Trandolapril

Peters, Dene C.; Noble, Stuart; Plosker, Greg L.

doi:10.2165/00003495-199856050-00014

Cited by 17 publications

(5 citation statements)

References 48 publications

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“…Inhibition of ACE decreases levels of angiotensin II in the body leading to a decrease in blood pressure. ACE is one of the most studied drug design targets, and inhibitor development has been extensively described in numerous reviews. , Ten ACE inhibitors are approved by the FDA for therapeutic use including captopril ( 112 ) (IC 50 = 23 nM), enalapril ( 113 ) and enalaprilat (the diacid metabolite of enalapril) (IC 50 = 4.5 nM), lisinopril (IC 50 = 4.7 nM), benazepril (IC 50 = 1.7 nM), moexipril ( 114 ) (IC 50 = 2.6 nM), trandolapril ( 115 ) (IC 50 = 0.93 nM), fosinopril ( 116 ) (IC 50 = 1 nM), ramipril (IC 50 = 4 nM), and quinapril (IC 50 = 8.3 nM). The IC 50 values shown are for deesterified active metabolites.…”

Section: Metalloprotease Inhibitorsmentioning

confidence: 99%

Protease Inhibitors: Current Status and Future Prospects

2000

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in 1997. She is currently completing her Ph.D. degree in the Centre for Drug Design and Development. Her Ph.D. studies are directed at designing and developing competitive reversible protease inhibitors, particularly for serine and cysteine proteases involved in viral and parasitic infections, Alzheimer's disease, and apoptosis. Giovanni (John) Abbenante received his B.Sc. (Hons) degree from the Department of Chemistry of the University of Adelaide and his Ph.D. degree on the synthesis of GABA b receptor antagonists from Flinders University in 1992. He undertook postdoctoral studies on the synthesis of ladderanes at Central Queensland University and of HIV-1 protease inhibitors at the University of Queensland. He is currently a Senior Research Officer in the Chemistry Group of the Centre for Drug Design and Development with interests in drug design and in the synthesis of protease inhibitors, macrocycles, receptor antagonists, and peptidomimetics. David P. Fairlie received a B.Sc. (Hons) degree from the University of Adelaide and a Ph.D. from the University of South Wales and did postdoctoral research at Stanford University and University of Toronto. He has held research/ teaching appointments in six Australian universities and has led the Chemistry Group in the Centre for Drug Design and Development since 1991. He is Scientific Director of Promics Pty Ltd. Research interests are in chemical synthesis (organic, inorganic), molecular recognition (DNA-, RNA-, protein-, metalbinding compounds), peptide and protein mimetics, enzyme inhibitors and receptor antagonists for viral infections, inflammatory disorders, cancers, and neurodegenerative diseases, and in mechanisms of chemical reactions, biological processes, disease development, and drug action.

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Section: Metalloprotease Inhibitorsmentioning

confidence: 99%

Protease Inhibitors: Current Status and Future Prospects

2000

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“…Trandolapril (non-sulfhydryl prodrug) (Figure .1) is a potent ACE inhibitor quickly get converted in the liver to the trandolaprilat. 1,2 It belongs to BCS II and BDDCS II. 3 Clinically, it is used to manage patients with CHF and myocardial infarction.…”

Section: Introductionmentioning

confidence: 99%

“…3 Clinically, it is used to manage patients with CHF and myocardial infarction. 1,2 For overweight individuals with primary hypertension, trandolapril is also effective as well as safe. 2 Due to its strong affinity for ACE and high lipophilicity index, it is very effective when compared to other ACE (Angiotensin converting enzyme) inhibitors.…”

Section: Introductionmentioning

confidence: 99%

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Development and Characterization of Trandolapril Immediate Release Tablets Using Different Superdisintegrating Agents

Indurkhya¹,

PATEL²,

MASHEER³

2023

Curr. Res. Pharm. Sci.

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A potent non-sulfhydryl prodrug, trandolapril is transformed into the active substance, trandolaprilat, in the liver. For obese individuals with mild-to-moderate essential hypertension, Trandolapril is effective and safe. The elimination t1/2 of trandolapril and trandolaprilat are approximately 6 hours and 16–24 hours, respectively. The goal of present work is to develop the Trandolapril immediate release tablet using various superdisintegrants. Crospovidone, Sodium starch glycolate and Croscarmellose sodium in concentrations of 2%, 4%, and 6% were used as superdisintegrating agents for the optimization. Direct compression technique was used to make nine formulations (IRTR 1 to IRTR 9). The powder blends of all batches were evaluated for different parameters to know the powder flow characteristics and it was found that the powder blend had excellent flow and compressibility characteristics. Then, compressed tablets were tested for quality control parameters as per the IP. In formulation IRTR1-IRTR9, disintegration time was observed 30.23 to 71.67 Sec and more than 70% drug was released in 30 min. Thus, based on evaluation results, it is concluded that formulation of immediate release (IR) tablets of Trandolapril were successfully developed. Minimum disintegration time 30.23 seconds 90.56% drug release in 30 min was obtained with IRTR3. KEYWORDS: Trandolapril, Immediate release, Crospovidone, Sodium starch glycolate, crocarmellose sodium

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“…Trandolapril, {(2S, 3aR, 7aS 11), is the ethyl ester derivative of the diacid metabolite Trandolaprilat, an inhibitor of the peptidase 'Angiotensin Converting Enzyme' (ACE). Such inhibition of ACE activity results in an antihypertensive effect and therefore Trandolapril may be used to lower high blood pressure [21]. At present a number of strategies are known for the synthesis of Trandolapril.…”

Section: Trandolapril 421 Introduction and Backgroundmentioning

confidence: 99%

Laboratory for Process Research – Ten Years of Successful Partnership between University of Zurich and the Pharmaceutical Industry

Bader¹

2006

Chimia

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In 1996, the Laboratory for Process research (Labor für Prozessforschung = LPF) was founded as a collaboration between the University of Zurich and the pharmaceutical industry. This joint venture is based on the concept of providing a professional training platform in industrial process chemistry for Ph.D. graduates and performing highly sophisticated process research and development at the same time. The well-equipped LPF facilities, approved by swissmedic, operate according to the standards of Good manufacturing Practice (GmP). Chemical processes for manufacturing of active pharmaceutical ingredients (API) are developed from bench to production under GMP compliance. A large number of projects were successfully developed in the last decade, for which production was carried out at the LPF and/or after transfer of the whole technology to customers or contract manufacturers worldwide. In the course of these projects, the development of numerous innovative reactions and routes has resulted in several patents.

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Trandolapril

Cited by 17 publications

References 48 publications

Protease Inhibitors: Current Status and Future Prospects

Protease Inhibitors: Current Status and Future Prospects

Development and Characterization of Trandolapril Immediate Release Tablets Using Different Superdisintegrating Agents

Laboratory for Process Research – Ten Years of Successful Partnership between University of Zurich and the Pharmaceutical Industry

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