Hydrophilic polymers as release modifiers for primaquine phosphate: Effect of polymeric dispersion

Authors

  • S Sant Department of pharmaceutics, National Institute for Pharmaceutical Education and Research
  • S Swati Department of pharmaceutics, National Institute for Pharmaceutical Education and Research
  • K Awadhesh Department of pharmaceutics, National Institute for Pharmaceutical Education and Research
  • MA Sajid Department of pharmaceutics, National Institute for Pharmaceutical Education and Research
  • GD Pattnaik Department of pharmaceutics, National Institute for Pharmaceutical Education and Research
  • MA Tahir Department of pharmaceutics, National Institute for Pharmaceutical Education and Research
  • S Farheen Azad Institute for Pharmacy and Research

Keywords:

Primaquine phosphate, Extended release tablets, Hydroxypropylmethylcllulose, Sodium CMC, Sodium alginate, Fickian

Abstract

Primaquine (PQ), a synthetic compound with potent antimalarial activity is characterized by low plasma half life, requiring frequent administration leading to several undesired side effects, patient incompliance. The objective of the present study was to design an extended release formulation incorporating PQ in hydrophillic matrix composed of HPMC,Sodium CMC, Sodium alginate. Effects of polymeric dispersions of ethyl cellulose (EC) and polyvinylpyrrolidone (PVP) was also studied. Tablets were prepared by wet granulation method. The results of angle of repose (<30) and compressiblity index (upto 15%) indicate good flow properties. Tablets were subjected to weight variation, hardness, friability and drug content tests. The swelling and drug release profile were investigated under dissolution condition. The result showed that the swelling index & release retarding capacity follows HPMC>Sodium CMC>Sodium alginate, which was further sustained by polymeric dispersions of EC and PVP. The kinetics of drugs showed extended release of up to 20 hrs (F3) following non fickian diffusion (0.45<n<0.89).

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References

Goodman LS, Gilman AG, Hardman JG, and Limbird LE, Goodman & gilman’s the pharmacological basis of therapeutics. 10th Ed. New York: 2003

Baird JK, Fryauff DJ, and. Hoffman SL. Primaquine for Prevention of Malaria in Clinical Infectious Diseases 2003;37:1659–1667

Bami HL, Dhatt MS, Ahluwalia GS, Ray AP. Studies on metabolic degradation of pamaquin (plasmoquin) in monkeys. Indian journal of malariology. 1960; 14:1-13

Hay SI, Guerra CA, Tatem AJ, Noor AM, Snow RW, The global distribution and population at risk of malaria: past, present, and future. Lancet Infect. Dis.2004;4 (6): 327–336.

White NJ. The treatment of malaria. New Eng. J. Med Sept 12 1996; 335(11) : 800-806.

Klotsas EG, Andrew Lever ML. An update on malaria prevention, diagnosis and treatment for the returning traveler. Blood Reviews.2007;21(2):73-87

Bhadra D, Yadav AK, Bhadra S, Jain NK. Glyco dendrimeric nanoparticulate carriers of primaquine phosphate for liver targeting. International Journal of Pharmaceutics. 2005; 295 (1-2):221-233

Green M D, D'Souza MJ, Holbrook JM and Wirtz RA. In vitro and in vivo evaluation of albumin encapsulated primaquine diphosphate prepared by nebulization into heated oil. J Microencapsu. 2004;21(4):433 – 444

Singh KK ,Vingkara SK. Formulation of antimalarial activity and biodistribution of oral lipid nanoemulsion of primaquine. International Journal of Pharmaceutics.2008; 347(1-2):136-143

Jeans CW, Heard CM. A therapeutic dose of primaquine can be delivered across excised human skin from simple transdermal patches. International Journal of Pharmaceutics.1999; 189(1):1-6

Noel S, Sharma S, Shanker R, Rath SK. Primaquine induced differential gene expression analysis in mice liver using DNA microarrays. Toxicology 2007;239(1-2):96-107

Singh P, Desai SJ, Simonelli AP, Higuchi WI. Role of wetting on the rate of drug release from inert matrices. Journal of Pharmaceutical Sciences. 1968;57 (2), 217-226

Sujja-areevatha J, Mundaya DL, Coxa PJ, Khan KA. Relationship between swelling, erosion and drug release in hydrophilic natural gum mini-matrix formulations. European Journal of Pharmaceutical Sciences. 1998; 6:207–217

Colombo P. Swelling-controlled release in hydrogel matrices for oral route. Advanced Drug Delivery Reviews 1993; 11(1-2):37-57

Siepmann J, Kranz H, Bodmeier R, Peppas NA. HPMC-matrices for controlled drug delivery: a new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res. 1999;16:1748-1756.

Lee BJ, Ryu SG, Cui JH. Formulation and Release Characteristics of Hydroxypropyl Methylcellulose Matrix Tablet Containing Melatonin. Drug development and industrial pharmacy. 1999;25(4):493–501

Liew CV, Chan LW, Ching AL, Sia Heng PW. Evaluation of sodium alginate as drug release modifier in matrix tablets. International Journal of Pharmaceutics. 2006; 309:25–37

Emami J, Tajeddin M and Ahmadi F. Preparation and In Vitro Evaluation of Sustained-Release Matrix Tablets of Flutamide Using Synthetic and Naturally Occurring Polymers. Iranian Journal of Pharmaceutical Research 2008, 7(4):247-257

Avachat A and Kotwal V. Design and Evaluation of Matrix-Based Controlled Release Tablets of Diclofenac Sodium and Chondroitin Sulphate. AAPS PharmSciTech 2007;8 (4):E1-6

Published

2011-09-20

How to Cite

1.
Sant S, Swati S, Awadhesh K, Sajid M, Pattnaik G, Tahir M, Farheen S. Hydrophilic polymers as release modifiers for primaquine phosphate: Effect of polymeric dispersion. Ars Pharm [Internet]. 2011 Sep. 20 [cited 2024 Jul. 19];52(3):19-25. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/4740

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Original Articles