European Journal of Applied Sciences 5 (2): 36-42, 2013
ISSN 2079-2077
© IDOSI Publications, 2013
DOI: 10.5829/idosi.ejas.2013.5.2.1113
Corresponding Author: G. Poovi, Department of Pharmaceutics, College of Pharmacy, Mother Theresa Post Graduate
and Research Institute of Health Sciences, Puducherry-6, India.
36
Development of Domperidone Solid Dispersion
Powders Using Sodium Alginate as Carrier
G. Poovi, M.Umamaheswari, S. Sharmila, Sujit Kumar and A.N. Rajalakshmi
Department of Pharmaceutics, College of Pharmacy, Mother Theresa Post Graduate
and Research Institute of Health Sciences, Puducherry-6, India
Abstract: Domperidone is a widely used antiemetic, poorly water soluble drug, erratically absorbed in stomach
and possess several dissolution-related problems thus it has poor bioavailability (13-17%). The rate and extent
of dissolution of the drug from any solid dosage form determines the rate and extent of absorption of the drug.
Several methods have been employed in order to improve the dissolution and bioavailability of sparingly
soluble drugs. Among the various approaches, the solid dispersion technique has proved to be the most
successful, simple and economic in improving the dissolution and bioavailability of poorly soluble drug.
The aim of the present study was to investigate the possibility of improving the solubility and dissolution rate
of a novel sodium alginate based solid dispersion of domperidone using fusion method, solvent evaporation
method and solvent melt method. The prepared solid dispersions were characterized for their drug content,
drug-carrier compatability and in-vitro dissolution study. All the formulation showed marked improvement in
the solubility and dissolution rate of drug which may be due to hydrophilic polymers would improve the
aqueous solubility, dissolution rate and thereby enhancing its systemic availability. It was concluded that
sodium alginate is a suitable carrier in solid dispersion technique to improve the solubility and dissolution rate
of the poorly soluble drug like domperidone.
Key words: Domperidone% Sodium Alginate% Solid Dispersion% Bioavailability
INTRODUCTION enhancement of oral bioavailability of poor water soluble
Domperidone, a dopamine D2 receptor antagonist, is drug development [12]. Together with the permeability,
used as a prokinetic and antiemetic agent for the treatment the solubility behaviour and the dissolution rate of a drug
of gastroparesis, nausea and vomiting [1]. Domperidone is a key determinant of its oral bioavailability and is one of
is a weak base with good solubility in acidic pH but in the most important concerning aspects of the
alkaline pH, its solubility is significantly reduced [2] and pharmaceutical industries [11, 13, 14].
it is poorly water soluble drug (log p, 3.1), has low Many methods are available to improve dissolution
absorbability after oral administration and undergoes rate, solubility characteristics, including salt formation,
extensive first pass metabolism [3-5]. The poor aqueous micronization and addition of solvent or surface active
solubility may be one possible reason for its low agents. Solid dispersion (SDs) is one of these methods,
bioavailability (13-17%). In addition, drug release is a which was most widely and successfully applied to
critical and rate limiting step for oral drug bioavailability, improve the solubility, dissolution rates and consequently
particularly for drugs possessing low gastrointestinal the bioavailability of poorly soluble drugs. The concept
solubility and high permeability [3, 6]. of solid dispersions (SDs) was introduced in 1961 by
Oral bioavailability of drugs depends on its Sekiguchi and Obi [7], in which the drug is dispersed in
solubility and/or dissolution rate, therefore major inert water - soluble carrier at solid state. This technique
problems associated with these drugs was its very low has been used for a wide variety of poorly aqueous
solubility in biological fluids, which results into poor soluble drugs such as nimesulide [15], ketoprofen
bioavailability after oral administration [7-11]. The [16], tenoxicam [17], nifedipine [18], nimodipine [19].
drugs remains one of the most challenging aspects of