Top

European Journal of Drug Metabolism and Pharmacokinetics

Published in:

01-06-2016 | Original Paper

Pharmacokinetic and biodistribution study of eserine and pralidoxime chloride in rabbits following a single application of a transdermal patch

Authors: Subham Banerjee, Pronobesh Chattopadhyay, Animesh Ghosh, Aseem Bhatnagar, Vijay Veer

Published in: European Journal of Drug Metabolism and Pharmacokinetics | Issue 3/2016

Abstract

In the present study, a simple reverse-phase high-performance liquid chromatography method with diode array detection has been developed and validated for the simultaneous determination and quantification of eserine and pralidoxime chloride in rabbit plasma and its application to pharmacokinetic study. The pharmacokinetic study was performed after transdermal application of single patch in rabbits. The plasma levels of both drugs following transdermal application of single patch were maintained for 72 h after removal of the patch. The maximal concentrations (C _max) of both drugs were significantly reduced while the mean areas under the plasma concentration vs. time moment curve and mean residence times were evidently increased and extended, respectively. A sustained activity was observed over a period of 3 days. This sustained activity was due to the controlled release of drug into the systemic circulation following transdermal application. Linear correlation was also observed when fraction of drug permeated was correlated with the fraction of drug absorbed at the same time point. Gamma scintigraphy imaging on rabbit following transdermal patch application was performed to ascertain the localization of drugs in rabbit brain.

Available only for authorised users

Abbara C, Bardot I, Cailleux A, Lallement G, Bouil AL, Turcant A, Clair P, Diquet B (2008) High-performance liquid chromatography coupled with electrospray tandem mass spectrometry (LC/MS/MS) method for the simultaneous determination of diazepam, atropine and pralidoxime in human plasma. J Chromatogr B 874:42CrossRef

Asthana S, Greig NH, Hegedus L, Holloway HH, Raffaele KC, Schapiro MB, Soncrant TT (1995) Clinical pharmacokinetics of physostigmine in patients with Alzheimer’s disease. Clin Pharmacol Ther 58:299CrossRefPubMed

Banerjee S, Chattopadhyay P, Ghosh A, Kaity S, Veer V (2013a) Development and validation of a reverse phase liquid chromatography method for the simultaneous quantification of eserine and pralidoxime chloride in drugs-in-adhesive matrix type transdermal patches. Arzneimittelforschung/Drug Res. 63:450

Banerjee S, Chattopadhyay P, Ghosh A, Pathak MP, Singh S, Veer V (2013b) Acute dermal irritation, sensitization, and acute toxicity studies of a transdermal patch for prophylaxis against (±)-Anatoxin A poisoning. Int J Toxicol. 32:308CrossRefPubMed

Banerjee S, Singh S, Policegoudra R, Chattopadhyay P, Ghosh A, Veer V (2013c) Evaluation of the mutagenic potential of a prophylactic transdermal patch by Ames test. J Immbio 28:322

Banerjee S, Chattopadhyay P, Ghosh A, Bhattacharya SS, Kundu A, Veer V (2014a) Accelerated stability testing study of a transdermal patch composed of eserine and 2-PAM for prophylaxis against (±) Anatoxin-A poisoning. J Food Drug Anal. 22:264CrossRef

Banerjee S, Chattopadhyay P, Ghosh A, Pathak MP, Gogoi J, Veer V (2014b) Protection by a transdermal patch containing eserine and 2-PAM for prophylaxis against (±) Anatoxin-A poisoning in rats. Eur J Pharm Sci 56:28CrossRefPubMed

Bhattacharya SS, Banerjee S, Ghosh AK, Chattopadhyay P, Verma A, Ghosh A (2013) A RP-HPLC method for quantification of diclofenac sodium released from biological macromolecules. Int J Biol Macromol 58:354CrossRefPubMed

Bhavna Ahmad FJ, Mittal G, Jain GK, Malhotra G, Khar RK, Bhatnagar A (2009) Nano-salbutamol dry powder inhalation: a new approach for treating bronchoconstructive conditions. Eur J Pharm Biopharm 271:282

Brodie RR, Chasseaud LF, Robbins AD (1987) Determination of physostigmine in plasma by high-performance liquid chromatography. J Chromatogr 415:423CrossRefPubMed

Carmichael WW (2001) Health effects of toxin-producing cyanobacteria: “the CyanoHABs”. Hum Ecol Risk Assess 7:1393CrossRef

Chattopadhyay P, Banerjee S, Ghosh A, Veer V (2013) Matrix type transdermal patch formulations. Patent Application No. 3033/DEL/2013

Cho Y, Kim WS, Hur GH, Ha YC (2012) Minimum effective drug concentrations of a transdermal patch system containing procyclidine and physostigmine for prophylaxis against soman poisoning in rhesus monkey. Envt Toxicol Pharmacol 33:1CrossRef

Damodharan N, Roy G, Ghosh S, Mukherjee B (2010) Skin permeation of rosiglitazone from transdermal matrix patches. Pharm Technol 34:56

Devlin JP, Edwards OE, Gorham PR, Hunter NR, Pike RK, Stavric B (1977) Anatoxin-a, a toxic alkaloid from Anabaena flos aquae NRC-44 h. Can J Chem 55:1367CrossRef

Dunn MA, Sidell FR (1989) Progress in medical defense against nerve agents. J Am Med Assoc 262:649CrossRef

Elsayed NM, Ryabik JRG, Ferraris S, Wheeler CR, Korte DW (1989) Determination of physostigmine in plasma by high-performance liquid chromatography and fluorescence detection. Anal Biochem 177:207CrossRefPubMed

Food and Drug Administration of the United States, Guidance for Industry-Bioanalytical Method Validation, U.S. Department of Health and Human Services, Center for Drug Evaluation and Research (CDER), Center for Veterinary Medicine (CVM), May 2001. http://www.fda.gov/cder/guidance/index.htm

Hai NT, Kim J, Park ES, Sang-Cheol C (2008) Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine. Int J Pharm 357:55CrossRefPubMed

Hartvig P, Wiklund L, Lindstrom B (1986) Pharmacokinetics of physostigmine after intravenous, intramuscular, and subcutaneous administration in surgical patients. Acta Anaesthesiol Scand 30:177CrossRefPubMed

Houze P, Borron SW, Scherninski F, Bousquet B, Gourmel B, Baud F (2005) Measurement of serum pralidoxime methylsulfate (Contrathion) by high-performance liquid chromatography with electrochemical detection. J Chromatogr B 814:149CrossRef

Hsieh JYK, Yang RK, Davis KI (1982) Rapid high-performance liquid chromatographic determination of physostigmine in plasma. J Liq Chromatogr 5:1691CrossRef

Jenner A, Saleem A, Swanston D (1994) Transdermal delivery of physostigmine. A pretreatment against organophosphate poisoning. J Pharm Pharmacol 47:206CrossRef

Kim WS, Cho Y, Kim JC, Hang ZZ, Park SH, Choi EK, Shin SH, Nam SY, Kang JK, Hwang SY, Kim YB (2005) Protection by a transdermal patch containing physostigmine and procyclidine of soman poisoning in dogs. Eur J Pharmacol 525:135CrossRefPubMed

Knapp S, Wardlow ML, Thal LJ (1990) Sensitive analysis of plasma physostigmine levels using dual-cell electrochemistry in the redox mode. J Chromatogr 526:97CrossRefPubMed

Kottke MK, Rhodes CT (1991) Limitations of presently available in vitro release data for the prediction of in vivo performance. Drug Dev Ind Pharm 17:1157CrossRef

Kumar N, Soni S, Jaimini A, Ahmad FJ, Bhatnagar A, Mittal G (2011) Edetate calcium disodium nanoparticle dry powder inhalation: a novel approach against heavy metal decorporation. Int J Pharm 416:376CrossRefPubMed

Lukey BJ, Marlow DD, Clark CR, McCluskey MP, Lieske CN (1989) Application of a new radiometric high-performance liquid chromatographic assay to define physostigmine pharmacokinetics in guinea pigs. J Chromatogr 493:117CrossRefPubMed

Medicis JJ, Stork CM, Howland MA, Hoffman RS, Goldfrank LR (1996) Pharmacokinetics following a loading plus a continuous infusion of pralidoxime compared with the traditional short infusion regimen in human volunteers. J Toxicol Clin Toxicol 34:289CrossRefPubMed

Mittal G, Singh T, Goomer NC, Bhatnagar A, Lulla A, Malhotra G, Kashyap R, Tripathi RP (2008) Formulations and methods thereof for making radiolabeleddry powder. Patent No. 1536/DEL/2008

Mohs RE, Davis BM, Mathe AA, Rosen WQ, Johns CA, Greenwald BS, Horvath TB, Davis KL (1985) Intravenous and oral physostigmine in Alzheimer‘s disease. Interdiscipl Topics Geront Basel Karger 20:140

Osswald J, Rella´n S, Carvalho AP, Gago A, Vasconcelos V (2007) Acute effects of an anatoxin-a producing cyanobacterium on juvenile fish-Cyprinus carpio L Toxicon 49:693

Ray S, Banerjee S, Maiti S, Laha B, Barik S, Sa B, Bhattacharyya UK (2010) Novel interpenetrating network microspheres of xanthan gum–poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine—in vitro and in vivo evaluation. Drug Deliv. 17:508CrossRefPubMed

Ren C, Fang L, Ling L, Wang Q, Liu S, Zhao LG, He Z (2009) Design and in vivo evaluation of an indapamide transdermal patch. Int J Pharm 370:129CrossRefPubMed

Rogers EH, Hunter III ES, Moser VC, Phillips PM, Herkovitz J, Mun˜oz L, Hall LL, Chernoff N (2005) Potential developmental toxicity of Anatoxin-a, a cyanobacterial toxin. J Appl Toxicol 25:527

Rowland M, Tozer TN (1996) Clinical pharmacokinetics: concepts and applications. BI Waverly Pvt. Ltd, New Delhi, p 469

Singh AK, Verma J, Bhatnagar A, Sen S, Bose M (2003) Tc-99 m Isoniazid:a specific agent for diagnosis of tuberculosis. World J Nucl Med 2:292

Solana RP, Harris LW, Carter WH, Talbot BG, Carchman RA, Gennings C (1990) Evaluation of a two drug combination pretreatment against organophosphate exposure. Toxicol Appl Pharmacol 102:421CrossRefPubMed

Soliakov L, Gallagher T, Wonnacott S (1995) Anatoxin-A evoked [³H] dopamine release from rat striatal synaptosomes. Neuropharmacology 34:1535CrossRefPubMed

Somani SM, Khalique A (1985) Determination of physostigmine in plasma and brain by HPLC. J Anal Toxicol 9:71CrossRefPubMed

Stone D, Bress W (2007) Addressing public health risks for cyanobacteria in recreational freshwaters: the Oregon and Vermont framework. Integrat Environ Assessm Manag 3:137CrossRef

Sun Y, Fang L, Zhu M, Li W, Meng P, Li L, He Z (2009) A drug-in-adhesive transdermal patch for S-amlodipine free base: in vitro and in vivo characterization. Int J Pharm 382:165CrossRefPubMed

Thomas P, Stephens M, Wilkie G, Amar M, Lunt GG, Whiting P, Gallagher T, Pereira E, Alkondon M, Albuquerque EX, Wonnacott S (1993) (+)-Anatoxin-a is a potent agonist at neural nicotinic acetylcholine receptors. J Neurochem 60:2308CrossRefPubMed

Toutain PL, Bousquet-me´lou A (2004) Plasma terminal half-life. J Vet Pharmacol Therap 27:427CrossRef

Unni LK, Hannant ME, Becker RE, Glacobini E (1989) Determination of physostigmine in plasma and cerebrospinal fluid by liquid chromatography with electrochemical detection. Clin Chem 35:292PubMed

Valiverti S, Hammell DC, Paudel IS, Hamad MO, Crooks PA, Stinchcomb AL (2005) In vivo evaluation of 3-alkyl ester transdermal prodrugs of naltrexone in hairless guinea pigs. J Control Release 102:509CrossRef

Wagner JG, Nelson E (1963) Percent absorbed time plots derived from blood level and/or urinary excretion data. J Pharm Sci 52:610CrossRefPubMed

Walter K, Muller M, Barkworth MF, Nieciecki AV, Stanislaus F (1995) Pharmacokinetics of physostigmine in man following a single application of a transdermal system. Br J Clin Pharmacol 39:59CrossRefPubMedPubMedCentral

Whelpton R (1983) Analysis of plasma physostigmine concentrations by liquid chromatography. J Chromatogr 272:216CrossRefPubMed

Whelpton R, Moore T (1985) Sensitive liquid chromatographic method for physostigmine in biological fluids using dual-electrode electrochemical detection. J Chromatogr 341:361CrossRefPubMed

Willems JL, Langenberg JP, Verstraete AG, Loose MD, Vanhaesebroeck B, Goethals G, Belpaire FM, Buylaert WA, Vogelaers D, Colardyn F (1992) Plasma concentrations of pralidoxime methylsulphate in organophosphorus poisoned patients. Arch Toxicol 66:260CrossRefPubMed

Ye JC, Zeng S, Zheng GL, Chen GS (2008) Pharmacokinetics of huperzine A after transdermal and oral administration in beagle dogs. Int J Pharm 356:187CrossRefPubMed

Young AC, Choi JK, Choi YK, Ki HM, Bae JH (2010) A novel transdermal patch incorporating meloxicam: in vitro and in vivo characterization. Int J Pharm 385:12CrossRef

Zhao B, Moochhala SM, Chaw CS, Yang YY (2003) Simple liquid chromatographic method for the determination of physostigmine and its metabolite eseroline in rat plasma: application to a pharmacokinetic study. J Chromatogr B 784:323CrossRef

Zhao JH, Fu JH, Wang SM, Su CH, Shan Y, Kong SJ, Wang Y, Lu WL, Zhang H, Zhang S, Li L, Zhang EH, Wang L, Pei QL, Wang JC, Zhang X, Zhang Q (2007) A novel transdermal patch incorporating isosorbide dinitrate with bisoprolol: in vitro and in vivo characterization. Int J Pharm 337:88CrossRefPubMed

Zhao L, Li Y, Fang L, He Z, Liu X, Wang L, Xu Y, Ren C (2009) Transdermal delivery of tolterodine by o-acylmenthol:in vitro/in vivo correlation. Int J Pharm 374:73CrossRefPubMed

Title: Pharmacokinetic and biodistribution study of eserine and pralidoxime chloride in rabbits following a single application of a transdermal patch
Authors: Subham Banerjee
Pronobesh Chattopadhyay
Animesh Ghosh
Aseem Bhatnagar
Vijay Veer
Publication date: 01-06-2016
Publisher: Springer International Publishing
Published in: European Journal of Drug Metabolism and Pharmacokinetics / Issue 3/2016
Print ISSN: 0378-7966
Electronic ISSN: 2107-0180
DOI: https://doi.org/10.1007/s13318-014-0250-5

At a glance: The STEP trials

Springer Medicine

Pharmacokinetic and biodistribution study of eserine and pralidoxime chloride in rabbits following a single application of a transdermal patch

Abstract

At a glance: The STEP trials

Springer Medicine

Abstract

Please log in to get access to this content

Other articles of this Issue 3/2016

Physiologically based modeling of the pharmacokinetics of acetaminophen and its major metabolites in humans using a Bayesian population approach

Comparison of pharmacokinetic and safety profiles between Bemfola® and Gonal-f® after subcutaneous application

Preparation, characterization and pharmacokinetics evaluation of clarithromycin-loaded Eudragit® L-100 microspheres

The CYP4502D6 *4 and *6 alleles are the molecular genetic markers for drug response: implications in colchicine non-responder FMF patients

A comparison of the pharmacokinetics of three different preparations of total flavones of Hippophae rhamnoides in beagle dogs after oral administration

Effects of dose, flow rate, and bile acid on diclofenac disposition in the perfused rat liver

The CYP4502D6 4 and 6 alleles are the molecular genetic markers for drug response: implications in colchicine non-responder FMF patients