The dissolution property of raloxifene HCl solid dispersion using hydroxypropyl methylcellulose

Oh, Min; Shim, Jung Bo; Yoo, Hai-Soo; Lee, Ga Young; Jo, Hansu; Jeong, Sang Ho; Yuk, Soon Hong; Lee, Dongwon; Khang, Gilson

doi:10.1007/s13233-012-0127-x

Cited by 15 publications

(4 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Approximately 30-60% of the RLX powder was dissolved in 110 min, and the cumulative drug dissolution was in the order of SGF (60.8%) > water (46.9%) > SIF (30.2%). The dissolution profiles of RLX powder were consistent with the saturation solubility results, and the higher dissolution rate of RLX in SGF could be ascribed to its higher solubility than that in SIF [67]. In contrast, the RLX-SMEDDS showed substantially higher dissolution rates than RLX powder in each dissolution medium.…”

Section: Saturation Solubility and Dissolution Profile Of Rlx-smeddssupporting

confidence: 78%

Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability

Ansari

Choi

et al. 2023

Pharmaceutics

View full text Add to dashboard Cite

Poor aqueous solubility and dissolution limit the oral bioavailability of Biopharmaceutics Classification System (BCS) class II drugs. In this study, we aimed to improve the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RLX), a BCS class II drug, using a self-microemulsifying drug delivery system (SMEDDS). Based on the solubilities of RLX, Capryol 90, Tween 80/Labrasol ALF, and polyethylene glycol 400 (PEG-400) were selected as the oil, surfactant mixture, and cosurfactant, respectively. Pseudo-ternary phase diagrams were constructed to determine the optimal composition (Capryol 90/Tween 80/Labrasol ALF/PEG-400 in 150/478.1/159.4/212.5 volume ratio) for RLX-SMEDDS with a small droplet size (147.1 nm) and stable microemulsification (PDI: 0.227). Differential scanning calorimetry and powder X-ray diffraction of lyophilized RLX-SMEDDS revealed the loss of crystallinity, suggesting a molecularly dissolved or amorphous state of RLX in the SMEDDS formulation. Moreover, RLX-SMEDDS exhibited significantly higher saturation solubility and dissolution rate in water, simulated gastric fluid (pH 1.2), and simulated intestinal fluid (pH 6.8) than RLX powder. Additionally, oral administration of RLX-SMEDDS to female rats resulted in 1.94- and 1.80-fold higher area under the curve and maximum plasma concentration, respectively, than the RLX dispersion. Collectively, our findings suggest SMEDDS is a promising oral formulation to enhance the therapeutic efficacy of RLX.

show abstract

Section: Saturation Solubility and Dissolution Profile Of Rlx-smeddssupporting

confidence: 78%

Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability

Ansari

Choi

et al. 2023

Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…For HPMC E5, the characteristic peaks were shown at 3400 cm -1 due to O-H stretching vibration peak, 1153.43 cm -1 due to C-O-C stretching vibration peak and 1109.07 cm -1 due to C-O stretching. Oh and his colleagues (2012) highlighted similar FT-IR peaks of HPMC E5 [41].…”

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 92%

Formulation, Analysis and Validation of Nanosuspensions-Loaded Voriconazole to Enhance Solubility

AL-EDRESI,

ABDUL-HASAN,

HADI SALAL

2024

Int J App Pharm

View full text Add to dashboard Cite

Objective: This study aimed to enhance the solubility of voriconazole (VRZ) via loading to nanosuspensions using solvent/anti-solvent technique. The optimisation of independent variables (polymer concentrations) was carried out to achieve the desired particle size and maximise the percentage of entrapment efficiency (EE %) and drug loading (DL %) using design-expert®software. Methods: Design-Expert® software, version 13, was used to design and optimise nanosuspensions-loaded VRZ using 23 factorial designs. Concentrations of polyvinylpyrrolidone, hydroxypropyl methylcellulose and poloxamers were selected as independent variables to achieve ideal particle size, polydispersity index (PDI), entrapment efficacy (EE %) and drug loading (DL %). Atomic force microscopy (AFM), differential scanning calorimetry (DSC) and saturated solubility were used to assess the lyophilized nanoparticles. The compatibility between the drug and the polymers was studied using Fourier transform infrared spectroscopy (FTIR). Results: The particle size, PDI, EE %, and DL % were in the range of 15.6–145.6 nm, 0.010-0.120, 55.9 %-91.9 %, and 6.68-36.76 %, respectively. The saturated solubility of nanosuspensions-loaded VRZ (NS-VRZ) relative to free VRZ was increased tenfold in DW and twelvefold in PBS (pH 7.4). DSC thermogram confirmed the incorporation of VRZ in the nanosuspensions. The AFM of NS-VRZ validated spherical tiny particle size with a smooth surface. There is no chemical interaction between VRZ and the polymers, according to an FTIR investigation. Conclusion: The solubility of VRZ was successfully enhanced by loading to nanosuspensions. The solvent/anti-solvent technique was proven to be cost-effective, easy to operate and suitable for the preparation of NS-VRZ using Design-Expert®software.

show abstract

“…Additionally, an indacenodithiophene polymer with an alkyl side chain (PIDTC16-BT), which hinders and delays ion movement, was employed to achieve long-term retention. [44] The two synaptic transistors were connected in parallel to enable reconfigurable characteristics. The operational modes of the reconfigurable logic gate are determined by the number of input pulses provided to the RS.…”

Section: Introductionmentioning

confidence: 99%

Reconfigurable Logic Gates Capable of Device‐Level Parallel Processing Through Multi‐Input Synaptic Device

Roe,

Park,

Jeong

et al. 2024

Adv Funct Materials

View full text Add to dashboard Cite

Synaptic devices have gained prominence as viable alternatives to conventional complementary metal‐oxide‐semiconductor‐based (CMOS) electronics in the information processing field owing to their inherent advantages in analog and parallel operations. The potential of synaptic devices has not yet been fully utilized for logic operations because only the conventional binary logic structure has been applied to analog synaptic devices, leading to the loss of advantages unique to analog signals. To resolve this issue, an innovative concept is proposed: an analog logic gate that can perform parallel operations at the device level and is coupled with logic reconfigurations, enabling comprehensive analog computation. This logic gate comprises two synaptic devices with different retention characteristics, adjusted by the side‐chain engineering of an organic polymer. The long‐term and short‐term synaptic devices serve as reconfigurable synapse for logic mode selection and parallel processable logic synapse, respectively. In this study, the reconfigurable and parallel processable synaptic logic circuit is effectively implemented in a personalized disease risk diagnostic system. This innovative approach not only allows for the simultaneous computation of analog‐formed diagnostic data, but also enhances both computing efficiency and system complexity in general synaptic systems.

show abstract

The dissolution property of raloxifene HCl solid dispersion using hydroxypropyl methylcellulose

Cited by 15 publications

References 19 publications

Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability

Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability

Formulation, Analysis and Validation of Nanosuspensions-Loaded Voriconazole to Enhance Solubility

Reconfigurable Logic Gates Capable of Device‐Level Parallel Processing Through Multi‐Input Synaptic Device

Contact Info

Product

Resources

About