The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
Antacids are commonly used drugs which are considered inert and free of pharmacological effect by many patients and physicians. They are weak bases that neutralize the gastric acid and relief pain. These weak bases dissociate to neutralize gastric acid and form neutral salts. The ultimate goal of antacid therapy is to reduce the concentration and a total load of acid in gastric juice to a pH 4 - 5. This in vitro study was promised to study the acid neutralizing capacity (ANC) of six commonly available antacids tablets in the Iraqi market by using back titration method. The highest ANC values were for Rennie (17.131± 0.083 and 16.926± 0.052 mEq) in two different hydrochloric acid (HCl) concentrations 1N and 0.5 N, respectively. The static
... Show MoreABSTRACTObjective: The objective of this study is to develop a controlled release matrix tablet of candesartan cilexetil to reduce the frequency of administration,enhance bioavailability and improve patient compliance; a once daily sustained release formulation of candesartan cilexetil is desirable.Methods: The prepared tablets from F1 to F24 were evaluated with different evaluation parameters like weight variation, drug content, friability,hardness, thickness and swelling ability. In vitro release for all formulas were studied depends on the type and amount of each polymer, i.e. (16 mg,32 mg and 48 mg) respectively beside to the combination effect of polymers on the release of the drug from the tablet.Results: In vitro release show
... Show MoreBackground: The estimation of ferritin and related variables by complete serum iron profile, for Iraqi hashimoto’s patients to see the effect of thyroid hormone insufficiency, which may lead to deficiency of ferritin iron stores, this may be quite useful during the diagnosis and treatment of hashimoto’s patients. Patients and Method: The study was performed at National Center of Teaching laboratories of Medical city institute in Baghdad. Fifty newly diagnosed patients with hashimoto’s and forty apparently healthy controls. Diagnosis based on thyroid profile analysis including:Thyroid Stimulating Hormone (TSH), Thyroxine (totalT4) and Triiodothyronine (total T3), estimation of antibodies against thyroperoxidase, iron profile including:
... Show MoreObjective: This study goal was to screen participants from different settings in Baghdad for depression using Beck Depression Inventory (BDI) scale and identify factors influencing the levels of depression. Methods: This cross-sectional study included a convenience sample of 313 people from four settings (teaching hospital, college of medicine, college of pharmacy, and high school) in Baghdad, Iraq. The participants were screened using paper survey relying on the BDI scale during spring 2018. Using multiple linear regression analysis, we measured the association between depression scores and six participant factors. Results: The overall prevalence of depression in our sample was 57.2%. Female participants had higher BDI
... Show MoreIbuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard
... Show MorePathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic
... Show MorePharmaceutical companies assign a budget for activities and promotions that aim to change the prescription habits of the physicians to choose the most suitable medications for their patients, which will eventually grow their sales. The study's objectives were to explore physicians' and medical representatives' perspectives on the criteria of impactful professional PP and the factors influencing the interaction between physicians and medical representatives. Qualitative in-depth interviews with flexible probing techniques were carried out in 2023. A semi-structured, open-ended interview questionnaire was used to interview physicians and medical representatives (MRs) from different private clinics in several governorates in Iraq. Ten physicia
... Show MoreThis research included the study of different factors that may effect on gatifloxacin stability (anew quinolone synthetic antibacterial agent) in its aqueous solution in order to develop and optimize the best delivary of the drug to the eye (as eye drop) with maximum local concentration and minimum systemic absorption and toxicity.Different formulas of gatifloxacin solution for ophthalmic use (0.3%)w/v were prepared in citrate, acetate,citrate/phosphate and phosphate buffers,their tonicity adjusted with suitable quantity of sodium chloride.The effect of different factors that might affectthe stability of gatifloxacin in its prepared ophthalmic solution was studied and determined spectrophotometrically at 287 nm. The results showed t
... Show MoreTransdermal drug delivery has made an important contribution to medical practice but has yet to fully achieve its potential as an alternative to oral delivery and hypodermic injections. Transdermal therapeutic systems have been designed to provide controlled continuous delivery of drugs through the skin to the systemic circulation. A transdermal patch is an adhesive patch that has a coating of drug; the patch is placed on the skin to deliver particular amount of drug into the systemic circulation over a period of time. The transdermal drug delivery systems (TDDS) review articles provide information regarding the transdermal drug delivery systems and its evaluation process as a ready reference for the research scientist who is involved
... Show MoreThe purpose of this research work is to synthesize conjugates of NSAIDs (ibuprofen, and naproxen) with sulfadiazine as possible mutual prodrugs to overcome the local gastric irritation of NSAIDs with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo bond that undergo reduction only by colonic bacterial azoreductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
Bilosomes are nanocarriers that contain bile salts in their vesicular bilayer, thereby enhancing their flexibility and durability in the gastrointestinal tract. Unlike conventional vesicular systems they provide distinct advantages such as streamlined manufacturing procedures, cost efficiency, and improved stability. The main objective of this study was to attain a comparison of the pharmacokinetic parameters of nisoldipine (NSD) after administering an ordinary NSD suspension and an NSD-loaded bilosome suspension. The study used 60 Swiss albino rats weighing 200±15 g and divided into two groups (n=30 each). A dose of 2.2 mg/kg of NSD was administered from the ordinary NSD suspension to the rats of the first group and the same dose
... Show MoreIbuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard compoun
... Show MoreObjectives: To study the prevalence of rs1799964 (-1031 T/C) and rs361525 (- 238 G/A) SNPs and their effect on the disease activity, severity, and cytokines production in newly diagnosed Iraqi rheumatoid arthritis patients. Patients and Methods: sixty-three patients were diagnosed by a specialist physician while attending the rheumatology unit and twenty control participated. The inflammatory markers were measured and PCR amplification and sequencing were performed to demonstrate TNF-α SNPs. Results: Regarding (-1031 C/T) SNP, the TT genotype and allele C were significantly present in the controls, and the CT genotype was distributed significantly in the patients. The TT genotype was mostly distributed in the mild-moder
... Show MoreObjective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement sho
... Show MoreThe objective of this study is to determine levels of some pro-inflammatory cytokines (IL-12 and SIL-2R) in pregnant women with polycystic ovary syndrome (PCOS) and also to determine incidence of spontaneous abortion during first trimester in pregnant women with PCOS compared with non-PCOS pregnant women. This Study was performed on (93) women, consisted of: 1- (63) pregnant women during the first trimester, which included:A- (33)PCOS pregnant women and subdivided into the following groups: (20) successful pregnant PCOS, (7) blighted Ovum PCOS and (6) missed abortion PCOS. B- (30) non-PCOS pregnant women, which included: (27) successful pregnant control and (3) non-PCOS pregnant women were withdrawn from this study because of their abortion
... Show MoreThe aim of the current study was to evaluate the knowledge and perception of the fifth stage pharmacy students (college of pharmacy/ University of Baghdad /Iraq) regarding generic medicines. This study is a cross-sectional study carried in a college of pharmacy /University of Baghdad during the period from (November 2018- March 2019). The number of students included in the current study was 168 undergraduate stager pharmacists. A questionnaire was used to collect data of the study. Nearly 86% of the students said that they had heard of generic and brand medicines, and pharmacy was the main source of knowledge regarding generic medicines (66.7%). About (33.3%) of the respondents agreed that generic medicines are bioequivalent to br
... 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 MoreAbstract:
Background: Retinol binding protein 4 (RBP4), an adipokine that participate in a lipid metabolism or insulin resistance through a complex regulatory network. Recently, RBP4 was reported to be associated with many cardiovascular diseases (CVDs) risk factors in patients of type 2 diabetes mellitus (T2DM). This study aims to study the correlation of serum RBP4 with some markers of glycemic control, dyslipidemia, hypertension and obesity in T2DM Iraqi patients.
Subjects and Methods: one hundred fifty participants were enrolled in this coss-sectional study, 120 of participants were T2DM patients and 30 were apparently healthy individuals to serve as control gro
... 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 More3-coumarin/chalcone B1/B2/B3 hybrids served as malleable antecedents for the development of novel bioactive pharmacophores. In this study, the matching coumarin-chalcones hybrid was obtained from 3-acetylcoumarin (comp A) via condensation with several aromatic aldehydes in ethanolic piperidine solution. To further modify these hybrids, we reacted them with thiourea in the presence of base in ethanol, yielding pyrimidine derivatives C1, C2, and C3. Their chemical characteristics and spectroscopic data were used to characterize the newly synthesized heterocyles. The antibacterial efficacy of all freshly produced compounds was tested. Compound (C3) was shown to have the highest antibacterial activity against both gram positive and gram nega
... Show MoreBackground: Pharmacy internship programmes are driven by most developed countries to outweigh the ongoing growth in the pharmacy career which encourages pharmacists to play a significant role as healthcare providers. Objectives: This study examines pharmacy students' perception, satisfaction, challenges, and limitations with the internship curriculum. Method: A cross-sectional study was conducted using an online survey with different elements to examine students' perceptions of various aspects. Result: Most students reported a positive impression regarding their internships, however, they were less satisfied with the allowance for filling prescriptions and compounding also, the college's follow-up was inadequate. F
... Show MoreObjective: The aim of this work was to detect terpenes other than boswellic acid derivatives in olibanum of Boswellia Serrata found in Iraq. Methods: The olibanum of Boswellia Serrata was macerated in methanol for one day, then filtration. Filter at was concentrated till reddish brown syrupy residue was gained, (3%) potassium hydroxide was added till basification. This basic solution was stirred continuously until a uniform emulsion was formed, then extracted with chloroform in a separatory funnel; the chloroform fraction was analyzed by GC /MS spectrometry. Results: GC /MS analysis reveal the presence of terpenes and non-terpenes constituents. Conclusion: Most of the detected terpenes were sesquiterpenes and the least one was di-terpenes.
Objective: The study aimed to assess Leucine-rich alpha-2-glycoprotein-1 biomarker serum level in hospitalized COVID-19 patients. Methods: The case control study from multi-centers in Baghdad included 45 adult patients (19 females and 26 males) with COVID-19, diagnosed with a positive real-time reverse transcription polymerase chain reaction and excluded negative RT-PCR for COVID-19 and comorbidity conditions. Second group, was 43 control (20 females and 23 males). Results: This study found a decrease Leucine-rich alpha-2-glycoprotein-1 biomarker serum level in these patients and a significant difference in D. dimer, neutrophil count, lymphocyte count, and the neutrophil-lymphocyte ratio between the patients and controls at a P valu
... 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.
Objective: Schiff’s and Mannich bases of isatins are an important group of heterocyclic compounds which are of great importance in medicinal chemistry as antimicrobial agents. In the vision of these facts, new bis-Schiff bases and Mannich bases of isatins were synthesized. Methods: Three different bis-Schiff bases (3a-c) have been synthesized by reacting isatin, 5-fluoroisatin and 5-methoxy isatin with thiophene-2- carboxaldehyde using hydrazine hydrate to link between the carbonyl compounds, and then these bis- Schiff bases were condensed with two different secondary amines (piperidine and morpholine) separately, and formaldehyde to form the Mannich bases (4a-c and 5a-f), respectively. Results: The structures of the newly synthesized com
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