Dissolution Test Research Articles

Acid-Neutralizing Omeprazole Formulation for Rapid Release and Absorption

Background/Objectives: Omeprazole undergoes degradation in acidic conditions, which makes it unstable in low pHs found in the gastric environment. The vast majority of already marketed omeprazole formulations use enteric polymer coatings to protect the drug from exposure to acidic pH in the stomach, allowing for drug release in the small intestine where the pH is higher. This study aimed to explore the technical aspects of using stomach acid neutralizers as an alternative to polymeric coatings for omeprazole. Methods: After evaluating various neutralizers, magnesium oxide and sodium bicarbonate were chosen to be incorporated into capsules containing omeprazole, which then underwent in vitro dissolution testing to assess their ability to maintain optimal pH levels and ensure appropriate dissolution kinetics. Hygroscopicity and chemical stability of the selected formulation were tested to prove pharmaceutical quality of the product. An in vivo pharmacokinetic study was conducted to demonstrate the efficacy of the omeprazole–sodium bicarbonate formulation in providing faster absorption in humans. Results: Sodium bicarbonate was selected as the most suitable antacid for ensuring omeprazole stabilization. Its quantity was optimized to effectively neutralize stomach acid, facilitating the rapid release and absorption of omeprazole. In vitro studies demonstrated the ability of the formulation to neutralize gastric acid within five minutes. In vivo studies indicated that maximum concentrations of omeprazole were achieved within half an hour. The product met the requirements of pharmaceutical quality. Conclusions: An easily manufacturable, fast-absorbing oral formulation was developed as an alternative to enteric-coated omeprazole.

Sustainability assessment of the micellar optimized HPLC method for concomitant quantification of a common triple regimen for cardiovascular disorders: application to marketed formulations and in vitro dissolution testing.

Hypertension and dyslipidemia are two of the most frequently co-occurring cardiovascular risk factors. The combined regimen of hydrochlorothiazide (HCTZ), rosuvastatin (ROS), and losartan (LOS) helped in the successful management of both conditions. This work's objective is to develop an eco-friendly, sensitive, simple, and reliable chromatographic method for the simultaneous estimation of HCTZ, ROS, and the LOS ternary mixture in their pure form, and pharmaceutical formulations. Utilizing sodium dodecyl sulphate (SDS) in combination with polyoxyethylene-23-lauryl ether (Brij-35) could be a greener option with minimal environmental impact in liquid chromatographic separation techniques. Therefore, a micellar HPLC protocol was optimized and validated employing a mobile phase comprising a mixture of micelles of SDS (0.15 mol L-1) and Brij-35 (0.03 mol L-1) with 0.01 M monobasic potassium phosphate buffer, pH 3.5. The cited drugs were detected at 230 nm within five minutes, using a symmetry RP-C18 column, an isocratic elution mode, and a flow speed of 1 mL min-1. Method validation was successfully performed as stated by ICH. The suggested HPLC approach was effectively applied to determine the mentioned drugs in three pharmaceutical preparations. It was also employed for monitoring their in vitro release pattern using two innovator tablet formulations, applying the USFDA guidelines. The applied procedure was evaluated and compared with previously published HPLC approaches using various metrics, including the Eco-Scale Scoring method (AES), the Green Analytical Procedure Index (GAPI), and the Analytical Greenness Calculator (AGREE) for greenness, the most current Blue Applicability Grade Index (BAGI) for blueness, and the more inclusive RGB 12 algorism for whiteness assessment.

A comparative study of two data-driven modeling approaches to predict drug release from ER matrix tablets.

The pharmaceutical industry is striving to develop innovative and promising tools, increasingly embracing new data-driven approaches, to understand, improve and accelerate the drug product development process. While extended release (ER) oral formulations offer a number of advantages, including maintenance of therapeutic drug levels, a reduction in dosing frequency, and minimization of side effects, achieving consistent drug release profiles remains a significant challenge. As a critical attribute for drug absorption into systemic circulation, in vitro dissolution testing represents a time-consuming and complex method for the evaluation of such formulations. The main objective of this study was to develop a model for predicting drug dissolution in the quality by design (QbD)-based development of ER oral hydrophilic matrix tablets comprising polyethylene oxide (PEO). Two main modeling approaches are conducted and compared: (i) model screening to fit and compare multiple predictive machine learning (ML) models and then deploy the best model, in this case, artificial neural networks (ANN), and (ii) functional data analysis (FDA) combined with the design of experiments (DoE) that fit a smoothing model to each dissolution curve as a continuous function. A dataset comprising 91 ER matrix tablet formulations was analyzed, with the dissolution data split into training, validation, and test sets (70%, 20%, and 10%, respectively). The results demonstrated that both ANN and functional DoE (FDOE) models achieved high similarity with the experimental dissolution profiles, as indicated by f2 values ranging from 48 to 88 for the FDOE and 52 to 88 for ANN. This work highlights the potential of integrating advanced data-driven modeling techniques into ER drug development to enhance dissolution prediction accuracy and streamline the formulation process, thus reducing time and costs.

Formulation of Cefdinir Ternary Solid Dispersion and Stability Study under Harsh Conditions

Cefdinir (CEF) is classified as a third-generation cephalosporin within class IV of the Biopharmaceutical Classification System (BCS). Cefdinir has low solubility and permeability, which may reduce oral bioavailability. The aim of this research was the preparation of cefdinir ternary solid dispersion in order to enhance its solubility. Then, after evaluating this ternary SD, investigate its stability under harsh conditions. In addition, formulation and evaluation of CEF ternary SD as capsule dosage form. The ternary SD is prepared by the solvent evaporation method using CEF, curcumin, and polyvinylpyrrolidone k30 in a weight ratio of 1:1:1. The ternary SD is subject to evaluation using Differential Scanning Calorimetry (DSC), Powder X-ray Diffractometry (PXRD), and Fourier Transform Infrared Spectroscopy (FTIR), saturated solubility, release, antibacterial activity, and a two months stability study under conditions of 40 ºC and 75% relative humidity. Then, six different capsule formulas were prepared using different excipients; each formula contained 300 mg of CEF. The capsule formulas were subjected to pre-formulation and capsule evaluation tests, which included weight variation, drug content, disintegration time, and In-vitro dissolution tests. The selected optimum capsule formula was subjected to further antibacterial activity test. Evaluation of ternary SD showed that, the system is totally amorphous with enhanced dissolution, saturated solubility, and antibacterial activity compared to pure CEF. Stability studies showed that, ternary SD remains amorphous after two months. Compared to commercial capsules (Sefarin® 300 mg) and other formulas, the F6 formula released 90% of CEF in 30 min. Antibacterial activity test results showed that the F6 formula was active against Staphylococcus aureus and Proteus vulgaris bacterial isolate. This research concludes that CEF solubility, antibacterial activity enhancement, and stability insurance could be obtained by preparing CEF ternary SD. All the ternary SD prepared capsule formulas showed enhancements in release compared to commercial capsules.

Disintegration Mechanism of Coal-Bearing Soil Based on Granularity Entropy and Water-Air Two-Phase Flow.

Coal-bearing soils (CBS), products of coal-bearing strata weathering, are particularly prone to disintegration due to the effects of dry-wet cycles. Static water disintegration tests, environmental scanning electron microscopy (ESEM), and mineral chemical composition analyses were conducted on CBS. The disintegration evolution of CBS is characterized by granularity entropy and is analyzed concerning the disintegration ratio. Furthermore, the disintegration mechanism is examined based on the water-air two-phase flow (WTF) and mineral chemical reactions. Results show a significant exponential relationship between the standard basic entropy (A) and disintegration ratio (DR), where the disintegration ratio decreases as the standard basic entropy increases. As the number of dry-wet cycles increases, A initially decreases rapidly before stabilizing, mirroring the variation pattern of the particle size distribution curve and its derived indicators. Illite produces significant short-range hydration repulsion, leading to the formation of additional cracks in CBS. WTF significantly influences disintegration; water intrusion increases air pressure, and the subsequent pressure release plays a critical role in damaging soil structure. These findings are significant for the safety and protection of CBS slope engineering.

Silybin Cocrystals with Improved Solubility and Bioavailability.

Backgroud/Objectives: Silymarin, an extract from milk thistle, is widely recognized for its therapeutic potential in treating liver disorders. However, its clinical utility is limited by the poor solubility and low bioavailability of its key active ingredient, Silybin. In this study, we sought to address this issue through the development of a novel cocrystal of Silyin. Methods: Silybin-L-proline cocrystal was synthesized and the physicochemical properties of the cocrystal were characterized by PXRD, TGA, DSC, and FTIR. Dissolution tests were conducted in various pH solutions, and the impact of precipitation inhibitors was evaluated. Furthermore, pharmacokinetic study in rats were performed to assess the bioavailability. Results: The dissolution studies demonstrated that the cocrystal has a significant improvement in dissolution performance, particularly in acidic environments. Furthermore, the use of precipitation inhibitors, such as PVP, prolonged the supersaturation period for adequate absorption. Pharmacokinetic studies in rats revealed that the cocrystal exhibited a 16-fold increase in bioavailability compared to the raw Silybin extract, outperforming the commercial Silybin-phosphatidylcholine complex. Conclusions: The Silybin-L-proline cocrystal significantly enhances dissolution and bioavailability, indicating its potential to improve the therapeutic efficacy of Silybin in clinical applications.

Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design

Itraconazole (ITZ) is a broad-spectrum triazole antifungal agent suitable for the treatment of superficial and systemic mycoses. This study aimed to formulate, characterize, and evaluate the in vitro antifungal performance of single-jet electrospun itraconazole-loaded polyvinylpyrrolidone-based fibers. Fibrous mats were prepared under the following experimental conditions: 10, 12.5, and 15 cm needle–collector distance, 20 kV tension, and 1, 1.5, and 2 mL/hour flow rate. The fibers were characterized by SEM, DSC, FTIR, assays, disintegration tests, dissolution tests, and in vitro antifungal activity. Using a 22 factorial design, the effects of preparation variables on the characteristics of the fibrous sheets were described. The electrospinning process led to smooth-surfaced, randomly oriented, and bead-free fibers. The average fiber diameter ranged from 887 nm to 1175 nm. The scanning calorimetry of pure ITZ revealed a sharp endothermic melting point at a temperature of 170 °C, not present in the curves of the fibers. After 60 min, between 70 and 100% of ITZ was released. The antifungal assay revealed that the fibers inhibited the growth of Candida albicans and Candida parapyilosis. The obtained fiber mats prepared from the hydrophilic polymer presented almost instantaneous disintegration, with potential applications for rapid antifungal delivery in oral or topical pharmaceutical form.

Prednomel Preparation Utilizing Novel Method

The World Anti-Doping Agency (WADA) lists Prednisolone as an anti-inflammatory steroidal medication that belongs to the glucocorticoid class. Due to their strong immunosuppressive and anti-inflammatory qualities, glucocorticoids (GC) are frequently used to treat acute multiple sclerosis (MS) relapses. According to pharmacopeia, every tablet passed the weight variation and hardness, thickness, friability, disintegration, and dissolution tests. This research aims to create quality control parameter prediction models. The following characteristics were evaluated: assay, dissolution, hardness, thickness, friability, and disintegration.

Impact of Simulated Gastrointestinal Fluid: Viscosity, Surface Tension, and pH on the Dissolution and Rheology Assessment of Viscosity of Two Commercial Candesartan Cilexetil Products.

The aim of this study was to ivnestigate the effect of simulated gastrointestinal viscosity, surface tension, and pH on the dissolution rate of two commercial candesartan cilexetil (CC) products. In vitro dissolution of two commercial CC products and immediate release of 16 mg of CC were applied under two conditions: (1) the requirements of the United States Pharmacopeia (USP) and (2) conditions physiologically related to the gastrointestinal tract mimicking viscous food intake. The solubility of CC in different simulation fluids was also measured. The dissolution media's viscosity, surface tension, and pH were also measured. The viscosity of the gel layer was measured during CC dissolution. The CC dissolution rate was highest in the USP medium. It was found that the media type affected CC dissolution. The non-USP media exhibited a slower dissolution rate than the USP specification. The highest viscosity media lowered the dissolution rate in one of the CC products. Acidic pH showed a significant decrease in dissolution for both CC products. The solubility of CC was affected by solvent type (p value < 0.001). Higher viscosity media slow the dissolution rate of a product, where a gel layer forms on the tablet surface.The results show variation in the dissolution media. This may reveal differences in the dissolution rates of the same drug in different products and media. Considering, viscosity's effect on dissolution might improve patient outcomes when treated with different products.

Selection of In Vivo Relevant Dissolution Test Parameters for the Development of Cannabidiol Formulations with Enhanced Oral Bioavailability.

Background: Cannabidiol (CBD) shows interesting therapeutic properties but has yet to demonstrate its full potential in clinical trials partly due to its low solubility in physiologic media. Two different formulations of CBD (amorphous and lipid-based) have been optimized and enable an increase in bioavailability in piglets. In vivo studies are time-consuming, costly and life-threatening. Therefore, we need to develop in vitro tests that can predict what will happen in vivo. Methods: Comparisons in terms of dissolution were made especially by using different media (FaSSGF, FaSSIF, FeSSIF, HCl 0.1N with or without SLS, phosphate buffer pH 6.8 with or without SLS) and different conditions (sink or non-sink conditions). These in vitro results were confronted with in vivo results to select the most appropriate dissolution test conditions. Results: The importance of the presence of surfactants to enable solubilization of CBD was demonstrated. Neutral media enabled a relatively good prediction of the extent of absorption observed in vivo, whereas the rate of absorption was more complicated to predict. Conclusions: FeSSIF media, and FaSSIF sink media to a lesser extent, were the only compositions enabling predictions of both extent and rate, indicating that emulsification is possibly a major contributor to the in vivo availability of the drug.

Unveiling the potential of pullulan in enhancing ketoprofen release from PHBV filaments.

In this study, sustainable poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) and pullulan (PUL)/PHBV filaments were prepared with ketoprofen for scaffold preparation. The research aimed evaluate the influence of pullulan in the filament properties, such as thermal, morphological, and biological behavior. Hansen parameters demonstrated the difference in the miscibility of the polymers and drug in the blend. This difference in solubility contributed to thermal stabilization, and reduced the crystallinity of the blend, observing a reduction in crystalline peak at 30.82° (002). The morphology change was observed by SEM images, in which ketoprofen appears to smooth and homogenize the filament surface. Cytotoxicity tests on osteoblast cells confirmed that all samples were biocompatible, and the presence of ketoprofen was comparable to the control group. Importantly, the in vitro release of ketoprofen revealed that the presence of pullulan increased the cumulative release of ketoprofen, from 0.1% to 36%, within 240min of the dissolution test. This highlights the crucial role of pullulan in fine-tuning drug release. These findings underscore the potential of these materials for bone regeneration applications, combining the cytotoxic and cell adhesion properties of PHBV with the osteoblasts, and offering precise control over the degradation process and drug release through the incorporation of pullulan.

Characterization of Alpha Mangostin Loaded-Mesoporous Silica Nanoparticle and the Impact on Dissolution and Physical Stability.

Improving drug solubility is crucial in formulating poorly water-soluble drugs, especially for oral administration. The incorporation of drugs into mesoporous silica nanoparticles (MSN) is widely used in the pharmaceutical industry to improve physical stability and solubility. Therefore, this study aimed to elucidate the mechanism of poorly water-soluble drugs within MSN, as well as evaluate the impact on the dissolution and physical stability. Alpha mangostin (AM) was adopted as a model of a poorly water-soluble drug, while MSN with the pore size of 45 Å (MSN45) and 120 Å (MSN120) were used as Mesoporous materials. AM-loaded MSN (AM/MSN45 and AM/MSN120) was prepared by solvent evaporation method. The amorphization of AM/MSN45 and AM/MSN120 was confirmed by the halo pattern observed in the powder X-ray diffraction pattern and the absence of the melting peak and the glass transition of AM in the DSC curves. This signified the successful incorporation of AM into MSN. FT-IR measurements suggested the formation of hydrogen bond interaction between the carbonyl group of AM and the silica surface of MSN. In the dissolution test, the presence of the AM within MSN improved the dissolution rate and generated the supersaturation of AM. However, the difference of pores size of MSN could affect the dissolution profile of AM within MSN. Additionally, it retained the X-ray halo patterns after 30 d of storage at 25 oC and 0% RH. In conclusion, AM-loaded mesoporous silica significantly improved the dissolution and physical stability.

Preparation and characterization of andrographolide nano-cocrystals using hummer acoustic resonance technology.

Andrographolide (AG) is a diterpene lactone with significant anti-inflammatory and antitumor activities. However, the poor water solubility limits its clinical application. An andrographolide-salicylic acid (AG-SLA) nano-cocrystal delivery system was rapidly developed using hummer acoustic resonance (HAR) technology in this research. The formulation of the AG-SLA nano-cocrystal suspension and the process parameters for HAR technology were optimized in a high-throughput manner, with SDS-Tween 80 as the optimal composite stabilizer. Nano-cocrystal suspension of AG-SLA with an average particle size of 190 nm were successfully prepared, and then the optimal formulation were tenfold scaled up. Freeze-drying was adopted to solidify the nano-cocrystal and improve its stability. Various analytical techniques were used to characterize the particle size and solid state of the nano-cocrystals. The high-energy input from the HAR instrument induced partial amorphization of the nano-cocrystals, as confirmed by PXRD and DSC analyses. Saturation solubility experiments demonstrated that the solubility in pH 1.2 hydrochloric acid buffer and pH 6.8 phosphate buffer increased by 5.74 times and 6.82 times, respectively, compared to raw AG. In vitro dissolution tests indicated that the cumulative release over 120min in pH 1.2 hydrochloric acid buffer and pH 6.8 phosphate buffer increased by 1.60 times and 1.88 times, respectively, compared to raw AG.

Disintegration characteristics of undisturbed loess in response to train vibration frequency

AbstractDisintegration fragments the loess body, causing erosion and the emergence of significant geohazards. The impact of vibrations on soil disintegration has been slightly documented; however, the contribution and mechanism of train vibration frequency in the disintegration of undisturbed loess remain unclear. In this study, train vibrations were monitored in situ, and the resulting vibrational parameters were used in loess disintegration tests using a customised vibration‐disintegration apparatus. The changes in the meso‐parameters of the disintegrated loess and aqueous solutions were quantified, and the microstructural differences in the residual loess after disintegration were compared under non‐vibrating and vibrating conditions. The results revealed that train vibrations in the loess progressively diminished with increasing distance from the track, with dominant vibration frequencies ranging from 17 to 49 Hz. Increasing the vibration frequency accelerated loess disintegration and enhanced the dispersion of the disintegrated fragments. Notably, the acceleration effect of disintegration was particularly pronounced in the early stages of increasing vibration frequency, and it tended to plateau above 15 Hz. The relationship between the vibration frequency and disintegration velocity (DV) of loess influenced by the initial water content can be expressed as a power function with variables. Vibrations accelerate loess disintegration primarily attributed to repetitive particle displacement and the vibrations of free water in the pores which lead to frictional damage to the weakly cemented structure and pore expansion. Higher vibration frequencies generate greater inertial forces and facilitate more frequent particle jumps, allowing the loess to reach the disintegration threshold conditions more readily than at lower frequencies. These findings provide theoretical value for the prevention and mitigation of water‐induced loess geohazards and land degradation in vibrating environments.

A review on current updates on drug dissolution eplerenone testing for immediate relese oraldosage forms

Immediate-release oral dosage forms, also known as IR dosage forms, are widely favoured for medication delivery due to their rapid dissolution rate. This characteristic enables the medication to quickly enter the bloodstream, offering swift relief to patients. In formulation development, dissolution is a critical factor, providing essential insights for quality control. In vitro dissolution tests-a laboratory method simulating the medication's dissolution in the body—plays a key role across various stages of drug development. From a regulatory standpoint, validating dissolution enhances the review process for preclinical and clinical data. In certain situations, dissolution test results may also be utilized to assess the biopharmaceutical impact of product modifications. Such testing ensures that medications are not only effective but also safe and dependable for patients.

Berberine nanostructured lipid carriers by ultrasonication technique: initial study for skin and oral administration

Abstract Berberine (BBR), a natural bioactive ingredient from Eastern nations, has low solubility and permeability that limits its applications. Hence, berberine nanostructured lipid carriers (BBR-NLCs) were fabricated to improve the drug therapeutic effectiveness. Glycerol monostearate, stearic acid and oleic acid were chosen for lipid base whereas Pluronic F127, Span 80, and Transcutol-P were used as the surfactant and co-surfactant. BBR-NLCs had an average particle size of 82 nm, zeta potential of −32 mV, and narrow size distribution (PDI approximately 0.2), prepared with probe ultrasonication at 490 W in 15 min. In addition, BBR-NLCs prepared at optimized conditions showed around 92% of encapsulation efficiency with drug loading over 5.5%. NLCs presented sustained released through mouse skin, dialysis membrane in Franz cell model, and oral dissolution test, compared with free drug over 24 h. Moreover, blank NLCs even increased the cell viability of HaCaT and HEK293T cells at lower concentrations. NLCs significantly enabled higher interactive BBR quantity with investigated cells. Therefore, BBR-NLCs could be considered as a potential nanocarrier for improved bioavailability of this therapeutic agent.

Enteric Coated Pellets with Lactoferrin for Oral Delivery: Improved Shelf Life of the Product.

Lactoferrin (Lf), a multifunctional iron-binding protein, has considerable potential for use as an active ingredient in food supplements due to its numerous positive effects on health. As Lf is prone to degradation, we aimed to develop a formulation that would ensure sufficient stability of Lf in the gastrointestinal tract and during product storage. A simple, efficient, and well-established technology that has potential for industrial production was used for the double-coating of neutral pellet cores with an Lf layer and a protective enteric coating. The encapsulation efficiency was 85%, which is among the highest compared to other reported Lf formulations. The results of the dissolution tests performed indicated effective protection of Lf from gastric digestion. A comprehensive stability study showed that the stability was similar regardless of the neutral pellet core used, while a significant influence of temperature, moisture, product composition, and packaging on the stability of Lf were observed, and were therefore considered in the development of the final product. The experimentally determined shelf life is extended from 15 to almost 30 months if the product is stored in a refrigerator instead of at room temperature, which ensures the commercial applicability of the product. We successfully transferred a technology commonly used for small molecules to a protein-containing product, effectively protected it from the destructive effects of gastric juice, and achieved an acceptable shelf life.

Development and Characterization of Trihexyphenidyl Orodispersible Minitablets: A Challenge to Fill the Therapeutic Gap in Neuropediatrics.

Background: Trihexyphenidyl (THP) has been widely used for over three decades as pediatric pharmacotherapy in patients affected by segmental and generalized dystonia. In order to achieve effective and safe pharmacotherapy for this population, new formulations are needed. Objective: The aim of this work is the development of trihexyphenidyl orodispersible minitablets (ODMTs) for pediatric use. Methods: Six different excipients were tested as diluents. The properties of powder mixtures were evaluated before direct compression and pharmacotechnical tests were performed on the final formulation. The determination of the API content, uniformity of dosage, and physicochemical stability studies were analyzed by an HPLC-UV method. Results: The developed ODMTs met pharmacopeia specifications for content, hardness, friability, disintegration, and dissolution tests. The physicochemical stability study performed over 18 months shows that API content remains within 90.0-110.0% at least for this period. Conclusions: These ODMTs will allow efficient, safe, and high-quality pharmacotherapy.

Selective Laser Sintering 3D Printing of Carvedilol Tablets: Enhancing Dissolution Through Amorphization.

Selective laser sintering (SLS) is one of the most promising 3D printing techniques for pharmaceutical applications as it offers numerous advantages, such as suitability to work with already approved pharmaceutical excipients, the elimination of solvents, and the ability to produce fast-dissolving, porous dosage forms with high drug loading. When the powder mixture is exposed to elevated temperatures during SLS printing, the active ingredients can be converted from the crystalline to the amorphous state, which can be used as a strategy to improve the dissolution rate and bioavailability of poorly soluble drugs. This study investigates the potential application of SLS 3D printing for the fabrication of tablets containing the poorly soluble drug carvedilol with the aim of improving the dissolution rate of the drug by forming an amorphous form through the printing process. Using SLS 3D printing, eight tablet formulations were produced using two different powder mixtures and four combinations of experimental conditions, followed by physicochemical characterization and dissolution testing. Physicochemical characterization revealed that at least partial amorphization of carvedilol occurred during the printing process. Although variations in process parameters were minimal, higher temperatures in combination with lower laser speeds appeared to facilitate a greater degree of amorphization. Ultimately, the partial conversion to the amorphous form significantly improved the dissolution of carvedilol compared to its pure crystalline form. Obtained results suggest that the SLS 3D printing technique can be effectively used to convert poorly water-soluble drugs to their amorphous state, thereby improving solubility and bioavailability.

Enhanced Oral Absorption and Bioavailability of Ivermectin Through Amorphous Solid Dispersion Techniques

The purpose of this study was to develop a high-loading amorphous solid dispersion (ASD) of ivermectin to significantly enhance its oral absorption and bioavailability. Using a solvent method, we formulated a novel ternary ASD with polyvinylpyrrolidone PVPK30 and Poloxamer 188 (P188) in a 1:0.5:1.5 ratio of drug to PVPK30 to P188. We characterized the physicochemical properties of five ASD formulations through in vitro dissolution tests. The selected formulation, SD3, was further assessed using X-ray powder diffraction, scanning electron microscopy, differential scanning calorimetry, and pharmacokinetic studies in rats. Notably, SD3 enhanced drug loading more than 30-fold compared to commercial tablets. SD3 exhibited significantly faster dissolution rates and maintained an amorphous state that remained stable after two months of storage at 4°C. Pharmacokinetic analysis at a 20 mg/kg oral dose in rats showed that SD3 achieved the highest maximum concentration (Cmax), plasma exposure (AUC), and oral bioavailability compared to the pure drug and commercial tablets. The assessment of the oral absorption rate constant (Ka) revealed an increased Ka and intestinal permeability through this ASD, elucidating the possible mechanism behind these improvements.