IN VITRO EVALUATION OF IBUPROFEN HOT-MELT EXTRUDED PELLETS EMPLOYING DIFFERENT DESIGNS OF THE FLOW THROUGH CELL

  • Laila Hassanien Emara Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
  • Fatma Mohamed Abdelfattah Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
  • Nesrin Fouad Taha Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
  • Ahmed Abdel-rahman El-ashmawy Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
  • Nadia Mohamed Mursi Department of Pharmaceutics, Faculty of Pharmacy, Cairo University.

Abstract

Objective: Hot-melt extrusion technique (HME) was used to prepare a sustained release (SR) multiparticulate oral dosage form (pellets) containing Ibuprofen (IBU). Prepared IBU-HME pellets were in vitro evaluated by flow-through cell dissolution tester (FTC, USP Apparatus #4) using different flow conditions and FTC designs.

Methods: In this study, Sucroester®WE15 was used as the polymeric carrier to prepare two different IBU loadings (60 % and 30 % w/w). In order to optimize the FTC conditions, different cell sizes, pellets loading and hydrodynamic conditions of FTC on IBU release rate from pellets were proposed.

Results: The results showed that the IBU release rate was increased in the larger cell than the small cell. In addition, laminar flow showed more reproducible results than turbulent flow. It was found that the large cell with laminar flow rate and homogeneous mixing of the pellets with glass beads was the optimum conditions for in vitro evaluation of these preparations.

Conclusion: Improper methods of sample loading as well as cell size may result in confusing or erroneous data if not analyzed carefully. Therefore, it might be critical to choose a specific cell design of the FTC for in vitro evaluation of pellets to obtain reliable and discriminative results reflecting the major as well as minor formulation variables.

 

Keywords: Ibuprofen, Flow-through cell, Hot-melt extrusion, Pellets, Sustained-release, Sucroester.

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Author Biographies

Laila Hassanien Emara, Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
Medical and Pharmaceutical Chemistry Department
Fatma Mohamed Abdelfattah, Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
Medical and Pharmaceutical Chemistry Department
Nesrin Fouad Taha, Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
Medical and Pharmaceutical Chemistry Department
Ahmed Abdel-rahman El-ashmawy, Industrial Pharmacy Laboratory,Medical and Pharmaceutical Chemistry Department, Division of Pharmaceutical Industries, National Research Centre.
Medical and Pharmaceutical Chemistry Department
Nadia Mohamed Mursi, Department of Pharmaceutics, Faculty of Pharmacy, Cairo University.
Department of Pharmaceutics

References

1. Davies NM. Clinical Pharmacokinetics of Ibuprofen. Clin Pharmacokinet 1998;34(2):101-54.
2. Kawabata Y, Wada K, Nakatani M, Yamada S, Onouea S. Formulation Design for Poorly Water-Soluble Drugs Based on Biopharmaceutics Classification System: Basic Approaches and Practical Applications. Int J Pharm 2011;420:1–10.
3. Ozdemir N, Sahin J. Design of a Controlled Release Osmotic Pump System of Ibuprofen. Int J Pharm 1997;158:91-7.
4. Khana GM, Zhub JB. Studies on Drug Release Kinetics from Ibuprofen–Carbomer Hydrophilic Matrix Tablets: Influence of Co-excipients on Release Rate of the Drug. J Cont Rel 1999;57:197–203.
5. Khan GM, Zhub JB. Ibuprofen Release Kinetics from Controlled-Release Tablets Granulated with Aqueous Polymeric Dispersion of Ethylcellulose II: Influence of Several Parameters and Coexcipients. J Cont Rel 1998;56:127–34.
6. Khana GM, Zhub JB. Studies on Drug Release Kinetics from Ibuprofen–Carbomer Hydrophilic Matrix Tablets: Influence of Co-excipients on Release Rate of the Drug. J Cont Rel 1999;57:197–203.
7. Nerurkar J, Jun HW, Price JC, Park MO. Controlled-Release Matrix Tablets of Ibuprofen using Cellulose Ethers and Carrageenans: Effect of Formulation Factors on Dissolution Rates. Eur J Pharm Biopharm 2005;61:56–68.
8. Novoaa GAG, Heinamakib J, Mirzab S, Antikainenb O, Colartea AI, Pazd AS, et al. Physical Solid-State Properties and Dissolution of Sustained-Release Matrices of Polyvinylacetate. Eur J Pharm Biopharm 2005;59:343–50.
9. Chandran S, Asghar LFA, Mantha N. Design and Evaluation of Ethyl Cellulose Based Matrix Tablets of Ibuprofen with pH Modulated Release Kinetics. Indian J Pharm Sci 2008;70(5):596-602.
10. Abbaspour MR, Sadeghi F, Garekani AH. Design and Study of Ibuprofen Disintegrating Sustained-Release Tablets Comprising Coated Pellets. Eur J Pharm Biopharm 2008;68:747–59.
11. Kumar DS, Pandit JK. Relationship between Dissolution Rate and Bioavailability of Sustained-Release Ibuprofen Capsules. Drug Dev Ind Pharm 1997;23(10):987-92.
12. Kamble R, Kumar A, Mahadik K, Paradkar A. Ibuprofen-Glyceryl Monostearate (GMS) Beads using Melt Solidification Technique: Effect of HLB. Int J Pharm Pharm Sci 2010;2(4):100–4.
13. Salústio PJ, Cabral-Marques HM, Costa PC, Pinto JF. Comparison of Ibuprofen Release from Minitablets and Capsules Containing Ibuprofen: β-Cyclodextrin Complex. Eur J Pharm Biopharm 2011;78:58–66.
14. Abbaspour MR, Sadeghi F, Garekani HA. Preparation and Characterization of Ibuprofen Pellets Based on Eudragit RS PO and RL PO or their Combination. Int J Pharm 2005;303:88–94.
15. Santos H, Veiga F, Pina ME, Sousa JJ. Compaction, Compression and Drug Release Properties of Diclofenac Sodium and Ibuprofen Pellets Comprising Xanthan Gum as a Sustained Release Agent. Int J Pharm 2005;295:15–27.
16. Patwekar SL, Baramade MK. Controlled Release Approach to Novel Multiparticulate Drug Delivery System. Int J Pharm Pharm Sci 2012;4(3):757-63.
17. Kalivoda A, Fischbach M, Kleinebudde P. Application of Mixtures of Polymeric Carriers for Dissolution Enhancement of Oxeglitazar using Hot-Melt Extrusion. Int J Pharm 2012;439:145–56.
18. Young CR, Crowley M, Dietzsch C, McGinity JW. Physicochemical Properties of Film-Coated Melt-Extruded Pellets. J Microencapsul 2007;24:57-71.
19. Vasconcelos T, Sarmento B, Costa P. Solid Dispersions as Strategy to Improve Oral Bioavailability of Poor Water Soluble Drugs. Drug Discovery Today 2007;12(23/24):1068-75.
20. Repka MA, Shah S, Lu J, Maddineni S, Morott J, Ratwardhan K, et al. Melt Extrusion: Process to Product. Expert Opin Drug Deliv 2012;9(1):105-25.
21. Szuts A, Makai Z, Rajkó R, Szabó-Révész P. Study of the Effects of Drugs on the Structures of Sucrose Esters and the Effects of Solid-State Interactions on Drug Release. J Pharm Biomed Anal 2008;48:1136–42.
22. Otsuka M, Ofusa T, Matsuda Y. Dissolution Improvement of Water-Insoluble Glybuzole by Co-grinding and Co-melting with Surfactants and their Physicochemical Properties. Colloids Surf B 1998;10:217–26.
23. Brabander CD, Vervaet C, Remon JP. Development and Evaluation of Sustained Release Mini-Matrices Prepared via Hot Melt Extrusion. J Cont Rel 2003;89:235–47.
24. Nama M, Gonugunta CS, Reddy Veerareddy P. Formulation and Evaluation of Gastroretentive Dosage Forms of Clarithromycin. AAPS Pharm Sci Tech 2008;9(1):231–7.
25. Bhattachar SN, Wesley JA, Fioritto A, Martin PJ, Babu SR. Dissolution Testing of a Poorly Soluble Compound using the Flow-Through Cell Dissolution Apparatus. Int J Pharm 2002;236:135–43.
26. Fotaki N. Flow-Through Cell Apparatus (USP Apparatus 4):Operation and Features. Dissolution Technol 2011;18:46-9.
27. Moore JW, Flanner HH. Mathematical Comparison of Dissolution Profiles. Pharm Tech 1996;20:64–74.
28. Emara LH, Taha NF, Mursi NM. Investigation of the Effect of Different Flow-Through Cell Designs on the Release of Diclofenac Sodium SR Tablets. Dissolution Technol 2009;16:23-31.
29. Emara LH, Abdou AR, El-Ashmawy AA, Badr RM, Taha NF, Mursi NM. In Vitro Release Evaluation of Gastroretentive Amoxicillin Floating Tablets Employing a Specific Design of the Flow-Through Cell. Dissolution Technol 2013;20:27-34.
30. Banakar UV. Pharmaceutical Dissolution Testing. Marcel Dekker, Inc. New York; 1992.
31. Kasperek R. Simultaneous Release of Diclofenac Sodium and Papaverine Hydrochloride from Tablets and Pellets using the Flow-Through Cell Apparatus Described by Dimensionless Equations. Acta Pol Pharm 2011;68:261-72.
32. Chevalier E, Viana M, Artaud A, Chomette L, Haddouchi S, Devidts G, et al. Comparison of Three Dissolution Apparatuses for Testing Calcium Phosphate Pellets used as Ibuprofen Delivery Systems. AAPS Pharm Sci Tech 2009;10(2):597-605.
33. Badr RM. Improvement of Nifedipine Bioavailability in Oral Drug Delivery Systems. PhD Thesis: Cairo University; 2006.
34. Cammarn SR, Sakr A. Predicting Dissolution via Hydrodynamics: Salicylic Acid Tablets in Flow Through Cell Dissolution. Int J Pharm 2000;201:199–209.
35. Hülsmann S, Backensfeld T, Keitel S, Bodmeier R. Melt Extrusion–An Alternative Method for Enhancing the Dissolution Rate of 17β-Estradiol Hemihydrate. Eur J Pharm Biopharm 2000;49:237–42.
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How to Cite
Emara, L. H., F. M. Abdelfattah, N. F. Taha, A. A.- rahman El-ashmawy, and N. M. Mursi. “IN VITRO EVALUATION OF IBUPROFEN HOT-MELT EXTRUDED PELLETS EMPLOYING DIFFERENT DESIGNS OF THE FLOW THROUGH CELL”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 6, no. 9, 1, pp. 192-7, https://innovareacademics.in/journals/index.php/ijpps/article/view/2057.
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