An in vitro kinetic method for detection of precipitation of poorly soluble drugs

2005 ◽  
Vol 304 (1-2) ◽  
pp. 1-3 ◽  
Author(s):  
Zimei Wu ◽  
Ian G. Tucker ◽  
Majid Razzak ◽  
Natalie J. Medlicott
Author(s):  
Risa Aihara ◽  
Roman Messerschmid ◽  
Masashi Mizoguchi ◽  
Koichi Wada ◽  
Keiko Minami ◽  
...  

2019 ◽  
Vol 9 (1-s) ◽  
pp. 185-195
Author(s):  
SANTOSH KUMAR RADA ◽  
T. Naga Satya Yagnesh

Objective: To enhance the solubility of poorly soluble drugs by using 23 factorial design in the formulation of fast dissolving tablets by employing starch oxalate as a superdisintegrant. Methods: Starch oxalate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch oxalate. By using 23 factorial design, atenolol fast dissolving tablet was prepared by employing starch oxalate as a superdisintegrant in different proportions in each case by direct compression method. In the evaluation of fast dissolving tablets the drug content, hardness, friability, disintegration time and other dissolution characteristics were utilized. Results: The starch oxalate prepared was found to be fine, free-flowing completely amorphous powder. The compatibility between atenolol and starch oxalate were studied and showed no interaction. The drug content, hardness, and friability have been effective with regard to all the formulated fast dissolving tablets employing starch oxalate. The optimised formulation F8 has the least disintegration time i.e., 24±0.06s. The In–vitro wetting time was less (i.e., 28s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be more in F8 formulation 94.42±0.18%. The cumulative drug dissolved in the optimized formulation F8 was found to be 98.70±0.24% in 5 min. Conclusion: The dissolution efficiency of atenolol was enhanced when starch oxalate was found to be a superdisintegrant when combined with sodium starch glycolate, crospovidone and, hence to provide immediate release of the formulated fast dissolving tablets contained drug it could be used.


Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1809
Author(s):  
Jifen Zhang ◽  
Yanhua Wang ◽  
Jirui Wang ◽  
Tao Yi

A drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE by spray-drying. A series of water-soluble solid carriers were compared and then Box-Behnken design was used to optimize the parameters of spray-drying. The drug release and stability of the optimized solid NSSPE in vitro were also investigated. The results showed that hydroxypropyl-β-cyclodextrin (HP-β-CD), rather than solid carriers commonly used in solidification of traditional Pickering emulsions, was suitable for the solid NSSPE to retain the original appearance and size of emulsion droplets after reconstitution. The amount of HP-β-CD had more influences on the solid NSSPE than the feed rate and the inlet air temperature. Fluorescence microscopy, confocal laser scanning microscopy and scanning electron microscopy showed that the reconstituted emulsion of the solid NSSPE prepared with HP-β-CD had the same core-shell structure with a core of oil and a shell of puerarin nanocrystals as the liquid NSSPE. The particle size of puerarin nanocrystal sand interfacial adsorption rate also did not change significantly. The cumulative amount of released puerarin from the solid NSSPE had no significant difference compared with the liquid NSSPE, which were both significantly higher than that of puerarin crude material. The solid NSSPE was stable for 3 months under the accelerated condition of 75% relative humidity and 40 °C. Thus, it is possible todevelop the solid NSSPE preserving the unique microstructure and the superior properties in vitro of the liquid NSSPE for poorly soluble drugs.


2020 ◽  
Vol 9 (4-s) ◽  
pp. 1183-1190
Author(s):  
Arvind Sharma ◽  
Alok Pal Jain ◽  
Sandeep Arora

Introduction:-Poor solubility of drug compounds which accounts for 40% of new molecules investigated at present is an issue of great concern in pharmaceutical industry and reducing particle size (i,e to reduce below 1000 nm )of drug candidate to be investigated is one of the simplest and efficient ways to overcome this challenge. Drug nanocrystals, solid nanosized drug particles are defined as formulation having 100% drug, which are covered by a stabilizer layer. In this study attempt was made to formulate and evaluate nanocrystals of poorly soluble drugs having low oral bioavailability. Material and method:- Nanocrystals were prepared successfully by varying concentration of different stabilizers by anti-solvent precipitation method. The formulated nanocrystals were evaluated by determining physicochemical characteristics such as physical appearance, Differential Scanning Calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffractometry, solubility studies, particle size distribution, zeta potential, and in vitro drug release profile studies. Results:- An in-vitro study was performed on the successful formulation in comparison to drug powder using dissolution apparatus The particle size of RVT and PSNC-3 was found to be 1975.3 nm and 790.1 nm respectively. Conclusion: Precipitated Nanocrystals formulated with different stablizer’s method resultedin formation of small and uniform RVT nanocrystals with an improved saturation solubility, dissolution rate. Keywords: Nanocrystal, poorly soluble drugs


2012 ◽  
Vol 45 (3) ◽  
pp. 336-343 ◽  
Author(s):  
Michael Linn ◽  
Eva-Maria Collnot ◽  
Dejan Djuric ◽  
Katja Hempel ◽  
Eric Fabian ◽  
...  

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