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Bioequivalence and Pharmacokinetics Comparison of Two Formulations of Extended-Release Pentoxifylline Tablets in Healthy Subjects after Fasting and Fed Conditions
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The pharmacokinetics and bioequivalence of a newly developed extended-released (ER) tablet containing 400 mg pentoxifylline as a test product was compared with the reference brand product Trental® 400 mg ER tablet produced by Sanofi-Aventis. Two separate studies were conducted simultaneously. The first study was conducted under fasting condition, whereas, the second study was conducted under fed condition; using the same batches of the test and reference products in both studies. In each study, both products were administered to 32 healthy male adult volunteers applying a single-dose, two-treatment, two-period, two-sequence, randomized crossover design with one-week washout period between dosing. Twenty two blood samples were withdrawn from each volunteer over 24 hours period.  Pentoxifylline concentrations were determined in plasma by a validated HPLC method according to FDA Bioanalytical Method Validation Guidance using UV detection and chloramphenicol as internal standard. The lower limit of quantitation of the drug in plasma was 5 ng/ml and the upper limit of quantitation was 500 ng/ml. From the plasma concentration-time data of each individual, the pharmacokinetic parameters; Cmax,  AUC0-t, AUC0-Â¥, Cmax/AUC0-Â¥, Tmax, lZ & T0.5; were calculated applying non-compartmental analysis. Data of the test and reference products were statistically analyzed to test for bioequivalence of the two products, using criteria of FDA and EMEA Guidance.  The pharmacokinetic parameters mentioned above were statistically analyzed by descriptive statistics, ANOVA test and 90% Confidence Interval (CI). ANOVA test involved the calculation of the effects of: treatment, period, sequence and subjects nested in sequence. According to the above guidance, the primary pharmacokinetic parameters used for bioequivalence testing, namely Cmax, AUC0-t and AUC0-Â¥ were also statistically analyzed by ANOVA & CI tests using the corresponding Ln-transformed values. The mean values  Cmax,  AUC0-t , AUC0-Â¥ , Cmax/AUC0-Â¥ , Tmax, lZ & T0.5 for the test formula obtained from the fasting study  were; 144.4 ng/ml,  845.4 ng.hr/ml, 868.4 ng.hr/ml, 0.186 hr-1, 3.29 hr, 0.561 hr-1 and 1.65 hr, respectively; and the mean values of these parameters for the reference formula were; 150.0 ng/ml,  871.1 ng.hr/ml, 893.7 ng.hr/ml, 0.177 hr-1, 3.70 hr, 0.558 hr-1 and 1.59 hr,  respectively.  The mean values of the above mentioned parameters for the test formula obtained from the fed study were; 157.8 ng/ml, 826.5 ng.hr/ml, 853.8 ng.hr/ml, 0.198 hr-1, 5.4 hr, 0.458 hr-1 and 2.06 hr, respectively; and the mean values of these parameters for the reference formula were; 162.1 ng/ml, 869.7 ng.hr/ml, 894.8 ng.hr/ml, 0.196 hr-1, 4.1 hr, 0.525 hr-1 and 1.80 hr, respectively.  Based on criteria of FDA and   EMEA Guidance on Bioavailability and Bioequivalence, the results of the fasting and fed studies demonstrated bioequivalence of the two products under either condition. Accordingly, it is concluded that the newly developed ER tablet containing 400 mg pentoxifylline is bioequivalent to Trental® 400 mg ER tablet produced by Sanofi-Aventis.

Keywords: Pentoxifylline, Pharmacokinetics, Bioequivalence.

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Publication Date
Thu Jun 23 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Flow Injection Spectrophotometric Technique for Determining of Genistein in Pure and Supplements Formulations Through Diazotization Coupling Reaction
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Genistein (GEN) is The major isoflavone found in soybeans, has a number of cardiovascular health benefits, Postmenopausal syndrome and osteoporosis. A direct flow injection analysis method for estimation of (GEN) in pure and supplements formulation . This system is based on diazotization coupling reactions between procaine penciline (PR) and genistein in basic medium, they formed yellow dyes have maximum absorption at 416 nm. Calibration curve were constructed over different GEN concentrations, linearity for GEN was 10-100 µg.mL-1 and detection limits of 1.51 ?g/mL. In the FIA technique, all analytical factors were analyzed and optimized. The established method was successfully used to determine GEN in the formulations of its supplement

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Publication Date
Fri Jan 19 2024
Journal Name
Turkish Journal Of Pharmaceutical Sciences
Taste Masking of Steroids for Oral Formulations
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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)
Controlled Release Floating Matrix Tablet of Captopril
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The present study was done to prepare a gastroretentive floating tablet of captopril (CAP) which is an angiotensin converting enzyme inhibitor (ACE-inhibitor) used in the treatment of hypertension and heart failure. CAP is mainly absorbed from the proximal intestine and to a lesser extent from the stomach, also CAP stability decreases as the pH raised above 1.2 and this makes it a suitable candidate for floating dosage form.Effervescent floating tablets of CAP were prepared in order to prolong the gastric residence time and increase the bioavailability of the drug. The floating tablets of CAP were prepared by direct compression and wet granulation technique, using the polymer hydroxypropylmethylcellulose (HPMC) as the primary retarding p

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Publication Date
Sat Jun 30 2018
Journal Name
International Journal Of Medical Research & Health Sciences
Assessment of the Healthy Women by Detection and Determination of Cells in Conventional Pap Stained Cervical Smear Images
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Introduction: A Pap test can detect pre-cancerous and cancerous cells in the vagina and uterine cervix. Cervical cancer is the easiest gynecologic cancer to be prevented and diagnosed using regular screening tests and follow-up. This study aimed to estimate the cytological changes and the precancerous lesions using Pap smear test and visual inspection of the cervices of Iraqi women, and also to determine the possible relationship of this cancer with patients’ demographic characteristics. Methods: The study included 140 women aged (18-67) years old referred to the National Cancer Research Center (NCRC), Baghdad, Iraq, during the period 2011-2016. Both visual inspections of the uterine cervix and Papanicolaou smear screening were performed

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Publication Date
Tue Dec 20 2022
Journal Name
Biomedical And Pharmacology Journal
Phytochemical Comparison Study for Evaluating the Hypolipidemic Effect Between Two Iraqi Pepper Spp in the Rats Model.
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Hypercholesterolemia is a predominant risk factor for atherosclerosis and cardiovascular disease (CVD). The World Health Organization (WHO), ) recommended reducing the intake of cholesterol and saturated fats. On the other hand, limited evidence is available on the benefits of vegetables in the diet to reduce these risk factors, so this research was conducted to compare the hypolipidemic effect between the extracts of two different types of Iraqi peppers, the fruit of the genus Capsicum traditionally known as red pepper extract (RPE), and Piper nigrum as black pepper extract (BPE), respectively, in different parameters and histology of the liver of the experimental animals. The red pepper was extracted by ethyl acetate, while the black pepp

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Publication Date
Thu Oct 01 2015
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Effect of 1,3-Oxazepine Derivative on Alkaline Phosphatase and Lactate Dehydrogenase Activity in Healthy Iraqi Females Serum
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Background: Heterocyclic compounds and its derivatives have biological activities and used as analgesic, anti-helminthic, antituberculer, antifungal, antiviral, anticancer and inhibitor of some enzymes. Oxazepine (benzodiazepine) derivative used in relief of psychoneuroses characterized by anxiety and tension. Alkaline phosphatase (ALP) hydrolyzes phosphate monoesters, while Lactate dehydrogenase (LDH) catalyses oxidation of L-lactate to pyruvate utilizing NAD+Objective: The study was carried out to know of the impact of 1,3-oxazepine derivative on the ALP and LDH enzyme activity on human serum in vitro.Methods: The study included the effect of synthesized 1,3-oxazepine divertive [(Z)-3-(5-mercapto-1-3,4-Thiadizol-2-yl)-2-(4-nitroph

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Publication Date
Wed Dec 01 2021
Journal Name
Journal Of Economics And Administrative Sciences
Comparison Between Nelson-Olson Method and Two-Stage Limited Dependent Variables (2SLDV ) Method for the Estimation of a Simultaneous Equations System (Tobit Model)
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This study relates to  the estimation of  a simultaneous equations system for the Tobit model where the dependent variables  ( )  are limited, and this will affect the method to choose the good estimator. So, we will use new estimations methods  different from the classical methods, which if used in such a case, will produce biased and inconsistent estimators which is (Nelson-Olson) method  and  Two- Stage limited dependent variables(2SLDV) method  to get of estimators that hold characteristics the good estimator .

That is , parameters will be estim

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Publication Date
Sat Feb 22 2025
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
In vivo Brain Pharmacokinetics of Dolutegravir Sodium-Loaded Nanostructured Lipid Carrier in situ Gel: Comparative Study with an Intravenous Drug Solution
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Background: Dolutegravir sodium (DTG), used to treat HIV, faces challenges in delivering effective therapeutic concentrations to the brain due to the blood-brain barrier (BBB). Nanostructured lipid carriers (NLCs) combined with in situ gels present a promising strategy for enhancing brain drug delivery via the intranasal route. Objective: To compare brain pharmacokinetics of DTGs delivered via NLC-loaded in situ gel intranasal administration with the conventional intravenous (IV) drug solution. Methods: 80 Wistar rats, which were divided into three groups: two groups consisting of 39 animals each and a control group with 2 animals. Rats were administered with a dose of 1.0 mg/kg of DTGs IV, and DTGs NLC-loaded in situ gel were admin

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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)
Role of Fasting Mimicking Diet in Farnesoid x Receptor for Suppressing Epithelial-to-Mesenchymal Transition, Cell Cycle Progression, and Viability of Prostate Cancer Cells
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The systemic and resistant nature of metastatic castration-resistant prostate cancers (mCRPC) renders it largely incurable even after intensive multimodal therapy. Proliferation, survival, and epithelial-mesenchymal transition (EMT) are three fundamental events that are deeply linked to carcinogenesis.  Hence, it is necessary to find a new combination of several therapies, targeting those vital mechanisms without causing side effects. Significant research works have shown differential low expression of the metabolic Farnesoid X receptor (FXR) in primary and metastatic prostate cancer suggesting their importance in prostate pathogenesis. Obticholic acid (INT 747), a potent FXR agonist is widely used in primary biliary chola

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Publication Date
Sat Dec 01 2018
Journal Name
Political Sciences Journal
Iraq after war and strategy of reconstruction : Analytical study in reality and future horizon
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Abstract (Iraq post – war reconstruction strategy: analytical study in fact and future prospects.) There search aims at identifying the causes of internal instability in Iraq from the political ,economic , social and security aspects , to diagnose the imbalance and to work towards finding real solutions to this . The study also aims at identifying the reconstruction proposals to completely eliminate the organizationof the terrorist advocate, as well as to know. theproblem of research lies in the ability of Iraqi political elites to achieve internal stability and to employ reconstruction proposals at all levels . The hypothesis of the research lies in the equation that the process of building stability (political – economic)and (socia

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