Preparation and in vitro evaluation of verapamil HCl and ibuprofen containing carrageenan beads

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Abstract

The objective of this study was to prepare and evaluate carrageenan beads as a controlled release system for a freely water soluble drug verapamil hydrochloride and a slightly water soluble drug ibuprofen. Beads were prepared by ionotropic gelation method. The influence of formulation factors (drug content, polymer concentration, counterion type and concentration, outer phase volume) on the particle size, encapsulation efficiency and in vitro release characteristics of beads was investigated. The encapsulation efficiency of veraparnil HCl in the beads (34.8–71.1%) was higher than that of ibuprofen (23.6–58%). While about 30% of ibuprofen was released at 6 h, about 70% of verapamil HCl was released in 5 h from the carrageenan beads prepared.

Introduction

In recent years natural water soluble polymers have been examined for their suitability to prepare multiparticulate controlled release drug delivery systems. Thus the use of organic solvents needed to solubilize the water insoluble polymers can be avoided.

Carrageenan has been used increasingly in pharmaceutical formulation studies. Suzukı and Lım (1994) used ι-carrageenan together with locust bean gum to prepare microcapsules for the sustained release of gentamicin sulphate. The influence of the locust bean gum on the ι-carrageenan microcapsule membrane led to a near zero order release of gentamicin sulphate.

Patıl and Speaker (2000) formulated a model protein, horse radish peroxidase (HRP) in a microcapsule delivery system using ι-carrageenan. This encapsulation system employing the ionic interaction between ι-carrageenan and a series of amines successfully captured the protein, HRP.

Garcıa and Ghaly (1996) used carrageenan in order to control acetaminophen release from spheres prepared by cross linking technique. The results showed that carrageenan could exert control over the rate and amount of drug released from the spheres prepared.

In this article we have investigated the incorporation of a freely water soluble drug, verapamil hydrochloride and a slightly water soluble drug, ibuprofen in carrageenan beads. The beads were characterized by particle size determination, encapsulation efficiency and release rates of drugs. The influence of preparation technique and of the solubilities of the model drugs on these properties were examined.

Section snippets

Materials and methods

Verapamil HCl Knoll, ibuprofen Atabay, ι-carrageenan FMC and κ-carrageenan Sigma and Hercules. These substances were all donations of the manufacturers. Other substances used were of pharmaceutical grade.

Results and discussion

The equilibrium solubilities of verapamil HCl and ibuprofen in pH 7.4 phosphate buffer solution were found to be 123.87±6.07 and 7.43±0.51 mg/ml respectively, indicating the sink condition limits for the dissolution studies.

In order to obtain the optimum bead formulation various salts were investigated with different iota and kappa carrageenan types (Table 1). Contrary to κ-carrageenan, no spherical beads were formed with ι-carrageenan formulations using the salt solutions seen in Table 1. This

Conclusion

Drug containing carrageenan beads were prepared by ionotropic gelation method. While about 30% of ibuprofen was released at 6 h, about 70% of verapamil HCl was released in 5 h from the carrageenan beads prepared. This study has proved the usefulness of the natural polymer carrageenan for the preparation of controlled release systems of both water soluble drug verapamil HCl and slightly water soluble drug ibuprofen.

Acknowledgements

The authors would like to thank Knoll (Turkey), Atabay (Turkey) and Yýlbak (Turkey) for providing the substances. Furthermore they are grateful to Mr. Yücel Öztürk (M.U. Faculty of Medicine, Histology Department) for technical assistance in the SEM analysis.

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This work was presented at the 4th European Congress of Pharmaceutical Sciences, 11–13 September 1998, Milan, Italy.

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