The aim of this study was to formulate and characterize fast dissolving films containing dextromethorphan hydrobromide (DM) for oral use. Hydroxylpropyl methylcellulose E15 (HPMC) was used as the film forming polymer and crosspovidone (CPV), microcrystalline cellulose (MCC) were used as superdisintegrants. In this study, medicated films were prepared by solvent casting method. The physicochemical characterizations were done by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) for DM-loaded fast dissolving films and their corresponding physical mixtures as well as the individual components to investigate the drug polymer interaction. The obtained DSC and FTIR results indicated that DM was molecularly dispersed in the matrix of HPMC. The prepared films were also characterized for their tensile strength, percentage of elongation, taste palatability, surface pH, weight and their content uniformity. In addition, DM-loaded oral films were elegant enough, transparent, flexible, smooth, homogeneous and palatable. It was found also that both of film disintegration and drug release increased as the concentration of disintegrant in the film increased.

Famotidine (FM) is a potent H2-receptor antagonist used for the treatment of peptic ulcer. It has a low and variable bioavailability which is attributed to its low water solubility. In this study, the dissolution of the drug was enhanced by a preparation of solid dispersion using two hydrophilic carriers, namely Gelucire 50/13 and Pluronic F-127. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), which indicated that there were no signs of interaction of the drug with the carriers used in the case of solid dispersions containing higher polymeric contents (1:3 and 1:5). FM solid dispersions in the matrices of Gelucire 50/13 and Pluronic F-127 (1:3) were used to prepare pellets. The scanning electron microscope (SEM) images of pellets showed that the pellets have spherical shape and their size depends on the carrier used. The dissolution of the drug from either solid dispersion or pellets was performed. The dissolution study depicted that, the presence of the drug in solid dispersion enhanced its dissolution in comparison with the drug itself. Also, the drug release from the manufactured pellets was found to be improved in the case of solid dispersions (drug : carrier 1:3). A complete drug release occurred after 30 min from pellets containing solid dispersions, while only about 30% of the loaded FM was released from pellets containing untreated drug after 2 h.

Temperature dependent solubility data of tadalafil (TDL) in diethylene glycol monoethyl ether (Transcutol) + water co-solvent mixtures are not available in literature. Therefore, the aim of present study was to determine the temperature dependent solubility data of crystalline TDL in mono-solvents and various Transcutol + water co-solvent mixtures from 298.15 to 333.15 K at atmospheric pressure. The experimental solubilities of crystalline TDL were measured using the shake flask method. The experimental solubilities were correlated with the Apelblat model. The solubilities of crystalline TDL were regressed by Apelblat equation with a relative deviation in the range of 0.02 to 6.81% in all co-solvent mixtures investigated at 298.15 to 333.15 K. The root mean square deviations were observed in the range of 0.013 to 0.058. However, the correlation coefficients were observed in the range of 0.996 to 0.999. The solubility of crystalline TDL was found to be increased with increase in temperature and mass fraction of Transcutol in co-solvent mixtures. The mole fraction solubility of crystalline TDL was observed highest in pure Transcutol (8.76×10−3 at 298.15 K) as compared to water (5.74×10−7 at 298.15 K). Around 15,263 fold enhancements in solubility of crystalline TDL in Transcutol were observed as compared to its aqueous solubility at 298.15 K. The dissolution of TDL in most of the co-solvent mixtures was assumed to be non-spontaneous, endothermic and an entropy driven process. Overall, the results of these studies indicated that Transcutol could be used as a co-solvent in formulation development especially in terms of liquid dosage forms of crystalline TDL.

In present study, the solubility data of tadalafil in mono-solvents and various polyethylene glycol 400 (PEG 400) + water co-solvent mixtures from 298.15 to 333.15 K was measured. The experimental mole fraction solubility data of TDL from 298.15 to 333.15 K was measured and correlated. The experimental solubilities of TDL were regressed by the modified Apelblat model with absolute relative deviation in the range of 0.0006-2.2000 % in all co-solvent mixtures. However, the correlation coefficients were observed in the range of 0.9955-0.9998. The mean absolute errors by Yalkowsky model were observed in the range of 0.332-0.442. The mole fraction solubility of TDL was found to be highest in pure PEG 400 (1.86 × 10- 2 at 298.15 K) as compared to water (5.7 × 10- 7 at 298.15 K). The thermophysical parameters such as enthalpies and entropies for TDL dissolution indicated that the dissolution of TDL is endothermic and an entropy-driven process.

The aim of this study was to measure and correlate the temperature dependent solubility data of tadalafil (TDL) in water, ethanol, propylene glycol (PG), polyethylene glycol-400 (PEG-400), and Transcutol from (298.15 to 333.15) K at atmospheric pressure using the shake flask method. The experimental solubilities were regressed by Apelblat equation with a relative deviation in the range of (1.20 to 5.74) % in all solvents investigated at (298.15 to 333.15) K. The root mean square deviation between experimental and calculated solubility was observed less than 1.10 in all solvents investigated. The correlation coefficients in water, ethanol, PG, PEG-400, and Transcutol were observed in the range of 0.997 to 0.999. The solubility of TDL was found to be increased with an increase in temperature in all solvents investigated. The mole fraction solubility of TDL was found to be higher in PEG-400 (1.86•10–2 at 298.15 K) and Transcutol (8.76•10–3 at 298.15 K) as compared to water (5.74•10–7 at 298.15 K), ethanol (1.77•10–4 at 298.15 K) and PG (4.1•10–4 at 298.15 K).

The aim of this study was to measure and correlate the temperature dependent solubility data of tadalafil (TDL) in water, ethanol, propylene glycol (PG), polyethylene glycol-400 (PEG-400), and Transcutol from (298.15 to 333.15) K at atmospheric pressure using the shake flask method. The experimental solubilities were regressed by Apelblat equation with a relative deviation in the range of (1.20 to 5.74) % in all solvents investigated at (298.15 to 333.15) K. The root mean square deviation between experimental and calculated solubility was observed less than 1.10 in all solvents investigated. The correlation coefficients in water, ethanol, PG, PEG-400, and Transcutol were observed in the range of 0.997 to 0.999. The solubility of TDL was found to be increased with an increase in temperature in all solvents investigated. The mole fraction solubility of TDL was found to be higher in PEG-400 (1.86•10–2 at 298.15 K) and Transcutol (8.76•10–3 at 298.15 K) as compared to water (5.74•10–7 at 298.15 K), ethanol (1.77•10–4 at 298.15 K) and PG (4.1•10–4 at 298.15 K).

This study was designed to evaluate the suitability of Pluronic F-127, different grades of Carbopol and cellulosic polymers as gel bases containing tolmetin, a non-steroidal anti-inflammatory drug. In vitro release characteristics, effect of enhancers, viscosity and the mechanism of drug release for different gel bases was studied as well as the anti-inflammatory activity were evaluated. The results showed that the HPMC gel has the superior percent of drug release than the others. The percent released of drug from Carbopol and the Pluronic F-127 gels is concentration defendants. It was found that the drug release from the tested gel bases obeyed the diffusion mechanism. The use of propylene glycol and urea in different concentrations (3.0, 5.0 and 10 % w/v) had enhanced the percent of drug release significantly (p 0.05). The anti-inflammatory activity of the drug in Carbopol gel formulation showed excellent anti-inflammatory activity. These finding highlight the potential local application of tolmetin gel as topical anti-inflammatory medication.

This study was aimed to prepare and characterize fast dissolving films containing antiemetic drug, Metoclopramide hydrochloride (MH), for oral use to avoid more stimulation of emesis by using other dosage forms such as tablets or syrups. Methylcellulose (MC) was used as the film forming polymer and croscarmelose Sodium (CCS) and sodium starch glycolate (SSG) were used as super disintegrants. Medicated films were prepared by solvent casting method. The physicochemical characterizations were done by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) for MH-loaded fast dissolving films and their corresponding physical mixtures as well as the individual components to investigate the drug polymer interaction. The obtained DSC and FTIR results indicated that MH was molecularly dispersed in the matrix of MC. The prepared films were also characterized for their tensile strength, percentage of elongation, taste palatability, surface pH, weight and their content uniformity. In addition, MH-loaded oral films were elegant enough, transparent, flexible, smooth, homogeneous and palatable. The films were disintegrated within seconds and the drug was released within 3 min. It was found also that neither addition of superdisintegrant nor their concentrations have an effect on the drug dissolution.

This study was aimed to prepare and characterize fast dissolving films containing antiemetic drug, Metoclopramide hydrochloride (MH), for oral use to avoid more stimulation of emesis by using other dosage forms such as tablets or syrups. Methylcellulose (MC) was used as the film forming polymer and croscarmelose Sodium (CCS) and sodium starch glycolate (SSG) were used as super disintegrants. Medicated films were prepared by solvent casting method. The physicochemical characterizations were done by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) for MH-loaded fast dissolving films and their corresponding physical mixtures as well as the individual components to investigate the drug polymer interaction. The obtained DSC and FTIR results indicated that MH was molecularly dispersed in the matrix of MC. The prepared films were also characterized for their tensile strength, percentage of elongation, taste palatability, surface pH, weight and their content uniformity. In addition, MH-loaded oral films were elegant enough, transparent, flexible, smooth, homogeneous and palatable. The films were disintegrated within seconds and the drug was released within 3 min. It was found also that neither addition of superdisintegrant nor their concentrations have an effect on the drug dissolution.

Self-emulsifying drug delivery systems (SEDDS) have been widely employed to improve the oral bioavailability of poorly soluble drugs. In the past few years, SEDDS were extensively investigated to overcome various barriers encountered in the oral delivery of hydrophilic macromolecules (e.g., protein/peptide therapeutics and plasmid DNA (pDNA)), as well as in lowering the effect of food on drugs' bioavailability. However, the main mechanism(s) by which SEDDS could achieve such promising effects remains not fully understood. This review summarizes the recent progress in the use of SEDDS for protecting protein therapeutics and/or pDNA against enzymatic degradation and increasing the oral bioavailability of various drug substances regardless of the dietary condition. Understanding the underlying mechanism(s) of such promising applications will aid in the future development of rationally designed SEDDS. Entrapment of hydrophilic macromolecules in the oil phase of the formed emulsion is critical for protection of the loaded cargoes against enzymatic degradation and the enhancement of oral bioavailability. On the other hand, drug administration as a preconcentrated solution in the SEDDS preconcentrate allows the process of drug absorption to occur independently of the dietary condition, and thus reducing interindividual variability that results from concomitant food intake.