الفهرس 
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Abstract
Sulpiride (Sul) is a substituted benzamide antipsychotic that is reported to be a selective antagonist of central dopamine (D2, D3, and D4) receptors. It is also claimed to have mood elevating properties. Sulpiride (Sul) is mainly used in the treatment of psychoses such as schizophrenia. Sulpiride has a poor solubility in water and so a low oral bioavailability.
The objective of this study is to enhance the solubility of sulpiride by solid dispersion technique, then to formulate and evaluate several pharmaceutical dosage forms containing sulpiride (Sul) or its solid dispersion such as suppositories, topical formulations and microspheres.
The present study was divided into five parts as following:
Part (I)
Formulation and Evaluation of Sulpiride Solid Dispersions
The purpose of this part was to improve the dissolution rate of sulpiride since it is poorly water soluble.
Physical mixtures (PMs) and solid dispersions (SDs) of sulpiride with each of B-cyclodextrin, Lactose anhydrous, Glucose anhydrous and Eudragit E100 in ratios of 1:0.5, 1:1 and 1:2 (drug to carrier W/W), with Polyethylene glycol (PEG) 4000 in ratios of 1:1, 1:3 and 1:5, with Polyethylene glycol (PEG) 6000 in ratios of 1:1, 1:3, 1:5, 1:7 and 1:9, with tartaric acid in ratios of 1:0.125, 1:0.1875 and 1:0.25, with Urea, Poloxamer 188 and Maltose monohydrate in ratios of 1:1, 1:2 and 1:3
and with polyvinyl pyrrolidone (PVP) K30 in ratios of 1:0.5, 1:1, 1:2 and 1:3 were prepared. SDs of sulpiride with urea in ratio of 1:2 containing , Brij 35 (1%), Brij 52 (1%), Brij 92 (1%), Mrij59 (1%) , Tween 80 (0.5-1-
Abstract
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2-5%), Transcutol (1%), Cetrimide (1%) and Sodium lauryl sulphate (SLS) (1%) were also prepared.
All previously mentioned SDs were prepared by solvent evaporation method.
The equilibrium solubility of sulpiride in presence of different concentrations of the above mentioned carriers was determined at 25°C and the influence of different pH on the solubility of sulpiride was also examined.
The dissolution of all prepared samples (PMs and SDs) was carried out in distilled water.
Some SDs and PMs as well as individual components were subjected to inspection by FTIR spectroscopy, DSC and X-ray powder diffraction.
Results revealed that:
The used carriers can be ranked according to their effect on increasing the aqueous solubility of sulpiride as following: tartaric acid > PVP > PEG 4000 > urea > glucose > lactose > maltose > PEG 6000 > poloxamer 188 > β-cyclodextrin.
The solubility decreased with increasing pH (higher in acidic rather than in alkaline one).
The type of carrier and drug to carrier ratio had great influence on the rate and extent of dissolution of sulpiride from its PMs and SDs. Tartaric acid had the most influential effect on the rate and the extent of dissolution of sulpiride, followed by PEG 4000, PVP, glucose, PEG 6000, maltose, lactose, eudragit E100, poloxamer 188, urea and finally β-cyclodextrin at ratios of (1:0.25) , (1:5), (1:1) , (1:1) , (1:5) , (1:2) , (1:1) , (1:1) , (1:2) , (1:2) and (1:1) respectively.