COMPATIBILITY AND PROCESSING METHODS STUDY OF FORMULATION OF ARTEMETHER–LUMEFANTRINE FIXED DOSE COMBINATION USING ANALYTICAL TOOLS


Musibau Aderibigbe Mustapha, Magnus A. Iwuagwu, Michael U. Uhumwangho

Abstract


ABSTRACT

Objective: This study was undertaken to devise the best way to incorporate artemether-lumefantrine (AL) as model drugs during processing without compromising quality.

Methods: Utilization of analytical tools revealed how compatibility of formulation components and suitability of process methods were monitored and controlled to achieve quality outcome.  Excipients of proven performance in wet granulation method as well as AL as model drugs were designed into six formulations coded F-1 to F-6 to reflect modes of incorporation. Physical mixtures and wet granulated samples at different levels of processing were screened as in-process materials for compatibility and method suitability using Fourier Transform Infrared (FTIR), Differential Scanning Calorimetry (DSC) and High Performance Liquid Chromatography (HPLC) techniques. Assessment of potential risks inherent in formulation and process unit operations was adequately addressed by these instruments.

Results: Matching spectra, thermograms and chromatograms at different levels of processing indicated that there were no disappearance of old or appearance of new spectral bands; showed reduction of melting endotherm and similar characteristic elution times of AL as they transformed from pure material to physical mixture (PM) and to granules.

Conclusion: Results from this work alluded to compatibility of formulation components and process method suitability to the extent that the resultant granulates were good enough for further processing.


| PDF |

References


Narayankar S, Phadke M, Patil D, Jadhav RK, Ramesh S, Yamgar RS. Development of Discriminating Dissolution Procedure for Artemether and Lumefantrine Tablets. Der Pharma Chemica 2010; 2(6): 394-399.

Fule R, Meer T, Sav A, Amin P. Solubility and dissolution rate enhancement of Lumefantrine using hot melt extrusion technology with physicochemical characterization. Journal of Pharmaceutical Investigation 2013; 43: 305–321. DOI 10.1007/s40005-013-0078-z

World Health Organization. Guidelines for the treatment of Malaria,1st edition. Geneva, WHO [Online], 2006; Available at: www.who.int/malaria/docs/TreatmentGuidelines 2006.pdf. (Accessed January 18, 2014)

World Health Organization. Guidelines for the treatment of Malaria, 2nd edition. Geneva, WHO press, pdf document, 2010; 1-210.

World Health Organization. Survey of the quality of selected antimalarial medicines circulating in six countries of sub-Saharan Africa (QAMSA study report). Geneva, WHO, Department of Essential Medicines and Pharmaceutical services 2011.

Bargal JS, Dhawale SC, Landage SN, Kulkarni RV. Formulation and evaluation of Eudragit RS 100 loaded Microsponges of Flutrimazole. Int J Pharm Sci Res 2013; 4(8): 3039-3045. doi: 10.13040/IJPSR. 0975-8232.4(8).3039-45

Gudikandula R, Madhavi K, Thakkalapally SR, Veeramalla A and Prasad IR. Enhancement of Solubility and Dissolution rate of Ezetimibe through Liquisolid Technique. Int J Pharm Sci Res 2013; 4(8): 3229-3238. doi: 10.13040/IJPSR. 0975-8232.4(8).3229-38

Hosny KM, Khames A, Abd Elhady SS. Preparation and Evaluation of Orodispersible Tablets Containing Hydroxylbutyl-β-Cyclodextrin-Simvastatin Solid Dispersion. Trop J Pharm Res 2013; 12(4): 469 – 476.

Rahman Z, Zidan AS, Khan MA. Formulation and Evaluation of a Protein-loaded Solid Dispersions by Non-destructive Methods. The AAPS Journal 2010; 12(2): 158 – 170. DOI: 10.1208/s12248-009-9171-7

Maddela S, Maddi EG, Nadendla R. Immediate Release Formulation of Valsartan Capsule and Evaluation of its Compatibility by Non-thermal Methods. American Journal of Advanced Drug Delivery 2013; 1(3): 180-196

Otsuka M, MouriY, Matsuda Y. Chemometric Evaluation of Pharmaceutical Properties of Antipyrine Granules by Near-Infrared Spectroscopy. AAPS PharmSciTech 2003; 4 (3): Article 47, 1–7

Short SM, Cogdill RP, Anderson CA. Determination of Figures of Merit for Near-Infrared and Raman Spectrometry by Net Analyte Signal Analysis for a 4-Component Solid Dosage System. AAPS PharmSciTech 2007; 8(4): Article 96, 1–11

Mustapha MA, Igwilo CI, Silva BO. Effects of Wet Granulation Process Variables on the properties of Nifedipine Granules. International Journal of Drug Formulation and Research 2011; 2(5): 320–332

Mustapha MA, Igwilo CI, Silva BO. Influence of concentration of modified maize starch on compaction characteristics and mechanical properties of Paracetamol tablet formulation. Medical Journal of Islamic World Academy of Sciences 2013; 21(3): 125– 131

Hancock BC, Colvin JT, Mullarney MP, Zinchuk AV. The relative densities of pharmaceutical powders, blends, dry granulations, and immediate-release tablets, Pharm. Tech 2003; 4: 64-80

Kannan V, Kandarapu R, Garg S. Optimization Techniques for the Design and Development of Novel Drug Delivery Systems, Part 1. Pharm. Tech 2003; 2: 74–90.

The International Pharmacopoeia. 4th Edition. CD-ROM. Geneva, WHO Department of Essential Medicines and Pharmaceutical Policies, (2008)

Hellstrom J. A protocol for characterization of tablet manufacturability of drug and Pharmaceutical additives: [On line], 2005. Available at: www.farmfak.uu.se/farm /galfaf 2005. (Accessed June 15, 2010)

Dias VH, Pinto JF. Identification of the most relevant factors that affect and reflect the Quality of Granules by Application of canonical and cluster Analysis. J. Pharm. Sci. 2002; 19(1): 273–281

Mustapha MA. Formulation and process optimization of artemether-lumefantrine fixed dose combination tablets using Quality by Design approach. PhD Thesis, University of Benin: Benin City, December 2014.




About this article

Title

COMPATIBILITY AND PROCESSING METHODS STUDY OF FORMULATION OF ARTEMETHER–LUMEFANTRINE FIXED DOSE COMBINATION USING ANALYTICAL TOOLS

Date

01-04-2015

Additional Links

Manuscript Submission

Journal

Innovare Journal of Sciences
Vol 3 Issue 2 2015 ( April - June ) Page: 1-6

Online ISSN

2321-5496

Statistics

366 Views | 645 Downloads

Authors & Affiliations

Musibau Aderibigbe Mustapha
Department of Pharmaceutics and Pharmaceutical Technology. Faculty of Pharmacy. University of Benin. Benin City 300 001, Edo state. Nigeria.
Nigeria

Magnus A. Iwuagwu
Department of Pharmaceutics and Pharmaceutical Technology. Faculty of Pharmacy. University of Benin. Benin City 300 001, Edo state. Nigeria.
Nigeria

Michael U. Uhumwangho
Nigeria


Refbacks

  • There are currently no refbacks.