The aim of this study was to improve the chemical stability of cycloserine containing organic and inorganic compounds. Composite particles were manufactured with a 1:1 weight ratio of organic/inorganic compounds and cycloserine. The influence of organic/inorganic compounds on the stability of cycloserine was investigated under accelerated stress conditions at 60°C/75% RH for 24 hours. In addition, the properties of the composite particles were evaluated using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and the dissolution of the drug was assessed by preparing it as a hard capsule. Among the organic and inorganic compounds investigated, calcium hydroxide most improved the stability of cycloserine under accelerated stress conditions (53.3 ± 2.2% vs 1.7 ± 0.2%). DSC results confirmed the compatibility between calcium hydroxide and the cycloserine, and SEM results confirmed that it was evenly distributed around the cycloserine. Calcium hydroxide also showed more than 90% cycloserine dissolution within 15 minutes. Therefore, the calcium hydroxide and cycloserine composite particles may be candidates for cycloserine oral pharmaceuticals with enhanced drug stability.

This study aims to prepare a colloidal silica-containing powder to enhance the solubility and dissolution rate of rivaroxaban using a self-nanoemulsifying drug delivery system (SNEDDS). We investigate the impact of colloidal silica on a nanoemulsion system for preparing powdered SNEDDS. The liquid SNEDDS comprises 30/20/50 (w/w/w) Peceol/ Cremophor RH40/Tween 80, which results in the formation of the smallest droplets. Three powdered SNEDDS formulations are prepared by suspending the liquid SNEDDS formulation using colloidal silica and spray drying. The powdered SNEDDS prepared with liquid SNEDDS and colloidal silica at a ratio of 1/0.5 (w/w) exhibits the highest water solubility (0.94 ± 0.62 vs. 26.70 ± 1.81 μg/mL) and dissolution rate (38.4 ± 3.6 vs. 85.5 ± 3.4%, 45 min) when compared to the drug alone. Morphologically, the liquid SNEDDS is adsorbed onto colloidal silica and forms smaller particles. In conclusion, an SNEDDS containing rivaroxaban, prepared using colloidal silica, facilitates the creation of a nanoemulsion and enhances the water solubility of rivaroxaban. Accordingly, this technology holds significant potential for commercialization.

The purpose of this study is to develop and evaluate amorphous spray-dried microparticles (SDM) containing levosulpiride to increase its solubility. SDM are prepared via solvent evaporation using polyvinylpyrrolidone (PVP) as the water-soluble polymer and Cremophor RH40 as the surfactant. The SDM is prepared by varying the amounts of PVP and Cremophor RH40, and its physicochemical properties, solubility, and dissolution are confirmed. All levosulpiride-loaded SDMs converted the crystalline drug into an amorphous form, significantly improving drug solubility and dissolution compared with the drug alone. SDM consisting of drug/PVP/Cremophor RH40 in a weight ratio of 5:10:3, with increased solubility (720 ± 36 vs. 1822 ± 51 μg/mL) and dissolution rate (10.3 ± 2.2 vs. 92.6 ± 6.0%) compared with drug alone, shows potential as a commercial drug for improved oral bioavailability of levosulpiride.

The objective of this study is to assess the impact of spray drying conditions on medium-chain triglyceride (MCT) loading, solubility, and release of an MCT-loaded solid self-emulsifying system in a water-insoluble oily substance. MCT-loaded solid self-emulsifying systems are prepared by spray drying with SDS and calcium silicate. The effects of inlet temperature (60, 80, or 100oC) and feed solution composition (0, 10, 50, 90, or 100% ethanol) on physicochemical properties of MCT-loaded solid self-emulsifying systems are studied. The inlet temperature significantly affects the water solubility of MCT. Moreover, the feed solution composition significantly affects water solubility, release rate, and MCT loading. The MCT-loaded solid self-emulsifying system obtained at 60oC using 90% ethanol feed solution shows the best physicochemical properties among the synthesized products and exhibits better water solubility (4.43 ± 0.44 vs. 0 μg/mL) and release (94.4 ± 1.6 vs. 32.8 ± 7.4%, 60 min) than a commercial product. Furthermore, the MCT-loaded solid self-emulsifying system shows an excellent emulsion droplet size (approximately 230 nm).

The purpose of this study is to optimize the powder formulation and manufacturing conditions for the solidification of an extract of the herb Bangpungtongseong-san (BPTS). To develop BPTS-loaded particles for the tablet dosage form, various BPTS-loaded particles composed of BPTS, dextrin, microcrystalline cellulose (MCC), silicon dioxide, ethanol, and water are prepared using spray-drying and high shear granulation (high-speed mixing). Their physical properties are evaluated using scanning electron microscopy and measurements of the angle of repose, Hausner ratio, Carr’s index, hardness, and disintegration time. The optimal BPTS-loaded particles exhibit improved flowability and compressibility. In particular, the BPTS-loaded particles containing silicon dioxide show significantly improved flowability and compressibility (the angle of repose, Hausner ratio, and Carr’s index are 35.27 ± 0.58°, 1.18 ± 0.06, and 15.67 ± 1.68%, respectively), hardness (18.97 ± 1.00 KP), and disintegration time (17.60 ± 1.50 min) compared to those without silicon dioxide. Therefore, this study suggests that particles prepared by high-speed mixing can be used to greatly improve the flowability and compressibility of BPTS using MCC and silicon dioxide.

To develop Gastrodia elata (GE)-loaded particles for herbal extract dosage forms, various GE-loaded particles containing dextrin, isomalt, maltodextrin, and silicon dioxide as solidifying carriers in the GE water extract are prepared using the spray drying method. Their physical properties are evaluated using the repose angle, Hausner ratio, Carr's index, weight increase rate at 40oC/75% RH condition, and scanning electron microscopy (SEM). Particles made of dextrin improve the fluidity, compressibility, and water stability. In addition, 2% silicon dioxide increases the fluidity and moisture stability. The best flowability and compressibility of GE-loaded particles are observed with TP, dextrin, and silicon dioxide amounts in the ratio of 6/4/0.2 (34.29 ± 2.86°, 1.48 ± 0.03, and 38.29 ± 2.39%, repose angle, Hausner Ratio, and Carr’s index, respectively) and moisture stability with a 2% weight increase rate for 14 h at 40oC/75% RH condition. Therefore, our results suggest that the particles prepared by the spray drying method with dextrin and 2% silicon dioxide can be used as powerful particles to improve the flowability, compressibility, and moisture stability of GE.

To develop Taraxacum platycarpum extract (TP)-loaded particles for tablet dosage form, various TP-loaded particles composed of TP, dextrin, microcrystalline cellulose (MCC), silicon dioxide, ethanol, and water are prepared using a spray-drying method and fluid-bed-drying method. Their physical properties are evaluated using angle of repose, Hausner ratio, Carr’s index, hardness, disintegrant time, and scanning electron microscopy. Optimal TP-loaded particles improve flowability and compressibility. Furthermore, 2% silicon dioxide gives increased flowability and compressibility. The formula of TP-loaded fluid-bed-drying particles at a TP/MCC/silicon-dioxide amount of 5/5/0.2 improves the angle of repose, Hausner ratio, Carr’s index, hardness, and disintegrant time as compared with the TP-loaded spray-drying particles. The TP-loaded fluid-bed-drying particles considerably improve flowability and compressibility (35.10° vs. 40.3°, 0.97 vs. 1.17, and 18.97% vs. 28.97% for the angle of repose, Hausner ratio, and Carr’s index, respectively), hardness (11.34 vs. 4.7 KP), and disintegrant time (7.4 vs. 10.4 min) as compared with the TP-loaded spray-drying particles. Thus, the results suggest that these fluid-bed-drying particles with MCC and silicon dioxide can be used as powerful particles to improve the flowability and compressibility of the TP.