Effect of acrylic polymers on physical parameters of spheronized pellets using an aqueous coating system

Afsana Akhter, Golam Kibria

Abstract


The aim of this study was to develop ambroxol hydrochloride sustained release pellets by an extrusion-spheronization echnique and subsequent coating with acrylic polymers. Acrylic polymers like Eudragit RL 30 D, Eudragit RS 30 D
and Eudragit NE 30 D were used as release retarding coating polymers. The release retarding capability of these polymers was also investigated. In each case, 10% polymer on dry basis was loaded. The flow property, surface roughness as well as the drug release behavior of the pellets was found to be the subject of types of polymers. About 35% drug was released at the first hour in 0.1N HCl media (pH 1.2) from Eudragit RL 30 D-coated pellets but from Eudragit RS 30 D and Eudragit NE 30 D-coated pellets, only 13.75 and 2.43% drug was released, respectively. In buffer media (pH 6.8), about 54% drug was released at the first hour from Eudragit RL 30 D-coated pellets but only 64% drug was released at 10 h. From Eudragit RL 30 D- and Eudragit NE 30 D-coated pellets only 7.28 and 1.14% drug was released at 1 h, respectively, but about 5.14 and 5.86 h was required for 50% drug release from these two polymers and about 80% drug was released at 10 h.The functional groups present in the polymeric films played a significant role on in vitro release kinetics of the drug from the coated pellets. Different kinetic models like zero order, first order and Higuchi were used for fitting the drug release pattern. The Higuchi model was the best fitted for ambroxol release from the coated pellets. The drug release mechanism
was derived with Korsmeyer equation.


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References


Fekete R, Zelkó R, Marton S, Rácz I. Effect of the formulation parameters

on the characteristics of pellets. Drug Dev Ind Pharm 1998;24:1073-6.

Vergote GJ, Vervaet C, van Driessche I, Hoste S, de Smedt S, Demeester J,

et al. An oral controlled release matrix pellet formulation containing

nanocrystalline ketoprofen. Int J Pharm 2001;219:81-7.

Krogars K, Heinämäki J, Vesalahti J, Marvola M, Antikainen O, Yliruusi J.

Extrusion-spheronization of pH-sensitive polymeric matrix pellets for

possible colonic drug delivery. Int J Pharm 2000;199:187-94.

Hileman GA, Upadrashta SM, Neau SH. Drug solubility effects on

predicting optimum conditions for extrusion and spheronization of

pellets. Pharm Dev Technol 1997;2:43-52.

Thoma K, Ziegler I. Investigations on the influence of the type of

extruder for pelletization by extrusion-spheronization. II. Sphere

characteristics. Drug Dev Ind Pharm 1998;24:413-22.

Kleinebudde P, Schröder M, Schultz P, Müller BW, Waaler T, Nymo L.

Importance of the fraction of microcrystalline cellulose and

spheronization speed on the properties of extruded pellets made from

binary mixtures. Pharm Dev Technol 1999;4:397-404.

Wu C, McGinity JW. Influence of ibuprofen as a solid-state plasticizer in

Eudragit RS 30 D on the physicochemical properties of coated beads.

AAPS PharmSciTech 2001;2:24.

Okor RS, Obi CE. Drug release through aqueous-based film coatings of

acrylate-methacrylate, a water-insoluble copolymer. Int J Phamaceutics

;58:89-91.

Lehmann K, Dreher D. Coating of tablets and small particles with

acrylic resins by fluid bed technology. Int J Pharm Technol Prod Manuf

;2:31-43.

Kibbe AH. Handbook of Pharmaceutical Excipients. 3 ed. American

Pharmaceutical Association and Pharmaceutical Press; 2000. p. 401-3.

Lehmann K. Chemistry and application properties of polymethacrylate

coating system. In: Aqueous polymeric coating for pharmaceutical

dosage forms. 2 ed. Marcel Decker Inc; 1996. p. 101-74.

Lin AY, Muhammad NA, Pope D, Augsburger LL. Effect of curing and

storage conditions on drug release from pellets coated with Eudragit

NE30D. AAPS PharmSci 2000;2.

Lin AY, Muhammad NA, Pope D, Augsburger LL. Study of crystal

lization of endogenous surfactant in Eudragit NE 30D-free films

and its influence on drug-release properties of controlled-release

diphenhydramine HCl pellets coated with Eudragit NE30D. AAPS

PharmSciTech 2001;3:14.

Barar FSK. Essentials of Pharmacotherapeutics. 3 ed. S Chand and

Company Ltd., New Delhi; 2005. p. 550.

Martindale SC. The Complete Drug Reference. 33 ed. The Pharmaceutical

Press, London; 2002. p. 1084.

. Vergin H, Bishop-Freudling GB, Miczka M, Nitsche V, Strobel K,

Matzkies F. The pharmacokinetics and bioequivalence of various dosage

forms of ambroxol. Arzneimittelforschung 1985;35:1591.

Alighieri T, Avanessian S, Berlini S, Bianchi SG, Deluigi P, Valducci R,

et al. Arzneim Forsch. Drug Res 1988;38:92.

Ahmed I, Roni MA, Kibria G, Islam MR, Rahman MH. Effect of plastic

and acrylic polymers on the release profile of ambroxol hydrochloride

controlled release pellets prepared by extrusion-spheronization

technique and fluid bed coating. Dhaka Univ J Pharm Sci 2008;7:181-6.

Kibria G, Islam KM, Jalil RU. Stability study of ambroxol hydrochloride

sustained release pellets coated with acrylic polymer. Pak J Pharm Sci

;22:36-43.

Lehmann K, Abmus M, Bossler H, Dreher D, Liddiard C, Petereit H,

et al. Controlled drug release through film coatings. In: Practical course

in film coating of pharmaceutical dosage forms with Eudragit. Rohm

GmbH and Co. Germany; 2001. p. 8-15.

Kibria G, Ul-Jalil R. The effect of the ratio of two acrylic polymers on

the in vitro release kinetics of ketoprofen from pellets prepared by

extrusion and spheronisation technique. Pak J Pharm Sci 2008;21:92-7.

“News Pharma Polymers” Bulletin. Rohm GmbH and Co. Germany;




DOI: http://dx.doi.org/10.22377/ajp.v3i4.282

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