scholarly journals Physicochemical characterization and in vitro dissolution studies of solid dispersions of ketoprofen with PVP K30 and d-mannitol

2013 ◽  
Vol 21 (1) ◽  
pp. 77-84 ◽  
Author(s):  
Pankajkumar S. Yadav ◽  
Vikas Kumar ◽  
Udaya Pratap Singh ◽  
Hans Raj Bhat ◽  
B. Mazumder
2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Abdulla Sherikar ◽  
Mohd Usman Mohd Siddique ◽  
Mahesh More ◽  
Sameer N. Goyal ◽  
Milan Milivojevic ◽  
...  

Solubility of phytochemicals is a major concern for drug delivery, permeability, and their biological response. However, advancements in the novel formulation technologies have been helping to overcome these challenges. The applications of these newer technologies are easy for commercialization and high therapeutic outcomes compared to conventional formulations. Considering these facts, the present study is aimed to prepare a silymarin-loaded eutectic mixture with three different ratios of Polyvinylpyrrolidone K30 (PVP K30) and evaluating their anti-inflammatory, and hepatoprotective effects. The preliminary phytochemical and characterization of silymarin, physical mixture, and solid dispersions suggested and successfully confirmed the formation of solid dispersion of silymarin with PVP K30. It was found that the solubility of silymarin was increased by 5-fold compared to pure silymarin. Moreover, the in vitro dissolution displayed that 83% of silymarin released within 2 h with 2.8-fold increase in dissolution rate compared to pure silymarin. Also, the in vivo study suggested that the formulation significantly reduced the carbon tetrachloride- ( 0.8620 ± 0.05034 ∗ ∗ for 1 : 3 ratio), paracetamol- ( 0.7300 ± 0.01517 ∗ ∗ for 1 : 3 ratio), and ethanol- ( 0.8100 ± 0.04037 ∗ ∗ for 1 : 3 ratio) induced hepatotoxicity in rats. Silymarin solid dispersion was prepared using homogenization methods that have prominent anti-inflammatory effect ( 0.6520 ± 0.008602 ∗ ∗ with 8.33%) in carrageenan-induced rat paw model.


Author(s):  
Sanjesh G. Rathi ◽  
Dhruv B. Chaudhari

The solid dispersions of Bilastine with HPMC, PVP K30 and HPC have been prepared in different weight ratios by using solvent evaporation method. DSC was used to characterize the samples of solid dispersions and pure drug. Drug found compatible with the excipients. The highest improvements in solubility and in-vitro drug release were observed in solid dispersion prepared with HPC (F14) by solvent evaporation method. The increased dissolution rate of drug from solid dispersion may be due to surface tension lowering effect of polymer to the medium and increased wettability and dispersibility of drug. Hence, F14 Solid dispersion with the HPC carrier considered as most satisfactory among all solid dispersions.


2020 ◽  
Vol 23 (1) ◽  
pp. 44-53
Author(s):  
Sharmin Akhter ◽  
AKM Saif Uddin ◽  
Aninda Kumar Nath ◽  
Md Salahuddin ◽  
Mohammad Fahim Kadir ◽  
...  

Ketoprofen [2-(3-benzoylphenyl)-propionic acid], a non-steroidal anti-inflammatory drug exhibits poor dissolution pattern. Solid dispersion (SD) techniques were used because it is particularly promising to improve the oral absorption and bioavailability of BCS Class II drugs. This investigation entails solid dispersion of ketoprofen which was formulated and characterized for better release profile and immediate action of the drug. Melting method was applied to prepare solid dispersion by using two immediate release (IR) polymer PEG 6000 and HPMC 6 cps at different weight ratios. In the formulation, a fixed amount of lactose was used as adsorbent. The solid dispersions were investigated for drug entrapment efficiency and dissolution behavior. In vitro dissolution study was performed in phosphate buffer (pH 7.4) medium for one hour. Percent cumulative drug release from solid dispersion was found to be minimum 92.19% and maximum 98.95% within one hour, which showed a better dissolution compared to the active drugs. Evaluation of the properties of the solid dispersion was also performed by using Scanning Electron Microscopy (SEM) study and Differential Thermal Analysis (DTA). SEM results indicated that ketoprofen crystallinity in SDs was significantly reduced, and that the majority of ketoprofen was in amorphous form. No interaction was found between drug and polymers from DTA and Fourier-transform infrared (FTIR) spectroscopy analysis. So, solid dispersion technique may be an effective technique to enhance dissolution rate of ketoprofen. Bangladesh Pharmaceutical Journal 23(1): 44-53, 2020


Molecules ◽  
2017 ◽  
Vol 22 (2) ◽  
pp. 274 ◽  
Author(s):  
Qi Zhang ◽  
Yiqiong Pu ◽  
Bing Wang ◽  
Yuqin Wang ◽  
Tina Dong ◽  
...  

2011 ◽  
Vol 73 (2) ◽  
pp. 243 ◽  
Author(s):  
K. R. S. Sambasiva Rao ◽  
K. P. R. Chowdary ◽  
MV Nagabhushanam

Author(s):  
G. Muralichand ◽  
D. V. R. N. Bhikshapathi

The objective of this study was to develop solid dispersions of Nifedipine which has low aqueous solubility and bioavailability. Preliminary solubility studies were carried out using various hydrophilic polymers. The formulations were then optimized and evaluated by in-vitro dissolution studies, X-ray diffraction, FTIR and SEM. Formulation with 1:4:2 ratios of Nifedipine, Labrosol and SLS was found to be the best as it possessed better drug release properties compared to pure drug and other physical mixtures. The optimized formulation SD12 was found to have better drug release of 98.74±5.19% in 90 minutes. From FTIR studies no interaction was takes place between drug and polymers. XRD peaks indicate the successful transformation of drug from crystalline to amorphous form. The final results indicate that the solid dispersion of Nifedipine remained stable over 90 days.


Author(s):  
Narendar D ◽  
Ettireddy S

The content of this investigation was to study the influence of β-cyclodextrin and hydroxy propyl-β-cyclodextrin complexation on enhancement of solubility and dissolution rate of isradipine. Based on preliminary phase solubility studies, solid complexes prepared by freeze drying method in 1:1 molar ratio were selected and characterized by DSC for confirmation of complex formation. Prepared solid dispersions were evaluated for drug content, solubility and in vitro dissolution. The physical stability of optimized formulation was studied at refrigerated and room temperature for 2 months. Solid state characterization of optimized complex performed by DSC and XRD studies.  Dissolution rate of isradipine was increased compared with pure drug and more with HP-β-CD inclusion complex than β-CD. DSC and XRD analyzes that drug was in amorphous form, when the drug was incorporated as isradipine β-CD and HP-β-CD inclusion complex. Stability studies resulted in low or no variations in the percentage of complexation efficiency suggesting good stability of molecular complexes. The results conclusively demonstrated that the enhancement of solubility and dissolution rate of isradipine by drug-cyclodextrin complexation was achieved.   


Author(s):  
R. Nagaraju ◽  
Rajesh Kaza

Salbutamol and theophylline are available in conventional dosage forms, administered four times a day, leading to saw tooth kinetics and resulting in ineffective therapy. The combination of these two drugs in a single dosage form will enhance the patient compliance and prolong bronchodilation. Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M), hydroxy propyl methylcellulose K100M (HPMC- K100M), xanthan gum, ethyl cellulose and hydroxy propyl methylcellulose phthalate (HPMC-P) were studied. HPMC-P and HPMC- K4M were found to be best in controlling the release. In-vitro dissolution studies were carried out for all the bi-layered tablets developed using USP dissolution apparatus type 2 (paddle). It was found that the tablet FB15-FW3 showed 50% release of salbutamol in first hour and the remaining was released for eight hours. However, theophylline was found to be released as per the USP specifications. The IR spectrum was taken for FB15-FW3 formulation and it revealed that there is no disturbance in the principal peaks of pure drugs salbutamol and theophylline. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. Also, formulation of FB15-FW3 has shown required release pattern and complies with all the evaluated parameters and comparable to the marketed formulation.


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