A Review on Analytical Method Development and Validation of Flecainide using HPLC

 

Harsha Vasudev Chaudhari1, Javesh Kashinath Patil2, Devshree Yashwanthbhai Patel3, Aniket Rajesing Girase4

1Department of Pharmaceutical Quality Assurance P.S.G.V.P. M’s College of Pharmacy,

Shahada, Dist. – Nandurbar, 425409.

2Associate Professor, Department of Pharmaceutical Quality Assurance P.S.G.V.P.M’s College of Pharmacy, Shahada, Dist. – Nandurbar, 425409.

3Department of Pharmaceutical Quality Assurance P.S.G.V.P. M’s College of Pharmacy,

Shahada, Dist. – Nandurbar, 425409.

4Department of Pharmaceutical Quality Assurance P.S.G.V.P. M’s College of Pharmacy,

Shahada, Dist. – Nandurbar, 425409.

*Corresponding Author E-mail: harshavasudevc213@gmail.com

 

ABSTRACT:

Analytical chemistry, the discipline focused on matter separation, identification, and quantification, encompasses traditional wet chemistry methods and modern instrumental approaches. Techniques like spectrophotometry and high-performance liquid chromatography (HPLC) are integral to analyte analysis. Spectrophotometry, particularly ultraviolet-visible (UV-Vis) spectroscopy, measures a sample's absorption of uv and visible light, aiding in the determination of chemical concentrations in various fields. UV-vis spectroscopy operates on the principle that electron excitation in atoms and molecules, caused by UV and visible light absorption, results in quantized energy level transitions. HPLC, a type of column chromatography, separates, identifies, and quantifies substances based on their interactions with a stationary phase and a mobile phase. Key components of hplc include a column, pump, and detector, with separation efficiency influenced by the analyte's interactions with the stationary phase. Method validation, as defined by ich q2 (r1), ensures that analytical procedures consistently yield reliable results. Critical validation criteria include specificity, accuracy, precision, linearity, range, limit of detection (lod), limit of quantification (loq), and robustness. Specificity confirms the method's ability to measure the analyte accurately amidst other substances. Accuracy is assessed through recovery studies, while precision involves repeatability and reproducibility. Linearity and range ensure the method's effectiveness across different concentrations. Lod and loq determine the method's sensitivity. Robustness evaluates the method's reliability under varying conditions. This review also examines flecainide acetate, a class ic antiarrhythmic agent, focusing on its analysis using hplc. Various studies highlight different mobile phases and columns used for flecainide's analysis, emphasizing the importance of method optimization for accurate results. Flecainide's mechanism involves inhibiting sodium channels, extending the heart's refractory period, and reducing calcium release from the sarcoplasmic reticulum, showcasing its significance in treating arrhythmias.

 

KEYWORDS: Analytical Chemistry, UV-Vis Spectroscopy, High-Performance Liquid Chromatography (HPLC), Method Validation, Flecainide Acetate.

 

 

INTRODUCTION:

The study and application of methods and tools for matter separation, identification, and quantification is known as analytical chemistry.1 separation, identification, and quantification can be applied singly or in conjunction with other techniques. Separation is used to identify analytes.


 

Fig 1: UV -Visible Spectroscopy

 


Analytes are identified by qualitative analysis, whereas quantitative analysis shows the numerical amount or concentration. Analytical chemistry is made consists of both traditional, wet chemistry methods and modern, instrumental approaches.2

 

The method used in spectrophotometry:

Spectrophotometry is a branch of electromagnetic spectroscopy that quantifies the wavelength-dependent transmission or reflection properties of a substance.3 it can therefore be used to determine the absorber concentration in a solution for a given path length. Knowing how rapidly absorbance changes with concentration is crucial.4

 

Ultraviolet-visible spectroscopy:

An instrument for analysis called a uv-vis spectrophotometer calculates how much ultraviolet (uv) and visible light a sample absorbs. It is a commonly used method for identifying and quantifying chemicals in a range of samples in the domains of chemistry, biochemistry, and other sciences.5

 

Principle of UV-Visible spectroscopy:

The underlying idea of UV spectroscopy is that the excitation of electrons in both atoms and molecules from lower to higher energy levels is related to the absorption of visible and UV light (200–400nm). Only light with the precise energy required to create transitions between levels will be absorbed since matter's energy levels are quantized. UV spectrophotometric systems record and mathematically process the absorption spectra of standard solutions and sample solutions in the same way or differently, depending on the additivity and absorbance principles.6

 

HPLC METHOD:

To separate, identify, and quantify active substances in biochemistry and analysis, high-performance liquid chromatography, or HPLC, is a type of column chromatography that is frequently utilized.7 the main components of HPLC are a column that contains the stationary phase (packing material), a pump that circulates the mobile phase(s) through the column, and a detector that shows the retention periods of the molecules. The interactions of the stationary phase, the molecules under analysis, and the solvent(s) influence the retention time.8 Small amounts of the sample to be analysed are added to the stream of the mobile phase, where it is slowed down by particular chemical or physical reactions with the stationary phase. The analyte's composition and nature dictate how much retardation occurs.

 

PRINCIPLE OF HPLC:

The distribution of the analyte (sample) between a stationary phase (column packing material) and a mobile phase (eluent) is the foundation of the HPLC separation principle. The molecules vary based on the substance as the analyte moves through the stationary phase, its structure slows down. The exact interaction between molecules. A sample's characteristics are determined by the interactions between its molecules and the packing material. "On-column" moment. Consequently, various components within a sample elute at disparate rates. Periodically. Consequently, the ingredients for the sample are divided. A revelation the device (UV detector, for example) identifies the analytes after they have exited the column. The signs they are converted and recorded by computer software called a data management system. The outcomes are subsequently shown in a chromatogram. The detection unit is passed through by the mobile. Phase may come into contact with garbage, additional detector units, or a fraction collection device. The following modules make up an hplc system in general: a column, a detector unit, a pump, an injection valve, a solvent reservoir, and a data processing unit. The solvent (eluent) is delivered under high pressure by the pump. The system moves at a constant speed. To minimize drift and noise from the detector to retain the gnal as long as feasible, the pump must have a steady, pulseless flow. Analyte (sample) is delivered to the eluent by the injection valve.9


 

Fig 2: HPLC (high performance liquid chromatography)

 


METHOD DEVELOPMENT:

Information on sample

Define separation goals

Need for special HPLC procedure sample pretreatment

Choose detector and detector settings

Choose LC method; Preliminary run; Estimate best separation

Optimize separation

Check for problems or requirement for Special procedure

 

 

Recover purified

material

 

Quantitative

calibration

 

Qualitative

method

Validate method for release to routine laboratory

 


METHOD VALIDATION:

As per the definition provided by ich q2 (r1), method validation involves creating a documented proof that offers a high level of assurance that a certain process will consistently yield the desired outcome at the prearranged parameters and quality characteristics. Stated simply, it is the process of demonstrating that analytical procedures support the identity, quality, purity, and potency of drug substances and drug products and are appropriate for the intended use. When a novel method is produced or when established methods are employed by various analysers in different laboratories, method validation is required. The performance criteria needed to verify different approaches using different recommendations—such as USA, ICH, FDA, european guidelines, etc.10,11

 

1. Specificity:

The capacity to evaluate the analyte with certainty in the presence of substances that are anticipated to be present, such as contaminants, excipients, and mobile phase components, is known as specificity12. It might be evaluated by spiking a sample with the right amounts of contaminants or excipients and confirming that there are no interfering peaks at the analyte retention time. The goal peak's single component correspondence can be ascertained by using a diode array detector to measure peak purity.

 

2. Accuracy:

Accuracy of measurement is the degree to which the measured value agrees with the true value. The majority of the time, recovery studies are performed to demonstrate and assess accuracy. Experiments on recovery were conducted to verify the accuracy of the established approach13.

 

3. Precision:

The degree of agreement (or scatter) between a set of measurements obtained by repeatedly sampling the same homogenous sample under predefined conditions is the definition of precision in analytical methods. Reproducibility, moderate precision, and repeatability are the three different categories of accuracy. In fact, homogenous samples are the best choice for precision studies. However, synthetic samples or sample solutions may be used for research purposes if a homogenous sample cannot be obtained. A collection of measures' variance, standard deviation, or coefficient of variation is frequently used to illustrate how accurate an analytical process is.

 

3.1 Repeatability:

The capacity to transmit accuracy across a short distance while maintaining the same operational parameters is known as repeatability. Repeatability can also be referred to as intra-assay precision.

 

3.3 Reproducibility:

The precision between laboratories is expressed by reproducibility (collaborative studies, usually used to standardisation of methodology)

 

4. Linearity:

Linearity is the ability of an analytical procedure to yield test results that, within a given range, are precisely proportionate to the concentration (amount) of analyte in the sample.

 

5. Range:

The range of analyte concentrations (amounts) in the sample, including these quantities for which the analytical procedure has demonstrated an adequate level of linearity, accuracy, and precision, is known as the analytical technique's range.14

 

6. Limit Of Detection:

The lowest detectable limit is referred to as the lod. The standard deviation and response slope can affect the equation for the limit of detection (lod). The lod is 3.x average sd/slope.

 

7. Limit Of Quantification:

Lower limit of quantification (loq) is the lowest concentration at which a measurement can be taken. Using the response’s slope and standard deviation,

The quantitation limit (loq) may be expressed as:

Loq = 10 (sd)/ s

Where, sd = standard deviation y intercept

S = slope15

 

8. Robustness:

Small adjustments to the optimised technique parameters, such as the mobile phase ratio, flow rate, and detection wavelength, were made in order to conduct the robustness investigation. Retention time and tailing factor are unaffected significantly.16

 

Literature review:

Table no 1: Literature review of Metoprolol succinate and Flecainide

Drug

Authors

Details

Ref.

No.

Flecainide acetate

Redasani V.K, et. al.,

Mobile phase: water: acetonitrile (60:40 v/v) with mobile phase pH adjusted with orthophosphoric acid (pH3.0)

Column:  C18 Qualisil BDS (250mm×4.5mm×5µm) column

17

Flecainide acetate

Md. Mustafa, et. Al.,

 mobile phase:    buffer: acetonitrile (40:60 v/v), pH adjusted to 3.0

Column: C18 ODS 250cm x 4mm x 5µm

18

Flecainide acetate in presence of its degradation products

El ‐ragehy, N., et. Al.,

Mobile phase: phosphate buffer pH 3.3–acetonitrile–triethylamine (53:47:0.03 v/v).

Column: C18 column with isocratic elution

19

Flecainide serum

Rei Nakagawa., et al.,

Mobile phase: 0.1 m 1-pentanesulfonic acid sodium salt, acetonitrile, and acetic acid (250:206:2.5 v/v/v)

Column: octa decyl silyl silica (ODS)

20

 

Drug profile:

FLECAINIDE:

Category: classic antiarrhythmic agent

Molecular formula: C17H20F6N2O3

Chemical name: (RS)-n-(piperidin-2-ylmethyl)-2,5-bis (2,2,2-trifluoroethoxy) benzamide

Molecular weight: 414.34 g/mol

Description: white to off white powder

Melting point: 105-107°C

Solubility: Soluble in ethanol, DMSO and dimethyl formamide (DMF).

 

Structure:

 

Fig no 3: Structure of Flecainide

 

Mechanism of action:

The heart's refractory time is extended with flecainide, which inhibits rapid inward sodium channels and gradually unbinds during diastole. The duration of action potentials via the purkinje fibres is likewise shortened by this blockage. Moreover, flecainide prolongs the action potential through the ventricular and atrial muscle fibber’s by blocking the activation of delayed rectifier potassium channels.10- lastly, flecainide also inhibits the opening of the ryanodine receptor, which lowers the release of calcium from the sarcoplasmic reticulum and lessens cell depolarization.

 

Conclusion:

Analytical chemistry, through techniques like UV-vis spectroscopy and HPLC, is essential for the precise separation, identification, and quantification of chemical substances. Method validation, encompassing criteria such as specificity, accuracy, precision, and robustness, ensures the reliability of these analytical procedures. The analysis of flecainide acetate, an antiarrhythmic agent, illustrates the practical application of these methods. Optimizing HPLC conditions for flecainide highlights the importance of accurate analytical techniques in pharmaceutical analysis. Overall, the integration of advanced analytical methods and rigorous validation processes is crucial for scientific progress and pharmaceutical quality assurance.

 

References:

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3.      Allen, DW; Cooksey, C; Tsai, BK (Nov 13, 2009). Spectrophotometry. NIST. Retrieved Dec 23, 2018.

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9.      Meyer, V.R. Practical High-Performance Liquid Chromatography. 5. Aufl. Chichester: Wiley, 2010.

10.   Reddy V.P, Rajan T.V.S, Kumar A. N, A Review on Analytical Method Validation. Int J Rev Life Sci. 1: 141-144.

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12.   Eserian, J. K., Lombardo, M.  Method validation in pharmaceutical analysis: from theory to practical optimization. Innovations in Pharmacy. 2015; 6(1). https://doi.org/10.24926/iip.v6i1.376

13.   Patil M A, Patil J K. Stability Indicating Method Development And Validation Of Ziprasidone By Using RP-HPLC Method. 2023. Https://Doi.Org/10.5281/Zenodo.8394540

14.   Validation of Analytical Procedures: Text and Methodology Q2(R1) Current Step 4 Version Parent Guideline Dated 27 October 1994 (Complementary Guideline On Methodology Dated 6 November 1996 Incorporated In November 2005)

15.   Patel Kiran, Patil Javesh. Development And Validation of UV-Spectroscopy And UHPLC Method For Gemfibrozil In Bulk Drug And Pharmaceutical Dosage Form [Data Set]. In International Journal of Pharma Research and Technology. 2023; 2(3). Https://Doi.Org/10.5281/Zenodo.10039607

16.   Kapil, Patil, Sunil, Pawar and Patil, Javesh. Development And Validation of RP-HPLC Method For Simultaneous Estimation of Amoxicillin and Dicloxacillin in Bulk Drug And Capsules. 2014

17.   Redasani, V. K. Analytical Method Development and Validation of Flecainide Acetate By Chromatographic And Spectrophotometric Techniques. Medicinal and Analytical Chemistry International Journal. 2020; 4(2): Https://Doi.Org/10.23880/Macij-16000164

18.   Md. Musthafa, Ravi Kumar Vejendla, J. Srawanthi, Arshiya Jabeen, K. Sindhu. RP-HPLC Method Development and Validation For Estimation of Flecainide Acetate In Bulk And Tablet Dosage Form.

19.   El‐Ragehy, N. A., Hassan, N. Y., Tantawy, M. A., Abdelkawy, M. Stability-Indicating Chromatographic Methods for Determination of Flecainide Acetate In The Presence Of Its Degradation Products; Isolation and Identification Of Two Of Its Impurities. Biomedical Chromatography/Bmc. Biomedical Chromatography. 2016; 30(10): 1541–1548. Https://Doi.Org/10.1002/Bmc.3719

20.   Nakagawa R, Homma M, Kuga K, Yamaguchi I, Kobayashi D, Morimoto Y, Kohda Y. High Performance Liquid Chromatography for Routine Monitoring of Serum Flecainide. J Pharm Biomed Anal. 2002; 30(1): 171-4. Doi: 10.1016/S0731-7085(02)00224-8. Pmid: 12151077.

 

 

 

Received on 17.06.2024                    Modified on 12.07.2024

Accepted on 01.08.2024                   ©AJRC All right reserved

Asian J. Research Chem. 2024; 17(4):250-254.

DOI: 10.52711/0974-4150.2024.00044