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      Application of UV spectrophotometric method for easy and rapid estimation of lafutidine in bulk and pharmaceutical formulation

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          Abstract

          Introduction:

          The present research work discusses the development of a UV estimation method for lafutidine. Simple, accurate, cost efficient, and reproducible spectrophotometric method has been developed for the estimation of Lafutidine in bulk and pharmaceutical dosage form.

          Materials and Methods:

          The Stock solution was prepared in a mixture of water and methanol (1:1). Further dilutions were made in water.

          Results:

          The drug was determined at maximum wavelength (λ max) 279 nm. Beers law was obeyed in the concentration range of 10–50 μg/ml having line equation y = 0.0100x + 0.035 with correlation coefficient of 0.999. Results of the analysis were validated statistically and by recovery study.

          Conclusion:

          The result of analysis was validated as per ICH guidelines and this method can be used for the routine analysis of lafutidine formulation.

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          Lafutidine, a Protective H2 Receptor Antagonist, Enhances Mucosal Defense in Rat Esophagus

          Yasutada Akiba, Jonathan Kaunitz (2010)
          Background Luminal acid or CO2 induces a hyperemic response in the esophagus, via activation of acid sensors on capsaicin-sensitive afferent nerves (CSAN). Since disruption of the hyperemic response to luminal CO2 acidifies the interstitium of the esophageal mucosa, the hyperemic response may maintain interstitial pH (pHint). We hypothesized that acid-related hyperemia maintains pHint, preventing acid-induced injury in the esophageal mucosa. Methods We examined the effects of capsaicin (Cap) or lafutidine (Laf), a mucosal protective H2 antagonist, on the regulation of pHint and blood flow in rat esophagus using ratiometric microimaging and laser-Doppler measurements of the lower esophageal mucosa of living rats. The esophagus was topically superfused with pH 7.0 buffer, or a pH 1.0 or pH 1.0 + pepsin (1 mg/ml) solution with or without Laf. Results Cap (30 or 100 µM) or Laf (0.1 or 1 mM) dose-dependently increased blood flow, accompanied by increased pHint. The pH 1.0 solution increased blood flow without pHint change, whereas Laf (1 mM) increased blood flow and pHint during acid exposure. The effects of Laf were abolished by ablation of CSAN. Perfusion of the acidified pepsin solution gradually decreased pHint, inhibited by Laf perfusion. Conclusions Activation of CSAN by Laf with or without acid, accompanied by hyperemia, increased pHint, preventing acidified pepsin-induced interstitial acidification. Stimulation of the capsaicin pathway with compounds such as Laf enhances mucosal protection from acid-related injury in the upper gastrointestinal tract.
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            Separation and identification of cis and trans isomers of 2-butene-1,4-diol and lafutidine by HPLC and LC-MS.

            Chun-xiu PAN, Xiu-zhu Xu, Hong-mei He … (2005)
            The cis and trans isomers separation of 2-butene-1,4-diol and lafutidine were studied by HPLC on two kinds of chiral columns: (S,S)-Whelk-O 1 and ChiraSpher. The isomers of 2-butene-1,4-diol can be separated on both chiral columns while the isomers of lafutidine can only be resolved on ChiraSpher column. The influence of different type and amount of mobile phase modifier on the isomers separation was extensively studied. The resolution of cis and trans isomers of 2-butene-1,4-diol was 2.61 on (S,S)-Whelk-O 1 column with hexane-ethanol (97:3, v/v) as the mobile phase. The resolution of lafutidine was 1.89 on ChiraSpher column with hexane-ethanol-THF-diethylamine (92:3:5:0.1, v/v/v/v) as the mobile phase. LC-MS methods were developed to identify the isomer peaks.
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              Simple, sensitive and rapid LC–ESI–MS method for the quantitation of lafutidine in human plasma—Application to pharmacokinetic studies

              Wei-Dong Chen, Yan Liang, Hao Li … (2006)
              A sensitive and specific liquid chromatography electrospray ionization mass spectrometry (LC-ESI-MS) method has been developed and validated for the identification and quantification of lafutidine in human plasma. Lafutidine and internal standard were isolated from plasma samples by liquid-liquid extraction with diethyl ether. The chromatographic separation was accomplished on a stainless-steel column (C18 Shim-pack 5 microm 150 mm x 2.0 mm i.d. Shimadzu) at a flow rate of 0.2 ml/min by a gradient elution. Detection was performed on a single quadrupole mass spectrometer by selected ion monitoring (SIM) mode via electrospray ionization (ESI) source. The method was proved to be sensitive and specific by testing six different plasma batches. Linearity was established for the range of concentrations 1.0-400.0 ng/ml with a coefficient of determination (r) of 0.9998 and good back-calculated accuracy and precision. The intra- and inter-day precision (R.S.D.%) was lower than 10% and accuracy ranged from 85 to 115%. The lower limit of quantification was identifiable and reproducible at 0.5 ng/ml with 0.2 ml plasma. The proposed method enables the unambiguous identification and quantification of lafutidine for pharmacokinetic, bioavailability or bioequivalence studies.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Pharm Methods
                Journal ID (iso-abbrev): Pharm Methods
                Journal ID (publisher-id): PMeth
                Title: Pharmaceutical Methods
                Publisher: Medknow Publications & Media Pvt Ltd (India )
                ISSN (Print): 2229-4708
                ISSN (Electronic): 2229-4716
                Publication date (Print): Oct-Dec 2011
                Volume: 2
                Issue: 4
                Pages: 264-267
                Affiliations
                [1]Department of Pharmaceutical Analysis, Genba Sopanrao Moze College of Pharmacy, Wagholi, Pune, India
                Author notes
                Address for correspondence: Ms. Kiran Jadhav, Genba Sopanrao Moze College of Pharmacy, GAT No. 2181, Wagholi, Pune – 412 207, Maharashtra, India. E-mail: kiranjadhav112@ 123456yahoo.co.in
                Article
                Publisher ID: PMeth-2-264
                DOI: 10.4103/2229-4708.93398
                PMC ID: 3658075
                PubMed ID: 23781468
                SO-VID: 42c71de6-d106-4525-a4ac-213c690cab2f
                Copyright © Copyright: © Pharmaceutical Methods
                License:

                This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                Categories
                Subject: Original Article

                Keywords: lafutidine,uv spectrophotometry,validation
                Data availability:
                Keywords: lafutidine, uv spectrophotometry, validation

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