The purpose of this research was to develop an inclusion complex of meloxicam (MEL)/β-cyclodextrin (β-CD) incorporated into an orally disintegrating tablet (ODT), using statistical analysis to optimize the ODT formulation based on a quality by design (QbD) approach. MEL/β-CD complexation was performed by kneading, co-precipitation and spray drying methods under different molar ratios. Fourier transform infrared spectroscopy, X-ray diffraction and thermal analysis were utilized to evaluate the complexes. A central composite design (α = 2) was applied to optimize and assess the influence of Primojel, Primellose and crushing strength (CS) as independent variables on tablet friability, disintegration behavior, wicking properties and drug release. The spray drying method induced formation of an amorphous complex and enhanced solubility and drug release of MEL. Furthermore, a QbD-based statistical analysis was successfully utilized to optimize the ODT formulation. Primojel, Primellose and CS showed unique main effects and interactions at different levels. CS was the dominant factor, affecting friability, disintegration behavior and drug release, while wicking properties were affected by Primojel and its interaction with Primellose. Therefore, according to the overlay plot, CS was dominant factor in determining the optimum region based on a QbD approach.

Solidification of liquid self-nano emulsifying drug delivery system (SNEDDS) formulation is required to enhance the feasibility and flexibility for further formulation processes. This study purposed to compare the soluble and insoluble carriers namely mannitol and fumed silica, respectively on the nano-emulsion formation and physical properties. The optimized SNEDDS formulation comprising of virgin olive oil, Tween 80, and PEG 400; and meloxicam was impregnated into solid carriers e.g. mannitol and fumed silica using a freeze-drying method. The physical mixture was carried out to compare the aforementioned method. Vibrational spectroscopy, thermal analysis, and morphological characteristic, droplet size and distribution, and drug release were performed to characterize the solid SNEDDS (S-SNEDDS). The result showed that crystallization of meloxicam did not observe in the S-SNEDDS formulations, which confirmed by the vibrational spectroscopy and thermal analysis. The morphological characteristic of S-SNEDDS was similar to the native carriers. The soluble carrier did not affect the formation of the nano-emulsion compared to the insoluble carrier. In addition, the S-SNEDDS enhanced the drug release of meloxicam up to 3-4 folds increment.

Purpose: Recently, a self-nanoemulsifying drug delivery system (SNEDDS) has shown great improvement in the enhancement of drug bioavailability. The selection of appropriate compositions in the SNEDDS formulation is the fundamental step towards developing a successful formulation. This study sought to evaluate the effectiveness of fractional factorial design (FFD) in the selection and screening of a SNEDDS composition. Furthermore, the most efficient FFD approach would be applied to the selection of SNEDDS components. Methods: The types of oil, surfactant, co-surfactant, and their concentrations were selected as factors. 26 full factorial design (FD) (64 runs), 26-1 FFD (32 runs), 26-2 FFD (16 runs), and 26-3 FFD (8 runs) were compared to the main effect contributions of each design. Ca-pitavastatin (Ca-PVT) was used as a drug model. Screening parameters, such as transmittance, emulsification time, and drug load, were selected as responses followed by particle size along with zeta potential for optimized formulation. Results: The results indicated that the patterns of 26 full FD and 26-1 for both main effects and interactions were similar. 26-3 FFD lacked adequate precision when used for screening owing to the limitation of design points. In addition, capryol, Tween 80, and transcutol P were selected to be developed in a SNEDDS formulation with a particle size of 69.7± 5.3 nm along with a zeta potential of 33.4± 2.1 mV. Conclusion: Herein, 26-2 FFD was chosen as the most efficient and adequate design for the selection and screening of SNEDDS composition. The optimized formulation fulfilled the requirement of a quality target profile of a nanoemulsion.

ABSTRACT:In this study, central composite design (CCD) was used for optimization of high performance liquid chromatographic (HPLC) method for simultaneous analysis of curcumin (CUR) and demethoxycurcumin (DMC) in tablets containing Curcuma extract. Separation of CUR and DMC was performed using X-Bridge C18 column (250 x 4.6 mm i.d; 5 µm). Four factors that were investigated include the concentration of acetic acid (X1), ratio of acetic acid (X2), flow rate of mobile phase (X3) and column temperature (X4). Based on responses obtained (retention time, peak area, resolution and tailing factor), the optimum condition selected was X1 = 3.00%, X2 = 51%, X3 = 1.05 mL/min and X4 = 45oC. This HPLC condition was validated by assessing several validation parameters including system suitability test, selectivity, linearity, precision, accuracy and robustness according to International Conference Harmonization (ICH). All validation parameters meet the acceptance criteria set by ICH. The validated method was successfully used for analysis of CUR and DMC in tablets containing Curcuma extract. CCD was effective means in optimization of HPLC for analysis of CUR and DMC in pharmaceutical formulation.