Piroxicam ternary solid dispersion system for improvement of dissolution (%) and in vitro anti-inflammation effects

2020 ◽  
Vol 261 ◽  
pp. 114651 ◽  
Author(s):  
Jeong Sun Sohn ◽  
Eui Jin Kim ◽  
Ji-Won Park ◽  
Jin-Seok Choi
1996 ◽  
Vol 44 (12) ◽  
pp. 2309-2313 ◽  
Author(s):  
Katsuhiko YANO ◽  
Atsushi KAJIYAMA ◽  
Shigeru YAMAZAKI ◽  
Yoshisuke MATSUMURA ◽  
Kouji WATANABE ◽  
...  

Author(s):  
Erizal Zaini ◽  
Salman Umar ◽  
Nurhidayah Nurhidayah

ABSTRACTObjective: To improve dissolution rate of valsartan from solid dispersion system of valsartan and D(−) mannitol using co-grinding approach.Methods: Valsartan solid dispersion with different ratio of D(−) mannitol (1:1; 1:3 and 1: 5) were prepared by co-grinding method. Solid statecharacterization of the solid dispersion system was evaluated in term of crystallographic properties (powder X-ray diffraction), thermal behavior(differential scanning calorimetry [DSC]) and morphology (scanning electron microscope). The profile of dissolution rate was examined using USPdissolution apparatus type I at a temperature of 37±0.5°C.Results: Based on thermal analysis DSC and powder X-ray diffraction analysis, valsartan was transformed from semicrystalline phase to amorphousstate as indicated by the disappearance of its melting endothermic peaks and the characteristic diffraction peaks. The in vitro dissolution rate studyrevealed that all solid dispersion system showed significant increase in dissolution rate compared with the intact valsartan.Conclusion: Solid dispersion of valsartan with D(−) mannitol prepared by co-grinding technique has successfully improved the dissolution ratecompared with intact valsartan.Keywords: Valsartan, D(−) mannitol, Solid dispersion, Co-grinding, Dissolution rate.


2020 ◽  
Vol 54 (2) ◽  
pp. 302-309
Author(s):  
Uday Baburao Bolmal ◽  
Ramnathkar Prajakta Subhod ◽  
Anand Panchaxari Gadad ◽  
Archana Sidagouda Patill

2021 ◽  
Author(s):  
Marouene Bejaoui ◽  
Hanen Oueslati ◽  
Haykel Galai

Amorphous ternary solid dispersion has become one of the strategies commonly used for improving the solubility and bioavailability of poorly water soluble drugs. Such multicomponent solid dispersion can be obtained by different techniques, this chapter provides an overview of ternary solid dispersion by co-milling method from the perspectives of physico-chemical characteristics in vitro and in vivo performance. A considerable improvement of solubility was obtained for many active pharmaceutical ingredients (e.g., Ibuprofen, Probucol, Gliclazid, Fenofibrate, Ibrutinib and Naproxen) and this was correlated to the synergy of multiple factors (hydrophilicity enhancement, particle size reduction, drug-carrier interactions, anti-plasticizing effect and complexation efficiency). This enhanced pharmacokinetic properties and bioavailability of these drug molecules (1.49 to 15-folds increase in plasma drug concentration). A particular focus was accorded to compare the ternary and binary system including Ibuprofen and highlighting the contribution of thermal and spectral characterization techniques. The addition of polyvinylpyrrolidone (PVP K30), a low molecular weight molecule, into the binary solid dispersion (Ibuprofen/β-cyclodextrin), leads to a 1.5–2 folds increase in the drug intrinsic dissolution rate only after 10 min. This resulted from physical stabilization of amorphous Ibuprofen by reducing its molecular mobility and inhibiting its recristallization even under stress conditions (75% RH and T = 40°C for six months).


2020 ◽  
Vol 8 (A) ◽  
pp. 16-19
Author(s):  
Fifi Harmely ◽  
Salman Umar ◽  
Yufri Aldi ◽  
Ellyza Nasrul ◽  
Erizal Zaini

AIM: The aim of the present study was to prepare and characterize the solid dispersion of poorly soluble drugs irbesartan with hydrophilic polymer poloxamer 188 by solvent co-evaporation technique. METHODS: The ratio of irbesartan to poloxamer 188 in solid dispersion system was 1:0.5; 1:1; and 1:3. Physicochemical properties characterization was analyzed by X-ray powder diffraction, Fourier-transform infrared (FT-IR) spectroscopy, differential thermal analysis, and scanning electron microscopy (SEM). The in vitro dissolution rate profile of solid dispersion was performed by Type II United States Pharmacopeia dissolution testing apparatus. RESULTS: The results of the X-ray powder diffraction pattern showed that the degree of crystallinity of irbesartan crystalline phase reduced in a solid dispersion system. FT-IR spectra indicate that there is no chemical interaction between irbesartan and poloxamer 188 in a solid dispersion system. SEM microscopy demonstrated a homogenous phase of a solid dispersion system with distinct crystal habit. In general, in vitro dissolution rate of all solid dispersions was higher than intact irbesartan. The highest percentage of dissolved irbesartan was the solid dispersion of irbesartan-poloxamer 188 (1:0.5 w/w). CONCLUSIONS: The study concludes that the solid dispersion can be applied to improve the dissolution rate of irbesartan.


Author(s):  
Sharmin Akhter ◽  
Md. Sajjad Hossen ◽  
Md. Salahuddin ◽  
Muazzem Ahmed Sunny ◽  
Farzana Akther Sathi ◽  
...  

Glimepiride (GMP) is poorly water soluble drug, so solubility is the main constraint for its oral bioavailability. Because, poor aqueous solubility and slow dissolution rate of the glimepiride lead to irreproducible clinical response or therapeutic failure in some cases due to sub therapeutic plasma drug levels. In this study, binary and ternary solid dispersion of glimepiride were prepared with polyethylene glycol 6000 (PEG 6000) and polyethylene glycol 4000 (PEG 4000) at different weight ratios using the solvent evaporation and melting method. It was found the drug was released 0.46% after 5 minutes and only 15.83% within 60 minutes from active glimepiride on the other hand the release pattern of glimepiride from the binary formulation containing PEG 4000 in 1:5 (Formulation coding: G5) showed the best result. It was found that the ternary different SD formulation containing(PEG4000:Glimepiride:Povidone) In ratio 1:1:0.25 (Formulation coding were : G13) showed the best result. The drug was changed to amorphous form after solid dispersion. Itwas also evident that solid dispersions improve solubility of drug particles thus enhancing dissolution characteristics of drugs they increase the oral bioavailability. Peer Review History: UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file Average Peer review marks at initial stage: 4.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Name: Dr. Mohammed Abdel-Wahab Sayed Abourehab  Affiliation: Umm Al-Qura University;  Makkah Al-Mukarramah, Saudi Arabia E-mail: [email protected]   Name: Dr. Evren Alğin Yapar Affiliation: Turkish Medicines and Medical Devices Agency, Turkiye E-mail: [email protected] Comments of reviewer(s):


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