Main Article Content
Abstract
Introduction. Depuis quelques années, les Combinaisons Thérapeutiques à base d’Artémisinine (CTA) sont l’objet de nombreux cas de résistances thérapeutiques. Par ailleurs, plusieurs études ont démontré l’efficacité d’Artemisia annua (Asteraceae) sur les formes résistantes de Plasmodium. Ce travail a donc pour objectif de mettre au point des gélules à base de la poudre de feuilles et de tiges d’A. annua afin d’améliorer la prise en charge du paludisme en Afrique. Méthodes. Cette étude a consisté à caractériser la poudre et les granulés d’A. annua, obtenus par granulation humide par ajout de l’empois d’amidon de maïs. Puis des gélules dosées à 125 mg d’A. annua, ont été formulées et contrôlées selon la pharmacopée européenne 9e éd. Résultats. L’analyse granulométrique de la poudre a donné un diamètre médian (d50) inferieur à 50 µm et 600 µm pour les granulés. Les gélules obtenues, ont une répartition uniforme de la masse (125,7 mg). Le temps de désagrégation des gélules est de 3,5 ± 1,4 mn. Les teneurs en flavonoïdes totaux de la poudre et des gélules sont de 8,8 ± 1,2 mg et 1,6 ± 0,1 mg équivalent de quercétine. Conclusion. Ce travail a permis de mettre au point des gélules à base de feuilles et de tiges d’A. annua conformes à la Pharmacopée européenne 9e éd.
ABSTRACT
Introduction. In recent years, Artemisinin-based Therapeutic Combinations (CTAs) was the subject of numerous cases of therapeutic resistance. In addition, several studies have demonstrated the efficacy of Artemisia annua (Asteraceae) on the resistant forms of Plasmodium. This work therefore aims to develop capsules based on the powder of leaves and stems of A. annua to improve the management of malaria in Africa. Methods. This study consisted in characterizing the powder and granules of A. annua, obtained by wet granulation by adding corn starch paste. Then capsules containing 125 mg of A. annua, have been formulated and controlled according to the European Pharmacopoeia 9th Ed. Results. The particle size analysis of the powder gave a median diameter (d50) of less than 50 µm and 600 µm for the granules. The capsules obtained have a uniform distribution of mass (125.7 mg). The disintegration time of the capsules is 3.5 ± 1.4 min. The total flavonoid contents of the powder and capsules are 8.8 ± 1.2 mg and 1.6 ± 0.1 mg equivalent of quercétine. Conclusion. This work made it possible to develop capsules based on leaves and stems of A. annua conform to the European Pharmacopoeia 9th Ed.
Article Details
References
- Organisation mondiale de la santé, World malaria report 2018, 2018.
- OMS | Traitement du paludisme. www.who.int/malaria/areas/treatment/overview/fr/
- M.A. Elfawal, M.J. Towler, N.G. Reich, P.J. Weathers, S.M. Rich, Dried whole-plant Artemisia annua slows evolution of malaria drug resistance and overcomes resistance to artemisinin, Proc. Natl. Acad. Sci. 112 (2015) 821–826.
- C. Nsanzabana, Resistance to artemisinin combination therapies (ACTs): do not forget the partner drug!, Trop. Med. Infect. Dis. 4 (2019) 26.
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- J.O. Suberu, A.P. Gorka, L. Jacobs, P.D. Roepe, N. Sullivan, G.C. Barker, A.A. Lapkin, Anti-Plasmodial Polyvalent Interactions in Artemisia annua L. Aqueous Extract – Possible Synergistic and Resistance Mechanisms, PLOS ONE. 8 (2013) e80790. https://doi.org/10.1371/journal.pone.0080790.
- T. Aftab, M. Naeem, M. Idrees, M.M.A. Khan, L. Varshney, Cumulative role of irradiated sodium alginate and nitrogen fertilizer on growth, biochemical processes and artemisinin production in Artemisia annua, Ind. Crops Prod. 50 (2013) 874–881.
- M. Ali, B.H. Abbasi, Production of commercially important secondary metabolites and antioxidant activity in cell suspension cultures of Artemisia absinthium L., Ind. Crops Prod. 49 (2013) 400–406.
- M. Onimus, S. Carteron, P. Lutgen, The surprising efficiency of Artemisia annua powder capsules, Med. Aromat Plants. 2 (2013) 2167–0412.
- Y.-D. Wan, Q.-Z. Zang, J.-S. Wang, Studies on the antimalarial action of gelatin capsule of Artemisia annua, Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 10 (1992) 290–294.
- P.J. Weathers, M.J. Towler, Changes in key constituents of clonally propagated Artemisia annua L. during preparation of compressed leaf tablets for possible therapeutic use, Ind. Crops Prod. 62 (2014) 173–178.
- K. Räth, K. Taxis, G. Walz, C.H. Gleiter, S.-M. Li, L. Heide, Pharmacokinetic study of artemisinin after oral intake of a traditional preparation of Artemisia annua L.(annual wormwood), Am. J. Trop. Med. Hyg. 70 (2004) 128–132.
- S.P. Agarwal, A. Ali, Y. Dua, S. Ahuja, Determination of artemisinin in bulk and pharmaceutical dosage forms using HPTLC, Indian J. Pharm. Sci. 71 (2009) 98.
- G.D. Brown, The biosynthesis of artemisinin (Qinghaosu) and the phytochemistry of Artemisia annua L.(Qinghao), Molecules. 15 (2010) 7603–7698.
- Test No. 105: Water Solubility, (n.d.). https://www.oecd-ilibrary.org/environment/test-no-105-water-solubility_9789264069589-en.
- European Pharmacopoeia 9th Edition | EDQM - European Directorate for the Quality of Medicines, (n.d.). https://www.edqm.eu/en/european-pharmacopoeia-9th-edition.
- P.G.C. Petean, M.L. Aguiar, Determining the adhesion force between particles and rough surfaces, Powder Technol. 274 (2015) 67–76. doi.org/10.1016/j.powtec.2014.12.047.
- A. Alghunaim, S. Kirdponpattara, B.Z. Newby, Techniques for determining contact angle and wettability of powders, Powder Technol. 287 (2016) 201–215. https://doi.org/10.1016/j.powtec.2015.10.002.
- S. Bhaskaran, G.C. Pradeep, P.K. Lakshmi, Formulation and evaluation of Diphenhydramine hydrochloride and Ibuprofen soft gelatin capsules. Http://Www.Japsonline.Com/Counter.Php?Aid=110. (2011).
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- E. Agouri, R. Laputte, J. Rideau, Process for chemical modification of polyolefins to improve their wettability, Google Patents, 1978. www.google.com/patents/US4080405.
- M. Fuji, T. Takei, T. Watanabe, M. Chikazawa, Wettability of fine silica powder surfaces modified with several normal alcohols, Colloids Surf. Physicochem. Eng. Asp. 154 (1999) 13–24.
- S. Iqbal, U. Younas, K.W. Chan, M. Zia-Ul-Haq, M. Ismail, Chemical Composition of Artemisia annua L. Leaves and Antioxidant Potential of Extracts as a Function of Extraction Solvents, Molecules. 17 (2012) 6020–6032. https://doi.org/10.3390/molecules17056020.
- A. Schüssele, A. Bauer-Brandl, Note on the measurement of flowability according to the European Pharmacopoeia, Int. J. Pharm. 257 (2003) 301–304.
- K. Thalberg, D. Lindholm, A. Axelsson, Comparison of different flowability tests for powders for inhalation, Powder Technol. 146 (2004) 206–213. https://doi.org/10.1016/j.powtec.2004.08.003.
- A. Peinado, J. Hammond, A. Scott, Development, validation and transfer of a near infrared method to determine in-line the end point of a fluidised drying process for commercial production batches of an approved oral solid dose pharmaceutical product, J. Pharm. Biomed. Anal. 54 (2011) 13–20.
- W.-J. Sun, H. Chen, A. Aburub, C.C. Sun, A platform direct compression formulation for low dose sustained-release tablets enabled by a dual particle engineering approach, Powder Technol. 342 (2019) 856–863.
- P. Begat, D.A.V. Morton, J.N. Staniforth, R. Price, The Cohesive-Adhesive Balances in Dry Powder Inhaler Formulations I: Direct Quantification by Atomic Force Microscopy, Pharm. Res. 21 (2004) 1591–1597. doi.org/10.1023/B:PHAM.0000041453.24419.8a.
- Fluidization of cohesive powders - ScienceDirect, www.sciencedirect.com/science/article/pii/0032591084800030.
- R. Agrawal, Y. Naveen, Pharmaceutical processing–A review on wet granulation technology, Int. J. Pharm. Front. Res. 1 (2011) 65–83.
- The effect of dry granulation on flow behaviour of pharmaceutical powders during die filling | Request PDF, ResearchGate. (n.d.). http://dx.doi.org/10.1016/j.powtec.2017.08.064.
- P. Arnaud, D. Brossard, J.C. Chaumeil, Effect of the granulation process on nitrofurantoin granule characteristics, Drug Dev. Ind. Pharm. 24 (1998) 57–66.
- M.R. Desrosiers, P.J. Weathers, Effect of leaf digestion and artemisinin solubility for use in oral consumption of dried Artemisia annua leaves to treat malaria, J. Ethnopharmacol. 190 (2016) 313–318.
- M.E. Mustafa, A.O. Nur, Z.A. Osman, S.A. Ahmed, Influence of drug solubility and polymers supply source on the physical performance of matrix tablets, Int J Pharm Pharm Sci. 6 (2014) 308–12.
- J. Munyangi, L. Cornet-Vernet, M. Idumbo, C. Lu, P. Lutgen, C. Perronne, N. Ngombe, J. Bianga, B. Mupenda, P. Lalukala, Artemisia annua and Artemisia afra tea infusions vs. artesunate-amodiaquine (ASAQ) in treating Plasmodium falciparum malaria in a large scale, double blind, randomized clinical trial, Phytomedicine. 57 (2019) 49–56.
- W. Faisal, F. Farag, A.A. Abdellatif, A. Abbas, Taste masking approaches for medicines, Curr. Drug Deliv. 15 (2018) 167–185.
- S.F. Barakh Ali, S. Dharani, H. Afrooz, M.A. Khan, E.M. Mohamed, K. Kohli, Z. Rahman, Application of salt engineering to reduce/mask bitter taste of clindamycin, Drug Dev. Ind. Pharm. (2019) 1–23.
- M. Blessy, R.D. Patel, P.N. Prajapati, Y.K. Agrawal, Development of forced degradation and stability indicating studies of drugs—A review, J. Pharm. Anal. 4 (2014) 159–165.
- P.E. Ogwang, J.O. Ogwal, S. Kasasa, F. Ejobi, D. Kabasa, C. Obua, Use of Artemisia annua L. infusion for malaria prevention: mode of action and benefits in a Ugandan community, Br. J. Pharm. Res. 1 (2011) 124.
- J.F. Ferreira, D.L. Luthria, T. Sasaki, A. Heyerick, Flavonoids from Artemisia annua L. as antioxidants and their potential synergism with artemisinin against malaria and cancer, Molecules. 15 (2010) 3135–3170.
- A.R. Bilia, P.M. de Malgalhaes, M.C. Bergonzi, F.F. Vincieri, Simultaneous analysis of artemisinin and flavonoids of several extracts of Artemisia annua L. obtained from a commercial sample and a selected cultivar, Phytomedicine. 13 (2006) 487–493.
- P.J. Weathers, M.J. Towler, The flavonoids casticin and artemetin are poorly extracted and are unstable in an Artemisia annua tea infusion, Planta Med. 78 (2012) 1024–1026.
- U. Soni, S. Brar, V.K. Gauttam, Effect of seasonal variation on secondary metabolites of medicinal plants, Int. J. Pharm. Sci. Res. 6 (2015) 3654–3662.
- C. van den Berg, C.P.M. Roelands, P. Bussmann, E.L.V. Goetheer, D. Verdoes, L.A.M. van der Wielen, Preparation and analysis of high capacity polysulfone capsules, React. Funct. Polym. 69 (2009) 766–770. https://doi.org/10.1016/j.reactfunctpolym.2009.06.008.
References
Organisation mondiale de la santé, World malaria report 2018, 2018.
OMS | Traitement du paludisme. www.who.int/malaria/areas/treatment/overview/fr/
M.A. Elfawal, M.J. Towler, N.G. Reich, P.J. Weathers, S.M. Rich, Dried whole-plant Artemisia annua slows evolution of malaria drug resistance and overcomes resistance to artemisinin, Proc. Natl. Acad. Sci. 112 (2015) 821–826.
C. Nsanzabana, Resistance to artemisinin combination therapies (ACTs): do not forget the partner drug!, Trop. Med. Infect. Dis. 4 (2019) 26.
N.B. Daddy, L.M. Kalisya, P.G. Bagire, R.L. Watt, M.J. Towler, P.J. Weathers, Artemisia annua dried leaf tablets treated malaria resistant to ACT and iv artesunate, Phytomedicine. 32 (2017) 37–40.
J.O. Suberu, A.P. Gorka, L. Jacobs, P.D. Roepe, N. Sullivan, G.C. Barker, A.A. Lapkin, Anti-Plasmodial Polyvalent Interactions in Artemisia annua L. Aqueous Extract – Possible Synergistic and Resistance Mechanisms, PLOS ONE. 8 (2013) e80790. https://doi.org/10.1371/journal.pone.0080790.
T. Aftab, M. Naeem, M. Idrees, M.M.A. Khan, L. Varshney, Cumulative role of irradiated sodium alginate and nitrogen fertilizer on growth, biochemical processes and artemisinin production in Artemisia annua, Ind. Crops Prod. 50 (2013) 874–881.
M. Ali, B.H. Abbasi, Production of commercially important secondary metabolites and antioxidant activity in cell suspension cultures of Artemisia absinthium L., Ind. Crops Prod. 49 (2013) 400–406.
M. Onimus, S. Carteron, P. Lutgen, The surprising efficiency of Artemisia annua powder capsules, Med. Aromat Plants. 2 (2013) 2167–0412.
Y.-D. Wan, Q.-Z. Zang, J.-S. Wang, Studies on the antimalarial action of gelatin capsule of Artemisia annua, Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 10 (1992) 290–294.
P.J. Weathers, M.J. Towler, Changes in key constituents of clonally propagated Artemisia annua L. during preparation of compressed leaf tablets for possible therapeutic use, Ind. Crops Prod. 62 (2014) 173–178.
K. Räth, K. Taxis, G. Walz, C.H. Gleiter, S.-M. Li, L. Heide, Pharmacokinetic study of artemisinin after oral intake of a traditional preparation of Artemisia annua L.(annual wormwood), Am. J. Trop. Med. Hyg. 70 (2004) 128–132.
S.P. Agarwal, A. Ali, Y. Dua, S. Ahuja, Determination of artemisinin in bulk and pharmaceutical dosage forms using HPTLC, Indian J. Pharm. Sci. 71 (2009) 98.
G.D. Brown, The biosynthesis of artemisinin (Qinghaosu) and the phytochemistry of Artemisia annua L.(Qinghao), Molecules. 15 (2010) 7603–7698.
Test No. 105: Water Solubility, (n.d.). https://www.oecd-ilibrary.org/environment/test-no-105-water-solubility_9789264069589-en.
European Pharmacopoeia 9th Edition | EDQM - European Directorate for the Quality of Medicines, (n.d.). https://www.edqm.eu/en/european-pharmacopoeia-9th-edition.
P.G.C. Petean, M.L. Aguiar, Determining the adhesion force between particles and rough surfaces, Powder Technol. 274 (2015) 67–76. doi.org/10.1016/j.powtec.2014.12.047.
A. Alghunaim, S. Kirdponpattara, B.Z. Newby, Techniques for determining contact angle and wettability of powders, Powder Technol. 287 (2016) 201–215. https://doi.org/10.1016/j.powtec.2015.10.002.
S. Bhaskaran, G.C. Pradeep, P.K. Lakshmi, Formulation and evaluation of Diphenhydramine hydrochloride and Ibuprofen soft gelatin capsules. Http://Www.Japsonline.Com/Counter.Php?Aid=110. (2011).
C.-C. Chang, M.-H. Yang, H.-M. Wen, J.-C. Chern, Estimation of total flavonoid content in propolis by two complementary colorimetric methods, J. Food Drug Anal. 10 (2002).
M.L. Willcox, S. Burton, R. Oyweka, R. Namyalo, S. Challand, K. Lindsey, Evaluation and pharmacovigilance of projects promoting cultivation and local use of Artemisia annua for malaria, Malar. J. 10 (2011) 84.
E. Agouri, R. Laputte, J. Rideau, Process for chemical modification of polyolefins to improve their wettability, Google Patents, 1978. www.google.com/patents/US4080405.
M. Fuji, T. Takei, T. Watanabe, M. Chikazawa, Wettability of fine silica powder surfaces modified with several normal alcohols, Colloids Surf. Physicochem. Eng. Asp. 154 (1999) 13–24.
S. Iqbal, U. Younas, K.W. Chan, M. Zia-Ul-Haq, M. Ismail, Chemical Composition of Artemisia annua L. Leaves and Antioxidant Potential of Extracts as a Function of Extraction Solvents, Molecules. 17 (2012) 6020–6032. https://doi.org/10.3390/molecules17056020.
A. Schüssele, A. Bauer-Brandl, Note on the measurement of flowability according to the European Pharmacopoeia, Int. J. Pharm. 257 (2003) 301–304.
K. Thalberg, D. Lindholm, A. Axelsson, Comparison of different flowability tests for powders for inhalation, Powder Technol. 146 (2004) 206–213. https://doi.org/10.1016/j.powtec.2004.08.003.
A. Peinado, J. Hammond, A. Scott, Development, validation and transfer of a near infrared method to determine in-line the end point of a fluidised drying process for commercial production batches of an approved oral solid dose pharmaceutical product, J. Pharm. Biomed. Anal. 54 (2011) 13–20.
W.-J. Sun, H. Chen, A. Aburub, C.C. Sun, A platform direct compression formulation for low dose sustained-release tablets enabled by a dual particle engineering approach, Powder Technol. 342 (2019) 856–863.
P. Begat, D.A.V. Morton, J.N. Staniforth, R. Price, The Cohesive-Adhesive Balances in Dry Powder Inhaler Formulations I: Direct Quantification by Atomic Force Microscopy, Pharm. Res. 21 (2004) 1591–1597. doi.org/10.1023/B:PHAM.0000041453.24419.8a.
Fluidization of cohesive powders - ScienceDirect, www.sciencedirect.com/science/article/pii/0032591084800030.
R. Agrawal, Y. Naveen, Pharmaceutical processing–A review on wet granulation technology, Int. J. Pharm. Front. Res. 1 (2011) 65–83.
The effect of dry granulation on flow behaviour of pharmaceutical powders during die filling | Request PDF, ResearchGate. (n.d.). http://dx.doi.org/10.1016/j.powtec.2017.08.064.
P. Arnaud, D. Brossard, J.C. Chaumeil, Effect of the granulation process on nitrofurantoin granule characteristics, Drug Dev. Ind. Pharm. 24 (1998) 57–66.
M.R. Desrosiers, P.J. Weathers, Effect of leaf digestion and artemisinin solubility for use in oral consumption of dried Artemisia annua leaves to treat malaria, J. Ethnopharmacol. 190 (2016) 313–318.
M.E. Mustafa, A.O. Nur, Z.A. Osman, S.A. Ahmed, Influence of drug solubility and polymers supply source on the physical performance of matrix tablets, Int J Pharm Pharm Sci. 6 (2014) 308–12.
J. Munyangi, L. Cornet-Vernet, M. Idumbo, C. Lu, P. Lutgen, C. Perronne, N. Ngombe, J. Bianga, B. Mupenda, P. Lalukala, Artemisia annua and Artemisia afra tea infusions vs. artesunate-amodiaquine (ASAQ) in treating Plasmodium falciparum malaria in a large scale, double blind, randomized clinical trial, Phytomedicine. 57 (2019) 49–56.
W. Faisal, F. Farag, A.A. Abdellatif, A. Abbas, Taste masking approaches for medicines, Curr. Drug Deliv. 15 (2018) 167–185.
S.F. Barakh Ali, S. Dharani, H. Afrooz, M.A. Khan, E.M. Mohamed, K. Kohli, Z. Rahman, Application of salt engineering to reduce/mask bitter taste of clindamycin, Drug Dev. Ind. Pharm. (2019) 1–23.
M. Blessy, R.D. Patel, P.N. Prajapati, Y.K. Agrawal, Development of forced degradation and stability indicating studies of drugs—A review, J. Pharm. Anal. 4 (2014) 159–165.
P.E. Ogwang, J.O. Ogwal, S. Kasasa, F. Ejobi, D. Kabasa, C. Obua, Use of Artemisia annua L. infusion for malaria prevention: mode of action and benefits in a Ugandan community, Br. J. Pharm. Res. 1 (2011) 124.
J.F. Ferreira, D.L. Luthria, T. Sasaki, A. Heyerick, Flavonoids from Artemisia annua L. as antioxidants and their potential synergism with artemisinin against malaria and cancer, Molecules. 15 (2010) 3135–3170.
A.R. Bilia, P.M. de Malgalhaes, M.C. Bergonzi, F.F. Vincieri, Simultaneous analysis of artemisinin and flavonoids of several extracts of Artemisia annua L. obtained from a commercial sample and a selected cultivar, Phytomedicine. 13 (2006) 487–493.
P.J. Weathers, M.J. Towler, The flavonoids casticin and artemetin are poorly extracted and are unstable in an Artemisia annua tea infusion, Planta Med. 78 (2012) 1024–1026.
U. Soni, S. Brar, V.K. Gauttam, Effect of seasonal variation on secondary metabolites of medicinal plants, Int. J. Pharm. Sci. Res. 6 (2015) 3654–3662.
C. van den Berg, C.P.M. Roelands, P. Bussmann, E.L.V. Goetheer, D. Verdoes, L.A.M. van der Wielen, Preparation and analysis of high capacity polysulfone capsules, React. Funct. Polym. 69 (2009) 766–770. https://doi.org/10.1016/j.reactfunctpolym.2009.06.008.