The aim of this study was to enhance the dissolution rate of water-insoluble, weakly basic antiemetic drug; Domperidone (DMP), through the formulation of adsorbates and co-adsorbates. Adsorption of drug onto the surface of three different adsorbents; Avicel PH 101, Florite R and Aerosil 200 was studied and Langmuir adsorption isotherms were constructed. Adsorbates of drug with the used adsorbents were prepared in different weight ratios by physical mixing, grinding and solvent evaporation methods. Co-adsorbates of drug with Aerosil 200 and Tween 80 were prepared by solvent evaporation method in different weight ratios. The prepared systems were physico-chemically characterized by Fourier- transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and powder X-ray diffractometry (P-XRD). FT-IR data confirmed the absence of any chemical interaction between DMP and the used adsorbents. P-XRD results confirmed the transformation of some systems from the crystalline state to the amorphous state which aided in the dissolution rate enhancement. Furthermore, the in-vitro dissolution rate of drug from these systems was studied which showed marked enhancement of DMP dissolution rate at both pH 1.2 and pH 6.8 (7 fold and 5 fold, respectively) compared to drug alone .It can be concluded that the dissolution rate

The aim of this study was to enhance the dissolution rate of water-insoluble, weakly basic antiemetic drug; Domperidone (DMP), through the formulation of adsorbates and co-adsorbates. Adsorption of drug onto the surface of three different adsorbents; Avicel PH 101, Florite R and Aerosil 200 was studied and Langmuir adsorption isotherms were constructed. Adsorbates of drug with the used adsorbents were prepared in different weight ratios by physical mixing, grinding and solvent evaporation methods. Co-adsorbates of drug with Aerosil 200 and Tween 80 were prepared by solvent evaporation method in different weight ratios. The prepared systems were physico-chemically characterized by Fourier- transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and powder X-ray diffractometry (P-XRD). FT-IR data confirmed the absence of any chemical interaction between DMP and the used adsorbents. P-XRD results confirmed the transformation of some systems from the crystalline state to the amorphous state which aided in the dissolution rate enhancement. Furthermore, the in-vitro dissolution rate of drug from these systems was studied which showed marked enhancement of DMP dissolution rate at both pH 1.2 and pH 6.8 (7 fold and 5 fold, respectively) compared to drug alone .It can be concluded that the dissolution rate

The aim of this study was to enhance the dissolution rate of water-insoluble, weakly basic antiemetic drug; Domperidone (DMP), through the formulation of adsorbates and co-adsorbates. Adsorption of drug onto the surface of three different adsorbents; Avicel PH 101, Florite R and Aerosil 200 was studied and Langmuir adsorption isotherms were constructed. Adsorbates of drug with the used adsorbents were prepared in different weight ratios by physical mixing, grinding and solvent evaporation methods. Co-adsorbates of drug with Aerosil 200 and Tween 80 were prepared by solvent evaporation method in different weight ratios. The prepared systems were physico-chemically characterized by Fourier- transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and powder X-ray diffractometry (P-XRD). FT-IR data confirmed the absence of any chemical interaction between DMP and the used adsorbents. P-XRD results confirmed the transformation of some systems from the crystalline state to the amorphous state which aided in the dissolution rate enhancement. Furthermore, the in-vitro dissolution rate of drug from these systems was studied which showed marked enhancement of DMP dissolution rate at both pH 1.2 and pH 6.8 (7 fold and 5 fold, respectively) compared to drug alone .It can be concluded that the dissolution rate

The aim of this work was to enhance the oral bioavailability of water-insoluble, weaklybasic, anti-emetic drug; Domperidone (DMP), which has a poor oral bioavailability (13-17%). Adsorption of drug onto the surface of Aerosil 200 was achieved by solvent evaporation method to enhance the drug dissolution rate. Then, the adsorbates were formulated into gastro-retentive floating tablets to retain the drug in the acidic medium of stomach which is favorable for the drug dissolution. Different drug: adsorbent ratios were prepared and tested for their in-vitro dissolution rate to select the best ratio for the final formulation. Different concentrations of several polymers were used in the preparation of tablets matrices together with sodium bicarbonate to induce the floating effect via reaction with gastric HCl. Drug-excipient compatibility studies were performed using Fouriertransform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC)which confirmed the absence of incompatibilities between the drug and the used excipients. The tablets were prepared by direct compression technique and evaluated for their weight uniformity, drug content, friability, hardness, thickness, floating properties, in-vitro dissolution rate and kinetics of drug release. Formulae F7 (containing 30% w/w sodium alginate) and F8 (containing 40% w/w sodium alginate) showed the best results and thus; they were selected for in-vivo studies in rabbits. The selected formulae showed marked enhancement of domperidone bioavailability compared with the commercial conventional immediate-release tablets; Motinorm®, with relative bioavailability values of 298.26±11.53% and 315.04±13.39% for F7 and F8, respectively and proved that the selected formulae successfully controlled the drug release.

The aim of this work was to enhance the oral bioavailability of water-insoluble, weaklybasic, anti-emetic drug; Domperidone (DMP), which has a poor oral bioavailability (13-17%). Adsorption of drug onto the surface of Aerosil 200 was achieved by solvent evaporation method to enhance the drug dissolution rate. Then, the adsorbates were formulated into gastro-retentive floating tablets to retain the drug in the acidic medium of stomach which is favorable for the drug dissolution. Different drug: adsorbent ratios were prepared and tested for their in-vitro dissolution rate to select the best ratio for the final formulation. Different concentrations of several polymers were used in the preparation of tablets matrices together with sodium bicarbonate to induce the floating effect via reaction with gastric HCl. Drug-excipient compatibility studies were performed using Fouriertransform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC)which confirmed the absence of incompatibilities between the drug and the used excipients. The tablets were prepared by direct compression technique and evaluated for their weight uniformity, drug content, friability, hardness, thickness, floating properties, in-vitro dissolution rate and kinetics of drug release. Formulae F7 (containing 30% w/w sodium alginate) and F8 (containing 40% w/w sodium alginate) showed the best results and thus; they were selected for in-vivo studies in rabbits. The selected formulae showed marked enhancement of domperidone bioavailability compared with the commercial conventional immediate-release tablets; Motinorm®, with relative bioavailability values of 298.26±11.53% and 315.04±13.39% for F7 and F8, respectively and proved that the selected formulae successfully controlled the drug release.

The aim of this work was to enhance the oral bioavailability of water-insoluble, weaklybasic, anti-emetic drug; Domperidone (DMP), which has a poor oral bioavailability (13-17%). Adsorption of drug onto the surface of Aerosil 200 was achieved by solvent evaporation method to enhance the drug dissolution rate. Then, the adsorbates were formulated into gastro-retentive floating tablets to retain the drug in the acidic medium of stomach which is favorable for the drug dissolution. Different drug: adsorbent ratios were prepared and tested for their in-vitro dissolution rate to select the best ratio for the final formulation. Different concentrations of several polymers were used in the preparation of tablets matrices together with sodium bicarbonate to induce the floating effect via reaction with gastric HCl. Drug-excipient compatibility studies were performed using Fouriertransform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC)which confirmed the absence of incompatibilities between the drug and the used excipients. The tablets were prepared by direct compression technique and evaluated for their weight uniformity, drug content, friability, hardness, thickness, floating properties, in-vitro dissolution rate and kinetics of drug release. Formulae F7 (containing 30% w/w sodium alginate) and F8 (containing 40% w/w sodium alginate) showed the best results and thus; they were selected for in-vivo studies in rabbits. The selected formulae showed marked enhancement of domperidone bioavailability compared with the commercial conventional immediate-release tablets; Motinorm®, with relative bioavailability values of 298.26±11.53% and 315.04±13.39% for F7 and F8, respectively and proved that the selected formulae successfully controlled the drug release.

The aim of this work was to enhance the oral bioavailability of water-insoluble, weaklybasic, anti-emetic drug; Domperidone (DMP), which has a poor oral bioavailability (13-17%). Adsorption of drug onto the surface of Aerosil 200 was achieved by solvent evaporation method to enhance the drug dissolution rate. Then, the adsorbates were formulated into gastro-retentive floating tablets to retain the drug in the acidic medium of stomach which is favorable for the drug dissolution. Different drug: adsorbent ratios were prepared and tested for their in-vitro dissolution rate to select the best ratio for the final formulation. Different concentrations of several polymers were used in the preparation of tablets matrices together with sodium bicarbonate to induce the floating effect via reaction with gastric HCl. Drug-excipient compatibility studies were performed using Fouriertransform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC)which confirmed the absence of incompatibilities between the drug and the used excipients. The tablets were prepared by direct compression technique and evaluated for their weight uniformity, drug content, friability, hardness, thickness, floating properties, in-vitro dissolution rate and kinetics of drug release. Formulae F7 (containing 30% w/w sodium alginate) and F8 (containing 40% w/w sodium alginate) showed the best results and thus; they were selected for in-vivo studies in rabbits. The selected formulae showed marked enhancement of domperidone bioavailability compared with the commercial conventional immediate-release tablets; Motinorm®, with relative bioavailability values of 298.26±11.53% and 315.04±13.39% for F7 and F8, respectively and proved that the selected formulae successfully controlled the drug release.

Objective: The aim of this work was to enhance the bioavailability of poorly soluble, anti-emetic drug; domperidone (DMP) having a poor oral bioavailability (13-17%) due to extensive first pass metabolism. The goal of this study was achieved through solubilization of DMP using solid dispersion technology followed by incorporation of solid dispersions into sublingual tablets to bypass pre-systemic metabolism. Methods: Solid dispersions of DMP with Pluronic F-68 were prepared in different weight ratios by fusion method and they were evaluated for their in vitro dissolution rate to select the best ratio for final formulation. Then, solid dispersions were formulated into sublingual tablets in combination with various soluble excipients. Sublingual tablets were prepared by direct compression technique and evaluated for their physical properties, in vitro dissolution rate and kinetics of drug release. The best formulae were selected for in vivo studies in rabbits in comparison with marketed oral tablets; Motinorm®. Results: Solid dispersions of DMP with Pluronic F-68 in a weight ratio of 1:7 (w/w) showed the highest dissolution rate and were selected for sublingual tablets formulation. Sublingual tablets formulae S16 (containing Fructose and 10% w/w Ac-Di-Sol) and S20 (containing Fructose and 10% w/w Explotab) showed the best results and were selected for in vivo studies in rabbits. The selected formulae showed marked enhancement of DMP bioavailability compared with the commercial oral tablets; Motinorm®, with relative bioavailability values of 432.49±10.13% and 409.32±11.59 % for S16 and S20, respectively. Conclusion: The results confirmed that sublingual tablets were an effective tool for DMP delivery with marked enhancement of bioavailability.

Objective: The aim of this work was to enhance the bioavailability of poorly soluble, anti-emetic drug; domperidone (DMP) having a poor oral bioavailability (13-17%) due to extensive first pass metabolism. The goal of this study was achieved through solubilization of DMP using solid dispersion technology followed by incorporation of solid dispersions into sublingual tablets to bypass pre-systemic metabolism. Methods: Solid dispersions of DMP with Pluronic F-68 were prepared in different weight ratios by fusion method and they were evaluated for their in vitro dissolution rate to select the best ratio for final formulation. Then, solid dispersions were formulated into sublingual tablets in combination with various soluble excipients. Sublingual tablets were prepared by direct compression technique and evaluated for their physical properties, in vitro dissolution rate and kinetics of drug release. The best formulae were selected for in vivo studies in rabbits in comparison with marketed oral tablets; Motinorm®. Results: Solid dispersions of DMP with Pluronic F-68 in a weight ratio of 1:7 (w/w) showed the highest dissolution rate and were selected for sublingual tablets formulation. Sublingual tablets formulae S16 (containing Fructose and 10% w/w Ac-Di-Sol) and S20 (containing Fructose and 10% w/w Explotab) showed the best results and were selected for in vivo studies in rabbits. The selected formulae showed marked enhancement of DMP bioavailability compared with the commercial oral tablets; Motinorm®, with relative bioavailability values of 432.49±10.13% and 409.32±11.59 % for S16 and S20, respectively. Conclusion: The results confirmed that sublingual tablets were an effective tool for DMP delivery with marked enhancement of bioavailability.

Objective: The aim of this work was to enhance the bioavailability of poorly soluble, anti-emetic drug; domperidone (DMP) having a poor oral bioavailability (13-17%) due to extensive first pass metabolism. The goal of this study was achieved through solubilization of DMP using solid dispersion technology followed by incorporation of solid dispersions into sublingual tablets to bypass pre-systemic metabolism. Methods: Solid dispersions of DMP with Pluronic F-68 were prepared in different weight ratios by fusion method and they were evaluated for their in vitro dissolution rate to select the best ratio for final formulation. Then, solid dispersions were formulated into sublingual tablets in combination with various soluble excipients. Sublingual tablets were prepared by direct compression technique and evaluated for their physical properties, in vitro dissolution rate and kinetics of drug release. The best formulae were selected for in vivo studies in rabbits in comparison with marketed oral tablets; Motinorm®. Results: Solid dispersions of DMP with Pluronic F-68 in a weight ratio of 1:7 (w/w) showed the highest dissolution rate and were selected for sublingual tablets formulation. Sublingual tablets formulae S16 (containing Fructose and 10% w/w Ac-Di-Sol) and S20 (containing Fructose and 10% w/w Explotab) showed the best results and were selected for in vivo studies in rabbits. The selected formulae showed marked enhancement of DMP bioavailability compared with the commercial oral tablets; Motinorm®, with relative bioavailability values of 432.49±10.13% and 409.32±11.59 % for S16 and S20, respectively. Conclusion: The results confirmed that sublingual tablets were an effective tool for DMP delivery with marked enhancement of bioavailability.