustainable and green methods applied without compromising the analytical criteria.

01 Aug 2018·Pharmacology & TherapeuticsQ1 · MEDICINE

Discovery of Leonuri and therapeutical applications: From bench to bedside

Q1 · MEDICINE

Review

Author: Yi Zhun Zhu ; Xinhua Liu ; Qing Zhu ; Weijun Wu

Despite several advances in percutaneous coronary intervention and the discovery of new drugs, the incidence of myocardial infarction and deaths due to cardiovascular diseases (CVD) has not decreased markedly in China. The quality of life is affected seriously, which further results in great social and family burden. Many drugs, from the century-old aspirin to the newly FDA-approved Byvalson, have been proven to be effective in the treatment and prevention of CVD. As clinically reported, those life-saving drugs still have their side effects in regards to the narrow therapeutic indexes influenced by individual genetic variations. Herba Leonuri, also known as Chinese Motherwort, which are naturally present in plants and traditionally are used for the uterotonic action, postpartum blood stasis, breast pain as well as other gynecological disorders in China for thousands of years. Since the last two decades, our group has reported leonurine, a unique alkaloid found in Herba Leonuri, exhibits various bioactivities such as antioxidant, anti-apoptotic effects, free radical scavenging and anti-inflammatory effects, in addition to improving micro-circulation. These bioactivities are related to the underlying mechanisms of ischemic heart diseases and cardiac fibrosis. Pharmacological studies have proven leonurine to be effective in treating CVD in various ways, particularly ischemic heart diseases. Besides the cardio protective effects, which are similar in the central nervous system, more specifically, inhibited mitochondrial reactive oxygen species production together with the restored mitochondrial function and redox state were observed in middle cerebral artery occlusion rats by leonurine treatment, which strongly reveals its neuroprotective effects and carries a therapeutic potential for recovery and prevention of stroke. Based on their mode of action, we propose that leonurine can be developed as drugs to treat ischemic heart diseases. Taking advantage of the most recent findings in pharmacological research including the effects of low toxicity and good pharmacokinetics characteristics, leonurine has a very attractive prospect of clinical application. Our recent promising pharmacological results may be able to eradicate the barrier hindering its sale on market. In sum, from bench to bedside is no longer a long way for leonurine.

12 Sep 2016·The Medical letter on drugs and therapeuticsQ4 · MEDICINE

Byvalson--a beta blocker/ARB combination for hypertension.

Q4 · MEDICINE

Article

100 Deals associated with Nebivolol Hydrochloride/Valsartan

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