Aim: The present study aims to improve the poor water solubility of zaltoprofen which is a non-steroidal anti-inflammatory drug (NSAIDs) with a potent analgesic effect using solid dispersion then formulate it as a hollow type suppository to be more convenient for geriatric patients. Materials and Method: Zaltoprofen solid dispersions were prepared by solvent evaporation technique in different zaltoprofen: Soluplus® ratios. Results: Among the formulations tested, zaltoprofen solid dispersion preparation using 1:5 (zaltoprofen: Soluplus®) ratio showed the highest solubility and selected for further investigation. Solid dispersion characterization was evaluated by differential scanning calorimetry (DSC), X-ray diffraction study (XRD) and Fou
... Show MoreFebuxostat (FEB) is a potent, non-purine-selective inhibitor of xanthine oxidoreductase used to manage gout. Gout is a type of arthritis that occurs due to the accumulation of uric acid crystals in the joints, leading to inflammation and pain. According to the Biopharmaceutical Classification System (BCS), FEB was classified under class II drugs. The low dissolution rate of the drug determines its bioavailability at approximately 49%. Drug nanosizing, such as Nanosuspensions (NS), represents an exciting and potentially beneficial method to improve the bioavailability of hydrophobic drugs. This study aimed to prepare and characterize FEB NS to increase the dissolution rate, which can enhance its oral bioavailability. Using solvent/anti-so
... Show MoreAspirin and clopidogrel are considered the most important oral platelets aggregation inhibitors. So it is widely used for treatment and prophylaxis of cardiovascular and peripheral vascular diseases related to platelets aggregation .In this study aspirin and clopidogrel were formulated together as floating bilayer tablet system. Three different formulas of 75 mg aspirin were prepared by wet granulation method as immediate release layer; different disintegrants used to achieve rapid disintegration. Formula with crosscarmellose as disintegrant achieve rapid disintegration was selected for preparation of bilayer tablet.
Different formulas of 75 mg clopidogrel were prepared as sustained release floating layer by wet granulation (effe
... Show MoreFluoxetine (FX) is an antidepressant drug administered only orally in humans. Despite the wide use of FX, until now, there is only limited literature concerning the pharmacokinetics (PK) of FX and the effect of food on its PK. Thus, the objective of this investigation was to study the PK of FX in Arabic healthy male adult volunteers under fasting and fed conditions. In the fasting study, FX 20 mg capsules (Prozac®, Eli Lilly, Canada) were administered to 41 volunteers after overnight fasting of 12 hours, followed by blood sampling from each volunteer immediately before dosing (zero time) and then at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 24, 36, 48, 60, 72, 96, 120, and eventually at 144 hours after FX dosing. The fed study was conduct
... Show MoreIncreasing requests for modified and personalized pharmaceutics and medical materials makes the implementation of additive manufacturing increased rapidly in recent years. 3D printing has been involved numerous advantages in case of reduction in waste, flexibility in the design, and minimizing the high cost of intended products for bulk production of. Several of 3D printing technologies have been developed to fabricate novel solid dosage forms, including selective laser sintering, binder deposition, stereolithography, inkjet printing, extrusion-based printing, and fused deposition modeling. The selection of 3D printing techniques depends on their compatibility with the printed drug products. This review intent to provide a perspecti
... Show MoreLafutidine (LAF) a newly developed histamine H2-receptor antagonist with absorption window makes it a good candidate to be prepared as floating drug delivery system. The current study involves formulation and in- Vitro evaluation of lafutidine as floating microspheres. Different formulation variables that affect the physicochemical properties of the prepared microspheres besides to the drug release behavior were investigated. Fourteen formulas were prepared by emulsion (o/w) solvent evaporation method using Ethyl cellulose (EC) as the polymeric matrix and tween 80 (TW80) as an emulsifying agent. The prepared formulas were evaluated for their percentage buoyancy (%), Percentage yield (%) and Entrapment efficiency (EE %). The results obt
... Show MorePulsatile drug delivery systems (PDDS) are developed to deliver drug according to circadian behavior of diseases. They deliver the drug at the right time, action and in the right amount, which provides more benefit than conventional dosages and increased patient compliance. The drug is released rapidly and completely as a pulse after a lag time. These systems are beneficial for drugs with chrono-pharmacological behavior, where nighttime dosing is required and for the drugs having a high first-pass effect and having specific site of absorption in the gastrointestinal tract. This article covers methods and marketed technologies that have been developed to achieve pulsatile delivery. Diseases wherein PDDS are promising include asthma, peptic u
... Show MoreObjective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citri
... Show MoreCilnidipine is a dihydropyridine class of calcium channel blockers, it is classified as a BCS class II drug, characterized by a low oral bioavailability of 13%. Consequently, the utilization of nanoparticle preparation is anticipated to enhance its bioavailability. The objective of the research is to integrate cilnidipine nanoparticles into oral films as a means of enhancing patient adherence. The optimal polymers for producing Cilnidipine films were PVA cold and or HPMC E5 at different concentrations using a casting technique with glycerol as a plasticizer. The Nano suspension-based preparation of Cilnidipine's oral film containing the combination of polymers exhibited a significant enhancement in vitro dissolution, with a percentage excee
... Show MoreAtorvastatin calcium (ATR) is an antihyperlipidemic agent used for lowering blood cholesterol levels. However, it is very slightly soluble in water with poor oral bioavailability, which interferes with its therapeutic action. It is classified as a class II drug according to Biopharmaceutical Classification System (low solubility and high permeability).
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
... Show MoreBackground: Bilastine is a non-sedating, second-generation antihistamine used to treat urticaria and allergic conjunctivitis. Objective: to formulate and test bilastine as a mucoadhesive ophthalmic in situ gel in order to extend its presence at site for longer time and help treat conjunctivitis and allergic rhinitis. Methods: We prepared formulations using different concentrations of poloxamers (Poloxamer 407 (P407) and Poloxamer 188 (P188)) in combination with hydroxypropyl methyl cellulose (HPMC). The prepared formulas were evaluated for their physicochemical properties, sol-gel transition temperature, viscosity, mucoadhesive strength, drug release, and kinetic modeling. Results: The prepared in situ gels were clear and transparen
... Show MorePurpose: To validate a UV-visible spectrophotometric technique for evaluating niclosamide (NIC) concentration in different media across various values of pH. Methods: NIC was investigated using a UV-visible spectrophotometer in acidic buffer solution (ABS) of pH 1.2, deionized water (DW), and phosphate buffer solution (PBS), pH 7.4. The characterization of NIC was done with differential scanning calorimeter (DSC), powder X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). The UV analysis was validated for accuracy, precision, linearity, and robustness. Results: The DSC spectra showed a single endothermic peak at 228.43 °C (corresponding to the melting point of NIC), while XRD and FTIR analysis confirmed the identit
... Show MoreThe novel Vierordt’s approach, or simultaneous equation method, was created and validated for the concurrent determination of vincristine sulfate (VCS) and bovine serum albumin (BSA) in pure solutions utilizing UV spectrophotometry. It is simple, precise, economical, rapid, reliable, and accurate. This method depends on measuring absorbance at two wavelengths, 296 nm and 278 nm, which correspond to the λmax of VCS and BSA in deionized water, respectively. The calibration curves of VCS and BSA are linear at concentration ranges of 10–60 μg/mL and 200–1600 μg/mL, with correlation coefficient values (R2) of 1 and 0.999, respectively. The limits of detection (LOD) and quantification (LO
... Show MoreAcademic Entitlement (AE) is the expectation by students to receive high grades or preferential treatment without significant effort. Exploring AE from faculty perspective has not been investigated in Arab colleges of pharmacy. The aim of this study was to explore experiences and perceptions towards student AE among pharmacy faculty in the Arab World. A cross-sectional, self-administered, anonymous, electronic survey was sent to pharmacy faculty across pharmacy colleges in Arab countries. The survey collected demographic data, an AE measure including 17 items reflecting seven AE components, and faculty perceptions and perceived reasons for AE. A total of 345 responses were collected. The AE level wa
Ciprofloxacin is a broad spectrum fluoroquinolone, effective in the treatment of a wide range of infections, including genitourinary tract infections.In this study, bioadhesive vaginal tablets of ciprofloxacin hydrochloride were prepared by direct compression method using a combination of bioadhesivepolymers carbopol 934P(Cp), carboxymethylcellulose (CMC) and sodium alginate (SA) in different ratios.The prepared tablet formulations were characterized by measuring their swelling capacity, surface pH, bioadhesive properties, and in-vitro drug dissolution. It was found that the bioadhesive force was directly proportional to carbopol 934P content in different formulae and was further enhanced by the inclusion of carboxymethylcellulose.
... Show MoreOlmesartan medoxomil (OM) has low bioavailability and limited solubility. To enhance bioavailability, fast dissolving films (FDF) with mixed micelles of soluplus (SPL) and solutol HS15 (STL H15) were developed using solvent casting. The optimised formula, FM2, used polyvinyl alcohol (PVA) and showed high entrapment efficiency, rapid disintegration, and significant improvement in OM bioavailability compared to the market tablet (Olmetec®). FM2 also demonstrated stability and potential for enhanced drug delivery.
As a well-known oral and intravenous antifungal, voriconazole (VRN) has an extensive history of usage in the medical field. Solid lipid nanoparticles (SLNs) have been produced to treat ocular fungal keratitis in the eye. A 32Box-behnken design was used to produce a variety of new formulas for hot-melt extrusion. The SLNs were evaluated by entrapment efficiency (EE percent), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). A series of in-vitro and in-vivo studies were carried out on the new formula. The produced vesicles’ EE, PS, PDI, and ZP values were all good. SLNs eye drops were numerically adjusted to include carbopol, a stabilizer, lipids, and a surfactant, among other substances. ZP of -36.5 ± 0.20 m
... Show MoreBioavailability is the objective for an optimum formulation. The target of the analysis is to maximize both the fluidity and disintegration profile of class II weakly compounds that are water-soluble. Anti-dyslipidemia drug rosuvastatin calcium (RC) (bioavailability 20%) through formulating as nanofibers (NFs) using electrospinning (ES) technology. Twenty formulas were prepared, and different polymers and polymer combinations with various concentrations were used such as polyethylene oxide (PEO) polyvinyl pyrrolidine (PVPK-30), and hydroxypropyl methylcellulose (HPMC). Three distinct groups of maximum parameters, including polymeric solution, electrospinning method, and ambient parameter, are capable of influencing the creation alon
... Show MoreFlurbiprofen (FLB) is chemically 2-(3- fluoro-4-phenyl phenyl) propanoic acid. It is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of rheumatoid arthritis and osteoarthritis. Oral administration of this drug is associated with severe gastrointestinal side effects like ulceration and gastrointestinal bleeding. The solution to this problem lies in the fact that topically applied NSAIDs are safer than orally. This study aims to prepare different topical semisolid formulation of FLB as cream base (o/w), (w/o) and gel base using different gel-forming agents in different concentrations. Comparing characterization properties in addition to release and diffusion study for all the prepared formulas to select the best on
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