Preparation and In vitro Evaluation of Azithromycin Solid Dispersion tablet using PEG-6000

Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.


2020 ◽  
Vol 15 (3) ◽  
pp. 219-225
Author(s):  
Tapan Kumar Giri ◽  
Payel Roy ◽  
Subhasis Maity

Background: Chili peppers are widely used in many cuisines as a spice, and capsaicin is the main component. It has been reported that capsaicin acts as an antihyperglycemic agent. However, it shows poor aqueous solubility and bioavailability. Objective: The is to enhance the aqueous solubility and antihyperglycemic activity of capsaicin through solid dispersion formulation. Methods: Solid dispersions were prepared by the solvent evaporation method using polyethylene glycol 6000 (PEG 6000) as a hydrophilic carrier. Polymer-drug miscibility and drug crystallinity were characterized through the differential thermal analysis and X-ray powder patterns analysis. Solid dispersions were evaluated for solubility, in vitro drug dissolution and in vivo animal study in rats. Results: Results of x-ray powder patterns analysis showed a considerable reduction of drug crystallinity in solid dispersion. Differential thermal analysis result revealed a complete disappearance of capsaicin melting onset temperature in solid dispersion. From the phase solubility data, it was observed that the aqueous solubility of capsaicin was increased with increasing concentration of PEG 6000. Solid dispersion formulation showed considerable enhancement of in vitro release of drugs in comparison to pure capsaicin. In vivo animal study in rats shows that the solid dispersion containing capsaicin significantly reduced the blood glucose level in comparison to the free capsaicin. Conclusion: Higher anti-hyperglycemic effect of capsaicin loaded solid dispersion in comparison to the pure drug may be due to the enhancement of aqueous solubility of capsaicin. Thus, the solid dispersion of capsaicin showed a simple approach for capsaicin delivery with improved antidiabetic activity.


Author(s):  
S. Kaushik ◽  
Kamla Pathak

<p><strong>Objective: </strong>The aim of the present study was to develop and evaluate the monolithic osmotic tablet (MOT) composed of the solid dispersion of ketoprofen (KETO), a poorly water-soluble drug. Solid dispersion technique is generally used for immediate release, as this maximizes the amount of drug absorbed. Sustained release may be obtained by combining solid dispersion technique with MOT so as to increase the therapy efficacy and patient compliance.</p><p><strong>Methods: </strong>Solid dispersion of KETO was prepared by using solvent melt method with polyethylene glycol (PEG) 6000, a hydrophilic carrier. The ratio of KETO to PEG 6000 were 1:1, 1:3 and 1:5 (%w/w). These solid dispersions were characterized by differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA) and powder X-ray diffraction (PXRD) to ascertain whether there were any physicochemical interactions between drug and carrier.</p><p>The tablet core was prepared by using Polyox N80 (a suspending agent), sodium chloride (an osmotic agent), a solid dispersion consisting of PEG 6000 and KETO followed by a coating of cellulose acetate to make the monolithic osmotic tablet.</p><p><strong>Results: </strong>The results of DSC and PXRD indicated that the drug was in the amorphous state in solid dispersion when PEG 6000 was used as a carrier. The dissolution rate of the solid dispersion was much faster than those for the corresponding physical mixture and pure drug. The optimized MOT formulations were able to deliver KETO at the constant zero order release, above 95% <em>in vitro</em>, independent to environmental media and stirring rate. The release rate of KETO in the MOT is controlled by osmotic pressure, suspending agent and drug solubility in solid dispersion.</p><p><strong>Conclusion: </strong>The monolithic osmotic tablet containing solid dispersion has great potential in the controlled delivery of ketoprofen, a water-insoluble drug.</p><p><strong>Keywords: </strong>Ketoprofen, Monolithic osmotic tablet, Solid dispersion, Water insoluble</p>


2017 ◽  
Vol 2 (1) ◽  

The objective of this study was to formulate and prepare gliclazide capsule by solid dispersion method using different surfactants and their in vitro evaluation. Solubilising capacity of polyethylene glycol (PEG 6000, PEG 20000) and polyvinylpyrrolidone (PVP K 30) was determined at 2% concentration where gliclazide was used as a model drug and water was used as control for comparison. Results showed that PVP K 30 exhibited maximum solubilising capacity. Fusion method of solid dispersion was adopted for preparation of capsules using PEG 6000 & PEG 20000 in different ratios. Although these agents are claimed to be good surfactants but our results showed that, the highest cumulative drug release was 1.81 % for gliclazide and PEG 6000 in a ratio of 1:6. The flow property of capsule granules was determined by angle of repose. The capsules were also subjected to weight uniformity test, disintegration test and moisture permeation test and the chemical analysis of solid dispersions were done by FTIR. From this study, it can be concluded that it is possible to formulate and prepare gliclazide capsule by using solid dispersion method.


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


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