bluuebunny/crossref_metadata_2025_split huggingface dataset:
DEVELOPMENT AND VALIDATION OF STABILITY INDICATING RP-UPLC METHOD FOR THE QUANTIFICATION OF BALOXAVIR MARBOXIL IN TABLET FORMULATION
Authors: RAVEENDRANATH T. VENKATA , SARAVANAKUMAR R. T. , ANJANA C. H. K. V. L. S. N. 
Published: November 2020

Objective: Aim of the present work is to develop a simple, accurate and precise stability-indicating method for the quantification of baloxavir marboxil (BLMX) in tablet dosage form by UPLC.
Methods: Chromatographic elution was processed through a HSS C18 (100 x 2.1 mm, 1.8 mm) reverse phase column and the mobile phase composition of buffer 0.1% orthophosphoric acid and acetonitrile in the ratio of 50:50 was processed through a column at a flow rate of 0.3 ml/min. Column oven temperature was maintained at 30 °C and the detection wavelength was processed at 240 nm.
Results: Retention time of BLMX was found to be 0.87 min. Repeatability of the method was determined in the form of %RSD and the value was 0.2. The percentage mean recovery of the method was found to be 99.47%. LOD, LOQ values obtained from the regression equation of BLMX were 0.69 and 2.10 mg/ml, respectively. Regression equation and correlation coefficient values of BLMX were y = 16994x+7179.2 and 0.9996. Drug was subjected for acid, peroxide, photolytic, alkali, neutral and thermal degradation studies and the results shown that the percentage of degradation was found between 5.96% and 9.55%.
Conclusion: Retention time and total run time of the drug was decreased and the developed method was simple and economical. So, the developed method can be adopted in industries as a regular quality control test for the quantification of BLMX.
A MASS COMPATIBLE UPLC METHOD FOR THE QUANTIFICATION OF IMPURITIES IN FLUTICASONE PROPIONATE NASAL SPRAY
Authors: RAO MUGADA RAVI PRASADA , THOTA RAMA KRISHNA , SENTHI MAHIBALAN , MOGADATI PAUL , ARUTLA SRINIVAS 
Published: November 2020

Objective: The objectives of the present study were to develop and validate a mass compatible ultra-performance liquid chromatography (UPLC) method to quantify the impurities in fluticasone nasal spray, and to establish a suitable container-closure system for the formulation.
Methods: A gradient method was optimized with a flow rate of 0.5 ml/min, detector wavelength-240 nm, run time-25 min and 0.1% Trifluoroacetic acid (TFA) in water as solvent A and Methanol as solvent B.
Results: The developed method was linear over the range of 0.07-1.10 µg/ml for impurity-I, 0.16-2.47 µg/ml for impurity-II, 0.67-10.0 µg/ml for impurity-III, and 1.29-19.3 µg/ml for impurity-IV. The limit of quantification (LOQ) and limit of detection (LOD) were established as 0.07 and 0.02 µg/ml, 0.14 and 0.05 µg/ml, 0.59 and 0.19 µg/ml, 1.06 and 0.35 µg/ml for impurities I-IV respectively. The percent relative standard deviation (%RSD) of the replicate analysis for impurities I-IV, was within the acceptance criteria (0.4, 0.2, 0.3, and 0.1% respectively) that proved the precision of the method. The accuracy of the method was studied from 50%-150% of test concentration and the results ranged from 100.3% to 109.4%. The container-closure compatibility study revealed that the solution stored in the glass container system did not generate any additional peaks in the chromatogram.
Conclusion: Hence, the developed method can be employed by quality testing laboratories to quantify impurities in fluticasone propionate nasal spray. The study also suggests that glass containers could serve as a compatible system for the storage of fluticasone propionate nasal solution.
EFFECT OF BOILING AND MICROWAVE COOKING ON NUTRITIONAL, ANTI-NUTRITIONAL AND TOXICITY OF WILD EDIBLE PLANTS OF NORTH-EASTERN REGION IN INDIA
Authors: SEAL TAPAN 
Published: November 2020

Objective: The target of this appraisal was to explore the impacts of various cooking techniques, for example, boiling and microwave cooking on nutritional, antinutritional, minerals content and in vitro toxicity of ten wild consumable plants viz. Zanthoxylum acanthopodium, Viburnum foetidum, Houttuynia cordata, Sonchus arvensis, Oenanthe linearis, Perilla ocymoides, Clerodendrum colebrookeanum, Solanum gilo, Solanum kurzii, Potentilla lineata, widely consumed by the common individuals of North-Eastern area in India.
Methods: The proximate parameters like ash, moisture, protein, fat, fibre, carbohydrate, energy content, minerals viz. sodium, calcium, potassium, iron, magnesium, manganese, copper, zinc and antinutritional parameters like oxalate, phytate, tannin, saponin, cyanogenic glycoside content were evaluated in the selected wild edible plants using standard food analysis techniques. In vitro haemolytic toxicity of aqueous extracts (100, 300 and 500µg/cc) of ten palatable wild plants was done with the blood samples were gathered from healthy rat, mixed with Ethylenediaminetetraacetic acid(EDTA) and centrifuged at 5,000 Revolutions Per Minute (rpm) for five minutes. The 10 % erythrocyte suspension was set up in sterile Phosphate buffer saline (PBS, pH 7.4) for haemolytic examination. The genotoxic potential of the concentrates were assessed by a single-cell gel electrophoresis comet test. Cytotoxicity studies were evaluated with fresh goat livers procured from the local market were perfused in PBS (pH 7.4) with collagenase and the liver was then minced in minute pieces and cells were isolated utilizing cell strainer.
Results: Both cooking medications diminished the congregations of ash, fat, minerals, antinutritional parts and the destructive nature of the consumable plants while the carbohydrate and fiber substance were expanded. The protein focuses in the wild edibles were expanded fundamentally (P<0.05) in the range from 1.26 to 10.45% on microwave cooking while the indistinguishable were exhausted in the range out of 2.20 to11.55% on boiling treatment. The microwave cooking demonstrated lesser misfortunes in minerals in the consumable plants than those cooked by frothing. The microwave cooking also caused the colossal rot (P<0.05) of antinutritional parameters and damaging tendency to a more significant degree than the sputtering medications of the wild edibles.
Conclusion: Therefore, the outcomes uncovered that microwaving of appealing plants could be prescribed to expand the supporting quality and to diminish the fat, threatening to dietary structure and lethality. The toxicity assessment of the consumable plants at cell and genomic level showed that these are harmless to consume.
SYNTHESIS AND EVALUATION OF TASTE-MASKED IONIC LIQUID SALTS OF LORATADINE
Authors: GONDANE PRADNYA , SAPKAL NIDHI P. , JAISWAL NIDHI 
Published: November 2020

Objective: To synthesize and evaluate taste-masked ionic liquid (IL) salts of loratadine.
Methods: In the present work, pharmaceutically active IL salts of loratadine using selected counter-ions were synthesized. The synthesized IL salts were characterized using melting point, Ultraviolet (UV) spectroscopy, Fourier Transform Infra-Red (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC), and X-ray Diffraction (XRD). These salts were also evaluated for solubility, dissolution, and palatability studies.
Results: All synthesized IL salts of loratadine exhibited melting points below 100 °C. UV spectral data and FTIR data confirmed the formation of new salt forms with selected counter-ions. The absence of sharp melting point peaks during DSC studies revealed the amorphous nature of new salt forms. During XRD studies, loratadine-indomethacin IL salt yields completely amorphous compound while the intensity of characteristic peaks of loratadine was found to be reduced with other counter-ions. Solubility studies revealed that the solubility of loratadine is reduced from 35.85 mg/ml to 3.63 mg/ml, 15.39 mg/ml, 5.31 mg/ml, and 3.71 mg/ml in case of IL-1, IL-2, IL-3, and IL-4, respectively. Dissolution studies further confirmed this finding. Except for oleate, all the IL salts were found to be palatable by subjects with the score ranging from 2.5 to 2.8, which is the standard range for palatability.
Conclusion: Results obtained in the present work indicated that IL salts of loratadine can be synthesized successfully using selected counter-ions. This approach can be used to mask the bitter taste of pure loratadine and thus can be used for the development of drug products intended for children.
ADRENALINE AMPOULES QUALITY ASSESSMENT–THE ISRAELI EXPERIENCE
Authors: ZUR MEITAL , STEPENSKY DAVID , GORENBEIN PAVEL 
Published: November 2020

Objective: To characterize the differences in stability of L-adrenaline in adrenaline ampoules from different manufacturers that are used by the Israel Defense Forces (IDF).
Methods: Adrenaline ampoules from three different vendors (Products A, B and C; 52, 13, and 19 batches, respectively) were purchased by the IDF and were stored under the recommended storage conditions (room temperature) for different time periods. The content of L-adrenaline in these samples was determined using a chiral high-performance liquid chromatography (HPLC) assay with UV detection.
Results: The three analyzed drug products showed very dissimilar patterns of L-adrenaline degradation. The content of L-adrenaline in Product C was variable and declined below the 85% threshold much earlier than at the end of the 24-months storage period. Products A and B had less variable content of L-adrenaline and were more stable.
Conclusion: L-adrenaline is prone to degradation in solution. Its content in adrenaline ampoules from certain vendors can decline rapidly, below the stipulated threshold, and compromise their clinical effectiveness (e. g., during resuscitation). Stability of adrenaline ampoules from individual vendors should be analyzed at different storage conditions, using a chiral HPLC-based assay, to define the shelf-life period that can differ substantially between the vendors.
CNS DEPRESSION POTENTIAL EVALUATION, FORMULATION AND CHARACTERIZATION OF LYOPHILIZED HERBAL ORAL CAKE OF TERMINALIA CHEBULA FRUITS
Authors: ISLAM MD. MONIRUL , ANISUZZMAN MD. , BILLAH MUHAMMAD MASUM , ZILANI MD. NAZMUL HASAN , NAHAR SABIKUN , AMED MD. IQBAL , SALAM FAYAD BIN ABDUS 
Published: November 2020

Objective: Terminalia chebula fruits are used as traditional herbal medicine from the ancient era but still now, the extract has not revealed any research data on CNS depression activity as well as its lyophilized herbal formulation. The present study was designed to evaluate CNS depression activity and develop lyophilized oral cake of Terminalia chebula fruit extract.
Methods: CNS depression potential of Terminalia chebula fruit was examined using the hole board, hole cross, and thiopental sodium induced sleeping time test. The human equivalent dose was calculated based on US FDA guidelines of dose conversion between animals and humans. A novel lyophilized herbal oral cake of aqueous extract of Terminalia chebula fruits with additives was then formulated. The formulated cake was subjected to characterize its physicochemical properties such as appearance, residual humidity, drug content, dissolution, and drug release profile, extract-polymer compatibility by Fourier-transform infrared spectroscopy (FTIR) and stability. The prepared cake was further evaluated with the hole board and hole cross model in mice and compared with control to ensure its CNS depression activity.
Results: Crude extract at the doses of 100, 150, 200, and 400 mg/kg body weight showed significant (p<0.01) dose-dependent inhibition of locomotor behavior. Crude extract dose of 200 mg/kg body weight in mice compared with standard diazepam dose (1 mg/kg) was used to calculate the human equivalent dose of 1000 mg/60 kg. The formulation presented a rapid drug release profile while drug content was approximately 99.5%. FTIR spectroscopy of formulation showed no drug-excipient interaction. The oral cake at the dose of 200 mg/kg body weight showed significant (p<0.01) CNS depression activity.
Conclusion: CNS depression activity, FTIR, and stability analysis ensure the preservation of active ingredients in the lyophilized oral cake as in the crude extract.
HEPATOCYTE APOPTOSIS INDUCTION BY ACETAMINOPHEN THROUGH MODULATION OF CASPASE/BAX PATHWAY IN MICE
Authors: ABU-AJAMIEH RASHA N. , GHANIM BAYAN Y. , GAMMOH OMAR S. , QINNA NIDAL A. 
Published: November 2020

Objective: Acetaminophen (APAP) overdose contributes to liver damage through modulation of pro-apoptotic processing. This study evaluated the involvement of caspase/Bax factors in APAP hepatotoxicity in vivo and in vitro.
Methods: The involvement of caspase/Bax factors in APAP hepatotoxicity was evaluated in BALB/c mice and on isolated primary mouse hepatocytes. In vitro MTT assay was carried out on primary cultured mouse hepatocytes treated with APAP (2.5, 5, 10 mmol) and Annexin V/PI staining was employed to cell suspension for imaging under fluorescence microscopy. In addition, caspase-3 concentrations were determined in cell lysates. In vivo, mice were treated with a toxic dose of APAP (700 mg/kg) and immunodetection of Bax was made by Western Blot. Vitamin C (Vit C) was used as a hepato-protectant due to its known antioxidant activities.
Results: In vitro dose-dependent increase in mitochondrial electron transport capacity was evident in isolated mouse primary hepatocytes incubated with the high dose of APAP (10 mmol) compared to both nontreated cells and cells pre-treated with Vitamin C (Vit C) (0.5 mmol) (p<0.05). Apoptosis was confirmed in hepatocytes through Annexin V staining after APAP treatment and the signal was reduced when hepatocytes were pre-treated with Vit C. In addition, caspase-3 concentration was decreased in cells pretreated with Vit C prior to APAP exposure. In vivo, Bax immunodetection utilizing western blotting was increased in mice treated with the toxic dose of APAP (700 mg/kg) and attenuated through pre-treatment with Vit C.
Conclusion: Modulation of apoptotic caspase/Bax pathway is present in hepatocytes undergoing APAP-induced toxicity.
EVALUATION OF ETHOSOMAL EPIGALLOCATECHIN-3-GALLATE GEL FORMULATIONS AS AN ANTIOXIDANT AND THERMOGENIC AGENT
Authors: SARHAN WALAA M. , SARHAN OMNIA 
Published: November 2020

Objective: The aim of this study was to investigate in vitro and in vivo behavior of the prepared ethosomal formulations of green tea extract, which in turn would result in enhancing their therapeutic efficacy as antioxidants and thermogenic agents in obese mice.
Methods: Fat Wistar rats were acclimated for at least 7 d in environmentally controlled cages, then they were divided into five groups: 1st received only distilled water, 2nd received an oral dose of green tea extract, in 3rd group green tea extract loaded gel base was applied on the previously shaven dorsal side of rats and in the other 2 groups selected green tea extract loaded Ethosomal gel base were applied on the previously shaven dorsal side of rats. Total antioxidant capacity by ferric reducing ability of plasma (FRAP) method, catalase enzyme activity, malondialdehyde (MDA) and thiobarbituric acid reactive substance (TBARs) levels, and real-time qPCR of UCP2 and 3 were then determined.
Results: Formulation of green tea extract as ethosomal preparations exhibited a controlled release rate due to the reservoir action of ethosomes. The levels of TBARs and MDA were lower in groups supplemented with green tea extracts compared to control group and in groups (3-5) received it transdermal (P<0.0001 in all 3 groups) was lower than group received it orally with P = 0.0081. The messenger RNA levels of UCPs 2 and 3 in BAT were increased in those 3 groups.
Conclusion: The results support the efficiency of ethosomal gel in penetrating the lipid rich biological membrane. The in vivo study confirms the antioxidant and thermogenic behavior of transdermal applied green tea extract.
CEFPODOXIME PROXETIL FAST DISSOLVING TABLETS: COMPARATIVE STUDY
Authors: KUMAR INDER , PANDIT VINAY 
Published: November 2020

Objective: In the present investigation, fast dissolving tablets of cefpodoxime proxetil were formulated using superdisintegrants to impart fast disintegration.
Methods: In the current study, 12 formulations of fast dissolving tablets of cefpodoxime proxetil were formulated using two different approaches viz., direct compression and sublimation. Three different superdisintegrants viz., croscarmellose sodium, sodium starch glycolate, and crospovidone were used in a different concentration in all the respective formulations. The final powder blend was subjected for the pre-compression evaluation and all the formulations were evaluated for post-compression parameters. Stability studies were also evaluated for the best formulations as per ICH guidelines. Finally, results were statistically analyzed by the application of one way ANOVA test and t-test.
Results: Among all the formulations of different approaches, formulation cefpodoxime proxetil 4 (CP4) containing 6% crospovidone as a super disintegrant was showed the best results. In vitro dissolution data revealed that formulation CP4 prepared by direct compression method showed 99.387±0.270% drug release within 15 min whereas the percentage release by formulation prepared by using sublimation showed 83.927±0.735% release. The optimized formulation was further subjected to comparative in vitro study with two marketed formulation of different brands.
Conclusion: All the data of all formulations is shows that direct compression approach is the best approach for developing the fast dissolving tablets to enhance the onset of action and bioavailability.
THERAPEUTIC POTENCY OF SWEET ORANGE JUICE OVER LIVER GENOTOXICITY INDUCED BY PESTICIDE LANNATE IN RATS
Authors: BADR THANAA MOSTAFA , MOHAMED NOURA RADY 
Published: November 2020

Objective: The aim of the present investigation was to study the potential effect of sweet orange juice against liver genotoxicity induced by lannate.
Methods: adult 36 female rats were divided into 6 groups: group C (control group), group L (lannate group) injected intraperitoneal (i. p.) with 1 mg/kg b. wt. lannate for one day, group J (orange juice group) orally administered a dose of 0.1 ml/10 g b. wt. of orange juice for 48 h, group J+L received the orange juice prior to lannate, group J with L received lannate in continuous with the orange juice and group L+J received lannate prior to the orange juice. Tested parameters were DNA fragmentation, micronucleus, histopathology examination and biochemical analysis.
Results: it was found that, the intake of lannate caused high DNA fragmentation and significant increase (P<0.001) in the number of micronucleated polychromatic erythrocytes in the bone marrow. Furthermore, lannate exhibited some pathological changes in the liver tissues as well as a significant (P<0.001) decrease in the total antioxidative capacity (TAC) and a significant increase in the total oxidative capacity (TOC). On the other hand, orange juice administration of all treatments (pre-treatment, continuous and post-treatment) gave some amelioration against liver damage induced by lannate. While the best results were evidenced in the continuous treatment group where the juice could attenuate liver DNA fragmentation and significantly decreased (P<0.001) the number of micronucleated polychromatic erythrocytes. In addition, it improved the induced degenerative histopathological changes as well as ameliorated the changes occurred in TAC and TOC significantly (P<0.001).
Conclusion: the antigenotoxic impact of orange juice against lannate was therapeutic and hence can counteract the poisonous effect of the pesticide in people who exposed to it.
NEW DEVELOPED AND VALIDATED SPECTROSCOPIC METHOD FOR THE SIMULTANEOUS ESTIMATION OF TERBINAFINE HYDROCHLORIDE AND FLUCONAZOLE
Authors: THAKUR BHUMIKA , KUMAR INDER 
Published: November 2020

Objective: A new, simple, precise, accurate, and reproducible method or simultaneous equation method was developed and validated for the simultaneous estimation of terbinafine hydrochloride (TH) and fluconazole (FLZ) in pure form.
Methods: Simultaneous estimation of terbinafine hydrochloride and fluconazole was estimated by the ultraviolet (UV) spectrophotometry method. The method was based on the measurement of absorbance at two wavelengths 222 nm and 239 nm, of terbinafine hydrochloride and fluconazole in 0.1N HCl respectively.
Results: Calibration curves terbinafine hydrochloride and fluconazole were found to be linear in the concentration ranges of 0.5-3.0 μg/ml and 80-400 μg/ml, respectively, with their correlation coefficient values (R2) 0.999 and 0.998. LOD and LOQ of TH were found to be 0.067, 0.203 at 222 nm and 0.175, 0.531 at 239 nm, similarly for FLZ; 31.089, 94.210 at 222 nm and 94.380, 286.00 at 239 nm respectively. In the precision study, the % RSD value was found within limits (%). The percentage recovery at various concentration levels varied from 98.50 % to 103.96 % for TH and 97.27 % to 103.83 % for FLZ confirming that the expected method is accurate.
Conclusion: It could be concluded from the results obtained in the present study that this method for simultaneous estimation of TH and FLZ in pure is simple, precise, and economical. The proposed method can be applied successfully for the simultaneous estimation of TH and FLZ in the pure and pharmaceutical dosage form.
PARTIAL AMORPHIZATION OF POORLY-SOLUBLE SIMVASTATIN USP USING MEDIA MILLING IN SYNERGISM WITH SPRAY-DRYING
Authors: DESAI HARITA R. , RAJADHYAX ARCHANA B. , AMIN PURNIMA D. 
Published: November 2020

Objective: The objective of the current study was to explore top down methods of size reduction like high speed homogenisation and media milling in synergism with spray drying in amorphization and solubility enhancement of BCS Class II antilipidemic drug Simvastatin USP.
Methods: Spray-dried micronized simvastatin USP was formulated by homogenisation and media milling of drug suspension in optimized stabilizer solution. Stabilizer combination, duration of homogenisation and ball milling and drug: stabilizer ratio was optimized. The obtained dispersion was transformed into solid powder using spray drying. The obtained Spray-dried micronized Simvastatin USP was evaluated for visual morphology, Infrared spectroscopy, Differential scanning calorimetry, in vitro drug release studies, X-Ray diffractometry, Scanning electron microscopy, contact angle measurement, solubility studies, dispersibility studies and intrinsic dissolution rate testing.
Results: Spray-dried micronized simvastatin USP was found to show amorphization of crystalline Simvastatin USP as confirmed by the absence of drug peak in Differential scanning calorimetry and lowered signal intensity in X-Ray diffraction studies. Spray-dried micronized Simvastatin USP was found to show enhanced drug hydrophilicity and solubility as confirmed by lowering in contact angle and increase in solubility and ease of dispersibility observations. In vitro dissolution testing and intrinsic dissolution rate testing were found to show an increase in drug release from 11% to 79% and 4 mg min-1 cm-2 to 17 mg min-1 cm-2 for drug and Spray-dried micronized Simvastatin USP respectively.
Conclusion: Media milling in synergism with spray-drying was found to be a prospective solubility enhancement technique for poorly-soluble Simvastatin USP.