Solid dispersion (SD) is one of the most widely used methods to resolve issues accompanied by poorly soluble drugs. The present study was carried out to enhance the solubility and dissolution rate of Aceclofenac (ACE), a BCS class II drug with pH-dependent solubility, by the SD method. Effervescent assisted fusion technique (EFSD) using different hydrophilic carriers (mannitol, urea, Soluplus®, poloxamer 188, and poloxamer 407) in the presence of an effervescent base (sodium bicarbonate and citric acid) in different drug: carrier: effervescent base ratio and the conventional fusion technique (FSD) were used to prepare ACE SD. Solubility, dissolution rate, Fourier transformation infrared spectroscopy (FTIR), PowderX-ray diffraction study (PXRD), and Differential scanning calorimetry (DSC) were determined for the SD obtained from both techniques as a comparative study. The results showed that EFSD using ACE: Soluplus®: effervescent base in a ratio of 1:2:1 had higher solubility and dissolution rate than that obtained from FSD prepared by ACE: Soluplus® in a ratio of 1:2. However, the two techniques obtained the amorphous form according to XRD and DSC results. It can be concluded that EFSD is a promising method for the solubility and dissolution rate improvement of BCS class II drugs.
Background: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The fo
... Show MoreEbastine (EBS) is a non-sedating antihistamine with a long duration of action. This drug has predominantly hydrophobic property causing a low solubility and low bioavailability. Surface solid dispersions (SSD) is an effective technique for improving the solubility and dissolution rate of poorly soluble drugs by using hydrophilic water insoluble carriers.
The present study aims to enhance the solubility and dissolution rate of EBS by using surface solid dispersion technique. Avicel® PH101, Avicel® PH 102, croscarmellose sodium(CCS) and sodium starch glycolate(SSG) were used as water insoluble hydrophilic carriers.
The SSD formulations of EBS were prepared by the solvent evaporation method in different drug: carrier
... Show MoreEtoricoxib (EXB) is a highly selective cox-2 inhibitor which belongs to the non-steroidal anti-inflammatory drug (NSAID). EXB is a class II drug according to the biopharmaceutical classification system (BCS), which possess a very low aqueous solubility in water. In the present study, many trials were made to improve the aqueous solubility and dissolution rate of EXB by solid dispersion technique.
Eighteenth EXB formulas were formulated as a solid dispersion using a variety of hydrophilic polymers (as carriers) including poloxamer 407 (PXM 407), poloxamer 188 (PXM 188) and polyethylene glycol 4000 (PEG 4000) at different drug: polymer ratios (1:1, 1:3 and 1:5). These formulas were prepared by two methods; solvent
... Show MoreAtorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.
The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxam
... Show MoreAtorvastatin (ATR) is a poorly water-soluble anti-hyperlipidemic drug. The drug belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersion is an effective technique for enhancing the solubility and dissolution of drugs. Phospholipid solid dispersion (PSD) using phosphatidylcholine (PC) as a carrier with or without adsorbent (magnesium aluminum silicate, silicon dioxide 15nm, silicon dioxide 30nm, calcium silicate) was used to prepare ATR PSD using different drug: PC: adsorbent ratios by solvent evaporation method. The resulted PSD was evaluated for its percentage yield, drug content, solubility, dissolution rate, Fourier transforma
... Show MoreSolid dispersion is an attractive tool of pharmaceutical technology used to improve the physical properties of drugs. Among these properties is to enhance the solubility of the drugs.
Rebamipide is a poorly soluble drug of class IV of biopharmaceutical classification system (BCS).
Rebamipide is used as potent antiulcer, mucoprotective drug, by stimulating the generation of prostoglandine enhanced mucosal protection.
Rebamipide was formulated as a solid dispersion using different polymers such as pluronic F-127, PEG6000, PVP K30, and TPGS by using different preparation methods solvent evaporation, fusion, and kneading methods.
It was seen that rebamipide was successfully dispersed in a homogenous solid dispersion matrix by sol
Bilinear interpolation and use of perceptual color spaces (HSL, HSV, LAB, and LUV) fusion techniques are presented to improve spatial and spectral characteristics of the multispectral image that has a low resolution to match the high spatial resolution of a panchromatic image for different satellites image data (Orbview-3 and Landsat-7) for the same region. The Signal-to-Noise Ratio (SNR) fidelity criterion for achromatic information has been calculated, as well as the mean color-shifting parameters that computed the ratio of chromatic information loss of the RGB compound inside each pixel to evaluate the quality of the fused images. The results showed the superiority of HSL color space to fuse images over the rest of the spac
... Show MoreA new data for Fusion power density has been obtained for T-3He and T-T fusion reactions, power density is a substantial term in the researches related to the fusion energy generation and ignition calculations of magnetic confined systems. In the current work, thermal nuclear reactivities, power densities of a fusion reactors and the ignition condition inquiry are achieved by using a new and accurate formula of cross section, the maximum values of fusion power density for T-3He and TT reaction are 1.1×107 W/m3 at T=700 KeV and 4.7×106 W/m3 at T=500 KeV respectively, While Zeff suggested to be 1.44 for the two reactions. Bremsstrahlung radiation has also been determined to reaching self- sustaining reactors, Bremsstrahlung values are 4.5×
... Show MoreBackground: Telmisartan is an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension and renal disease. Based on the Biopharmaceutical Classification System. It’s a Class II poorly soluble drug.
Objective: To prepare a sublingual tablet by increasing the dissolution and solubility of Telmisartan utilizing the solid dispersion method.
Methods: Three methods were obtained to prepare the solid dispersion of telmisartan: solvent evaporation, Kneading, and microwave method. Each method uses surplus as a hydrophilic carrier in different ratios of 1%, 2%, and 3%. Preparation of ternary solid dispersion by adding potassium carbonate salt to
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The effective surface area of drug particle is increased by a reduction in the particle size. Since dissolution takes place at the surface of the solute, the larger the surface area, the further rapid is the rate of drug dissolution. Ketoprofen is class II type drug according to (Biopharmaceutics Classification System BCS) with low solubility and high permeability. The aim of this investigation was to increase the solubility and hence the dissolution rate by the preparation of ketoprofen nanosuspension using solvent evaporation method. Materials like PVP K30, poloxamer 188, HPMC E5, HPMC E15, HPMC E50, Tween 80 were used as stabilizers in perpetration of differ
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