Volume: 17  Issue: 2 - 2020
Hide Abstracts | << Back
1.Various in vitro bioactivities of secondary metabolites isolated from the sponge Hyrtios aff. erectus from the Red Sea coast of Egypt
Asmaa Nabil - Adam, Mohamed A. Shreadah, Nehad M Abd El Moneam, Samy A El-assar
Pages 127 - 135
INTRODUCTION: The present study confirmed the presence of bioactive constituents in Hyrtio saff.erectus Sponge extract (HESE) collected from Red Sea.
METHODS: The current study subjected to broad biochemical assays for example cytotoxicity, antioxidants (DPPH and ABTS),anti-inflammatory (IL-6, TNF-α,COX-1and COX-2,anticancer (PTK and SHK1) anti-Alzheimer using acetylcholinesterase.Furthermore different phytochemical screening.
RESULTS: The Cytotoxicity was tested against hepatocellular carcinoma cell lines as prescreening test. The HES extract had high content of total phenolic, flavonoids and carotenoid with 0.061, 0.2839 and 1.976 mg/g; respectively.The pharmacological and biochemical studies showed high antioxidant capacity with 93.0% and 99% at 1mg using DPPH and ABTS respectively. Cytotoxic activity against cancerous cell line cleared out that HES could inhibit cell growth effectively with IC50 = 47.5 µg/ml. Furthermore, anticancer activity using tyrosine kinase (PTK) and Sphingosine kinase 1(SHKI) inhibitor screening assays resulted in 71.66 and 85.21% inanition activity; respectively. The anti-inflammatory assays showed that the inhabitation activities against COX-1, COX-2, IL-6 and TNF-α were 71.82, 81.13, 80.89 and 59.74 %; respectively.At the same time, the anti-Alzheimer results showed high activity at 1mg with 83.51 %. Additionally the antiviral activities using reverse transcriptase inanition assay was 91.70%.
DISCUSSION AND CONCLUSION: The Hyrtio saff erectus sponge isolated from red sea showed tremendous activity against many diseases and it is consider as an excellent source for bioactive pharmaceutical compounds.
Abstract

2.In-vivo antioxidant activity of different fractions of Indigofera barberi against paracetamol induced toxicity in rats
Shaik Amina Bee, Atmakuri Lakshmana Rao, Chinna Eswaraiah Rao
Pages 136 - 140
INTRODUCTION: To evaluate the in-vivo antioxidant activity of chloroform extract fractions of Indigofera barberi (whole plant) against paracetamol induced toxicity in rats.
METHODS: For 7 days, animals were treated with chloroform extract fractions and the toxicity was induced with a single dose of paracetamol intra peritoneal injection. Group of animals pre-treated with 100 mg/kg p.o of fraction D of Indigofera barberi improved the SOD, catalase, peroxidase and glutathione levels significantly as compared to control group.
RESULTS: The results showed that the activities of SOD, catalase, peroxidase and glutathione in group treated with paracetamol are 33.6 ± 0.09, 5.5 ± 0.23, 0.131 ± 0.15 & 46.1 ± 5.81 and SOD, catalase, peroxidase & glutathione in fraction D treated group are 61.8 ± 0.07, 10.6 ± 0.16, 0.913 ± 0.23 & 87.6 ± 1.4 respectively. So, the present study revealed that fraction D of Indigofera barberi has significant in-vivo antioxidant activity and can be used to protect tissue from oxidative stress.
DISCUSSION AND CONCLUSION: From the results, fraction D of Indigofera barberi in the dose of 100 mg/kg, p.o. has improved the SOD, catalase, peroxidase and glutathione levels significantly. Based on this study we conclude that fraction D of Indigofera barberi possesses in-vivo antioxidant activity and can be employed in protecting tissue from oxidative stress.
Abstract

3.Development and Validation of Stability Indicating RP-HPLC Method for Simultaneous Estimation of Teneligliptin and Metformin
Rajani Vetapalem, Rajendra Prasad Yejella, Lakshmana Rao Atmakuri
Pages 141 - 147
GİRİŞ ve AMAÇ: Bu çalışmanın temel amacı, Teneligliptin ve Metformin'i toplu ve tablet dozaj formunda eş zamanlı tahmin etmek için basit, kesin, spesifik ve stabil bir RP-HPLC yöntemi geliştirmekti.
YÖNTEM ve GEREÇLER: Analiz, mobil faz olarak tampon: asetonitril: metanol (65: 25: 10, v/v/v) kullanılarak 30°C'de Kromasil C18 kolonu (250 x 4.6 mm, 5u) kullanılarak gerçekleştirilmiştir. Saptama, 1.0 ml/dak akış hızında 254 nm'de gerçekleştirilmiştir.
BULGULAR: Teneligliptin ve Metformin retansiyon süresi sırasıyla 2.842 dk ve 2.017 dk olarak bulundu. Doğrusallık aralığı, Teneligliptin için 5-30 µg / ml ve Metformin için sırasıyla 125-750 µg / ml idi. Zorunlu bozunma çalışmaları, asit, alkali, oksidatif, termal, foto stabilite ve nötr koşullar altında ICH'nin talimatlarına göre yapıldı.
TARTIŞMA ve SONUÇ: Geliştirilen yöntem tüm parametreler için başarıyla doğrulandı ve sınırlar içinde bulundu. Geliştirilen metot, Teneligliptin ve Metformin'in yığın ve tablet dozaj formunda eş zamanlı tahmini için başarıyla kullanılabilir.
INTRODUCTION: The main objective of the present work was to develop a simple, precise, specific & stability indicating RP-HPLC method for simultaneous estimation of Teneligliptin and Metformin in bulk and tablet dosage form.
METHODS: The analysis has been performed using Kromasil C18 column (250 x 4.6 mm, 5µ) at 30°C using buffer: acetonitrile: methanol (65: 25: 10, v/v/v) as mobile phase. The detection was carried out at 254 nm with a flow rate of 1.0 ml/min.
RESULTS: The retention time of Teneligliptin and Metformin was found to be 2.842 min & 2.017 min respectively. The linearity range was 5-30 µg/ml for Teneligliptin and 125-750 µg/ml for Metformin respectively. The forced degradation studies were performed as per the guidelines of ICH under acidic, alkaline, oxidative, thermal, photo stability & neutral conditions.
DISCUSSION AND CONCLUSION: The developed method was successfully validated for all the parameters and was found to be within the limits. The developed method could be successfully employed for the simultaneous estimation of Teneligliptin and Metformin in bulk and tablet dosage form.
Abstract

4.High Performance Thin Layer Chromatographic method using DoE approach for estimation of phytochemicals in Moringa oleifera leaves extract
Asha Thomas, Abhilash Kanakdhar, Adinath Shirsat, Sanjeevani Deshkar, Lata Kothapalli
Pages 148 - 158
INTRODUCTION: A systematic Design of Experiment (DoE) based sensitive, robust high performance thin layer chromatographic (HPTLC) method was established for simultaneous estimation of gallic acid (GA), quercetin (QT) and rutin (RT) from ethanolic and aqueous leaves extracts of Moringa oleifera.
METHODS: The chromatographic separation was carried on Merck TLC aluminum sheets of silica gel 60 F254 (10 X 10 cm) with mobile phase of toluene: ethyl acetate: methanol: formic acid (4.9: 4.1: 2: 0.5, v/v/v/v) with densitometric scanning at 300 nm. The Critical Method Parameters were initially identified by Regular Two Level Factorial design and further systematically optimized using Central Composite design, evaluating effect on selected Critical Analytical Attributes, retention factor (Rf) and Peak-area.

RESULTS: The Pareto charts, 3D response surface plots and polynomial equations for the generated models suggested significant influence of selected factors on responses of QT, GA and RT. Desirability and overlay plots employed provided appropriate solutions which were experimentally validated. Under the optimized conditions, the biomarkers were suitably resolved with Rf values of 0.64 ± 0.02, 0.80 ± 0.03 and 0.22 ± 0.02 for GA, QT, and RT respectively with wide linear dynamic range (200-1200 ng/band each), high accuracy (98.1-99.4 %) and intra- and inter-day precision (%RSD<2%).
DISCUSSION AND CONCLUSION: When employed for quantification of these biomarkers in Moringa oleifera extracts, the ethanolic and aqueous extracts exhibited higher content of QT (993.5µg/g and 832 µg/g respectively).The ethanolic extract showed larger amount of RT (701µg/g). In contrast, aqueous extract exhibited higher proportion of GA (591.1µg/g) compared to ethanolic extract (150µg/g).
Conclusions: This validated HPTLC method developed through DoE approach was successfully employed for quantification of GA, QT and RT from Moringa oleifera extracts and may also be extended for their simultaneous estimation in other herbal extracts thereby reducing time and may serve as a cost effective tool for analysis.


Abstract

5.Floating Microspheres of Enalapril Maleate as a Developed Controlled Release Dosage Form: Investigation the Effect of Ionotropic Gelation Technique
Ali Khidher Abbas, Anas Tarik Alhamdany
Pages 159 - 171
GİRİŞ ve AMAÇ: Bu çalışmanın amacı, bir hidrofilik taşıyıcı kullanılarak iyonotropik jelleştirme tekniği ile enalapril maleatin yüklü yüzen mikro kürelerin emilimini ve biyoyararlanımını arttırmak için yeni onaylanmış bir çalışma ile bir kontrol ilacı verme sistemi sağlamaktır
YÖNTEM ve GEREÇLER: Bu çalışma kapsamında, yüzen mikrokürelerin onbir gelişmiş formülasyonu, sodyum aljinat, iotacarrageenan, sodyum bikarbonat, balmumu klorür ve ilacın farklı konsantrasyonlarıkullanılarak iyonotropikjelasyon yöntemi ile hazırlanmıştır. Bu mikrokürelerin karakterizasyonu, mikrometrik özellikler, yüzdelik verim, yakalama randımanı, In-Vitro yüzme tekniği, In-Vitro ilaç salımı ve ilaç salımınım kinetiği gibi çeşitli parametreler kullanılarak yapıldı. Optimum formül, Fourier dönüşümü kızılötesi spektroskopisi (FT-IR), yüzey morfolojisi, toz X-ışını difraksiyonu (PXRD) ve diferansiyel taramalı kalorimetri (DSC) kullanılarak ilaç-yardımcı madde uyumluluğu için değerlendirildi ve tanımlandı.
BULGULAR: Sonuçlardan; F4 matristen ilacın daha hızlı ve prim salınımını sağladığı için optimum formül olarak seçildi (% 91.4). İyonlaşma kinetiği (R2) en iyi Korsemeyer modeli ve 0.43-0.84 arasında gösterilen salınım üssü (n) ile donatıldığı için, ilaç salımının kinetiği hem difüzyon hem de erozyon mekanizmalarına dayanmak üzere kurulmuştur.SEM görüntüleri, parçacık boyutu 199.4 ± 0.04 olan küresel, keskin ve serbestçe dönen mikroküreleri gösterir. Optimun yüzdürme özellikleri, yüzdelik verim ve ilaç yakalama etkinliği elde edilmiştir. FTIR enalapril ve polimerler arasında hiçbir etkileşim olmadı. DSC ve XRD, hazırlanan mikro kürelerde yüklü enalapril'instabil kristalin özelliklerini korurken, polimerler ile ilacın karışabilirliğini atfetmiştir
TARTIŞMA ve SONUÇ: Enalapril maleatin gelişmiş yüzer mikro küreciklerinin ümit vadeden kontrollü bir ilaç verme sistemi olarak kabul edilebileceği sonucuna varılabilir, böylelikle hasta uyumu geliştirir.
INTRODUCTION: The purpose of this study is to provide a control drug delivery system through a newly approved work to enhance absorption and bioavailability of enalapril maleate loaded floating microspheres by ionotropic gelation technique using a hydrophilic carrier.
METHODS: Over this study, eleven developed formulations of floating microspheres were prepared by ionotropic gelation method using different concentrations of sodium alginate, iota carrageenan, sodium bicarbonate, calcium chloride, and the drug. Characterization of these microspheres was done using a diversity of parameters like micrometric properties, percentage yield, entrapment efficiency, In-Vitro buoyancy, In-Vitro drug release, and kinetics of drug release. The optimum formula was evaluated and identified for drug-excipients compatibility using Fourier transform infrared spectroscopy (FT-IR), surface morphology, powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC).
RESULTS: From the results; F4 was selected as an optimum formula since it provides a faster and premium release of drug from the matrix (91.4%). Kinetics of drug release was founded to depend on both diffusion and erosion mechanisms, as the correlation coefficient (R2) was best fitted with Korsemeyer model and release exponent (n) shown to be between 0.43-0.84. SEM images demonstrate spherical, discrete and freely flowing microspheres with a particle size of 199.4 ± 0.04. Optimum buoyancy properties, percentage yield, and drug entrapment efficiency were achieved. FTIR decided no interaction between enalapril and the polymers. DSC and XRD ascribed the miscibility of the drug with the polymers while maintaining stable crystalline properties of enalapril loaded in the prepared microspheres.
DISCUSSION AND CONCLUSION: It can be concluded that the developed floating microspheres of enalapril maleate can be considered as a promising controlled drug delivery system; thereby improve patient compliance.
Abstract

6.Compare of Lipid and Lipoprotein Values of Wrestlers and Soccer Players
Hasan Nedim Çetin, Cuma Ece, Semra Çetin, Meltem Paksoy
Pages 172 - 176
GİRİŞ ve AMAÇ: Bu çalışmanın amacı güreşçilerin ve futbolcuların lipit ve lipoprotein değerlerinin karşılaştırılmasıdır.
YÖNTEM ve GEREÇLER: Bu çalışmaya 11,5 yıl spor yapan 17 erkek güreşçi, 11,9 yıl spor yapan 18 erkek futbolcu öğrencisi olmak üzere toplam 35 kişi katılmıştır. Trigliserit (TG), Total Kolesterol (TC), yüksek dansiteli lipoprotein kolesterol (HDL-C) ve düşük dansiteli lipoprotein kolesterol (LDL-C) düzeyleri Hitachi 717 otoanalizörü ile belirlenmiştir. Güreşçi ve futbolcu arasındaki farkları belirlemek için “bağımsız t” testi yapılmıştır.
BULGULAR: Güreşçiler ile futbolcular arasında vücut ağırlığı ve vücut kitle indeksinde anlamlı bir fark bulunmuştur (p <0,05). Ayrıca, güreşçiler ve futbolcular arasında plazma TC, LDL-C ve HDL-C değerlerinde anlamlı farklılıklar tespit edilmiştir (p <0,05, p <0,001). Bununla birlikte Güreşçiler ve futbolcular arasında plazma TG değerlerinde anlamlı bir fark bulunmamıştır (p>0,05). Güreşçilerin TC ve LDL-C değerleri futbolculara göre anlamlı derecede yüksek olup (p <0,05), futbolcuların ise HDL-C değerleri güreşçilerden anlamlı derecede yüksek bulunmuştur (p<0,05). Güreşçilerin TC / HDL-C oranının futbolculara göre daha yüksek olması anlamlıdır (p <0,05).
TARTIŞMA ve SONUÇ: Güreşçiler ve futbolcular arasında lipit ve lipoprotein değerlerinde farklılık olduğu bulunmuştur. Bu durumun branş ve antrenman farklılığından kaynaklandığı düşünülmektedir. Güreşçilerin ve futbolcuların lipit ve lipoprotein değerleri, onların kardiyovasküler hastalık tehlikesi taşımadıklarını göstermiştir. Bununla birlikte güreşçilerin düzenli antrenmanlarında koşu veya aerobik antrenmanlara daha fazla yer vermeleri tavsiye edilir.
INTRODUCTION: The aim of this study was to compare of lipid and lipoprotein values of wrestlers and soccer players.
METHODS: Total of 35 subjects, 17 male wrestlers who do sports for 11.5 years, 18 male soccer player students who sports average 11.9 years, participated in this study. Triglyceride (TG), Total Cholesterol (TC), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C) levels were determined by Hitachi 717 autoanalyser. To determine the differences between wrestler and soccer players “independent t” test were performed.
RESULTS: There is a significant difference in body weight and body mass index between wrestlers and soccer players (p<0.05). Moreover, significant differences in plasma TC, LDL-C, and HDL-C values between wrestlers and soccer players (p<0.05, p<0.001). However, no significant differences in plasma TG values between wrestlers and soccer players (p>.05).TC and LDL-C values of wrestlers were significantly higher than the soccer players (p<0.05). HDL-C values of soccer players were significantly high from wrestlers (p<0.05). It is meaningful that the ratio TC / HDL-C of wrestlers is higher than soccer players (p<0.05).
DISCUSSION AND CONCLUSION: Total cholesterol, triglyceride, high and low-density lipoprotein cholesterol of soccer players were found better than wrestlers. This situation can be caused by branches and training differences. This result shows that between wrestlers and soccer players did differences in lipid and lipoprotein levels. Lipid and lipoprotein values of wrestlers and soccer players have shown that they do not carry the risk of cardiovascular disease. In addition, it is recommended that the wrestlers should have jogging or aerobic training in their daily regular training.
Abstract

7.Theoretical study on ionization of boric acid in aqueous solution by ab initio and DFT methods at T = 298.15 K
Hoodad Ghanizadeh, Farhoush Kiani, Fardad Koohyar, Bahareh Khanlarzadeh
Pages 177 - 181
INTRODUCTION: Boric acid has antifungal and antiviral properties. It is used in various prescription pharmaceutical products. In this research work, we theoretically calculated the pKa value of boric acid in aqueous solution by ab initio and DFT methods at T = 298.15 K. To explain the determined acidic dissociation constant, the various molecular conformations and solute-solvent interactions of the species of boric acid were considered. The basis set at the B3LYP/6-31+G (d) level of theory was selected for DFT calculations. We analyzed the formation of intermolecular hydrogen bonds between several species of boric acid and water molecules through Tomasʼs method. The result shows that there is a comparable agreement between the experimentally and theoretically determined pKa values for boric acid.
METHODS: Initially, the structure of species of boric acid was optimized by semi empirical PM3 method in program Hyper Chem (CS Chem 3D version 5.0). All calculations about geometries of the initial and solvated molecules in water were done using Gaussian 09 program package. DFT calculations were carried out using the hybrid exchange – correlation functional of Becke, Lee, Yang, and Parr (B3LYP) and the Gaussian 6-31G (d) basis set was used [16].
To analyze the solvent effects on all species involved in the selected ionization reaction, the polarized continuum model (PCM) of Tomasi et al. was used. In this method, the solvent is represented as a structure less polarizable medium characterized by its dielectric constant [17].
Finally, we selected the solvation of the species by means of intermolecular hydrogen bonds (IHBS) that involve one molecule of the mentioned species and some molecules of water.

RESULTS: The trend of a molecule to lose its H+ is quantified as pKa. Boric acid is a weak acid and it has three acid groups. A proton can separate from hydroxyl group to give ionized specie (Fig. 1). This concept of microscopic ionization constant is shown in the Eq. 1:

(1)

The total energies of the single and solvated species of boric acid, in water, were calculated at the B3LYP/6¬-31+G (d) level of the theory, using Tomasiʼs method at T = 298.15 K and the results were showed in Table 1.
It can be found from Table 1 that the total free energy for various species of boric acid increases by increasing the number of water molecules. It shows that the solvation of the boric acid is an endothermic process.
Various reactions including the neutral and anion species of boric acid were considered in an excel program and some of these reactions were not further considered because their equilibrium constants are not comparable with experimental ones. The selected equation for deprotonation process of boric acid as well as the experimentally determined and theoretically calculated pKa have been shown in Table 2.

Ionization constant of boric acid:
In aqueous solutions, the molecule of boric acid can involve in below reaction:
H3L(H2O)4 + OH- ⇌ H2L-(H2O)3 + 2H2O Kc (2)
In the above reaction, H3L(H2O)4 (Fig. 2A) is the neutral specie of boric acid solvated with four molecules of water and H2L-(H2O)3 (Fig. 2B) represents the anion specie of boric acid solvated with three water molecules.
During reaction of Eq. 2, the autopyrolysis of two water molecules, in pure water, can occur as the below:
2H2O ⇌ OH– + H3O+ Kw = 1.008×10-14 (3)
The very low amount of Kw shows that a few water molecules are ionized in pure liquid water.
The reaction of Eq. 4 can be obtained by combining Eqs. 2 and 3:
H3L(H2O)4 ⇌ H2L-(H2O)3 + H3O+ Ka (4)
It is clear that the value of Ka can be calculated using Kc and Kw as the below:
Ka = Kc × Kw (5)
Eq. 5 was applied to calculate the values of the ionization constant of boric acid, Ka, in water at T = 298.15 K. The theoretically calculated value of pKa for boric acid at T = 298.15 K is shown in Table 2. As it can be seen in this table, there is a good agreement between experimentally determined and theoretically calculated pKa values of boric acid at this temperature.
Table 3 shows the optimized values of structural properties for the anion and neutral species of boric acid, in water, obtained at the B3LYP/6-31+G (d) level of theory with Tomasiʼs method at T = 298.15 K.
As it can be seen in Table 3, for boric acid, the values of qO4 for HL-(H2O)3 and H2L(H2O)4 are -1.104481 and -0.907847, respectively. It shows that the absolute value of electrical charge around O4 atom in HL-(H2O)3, compared to that of in H2L(H2O)4, increases and it can imply to separate H+ form O4 atom during deprotonation process of boric acid in water.

Study on H-bonding between selected species of boric acid and water
The structural properties of specie, solved in water, can help us to understand the interaction between this specie and water (H-bonding). One of the most important of these structural properties is the bond length between the indicated atoms form solute and solvent (water) molecules (in Å). These data, for neutral and cation species of boric acid, are listed in Table 3. The power of hydrogen bonds can be classified as strong (bond length is between 1.2 Å to 2.2 Å and the angle is between 175° to 180°), moderate (bond length is between 1.5 Å to 2.2 Å and the angle is between 130° to 180°), and weak (bond length is between 2.2 Å to 3.2 Å and the angle is between 90° to 150°) [18]. As it can be seen in Table 3, for H2L(H2O)4, the bond length between atom H6, from boric acid, and O9, from water, is 2.124582 (dH6O9 = 2.124582). In addition, for H2L-(H2O)3, the bond length between atom O2, from boric acid, and H19, from water, is 2.098563 (dH19O2 = 2.098563). These data shows that for boric acid, the power of H-bonding between H2L(H2O)4 and water and also, between H2L-(H2O)3 and water are classified as moderate. It must be noted that IHBs data can be used in the design of benefit and help us to predict Nano drug [19].


DISCUSSION AND CONCLUSION: In this research work, we showed the feasibility of a theoretical method, DFT and ab ignition, to calculate the ionization constants of boric acid at T = 298.15 K. As a result, we selected various acid-base reaction that include the solvation of the hydrogen, hydroxyl ions, and other anions or neutral molecules in protic solvents such as water, which process a high hydrogen-bond-donor capability. The calculations performed at the B3LYP/6-31+G(d) levels of theory using Tomasi s method allowed us to prove that neutral molecules and anions form IHBs with some molecules of water. In addition, the comparison between experimentally determined and theoretically calculated pKa,s, for boric acid, shows that there is a good agreement between them at 298.15 K.
Abstract

8.Cleaning method validation for estimation of dipyridamole residue on surface of the drug product manufacturing equipment using the swab sampling and by using high performance liquid chromatographic technique.
Sriram Valavala, Nareshvarma seelam, Subbaiah Tondepu, Vivekanandan Sundaramurthy
Pages 182 - 189
INTRODUCTION: The cleaning validation is the procedure use to ensure the cleaning process to eliminate the residues of the drug substance after drug product manufactured in the equipment surface. A simple, sensitive, robust, accurate HPLC method was developed for the quantitative estimation of dipyridamole in the swab samples from drug product manufacturing of the Dipyridamole modified release capsules equipment surface after manufacturing.
METHODS: The method was developed by using Hypersil BDS C18 (150 mm x 4.6 mm, 5 µm) column with mobile phase containing mixture of buffer (Potassium dihydrogen phosphate buffer, pH 7.0 ± 0.05) and methanol in the ration of 30: 70 v/v, flow rate 1.5 mL/min, column temperature 45°C and injection volume as 5µL.
RESULTS: The method was validated, the specificity study was conducted to prove that, there was no interference from blank and swab blank at the retention time of dipyridamole. The limit of detection and limit of quantification limit was established by using the series of linearity solutions and found 0.041 µg/mL and 0.124 µg/mL respectively. The method precision at limit of quantification level 8.6 % RSD, Method precision 0.2 % RSD and ruggedness study results were found 0.3 % RSD. The method was accurate from the concentration of 0.13 µg/mL to 21.80 µg/mL, the recovery results were meeting the acceptance criteria. The linearity of the method was found from 0.12 µg/mL to 20.14 µg/mL and found (r2) value is 0.997. The robustness study for the flow rate, wave length, column temperature, Buffer pH and Mobile phase ratio variations were conducted, and all the system suitability parameters were meeting.
DISCUSSION AND CONCLUSION: The method validation was performed as per the regulatory requirements and guidelines. The validation parameters were meeting the acceptance criteria and proposed method can be applied for the intended swab routine analysis.
Abstract

9.Inhibitory Effect of Roselle Aqueous Extracts-HPMC 6000 Gel on the Growth of Staphylococcus aureus ATCC 25923
isnaeni isnaeni, esti Hendradi, Natalia Zara Zettira
Pages 190 - 196
INTRODUCTION: Roselle (Hibiscus sabdariffa L.) is one of medicinal plants commonly used as beverage herbal medicine. Complexity compounds in the aqueous extracts have provided good antibacterial activity by which growth of Gram negative and positive bacteria are inhibited. The aims of this research were to formulate HPMC 6000 gel containing the extract and investigate inhibitory activity of the extract and its gel formula against Staphylococcus aureus ATCC 25923.
METHODS: Thin-layer Chromatography on Silica-gel GF254 was used for analyzing flavonoids and Polyphenols using butanol-acetic acid-water (4: 1: 5) and chloroforms-ethyl acetate-formic acid (0.5: 9: 0.5) as eluent, respectively. The serial dilution of aqueous extracts powder in citrate buffer was made to obtain 0.50, 0.25, 0.10, 0.05 and 0.02 mg/mL solution. The Roselle aqueous extracts (3%) was formulated as a component of gel containing HPMC 6000 in various concentrations (2%, 3%, and 4%). A diffusion agar method on two layers of nutrient agar media was applied using Staphylococcus aureus ATCC 25923 and gentamicin 25 ppm as bacterial test and standard respectively. After incubating for 24 hours at 37°C, the inhibitory effect was denoted by clear zone around the hole and the inhibitory activity was measured as MIC.
RESULTS: The aqueous extract of Hibiscus sabdariffa L. contained flavonoid and polyphenol compound based on the TLC-chromatogram profile. It was found that the gel formula containing 3% of HPMC 6000 and the aqueous extract 3% gave a good physical characteristic and the lowest MIC (6.0 mg/ml), equivalent to 7.58 ppm of gentamicin standard at 12.0 mg/mL concentration.
DISCUSSION AND CONCLUSION: The HPMC 6000 at 3% (w/w) concentration in Roselle aqueous extracts gel preparation gave good physical characteristics. The gel preparation exhibited inhibitory activity against Staphylococcus aureus ATCC 25923 depicted by Minimum Inhibitory Concentration 6.0 mg/mL. The formula 2 is recommended and prospects for further investigated to be implemented as topical preparations.
Abstract

SHORT COMMUNICATION
10.Evaluation of Antioxidant Potency on Seseli L. Species (Apiaceae)
Alev - Önder, Ahsen Sevde Çınar, Sezen - Yılmaz Sarıaltın, Mehmet Necat İzgi, Tülay - Çoban
Pages 197 - 202
GİRİŞ ve AMAÇ: Bu çalışmada, Seseli L. türlerinin toprak üstü kısımlarından elde edilen, etil asetat (AcOEt) ve metanol (MeOH) ekstrelerinin antioksidan potansiyelleri ilk kez araştırılmıştır.
YÖNTEM ve GEREÇLER: Türkiye'de yetişen bazı Seseli L. türleri, Seseli andronakii Woronow ex Schischk., S. campestre Besser, S. corymbosum Boiss. & Heldr., S. gummiferum subsp. gummiferum Pall. ex Sm., S. hartvigii Parolly & Nordt, S. libanotis (L.) W. Koch, S. petraeum M. Bieb., S. arenarium M. Bieb., S. resinosum Freyn & Sint., S. tortuosum L., DPPH (1,1-difenil-2-pikrilhidrazil) radikal süpürücü yöntem ve LPO (lipit peroksidasyon inhibisyonu) yöntemleri kullanılarak antioksidan kapasiteleri değerlendirilmiştir.
BULGULAR: Seseli arenarium (IC50=0.49 mg/mL) ve S. libanotis (IC50=0.75 mg/mL) EtOAc ekstrelerinde en yüksek radikal süpürücü etki bulunmuş, α-tokoferol pozitif control olarak kullanılmıştır. Diğer yandan, LPO deneyinde, S. tortuosum ve S. libanotis (84-94%)’in EtOAc and MeOH (5 mg/mL dozda) ekstrelerinde tespit edilmiştir.
TARTIŞMA ve SONUÇ: Bu çalışmada, Seseli L. türlerinin antioksidan kapasitesi hakkında önemli bilgiler verilmiştir. Antioksidan kapasiteleri üzerine yapılan bu araştırma ile, bazı türlerin Doğu Anadolu'da gıda olarak (salatalarda) kullanımının doğruluğu bir kez daha gösterilmektedir. Türkiyede yetişen Seseli L. türlerinde yapılan bu tarama çalışması ile, gelecekte, antioksidan etki gösteren bileşiklerin en aktif Seseli L. türlerinden izole edilmesi planlanmaktadır.
INTRODUCTION: In the present study, the antioxidant potency of ethyl acetate (AcOEt) and methanol (MeOH) extracts from aerial parts of Seseli L. species have been investigated for the first time.
METHODS: The Seseli species L. such as Seseli andronakii Woronow ex Schischk., S. campestre Besser, S. corymbosum Boiss. & Heldr., S. gummiferum subsp. gummiferum Pall. ex Sm., S. hartvigii Parolly & Nordt, S. libanotis (L.) W. Koch, S. petraeum M. Bieb., S. arenarium M. Bieb., S. resinosum Freyn & Sint., S. tortuosum L. growing in Turkey were collected and evaluated for antioxidant capacity by using DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging method and LPO (lipid peroxidation inhibition) methods.
RESULTS: The highest activities as scavenger DPPH radical were found in the AcOEt extracts of Seseli arenarium (IC50=0.49 mg/mL) and S. libanotis (IC50=0.75 mg/mL), α-tocopherol used as positive control. On the other hand, in the LPO assay, the highest activities were determined in AcOEt and MeOH extracts (at 5 mg/mL) of S. tortuosum and S. libanotis (84-94%).
DISCUSSION AND CONCLUSION: This report is given considerable information about the antioxidant capacity of Seseli L. species. This research on antioxidant capacity proves that the use of some species used in Eastern Anatolia is correct. With this screening study performed in Seseli L. species grown in Turkey, in the future, it is planned to isolate antioxidant compounds from the most active strains of Seseli L..
Abstract

11.Comparative in vitro and in vivo evaluation of fenofibric acid as anti-hyperlipidemic drug
Yulias Ninik Windriyati, Yeyet Cahyati Sumirtapura, Jessie Sofia Pamudji
Pages 203 - 210
INTRODUCTION: Fenofibric acid (FA) is antihyperlipidemic agent and commercially available as a tablet formulation weighs 840 mg for 105 mg active substance. A new formulation with less inactive substance was developed as an alternative to conventional formulation. The purpose of this study was to evaluate the dissolution study and the relative bioavailability of the surface solid dispersion (SSD) and conventional formulations of FA by comparing them to the reference formulation in its commercial tablets. The in vitro-in vivo correlation (IVIVC) among these tablet formulations was also evaluated.
METHODS: The dissolution study was performed in phosphate buffer pH 6.8 and biorelevant Fasted State Simulated Intestinal Fluid (FaSSIF). Dissolution efficiency (DE) and mean dissolution time (MDT) was used to compare the dissolution profiles. The bioavailability study using nine healthy volunteers was conducted based on a single-dose, fasted, randomized, crossover design. The in vivo performance was compared using pharmacokinetic parameters Cmax, Tmax, AUC0-72, and AUC0-∞. Linear correlation model was tested using MDT and mean residence time (MRT).
RESULTS: The results indicated that there were significant differences found in the dissolution performances and no significant differences observed among the mean Cmax, Tmax, AUC0-72, and AUC0-∞, estimated from the SSD, conventional, and reference formulations.Poor correlation was found between MRT and MDT of three formulations.
DISCUSSION AND CONCLUSION: The SSD formulation led to an instantaneous dissolution due to the presence of the polymer and physical structure of the SSD. The conventional formulation could not achieve rapid dissolution despite it satisfied the requirement for immediate drug release dosage form. The both formulations could be considered bioequivalent with reference.The in vitro dissolution behavior of fenofibric acid using single medium did not reflect their in vivo properties at the fasted condition. There was no correlation between the in vitro dissolution and the in vivo bioavailability of fenofibric acid at this condition.
Abstract

12.Ethnobotanical study of medicinal plants in the Aziziye district (Erzurum, Turkey)
Songül KARAKAYA, Ahmet Polat, Özkan Aksakal, Yusuf Ziya Sümbüllü, Ümit İncekara
Pages 211 - 220
GİRİŞ ve AMAÇ: Sunulan bu araştırma, Erzurum'un batı kesiminde yer alan Aziziye ilçesinde yaşayan insanların kullandıkları şifalı bitkilerin kullanımı, kullanılan bitki kısımları, ve hazırlama yöntemlerini belgelemek amacıyla yapılmıştır.
YÖNTEM ve GEREÇLER: Yerel halkın terapötik amaçlar için kullandığı şifalı bitkiler toplanıp, teşhis edildi. Geleneksel bitkisel ilaçlarla ilgili bilgiler toplandı; Herbaryum materyalleri hazırlandı; Atatürk Üniversitesi Fen Fakültesi Herbaryumu'na konuldu. Bilgiler, açık ve yarı yapılandırılmış görüşme ve anketler yoluyla elde edildi.
BULGULAR: Araştırmada 30 familyaya ait toplam 77 tıbbi bitki tanımlanmıştır. Bu türlerin 62’si doğal olarak yetişmekte ve 15 türün de ekimi yapılmaktadır. En yaygın tıbbi bitkiler Asteraceae (14), Rosaceae (7), Lamiaceae (5) ve Apiaceae (5) familyalarına aittir. En yaygın hazırlıklama şekli dekoksiyondur.
TARTIŞMA ve SONUÇ: Bu çalışmada elde edilen etnobotanik sonuçlar, şifalı bitkilerin Aziziye ilçesi sakinleri arasında kullanımı hakkında pratik veriler sunmaktadır. Dahası, bu sonuçlar kırsal topluluklar arasında kullanılan bölgenin şifalı bitkilerin, birinci basamak sağlık hizmetleri için önemli bitkisel ilaç kaynağı olduğunu ortaya koymaktadır. Bu araştırma, yeni bitki bazlı ticari ilaçların iyileştirilmesinde daha fazla bilimsel araştırma için temel bilgi kaynağı olarak kullanılabilir. Genç nesillerde şifalı bitkilerin geleneksel kullanımı ile ilgili bilgi kaybı yaşanmaktadır.
INTRODUCTION: The present research was conducted to document the usage of medicinal plants, plant parts utilized, and methods of preparation by the people living Aziziye district, situated in the West part of Erzurum.
METHODS: The medicinal plant species utilised by local people for remedial aims were collected and identified. The related knowledge about conventional herbal medicine was collected; herbarium materials were prepared; and they have been stored in the Herbarium of Faculty of Science, Ataturk University. The knowledge was acquired via semi-structured and unstructured interviews.
RESULTS: A total of 77 medical plants pertaining to 30 families were defined in this research. Amongst these, 62 species grew natural distribution and 15 species were cultivated. The most widespread medicinal plant families were Asteraceae (14), Rosaceae (7), Lamiaceae (5) and Apiaceae (5). The most widespread preparations was decoction.
DISCUSSION AND CONCLUSION: The ethnobotanical outcomes documented in this study provides practical evidence about the use of medicinal plants among the inhabitants of the Aziziye county. Furthermore, the results revealed that the medicinal plants of the region are a major resource of herbal drugs for primary health care utilized among the rural communities. This survey can be utilized as baseline knowledge for further scientific research to improve new plant-based commercial drugs. There is a gradual loss of traditional information as regards usage of medicinal herbs in younger generations.
Abstract

13.statistical design, optimisation of sustained release formulations of pravastatin
Raghavendra Kumar Gunda, Prasadarao Rao Manchineni
Pages 221 - 227
GİRİŞ ve AMAÇ: Bu çalışmanın amacı, Biyofarmasötik Sınıflandırma Sistemi III grubunda olan lipit düşürücü etkili Pravastatinin sürekli salım yapan formülasyonlarını geliştirmektir.
YÖNTEM ve GEREÇLER: Pravastatin 'in sürekli salimli tabletleri, 32 faktör tasarımına göre çeşitli oranlarda HPMCK4M ve Sodyum Karboksi Metil Selüloz kullanılarak hazırlanmıştır. Bağımsız değişkenler Pravastatin 'in uzun süreli salınımını elde etmek için gerekli HPMCK4M (X1) ve Sodyum Karboksi Metil Selüloz miktarı (X2); bağımlı değişkenler ise sırasıyla % 10,% 50,% 75,% 90 ilaç salımı için geçen süre seçilmiştir.
BULGULAR: 9 formülasyon geliştirilmiş ve bu formülasyonlara farmakopede belirtilen kontrol testleri uygulanmıştır. Geliştirilen tüm formülasyonların standart limit değerler arasında olduğu tespit edilmiştir. Tüm çözünme hızı sonuçları ilaç salım kinetikleri açısından değerlendirilmiştir. Polinomyal denklemler bağımlı değişkenler için geliştirilmiş ve doğrulanmıştır. 25 mg HPMCK4M ve 25 mg SCMC içeren formülasyondan (F5) Pravastatin salımı, piyasa preparatı (PRAVACHOL) ile benzer bulunmuştur (benzerlik faktörü f2 = 89.559, fark faktörü f1 = 1.546).

TARTIŞMA ve SONUÇ: En iyi formülasyonun (F5), Higuchi kinetiği, Fick kanununa uymayan Difüzyon Sıfırıncı derece kinetiği (n = 0.864) takip ettiği bulunmuştur
INTRODUCTION: The objective of current study is to formulate the sustained release formulation for Pravastatin. Pravastatin, an lipid lowering, BCS class-III agent.
METHODS: The Sustained Release tablets of pravastatin were prepared employing variable amounts of HPMCK4M and Sodium Carboxy Methyl Cellulose in various proportions by Direct Compression as per 32 factorial design. Amount of polymers, HPMCK4M and Sodium Carboxy Methyl Cellulose required to obtain the prolonged release of drug was chosen as independent variables, X1 and X2 respectively whereas, time taken for 10%, 50%, 75%, 90% of drug release were chosen as dependent variables.
RESULTS: 9 formulations were developed and are checked for pharmacopoeial tests. Results shows that all the factorial batches were lie with in the standard limits. Dissolution parameters of all formulations were subjected to kinetic fitting, various statistical parameters were determined. Polynomial equations were developed and verified for dependent variables. Formulation (F5) containing 25 mg of HPMCK4M and 25 mg of SCMC, is the most identical formulation (similarity factor f2=89.559, difference factor f1=1.546) with the marketed product (PRAVACHOL).
DISCUSSION AND CONCLUSION: Best formulation (F5) follows Higuchi’s kinetics, Non-Fickian Diffusion Zero order kinetics (n= 0.864).
Abstract

14.Extended Hildebrand Solubility Approach: Prediction and correlation of solubility of itraconazole in triacetin: water mixtures at 298.15K
Sachin Jagdale, RAJESH B NAWALE
Pages 228 - 234
INTRODUCTION: Context:
The solubility predictive methods based upon physicochemical properties of drug and solvent are of utmost importance in the design, development and optimization of various pharmaceutically important processes.
Aims:
To explore the suitability of empirical approach of Extended Hildebrand Solubility Approach (EHSA) to predict and correlate the solubility of crystalline drug itraconazole (ITRA) in triacetin: water mixtures.

METHODS: The physicochemical properties of ITRA like fusion enthalpy, solubility parameter, and ideal mole fraction solubility were estimated. The solubilities of ITRA in mixed solvent blends comprised of triacetin: water were determined at 298.15K. Theoretical solubilities were back calculated using polynomial regression equation of interaction energy parameter 'w' as a function of solubility parameter (δ_1) of solvent mixture. Similarly, the solubilities were predicted with direct method based on use of logarithmic experimental solubilities (〖logX〗_2) against solubility parameter (δ_1) solvent mixture. The predictive capabilities of both EHSA and direct method were compared using mean percent deviations.
RESULTS: The solubility of ITRA was increased in all the triacetin: water blends and was highest in the blend where solubility parameter of ITRA equaled with that of solvent mixture. The prediction capacities of direct method (mean % deviation was -1.89%) were better than EHSA (mean % deviation was 9.76%) in the fifth order polynomial regression equation.
DISCUSSION AND CONCLUSION: The results indicated that solubility of any crystalline solute can be adequately predicted and correlated with the mere knowledge of physicochemical properties and EHSA. The information obtained would be of help in process and formulation development.
Abstract

15.Psychoactive Bath Salts and Neurotoxicity Risk
Beril Altun, İsmet Çok
Pages 235 - 241
Sentetik katinonlar, mevcut yasa ve cezaları atlatabilmek amacıyla, kokain, amfetamin ve 3,4-metilendioksimetamfetamin (ekstazi) gibi yasadışı maddelerin etkilerini taklit etmek ve benzer ödüllendirici etkiler yaratmak üzere geliştirilmiş halüsinojenik ve psikostimulan özellikte yeni tasarım maddelerdir. "Banyo tuzları" olarak da bilinen sentetik katinonlar, 2000'li yılların ortalarından itibaren özellikle genç bireyler arasında popüler hale gelmeye başlamıştır. Diğer psikomotor uyarıcılara benzer şekilde, sentetik katinonlar da, dopamin, norepinefrin ve serotoninin plazma membran taşıyıcılarını hedef alarak sinaptik aralıktaki monoamin konsantrasyonunu arttırmaktadır. Amfetaminlere olan yapısal benzerlikleri nedeniyle, sentetik katinonların amfetamin homologları ile benzer nörotoksisite profiline sahip olabileceği düşünülmüştür. Bu nedenle, sentetik katinonların striatum, hipokampus ve kortekste monoamin sinir uçları üzerinde nörotoksisiteyi indükleyebileceği hipotezi öne sürülmüştür. Şimdiye dek sentetik katinonların nörotoksisitesi ile ilgili olarak yapılan in vitro/in vivo deneysel çalışmalarda, monoamin deplesyonu, biyosentetik enzim inhibisyonu, sitotoksisite, reaktif oksijen türlerinin oluşumu, pro-oksidasyon durumu ve nöroinflamasyon indükleme yeteneği gibi parametreler incelenmiştir. Sentetik katinonların nörotoksik etkiler açısından amfetamin homologlarından daha ılımlı olduğu görülmektedir. Ancak pekçok sentetik katinon kullanıcısının bu maddeleri benzodiazepinler, amfetaminler, ekstazi, tetrahidrokannabinol (THC) ve etanol gibi diğer ilaç ve uyuşturucu maddeler birlikte alması, nörotoksik etkileri modifiye edebilmektedir. Bu nedenle, çoklu madde maruziyeti durumundaki erken nörotoksik etkilerin anlaşılması önemlidir. Bu derlemede, sentetik katinonların suistimal potansiyeli, yasal statüsü, etki mekanizması ve özellikle nörotoksik etkileri hakkında bilgi verilmesi amaçlanmıştır.
Synthetic cathinones are new designer drugs that possess hallucinogenic and psychostimulant properties, designed to mimic the effects of illegal substances such as cocaine, amphetamines and 3,4-methylenedioxymethamphetamine (ecstasy) and to produce rewarding effects by circumventing existing laws and penalties. Synthetic cathinones, also entitled as ‘bath salts’, have become popular particularly among young people since mid-2000s. Similar to other psychomotor stimulants, synthetic cathinones have potential to increase monoamine concentration in synaptic cleft by targeting plasma membrane transporters of dopamine, norepinephrine and serotonin. Because of their structural similarities to amphetamines, it has been suggested that synthetic cathinones may have a similar neurotoxicity profile with their amphetamine congeners. Therefore, it has been hypothesized that synthetic cathinones may induce neurotoxicity on monoamine nerve endings in the striatum, hippocampus, and cortex. By now, with regard to synthetic cathinone neurotoxicity, parameters such as monoamine depletion, biosynthetic enzyme inhibition, cytotoxicity, generation of reactive oxygen species, pro-oxidation status and the ability to induce neuroinflammation were investigated both in vitro/in vivo experimental studies. Compared with amphetamines, synthetic cathinones seem to be more moderate than their amphetamine congeners in terms of neurotoxic effects. Many synthetic cathinone users take these substances simultaneously with other drugs such as benzodiazepines, amphetamines, ecstasy, tetrahydrocannabinol (THC) and ethanol so as to modify toxicity. Hence, it is important to understand the underlying mechanism of early neurotoxic effects in case of poly-substance use. In this review, it is aimed to summarize synthetic cathinones’ abuse liability, legal status, mechanism of action and particularly their neurotoxic effects.
Abstract