Pharmaceutical Sciences

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تقييم نظام إدارة المستودعات الطبية الحكومية
(AL-Quds University, 2004-07-20) وداد رشيد صالح القيق; Wedad Rasheed Saleh Al-qeeq; محمد عودة; سوزان شعشاعة; صلاح السويسي
Antibiotics Dispensing Patterns in The Community Pharmacies in Gaza Governorate
(Al-Quds University, 2008-03-01) Mostafa Omar El-Ghosain; مصطفى عمر الغصين
السلوك القيادي للمديرين وعلاقته بالنمو المهني للمعلمين من وجهة نظر معلمي المدارس الحكومية في محافظة الخليل
(AL-Quds University, 2013-06-26) هناء سعيد سليم شاهين; hana said saleem shaheen; محمد شعيبات; د. محمد عابدين; د. أحمد فتيحة
This study aimed at identifying the degree of principals’ leadership behavior and its relationship to teachers' professional development at governmental schools from the point of view of teachers at Hebron governorate during the academic year 2012-2013. The population of the study consisted of all teachers in Hebron (7962); a stratified random sample of 5% was chosen (399). However, statistical analysis was applied on 381 teachers. To achieve the objectives of the study, a questionnaire consisted of (33) items was developed to measure the principals’ leadership behavior distributed on three domains namely: administrative, technical and humanitarian. Another questionnaire consisted of (29) items was developed to measure professional development of teachers distributed on three domains: methods of teaching, evaluation and scientific materials. Validity and reliability of the study were verified by appropriate statistical methods. The results revealed that the estimates of teachers about the degree of the principals’ leadership behavior is medium at a mean of (3.56) and of a standard deviation (0.511). The administrative domain was the highest while the humanitarian was the lowest, and there were no significant statistical differences due to the variables of gender and experience while there were significant statistical differences due to the variable of qualification in the domains of administrative and technical in favor of teachers holding a degree of less than BA and directorate in favor of the north Hebron. Also it revealed that the estimates of teachers about the degree of professional development for teachers in government schools, came with a high degree a mean of 3.87 and a standard deviation of 0.80, and there were no significant statistical differences due to the variable of gender and qualification and experience, while there were differences due to the variable of directorate in the domain of scientific material in favor of the north Hebron. There was a weak positive correlation-i.e., Berson correlation coefficient (0.20) -between the variables of principals’ leadership behavior and the degree of their professional development. the researcher recommend that setting up criteria for choosing principals based on their leadership characteristics, and the necessity of continuing the process of development forteacher, especially in the field of teacher Evaluation by doing training courses for teachers and the school principal together.
التركيب الكيميائي والخصائص والقوى المحركة المخبرية لدوائيْن أوليّيْن جديديْن مبتكريْن من مضادات البكتيريا؛ الأموكسيلين والسيفالكسين
(AL-Quds University, 2014-02-22) غدير عبد مطر دقماق; GHADEER ABED MATAR DOKMAK; رفيق قرمان; د. أحمد عمرو; Nasr Shraim
Marketed antibacterial drugs suffer several problems, such as bitter taste and low stability which lead to patient incompliance. Prodrug technology for solving such problems is extremely exciting. Based on previously reported density functional theory calculations, amoxicillin ProD 1-2 and cephalexin ProD 1-2 were designed and synthesized. For the intraconversion of both antibacterial prodrugs the kobs and t1/2 values in different media were calculated from the linear regression equation obtained from the correlation of log concentration of the residual prodrug versus time. At constant temperature and pH the hydrolysis reaction for the above mentioned prodrugs displayed strict first order kinetics as the kobs was quite constant and a straight line was obtained. Kinetic studies in 1N HCl, pH 2.5 and pH 5 were selected to examine the intraconversion of both prodrugs to their parent drugs. The acid-catalyzed hydrolysis of the prodrugs was found to be much higher in 1N HCl than in pH 2.5 and pH 5. The experimental t1/2 values of amoxicillin ProD 1 in 1N HCl, pH 2.5 and pH 5 were 2.5, 7 and 81 hours respectively and for cephalexin ProD 1 in 1 N HCl and pH 2.5 were 2 and 14 hours respectively. In contrast, t1/2 values of amoxicillin ProD 2 in 1N HCl and pH 2.5 were 8 and 44 hours respectively and for cephalexin ProD 2 in 1 N HCl was 6 hours. On the other hand, at pH 7.4, the four prodrugs were quite stable and no release of the parent drugs was observed. At pH 5 the hydrolysis of the prodrugs was too slow. The four antibacterial prodrugs were found to be bitterless. The bitter taste masking by the prodrugs is believed to be via altering the ability of the drug to interact with bitter taste receptors.
تصنيع ودراسة المواصفات ل الأدوية المساعده المصممة ل حمض ترانزاميك و براسيتامول
(AL-Quds University, 2014-02-22) هبه نعيم خميس غريب; hiba naeem khamees ghareeb; رفيق قرمان; د. صالح أبو لافي; د. وليد صويلح
Prodrug is a chemical devise in which the drug is covalently linked to a chemical moiety; this linked moiety will temporarily affect the physicochemical properties of the drug for increasing their usefulness or decreasing their toxicity. The prodrug should be converted to its active form by metabolic or/and chemical processes, conversion process involves metabolism by enzymes distributed throughout the body. These enzymes might either decrease the drug’s bioavailability, or a genetic polymorphisms might lead to variability in prodrug activation and thus affect the efficacy and safety of designed prodrug. In the past few decades computational chemistry methods have been utilized in calculating physicochemical and molecular properties of compounds. This tool can be used to design prodrugs that chemically (intramolecular processes) interconvert to their parent drugs without any involvement of enzyme catalysis. The release of the active drug is solely dependent on the rate limiting step of the intramolecular process. Based on DFT calculations four different tranexamic acid prodrugs and three different bitter less paracetamol prodrugs were designed, synthesized and characterized using FT-IR, 1H-NMR LCMS and their in vitro intra-conversion to their parent drugs revealed that the t1/2 was largely affected by the pH of the medium. For tranexamic acid ProD 1 the experimental t1/2 values in 1N HCl, buffer pH 2 and buffer pH 5 were 54 minutes, 23.9 hours and 270 hours, respectively. Tranexamic acid ProD 2 was readily converted in 1 N HCl and pH 2 while it was entirely stable at pH 5 and pH 7.4. On the other hand, tranexamic acid ProD 3 and Prod 4 were stable in all media studied. The experimental t1/2 values for paracetamol ProD 2 in pH 3 and pH 7.4 were 3 hours and 18 minutes respectively and for paracetamol ProD 3 it was 27 hours in pH 3 and 12 hours in pH 7.4. In vitro binding for paracetamol ProD 2 to bitter taste receptors revealed that this prodrug lacks any binding affinity and it was found not to have any bitter sensation. This suggests, that paracetamol ProD 2 can replace its parent drug, paracetamol, for the use asbitterless antipyretic drug for geriatrics and pediatrics.
تصنيع ودراسة لمواصفات الأدوية المساعدة المصممة لمادة الغايفينيسين
(AL-Quds University, 2014-02-25) أمين محمود عبد المنعم ثوابته; Amin Mahd A. Thawabteh; رفيق قرمان; د. عماد عودة; Abdel Naser Zaid
Guaifenesin is an extremely bitter taste substance which affects its usage in pediatric and geriatric formulations. In this thesis we aimed to mask the bitter taste of guaifenesin by converting it to a potential tasteless prodrugs using different linkers. The prodrugs were synthesized by esterification of carboxylic acid anhydrides and guaifenesin. Maleic anhydride, succinic anhydride, and glutaric anhydride, respectively, were used to synthesize guaifenesin ester prodrugs (guaifenesin maleate, guaifenesin succinate, guaifenesin glutarate), 1 H-NMR, LC-MS, and FT-IR have confirmed the identity and purity of the new prodrugs. In vitro kinetic studies for the above mentioned prodrugs were done in four different aqueous media: 1 N HCl and buffers pH 3.3, pH 5.5 and pH 7.4. Under the experimental conditions the target prodrug was hydrolyzed to release the parent drug, guaifenesin, as was confirmed by HPLC determination. The kobs and the corresponding t1/2 values for guaifenesin prodrugs in 1N HCl were calculated from the linear regression equation correlating the log concentration of the prodrug versus time. The rate constant (kobs) was found to be 7.2x10-4 for guaifenesin maleate prodrug, 2.54x10-4 guaifenesin succinate prodrug, and 2.36x10-4 guaifenesin glutarate prodrug. Half-lives values (t1/2) were 2.01 hours for guaifenesin maleate prodrug, 7.03 hours for guaifenesin succinate prodrugs, and 7.17 hours for guaifenesin glutarate prodrug. On the other hand, at pH 3.3, 5.5 and 7.4, guaifenesin maleate, guaifenesin succinate, and guaifenesin glutarate prodrugs were entirely stable and no release of the parent drug, guaifenesin, was observed.
تحليل المركبات الثانوية لأوراق المريمية البرية/ المروية بواسطة GC-MS ودراسة تأثيراتها المضادة للأكسدة والميكروبات
(AL-Quds University, 2015-01-01) ريم نمر محمد سبوبه; Reem Nimer Mohammad Sabbobeh; صالح ابو لافي; خالد صولحة; عبد الناصر زايد
الفعالية المضادة للكائنات الدقيقه لدوائيْن أوليّيْن جديديْن مبتكريْن من مضادات البكتيريا؛ الأموكسيلين والسيفالكسين
(AL-Quds University, 2015-06-02) ساميه صلاح الدين عبد الغني كرد; samia salahaldeen abdalgani kord; رفيق قرمان; احمد عمرو; حاتم سلامة
The two novel prodrugs of amoxicillin and cephalexin were synthesized to improve the stability and bitter taste of their parent drugs. The in vitro susceptibility for both prodrugs was determined against Escherichia coli, staphylococcus epidermidis, staphylococcus aureus, Klebsiella pneumonia, streptococcus group A, streptococcus group B, and compared to that of their parents. The results revealed that both novel prodrugs have antibacterial activity on most bacterial strains with about the same potency as their parent drugs, In addition, Klebsiella pneumonia, and staphylococcus epidermidis showed resistance to both amoxicillin drug and its prodrug. Since klebsiella is gram negative bacteria and staphylococcus epidermidise is beta lactamase positive . It is worth noting that those two novel prodrugs are among a small number of prodrugs that have activity themselves before undergoing conversion via enzymatic or chemical processes to their corresponding parent drugs. The novel prodrugs exhibit their antibacterial activity against different types of bacterial strains due to the presence of beta lactam ring in their structures. In addition, it is expected that the novel two prodrugs will be much more stable in aqueous media than their corresponding parent drugs due to the fact that the sensitive amine group exists in the parent drugs was replaced with a more stable group, amide.
نوعية الحياة لمرضى زراعة الكلى في عيادات وزارة الصحة الفلسطينية في محافظة بيت لحم وشمال الخليل.
(AL-Quds University, 2015-07-15) محمد محمود الجوابرة; حسين الحلاق; د. ماهر الخضور; Dr. Waleed sweileh
QSAR study using the (PC-ANN) methodology was conducted to predict the inhibition constants of 127 symmetrical and unsymmetrical cyclic urea and cyclic cyanoguanidine derivatives containing different substituent groups such as: benzyl, isopropyl, 4- hydroxybenzyl, ketone, oxime, pyrazole, imidazole, triazole and having anti-HIV-1 protease activities. The results obtained by principal component-artificial neural network provided advanced regression models with good prediction ability. A 0.743 and 0.750 coefficients of determination were obtained using principal component-artificial neural network.
نوعية الحياة لمرضى زراعة الكلى في عيادات وزارة الصحة الفلسطينية في محافظة بيت لحم وشمال الخليل.
(AL-Quds University, 2015-07-15) خلود حسن طافش ذويب; kholoud Hassan tafish Dweib; حسين الحلاق; Dr. Maher Khdour; Dr. Waleed sweileh
تطوير وتقييم مخبري لمستحضر صيدلاني جديد يحتوي على فِيرّس جلوكونيت في حبه طافية في المعدة لفترة زمنية طويلة
(AL-Quds University, 2015-12-22) هلا عثمان عبد الرحيم حج حمد; hala othman abd-alraheem al-haj hamad; طارق الجعبة; احمد عمرو; نعمان مالكية
تصميم أدوية مساعدة مبتكرة من الفينيلفرين والباراسيتامول بالطرق الحسابية
(AL-Quds University, 2016-01-05) دنيا ابراهيم خالد قرمان; donia ibrahim khalid karaman; رفيق كرمان; Omer Deeb; Nasr Shraim
تطوير دواء اولي مبتكر للاتوفاكوون? الدواء المضاد للملاريا: تصنيع كيميائي, تشخيص و تقييم القوى المحركه المخبريه
(AL-Quds University, 2016-01-05) بيسان وضاح امين الفتاش; Beesan Waddah Amin Alfattash; رفيق قرمان; د أحمد عمرو; Dr. Nasr Shraim
Malaria is a global public health problem, resulting in tow million deaths per year .The majority of death cases are due to the most severe form of malaria caused by Plasmodium falciparum. As a result, efforts were directed toward the development of new effective medications intended for the treatment of this endemic disease. Atovaqoune is a new treatment option, showed an improvement in malaria treatment. Although Atovaqoune is an effective medication, it has its own limitations. Atovaqoune is highly lipophilic compound (water solubility < 0.2 µg/ mL), has low water solubility and low absorption, hence low bioavailability (< 10% in the fasted state). Accordingly, increasing atovaqoune aqueous solubility will improve its pharmacokinetic profile in particular bioavailability, thus improving its effectiveness and ability to administer the drug through different routs of administration. So that, our goal was to develop atovaqoune prod rug that possesses increased aqueous solubility by linking water soluble moiety to the 3- hydroxyl group, via chemical synthesis. Purification techniques including extraction, re-crystallization and column chromatography were used. Identity confirmation was done using, IR, NMR and LC/MS. Based on purity and identity results; in vitro kinetic studies using the HPLC instrument were performed at pH 2.2, 5.5 and 7.4. ATQ succinate (ProD1) has been successfully synthesized, purified and evaluated. T1/2 of ProD1 at pH 2.2, 5.5 and 7.4 is 28.8 days, 2.2 days, 3.2 days, respectively. It can be concluded from these data, that ProD1 is converted into ATQ in pH dependentmanner, and the hydrolysis of the prodrug follows first order kinetics, as the data plotted gives a straight line, and the Kobs is nearly constant. Concisely, modifying atovaqoune structure may result in enhancing its pharmacokinetic profile mainly absorption into body tissues, consequently increasing efficacy and ability to formulate atovaqoune in different dosage forms. Keywords: Malaria, drug resistance, atovaquone, bioavailability, prodrugs .
دراسة العلاقة الكمية بين الفاعلية والصيغة البنائية باستخدام طريقتي (MLR وPC-ANN ) لبعض المركبات التي لها فعالية على بروتين Translocator (TSPO
(AL-Quds University, 2016-01-05) هناء سليم حسين بني عودة; hanaa Saleem Hussein Baniowda; عمر ذيب; رفيق قرمان; Dr. Nasr Shraim
Quantitative structure-activity relationship study was performed to understand the activity of a set of 136 ligands of Translocator protein (TSPO) compounds. QSAR models were developed using multiple linear regression (MLR) as linear method. While principal component - artificial neural networks (PC-ANN) modeling method was used as nonlinear method. The results obtained offer good regression models having good prediction ability. The MLR resulted with models (12-24) which have coefficient of determination (R 2 ) >0.6, the best model (number 24) resulted with correlation coefficient (R) = 0.909, coefficient of determination (R 2 ) = 0.826, and adjusted coefficient of determination (R 2 adj) = 0.788. Cross Validation leave one out (LOO) and leave many out (LMO) were performed on the resulted MLR models, models 19-24 showed a good predictive power. After that principle component analysis (PCA) performed to divide the data into three data sets, then the ANN performed on the chosen models (19-24) from leave one out (LOO) and leave many out (LMO) validation. ANN resulted models were validated through randomization test, then the conditions proposed by Golbraikh and Tropsha were applied to conclude that the QSAR models has acceptable prediction power or not. However the best ANN model with a good predictivepower was model #24, with R test values 0.832
تصميم و تحضير مشتقات البيريميدين ثلاثية التفرع كمثبطات لبروتين مرافق المنشط لمستقبلات الاستروجين
(AL-Quds University, 2016-01-09) ميران محمد جمال طلال مسودى; Miran M.Jamal Talal Masswadeh; يوسف نجاجرة; Zaidoun Salah; Tawfeq Kaimari
Breast cancer (BC) is one of the most commonly diagnosed cancers in women. Estrogen signaling and the estrogen receptors (ERα, ERβ) are implicated in breast cancer progression. Majority of breast cancers start out as estrogen dependent as a result of overexpression of ER-regulated genes: Estrogen deprivation therapy using anti-estrogens (AEs) and aromatase inhibitors (AIs) to block ER activity and arrest the estrogen-dependent growth of BC still represents the primary treatment for breast cancer patients. This approach, however, frequently fails and patients develop resistant breast cancer, which is almost untreatable. In this project we focused on synthesizing a potent coactivator binding inhibitors (CBIs) molecules that block ER activity through a different mechanism that may arrest the estrogen-dependent growth of BC and offer a solution to the existing resistance. Coactivator binding inhibitors (CBIs) act by blocking the conformational change needed for DNA binding and gene expression. In this project set of compounds have been designed, synthesized through sequential substitution of the chlorine atoms of 2,4,6-trichloropyrimidine with amines or other nucleophiles. The synthesized compounds were purified using chromatography techniques, and characterized by (1H-NMR, 13C-NMR, FT-IR and MS (ESI)) spectroscopy. Some of these compounds were screened for their inhibitory activity against the acute myeloid leukemia cells (Molm-13) cells. Two forms of Molm-13 had been used to evaluate the role of p53. In one case cells were transfected with empty vector and in the other the cells were tranfected with sh-p53 RNA(sh-p53). The viability of cells was determined using WST-1 assay. Initial results of the tested compounds demonstrated that MY12 (35) and MY3 (26) exhibited potent activities against the two forms of Molm-13 cell lines and have a dose dependent effect while the compound MY2 (25) showed no significant inhibitory action on the same cell lines.
واقع أنشطة اللجنة الوطنية للمخيمات الصيفية في فلسطين لإكساب الأطفال المهارات الحياتية لعام (2011-2012)
(AL-Quds University, 2016-01-10) آيه انور محمد دار سلامه; Ayah Anwar Mohammad Dar Salameh; عبد الوهاب الصباغ; منصور غرابة; عبد الرحمن التميمي
This study was aimed to identify the reality of the activities of the National Committee for Palestinian Summer Camps, In terms of making children acquire life skills for the year 2011-2012. These skills are (contact and communication, problems solving, conflict management, self-understanding, creative writing, and scientific research). In order to achieve the objectives of the study, researcher used the descriptive analytical method, which considered the most commonly used method in the study of social and human phenomena. The researcher wanted through this approach to show the effectiveness of the activities of National Committee for Summer Camps, in terms of acquiring children specific life skills are the subject of this study. He also uses secondary sources for the purposes of the research, secondary sources consist of previous studies, scientific journals, and websites related to the problem of the study. Study population consisted of all participants in the Palestinian summer camps in 2011-2012 totaling (5814) participants according to the statistics of the National Committee for Summer Camps for the 2011-2012 year, the researcher used a random cluster sample represents a group of participants in these camps for the year 2011-2012. (360) questionnaire forms were distributed among the participants of these the camps, and (335) of them were recovered, and he used the probability sampling method, because the study population is specific. The sample size for the study was estimated by using appropriate statistical equations. The study reached several conclusions, including: That contact and communication skillsand conflict management as the views of the participants was very high, While the study showed that the creative writing skills, life analytical skills (such as problem solving, science, and technology), and the skill of self-understanding was high, but the skill ofscientific research, the study showed based on the opinion of participants is medium. In general, the results reflect a positive sign in many aspects, the negative aspects are limited, and must be studied again. The study came out a set of recommendations are represented by: The need to focus in summer camp activities on skills related to scientific research, such as the ability to gather and organize information and make use of them, working on removing misunderstanding in regard to the scientific and theoretical side in the camps, which should be transferred to its main resource (the school). Therefore, the researcher believes that should integrate the scientific aspect in the camp into recreational activities, and follow methods differ from the methods that are used in the school. The researcher also recommends the need to encourage summer camps and the activities which provided by, because of its positive outcomes in the short and long term. Activities that must be strengthened within the summer camps, interested in skills that use physical movements and signals, and skills of self-understanding, particularly with regard to strengthening the self-confidence, as well as problem-solving skills, in particular the aspect of perseverance and try more than once, away from surrender to failure. The researcher believes that the research is broad and deep, and can be studied from different aspects, so he suggests some topics relevant to the subject of research, that maybe form items for future researches': 12. Choosing older age group. 3. Comparing between summer camps in Palestine and other Arab countries. A comparative study among children and youth.
تأثيرمركبات لتيولين، ميدستيورين (PKC-412) و PD173074 على مراحل حياة فيروس Cytomegalovirus (HCMV) المختلفة.
(AL-Quds University, 2016-04-25) عامر عزت محمد دوفش; Amer Izzat Mohammad Doufish; ميساء العزة; د. عماد معتوق; الدكتور رائد الكوني
The cytoplasmic assembly compartment (AC) in HCMV-infected human foreskin fibroblasts (HFF) is a unique juxtanuclear ―bulb‖-like structure. Morphology of the AC is dependent on the activity of the viral-encoded serine/threonine kinase, pUL97. The ―bulb‖-like structure morphology is also altered when wt-HCMV infected cells are treated with kinase inhibitors NGIC-I, a kinase C inhibitor, or Staurosporine, a wide range serine/threonine kinase inhibitor. Infection with a UL97 deletion mutant simulated the inhibition with NGIC-I or Staurosporine of wt-HCMV infection, resulting in a less compact and a vacuole-rich AC. In all three cases viral titers were reduced 2-3 logs. Cellular kinases play central roles in regulation of cell replication and differentiation, making cellular kinase inhibitors attractive antiviral targets. Different protein kinases were identified to affect different stages of HCMV life cycle and infectivity, which prompted us to explore yet not recognized kinase inhibitors for their activity against HCMV infection. In this study, we employed protein kinase inhibitors Luteolin, Midostaurin (PKC-412) and PD173074, and investigated their influence on the assembly compartment, early stages of HCMV infection and viral load. Luteolin at 20 μM did indeed reduce viral load without any detectable effects on the assembly complex. Midostaurin, PKC-412, did not affect viral load or the assembly compartment. The most striking result was observed with the tyrosine kinase inhibitor, PD173074, at 5 μM concentration. Although PD173074 did not affect early stages of HCMV infection, it reduced viral load and induced a specific structure of the assembly compartment we referred to as ―vesicles’-rich AC pattern. Hereby, the AC remained its ―bulb‖-like structure, but was remarkably accompanied withvesicles spread throughout the cytoplasm, which arose at 48 h p.i. and were remarkable by 72 h p.i. and 96 h p.i.. These vesicles stained for markers of the assembly complex; viral tegument proteins pp28 and pp65 as well as WGA Golgi marker and accumulated densely along the cytoplasmic membrane of the infected cells. Taken together, our data provide the first evidence for a role of tyrosine kinase in HCMV assembly.
تطوير وتقييم شكل صيدلاني جديد بخاصية التحرر الفوري (أقراص بريغابالين)
(AL-Quds University, 2016-05-21) محمد سميح شفيق شناعة; MOHAMMED SAMIH SHAFIQ SHANAA; نعمان مالكية; إبراهيم كيالي; هاني اشتيه
Pregabalin is an anticonvulsant agent used for the peripheral and central neuropathic pain treatment, marketed as Capsule and Solution dosage forms. The purpose of this study is to develop an immediate release Pregabalin Tablet, as a new dosage form in the Palestinian market that is bioequivalent to the FDA approved Reference Pregabalin Capsules (Lyrica). Pregabalin drug substance and the finished product during the time of development were not described in either the British or US pharmacopoeia. The chemical and physical evaluation of bulk drug substance (Pregabalin) was accomplished following the manufacturer`s analytical method and specification. A new reversed-phase, isocratic LC method was developed and validated according to USP validation parameters, for the qualitative and quantitative determination of Pregabalin in pharmaceutical dosage forms using HPLC (LaChrome Elite) equipped with photodiode array UV detector. Mobile Phase is a mixture of Phosphate Buffer pH 6.9, and acetonitrile (94:6). Chromatographic System is Column: C-18 ODS 5 to 10µm in diameter (25cm X 4.6 mm id), detector: UV set at wavelength 210 nm, Flowrate: 1.5 ml / min and Injection Volume: 20 μL. Formula development was accomplished through a series of steps: Selection of excipients through compatibility studies, selection of manufacturing process and in-vitro comparison studies versus the reference product. Excipients compatibilities were studied by preparing a binary mixture of Pregabalin and excipient (1:1) then sealed in neutral glass vials and incubated at 40±2 °C/75 ±5% RH for 30 days. The mixtures were tested by means of FTIR for any possible interactions. The following excipients (Microcrystalline Cellulose, Pregelatinized Starch, Talc and Mg Stearate) were found to be compatible with Pregabalin.A series of pre formulation trials were composed and processed by direct compression method. Selection of formula was based on: Powder characteristics: (such as compressibility ratio, flowability, bulk density and tapped density), which would allow for a simplified method of manufacture, friability, hardness and disintegration of compressed tablets. The selected formulation was applied to prepare Pregabalin Tablets in two strengths, i.e. tablets containing 75mg/tablet and 300mg/tablet. They are prepared as dose weight proportional. The compressed tablets were film-coated with PVA based polymer by using water as solvent.The stability of film coated Pregabalin tablets were tested by incubating the finished products in their final package (PVC-Alum) at different storage conditions i.e. 25 ± 2 °C / 60 % ± 5% RH, 30 C ± 2 °C / 60% ± 5% RH and 40 C ± 2 °C / 75% ± 5% RH. Samples were tested biweekly for content of Pregabalin (assay), physical appearance, dissolution rate, and degradation products. Pregabalin Tablets proved to be stable in all aspects for the period tested (1 month) at all storage conditions. Biowavier study was performed between Pregabalin Tablets (75mg and 300mg) and the Reference Pregabalin Capsules (Lyrica 75 and 300mg Capsules) using paddle method rotated at 50 rpm in different dissolution media (0.06N Hydrochloric acid solution, Acetate buffer pH 4.5 and phosphate buffer pH 6.8. It was found that either Reference or Test products release more than 85% of their Pregabalin content in 15 minutes. As Pregabalin API, according to BCS is Class I drug and the dissolution profiles of Pregabalin Tablets is similar to that of Reference Pregabalin Capsules (Lyrica) under the same test conditions, and all excipients used are not suspect of having any relevant impact on bioavailability it is strongly believed that the developed Pregabalin Tablets are bioequivalent to the marketed Lyrica Capsules.
مدى انتشار استخدام الأدوية المصروفة بدون وصفة طبية لدى النساء الحوامل: دراسة مستعرضة في بعض المناطق في الضفة الغربية الفلسطينية
(AL-Quds University, 2016-05-28) ملفين مصطفى يوسف مصلح; malvin mustafa yousef musleh; حسين الحلاق; د. ماهر الخضور; Waleed Sweileh
Background: Over-the-counter medications are widely used by the Palestinian population, including pregnancy women. This study seeks to find out the prevalence of use OTC medications by pregnant women, and the effects of these drugs on their pregnancy. The objectives of the study are concluded in finding out the level of using OTC medications among pregnant women, and the awareness of the effects of such drugs on the women and their babies. This study has been motivated by the fact that taking of over the counter medicines has in some cases resulted in the birth of deformed babies among other challenges health and physical challenges. Methods: The study has employed a descriptive design. The population of the pregnant women will act as the target population. The sampling process was stratified by site and the researcher interviewed 555 pregnant women as target sample. Data were collected by interviewing the pregnant women in three main governate hospitals, in Nablus (North), Ramallah (Center), Hebron (South) and in private clinics and hospitals. These women filled out questionnaires to determine the prevalence of using OTC medications during their pregnancy. The data is analyzed by use of descriptive and inferential statistics andpresented by way of statistical means. Results: Of the 555 women, 391 (70.5%) women were taking OTC medications during pregnancy. The most reported medications used were; OTC vitamins, heartburn and acid reflux medications and analgesics with a percent of use 98.0%, 97.7% and 46.8% respectively. 67.8% of these mothers were in the ages between 20-40, and 64.1% were overweight women. The majority of those taking OTC medications during pregnancy had been directed by the doctors (58.2%), while the pharmacists were the lead source of theinformation (83.1%). 65.0% of pregnant women thought that OTC are safe, but with consultation of the professionals and 29.5 % thought that they are totally unsafe. Conclusion: This study is the first study that detected the prevalence of OTC medications use in Palestinian pregnant women. The prevalence of use was high. We have identified the predictors of OTC medications use and the problems faced during pregnancy leading them to take OTC medications. The lack of awareness on using these medications during pregnancy is alarming. Educational programs should be held for increasing the awareness among pregnant women on the effects of OTC medications on their pregnancy.
تصنيع ودراسة المواصفات والقوى المحركة المخبرية للأدوية المساعدة للدوبامين
(AL-Quds University, 2016-12-21) يحيى فؤاد رشيد خواجا; yahya fuad rasheed khawaja; رفيق قرمان; د. حاتم حجازي; Dr. Nasr Shraim
Parkinson patients have insufficient dopamine in specific regions of the brain, so attempts have been made to replenish the deficiency in the dopamine. Dopamine itself doesn't cross blood brain barrier, but its precursor, levodopa (LD) is actively transported into the CNS and is converted to dopamine in the brain. The bioavailability of LD is less than 10% with only 1% of administered oral levodopa penetrates the brain. Large doses of levodopa are required because much of the drug is decarboxylated to dopamine in the periphery, resulting in side effects that include nausea, vomiting, cardiac arrhythmias, and hypotension. To minimize the conversion to dopamine (DA) outside the central nervous system (CNS), LD is usually co- administered with peripheral inhibitors of amino acid decarboxylase (carbidopa and benserazide). In spite of that, other central nervous side effects such as dyskinesia, on-off phenomenon and end-of-dose deterioration still remain.Based on DFT calculations a novel dopamine prodrugs for the treatment of Parkinson’s disease that can improve the overall biopharmaceutical profile of the current medications to enhance effectiveness and to ease the use of the medications were synthesized, characterized, in vitro intra-conversion to their parent drugs and in silico pharmacokinetics and toxicity prediction were also studied. The synthesized dopamine prodrugs have a carboxylic group as a hydrophilic moiety and a hydrocarbon skeleton as a lipophilic moiety, where the combination of both groups ensures a moderate hydrophilic lipophilc balance value. The potential prodrugs are expected to give better bioavailability than the parental drug owing to improved absorption. Furthermore, these prodrugs are believed to be more effective than L-dopa because the latter undergoes decarboxylation in the periphery before reaching the blood– brain barrier. Additionally, the synthesized prodrugs can be used in different dosage forms (I.V., S.C., tablets, and others) because of their potential solubility in organic and aqueous media. For dopamine ProD 1 the experimental t½ values in 0.1N HCl, buffer pH 2.2, buffer pH 5.5 and buffer pH 7.4 were 60.3 hours, 54.66 hours, 99.93 hours and 138.13 hours, respectively. Dopamine ProD 2 was readily converted in 0.1N HCl, buffer pH 2.2, pH 5.5 and pH 7.4 with half -life time (t½) of 48.34 hours, 54.22 hours, 131.98 hours and 193.42 hours, respectively. Finally, in silico predicting of physiochemical parameters, ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) properties, oral bioavailability and BBB permeability for the synthesized prodrugs were studied. The results revealed that no prodrug had a high risk of toxicity, and all the prodrugs showed good pharmacokinetic properties. Moreover, all synthesized dopamine prodrugs were found to obey Lipinski’s rule of five.

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