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Formulation and Evaluation of Ezetimibe Nanoparticles
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The aim of this study is to formulate and evaluate ezetimibe nanoparticles using solvent antisolvent technology. Ezetimibe is a practically water-insoluble drug which acts as a lipid lowering drug that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe prepared as nano particles in order to improve its solubility and dissolution rate.

Thirty formulas were prepared and different stabilizing agents were used with different concentrations such as poly vinyl pyrrolidone (PVPK-30), poly vinyl alcohol (PVA), hydroxy propyl methyl cellulose E5 (HPMC), and poloxamer. The ratios of drug to stabilizers used to prepare the nanoparticles were 1: 2, 1:3 and 1:4.

The prepared nanoparticles were evaluated for particle size, entrapment efficiency, dissolution study, Fourier transform infrared spectroscopy, differential scanning calorimetry, and atomic force microscopy. The percentage of drug entrapment efficiency of F1-F30 was ranged from 85% ± 1 to 98 % ± 1. On the other hand dissolution rate increasing as the particle surface area is increase due to reduction of particle size to the nano range.

The results showed that poly vinyl pyrrolidone (PVPK-30) was found to be the best stabilizer.

 Keywords: Ezetimibe, Nanoparticles, Particle Size, poly vinyl alcohol.

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
In Situ Gelling Formulation of Naproxen for Oral Sustained Delivery System
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Naproxen is non-steroidal anti-inflammatory drug, which has antipyretic and anti-inflammatory effect. It is extensively bound to plasma albumin, and exhibits gastric toxicity, so it may be more efficient to deliver the drug in its sustained release dosage form and adequate blood level is achieved. Three liquid formulations with in situ gelling properties have been assessed for their potential for the oral sustained delivery of naproxen . The formulations were dilute solutions of: (a) pectin; (b) gellan gum and; (c) sodium alginate, all containing complexed calcium ion that form gels when these ions are released in the acidic environment of the stomach . The viscosity of the sols and drug release were measured, and was found to be depende

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Publication Date
Fri Nov 03 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Diacerein Loaded Novasome for Transdermal Delivery: Prepartion , In-Vitro Characterization and Factors Affecting Formulation
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Diacerein (DCN) is a semi-synthetic anthraquinone derivative of Rhein that is indicated for the management of osteoarthritis. Diacerein exhibits poor dissolution in the GIT fluids and suffers from low bioavailability upon oral administration in addition to the laxative effect of Rhein metabolites. The aim of the present study was to develop novasomal vesicles with optimized entrapment efficiency and size to serve as a carrier for transdermal delivery of diacerein. Novasomal vesicles were prepared by thin film hydration method thin film hydration. The prepared vesicles were optimized utilizing different surfactant to cholesterol molar ration, sonication type, different sonication times and varying fatty acid level. The prepared vesicles were

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Publication Date
Sat Aug 28 2021
Journal Name
Journal Of Pharmaceutical Research International
Effect of Formulation Parameter on Dissolution Rate of Flurbiprofen Using Liquisolid Compact
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Attempts were made to improve solubility and the liquisolid technology dissolving of medication flurbiprofen. Liquisolid pill was developed utilizing transcutol-HP, polyethylene glycol 400, Avecil PH 102 carrier material and Aerosil 200 layer coating material. Suitable excipient amounts were determined to produce liquisolid powder using a mathematical model. On the other hand, flurbiprofen tablet with the identical composition, directly compressed, was manufactured for comparison without the addition of any unvolatile solvent. Both powder combination characterizations and after-compression tablets were evaluated. The pure drug and physical combination, and chosen liquisolid tablets were studied in order to exclude interacting with t

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Development of Modified Release Nicotine Tablet Formulation for Treatment of Ulcerative Colitis
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One of the therapeutic effects of nicotine  is used as  a protective against developing ulcerative colitis . ulcerative colitis is an inflammatory disease of the bowel affecting the superficial lining mucosa in the rectum and large intestine. In this study nicotine tablets were formulated as modified release tablets targeted to the colon. All formulas were studied for drug release , effect of diluent, retardant concentration, avicel grade,and compression force, the selected formula was then further studied for drug release in 3 different pH ( coated tablets) .The kinetic study revealed acceptable shelf life  . Finally the selected formula was given to 6 patients in a pre-liminary clinical study which showed that nicotine c

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Publication Date
Fri Jun 16 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Assessment of Delayed/Slow-Release Diclofenac Sodium Edible Organogel Utilizing Low Molecular Weight Organogelators
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Organogel as a system was to estimate its capacity to delay and slow the drug release in the duodenum. The gelators, 12HSA (12-hydroxystearic acid), span 60. span 40 were used; the castor oil (CO) and anise oil (AO) also represented the liquid phase. To achieve the goal of this work was by using diclofenac sodium (DS). Organogels specifications were by estimating thermal attitude using tabletop rheology and differential scanning calorimetry (DSC). The organogel strength study was by applying oscillatory rheology tests the amplitude sweep and the frequency sweep. Realizing the morphology of the organogel was done utilizing an optical microscope. CO and AO binding capacity was also manifested. The transition temperatures for all organogels

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Publication Date
Thu Jul 04 2024
Journal Name
Pharmaceutics
Formulation Development of Meloxicam Binary Ethosomal Hydrogel for Topical Delivery: In Vitro and In Vivo Assessment
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Abstract: The article aimed to formulate an MLX binary ethosome hydrogel for topical delivery to escalate MLX solubility, facilitate dermal permeation, avoid systemic adverse events, and compare the permeation flux and efficacy with the classical type. MLX ethosomes were prepared using the hot method according to the Box–Behnken experimental design. The formulation was implemented according to 16 design formulas with four center points. Independent variables were (soya lecithin, ethanol, and propylene glycol concentrations) and dependent variables (vesicle size, dispersity index, encapsulation efficiency, and zeta potential). The design suggested the optimized formula (MLX−Ethos−OF) with the highest desirability to perform the

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Publication Date
Sat Sep 01 2018
Journal Name
King's College London
A novel sol-gel silica formulation for management of methadone hydrochloride abuse
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Introduction: Methadone hydrochloride (MDN) is an effective pharmacological substitution treatment for opioids dependence, adopted in different countries as methadone maintenance treatment (MMT) programmes. However, MDN can exacerbate the addiction problem if it is abused and injected intravenously, and the frequent visits to the MMT centres can reduce patient compliance. The overall aim of this study is to develop a novel extended-release capsule of MDN using the sol-gel silica (SGS) technique that has the potential to counteract medication-tampering techniques and associated health risks and reduce the frequent visits to MMT centres. Methods: For MDN recrystallisation, a closed container method (CCM) and hot-stage method (HSM) were conduc

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Publication Date
Fri Nov 03 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Study the Variables Affecting Formulation of Ethylcellulose-based Microsponges Loaded with Clobetasol
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Clobetasol propionate (CP) is a super potent corticosteroid widely used to treat various skin disorders such as atopic dermatitis and psoriasis. However, its utility for topical application is hampered due to its common side effects, such as skin atrophy, steroidal acne, hypopigmentation, and allergic contact dermatitis. Microsponge is a unique three-dimensional microstructure particle with micro and nano-meters-wide cavities, which can encapsulate both hydrophilic and lipophilic drugs providing increased efficacy and safety. The aim of the current study is to prepare and optimize clobetasol-loaded microsponges. The emulsion solvent diffusion method is used for the preparation of ethylcellulose (EC)-based microsponges. The impact of

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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation of Alpha Tocopherol Acetate as a Powder Dosage Form by Adsorption
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Alpha-tocopherol acetate is one of the most important vitamin E derivatives,that were used  as antioxidants. Adsorbents like kaolin, magnesium carbonate, and microcrystalline cellulose were used successfully to incorporate oily alpha-tocopherol acetate into an acceptable powder dosage form. The results revealed that microcrystalline cellulose as an adsorbents gave the best results with 50% loading capacity at time, 8 minutes before and after incubation period (3 months at 30C°), while kaolin and magnesium carbonate have been shown a significant difference before and after incubation. Addition of 1% w/w magnesium carbonate to the kaolin enhanced the loading capacity by decreasing the time of adsorption from 20 to 6 minutes and 47

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation of Metoprolol Bilayer Tablets as an Oral Modified Release Dosage Form
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Metoprolol is a β1 adrenergic blocker used in treatment of heart diseases. Metoprolol (100mg) tablets was formulated as a modified release oral system utilizing the concept of bilayer system, first layer contained (30mg) as immediate release and the other (70mg) in the sustained release matrix.  The immediate release layer consisted of lactose or microcrystalline cellulose as diluents with sodium starch glycolate or sodium croscarmellose as disintegrants. The result showed that the layer contains microcrystalline cellulose and 2% sodium starch glycolate gave disintegration time similar to that of conventional metoprolol tartrate tablet. This result was subjected in the subsequent preparation of the bilayer tablet. The

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