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Domperidone Research Paper

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Domperidone (DOM), C22H24ClN5O2, is an antiemetic and prokinetic agent used in treatment of nausea and vomiting for decades (1, 2). It has also been used for the treatment of migraine (3, 4), gastroparesis (5) and functional dyspepsia (6). DOM is structurally related to butyrophenones. The antiemetic properties of DOM may be attributed to its dopamine (D2) receptor-blocking activity in chemoreceptor trigger zone and at gastric level. As a prokinetic agent, DOM increases esophageal and gastric peristalsis and improves antroduodenal coordination which facilitates gastric emptying (7, 8). It is administered orally in the dose range of 10-40 mg daily and has elimination half life of 5-7 hrs (9). The short half life of DOM necessitates its frequent …show more content…

The use of β-cyclodextrin (βCD) to improve the solubility of poorly soluble drugs is limited due to low solubility of βCD itself (18 mg/ml). If βCD is used at a greater extent in a formulation, it may lead to certain toxic effects. Though the derivatives of βCD are highly soluble, they are costlier. Hence in order to improve the solubility and complexation efficiency of βCD, multicomponent inclusion complex is prepared by incorporating a third component during the complexation process which may consist of amino acid, hydroxy acid or hydrophilic polymer. Multicomponent inclusion complex also reduces amount of βCD required for complexation, thus reducing the formulation cost (16, 17). In our previous study it has been reported that the βCD alone increases the solubility of DOM by 2.2 folds where as ternary complex comprising of DOM, βCD and citric acid (CA) increases the solubility of DOM by 76 folds (18). Riebero et al. (2004) have reported that the quaternary inclusion complex (QIC) of a weakly basic drug such as vinpocetine, βCD, tartaric acid and water soluble polymers enhances the solubility of vinpocetine than the ternary complex involving vinpocetine, βCD and tartaric acid. It was found that the polymers increased the stability constant of QIC by co-complex formation (19). Mannitol has been …show more content…

Response surface methodology (RSM) is used for optimization of drug delivery systems which involves the use of various types of experimental designs, generation of polynomial relationships and mapping of the response over the experimental domain to select the optimum formulation (24–26). Amongst various experimental designs, the central composite design has been commonly used for designing and optimization of different pharmaceutical formulations and processes (27-29). This technique is more flexible, effective and provides large extent of information on experimental variable effects. In addition, it requires minimum number of experimental runs and

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