Dissolution Rate Of Tablets Research Articles

Effects of Glass Bead Size on Dissolution Profiles in Flow-through Dissolution Systems (USP 4).

The effects of glass bead size in the conical space of flow-through cells on the dissolution profiles were investigated in a USP apparatus 4. Dissolution tests of disintegrating and non-disintegrating tablets in flow-through dissolution systems were performed using semi-high precision glass beads with diameters ranging from 0.5mm to 1.5mm. Computational fluid dynamics (CFD) was used to evaluate the effect of shear stress from the dissolution media flow. The use of smaller glass beads in a larger cell resulted in a faster dissolution of the model formulations under certain test conditions. The effect on the dissolution was highly dependent on the size of the beads in the top layer, including those in contact with the tablets. The absence of a bead-size effect on the dissolution of an orodispersible tablet in a small cell can be explained by the floating fragments during the test. CFD analysis showed that smaller bead diameters led to greater shear stress on the tablet, which was correlated with the dissolution rate. Hence, fluid flow through the narrow gaps between the small beads generated strong local flows, causing shear stress. The size of the glass beads used in flow-through cells affects the dissolution rate of tablets by altering the shear stress on the tablets in certain cases (e.g., direct deposition of the formulation on glass beads, large cells, and very low flow rates). Thus, glass bead size must be considered for a robust dissolution test in a flow-through cell system.

Enhancement of Solubility and Dissolution Rate of Simvastatin Tablets by Liquisolid Compact Approach

The aim of the current work was to improve the solubility and dissolution rate of poorly water-soluble drug, simvastatin (SM) by using the liquisolid compact technique (LS; SM-LS). Liquid load factors, and excipient ratios were used to calculate the required amounts of excipients necessary to prepare the SM-LS and compressed to tablets according to mathematical models. Avicel PH102, Aerosil 200 and Crosspovidone (CP) was used as carrier, coating material and disintegrant, respectively. Drug-excipient mixtures were evaluated compatibility by Attenuated total reflectance (ATR) and differential scanning calorimetry (DSC). Prepared SM-LS formulations were evaluated for various pre-compression and post-compressional parameters, in-vitro dissolution, and stability studies (40 ± 2°C / 75 ± 5% RH) for 3 months. Among the different formulations, LS10 formulation which contains 30% drug, 5% CP, Avicel pH 102: Aerosil 200 (1:10) showed 14-folds increase in dissolution rate when compared with pure SM powder. FTIR-ATR and DSC studies confirmed that there was no interaction between the drug and excipients. Further, the LS10 formulation had shown comparable dissolution profile with commercially available tablet formulation. The LS10 formulation showed no significant changes in the physicochemical properties over 3 months during stability studies. Therefore, the SM loaded LS formulation could be considered as an alternative approach to enhance the solubility and dissolution for commercial formulations. Keywords: Liquisolids compacts, solubility, dissolution, carrier, coating material, stability.

The impact of sinkers on coning issues exhibited by tablets in USP2 dissolution apparatus

The objective of this research is to explore the impact of sinkers on the dissolution rate of tablets exhibiting coning in paddle dissolution tests. The ICH M9 guideline refers to the use of sinkers to mitigate coning issues. However, the effectiveness of sinkers on coning phenomena has not been comprehensively investigated. Therefore, this study evaluated whether applying sinkers of different shapes could alleviate coning problems. The dissolution profiles of amlodipine tablet formulations which had been clinically demonstrated to be bioequivalent were assessed in a USP2 Apparatus with and without sinkers. Moreover, the effects of artificially induced coning formed by adding cellulose particles of various sizes on dissolution profiles, and the impacts of sinkers on the dissolution delay caused by the cellulose particles were investigated. Our study suggested that the CLIPS sinker was effective in obtaining in vivo relevant dissolution profiles by facilitating the dispersion of coning. The effect of sinkers varied depending on their shapes and the characteristics of the particles that constituted the coning. These findings enhance our understanding of the effectiveness of sinkers in addressing coning issues and aid in predicting the in vivo dissolution performance of tablet formulations that exhibit coning during dissolution testing.

Investigating a Calcium Alginate-Xylitol Coating Methodology for Controlled Release Profiles of Multivitamin Tablet as a Model Drug

The drug delivery system promotes the release of the active pharmaceutical ingredient (API) to attain the desired therapeutic effect at the time most needed. Alginate is a natural polymer that is frequently employed in drug delivery systems. Calcium alginate can simply coat as a film type on the surface of a tablet, which might be created to be dissolved more quickly and predictably manners in the gastric fluid to deliver as needed in a patient-friendly system. In this study, the sodium alginate solution was reacted with a predetermined calcium compound and xylitol combination, while the multivitamin tablets’ surface was coated with calcium suppliers such as calcium chloride. Then, the coated tablets were subjected to a dissolution test in a simulated gastric fluid. Our study results showed that the sphere formation was excellent in terms of strength and size in 1.0% sodium alginate with 4% calcium chloride. Average sphere sizes were 0.5 ~ 2.0 mm. Their break force was 3.5 N, And the dissolution was the fastest in the coated tablets with 1% sodium alginate and calcium chloride. The dissolution rate was changed proportionally with calcium concentration. A high feasibility of dissolution rate was positively found. When a high concentration of xylitol was mixed with 4% calcium chloride, the dissolution rate was proportional to the concentration of xylitol. In conclusion, the study demonstrated that the dissolution rate of tablets with API might be controllable with the calcium alginate film coating with xylitol.

Predicting gastric emptying of drug substances taken under postprandial conditions by combination of biorelevant dissolution and mechanistic in silico modeling

Physiologically based pharmacokinetic (PBPK) models can help to understand the effects of gastric emptying on pharmacokinetics and in particular also provide a platform for understanding mechanisms of food effects, as well as extrapolation between different postprandial conditions, whether standardized clinical or patient-oriented, non-clinical conditions. By integrating biorelevant dissolution data from the GastroDuo dissolution model into a previously described mechanistic model of fed-state gastric emptying, we simulated the effects of a high-calorie high-fat meal on the pharmacokinetics of sildenafil, febuxostat, acetylsalicylic acid, theobromine and caffeine. The model was able to simulate the variability in Cmax and tmax caused by the presence of the stomach road. The main influences investigated to affect the gastric emptying process were drug solubility (theobromine and caffeine), tablet dissolution rate (acetylsalicylic acid) and sensitivity to gastric motility (sildenafil and febuxostat). Finally, we showed how PBPK models can be used to extrapolate pharmacokinetics between different prandial states using theobromine as an example with results from a clinical study being presented.

Effects of Beverage Solvents on Disintegration Time and Dissolution Rate of Metronidazole Tablets

Drug Disintegration time refers to the period within which a mechanical break-up of compressed tablet dissolve upon exposure to physiological fluids within a short period of time into tiny granules upon ingestion, while drug dissolution rate becomes a key tool in understanding the importance for its bioavailability and therapeutic effectiveness. Hence, the objective of this paper was to assess the impact of seven different solvents, which includes five non-alcoholic beverages (Exotic juice, soft drink, coffee, milk, and milo), one alcoholic beverage (beer), one dilute acid (0.1 M HCl) and a control distilled water (dil. H2O) on the disintegration time and dissolution rate of metronidazole tablets. The distilled water was used as control. The results obtained show that the mean disintegration times were 2.28 ± 0.04 (0.1 N HCl), 4.21 ± 0.12 (beer), 3.24 ± 0.05 (coffee), 3.23 ± 0.07 (distilled water), 5.21 ± 0.09 (Exotic juice), 3.17 ± 0.06 (Fanta), and 16.16 ± 0.11 (milk). The mean dissolution rates on the other hand were 98.87 ± 0.12, 78.09 ± 0.09, 84.27 ± 0.11, 86.52 ± 0.40, 67.98 ± 0.09, 92.70 ± 0.50, and 44.94 ± 0.22 respectively. Metronidazole tablets disintegrated and dissolved more in 0.1 N HCL than in other mediums and less in milk. From this study, although the disintegration time and dissolution rate of metronidazole were not greatly affected by the different beverages except for Exotic juice, and the mixture of milk and Milo, care should be taken when replacing water with any beverage in ingesting tablets.

The impact of diluents on the compaction, dissolution, and physical stability of amorphous solid dispersion tablets

Amorphous solid dispersion (ASD) is an effective approach for enhancing the solubility, dissolution, and bioavailability of poorly water-soluble drugs. However, these metastable forms can transform into more thermodynamically stable but less soluble crystalline forms. Despite this challenge, research on processing ASDs into solid dosage forms, such as tablets, is lacking. This work aims to fill this gap by investigating the impact of common diluents on the tableting behavior, dissolution, and physical stability of ASDs composed of itraconazole and hypromellose acetate succinate. Four widely used diluents found in commercially available ASD tablets were selected for the study: microcrystalline cellulose (MCC), anhydrous lactose, starch, and mannitol. The performance of ASD tablets varied significantly depending on the diluent used. Tablets prepared with MCC exhibited higher mechanical strength than those formulated using other diluents. ASD tablets containing mannitol and lactose revealed a faster release rate than those composed of MCC or starch. Notably, the study highlighted that the physical stability of ASDs within a tablet is not solely dependent on the amount of sorbed water; crystalline diluents like lactose and mannitol were found to facilitate ASD recrystallization within a tablet. In summary, the study underscores the importance of excipient selection, considering factors such as mechanical strength, dissolution rate, and physical stability of ASD tablets. These findings offer valuable insights into the selection of excipients for downstream ASD tablet development, leading to improved manufacturability, physical stability, and the overall quality of ASD drug products.

Formulation and characterization of amiodarone-methyl-beta-cyclodextrin inclusion complexes: A molecular modelling perspective

This study aimed to develop immediate-release tablets containing amiodarone hydrochloride (AM). AM is a BCS class II compound, i.e., high permeable, and poorly soluble. The interactions between amiodarone and methyl-β-cyclodextrin were DFT-based, theoretically measured, supporting the complexation of AM with cyclodextrin by using methyl-β-cyclodextrin through a spray-drying process. Thus, increasing substantially the drug solubility to 93.31% and 87.14%, respectively. Solubility studies demonstrated the formation of the Drug-Methyl-β-cyclodextrin inclusion complex with 1:1 stoichiometry. The complex formation was characterized by SBET, XRD, DSC, SEM, FTIR, and 1H NMR. Complementing, immediate-release tablets containing the inclusion complex were developed by direct compression, and in vitro dissolution studies were performed in gastrointestinal fluids using USP Pharmacopeia standard dissolution rate testing equipment. The dissolution rate of immediate-release tablets was substantially higher than the pristine drug in all mediums evaluated. These results confirm the application of methyl-β-cyclodextrin as an effective excipient for incorporation in novel dosage forms to increase the solubility of poorly soluble drugs.

Enhancing the dissolution rate of poorly soluble drug Febuxostat using spray dried amorphous solid dispersion technique

Introduction: Febuxostat belongs to Biopharmaceutical classification system (BCS) class II drugs, which have low solubility and high permeability. Amorphous solid dispersion is one of the techniques which can be useful to improve solubility and powder characteristics.
 Objective: To optimize the concentration of hydrophilic and hydrophobic polymers to improve the dissolution rate and solubility of febuxostat tablets.
 Methods: The amorphous solid dispersion of febuxostat was prepared by spray drying method using Kolliphor P237 (1:2). This amorphous solid dispersion was further used to compress the tablet. To improve solubility and dissolution rate, a full factorial design was applied to optimize the critical concentration of Kollidon SR and hydroxypropyl methyl cellulose (HPMC K4M). The prepared tablets were characterized by pre-compression and post-compression parameters.
 Result: The rate of drug release was sustained by formulating an amorphous solid dispersion technique. The optimized batch (FSRT-OB) was found to be fit for release average 93.30 % of the drug in sustain release manner up to 12hrs. The release kinetic data suggests that the drug release was controlled by combination of diffusion and chain relaxation mechanism. The optimized concentration for Kollidon SR and HPMC K4Mwas found to be 38.50 % and 7.72 % respectively.
 Conclusion: Amorphous solid dispersion technique is useful to enhance solubility, dissolution rate, and bioavailability of the Febuxostat tablet.

Determination of dissolution rate of prolonged-release tablets in bio-relevant media using USP apparatus III

Determination of dissolution rate of prolonged-release tablets in bio-relevant media using USP apparatus III

Polymeric hydrogel forming microneedle-mediated transdermal delivery of sildenafil citrate from direct-compressed tablet reservoir for potential improvement of pulmonary hypertension therapy

Pulmonary hypertension (PH) is a cardiovascular disease affecting patient’s life. Sildenafil citrate (SC), the first-line treatment, is present in oral and injectable forms with some drawbacks, primarily poor patient’s comfort and low oral bioavailability. To counter these limitations, stratum corneum-penetrating hydrogel-forming microneedles (HFM) was created, making it easier to distribute SC transdermally. HFM was fabricated using polyvinyl alcohol (PVA) and two variations of polyvinyl pyrrolidone’s (PVP) concentration as polymers and citric acid (CA) as crosslinking agent. The crosslinking time was also variated. The assessment of swelling, insertion characteristics, and mechanical resistance revealed that it possessed swelling capacities up to 470 % and strong insertion capabilities. This HFM was integrated with a tablet reservoir prepared using several concentrations of sodium starch glycolate (SSG) as super disintegrant. The tablet reservoir's hardness, dissolution rate, XRD, and FTIR profiles were evaluated and the results showed that 4 % of SSG was the option for enhancing SC’s solubility. According to ex vivo study, this system released 24.12 ± 0.92 % of SC. For the first time, SC was successfully incorporated into a system of HFM and tablet reservoir and was non-toxic, showing promise in terms of improving PAH therapy's efficacy following comprehensive in vivo studies in the future.

Surface Characterization as a Tool for Identifying the Factors Affecting the Dissolution Rate of Amorphous Solid Dispersion Tablets.

An amorphous solid dispersion (ASD) is a commonly used approach to enhancing the dissolution of poorly aqueous soluble drugs. Selecting the desired polymer and drug loading can be time-consuming. Surface properties, such as surface composition and wetting behavior, are essential factors controlling the dissolution of ASD tablets. Thus, our study aims to use surface characterization to understand the factors that affect the dissolution rate of ASD tablets. In this work, we prepared ASDs with itraconazole and hypromellose acetate succinate (HPMCAS) using spray drying. ASDs were prepared using three grades of HPMCAS and different drug loading levels (10%, 30%, and 50%). We prepared ASD tablets with two porosities. For each tablet, contact angles were measured using the Drop Shape Analyzer; surface free energies, disperse, and polar fractions were calculated based on the contact angles. We conducted near-infrared (NIR) and dissolution measurements of ASD tablets. Principal component analysis (PCA) was carried out to investigate the NIR spectra further. The relative PCA scores were reported with other sample properties. A partial least square (PLS) model using NIR scores, tablets' wetting properties, and dissolution rates revealed that water and buffer contact angles, surface free energy, and polar fraction are the most significant factors attributing to the dissolution rate of ASD tablets. This work understood the interplay between the surface properties and the dissolution rate of ASD tablets. Moreover, surface characterization can be the tool to screen the formulation and compaction process of ASD tablets in early development.

Ginkgo biloba Ketone Ester Tablets with different release rates prepared by fused deposition modeling 3D printing technology

The present study prepared a new type of Ginkgo biloba ketone ester(GBE50) preparation from polyethylene glycol and croscarmellose sodium with good biocompatibility and a certain viscosity by fused deposition modeling(FDM)-type 3D printing technique. Firstly, a cylindrical 3D printing model with a diameter of 9.00 mm and a height of 4.50 mm was established. Subsequently, the 3D-GBE50 preparations with three paths(concentric, zigzag, and grid), different layer heights, and different filling gaps were designed and prepared after the optimization of the proportions of excipients. The morphology, size, chemical properties, and dissolution activity of the 3D-GBE50 preparations were fully characterized and investigated. The results showed that 3D-GBE50 preparations had smooth appearance, clear texture, standard friability, good thermal stability, and stable chemical properties. Moreover, the printing path, layer height, and filling gap were directly related to the release rate of 3D-GBE50 preparations. The dissolution of 3D-GBE50 tablets with zigzag printing path was the fastest, while the dissolution rates of 3D-GBE50 tablets with concentric circle and grid-shaped printing paths were slower than that of commercially available G. biloba Ketone Ester Tablets. In addition, the dissolution of 3D-GBE50 tablets was faster with higher layer height and wider filling gap. As revealed by the results, th FDM-type 3D printing technique can flexibly regulate the drug release activity via controlling the printing parameters, providing effective ideas and methods for the pre-paration of personalized pharmaceutical preparations.

In- vitro Design and Formulation of Levitiracetam Extended Release Tablets

The objective of the present study is to evaluate the extended release tablets of levitiracetam by using HPMC K100, HPMC K15 and Xanthan gum/Ethyl cellulose effect of the dissolution rate of tablets. Tablet each containing 60mg of Levetiracetam were prepared selected combination of factors to evaluate their individual and interaction effects on dissolution rate. The FTIR spectra of pure drug and mixture with various excipients are similar. It’s indicates no chemical intration between drug and excipients. The drug release from all the tablets was diffusion control as indicated by the linear Higuchi plots. The release data was analysed Peppas equation the release exponent (n) was found to be in the range 0.76-0.93. Amount all the levetiracetam tablets prepared formulation F2 (fa) formulated employing HPMC K100, 60mg, HMPC K15, 25mg , Xanthane gum 25mg. In the all cases formulations F1, F3, F4, F5, F8 Indicates non fickain diffusion and F2, F6, F7 Indicates super case II transport as release mechanism. The formulation F2 (Fa) was released 100% drug release in a 8 hrs. It is fulfil specifications for extended release tablets. The results of ANOVA of Ko values indicated that the individual and combined effect of the 3 factors is significant (P< 0.05).

Solid self‑emulsifying pellets: Solubility enhancement for oral delivery of poorly soluble BCS Class II drug

The review focused on technique of solid self-emulsifying pellets (SEPs) for solubility enhancement of poorly water soluble drug. The oral route of administration has been and still is currently the primary route of drug delivery owing to its potential advantages compared to the other routes. The solubility enhancement process of hydrophobic drugs plays a key role in the formulation development to achieve the bioavailability and therapeutic action of the drug at the target site.1 Around 40% of probe new drugs are characterized as belonging to class II in the BCS classification (poorly water soluble and highly permeable), giving rise to poor and erratic oral bioavailability. The solid SEPs system combines the advantages of liquid Self emulsifying drug delivery system with those of solid dosage form, which can overcome the limitations of liquid formulations and improve the storage stability and patient compliance. To enhance the dissolution and oral absorption of water insoluble drug selfmicroemulsifying pellets develop and evaluated. SEPs pellets showed a significant quicker redispersion rate than the dissolution rate of commercial tablets. The solid SEPs pellets might be an encouraging strategy to improve the oral absorption of Poorly water soluble drug and the extrusion–spheronization method is a feasible technology for the solidification of liquid SMEPs. Self microemulsifying drug delivery system (SEPs) as an effective bioavailability enhancement pharmaceutical technology has been widely used during the recent years and have some successful products in the market (e.g. Neoral®, Norvir® and Fortovase®).
 Keywords: Self Emulsifying Pellets, Bioavailability, Solubility, extrusion–spheronization, Biopharmaceutical Classification.

Application of hydroxypropylated crosslinked starch from the grains of Oryza sativa L. as potential disintegrant in compressed solid dosage form

Context: The modification of starch from the grains of NSICRc222 rice variety may provide a new material with enhanced disintegrating functionality in compressed solid dosage forms. Aims: To synthesize hydroxypropylated crosslinked rice starch that may possess characteristics of a good disintegrant. Methods: Starch was isolated by the wet milling method. The crosslinking was performed using trisodium trimetaphosphate as crosslinking agent, and successively hydroxypropylated by using phosphorous oxychloride. The evidences of chemical modifications were determined by FTIR, TGA, and DSC. The application of modified rice starch as a disintegrant was evaluated by determining the dissolution profile, and was compared to the performance of commercially available disintegrants. The compatibility of modified rice starch was employed using FTIR, and the stability of the formulation was subjected to an accelerated stability study. Results: The changes in infrared spectra and thermogram confirmed successful chemical modification of rice starch. Allopurinol and modified starch mixture staged from 0 to 3 months showed no significant changes in the infrared spectra, which suggest compatibility of HCR with allopurinol. The dissolution rate of allopurinol tablets at pH 1.2, pH 4.5, and pH 6.8 with various superdisintegrants were comparable to the dissolution rate that utilized hydroxypropylated crosslinked rice starch as disintegrant. The accelerated stability study showed no significant changes from 0th to 3rd month, and no degradation products were detected in the HPLC analysis. Conclusions: The chemical modification of rice starch through crosslinking and hydroxypropylation yielded a novel material comparable to the commercially available superdisintegrants.

Development and characterization of solid dispersion-based orodispersible tablets of cilnidipine

BackgroundCilnidipine, a calcium channel blocker, is the first-line drug for hypertension and belongs to Biopharmaceutics Classification System II. To mitigate its extensive first-pass metabolism and improve patient compliance, the present study was performed to develop and characterize solid dispersion-based orodispersible tablets.ResultsThe phase solubility study with polyvinyl pyrrolidone 15% has shown a 140-fold increase in solubility. X-ray diffraction and differential scanning calorimetry studies emphasized the conversion of solid dispersion from crystalline to amorphous state. Solid dispersion 3 resulted in 142-fold improvement in solubility, 96% of drug content, and percentage drug release was 71.9% at 60 min. F11 containing crospovidone (10 mg) and sodium starch glycolate (16 mg) in combination at higher concentration as super-disintegrants showed the least disintegration time of 26.6 s. In vitro dissolution results are subjected to statistical analysis and found that the formulation (F11) has shown an increased dissolution rate (88.62% at 10 min), compared to the marketed formulation (83% at 60 min).ConclusionsSolid dispersion prepared by a solvent evaporation method using PVP as a carrier can be utilized for enhancing the solubility of cilnidipine. The incorporation of super-disintegrants in combination improves the dissolution rate of orodispersible tablets. Further, the study can be substantiated by performing stability and in vivo studies in the future.Graphical

Stereomicroscope with Imaging Analysis: A Versatile Tool for Wetting, Gel Formation and Erosion Rate Determinations of Eutectic Effervescent Tablet.

Wettability, gel formation and erosion behaviors could influence the drug release pattern of solid dosage forms. Typically, these parameters are evaluated using a variety of techniques. Nonetheless, there has been no previous research on versatile tool development for evaluating several tablet characteristics with a single tool. The aim of this study was to develop the versatile tool for measuring various physical properties of eutectic effervescent tablets and also investigate the relationship between these parameters with parameters from drug dissolution. Ibuprofen (IBU)-poloxamer 407 (P407) eutectic effervescent tablets were fabricated with a direct compression method. Their wetting properties, gel formation and erosion behaviors were investigated using a stereomicroscope with imaging analysis in terms of the liquid penetration distance, gel thickness and erosion boundary diameter, respectively. In addition, the dissolution rate (k) and disintegration time of eutectic effervescent tablets in 0.1 N HCl buffer pH 1.2 were also determined. Incorporation of P407 into the IBU tablet improved the tablet wetting properties with increasing liquid penetration distance under stereoscope. CO2 liberation from effervescent agents promoted tablet surface roughness from matrix erosion. The relationship between observed physical properties and disintegration and dissolution parameters suggested that the combination of erosion by effervescent agents and gel formation by P407 had a potential influence on dissolution enhancement of the formulation. Therefore, a developed stereomicroscope with an imaging analysis technique was exhibited as an alternative versatile tool for determining the wetting properties, gel formation and erosion behaviors of pharmaceutical solid dosage forms.

Clinical investigation of the biopharmaceutical characteristics of nifurtimox tablets – Implications for quality control and application

Nifurtimox is approved in Chagas disease and has been used in endemic countries since the 1960s. Nifurtimox, available as a 120 mg tablet, is administered with food typically three times daily, and dose is adjusted for age and bodyweight. Accurately or reproducibly fragmenting the 120 mg tablet for dose adjustment in young children and those with low bodyweight is problematic. Based on the existing tablet formulation, new nifurtimox 30 mg and 120 mg tablets have been developed in a format that can be divided accurately into 15 mg and 60 mg fragments. In adults with chronic Chagas disease, we investigated whether nifurtimox bioavailability is affected by tablet dissolution rate, and whether different diets affect nifurtimox bioavailability. In an open-label, three-period cross-over study (n=36; ClinicalTrials.gov, NCT03350295), patients randomly received three 30 mg tablet formulations (slow, medium, or fast dissolution; a 4 × 30 mg dose of one formulation per period). In an open-label, four-period cross-over study (n=24; ClinicalTrials.gov, NCT03334838) patients randomly fasted or received one of three meal types (high-fat/high-calorie, low-fat, dairy-based) before ingesting nifurtimox (a 4 × 30 mg dose per period). Acceptance criteria for no difference between groups were 90% confidence intervals (CIs) of exposure ratios in the range 0.8–1.25. Nifurtimox bioavailability was unaffected by tablet dissolution kinetics. Ratios of area under the curve at final assessment (AUC(0–tlast) [90% CI]) were: fast/medium dissolution, 1.061 (0.990–1.137); slow/medium dissolution, 0.964 (0.900–1.033); fast/slow dissolution, 1.100 (1.027–1.179). Compared with a fasting state, nifurtimox bioavailability increased by 73% after a high-fat/high-calorie meal (AUC(0–tlast) ratio [90% CI], 1.732 [1.581–1.898]); smaller increases were seen with the other meal types (low-fat: 1.602 [1.462–1.755]; dairy-based: 1.340 [1.222–1.468]). Although type of diet can affect bioavailability, taking nifurtimox with food is most important.

Variation concentration effect of propyleneglycol, glycerin, and polyethyleneglycol 400 to physical properties and dissolution rate of loratadine liquisolid tablet.

This study aimed to evaluate the variation concentration effect of propyleneglycol, glycerin, and polyethyleneglycol 400 as a nonvolatile solvent on the physical properties and dissolution rate of the loratadine liquisolid tablet. The tablet was formulated into 10 formulas, where nine were liquisolid and one was conventional (CT). The concentration of propyleneglycol, glycerin, and polyethyleneglycol used in liquisolid tablets were 14, 15, and 16%. Furthermore, the mixture was evaluated based on flow properties and compressibility index. The tablet was evaluated based on hardness, friability, disintegration time, and dissolution, and the data obtained was evaluated with ANOVA or Kruskal-Wallis statistic program. The result showed that flow properties, disintegration time, and dissolution have a significant value less than 0.05. The tablet friability for all concentration solvents, hardness at 14 and 15% solvent concentration, and compressibility index at 15 and 16% have significant value more than 0.05. The 16% propyleneglycol type solvent concentration tablet has the physical properties and contains the best solution. From the result, it is reasonable to conclude that F7 is the tablet with all the physical properties and the best dissolution.