scholarly journals IMMEDIATE RELEASE SOLID DISPERSION TABLET OF AZILSARTAN: FORMULATION STRATEGY TO ENHANCE ORAL BIOAVAILABILITY

2020 ◽  
pp. 126-134
Author(s):  
JAMEER A. TAMBOLI ◽  
SHRINIVAS K. MOHITE
Keyword(s):  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Fold Increase ◽  
Immediate Release ◽  
Stability Study ◽  
Water Soluble ◽  
Compatibility Study ◽  
Saturation Solubility ◽  
In Vivo Absorption

Objective: Objective of the present study was to develop an immediate release solid dispersion tablet to enhance oral bioavailability of Azilsartan. Methods: Solid dispersion of azilsartan was developed using Soluplus® as a novel solubility enhancer by the solvent evaporation technique. 32factorial design was used in a fully randomized order to study effect of amount of azilsartan and Soluplus on solubility (µg/ml) and % drug dissolved in 30 min. Prepared solid dispersion was evaluated for different micromeritic properties, saturation solubility, and wettability. Then solid dispersion of all the batches compressed into an immediate-release tablet using sodium starch glycolate as a super disintegrant. Developed tablet formulations were evaluated for various post-compression parameters and satisfactory formulation among these were further studied for Fourier-transform infrared spectroscopy (FTIR), Differential Scanning Colorimeter (DSC), X-Ray Diffraction (XRD), in vivo absorption and stability study. Results: Results of micromeritic properties of solid dispersion showed that good flowability, compressibility, wettability, and saturation solubility. Post compression parameters of immediate-release tablets were found to be in acceptable limits. Batch ASD2 containing 40 mg Diacerein and 80 mg of Soluplus showed maximum drug release i.e. 99.82 % within 30 min. Compatibility study using FTIR, DSC, and XRD showed that drug is compatible with Soluplus. In vivo absorption study showed that, 2.67 fold increase in Area Under Curve (AUC) as compared to plain Azilsartan. Relative bioavailability was found to be 267.11 %. Results of stability study indicate that developed formulations were stable at accelerated temperature and humidity conditions. Conclusion: Study concluded that solid dispersion using Soluplus as a solubility enhancer is a suitable formulation strategy to enhance solubility, dissolution, and bioavailability of poorly water-soluble drug-like Azilsartan.

scholarly journals Enhanced Oral Bioavailability of Celecoxib Nanocrystalline Solid Dispersion based on Wet Media Milling Technique: Formulation, Optimization and In Vitro/In Vivo Evaluation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 328 ◽  
Author(s):  
Zhuang Ding ◽  
Lili Wang ◽  
Yangyang Xing ◽  
Yanna Zhao ◽  
Zhengping Wang ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Stability Study ◽  
Sprague Dawley ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Celecoxib (CLX), a selective COX-2 inhibitor, is a biopharmaceutics classification system (BCS) class II drug with its bioavailability being limited by thepoor aqueoussolubility. The purpose of this study was to develop and optimize CLX nanocrystalline(CLX-NC) solid dispersion prepared by the wet medium millingtechnique combined with lyophilizationto enhance oral bioavailability. In formulation screening, the resulting CLX-NC usingpolyvinylpyrrolidone (PVP) VA64 and sodiumdodecyl sulfate (SDS) as combined stabilizers showed the minimum particle size and a satisfactory stability. The formulation and preparation processwere further optimized by central composite experimentaldesign with PVP VA64 concentration (X1), SDS concentration (X2) and milling times (X3) as independent factors and particle size (Y1), polydispersity index (PDI, Y2) and zeta potential (Y3) as response variables. The optimal condition was determined as a combination of 0.75% PVP VA64, 0.11% SDS with milling for 90 min.The particle size, PDI and zeta potential of optimized CLX-NC were found to be 152.4 ± 1.4 nm, 0.191 ± 0.012 and −34.4 ± 0.6 mV, respectively. The optimized formulation showed homogeneous rod-like morphology as observed by scanning electron microscopy and was in a crystalline state as determined by differential scanning calorimetry and powder X-ray diffraction. In a storage stability study, optimized CLX-NC exhibited an excellent physical stability during six months’ storage at both the refrigeration and room conditions. In vivo pharmacokinetic research in Sprague-Dawley ratsdisplayed that Cmax and AUC0–∞ of CLX-NC were increased by 2.9 and 3.1 fold, compared with physical mixture. In this study, the screening and optimizing strategy of CLX-NC formulation represents a commercially viable approach forenhancing the oral bioavailability of CLX.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

scholarly journals In vivo evaluation of modified gum karaya as a carrier for improving the oral bioavailability of a poorly water-soluble drug, nimodipine

2002 ◽  
Vol 3 (2) ◽  
pp. 55-63 ◽  
Author(s):  
Gedela V. Murali Mohan Babu ◽  
Namballa R. Kumar ◽  
Kasina H. Sankar ◽  
Battu J. Ram ◽  
Namburu K. Kumar ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Water Soluble ◽  
In Vivo Evaluation ◽  
Gum Karaya ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

In vitro dissolution method fitted to in vivo absorption profile of rivaroxaban immediate-release tablets applying in silico data

2017 ◽  
Vol 44 (5) ◽  
pp. 723-728 ◽  
Author(s):  
Nathalie R. Wingert ◽  
Natália O. dos Santos ◽  
Sarah C. Campanharo ◽  
Elisa S. Simon ◽  
Nadia M. Volpato ◽  
...  
Keyword(s):  
In Silico ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Absorption Profile ◽  
Dissolution Method ◽  
In Vivo Absorption

In Vitro-In Vivo Correlation for Solid Dispersion of a Poorly Water-Soluble Drug Efonidipine Hydrochloride

2020 ◽  
Vol 21 (5) ◽  
Author(s):  
Xu Cheng ◽  
Jianlong Gao ◽  
Jiaqi Li ◽  
Gang Cheng ◽  
Meijuan Zou ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

In Vitro and In Vivo Evaluation of Olmesartan Medoxomil Microcrystals and Nanocrystals: Preparation, Characterization, and Pharmacokinetic Comparison in Beagle Dogs

2019 ◽  
Vol 16 (6) ◽  
pp. 500-510
Author(s):  
Rong Chai ◽  
Hailing Gao ◽  
Zhihui Ma ◽  
Meng Guo ◽  
Qiang Fu ◽  
...  
Keyword(s):  
Particle Size ◽  
Oral Bioavailability ◽  
Olmesartan Medoxomil ◽  
Water Soluble ◽  
Size Reduction ◽  
Drug Dissolution ◽  
Beagle Dogs ◽  
Enhanced Solubility

Background: Olmesartan medoxomil (OLM) is a promising prodrug hydrolyzed to olmesartan (OL) during absorption from the gastrointestinal tract. OL is a selective angiotensin II receptor antagonist, with high drug resistance and low drug interaction. However, OLM has low solubility and low bioavailability. Therefore, it is extremely urgent to reduce the drug particle size to improve its biological bioavailability. Objective: The aim of the study was to improve the oral bioavailability of poorly water-soluble olmesartan medoxomil (OLM) by using different particle size-reduction strategies. Method: Raw drug material was micronized or nanosized by either jet or wet milling processes, respectively. The particle sizes of the prepared nanocrystals (100-300 nm) and microcrystals (0.5-16 μm) were characterized by DLS, SEM, and TEM techniques. Solid state characterization by XPRD and DSC was used to confirm the crystalline state of OLM after the milling processes. Results: We demonstrated that OLM nanocrystals enhanced solubility and dissolution in the non-sink condition in which high sensitivity was found in purified water. After 1 h, 65.4% of OLM was dissolved from nanocrystals, while microcrystals and OLMETEC® only showed 37.8% and 31.9% of drug dissolution, respectively. In the pharmacokinetic study using Beagle dogs, an increase in Cmax (～2 fold) and AUC (～1.6 fold) was observed after oral administration of OLM nanocrystals when compared to microcrystals and reference tablets, OLMETEC®. In contrast, OLM microcrystals failed to improve the oral bioavailability of the drugs. Conclusion: Particles size reduction to nano-scale by means of nanocrystals technology significantly increased in vitro dissolution rate and in vivo oral bioavailability of OLM.

scholarly journals In Vitro Stability and in Vivo Absorption Studies of Colloidal Particles Formed from a Solid Dispersion System.

1996 ◽  
Vol 44 (12) ◽  
pp. 2309-2313 ◽  
Author(s):  
Katsuhiko YANO ◽  
Atsushi KAJIYAMA ◽  
Shigeru YAMAZAKI ◽  
Yoshisuke MATSUMURA ◽  
Kouji WATANABE ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Colloidal Particles ◽  
Dispersion System ◽  
Absorption Studies ◽  
In Vivo Absorption ◽  
In Vitro Stability
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