4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III whic
... Show MoreHypertrophic scars are fibroproliferative illnesses caused by improper wound healing, during that, excessive inflammation, angiogenesis, and differentiated human dermal fibroblast (HDF ) function contribute to scarring, whereas hyperpigmentation negatively affects scar quality. Over 100 million patients heal with a scar every year. To investigate the role of the beta 2 adrenergic receptor (β2AR); Ritodrine, in wound scarring, the ability of beta 2 adrenergic receptor agonist (β2ARag) to alter HDF differentiation and function, wound inflammation, angiogenesis, and wound scarring was explored in HDFs, zebrafish, chick chorioallantoic membrane assay (CAM), and a porcine skin wound model, respectively. A study identify a β2AR-mediated m
... Show MoreThe objective of the study was to develop microneedle (MN) patch, with suitable properties to ensure the delivery of a therapeutic level of lornoxicam (LXM) in a period suitable to replace parenteral administration in patients, especially those who fear needles. The used polymers were cold water-soluble polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP) of low molecular weight with PEG 400 as plasticizer and Tween 80 (to enhance the release) using micro molding technique. Patches were studied for needle morphology, drug content, axial fracture force measurement and drug release while the optimized formulas were further subjected to pH measurement, folding endurance, ex vivo permeation study, histopathology study, stability study and
... Show MoreA new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag
... Show MoreRecently, emulgel has emerged as one of the most interesting topical preparations in the field of pharmaceutics. In this research clotrimazole was formulated as topically applied emulgel ; different formulas were prepared. The prepared emulgels were evaluated for their physical appearance , rheological behaviour , and in vitro drug release . The influence of the type of gelling agent (carbopol 934 and methyl cellulose), the concentration of both the emulsifying agent (2% and 4% w/w of mixture of span 20 and tween 20) and the oil phase (5% and 7.5% w/w of liquid paraffin) and the type of oil phase (liquid paraffin and cetyl alcohol), on the drug release from the prepared emulgels was invest
... Show MorePiperine, a crystalline alkaloid compound isolated from Piper nigrum, piper longum, and other types of piper, has had many fabulous pharmacological advantages for preventing and treating some specific diseases, such as analgesic, anti-inflammatory, hepatoprotective, antimetastatic, antithyroid, immunomodulatory, antitumor, rheumatoid arthritis, osteoarthritis, Alzheimer's, and improving the bioavailability of other drugs. However, its potential for clinical use through oral usage is hindered by water solubility and poor bioavailability. The low level of oral bioavailability is caused by low solubility in water and is photosensitive, susceptible to isomerization by UV light, which causes piperine concentration to decrease. Many different
... Show MoreSolubility problem of many of effective pharmaceutical molecules are still one of the major obstacle in theformulation of such molecules. Candesartan cilexetil (CC) is angiotensin II receptor antagonist with very low water solubility and this result in low and variable bioavailability. Self- emulsifying drug delivery system (SEDDS) showed promising result in overcoming solubility problem of many drug molecules. CC was prepared as SEDDS by using novel combination of two surfactants (tween 80 and cremophore EL) and tetraglycol as cosurfactant, in addition to the use of triacetin as oil. Different tests were performed in order to confirm the stability of the final product which includes thermodynamic study, determination of self-emulsificat
... Show MoreThree new hydrazone derivatives of Etodolac were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy, and 1HNMR analysis. The synthesis of the target (P1-P3) compounds was accomplished following multistep reaction procedures. The synthesized target compounds were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac).
Three Schiff bases from Benzaldehyde and Salicylaldehyde have been synthesized (A, 1and 2) and two of them (1and 2) have been tested for anti-inflammatory activity. The p-aminobenzene sulfonamide has been synthesized from acetanilide through the addition of excess chlorosulfonic acid then concentrated ammonia solution; Schiff base of this derivative (2) exhibited good level of activity against egg-white induced edema in rat hind paw, while the other tested derivative exhibited no activity.
Key words: Schiff bases, sulfonamide derivatives, salicylaldehyde
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
... Show MoreThe plant Borago officinalis, which belongs to the Boraginaceae family and Celebrated as borage, is one of the useful medicinal plants cultivated in Iraq. It was used in olde medicine in Iraq, Irane, Syria and Europe for management of various diseases. It is commonly used as an atonic, tranquilliser, management of cough, sore throat, pneumonia, swelling, inflammatory diseases, antioxidant, and anticancer. This project provides the first comprehensive research done in Iraq to study the phytochemicals and the methods of extraction and isolation of active constituents from Borago officinalis cultivated in Iraq. The plant was harvested in spring from AL-Rifai, Nassiriyah city, IRAQ in February 2019.were w
... Show MoreBromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes ,the oral bioavailability is approximately 6%, therefore aim its prepare and evaluate bromocriptine mesylate as liquid self nano emulsifying drug delivery system to enhance its solubility , dissolution and stability . Solubility study was made in different vehicles to select the best excipients for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios of surfactant and co-surfactant, four formulations were pre
... Show MoreDarifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated overactive bladder (OAB). This study was aimed to formulate DH as fast dissolving buccal films (FDBFs) using a solvent casting method to enhance patient’s compliance.
Films were prepared by using polyvinyl alcohol (PVA) as a film forming polymer. Different types and concentrations of superdisintegrants (croscarmellose sodium, sodium starch glycolate, indion 414) were used to select the best formula by studying the physicochemical properties of the films, disintegration time (DT) and percent drug release.
&nb
... Show MoreSilybum marianum, from which silymarin (SM) is extracted, is a medicinal herb. In the Biopharmaceutics Classification System, it is of the class II type, meaning it is almost completely insoluble in water. It has a number of therapeutic properties, including anti-inflammatory as well as properties that promote wound healing.
This research target is to promote the dissolution and solubility of SM by employing a technique called solid dispersion and then incorporating the formula of solid dispersion into a topical gel that can be used for wound healing.
Solid dispersion is a technique used to enhance solubility and dissolve pharmaceuticals that are not water-soluble. This method is widely used because of its low cos
... Show MoreThis work targeted studying organogel as a potential floating system. Organgel has an excellent viscoelastic properties, floating system posses a depot property. Different formulations of 12-hydroxyoctadecanoic acid (HOA) in sesame oil were gelled and selecting F1, F3 and F5 HOA organogels for various examinations: tabletop rheology, optical microscopy, and oscillatory rheology studies. Also, the floating properties studies were conducted at in vitro and in-vivo levels. Lastly, the in-vitro release study using cinnarizine (CN) was to investigate the organogel depot property. Based on the results, the selected concentrations of HOA in sesame oil organogels showed temperature transitions fr
... Show MoreThe most prevalent chronic complication of diabetes mellitus is diabetic neuropathy. The pathogenesis of diabetic neuropathy is exacerbated by hyperglycemia-induced oxidative stress, which causes nerves to deteriorate in a programmed manner. Many clinical trials depend on supplement in an attempt to improve neuropathy symptoms such as (pain & tingling) and patient quality of life, one of them is Coenzyme Q10 which is reported to have an anti-inflammatory and antioxidant effects, and was totally nontoxic and non-reported side effects. This study aimed to evaluate using a Coenzyme Q10 supplement as an adjuvant therapy to gabapentin to improve the clinical symptoms of diabetic neuropathy in relation to its anti-inflammatory and antioxid
... Show MoreBiological drugs have an active substance that is made by a living organism or derived from a living organism. They are one of the important therapy options used in a wide range of diseases especially life-threatening diseases. Biological therapy opens new opportunities for treating different diseases for which drug therapy is minimal, but they have considerable differences in the safety consequences in comparison with non-biological drugs. The aim of the current study was to assess the post-marketing safety profile of biological drugs used in Iraqi hospitals by the analysis of the reported adverse drug reactions regarding their severity, seriousness, preventability, expectedness, and outcome. It is a retrospective study of the individu
... Show MorePatients with decompensated cirrhosis have typically prescribed a combination of therapeutic and prophylactic medications. Polypharmacy increases the probability of medication errors and drug related problems. Clinical pharmacists are highly effective at identifying, resolving, and preventing clinically important drug-related problems in their patients' care. The objectives of the study were the identification and classification of drug-related problems, as well as the discussion of these problems with health care providers (physicians, pharmacists, and nurses) and patients. Reduce their incidence as effectively as possible and educate all research participants on the significance of following their prescribed drug regimen
... Show MoreABSTRACT
Ticagrelor is an orally administered antiplatelet medicine, direct-acting P2Y12-receptor antagonist. Ticagrelor binds reversibly and noncompetitively to the P2Y12 receptor at a site distinct from that of the endogenous agonist adenosine diphosphate (ADP). Inhibition of platelet aggregation stimulated by ADP is a commonly used pharmacodynamic parameter for P2Y12-receptor antagonists.
Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10?g/mL at room temperature.
... Show MoreThis study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential activity as antimicrobial and/or cytotoxic. Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases.
These pharmacological properties of quinolones aroused our interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linke
... Show MoreNebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formul
... Show MoreIn Iraq, there is a limited research work exploring the clinical pharmacists' role from the point of view of other healthcare professionals.
To investigate physicians' assessment of clinical pharmacy services at Baghdad hospitals, and compare junior physicians with senior physicians' point of view.
The study was conducted in twelve governmental hospitals in Baghdad, Iraq. Data was collected from a sample of two hundred physicians, and through a validated, self-administered questionnaire, which comprised twenty statements in addition to a non-personal information form that precedes the questionnaire
The study findings reveal a somewhat positive point of view towards clinical pharmacists' performance in
... Show More