Delving into the Latest Updates on Azelnidipine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Azelnidipine (JP17/INN), CS-905, RS 9054

+ [5]

Target

L-type calcium channel

Action

blockers

Mechanism

L-type calcium channel blockers(Voltage-gated L-type calcium channel blockers)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Daiichi Sankyo Co., Ltd.

Lianyungang Runzhong Pharmaceutical Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (31 Jan 2003),

Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC33H34N4O6

InChIKeyZKFQEACEUNWPMT-UHFFFAOYSA-N

CAS Registry123524-52-7

In this study, a sustainable and eco-friendly method is developed to quantify azelnidipine and chlorthalidone in rabbit plasma by gradient liquid chromatography based on green chemistry principle and analytical quality by design. The separation was achieved on a Shim pack C18 (25 cm × 5 cm × 4.6 μm) column with L1 packing. The mobile phase compromised of ethanol and 50-Mm ammonium acetate buffer (pH.6) at flow rate of 0.6 mL/min with 25-min runtime. The resolution and asymmetric factor were identified as critical analytical attributes (CAAs). The screening studies employing Control Noise Experimentation revealed that mobile phase pH, flow rate and ethanol concentration at 6 and 15 min significantly affected the CAAs method. The critical method parameters were optimized using Central Composition design. Chromatogram showed peak of the drugs at retention time of 9.03 min for chlorthalidone and 16.83 min for azelnidipine. The greenness score of the analytical method was found to be 1876.43 using analytical method greenness score calculator. The validation of the developed method was done which showed linearity at the range of 16–520 ng/mL, with R2 of 0.9992 and 0.9996 for azelnidipine and chlorthalidone, respectively, furthermore accuracy, precision, recovery and stability studies are carried out.

01 Dec 2024·INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY

Stability indicating analytical method development and validation for azelnidipine and chlorthalidone by LC-MS method

Author: Nandhu, R. ; Manikandan, M. ; Gandhi, Meenal ; Sanjay, S. ; Tharik, A. Mohamed Sheik

An accurate, precise, and reproducible HPLC-MS-based stability-indicating was developed and validated for the simultaneous quantitative determination of Azelnidipine (AZL) and Chlorthalidone (CTE). HPLC-MS method employs an X Bridge C18 column (5 μm, 4.6 x 250 mm) and a mobile phase, 5mM Potassium dihydrogen phosphate: Acetonitrile (10:90 v/v) ratio with, pH 7.8 adjusted using Triethylamine, for the simultaneous determination of AZL and CTE. The detection was carried out at 261 nm with a flow rate of 1.0 ml/min. The method reveals linearity over the concentration ranges of 0.1-0.6 mcg/ml for AZL and 0.16-0.96 mcg/ml for CTE with correlation coefficients of 0.9901 and 0.9988, respectively. Precision (%RSD) for intraday analysis was found to be 0.98% for AZL and 0.88% for CTE. Accuracy was negotiated at three different concentrations, and the results indicated %Recovery within acceptable limits. Limits of detection and quantification were determined to be 52 ng/ml and 45.6 ng/ml for both compounds, respectively.. KEYWORDS :Azelnidipine, Chlorthalidone, LC-MS, Stability-Indicating method, Method development.

01 Dec 2024·INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY

Stability Assessment through HPTLC for Concurrent Assessment of Azelnidipine and Telmisartan in Mass and Integrated Tablet Drug Formulation

Author: Jayashree, J. ; Mohan, S. ; Haribhuvanesh, P.

This study aims to estimate the stability assessment through HPTLC for the concurrent assessment of (±)3-(1-diphenylmethylazetidin-3-yl)5-isopropyl-2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridine dicarboxylate (Azelnidipine) and 2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl] phenyl]benzoic acid (Telmisartan) in combined tablet formulation, a new HPTLC approach devised and validated that is simple, quick, precise, selective, and accurate stability suggesting. The adsorbent phase used is previously coated with a silica pack on TLC aluminum plates with 60F-254 using Chloroform: Ethyl acetate (5:5 v/v) of a total of 10 ml as the mobile phase. Both Azelnidipine (Rf 0.70) and Telmisartan (Rf 0.17), at 254 nm, densitometric scanning was performed in the reflectance absorptivity mode. In the linearity range of 1-6 μg/ml for Azelnidipine and 5-30 μg/ml for Telmisartan, the calibration graph demonstrated satisfactory linearity with r2 = 0.9967 and 0.9966, respectively. Azelnidipine and Telmisartan percentage assays were discovered to be 98.87 and 100.17. The percent RSD for intraday AZL and TLM experiments was 0.0184 and 0.0068. The percent RSD for AZL and TLM interday trials was discovered as 0.0126 and 0.0068. The LOD for AZL and TLM was discovered as 910 ng/mark and 4570 ng/mark. AZL and TLM were discovered to have LOQs of 2763 ng/mark and 13850 ng/mark, respectively. According to the ICH guidelines, drugs were exposed to acidic, basic, oxidative, photo, and heat-activated degradation. The medication degrades in acidic, basic, oxidative and heat environments but not in light or neutral environments (water). This procedure can be used to efficiently isolate the drug substance from its degradation products and this is used to indicate strength and stability.. KEYWORDS :Azelnidipine, Telmisartan, HPTLC, UV-visible spectroscopy, Validation, Stability studies.

1

News (Medical) associated with Azelnidipine

23 Oct 2021

·www.pharmaindustrial-india.com

NPPA releases draft version of proposed retail price calculation for five formulations

The National Pharmaceutical Pricing Authority (NPPA) has released draft version of proposed retail price calculation for five formulations, including a combination of telmisartan IP 40 mg and amlodipine besylate IP, which has a moving annual total (MAT) of Rs. 596.8 crore. The telmisartan IP and amlodipine besylate IP combination, manufactured by Pure & Cure Healthcare Pvt Ltd and marketed by J B Chemicals & Pharmaceuticals Ltd, has been proposed with a retail price of Rs. 9.51 per tablet excluding goods and services tax (GST) while the claimed retail price was Rs. 20.32 per tablet. The proposed retail price is 34.5 per cent lower than the highest price in the market, which is Rs. 12.52 per tablet for Telsartan AM from Dr Reddy’s Laboratories Ltd. Minimum price of Rs. 3.21 per tablet was reported by Systopic Laboratories Ltd, for its brand Newtel AM. 16 companies have one per cent or above market share for the formulation in the country. Retail price of hard gelatin capsule containing rosuvastatin calcium IP equivalent to rosuvastatin 10 mg (as pills) along with Aspirin IP 75 mg (as enteric coated pills) manufactured by Synokem Pharmaceuticals Ltd and marketed by Cadila Pharmaceuticals was fixed at Rs. 5.99 per capsule excluding GST while the claimed retail price was Rs 12.50 per capsule. The MAT of the formulation is around Rs. 73.81 crore, and there are 13 players with one per cent or above market share. Retail price of capsule containing rosuvastatin calcium IP equivalent to rosuvastatin 20 mg (as pellets) along with clopidogrel bisulphate IP equivalent to clopidogrel 75 mg (as pellets), manufactured by Synokem Pharma and marketed by Cadila Pharma, has been proposed at Rs. 19.64 per capsule, which was also the claimed retail price. The MAT of the formulation is Rs. 23.51 crore and there are five companies which has one per cent or above market share. Formulation of azelnidipine IP 8 mg and telmisartan IP 40 mg manufactured by Akums Drugs & Pharmaceuticals Ltd and marketed by IPCA Laboratories has been proposed with a retail price of Rs. 11.37 per tablet excluding GST, while the claimed retail price was Rs. 12.50 per tablet

Drug ApprovalLicense out/inNDA

100 Deals associated with Azelnidipine

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External Link

KEGG	Wiki	ATC	Drug Bank
D01145	Azelnidipine	C08CA	DB09230

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	Japan	Daiichi Sankyo Co., Ltd.	31 Jan 2003

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ISC2020	Not Applicable	Post-stroke Fatigue	36	Olmesartan/Azelnidipine combination	ojcwslekrl(rydryvmvmi) = qhwmyyiqpo kbrivvsbth (auiegrtvcn )	-	01 Feb 2020
				High-dose olmesartan	ojcwslekrl(rydryvmvmi) = pncriuvyci kbrivvsbth (auiegrtvcn )
201 (ESH2012)	Not Applicable	Hypertension	-	Azelnidipine	yjhaovgmfy(iwlqpelrts) = pcernosopq bldoidqrbl (jbniqziwrr ) View more	Positive	01 Sep 2012
				Amlodipine	yjhaovgmfy(iwlqpelrts) = xrpvgroyiw bldoidqrbl (jbniqziwrr ) View more
PP.1.32 (ESH2010)	Not Applicable	Functional disorder	-	Azelnidipine 0.3 mg/kg	lnrtahiayy(dfnuarcnmt) = aaerbefadl jiwcorqrrn (yfcqmnhohc, 5) View more	Positive	01 Jun 2010
				Labetalol 3 mg/kg	lnrtahiayy(dfnuarcnmt) = nkelewocju jiwcorqrrn (yfcqmnhohc, 4) View more