Simultaneous determination of azelnidipine and two metabolites in human plasma using liquid chromatography-tandem mass spectrometry

Kawabata, Kiyoshi; Urasaki, Yoko

doi:10.1016/j.jchromb.2006.06.031

Cited by 12 publications

(5 citation statements)

References 11 publications

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“…Azelnidipine was jointly developed by Ube Industries, Ltd. (Yamaguchi, Japan) and Daiichi Sankyo Co, Ltd (Tokyo, Japan) and launched into the market as Calblock in Japan in 2003 8. Different from all the existing dihydropyridine calcium antagonists having two methyl groups located at the 2- and 6-positions of the dihydropyridine ring, azelnidipine has an amino group displacing the methyl group at the 2-position 9. In addition, azelnidipine has two enantiomers (R-(−)- and S-(+)-enantiomers) due to an asymmetric carbon at the 4-position, and the (R)-(−) enantiomer of dihydropyridine calcium antagonists is considered to possess intrinsic pharmacological activity 10…”

Section: Pharmacology Mode Of Action Pharmacokinetics Of Azelnidipinementioning

confidence: 99%

Clinical use of azelnidipine in the treatment of hypertension in Chinese patients

Chen¹,

Zhang²,

Zhang³

2015

TCRM

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BackgroundHypertension is the most common chronic disease and the calcium channel antagonist is the most popularly used antihypertensive drug in Chinese patients. Azelnidipine is a third generation and long-acting dihydropyridine calcium channel antagonist. A series of research has demonstrated that azelnidipine produced an effective antihypertensive effect in patients with essential hypertension. Now it is need to summarize clinical use of azelnidipine in the treatment of hypertension in Chinese patients.MethodsRelevant literature was identified by performing searches in PubMed and CNKI (China National Knowledge Infrastructure), covering the period from January 2003 (the year azelnidipine was launched) to July 2014. We included studies that described pharmacology of azelnidipine, especially the pharmacokinetics, clinical efficacy, and safety and tolerability of azelnidipine in a Chinese population. The full text of each article was strictly reviewed, and data interpretation was performed.ResultsIn Chinese healthy volunteers, a single-dose oral administration of azelnidipine 8–16 mg had a peak plasma concentration of 1.66–23.06 ng/mL and time to peak plasma concentration was 2.6–4.0 hours and the area under the plasma concentration versus time curve from time 0 hour to 96 hours was 17.9–429 ng/mL·h and elimination half-life was 16.0–28.0 hours. A number of clinical trials have demonstrated that azelnidipine produced a significant reduction in blood pressure in Chinese patients with mild-to-moderate hypertension, which was similar to that of other effective antihypertensive drugs such as amlodipine, zofenopril, and nifedipine. In addition to its antihypertensive effect, azelnidipine had other cardiovascular protective effects as well, like anti-oxidative action, decreasing heart rate, and improving systolic and diastolic function. Azelnidipine was generally well tolerated in Chinese patients and no severe adverse events were observed.ConclusionAzelnidipine is effective and safe in the treatment of hypertension in Chinese patients.

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Section: Pharmacology Mode Of Action Pharmacokinetics Of Azelnidipinementioning

confidence: 99%

Clinical use of azelnidipine in the treatment of hypertension in Chinese patients

Chen¹,

Zhang²,

Zhang³

2015

TCRM

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“…[7] Literature studies revealed few analytical methods for the estimation of AZEL and TELM as a single component or combine with other drug formulation. These methods were: spectrophotometric, [11] High Performance Liquid Chromatography (HPLC), [12][13][14][15][16][17][18] liquid chromatography-mass spectrometry (LC-MS), [19,20] highperformance liquid chromatography mass analysis capabilities of mass spectrometry (HPLC-MS-MS). [21] So far only two HPLC method have been reported for their simultaneous estimation in their combined dosage form.…”

Section: Introductionmentioning

confidence: 99%

Advanced forced degradation technique for simultaneous estimation of azelnidipine and telmisartan implementing AQbD approach in its tablet dosage form

Bera

Shah

2022

ijhs

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For simultaneous estimation of Azelnidipine and Telmisartan in pharmaceutical dosage form, a simple, rapid, precise and reproducible RP-HPLC method was developed. Separation was achieved on a Phenomanax Luna C18; 5 μm, 150 mm × 4.6 mm i.d. column using water and methanol 50: 50 (v/v) as mobile phase and detected at 256 nm using PDA detector. Azelnidipine and Telmisartan were exposed to thermal, photolytic, hydrolytic and oxidative stress conditions and stressed samples were analyzed by the proposed method. Linearity, precision, accuracy, specificity and robustness were studied as reported in the International Council for Harmonization guidelines. Linearity of the proposed method was in the range of 4-12 μg mL-1 (r2 = 0.998) for Azelnidipine and 20-60 μg mL-1 (r2 = 0.997) for Telmisartan. Limits of Detection were 1.041 μg mL-1 and 0.208 μg mL-1, while Limits of Quantitation were 3.155 μg mL-1 and 0.631 μg mL-1 for Azelnidipine and Telmisartan respectively. Degradation products produced as a result of stress studies did not interfere with the detection. The proposed stability studies method for simultaneous estimation was found to be specific, accurate and economical that could be applied for routine analysis of drugs in bulk and multi component formulations in quality control laboratories.

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“…The dihydropyridine calcium antagonists have two methyl groups [2] and two enantiomers (R-(-)-and S-(+)-enantiomers [3].…”

Section: Introductionmentioning

confidence: 99%

Bioequivalence Study of Azelnidipine 16 Mg Tablet to Evaluate Pharmacokinetic Profile of Single Dose in Healthy, Adult, Human Volunteers Under Fasting Condition

Das¹,

Halder

Bose³

et al. 2021

Int J App Pharm

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Objective: The present study's objective is to conduct a comparative bioavailability study with a special emphasis on the test product's bioequivalence using a standard reference product as a comparator. Methods: Before initiating the bioequivalent study, the plasma sample analysis method was developed and validated by using LC-MS/MS method. The entire study was conducted as a single-dose crossover randomized bioequivalence study with open-label, two treatment, two-period, and two sequences on 24 healthy volunteers under fasting condition. With proper informed consent process the oral dose of the Reference product (R) or Test product (T) was administered on healthy volunteers at 0 h during each period of the study. After the drug's oral administration, a certain quantity of blood sample was collected, and the plasma sample was separated using a cold centrifuge. The plasma samples were analysed by using the validated LC-MS/MS method. The pharmacokinetic parameters, statistical data and ANOVA of the test and reference product were evaluated. Results: The Cmax, Auc0-t, AUC0-∞ and tmax of the test product were found to be 6.29 ng/ml, 117.0 ng. h/ml, 161.67 ng. h/ml and 3.33 h. respectively. And the Cmax, Auc0-t, AUC0-∞ and tmax of reference product were found 6.59 ng/ml, 123.21 ng. h./ml, 172.20 ng. h/ml and 3.38 h respectively. Relative bioavailability was found 94.96%. The overall results show that the 90% confidence intervals (Log-Transformed and Untransformed) for Cmax, AUC0-t and AUC0-∞ for Azelnidipine were within the acceptable limit of 80%-125%. Conclusion: The entire study's conclusion can be drawn as the test product was bioequivalent with the reference product's comparator.

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Simultaneous determination of azelnidipine and two metabolites in human plasma using liquid chromatography-tandem mass spectrometry

Cited by 12 publications

References 11 publications

Clinical use of azelnidipine in the treatment of hypertension in Chinese patients

Clinical use of azelnidipine in the treatment of hypertension in Chinese patients

Advanced forced degradation technique for simultaneous estimation of azelnidipine and telmisartan implementing AQbD approach in its tablet dosage form

Bioequivalence Study of Azelnidipine 16 Mg Tablet to Evaluate Pharmacokinetic Profile of Single Dose in Healthy, Adult, Human Volunteers Under Fasting Condition

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