bluuebunny/crossref_metadata_2025_split huggingface dataset:
Formulation and Characterization of Ciclopirox Olamine Mucoadhesive Effervescent Tablets for Vaginal Delivery
Authors: Rachh Milan R , Barot B S , Parejiya B S , Shelat P K , Deshpande S S 
Published: August 2020

The study was aimed to design and evaluate a new effervescent mucoadhesive vaginal drug delivery system for ciclopirox olamine (CPO), a broad-spectrum antifungal, antibacterial, and anti-inflammatory agent for effective treatment in vaginal candidiosis. Various polymers like Polyox 303, Carbopol 974P, HPMC K4M, Sodium CMC, HPC, Sodium Alginate, Xanthan Gum, Polycarbophil and Chitosan were used in the formulation of CPO effervescent mucoadhesive vaginal tablet (EMVT) employing direct compression as a method of preparation. The effervescent mixture (citric acid and sodium bicarbonate) was incorporated into the formulations to aid quick wetting and mucoadhesion of tablet followed by drug release modulation. The amount of polymer blends and effervescent mixture was optimized using 32 full factorial design. The swelling, mucoadhesive strength and in-vitro release were studied as dependent responses. The ex-vivo mucoadhesion was determined by modified mucoadhesion assembly. The ex-vivo residence test was carried out by modified USP dissolution test apparatus. In vitro anti-fungal activity of the CPO EMVT was determined in comparison to Candid®-V3 tablet. A good sustained effect and a moderate mucoadhesion (0.31N to 0.67N) were obtained with tablets containing HPMC K4M: Polyox 303 (1:1.4) and effervescent mixture (1:3). Ex-vivo mucoadhesion time of all the formulations was in the range of 8 to 24 h. The effervescent CPO tablet showed significantly higher in-vitro antifungal activity as compare to Candid®-V3 tablet (p< 0.05). The results of short term stability revealed stable characteristics of optimized formulation. The proposed formulation may provide a potential antifungal activity against Candida albicans.
Stability Indicating Liquid Chromatographic Method for the Determination of Fenofibrate and its Application to Kinetic Studies
Authors: Rao K. Srinivasa , N K Keshar , Jena N , Rao M.E.B , Patnaik A K 
Published: August 2020

A stability-indicating LC assay method was developed for the quantitative determination of fenofibrate (FFB) in pharmaceutical dosage form in the presence of its degradation products and kinetic determinations were evaluated in acidic, alkaline and peroxide degradation conditions. Chromatographic separation was achieved by use of Zorbax C18 column (250 × 4.0 mm, 5 μm). The mobile phase was established by mixing phosphate buffer (pH adjusted 3 with phosphoric acid) and acetonitrile (30:70 v/v). FFB degraded in acidic, alkaline and hydrogen peroxide conditions, while it was more stable in thermal and photolytic conditions. The described method was linear over a range of 1.0-500 μg/ml for determination of FFB (r= 0.9999). The precision was demonstrated by relative standard deviation (RSD) of intra-day (RSD= 0.56– 0.91) and inter-day studies (RSD= 1.47). The mean recovery was found to be 100.01%. The acid and alkaline degradations of FFB in 1M HCl and 1M NaOH solutions showed an apparent zero-order kinetics with rate constants 0.0736 and 0.0698 min−1 respectively and the peroxide degradation with 5% H2O2 demonstrated an apparent first-order kinetics with rate constant k = 0.0202 per min. The t1/2, t90 values are also determined for all the kinetic studies. The developed method was found to be simple, specific, robust, linear, precise, and accurate for the determination of FFB in pharmaceutical formulations.
New Drugs of 2012: A Concise Overview of the NMEs and Trends for Innovative Brand Market in the United States
Authors: Reddy D Samba 
Published: August 2020

Thirty-nine (39) new drugs have been approved by the U.S. FDA in 2012, a record highest number of approvals since 1996. The record is a sign that pharma companies are poised to tap recent advances from genomics and proteomics. This list includes novel new drugs, known as new molecular entities (NMEs), biologics and new products. Many life-saving drugs are approved for marketing. The list includes a total of 10 drugs for cancer treatment, and nearly a quarter of those approved in 2012 had orphan drug status. Among the breakthrough drugs approved in 2012 were ivacaftor (cystic fibrosis), vasmodegib (skin cancer), HPC-C (human cord blood product), ruxolitinib (myelofibrosis) and a new combination drug to treat HIV. In addition, several unique products were approved for the treatment of macular degeneration, chronic weight management, overactive bladder, actinic keratosis, erectile dysfunction, glaucoma, respiratory distress syndrome, and COPD. The approval of 39 drugs in 2012 underscores a robust success rate and confirms that innovation is once again beginning to pay off. In the existing climate of reduced revenues in the face of generic competitions, the future and survival of big companies rests heavily on their unique niche products. It is apparent that big Pharma and a growing number of emerging Biotechs alike have focused their attention on developing new NMEs for rare diseases. In 2012, the length of the FDA’s review is shorter than agencies in other countries. Innovative models adopted for R&D strategies, communications, and new regulatory changes appear to shorten development timelines. Despite record drug approvals, there is bleak scope for blockbusters because most of these drugs have a limited market. The pipeline for blockbusters appears very low. However, there is unmet medical need for new drugs in autism, Alzheimer’s disease and epilepsy. Overall, the new drug approval list unveils unique and reemerging trends indicating that the pharma companies are poised for big growth from new brands approved for marketing for narrow-spectrum indications.
Formulation and Evaluation of Sumatriptan Succinate Fast Disintegrating Films and Tablets
Authors: Kumar Y. Shravan , Gowthami R , H Sujitha , T Nagaraju , M Rajashekar , Kumar Murali Krishna , Rao Y. Madhusudhan 
Published: August 2020

Sumatriptan succinate is a 5-HT1B/1D receptor agonist which has well established efficacy in treating migraine. The main objective of the study was to formulate Oral Fast Disintegrating Films (ODF) and Oral Fast Disintegrating Tablets (ODT) to achieve a better dissolution rate and further improving the bioavailability of the drug. ODFs were prepared by solvent casting method using film forming polymers like HPMC – E15,5cps,50cps in different ratios & prepared batches of films were evaluated for the drug content, film thickness, disintegration time and in vitro dissolution studies. Among the prepared formulation F7 containing HPMC – 50cps (drug: polymer ratios = 1:1) was found to be best formulations which releases 98.2±1.1of the drug within 17±0.02 sec. ODTs prepared by direct compression method using in different concentrations of super-disintegrants. The prepared formulation T12 (combination of disintegrants) containing CP + CCS (6%) was considered to be the best formulation, which releases up to 100±0.38% of the drug in 23±0.75 sec, respectively. Based on these results, it is suggested that ODFs have faster disintegration time and drug release than ODTs.
Green Synthesis and Evaluation of 3-(Aryl)-2-Thioxo-2,3-Dihydroquinazolin- 4(1H)-ones as Novel Anticonvulsant Drugs
Authors: Sahoo Biswa Mohan , Dinda S C , B V V Ravi Kumar , Panda J.R 
Published: August 2020

Epilepsy is a chronic neurological disorder characterized by recurrent seizure attacks which are caused by an abnormal electrical discharge in the brain. Currently, there is a need for improved medicinal agents to treat epilepsy, since the currently available drugs are effective only in 60-80% of epileptic patients. So the indirect type of molecular modeling study was carried out to find out the 3D structural similarity between some reported anticonvulsant drugs and the newly designed quinazolinone derivatives. Thus, a new series of 3-(aryl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-ones were synthesized using an appropriate synthetic route. Microwave radiation provides an alternate to conventional heating for rapid synthesis of drug molecules. The ideal features of microwave-assisted organic synthesis (MAOS) involve reduction of time for a chemical reaction, instantaneous and uniform heating, carrying out solvent free reactions, and possibility of parallel synthesis. It has proved a bonanza for the researchers involved in drug development and discovery processes such as high-speed combinatorial chemistry. In aqueous mediums, it has resulted in the development of relatively sustainable and environmentally benign protocols for the synthesis of novel drugs. MAOS under controlled conditions has many applications in the field of medicinal chemistry and pharmaceutical research. All the newly synthesized compounds were produced in good yield and characterized by I.R, 1H-NMR, and LC-MASS and also evaluated for their anticonvulsant activity by maximal electroshock (MES) model in rats. These findings are helpful to design better quinazolinone derivatives as novel antiepileptic drugs.
Formulation and Evaluation of Nanosuspension Delivery System for Simvastatin
Authors: Shid L. Rupali , Dhole Shashikant N. , Kulkarni Nilesh , Shid L. Santosh L. 
Published: August 2020

Poor water solubility and slow dissolution rate are issues polydispersity index. The obtained results showed that for the majority of upcoming and existing biologically active
particlesize (nm) and rate of dissolution has been improved compounds. Simvastatin is poorly water-soluble drug and when nanosuspension prepared with the higher its bioavailability is very low from its crystalline form. The concentration of PVPK-30 with the higher concentration of purpose of the present investigation was to increase the
PVP K-30 and Poloxamer-188 and lower concentration of solubility and dissolution rate of simvastatin by the SLS. The partical size and zeta potential of optimized preparation of nanosuspension by Emulsification Solvent formulation was found to be 258.3 nm and 23.43. The rate Diffusion Method at laboratory scale. Prepared nanosus- of dissolution of the optimized nanosuspension was pension was evaluated for its particle size and in vitro enhanced (90.02% in 60 min), relative to plain simvastatin dissolution study and characterized by zeta potential, (21% in 60 min), mainly due to the formation of nanosized differential scanning calorimetry (DSC) and X-Ray particles. These results indicate the suitability of 23 factorial diffractometry (XRD), motic digital microscopy, entrapment design for preparation of simvastatin loaded efficiency, total drug content, saturated solubility study and nanosuspension significantly improved in vitro dissolution in vivo study. A 23 factorial design was employed to study rate, and thus possibly enhance fast onset of therapeutic the effect of independent variables, amount of SLS (X1), drug effect. In vivo study shows increase in bioavailability in amount of PVPK-30 (X2) and Poloxamer-188 (X3) and nanosuspension formulation than the plain simvastatin dependent variables are total drug content and drug.
Biosynthesis of Silver Nanoparticles from Aqueous Leaf Extract of Synedrella nodiflora under Sunlight Irradiation and Screening of its Antibacterial Activity
Authors: Jash Shyamal K. , Gorai Dilip , Gangopadhyay Arindam 
Published: August 2020

The field of nanotechnology and nanoscience is the most currently an area of intense scientific interest for researchers in modern materials science. However there are many chemical as well as physical methods, green synthesis of nanomaterials is the most emerging method of synthesis. We report the synthesis of antibacterial silver nanoparticles (AgNPs) using aqueous leaf extract of medicinal herb Synedrella nodiflora (L.) Gaertn (Family: Asteraceae) at direct sunlight and monitored by UV-Vis spectroscopy. Both leaf extract and resulting AgNPs is subjected to antibacterial study against five pathogenic bacterial strains such as Bacillus megaterium, Staphylococcus aureus, Listeria monocytogenes, Pseudomonas aeruginosa and Salmonella typhimurium. AgNPs exhibited higher antibacterial efficacy than leaf extract and found to be more effective against B. megaterium and S. aureus.
A Balance Scorecard of the European Paediatric Regulation
Authors: George Bobby , Tiwari Jyoti 
Published: August 2020

Due to the high complexity of testing drugs in children, the of discussion and debate. Some industry experts are of the cost of testing a drug in minors may well exceed the view that the regulation has been a trigger in the area of potential return on investment and, therefore, render it research on pediatric medications while others feel that it is economically unattractive to label drugs for pediatric use. a burden that has been unnecessarily imposed on the As a result, there has been a dearth of drugs for use in manufacturers, hampering the developmental process of children, and in many instances, pediatricians initially had medicines for adults. Through this article, the authors no therapeutic options apart from using drugs off-license havetried to summarize regulation’s main proposals, throw or off-label in European Union (EU). With the advent of light on the respective issues faced by industry, the “Pediatric Regulation” of EU, things have changed. benefits reaped by the pediatric population and pharma- However, over the years, this regulationhas become a topic
Pharmaceutical industry as a whole since its implementation.
Synthesis, Characterization and Evaluation of Azetidinylquinolines and Thiazolidinylquinolines as Antibacterial Agents
Authors: Sharma Shalabh , Saxena Kuldeep K 
Published: August 2020

Several molecules were synthesized like 8-ethoxy-4-methyl-2-amino-(3’-chloro-2’-oxo-4’-substitutedaryl-1’-azeti-dinyl)-quinolines 8-12 and 8-ethoxy-4-methyl-2-amino-(2’-substitutedaryl-4’-oxo-1’,3’-thiazolidin-3’-yl)quinolines 13-17 from 8-ethoxy-4-methyl-2-(substitutedarylidenylimino amino)-quinolines 3-7, and screened to evaluate their antibacterial activity against numerous strains of bacteria in vitro. The structures of new compounds were established on the basis of their elemental analysis, IR, 1H-NMR and mass spectral data. The results showed that three compounds 10, 11 and 16 were found to exhibit promising antibacterial activity as compared to the standard drug amphicillin.
Prevalence and Predictors of Pediatric Depression in the United States
Authors: Aparasu Rajender R , Nagar Saurabh , Patel Ayush , Bali Vishal 
Published: August 2020

Depression is common in children and adolescents. However, little is known about the predictors of depression in children and adolescents. This study examined the prevalence and predictors of pediatric depression in the United States. A cross sectional study was conducted using 2005-2006 Medical Expenditure Panel Survey (MEPS). The study population included 5-17 years old children and adolescents with diagnosis depression, ascertained using the International Classification of Diseases, Ninth Revision, Clinical Modification (ICD-9-CM) codes. Independent variables were categorized as personal, family and environmental characteristics. Descriptive statistics were computed using t-test for the continuous variables and chi-square test for the categorical variables. Multiple logistic regression analysis was used to examine personal, family, and environmental factors associated with pediatric depression. Our results indicate that around 1.25 million (2.33%) children and adolescents had a diagnosis of depression in 2005-2006. Prevalence was significantly higher among adolescents aged 12-17 years (3.86%), children with single parent (4.05%) and children of parents suffering from psychiatric illness (5.24%). The multiple logistic regression analysis found that the likelihood of depression was higher for adolescents aged 12-17 years (Odds Ratio, OR: 2.40, 95% Confidence Interval (CI): 1.60-3.59), those with a diagnosis of attention deficit hyperactivity disorder (OR: 5.64, 95% CI: 3.52-9.04), and anxiety disorder (OR: 4.96, 95% CI: 2.65-9.26). Among family characteristics, odds of depression were higher for a child having either or both parents with psychiatric disorders (OR: 2.39, 95% CI: 1.60-3.59), those belonging to a single-parent household (OR: 2.63, 95% CI: 1.68-4.12), and to a family of eight or more members (OR: 2.92, 95% CI: 1.60-3.59). In conclusions, both personal and family level factors are associated with depression in children and adolescents. Understanding of these risk factors can help in timely diagnosis and management of depression in pediatric population
A GC–ECD Method for Analysis of Prasugrel in Bulk and Pharmaceutical Dosage Forms
Authors: Housheh Samer , Trefi Saleh , Mohammad Haroun , M Fawaz Chehna 
Published: August 2020

Prasugrel is a novel ADP receptor inhibitor with antithrombotic properties. This paper proposes a new method for quantitative analysis of prasugrel in bulk and pharmaceutical dosage forms. The method used gas chromatography with electron-capture detection (GC–ECD). Chromatographic analysis was performed on an RTX-5 capillary column. Under the optimum conditions, good retention and peak response were achieved for prasugrel. The analytical method was fully validated by assessment of LOD and LOQ (0.24 µg/mL and 0.73 µg/mL), linearity (R = 0.997) over the range 0.5-2.5 µg/mL and extraction recovery (>98.7 %, with RSD below 1.0, for prasugrel spiked at 0.5, 1, 1.25, 2 and 2.5 µg/mL), the precision was 0.825% and the intermediate precision was 1.134%. The method required no clean-up of prasugrel before and after injection. It has been successfully used to determine prasugrel content in different commercial pharmaceutical dosage forms.
Synthesis and Antibacterial Activity of Azetidinonyl Norfloxacin Congeners
Authors: Sharma Shalabh , Saxena Kuldeep Kumar 
Published: August 2020

Some novel Schiff bases and azetidinone congeners of norfloxacin have been synthesized and screened for antibacterial activity. The structures of compounds 1-ethyl-6-fluoro-7-piperazinyl-4-oxo-3-(substitutedarylidinylcarboxy- hydrazido)quinolines (2-6) and 1-ethyl-6-fluoro-7-pipera-zinyl-4-oxo-3-(3′-choloro-2′-oxo-4′-substitutedaryl-3′-aze-tidinyl)-aminocarboxy quinolines (7-11) were established by spectral and elemental analysis. The compounds 2-11 were evaluated in vitro against various strains of bacteria: E. coli ATCC 25922, B. subtilis ATCC 1633 and S. aureus ATCC 25923 to determine their antibacterial activity and feasible structure-activity relationships. The results of the study were compared with reference drug. Compound 8: 1-ethyl-6-fluoro-7-piperazinyl-4-oxo-3-(3′-choloro-2′-oxo-4′-(4′′-methoxyphenyl)-3′-azetidinyl)-aminocarboxyquinoline has displayed more potent antibacterial activity as compared to standard drug, chloramphenicol.
Formulation Development and Characterization on the Impact of Superdisintegrants on Oral Dispersible Tablets of Didanosine
Authors: Swain Suryakanta , Eswara Bhanoji Rao Muddana , Patra Chinam Niranjan , Manohar Babu Sitty 
Published: August 2020

The present study was undertaken to develop and evaluate an oro-dispersible tablet of didanosine by direct compression using cross carmellose sodium, crosspovidone and sodium starch glycolate (5-20%) as a superdisintegrants, Avicel 102 (15-30%) was used as diluents along with directly compressible mannitol (20%) to enhance mouth feel, faster disintegration and dissolution rate of the drug. Absorption of the drug can be impacted by oral fast dissolving dosage form; this may have implication for medications to treat human immunodeficiency virus (HIV) infection and those having difficulty in swallowing tablets or capsules resulting in improved patient compliance. The prepared tablets were evaluated for impact of superdisintegrants on the disintegration behavior of the tablet in the oral cavity and also evaluated for post compression parameters and in vitro drug release characteristics. The tablets demonstrated a hardness of 3 to 6 kg/cm2, friability of 0.48 to 1 %, disintegration time of 5 to 14 sec and drug content was found to be 98 to 100 %. Based on evaluation parameters the formulation (F6) containing 20 % of crosspovidone and 15% of MCC Avicel 102 showed promising performance against all other formulations with hardness of 5 ± 0.13 kg/cm2 and faster disintegration within 5 s and better dissolution rate. An appropriate combination of excipients made it possible to obtain orally disintegrating immediate release tablets of didanosine using simple and conventional technique. The formulations were subjected to stability studies as per ICH guidelines and were found to be stable after a 3 months study.
Evaluation of Antibacterial Activity of Acer syriacum by Bioautography Method
Authors: Asfour B. Al , Al-kayali R. , Kitaz A. 
Published: August 2020

antibacterial activity of leaves, fruits and bark of acer syriacum was evaluated against both negative and positive gram bacterial strains. The powder of above parts were sequentially extracted with aqueous methanol 80%, acetone and petroleumether by maceration. The in vitro antibacterial activity of A. syriacum extracts (in concentration of 200 mg/mL) was performed by agar well diffusion method. Among the tested extracts, leaves methanolic extract has shown the highest growth inhibition. Further, the extract was fractionated, separated by thin layer chromatography (TLC) and submitted to bioautography. the results indicate that the ethyl acetate extract had the most efficient antibacterial compounds that displayed inhibition zones (25 mm) against Staphylococcus aureus ATCC25923 and (28mm) against Klebsiella pneumonia ATCC700603. the clear zones were located at RF= 0.15.
Development and Evaluation of Sustained Release Matrix Tablets of Tramadol Hydrochloride
Authors: Basarkar Ganesh , Suryawanshi Vijay , Hire Dinesh 
Published: August 2020

The objective of the present study was to control the release of freely water soluble Tramadol hydrochloride over a prolonged period of time by embedding the drug into novel wax matrix system. The matrix granules were prepared by melt granulation technique. The need for the administration two to four times a day when larger dose are required can decrease patient compliance. Sustained release formulation that would maintain plasma levels for 24 hrs for once daily dosing of Tramadol hydrochloride was prepared. The compatibility of the drug and wax examined using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectrophotometer (FTIR). The effect of wax concentration (5 to 35%) and channeling agents (Avicel PH-101 and Di-calcium phosphate) on the in vitro drug release at 24 hrs. was studied. Results of DSC confirmed drug-wax compatibility. Increasing the wax concentration resulted in a significant retardation of drug release. The drug release study revealed that the optimized formulation (F6) 30% novel wax sustained drug release for 24hrs. At the same wax concentration, drug release from tablets decreased with Di-calcium phosphate and increased with Avicel PH 101. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. A hydrophobic matrix system is thus useful technique for prolonging the drug release of freely water soluble drugs such as Tramadol hydrochloride