Formulation of Dihydroartemisinin-Piperaquine (DHP) Generic Tablet as Antimalarials Drug
Keywords:
Dihydroartemisinin, Piperaquine, Tablets, Film coated
Abstract
The incidence of malaria in Indonesia is about two million cases annually. Dihydroartemisinin-piperaquine (DHP) is the first line therapy recommended for uncomplicated malaria treatment, whereas DHP is still fully imported. The generic DHP tablet formulation has the potential to become the first of DHP drug which is locally produced. This study is aimed to formulate generic DHP film coated tablets for antimalaria drug. Tablets were compressed with the combination of wet granulation for piperaquine phosphate (PQP) and direct compression method for DHA and coated with a moisture barier coating material. The parameters to evaluate the quality of DHP tablets are physical properties, assay, and dissolution test. DHA and PQP assay were performed by HPLC method. The dissolution testing was conducted by in house method using HCl 0.1 N medium. The result shows physical properties of filmcoated tablets meet the requirement, i.e. uniform weight, 7.0-8.5 kp hardness, 0.02% friability and 3 minute 22 seconds disintegration. The assay to determine DHA in tablet was 95.17% and PQP was 97.05%. The result of dissolution testing shows the content of DHA and PQP in the tablet were 113.51% and 96.55%, respesctively. The formulation which is developed meets the general requirement of API in tablet 90–110% and dissolution requirement >75%.References
1. WHO. World Malaria Report 2015. Geneva: World Health Organization; 2015.
2. Badan Penelitian dan Pengembangan Kesehatan (Balitbangkes) Kementerian Kesehatan (Kemenkes) Republik Indonesia (RI). Riset kesehatan dasar (Riskesdas) 2010. Jakarta: Balitbangkes Kemenkes RI; 2010.
3. Badan Penelitian dan Pengembangan Kesehatan (Balitbangkes) Kementerian Kesehatan (Kemenkes) Republik Indonesia (RI). Riset kesehatan dasar (Riskesdas) 2013. Jakarta: Balitbangkes Kemenkes RI; 2013.
4. Murray CJL, Ortblad KF, Guinovart C, Lim SS, Wolock TM, Roberts DA, et al. Global, regional, and national incidence and mortality for HIV, tuberculosis, and malaria during 1990–2013: a systematic analysis for the Global Burden of Disease Study 2013. Lancet. 2014;384(9947):1005-70.
5. Laporan Malaria Indonesia 2014. Jakarta: Direktorat Pengendalian Penyakit Bersumber Binatang, Direktorat Jenderal PP & PL, Kementerian Kesehatan RI; 2014.
6. Sinclair D, Zani B, Donegan S, Olliaro P, Garner P. Artemisinin-based combination therapy for treating uncomplicated malaria (Review). Cochrane Database of Systematic Reviews. 2009;8(3):CD007483.
7. Pedoman penatalaksanaan kasus malaria di Indonesia. Jakarta: Direktorat Jenderal Pengendalian Penyakit dan Penyehatan Lingkungan, Kementerian Kesehatan RI; 2008.
8. Pedoman penatalaksanaan kasus malaria di Indonesia. Jakarta: Direktorat Jenderal Pengendalian Penyakit dan Penyehatan Lingkungan, Kementerian Kesehatan RI; 2011.
9. Hasugian AR, Purba HLE, Kenangalem E, Wuwung RM, Ebsworth EP, Maristela R, et al. Dihydroartemisinin-piperaquine versus artesunate-amodiaquine: superior efficacy and posttreatment prophylaxis against multidrug-resistant Plasmodium falciparum and Plasmodium vivax malaria. Clin Infect Dis. 2007;44(8):1067–74.
10. Ratcliff A, Siswantoro H, Maristela R, Kenangalem E, Laihad S, Ebsworth EP, et al. Two fixed-dose artemisinin combinations for drug-resistant falciparum and vivax malaria in Papua, Indonesia: an open-label randomised comparison. Lancet. 2007;369(9563):757-65.
11. Myint HY, Ashley EA, Day NPJ, Nosten F, White NJ. Efficacy and safety of dihydroartemisinin-piperaquine. Transac-tions of the Royal Society of Tropical Medicine and Hygiene. 2007;101(9):858-66.
12. Zani B, Gathu M, Donegan S, Olliaro PL, Sinclair D. Dihydroartemisinin-piperaquine for treating uncomplicated Plasmodium falciparum malaria. Cochrane Database of Systematic Reviews. 2014;1: CD010927.
13. Republik Indonesia. Keputusan Menteri Kesehatan Republik Indonesia Nomor HK.02.02/MENKES/523/2015 tentang Formularium Nasional. Jakarta:
Kementerian Kesehatan; 2014.
14. Farmakope Indonesia. Edisi V. Jakarta: Kementerian Kesehatan RI; 2014.
15. Lacaze C, Kauss T, Kiechel JR, Caminiti A, Fawaz F, Terrassin L, et al. The initial pharmaceutical development of an artesunate/amodiaquine oral formulation for the treatment of malaria: a public-private partnership. Malaria Journal. 2011;10:142: 1-12.
16. Rowe RC, Sheskey PJ, Quinn ME, editors. Handbook of pharmaceutical excipients 6th ed. London: Pharmaceutical Press; 2009.
17. The United States Pharmacopeial Convention. The United States Pharmacopeia-National Formulary. 34th ed. Maryland: The United States Pharmacopeia Convention; 2011.
18. Krämer J. Establishing a relationship between disintegration and dissolution [Internet]. 2009 [cited 2014 Dec 18]. Available from: https://www.aaps.org/ uploadedFiles/Content/Sections_and_Groups/Focus_Groups/KramerSA2.pdf
19. Brunton LL, Parker KL, Blumenthal DK, Buxton ILO, editors. Goodman & Gilman: manual farmakologi dan terapi. Jakarta: EGC; 2010.
20. Jones D. Fasttrack pharmaceutics: Dosage form and design. London: Pharmaceutical Press; 2008.
21. Augsburger L, Hoag S, editors. Pharmaceutical Dosage Forms - Tablets Volume 1 [Internet]. 3rd ed. New York: Informa Healthcare; 2008. Available from: http://www.crcnetbase.com/isbn/9781420025989
2. Badan Penelitian dan Pengembangan Kesehatan (Balitbangkes) Kementerian Kesehatan (Kemenkes) Republik Indonesia (RI). Riset kesehatan dasar (Riskesdas) 2010. Jakarta: Balitbangkes Kemenkes RI; 2010.
3. Badan Penelitian dan Pengembangan Kesehatan (Balitbangkes) Kementerian Kesehatan (Kemenkes) Republik Indonesia (RI). Riset kesehatan dasar (Riskesdas) 2013. Jakarta: Balitbangkes Kemenkes RI; 2013.
4. Murray CJL, Ortblad KF, Guinovart C, Lim SS, Wolock TM, Roberts DA, et al. Global, regional, and national incidence and mortality for HIV, tuberculosis, and malaria during 1990–2013: a systematic analysis for the Global Burden of Disease Study 2013. Lancet. 2014;384(9947):1005-70.
5. Laporan Malaria Indonesia 2014. Jakarta: Direktorat Pengendalian Penyakit Bersumber Binatang, Direktorat Jenderal PP & PL, Kementerian Kesehatan RI; 2014.
6. Sinclair D, Zani B, Donegan S, Olliaro P, Garner P. Artemisinin-based combination therapy for treating uncomplicated malaria (Review). Cochrane Database of Systematic Reviews. 2009;8(3):CD007483.
7. Pedoman penatalaksanaan kasus malaria di Indonesia. Jakarta: Direktorat Jenderal Pengendalian Penyakit dan Penyehatan Lingkungan, Kementerian Kesehatan RI; 2008.
8. Pedoman penatalaksanaan kasus malaria di Indonesia. Jakarta: Direktorat Jenderal Pengendalian Penyakit dan Penyehatan Lingkungan, Kementerian Kesehatan RI; 2011.
9. Hasugian AR, Purba HLE, Kenangalem E, Wuwung RM, Ebsworth EP, Maristela R, et al. Dihydroartemisinin-piperaquine versus artesunate-amodiaquine: superior efficacy and posttreatment prophylaxis against multidrug-resistant Plasmodium falciparum and Plasmodium vivax malaria. Clin Infect Dis. 2007;44(8):1067–74.
10. Ratcliff A, Siswantoro H, Maristela R, Kenangalem E, Laihad S, Ebsworth EP, et al. Two fixed-dose artemisinin combinations for drug-resistant falciparum and vivax malaria in Papua, Indonesia: an open-label randomised comparison. Lancet. 2007;369(9563):757-65.
11. Myint HY, Ashley EA, Day NPJ, Nosten F, White NJ. Efficacy and safety of dihydroartemisinin-piperaquine. Transac-tions of the Royal Society of Tropical Medicine and Hygiene. 2007;101(9):858-66.
12. Zani B, Gathu M, Donegan S, Olliaro PL, Sinclair D. Dihydroartemisinin-piperaquine for treating uncomplicated Plasmodium falciparum malaria. Cochrane Database of Systematic Reviews. 2014;1: CD010927.
13. Republik Indonesia. Keputusan Menteri Kesehatan Republik Indonesia Nomor HK.02.02/MENKES/523/2015 tentang Formularium Nasional. Jakarta:
Kementerian Kesehatan; 2014.
14. Farmakope Indonesia. Edisi V. Jakarta: Kementerian Kesehatan RI; 2014.
15. Lacaze C, Kauss T, Kiechel JR, Caminiti A, Fawaz F, Terrassin L, et al. The initial pharmaceutical development of an artesunate/amodiaquine oral formulation for the treatment of malaria: a public-private partnership. Malaria Journal. 2011;10:142: 1-12.
16. Rowe RC, Sheskey PJ, Quinn ME, editors. Handbook of pharmaceutical excipients 6th ed. London: Pharmaceutical Press; 2009.
17. The United States Pharmacopeial Convention. The United States Pharmacopeia-National Formulary. 34th ed. Maryland: The United States Pharmacopeia Convention; 2011.
18. Krämer J. Establishing a relationship between disintegration and dissolution [Internet]. 2009 [cited 2014 Dec 18]. Available from: https://www.aaps.org/ uploadedFiles/Content/Sections_and_Groups/Focus_Groups/KramerSA2.pdf
19. Brunton LL, Parker KL, Blumenthal DK, Buxton ILO, editors. Goodman & Gilman: manual farmakologi dan terapi. Jakarta: EGC; 2010.
20. Jones D. Fasttrack pharmaceutics: Dosage form and design. London: Pharmaceutical Press; 2008.
21. Augsburger L, Hoag S, editors. Pharmaceutical Dosage Forms - Tablets Volume 1 [Internet]. 3rd ed. New York: Informa Healthcare; 2008. Available from: http://www.crcnetbase.com/isbn/9781420025989
Published
2016-02-29
How to Cite
1.
Yunarto N, Isnawati A, Aini N, Kurniatri A, Adelina R, Setyorini H. Formulation of Dihydroartemisinin-Piperaquine (DHP) Generic Tablet as Antimalarials Drug. jki [Internet]. 29Feb.2016 [cited 3Jul.2024];6(1):8-5. Available from: http://ejournal2.litbang.kemkes.go.id/index.php/jki/article/view/2911
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