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Enhancement of Aqueous Solubility and Dissolution Rate of Etoricoxib by Solid Dispersion Technique
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Etoricoxib (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 evaporation and fusion method. The prepared formulas were evaluated for practical yield percent (PY %), drug content, saturated solubility and release rate, Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD).

It was found that the solubility was affected by the polymer type and the method of preparation. The polymers (as carriers) used to prepare EXB- solid dispersion showed improvement in the solubility in the following descending order; PXM 407>PXM 188> PEG 4000. The optimum formula (SD15) composed of the drug: PXM 407 at a ratio of 1:5 was prepared by solvent evaporation showed 7.76 folds (676.40%) solubility improvement as compared to pure EXB. The optimum formula showed a release rate of 99.8% through the first 15 min. The advance characterization of the selected formula indicated the possible transformation of the drug to the amorphous state.

Keywords: EXB, Solid dispersion, PXM 407, PXM 188, PEG 4000.

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Publication Date
Tue Jun 15 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Solubility and Dissolution Enhancement of Ebastine by Surface Solid Dispersion Technique
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Ebastine (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

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Publication Date
Thu Dec 06 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Enhancement of the Solubility and Dissolution Rate of Rebamipide by Using Solid Dispersion Technique (Part I)
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Solid 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

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique
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            Atorvastatin (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

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Publication Date
Sat Nov 04 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Solubility and Dissolution Enhancement of Atorvastatin Calcium using Phospholipid Solid Dispersion Technique
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Atorvastatin (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

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Enhancement of Solubility and Improvement of Dissolution Rate of Atorvastatin Calcium Prepared as Nanosuspension
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       Atorvastatin have problem of very slightly aqueous solubility (0.1-1 mg/ml). Nano-suspension is used to enhance it’s of solubility and dissolution profile. The aim of this study is to formulate Atorvastatin as a nano-suspension to enhance its solubility due to increased surface area of exposed for dissolution medium, according to Noyes-Whitney equation.

        Thirty one formulae were prepared to evaluate the effect of ; Type of polymer, polymer: drug ratio, speed of homogenization, temperature of preparation and inclusion of co-stabilizer in addition to the primary one; using solvent-anti-solvent precipitation method under high power of ultra-sonication.

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Publication Date
Sat Dec 11 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Formulation and Characterization of Nimodipine Nanoparticles for the Enhancement of solubility and dissolution rate
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Nimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which  Soluplus 

has been utilized as a stabilizer, has a par

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Publication Date
Mon Mar 25 2024
Journal Name
International Journal Of Drug Delivery Technology
Solubility and Dissolution Enhancement of Candesartan Cilexetil by Complexation with Cyclodextrin
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At present, numerous novel chemical compounds face challenges related to their limited solubility in aqueous environments. These compounds are classified under the Biopharmaceutical Classification System (BCS) as either class II or class IV substances. Different carriers were used to increase their solubility. Candesartan cilexetil (CC) is one of the most widely used antihypertensive drugs, which belongs to class II drugs. The aim of this research was to enhance the solubility and dissolution rate of CC through a complexation approach involving β-cyclodextrin and its derivatives, specifically hydroxypropyl beta cyclodextrin (HP-β-CD), methyl beta cyclodextrin (M-β-CD), and sulfonyl ether beta-cyclodextrin (SBE-β-CD), serving as

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Publication Date
Mon Jun 04 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Dissolution Enhancement of Raltegravir by Hot Melt Extrusion Technique
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The objective of the study to develop an amorphous solid dispersion for poorly soluble raltegravir by hot melt extrusion (HME) technique. A novel solubility improving agent plasdone  s630 was utilized. The HME raltegravir was formulated into tablet by direct compression method. The prepared tablets were assessed for all pre and post-compression parameters. The drug- excipients interaction was examined by FTIR and DSC. All formulas displayed complying with pharmacopoeial measures. The study reveals that formula prepared by utilizing drug and plasdone S630 at 1:1.5 proportion and span 20 at concentration about 30mg (trail-6) has given highest dissolution rate than contrasted with various formulas of raltegravir.

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Publication Date
Thu Nov 30 2023
Journal Name
Research Journal Of Pharmacy And Technology
Preparation and Evaluation of Aceclofenac Solid Dispersion by Fusion Technique and Effervescent Assisted Fusion Technique: Comparative Study
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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

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Publication Date
Thu Jun 09 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Improvement of the Solubility and Dissolution Characteristics of Risperidone via Nanosuspension Formulations
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Risperidone is an atypical antipsychotic drug that is used for treating schizophrenia, bipolar mania, and autism. Risperidone rebalances dopamine and serotonin to improve thinking, mood, and behavior by working on dopamine and serotonin α2receptor antagonism. Risperidone has poor solubility and high permeability through the intestine, so it belongs to Biopharmaceutical Classification System (BCS) class II exhibits poor oral biopharmaceutical properties.

 The aim of the present work was to improve solubility and dissolution of Risperidone by preparing nanosuspension using different stabilizers and different solvents‎ in a method known as solvent-antisolvent precipitation method.  Twenty-eight formulas were prepared

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