Intestinal permeability studies for piperaquine from dihydroartemisinin—piperaquine antimalarial product in the presence of lamivudine

Sunday O. Awofisayo; Ayodeji A. Agboke; Ekpedeme N. Essien; Chioma N. Igwe

doi:10.7324/JAPS.2018.81115

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Abstract

The study assessed the intestinal permeability of piperaquine (PQ) from dihydroartemisinin–piperaquine (DP) antimalarial in the presence of lamivudine (LMV). Excised tissues (duodenum and ileum) from New Zealand male albino rabbits (n = 2) were loaded with a suspension of DP equivalent to PQ (100 mg/ml) and LMV (100 mg/ml) and submerged in Tyrode solution (TS). DP suspension was similarly loaded as control. Sampling (5 ml) of TS was done post immersion of tissues and analyzed for PQ permeation using the high pressure liquid chromatographic system. LMV caused a significant increase in PQ permeation across the intestinal membranes. The rate constant (Ka) appearance in organ bath was (0.2457 ± 0.0040 hour−1 vs. 0.0367 ± 0.0008 hour−1, p = 0.010) for duodenum and (0.2428 ± 0.0006 hour−1 vs. 0.0327 ± 0.0021 hour−1, p = 0.008) for ileum. The Ka disappearance of PQ was (1.0121 ± 0.0013 hour−1 vs. 0.7600 ± 0.0008 hour−1, p = 0.001) from duodenum and (1.0092 ± 0.0003 hour−1 vs. 0.7340 ± 0.0072 hour−1, p = 0.017) from ileum. Area under the curve at 6 hours was (1.2868 ± 0.6725 μg.ml hour−1 vs. 3.3975 ± 0.3638 μg.ml hour−1, p = 0.034) for duodenum and (0.7425 ± 0.0089 μg.ml hour−1 vs. 5.6603 ± 0.1073 μg.ml hour−1, p = 0.013) for ileum. Co-loading of LMV with DP ex vivo caused significant uptake from the lumen but significant reduction in PQ permeation across the intestinal regions into the organ bath. This may be of biopharmaceutical implication requiring dosage adjustments.

Keyword: Dihydroartemisinin– piperaquine piperaquine lamivudine permeability intestinal membrane.

Citation:

Awofisayo SO, Agboke AA, Essien EN, Igwe CN. Intestinal permeability studies for piperaquine from dihydroartemisinin—piperaquine antimalarial product in the presence of lamivudine. J Appl Pharm Sci, 2018; 8(11): 103–108.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Reference

Antunes F, Andrade F, Ferreira D, Nielsen HM, Sarmento B. Models to predict intestinal absorption of therapeutic peptides and proteins. Curr Drug Metab, 2013; 14(1):4–20.https://doi.org/10.2174/138920013804545160
Ashley EA, Krudsood S, Phaipun L, Srivilairit S, McGready R, Leowattana W, Hutagalung R, Wilairatana P, Brockman S, Looaresuwaan F, Nosten F, White NJ. Random controlled dose-optimization studies of dihydroartemisinin-piperaquine for the treatment of uncomplicated multi-drug resistant falciparum malaria in Thailand. J Infect Dis, 2004:1773–82.https://doi.org/10.1086/425015
American Medical Association (AMA). World Medical Declaration of Helsinki Ethical Principles for Medical Research involving Human Subjects. J Am Med Assoc, 2003; 310(20):2191–4.
Awofisayo SO, Arhewoh MI, Okhamafe AO. In vitro interaction of food component with Artemether-Lumefantrine tablet. Int J Curr Res Rev, 2018; 10(1):22–6. Bader T, Korba B. Simvastatin potentiates the antihepatitis B virus activity of FDA-approved nucleoside analogue inhibitors in vitro. Antiviral Res, 2010; 86(3):241–5.https://doi.org/10.1016/j.antiviral.2010.02.325
Bazzoni G, Marengoni A, Teltamanti M, Franchi C, Pasina L, Djade CD, Fortino I, Bortolotti A, Merlino L, Nobili A. The drug prescription network: a systemic-level view of drug co-prescription in community-dwelling elderly people. Rejuvenation Res, 2015; 18(2):153–61.https://doi.org/10.1089/rej.2014.1628
Chapman KL, Wilson S. Pharmaceutical toxicology: designing studies to reduce animal use, while maximizing human translation. Regul Toxicol Pharmacol, 2013; 66(1):88–103.https://doi.org/10.1016/j.yrtph.2013.03.001
Centre for Drug Evaluation and Research (CDER). United States Department of Health and Human Services, Food and Drug Administration. Guidance for Industry Drug Interaction Studies— Study Design, Data Analysis, Implication for Dosing and labeling Recommendation, February 2012. Available via http://www.fda.gov/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/defeault.htm (Accessed 10 April 2017).
Caudros DF, Branscum AJ, Crowley PH. HIV-Malaria co-infection: effects of malaria on the prevalence of HIV in East sub-Saharan Africa. Int J Epidemiol, 2011; 40:931–9.https://doi.org/10.1093/ije/dyq256
Department of Health and Human Services (DHHS). Guidelines of panel on antiretroviral for adults and adolescents. Guidelines for the use of antiretroviral agents. 2015. Available via https://adsinfo.nih.gov/contentfiles/ Ivguidelines/adultandadoescentsgl.pdf (Accessed 10 March 2017).
Foca E, Odolini S, Brianese N, Carosi G. Malaria and HIV in adults: when the parasites run into the virus. Mediterr J Haematol Infect Dis, 2012; 4(1):e2012032; doi:10.4084/MJHID.2012.032https://doi.org/10.4084/mjhid.2012.032
German P, Greenhoise B, Coates C, Dorsey G, Rosenthal PJ, Charlebois E. Hepatotoxicity due to a drug interaction between amodiaquine plus artesunate and efavirenz. Clin Infect Dis, 2007; 44:889–91.https://doi.org/10.1086/511882
Gupta AK, Sehrawat A. Bioavailability enhancement of poorly water soluble drugs: a review. IJPLS, 2011; 2(3):640–50.
Henry OJ, Lagoro KD, Orachi CG. Prevalence of malaria and treatment seeking behaviours among pregnant women in postconflict internally displaced persons' camp in Gulu district. ISRN Pub Health, 2012: 1–5 Article ID 164935. http://DX.doi.org/10.5402/2012.
Hetal T, Bimehesi P, Sneha T. A review of techniques for oral bioavailability enhancement of drugs. Int J Pharm Rev Res, 2010; 4(3):201–23.
Li L, Dong, WJ, Sheng L, Xia XJ, Li Y, Liu YL. Preparation, formation mechanism and preliminary evaluation of oral absorption of a Biocyclol-phospholipid complex. Yao Xue Xue Bao, 2014; 49(11):1600–6.
Luo Z, Liu. Y, Zhao B, Tang M, Dong H, Zhang L. Ex vivo and in situ approaches used to study intestinal absorption. J Pharmacol Toxicol Method, 2013; 68(2):208–16.https://doi.org/10.1016/j.vascn.2013.06.001
Mave V, Kadam D, Kinikar A, Gupte N, Bhattacharya D, Bharadadwaj R. Impact of maternal hepatitis B virus co-infection on mother-to-child transmission of HIV. HIV Med, 2014; 15:347–54.https://doi.org/10.1111/hiv.12120
Mori AT, Ngalesoni F, Norheim OF, Robberstad B. Cost effectiveness of dihydroartemisinin-piperaquine with artemether-lumefantrine for treating uncomplicated malaria in children at a district hospital in Tanzania. Malar J, 2014; 13:363–70.https://doi.org/10.1186/1475-2875-13-363
Margolis HS, Coleman PJ, Brown RE, Mast EE, Sheingold SH, Arevalo JA. Prevention of hepatitis B virus transmission by immunization: an economic analysis of current recommendations. JAMA, 1995; 274(15):1201–8.https://doi.org/10.1001/jama.1995.03530150025029
Moore SJ, Min X, Hill N, Jones C, Zaixing Z, Cameron MM. Border malaria in China: Knowledge and use of personal protection by minority populations for malaria control. A quesstionnaire-based survey. BMC Pub Health, 2008. 8: 344–54. https://doi.org/10.1186/1471
Neuman MG, Schneider M, Nanau RM, Parry C. HIV-antiretroviral therapy induced liver, gastrointestinal and pancreatic injury. Int J Hepatology, 2012:1–23. doi:10.1155/2012/760706 (Accessed 23 October 2017).https://doi.org/10.1155/2012/760706
Oshikoya KA, Oreagba IA, Lawal S, Awodele O, Ogunleye OO, Senbanjo IO, Olayemi SO, Ezeaka VC, Temiye EO, Adeyemo TA, Opanuga O, Lesii OA, Akanmu SA. Potential drug interactions in HIV-infected children on antiretroviral therapy in Lagos, Nigeria. HIV AIDS (Auckl), 2014; 6:49–59.https://doi.org/10.2147/HIV.S52266
Piscitelli SC, Galliciano KD. Interactions among drugs for HIV and opportunistic infections. N Engl J Med, 2001; 344(13):984–96.https://doi.org/10.1056/NEJM200103293441307
Qureshi S. Drug interactions with antiretroviral therapy, 2016. Available via http://emedicine.Medscape (Accessed 12 February 2018).
Rijken MJ, McGready R, Phyo AP, Lindergardh N, Tarning NL, Than HH, Mu O, Win AK, Singhasivanon P, White N, Nosten F. Pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and non-pregnant women with uncomplicated falciparum malaria. Antimicrob Agents Chemother, 2011; 55(12):5500–6.https://doi.org/10.1128/AAC.05067-11
Sharma M, Sharma R, Jain DJ. Nanotechnology based approaches for enhancing oral bioavailability of poorly water soluble antihypertensive drugs. Scientifica, 2016; 1:1–12. doi:10.1155/2016/8525679https://doi.org/10.1155/2016/8525679
Shugart S, Benet LZ. The role of transporters in the pharmacokinetics of orally administered drugs. Pharm Res, 2009; 26(9):2039–54.https://doi.org/10.1007/s11095-009-9924-0
Suzuki M, Sai JK, Shimizu T. Acute pancreatitis in children and adolescents. W J Gastroenterol Pathophysiol, 2014; 5(4):416–20.https://doi.org/10.4291/wjgp.v5.i4.416
Tarning J, Ashley EA, Lindegardh N, Stepniewska K, Phaiphun L, Day PJ, McGready R, Ashton M, Nosten F, White NJ. Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand. Antimicrob Agents Chemother, 2008; 52(3):1052–61.https://doi.org/10.1128/AAC.00955-07
Thanh NV, Thuy-Nhien N, Tuyen NTK, Tong NT, Nha-Ca NT, Dong LT, Quang HH, Farrar J, Thwaites G, White NJ, Wolbers M, Hien TT. Rapid decline of the susceptibility of Plasmodium falciparum to dihydroartemisinin-piperaquine in the south of Vietnam. Malar J, 2017; 16:27.https://doi.org/10.1186/s12936-017-1680-8
Tseng A. Interactions between acid-reducing agents and antiretrovirals. Toronto General Hospital, Toronto, Ontario, 2015. Available via http://www.hivclinic.ca (Accessed 2 March 2018).
Uriel A, Lewthwaite P. Malaria therapy in HIV: Drug interactions between nevirapine and quinine. Int J STD AIDS, 2011; 22(12):768–75; doi:10.1258/ijsa2009.009489
Verma P, Thakur AS, Deshmukh KH, Jha AK, Verma S. Routes of drug administration. Int J Pharm Sci Res, 2010; 1(1):54–9.
Whirl-Carrillo M, McDonagh EM, Hebert JM, Gong L, Sangkuhl K, Thorn CJ, Altman RB, Patel JR, Barve KH. Intestinal permeability of lamivudine using single pass intestinal perfusion. Indian J Pharm Sci, 2012; 74(5):478–81.https://doi.org/10.4103/0250-474X.108441
Yuen GJ, Morris DM, Mydlow PK, Haidar S, Hall ST, Hussey EK. Pharmacokinetics, absolute bioavailability, and absorption characteristics of lamivudine. J Clin Pharmacol, 1995; 35(12):1174–80.https://doi.org/10.1002/j.1552-4604.1995.tb04043.x
Zhang C, Mcllerton H, Pen Y. Population pharmacokinetics of lopinavir and ritonavir in combination with rifampicin-based antitubercular treatment in HIV-infected children. Antiviral Ther, 2012; 25–33.

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Antunes F, Andrade F, Ferreira D, Nielsen HM, Sarmento B. Models to predict intestinal absorption of therapeutic peptides and proteins. Curr Drug Metab, 2013; 14(1):4–20.https://doi.org/10.2174/138920013804545160

Ashley EA, Krudsood S, Phaipun L, Srivilairit S, McGready R, Leowattana W, Hutagalung R, Wilairatana P, Brockman S, Looaresuwaan F, Nosten F, White NJ. Random controlled dose-optimization studies of dihydroartemisinin-piperaquine for the treatment of uncomplicated multi-drug resistant falciparum malaria in Thailand. J Infect Dis, 2004:1773–82.https://doi.org/10.1086/425015

American Medical Association (AMA). World Medical Declaration of Helsinki Ethical Principles for Medical Research involving Human Subjects. J Am Med Assoc, 2003; 310(20):2191–4.

Awofisayo SO, Arhewoh MI, Okhamafe AO. In vitro interaction of food component with Artemether-Lumefantrine tablet. Int J Curr Res Rev, 2018; 10(1):22–6. Bader T, Korba B. Simvastatin potentiates the antihepatitis B virus activity of FDA-approved nucleoside analogue inhibitors in vitro. Antiviral Res, 2010; 86(3):241–5.https://doi.org/10.1016/j.antiviral.2010.02.325

Bazzoni G, Marengoni A, Teltamanti M, Franchi C, Pasina L, Djade CD, Fortino I, Bortolotti A, Merlino L, Nobili A. The drug prescription network: a systemic-level view of drug co-prescription in community-dwelling elderly people. Rejuvenation Res, 2015; 18(2):153–61.https://doi.org/10.1089/rej.2014.1628

Chapman KL, Wilson S. Pharmaceutical toxicology: designing studies to reduce animal use, while maximizing human translation. Regul Toxicol Pharmacol, 2013; 66(1):88–103.https://doi.org/10.1016/j.yrtph.2013.03.001

Centre for Drug Evaluation and Research (CDER). United States Department of Health and Human Services, Food and Drug Administration. Guidance for Industry Drug Interaction Studies— Study Design, Data Analysis, Implication for Dosing and labeling Recommendation, February 2012. Available via http://www.fda.gov/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/defeault.htm (Accessed 10 April 2017).

Caudros DF, Branscum AJ, Crowley PH. HIV-Malaria co-infection: effects of malaria on the prevalence of HIV in East sub-Saharan Africa. Int J Epidemiol, 2011; 40:931–9.https://doi.org/10.1093/ije/dyq256

Department of Health and Human Services (DHHS). Guidelines of panel on antiretroviral for adults and adolescents. Guidelines for the use of antiretroviral agents. 2015. Available via https://adsinfo.nih.gov/contentfiles/ Ivguidelines/adultandadoescentsgl.pdf (Accessed 10 March 2017).

Foca E, Odolini S, Brianese N, Carosi G. Malaria and HIV in adults: when the parasites run into the virus. Mediterr J Haematol Infect Dis, 2012; 4(1):e2012032; doi:10.4084/MJHID.2012.032https://doi.org/10.4084/mjhid.2012.032

German P, Greenhoise B, Coates C, Dorsey G, Rosenthal PJ, Charlebois E. Hepatotoxicity due to a drug interaction between amodiaquine plus artesunate and efavirenz. Clin Infect Dis, 2007; 44:889–91.https://doi.org/10.1086/511882

Gupta AK, Sehrawat A. Bioavailability enhancement of poorly water soluble drugs: a review. IJPLS, 2011; 2(3):640–50.

Henry OJ, Lagoro KD, Orachi CG. Prevalence of malaria and treatment seeking behaviours among pregnant women in postconflict internally displaced persons' camp in Gulu district. ISRN Pub Health, 2012: 1–5 Article ID 164935. http://DX.doi.org/10.5402/2012.

Hetal T, Bimehesi P, Sneha T. A review of techniques for oral bioavailability enhancement of drugs. Int J Pharm Rev Res, 2010; 4(3):201–23.

Li L, Dong, WJ, Sheng L, Xia XJ, Li Y, Liu YL. Preparation, formation mechanism and preliminary evaluation of oral absorption of a Biocyclol-phospholipid complex. Yao Xue Xue Bao, 2014; 49(11):1600–6.

Luo Z, Liu. Y, Zhao B, Tang M, Dong H, Zhang L. Ex vivo and in situ approaches used to study intestinal absorption. J Pharmacol Toxicol Method, 2013; 68(2):208–16.https://doi.org/10.1016/j.vascn.2013.06.001

Mave V, Kadam D, Kinikar A, Gupte N, Bhattacharya D, Bharadadwaj R. Impact of maternal hepatitis B virus co-infection on mother-to-child transmission of HIV. HIV Med, 2014; 15:347–54.https://doi.org/10.1111/hiv.12120

Mori AT, Ngalesoni F, Norheim OF, Robberstad B. Cost effectiveness of dihydroartemisinin-piperaquine with artemether-lumefantrine for treating uncomplicated malaria in children at a district hospital in Tanzania. Malar J, 2014; 13:363–70.https://doi.org/10.1186/1475-2875-13-363

Margolis HS, Coleman PJ, Brown RE, Mast EE, Sheingold SH, Arevalo JA. Prevention of hepatitis B virus transmission by immunization: an economic analysis of current recommendations. JAMA, 1995; 274(15):1201–8.https://doi.org/10.1001/jama.1995.03530150025029

Moore SJ, Min X, Hill N, Jones C, Zaixing Z, Cameron MM. Border malaria in China: Knowledge and use of personal protection by minority populations for malaria control. A quesstionnaire-based survey. BMC Pub Health, 2008. 8: 344–54. https://doi.org/10.1186/1471

Neuman MG, Schneider M, Nanau RM, Parry C. HIV-antiretroviral therapy induced liver, gastrointestinal and pancreatic injury. Int J Hepatology, 2012:1–23. doi:10.1155/2012/760706 (Accessed 23 October 2017).https://doi.org/10.1155/2012/760706

Oshikoya KA, Oreagba IA, Lawal S, Awodele O, Ogunleye OO, Senbanjo IO, Olayemi SO, Ezeaka VC, Temiye EO, Adeyemo TA, Opanuga O, Lesii OA, Akanmu SA. Potential drug interactions in HIV-infected children on antiretroviral therapy in Lagos, Nigeria. HIV AIDS (Auckl), 2014; 6:49–59.https://doi.org/10.2147/HIV.S52266

Piscitelli SC, Galliciano KD. Interactions among drugs for HIV and opportunistic infections. N Engl J Med, 2001; 344(13):984–96.https://doi.org/10.1056/NEJM200103293441307

Qureshi S. Drug interactions with antiretroviral therapy, 2016. Available via http://emedicine.Medscape (Accessed 12 February 2018).

Rijken MJ, McGready R, Phyo AP, Lindergardh N, Tarning NL, Than HH, Mu O, Win AK, Singhasivanon P, White N, Nosten F. Pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and non-pregnant women with uncomplicated falciparum malaria. Antimicrob Agents Chemother, 2011; 55(12):5500–6.https://doi.org/10.1128/AAC.05067-11

Sharma M, Sharma R, Jain DJ. Nanotechnology based approaches for enhancing oral bioavailability of poorly water soluble antihypertensive drugs. Scientifica, 2016; 1:1–12. doi:10.1155/2016/8525679https://doi.org/10.1155/2016/8525679

Shugart S, Benet LZ. The role of transporters in the pharmacokinetics of orally administered drugs. Pharm Res, 2009; 26(9):2039–54.https://doi.org/10.1007/s11095-009-9924-0

Suzuki M, Sai JK, Shimizu T. Acute pancreatitis in children and adolescents. W J Gastroenterol Pathophysiol, 2014; 5(4):416–20.https://doi.org/10.4291/wjgp.v5.i4.416

Tarning J, Ashley EA, Lindegardh N, Stepniewska K, Phaiphun L, Day PJ, McGready R, Ashton M, Nosten F, White NJ. Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand. Antimicrob Agents Chemother, 2008; 52(3):1052–61.https://doi.org/10.1128/AAC.00955-07

Thanh NV, Thuy-Nhien N, Tuyen NTK, Tong NT, Nha-Ca NT, Dong LT, Quang HH, Farrar J, Thwaites G, White NJ, Wolbers M, Hien TT. Rapid decline of the susceptibility of Plasmodium falciparum to dihydroartemisinin-piperaquine in the south of Vietnam. Malar J, 2017; 16:27.https://doi.org/10.1186/s12936-017-1680-8

Tseng A. Interactions between acid-reducing agents and antiretrovirals. Toronto General Hospital, Toronto, Ontario, 2015. Available via http://www.hivclinic.ca (Accessed 2 March 2018).

Uriel A, Lewthwaite P. Malaria therapy in HIV: Drug interactions between nevirapine and quinine. Int J STD AIDS, 2011; 22(12):768–75; doi:10.1258/ijsa2009.009489

Verma P, Thakur AS, Deshmukh KH, Jha AK, Verma S. Routes of drug administration. Int J Pharm Sci Res, 2010; 1(1):54–9.

Whirl-Carrillo M, McDonagh EM, Hebert JM, Gong L, Sangkuhl K, Thorn CJ, Altman RB, Patel JR, Barve KH. Intestinal permeability of lamivudine using single pass intestinal perfusion. Indian J Pharm Sci, 2012; 74(5):478–81.https://doi.org/10.4103/0250-474X.108441

Yuen GJ, Morris DM, Mydlow PK, Haidar S, Hall ST, Hussey EK. Pharmacokinetics, absolute bioavailability, and absorption characteristics of lamivudine. J Clin Pharmacol, 1995; 35(12):1174–80.https://doi.org/10.1002/j.1552-4604.1995.tb04043.x

Zhang C, Mcllerton H, Pen Y. Population pharmacokinetics of lopinavir and ritonavir in combination with rifampicin-based antitubercular treatment in HIV-infected children. Antiviral Ther, 2012; 25–33.