Journal of Excipients and Food Chemicals, Jun 25, 2014
Directly compressed matrices were produced using a binary mixture of different chitosan (CH) and ... more Directly compressed matrices were produced using a binary mixture of different chitosan (CH) and xanthan gum (XG) ratios. These hydrophilic excipients were used to control the release of ambroxol HCl. CH and XG were investigated at three ratios of 1:1, 1:4 and 4:1. Mucosolvan LA ® was used as a commercially available reference product. The optimal CH to XG ratio was 1:1 and the optimal drug to polymer ratio was 1:3. Matrix erosion, hydration and drug release studies were carried out using a dissolution apparatus (basket method). The release mechanism is also discussed.
Adsorption isotherms of aqueous bromhexine hydrochloride (BHCI) were determined for activated cha... more Adsorption isotherms of aqueous bromhexine hydrochloride (BHCI) were determined for activated charcoal, kaolin, elcema, avicel PH 101 and 102. The affinity of BHCI adsorption on charcoal was the highest followed by kaolin, avicel, elcema in a decreasing order. The pH alteration affected the adsorption on charcoal slightly. Adsorption by microcrystalline cellulose. and kaolin increased moderately with pH increase. The presence of sodium chloride enhanced the adsorption on all adsorbents used. The larger the particle size the lower the adsorption. Adsorption from mediums containing ethanol and glycerine was lower than the corresponding aqueous solution. The extent of adsorption by charcoal and cellulose showed little dependence on temperature within the range 20-46". The standard thermodynamic functions, enthalpy, entropy and free energy were obtained. Adsorption on avicel proved to be favoured by both enthalpy and entropy, while enthalpy is the major driving force for adsorption on charcoal. Surface tension and conductivity measurements indicated that adsorption of BHCl may take place as a monomer.
The compressibility and compactibility studies of binary mixtures containing chitosan (CS) and xa... more The compressibility and compactibility studies of binary mixtures containing chitosan (CS) and xanthan gum (XG) were highlighted in this article. The compressibility of the examined powders was studied according to Heckel and Gurnham equations. Results indicated that CS exhibits more ductile character than XG. Moreover, in this study percolation theory has been applied to the tensile strength of different compacts obtained from CS-XG mixtures. The obtained percolation thresholds showed that higher pressures must be applied to form compacts with a specific strength as the mass fraction of XG was increased. Additionally, the values of the maximum tensile strength showed that the percolation threshold of CS occurs at equal mass fraction of the two polymers. Scanning electron microscope, light microscope techniques, and molecular mechanical calculations were also conducted in order to study the interactions between CS and XG. The obtained results revealed that 1:1 ratio (by weight) represents the maximum interactions between the two polymers.
The aim of the work reported herein was to study the effect of glucosamine HCl (GlcN·HCl) on the ... more The aim of the work reported herein was to study the effect of glucosamine HCl (GlcN·HCl) on the bioactivity (BA) of insulin, administered via subcutaneous (SC) and oral routes, in adult male Sprague Dawley rats. The oral insulin delivery system (insulin-chitosan reverse micelle [IC-RM]) was prepared by solubilizing insulin-chitosan (13 kDa) polyelectrolyte complex in a RM system consisting of oleic acid, PEG-8 caprylic/capric glycerides, and polyglycerol-6-dioleate. The BA of insulin in vivo was evaluated by measuring blood glucose level using a blood glucose meter; the results revealed that the extent of hypoglycemic activity of SC insulin was GlcN·HCl dose dependent when they were administered simultaneously. A significant reduction in blood glucose levels (P<0.05) was found for the insulin:GlcN·HCl at mass ratios of 1:10 and 1:20, whereas lower ratios (eg, 1:1 and 1:4) showed no significant reduction. Furthermore, enhancement of the action of SC insulin was achieved by oral administration of GlcN·HCl for 5 consecutive days prior to insulin injection (P<0.05). For oral insulin administration via the IC-RM system, the presence of GlcN·HCl increased the hypoglycemic activity of insulin (P<0.05). The relative BA were 6.7% and 5.4% in the presence and absence of GlcN·HCl (ie, the increase in the relative BA was approximately 23% due to incorporating GlcN·HCl in the IC-RM system), respectively. The aforementioned findings offer an opportunity to incorporate GlcN·HCl in oral insulin delivery systems in order to enhance a reduction in blood glucose levels.
The present invention relates to a pharmaceutical excipient comprising a mixture of sugar alcohol... more The present invention relates to a pharmaceutical excipient comprising a mixture of sugar alcohol and chitin and/ or chitin derivatives, a method for its preparation and use thereof.
The present invention relates in general to the field of drug delivery. More precisely, the prese... more The present invention relates in general to the field of drug delivery. More precisely, the present invention relates to a novel type of nanocapsule. In addition, the present invention concerns the use of such a nanocapsule for the delivery of an active component, such as a protein or polypeptide, such as, for example, insulin, a method for manufacturing such a nanocapsule and a pharmaceutical composition comprising such a nanocapsule.
The present invention relates to a combination of herbal extracts to treat male sexual dysfunctio... more The present invention relates to a combination of herbal extracts to treat male sexual dysfunction. More precisely, the present invention relates to a combination of five different herbal extracts including Ginseng extract, Tongkat AIi extract, Epimedium extract, Gotu Kola extract and flower pollen extract to restore male erectile function. The composition has a promoting effect on penile erectility, so that it can be effectively used for the improvement of erectile dysfunction.
Methyl-5-benzoyl-2-benzimidazole carbamate (mebendazole) is a drug used as an anthelmintic. A hig... more Methyl-5-benzoyl-2-benzimidazole carbamate (mebendazole) is a drug used as an anthelmintic. A high performance liquid chromatography method has been developed in this study to determine mebendazole and its degradation product in the pharmaceutical dosage forms (tablets and suspension). The expected major degradation product of mebendazole in the dosage forms has been prepared, and identified as 2-amino-5-benzoylbenzimidazole. The proposed HPLC assay was
The degree of deacetylation (DDA) of various low molecular weight chitosan (LMWC) species as the ... more The degree of deacetylation (DDA) of various low molecular weight chitosan (LMWC) species as the hydrochloride and free base (amine form) was determined by direct and back potentiometric titration,respectively. The DDA values obtained for the chitosan hydrochloride by direct titration were greater than 93% for all oligomers tested (Molecular weight (Mwt) between about 1.3 to 30.0 kDa). However, the DDA values obtained for chitosan amine oligomers using back titration were significantly lower, especially for the relatively high molecular weight (30.0 kDa) chitosan amine oligomers. Furthermore, after using the back titration method, greater DDA values were obtained for the same samples of chitosan amine after the chitosan solution had been heated to 60EC before titration. In addition, the DDA values showed a significant decrease with increased concentration for a given chitosan oligomer. Although the effects of hydration time,ionic strength and method specific behavior were not explic...
Molecular dynamics (MD) simulations using the Amber force field have been applied to obtain detai... more Molecular dynamics (MD) simulations using the Amber force field have been applied to obtain detailed information on inclusion complex formation between natural cyclodextrins (CDs) and organic molecules (1-alkanols, substituted phenols, and substituted imidazoles). The obtained MD trajectories were used to estimate the binding free energy of each guest/CD complex using the molecular mechanics/Poisson Boltzmann surface area (MM-PBSA) method. The calculated relative binding free energies of the inclusion complexes of some organic compounds with a-and b-CDs were in good agreement with the experimental data though the absolute values were not. Inspection of the binding free energy components revealed the dominant contribution of van der Waals interactions to inclusion complex stability. Both guest-host electrostatic interactions and the hydrophobic effect do also contribute to complex stability. It was also apparent from the calculations that the flexibility of the guest molecule has a significant contribution to complex stability.
Polymorphic modifications of terfenadine as well as solvates from various solvents have been prep... more Polymorphic modifications of terfenadine as well as solvates from various solvents have been prepared and characterised by X-ray powder diffraction (XRPD), infrared (IR) spectroscopy, differential scanning calorimetry (DSC) and thermogravimetric analysis. Crystallization of terfenadine from n-alkanols, except methanol and ethanol, resulted in the stable polymorph 1 (m.p. 151°C) while the iso-alkanols yielded the corresponding solvates. Water content, temperature of incubation and duration were found to have significant effect on transformation.
The effect of reduced (GSH) and oxidized (GSSG) glutathione on the bioactivity of insulin was stu... more The effect of reduced (GSH) and oxidized (GSSG) glutathione on the bioactivity of insulin was studied. A polyelectrolyte complex (PEC) of insulin with low molecular weight chitosan (13 kDa) was prepared and characterized. The PEC was then solubilized, in the presence and absence of GSH and GSSG, in a reverse micelle consisting of oleic acid and two surfactants (PEG-8 caprylic/capric glycerides and polyglycerol-6-dioleate). The in vitro and in vivo performances of the reverse micelle formulations (RMFs) were evaluated in rats. At pH 6.5 the association efficiency of the PEC was 76.2%. In vitro insulin release from the RMs was negligible at pH 1.2 and was markedly increased at pH 6.8. The hypoglycemic activity of insulin in the PEC was reduced when administered via the subcutaneous route, regardless of the GSH content. On the other hand, the presence of GSSG significantly enhanced hypoglycemia. When the RMF was administered via the oral route, the presence of GSH had no effect on the ...
Journal of Excipients and Food Chemicals, Jun 25, 2014
Directly compressed matrices were produced using a binary mixture of different chitosan (CH) and ... more Directly compressed matrices were produced using a binary mixture of different chitosan (CH) and xanthan gum (XG) ratios. These hydrophilic excipients were used to control the release of ambroxol HCl. CH and XG were investigated at three ratios of 1:1, 1:4 and 4:1. Mucosolvan LA ® was used as a commercially available reference product. The optimal CH to XG ratio was 1:1 and the optimal drug to polymer ratio was 1:3. Matrix erosion, hydration and drug release studies were carried out using a dissolution apparatus (basket method). The release mechanism is also discussed.
Adsorption isotherms of aqueous bromhexine hydrochloride (BHCI) were determined for activated cha... more Adsorption isotherms of aqueous bromhexine hydrochloride (BHCI) were determined for activated charcoal, kaolin, elcema, avicel PH 101 and 102. The affinity of BHCI adsorption on charcoal was the highest followed by kaolin, avicel, elcema in a decreasing order. The pH alteration affected the adsorption on charcoal slightly. Adsorption by microcrystalline cellulose. and kaolin increased moderately with pH increase. The presence of sodium chloride enhanced the adsorption on all adsorbents used. The larger the particle size the lower the adsorption. Adsorption from mediums containing ethanol and glycerine was lower than the corresponding aqueous solution. The extent of adsorption by charcoal and cellulose showed little dependence on temperature within the range 20-46". The standard thermodynamic functions, enthalpy, entropy and free energy were obtained. Adsorption on avicel proved to be favoured by both enthalpy and entropy, while enthalpy is the major driving force for adsorption on charcoal. Surface tension and conductivity measurements indicated that adsorption of BHCl may take place as a monomer.
The compressibility and compactibility studies of binary mixtures containing chitosan (CS) and xa... more The compressibility and compactibility studies of binary mixtures containing chitosan (CS) and xanthan gum (XG) were highlighted in this article. The compressibility of the examined powders was studied according to Heckel and Gurnham equations. Results indicated that CS exhibits more ductile character than XG. Moreover, in this study percolation theory has been applied to the tensile strength of different compacts obtained from CS-XG mixtures. The obtained percolation thresholds showed that higher pressures must be applied to form compacts with a specific strength as the mass fraction of XG was increased. Additionally, the values of the maximum tensile strength showed that the percolation threshold of CS occurs at equal mass fraction of the two polymers. Scanning electron microscope, light microscope techniques, and molecular mechanical calculations were also conducted in order to study the interactions between CS and XG. The obtained results revealed that 1:1 ratio (by weight) represents the maximum interactions between the two polymers.
The aim of the work reported herein was to study the effect of glucosamine HCl (GlcN·HCl) on the ... more The aim of the work reported herein was to study the effect of glucosamine HCl (GlcN·HCl) on the bioactivity (BA) of insulin, administered via subcutaneous (SC) and oral routes, in adult male Sprague Dawley rats. The oral insulin delivery system (insulin-chitosan reverse micelle [IC-RM]) was prepared by solubilizing insulin-chitosan (13 kDa) polyelectrolyte complex in a RM system consisting of oleic acid, PEG-8 caprylic/capric glycerides, and polyglycerol-6-dioleate. The BA of insulin in vivo was evaluated by measuring blood glucose level using a blood glucose meter; the results revealed that the extent of hypoglycemic activity of SC insulin was GlcN·HCl dose dependent when they were administered simultaneously. A significant reduction in blood glucose levels (P<0.05) was found for the insulin:GlcN·HCl at mass ratios of 1:10 and 1:20, whereas lower ratios (eg, 1:1 and 1:4) showed no significant reduction. Furthermore, enhancement of the action of SC insulin was achieved by oral administration of GlcN·HCl for 5 consecutive days prior to insulin injection (P<0.05). For oral insulin administration via the IC-RM system, the presence of GlcN·HCl increased the hypoglycemic activity of insulin (P<0.05). The relative BA were 6.7% and 5.4% in the presence and absence of GlcN·HCl (ie, the increase in the relative BA was approximately 23% due to incorporating GlcN·HCl in the IC-RM system), respectively. The aforementioned findings offer an opportunity to incorporate GlcN·HCl in oral insulin delivery systems in order to enhance a reduction in blood glucose levels.
The present invention relates to a pharmaceutical excipient comprising a mixture of sugar alcohol... more The present invention relates to a pharmaceutical excipient comprising a mixture of sugar alcohol and chitin and/ or chitin derivatives, a method for its preparation and use thereof.
The present invention relates in general to the field of drug delivery. More precisely, the prese... more The present invention relates in general to the field of drug delivery. More precisely, the present invention relates to a novel type of nanocapsule. In addition, the present invention concerns the use of such a nanocapsule for the delivery of an active component, such as a protein or polypeptide, such as, for example, insulin, a method for manufacturing such a nanocapsule and a pharmaceutical composition comprising such a nanocapsule.
The present invention relates to a combination of herbal extracts to treat male sexual dysfunctio... more The present invention relates to a combination of herbal extracts to treat male sexual dysfunction. More precisely, the present invention relates to a combination of five different herbal extracts including Ginseng extract, Tongkat AIi extract, Epimedium extract, Gotu Kola extract and flower pollen extract to restore male erectile function. The composition has a promoting effect on penile erectility, so that it can be effectively used for the improvement of erectile dysfunction.
Methyl-5-benzoyl-2-benzimidazole carbamate (mebendazole) is a drug used as an anthelmintic. A hig... more Methyl-5-benzoyl-2-benzimidazole carbamate (mebendazole) is a drug used as an anthelmintic. A high performance liquid chromatography method has been developed in this study to determine mebendazole and its degradation product in the pharmaceutical dosage forms (tablets and suspension). The expected major degradation product of mebendazole in the dosage forms has been prepared, and identified as 2-amino-5-benzoylbenzimidazole. The proposed HPLC assay was
The degree of deacetylation (DDA) of various low molecular weight chitosan (LMWC) species as the ... more The degree of deacetylation (DDA) of various low molecular weight chitosan (LMWC) species as the hydrochloride and free base (amine form) was determined by direct and back potentiometric titration,respectively. The DDA values obtained for the chitosan hydrochloride by direct titration were greater than 93% for all oligomers tested (Molecular weight (Mwt) between about 1.3 to 30.0 kDa). However, the DDA values obtained for chitosan amine oligomers using back titration were significantly lower, especially for the relatively high molecular weight (30.0 kDa) chitosan amine oligomers. Furthermore, after using the back titration method, greater DDA values were obtained for the same samples of chitosan amine after the chitosan solution had been heated to 60EC before titration. In addition, the DDA values showed a significant decrease with increased concentration for a given chitosan oligomer. Although the effects of hydration time,ionic strength and method specific behavior were not explic...
Molecular dynamics (MD) simulations using the Amber force field have been applied to obtain detai... more Molecular dynamics (MD) simulations using the Amber force field have been applied to obtain detailed information on inclusion complex formation between natural cyclodextrins (CDs) and organic molecules (1-alkanols, substituted phenols, and substituted imidazoles). The obtained MD trajectories were used to estimate the binding free energy of each guest/CD complex using the molecular mechanics/Poisson Boltzmann surface area (MM-PBSA) method. The calculated relative binding free energies of the inclusion complexes of some organic compounds with a-and b-CDs were in good agreement with the experimental data though the absolute values were not. Inspection of the binding free energy components revealed the dominant contribution of van der Waals interactions to inclusion complex stability. Both guest-host electrostatic interactions and the hydrophobic effect do also contribute to complex stability. It was also apparent from the calculations that the flexibility of the guest molecule has a significant contribution to complex stability.
Polymorphic modifications of terfenadine as well as solvates from various solvents have been prep... more Polymorphic modifications of terfenadine as well as solvates from various solvents have been prepared and characterised by X-ray powder diffraction (XRPD), infrared (IR) spectroscopy, differential scanning calorimetry (DSC) and thermogravimetric analysis. Crystallization of terfenadine from n-alkanols, except methanol and ethanol, resulted in the stable polymorph 1 (m.p. 151°C) while the iso-alkanols yielded the corresponding solvates. Water content, temperature of incubation and duration were found to have significant effect on transformation.
The effect of reduced (GSH) and oxidized (GSSG) glutathione on the bioactivity of insulin was stu... more The effect of reduced (GSH) and oxidized (GSSG) glutathione on the bioactivity of insulin was studied. A polyelectrolyte complex (PEC) of insulin with low molecular weight chitosan (13 kDa) was prepared and characterized. The PEC was then solubilized, in the presence and absence of GSH and GSSG, in a reverse micelle consisting of oleic acid and two surfactants (PEG-8 caprylic/capric glycerides and polyglycerol-6-dioleate). The in vitro and in vivo performances of the reverse micelle formulations (RMFs) were evaluated in rats. At pH 6.5 the association efficiency of the PEC was 76.2%. In vitro insulin release from the RMs was negligible at pH 1.2 and was markedly increased at pH 6.8. The hypoglycemic activity of insulin in the PEC was reduced when administered via the subcutaneous route, regardless of the GSH content. On the other hand, the presence of GSSG significantly enhanced hypoglycemia. When the RMF was administered via the oral route, the presence of GSH had no effect on the ...
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