scholarly journals The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

2019 ◽  
Vol 48 (2) ◽  
pp. 69-75 ◽  
Author(s):  
Abid Yousaf ◽  
Sundas Zulfiqar ◽  
Yasser Shahzad ◽  
Talib Hussain ◽  
Tariq Mahmood ◽  
...  
Author(s):  
SHRADHA S. TIWARI ◽  
SHAILESH J. WADHER ◽  
SURENDRA G. GATTANI

Objective: Nateglinide is a commonly used oral hypoglycemic, biopharmaceutical classification system Class II drug, which shows relatively poor water solubility and variable bioavailability. The objective of the present investigation was to develop the binary and ternary solid dispersions of nateglinide for improved solubility and dissolution. Methods: Nateglinide solid dispersions were prepared by a common solvent evaporation method. Polymers like soluplus, kolliphor P188, sylloid 244FP, gelucire 48/16, affinisol (HPMCAS), HPβCD, βCD were used in different combinations. The physicochemical characterization of the optimized ternary dispersion was studied by using FT-IR, DSC, and PXRD. Solubility and dissolution behavior of all dispersions were studied. Result: From all prepared ternary solid dispersions, nateglinide dissolution was significantly faster than pure nateglinide. With ternary solid dispersion of NTG, soluplus and kolliphor P188 there was a big improvement in solubility and dissolution. This combination enhanced the solubility of NTG by 23 folds. Another ternary dispersion of NTG with soluplus and gelucire 48/16 enhanced solubility by 25 fold. Conclusion: Ternary solid dispersion found superior over binary dispersions. For the ternary dispersions, showing the best solubility, tablets were prepared. Dissolution and drug release from the formulated tablet was as good as a marketed product.


2015 ◽  
Vol 21 (3) ◽  
pp. 268-276 ◽  
Author(s):  
Djordje P. Medarević ◽  
Kyriakos Kachrimanis ◽  
Miodrag Mitrić ◽  
Jelena Djuriš ◽  
Zorica Djurić ◽  
...  

Author(s):  
Kumar P ◽  
S Kumar ◽  
A Kumar ◽  
M Chander

The purpose of this study was to prepare and characterize solid dispersions of the antibacterial agent Cefdinir with PEG 4000 and PVP K-30 with a view to improve its dissolution properties. Investigations of the properties of the dispersions were performed using release studies, X-ray powder diffraction (XRD) and Fourier transform infrared (FTIR). The results obtained showed that the rate of dissolution of Cefdinir was considerably improved when formulated in solid dispersions with PVP K-30 and PEG 4000 as compared with pure drug and physical mixtures. The results from XRD studies showed the transition of crystalline nature of drug to amorphous form, while FTIR studies demonstrated the absence of drug-carriers interaction.


Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate


2020 ◽  
Vol 2020 ◽  
pp. 1-13
Author(s):  
Xiaoyu Sui ◽  
Yan Chu ◽  
Jie Zhang ◽  
Honglian Zhang ◽  
Huiyu Wang ◽  
...  

The effect of polyvinylpyrrolidone (PVP) as glycyrrhetic acid (GA) solid dispersions carrier at different molecular weights on the dissolution behavior and physicochemical properties was investigated. PVP-GA-SDs prepared with all four molecular weight PVPs displayed good enhancement of dissolution rate and equilibrium solubility compared with pure drug and corresponding physical mixtures. The results showed that the enhancement effect of molecular weight on dissolution rate and equilibrium solubility follows PVP   K 30 > PVP   K 60 > PVP   K 17 > PVP   K 15 . In addition, the dissolution rate and solubility of the SDs with a carrier-drug ratio of 8 : 1 were better than the samples of 4 : 1. The DSC and XRD patterns showed that the crystallization of GA in SDs prepared by PVP K30 and PVP K60 was significantly inhibited, and both were transformed to amorphous. Based on FTIR and Raman detection, a hydrogen-bond between PVP and drug molecules is formed. SEM results showed that there were no significant differences in the appearance of SDs prepared with four PVPs, and no crystalline morphology of GA was seen. In conclusion, the findings of this study demonstrated that the dissolution performance of the PVP-GA-SDs prepared by the solvent method is related to the molecular weight of PVP, and the change in the molecular weight of PVP does not cause a monotonic change in dissolution of GA. The samples with PVP K30 as the carrier have the best dissolution performance.


2011 ◽  
Vol 317-319 ◽  
pp. 185-188 ◽  
Author(s):  
Pornsak Sriamornsak ◽  
Srisuda Kontong ◽  
Yotsanan Weerapol ◽  
Jurairat Nunthanid ◽  
Srisagul Sungthongjeen ◽  
...  

The aim of this study was to manufacture the ternary solid dispersions composed of nifedipine, Eudragit® E and adsorbent. Dissolution enhancement of nifedipine was also investigated. The inert solid carriers were added in the mixtures of nifedipine and Eudragit® E at varying ratios. The physicochemical properties of ternary systems, compared to physical mixtures, were analyzed using powder x-ray diffraction (PXRD) and differential scanning calorimetry (DSC). The dissolution of nifedipine from ternary systems was compared to the drug alone. The influence of drug:polymer: adsorbent ratio and type of adsorbent on the dissolution rate of the drug was also evaluated. The PXRD and DSC results of the systems with high amount of polymer showed that the drug was present in an amorphous form. On the other hand, the diffraction patterns and DSC thermograms of the physical mixtures revealed that to some extent the drug was present in a crystalline form. The results from this study demonstrated that an improvement in dissolution rate of nifedipine with Eudragit® E and adsorbents was obtained.


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