bluuebunny/crossref_metadata_2025 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.
Antioxidant and Anti-inflammatory Activity of Eurycoma Longifolia Jack, A Traditional Medicinal Plant in Malaysia
Authors: Varghese Christapher Parayil , C Ambrose , Jin S C , Lim Y J , Keisaban T
Published: August 2020

Tongkat Ali (Eurycoma longifolia Jack, family, Simaroubaceae) is traditionally used in Malaysia as health supplement for hypertension, diarrhea, aches, persistent fever, malaria, sexual insufficiency, dysentery, and glandular swelling. In this study, hydroalcoholic extract of Eurycoma longifolia Jack was studied for its antioxidant and in-vitro anti-inflammatory properties. The antioxidant activity (free radical scavenging) was evaluated to determine the total antioxidant capacity of extract Eurycoma longifolia Jack. The DPPH assay showed significant antioxidant activity in all concentrations (10, 25, 50,100 and 250 µg/ml). The antioxidant property of the extract was compared with the values of ascorbic acid, a standard antioxidant. Human RBC (HRBC) stbilization method was utilized to evaluate the in-vitro anti-inflammatory activity of the extract. The extract showed a significant anti-inflammtory activity in all the concentrations tested (25, 50,100, 250, 500 and 1000 µg/ml) and the activity was increased in a concentration dependent manner.
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 of Irbesartan by Microcrystal Technology for Enhancing the Solubility and Dissolution Properties
Authors: Jain Stuti A. , Kurup Nalini S
Published: August 2020

The aim of this study was to develop the formulation of irbesartan by microcrystal technology to enhance the solubility and dissolution property of the drug. The area of interest in the study carried out is Class II drugs cited in the Biopharmaceutical Classification System. Microcrystal technology is a new carrier-free colloidal drug delivery system with reduced drug particle size and is considered a viable strategy in drug delivery to develop formulations of poorly soluble drugs. In the present study, an attempt was made to enhance the solubility of the drug irbesartan compared to its pure form by microcrystal technology. Drug microcrystals were prepared by the anti-solvent precipitation process. The specified amount of drug was dissolved in methanol and PVP K30 was dissolved in water. The two phases were mixed instantaneously, wherein the drug solution was kept on continuous stirring and the aqueous phase was added to this continuous phase. The particle size of the drug was not reduced, but enhancement in solubility and dissolution properties of the drug were still observed. This could be due to the wettability property of PVP K30. The FT-IR spectra and DSC thermograms confirmed no interference of drug and the stabilizer. XRD studies confirmed the formation of crystals of the drug irbesartan. Thus, it could be concluded that microcrystal technology is a promising approach for solubility enhancement of irbesartan.
Bilayer Floating Tablets for Gastroretentive Drug Delivery System
Authors: Palla Sai Sowjanya , Kotha Rajkumar , Paladugu Anusha , Reddy E. Rajesh Kumar , Adavi Suryasri Lavanya , Reddy K. Ramamohan
Published: August 2020

Oral delivery of the drug is by far the most preferable route of drug delivery due to the ease of administration, patient compliance and flexibility in the formulations but has a drawback of non-site specificity and short gastric resident time. In recent years, scientific and technological advancements have been made in the development of novel drug delivery systems by overcoming physiological troubles such as short gastric residence times and unpredictable gastric emptying times. Among Several approaches of floating systems, Bilayer floating technology is considered as promising approach. It combines the principle of bilayer technology and floating mechanism. The combined principle of bilayer floating tablet helps to release initial dose from the immediate release layer to reach the plasma concentration and then the floating layer absorbs gastric fluid forming an impermeable colloidal gel barrier on its surface, maintains a bulk density less than unity and thereby remains buoyant in stomach providing steady state concentration of drug in system. This review focuses on bilayer floating tablet technology a new era of gastro retentive drug delivery system, its advantages over conventional tablets and it also summarizes the bilayer tablet presses used in the industry, formulation design and evaluation parameters of bilayer floating tablets.
Formulation and In vitro Characterization of Floating Gel Beads of Metformin Hydrochloride
Authors: Mohd Yasir , Bhattacharyya A , Bajpai M , Yasir M , Asif M
Published: August 2020

A floating type dosage form, gel beads of metformin hydrochloride was prepared by emulsification gelation technique. The gel bead was formed by mixing the polymer in water, oil phase and it was extruded in the calcium chloride solution as curing agent. The formulation parameters optimized were polymer ratio, concentration of oil, curing time on drug content, floating lag time, morphology, swelling of beads and release kinetics.The scanning electron photomicrographs revealed morphology of beads. The size of beads was measured. Entrapment efficiency of drug loaded beads was found to be over 90%. In vitro release of metformin hydrochloride from alginate–pectin beads into simulated gastric fluid at 37 ºC showed no significant burst effect. The cumulative release reached above 74.71 ± 4.15% in about 12h. The use of sodium alginate and combinations of sodium alginate with pectin were used to study the effect on the sustained release of the drug from the formed beads. It was found that sodium alginate was not sufficient to sustain the drug release at gastric pH (fed condition). Appropriate combination of alginate and pectin could provide the sustained release of drug. Floating gel beads formulation provides an alternative delivery for metformin in diabetes treatment.
Optimization of RP-HPLC Assay for Pharmaceutical Analysis of Clopidogrel
Authors: Housheh Samer , Ali Daoud , Trefi Saleh , Mohammad Haroun , Chehna M. Fawaz
Published: August 2020

An accurate, sensitive, precise and stability-indicating reversed phase high performance liquid chromatographic (RP-HPLC) method for the analysis of clopidogrel bisulfate was developed and validated. The chromatographic conditions comprised of a reversible phase C18 column (250 × 4.6 mm, 5 μm) with a mobile phase consisting of a mixture of 50 mM potassium di-hydrogen phosphate and acetonitrile in the ratio of 75:25 at pH 3.0 adjusted with phosphoric acid. The flow rate was 1ml/min, the detection was carried out at 247 nm and the retention time of clopidogrel was 6.5 min. Clopidogrel was subjected to acid and alkali hydrolysis, oxidation and photodegradation. The method was validated for accuracy, precision and robustness. The results indicate that the drugs are susceptible to degradation in different conditions. All the peaks of degraded products were resolved from the active pharmaceutical ingredient with significant different retention times. As the method could effectively separate the drug from its degradation products, it could be employed as a stability-indicating method.
Ocular Drug Delivery Systems for Treatment of Glaucoma
Authors: Dubey Akhilesh , Prabhakara Prabhu
Published: August 2020

Glaucoma is a common eye disease that can cause irreversible blindness if left undiagnosed and untreated. Glaucoma is a prevalent neurodegenerative disorder of the eye. Glaucoma can be roughly divided into two main categories "open angle" and "closed angle" (or "angle closure") glaucoma. Every available treatment to prevent progressive glaucoma involves a certain amount of risk and financial expense. Conventional first-line treatment of glaucoma usually begins with the use of a topical selective or nonselective β-blockers or topical prostaglandin analogs. Second-line drugs of choice include α-agonists and topical carbonic anhydrase inhibitors. Parasympatho-mimetic agents, most commonly pilocarpine, are considered third-line treatment options. For patients who do not respond to antiglaucoma medications, laser trabeculoplasty and incisional surgery are further methods that can be used to lower intraocular pressure. Ocular drug delivery is hampered by the barriers protecting the eye. The bioavailability of the active drug substance is often the major hurdle to overcome. Conventional ocular dosage form, including eye drops, is no longer sufficient to combat ocular diseases. This article reviews the better understanding about glaucoma disease like prevention and diagnosis and explores various approaches like niosomes, liposomes, hydrogels, nanoparticles, nanosuspensions, microparticles, microemulsions, prodrugs and ocular inserts to improve the ocular bioavailability of drug and provide continuous and controlled release of the drug to the anterior and posterior chamber of the eye. In near future, a great deal of attention will be paid to develop a suitable and effective treatment for the vision threatening disorders like glaucoma.
Randomized Placebo-Controlled Clinical Study on the Role of Zinc in Low Birth Weight Neonates
Authors: Kumar Ch. Laxman , Chandar D. Sai , D Narendar , V Shireesha
Published: August 2020

Low birth weight (LBW) is one of the important causes of neonatal mortality and morbidity in developing countries. It is hypothesized that LBW neonates are zinc deficient and that might adversely affect postnatal growth. The objective of the investigation was to compare the effect of oral zinc supplementation on growth of low birth weight neonates by randomized controlled trail. 100 LBW neonates between 1501-2499 gm were randomized into zinc and placebo groups. We supplemented zinc 10 mg/day to zinc group and multivitamin drops to placebo group for 28 days. Measure the weight and length according to study schedule. Primary outcome was increment in weight and length and data were analyzed by SPSS. The mean birth weight was 1850 ± 302 gm and 1813 ± 271 gm for zinc and placebo groups, respectively. After 28 days 2595 ± 503 gm with mean weight gain of 26 ± 11 gm/day in zinc group and 2322 ± 472 gm with mean weight gain of 18 ± 9.4 gm/day in placebo group, which was statistically significant (p < 0.001). There was significant length gain (p < 0.001) in zinc group compare to placebo group. Zinc group experienced remarkably less problems like sepsis, duration of hospital stay and jaundice. There were no adverse effects noted in zinc group. Zinc supplementation for LBW neonates was found effective to enhance growth in neonatal period.
Patterns and Predictors of Antipsychotic usage among U.S. Adults: A National Co-Morbidity Survey Replication Study
Authors: Aparasu Rajender R , Nagar Saurabh , Mhatre Shivani K , Hatfield Mark D
Published: August 2020

The primary objective was to study patterns of antipsychotic usage among adults with mental health disorders in the U.S. using a national survey. The secondary objective was to examine patient and provider factors associated with antipsychotic usage. Data from the National Co-Morbidity Survey Replication study (NCS-R) of 2001-2003 was used to examine the prevalence of antipsychotic use among adults 18 years or older. Patient-reported adherence and effectiveness were reported. Multiple logistic regression analysis was used to determine the statistically significant determinants of antipsychotic use. Antipsychotic medications were used by 99 of 9282 (1.06%) NCS-R participants in the previous year. Among antipsychotic users, 42 (42.4%) used typical agents and 57 (57.6%) used atypical agents. Males over 65 (compared to age 18-45), non-white race, prescription by a psychiatrist, and presence of mood disorders were statistically significant predictors of increased antipsychotic use among patients with mental disorders, in the adjusted model. Mean adherence among typical users (17.78 ± 1.53 days) was less than atypical users (24.04 ± 0.82 days). No statistically significant difference in perceived effectiveness was found. In conclusion, these analysis shows that approximately 1% of Americans used antipsychotics within the past year, mostly using atypical over typical agents. Male, over 65, non-white race, prescription by a psychiatrist, and presence of mood disorders were the significant predictors of antipsychotic use.
Development and Evaluation of Dapsone Loaded Topical Liposomes
Authors: Kumbhar M.S. , Singh M.C
Published: August 2020

Topical liposomal drug delivery is becoming promising system with several advantages like skin deposition, controlled release, targeted action and reduced drug quantity etc. Topical treatments are used for various diseases and disorders. Acne vulgaris is a worldwide skin disease. For acne treatments oral, injectable routes are used but topical route is the better route for site delivery. Dapsone, as antibacterial and anti-inflammatory drug has been recommended in topical acne treatment. Multilamellar vesicles (MLV) of dapsone were prepared using conventional thin film hydration method. Optimization techniques were used to determine, formulation with high drug entrapment efficiency and optimum vesicle size. Soya lecithin and cholesterol were used as independent variables. The prepared liposomes were characterized for size, shape, entrapment efficiency, zeta potential, in-vitro drug release (by Franz diffusion cell) and skin deposition. Maximum entrapment was found to be 33.44%. In skin permeation study, liposomal gels resulted in significantly slower drug release than equivalent plain gels. Liposomal gels were found to have 2-3 fold increase in the skin deposition than plain gel, indicating liposome forms depots in skin layers and thus providing a better option to deal with skin-cited acne vulgaris. Amongst different storage conditions (kept for 2 months), the liposomes stored at 2 to 8 °C were found to be most stable, as compare to room temperature and 45 °C.
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.
Nanoparticles and their Therapeutic Applications in Pharmacy
Authors: Gadad A.P. , S M Vijay Kumar , Dandagi P M , Bolmol U B , Pallavi N. Pavani
Published: August 2020

Nanotechnology is providing solutions several pharma-ceutical drug delivery issues. With the emergence of nanotechnology, researchers become more interested in studying the unique properties of nanoscale materials. Nanoparticles are attractive tool in pharmaceutical and biomedical ﬁelds. These particulate systems have been used as a physical approach to alter and improve the pharmacokinetic and pharmacodynamic properties of various types of drug/proteins. Nanoparticles have been used in-vivo to protect the drug/proteins molecules in the systemic circulation, targeting of the drug to the chosen sites and to deliver the drug at a controlled and sustained rate to the site of action. Various types polymers have been used in the formulation of nanoparticles for drugs, proteins, and hormone delivery are discussed in this article. It also describes various methods of preparation, advantages, disadvantages and their applications in biomedical fields. It provides an overview of characterization of nanoparticles, storage, and commercially available nanoformulations.
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
Effect of Compression Force and Concentration of Superdisintigrant on Directly Compressed Tablets of Metformin HCl
Authors: Swain Suryakanta , Patra Chinam Niranjan , Panigrahi Kahnu Charan , Rao Muddana Eswara Bhanoji , Patro Rashmita
Published: August 2020

The present research work was to evaluate the effect of compression force and concentration of superdisintigrant on tableting properties of metformin HCl. Initially powder mixtures of drug, croscarmellose sodium (0.62% to 10% w/w) and microcrystalline cellulose PH-200 sufficient quantity were prepared and evaluate their pre-compression parameters of different formulation batches such as angle of repose, bulk density, tapped density, Hausner’s ratio and compressibility index. The prepared powder mixtures of different batches were compressed into tablet using hydraulic pellet press machine at two optimized compression forces (77 MPa and 154 MPa). The post compression parameters such as thickness, diameter, weight variation, hardness, friability, drug content, disintegration time and in-vitro drug release study of the prepared tablets were evaluated. FT-IR and DSC studies showed that no incompatibility of the selected drug with the selected excipients. At selected compression force (77 MPa) and increased concentration of superdisintigration (0.62% to 10% w/w) of formulations F1 to F5 indicated that, disintegration time were periodically decreased up to F3 (1.25% w/w croscarmellose sodium). When the concen-tration of superdisintigrant increased up to 10% showed that disintegration time were periodically increased. Similarly, at compression force 154 MPa there is increased in tablet hardness but this effect was less significant when the superdisintegrant concentration more than 1.25% w/w. The hardness and drug content of all the formulations were found to be 3.59 ± 0.23 to 4.85 ± 0.01 kg/cm2 and 97.89 ± 0.10% to 99.42 ± 0.03% respectively. The in-vitro drug release data suggested that drug release of all the formulations followed Higuchi’s kinetic (R> = 0.998). The release rate exponent values (n) suggested the mechanism of drug release followed Quasi-Fickian diffusion mechanism at compression force 77 MPa and anomalous diffusion mechanism at compression force 154 MPa, respectively.
Formulation and Evaluation of Self-Nanoemulsifying Drug Delivery System of Naproxen
Authors: D Saritha , Bose Penjuri Subhash Chandra , Ravoru Nagaraju
Published: August 2020

Self-emulsifying drug delivery systems (SEDDS) possess unparalleled potential in improving oral bioavailability of poorly water-soluble drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro or nanoemulsions containing the solubilized drug. The objective of the present work was to formulate a self nanoemulsifying drug delivery system (SNEDDS) for naproxen. Naproxen SNEDDS were formulated using Labrafac PG (Oil), Span 80 (Surfactant) and propylene glycol (Co surfactant). The developed SNEDDS were evaluated for turbidimetry, droplet size analysis, zeta potential, refractive index, viscosity, drug content and in vitro diffusion profiles. All formulations of naproxen SNEDDS showed globule size in nanometric range, good stability with no phase separation and rapidly formed clear emulsion. All formulations showed more than 95% of drug release at the end of 60 min. The SEDDS showed improved dissolution rate compared to pure naproxen. Anti-inflammatory studies were conducted in Wistar strain male albino rats and ibuprofen SNEDDS showed more significant activity than the pure drug. The study illustrated the potential of naproxen SNEDDS for oral administration and its biopharmaceutical performance.
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.
Quantification of Aceclofenac and Pregabalin in Pharmaceutical Formulations using Nucleophilic Aromatic Substitution Reactions
Authors: Gelani Hitendrakumar D , Chauhan Payal P , Shah Samir K.
Published: August 2020

Aceclofenac and Pregabalin in combination have significant reduction in pain as compared to individual drug in chronic low back pain. Literature reveals that all the reported spectrophotometric methods are either need tedious extraction procedures do not offer high sensitivity, uses non specific reagent and/or recommend the measurement of absorbance in the near UV region where interference most probably occurs that do not offer suitable linearity range. A novel, accurate, precise and extraction free UV spectrophotometric method has been developed for simultaneous estimation of Aceclofenac and Pregabalin in combined dosage form. The method employed was Dual wavelength method. The method is based on the reaction of Pregabalin with 1,2-naphthaquinone-4-sulphonate sodium, yielding an orange colored product. The different experimental parameters affecting the development and stability of the reaction product were carefully studied and optimized. Method involves measurement of Aceclofenac at 268.5 and 280.0 nm and measurement of Pregabalin at 324.0 and 339.5 nm. Rectilinear relationship with good regression coefficient 0.999 and 0.999 were found over the concentration ranges of 5-25 μg/ml and 3.75-18.75 μg/ml for Aceclofenac and Pregabalin, respectively with detection limit 0.62 and 0.50 μg/ml and Quantitation limit 1.87 and 1.52 μg/ml. The mean percentage recoveries were ranged 99.60 – 99.83 and 98.85 – 100.05 for Aceclofenac and Pregabalin, respectively. The developed methods were successfully applied to the analysis of the drug in its commercial tablet.
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 of Modified Release Atorvastatin Nanoparticles by Emulsion Interfacial Reaction Method
Authors: Sekar Sudhakar , May Shee Sim
Published: August 2020

The aim of the study is to formulate a modified release chitosan nanoparticles for the oral delivery of atorvastatin and to study the in vitro release of atorvastatin from chitosan nanoparticles. Atorvastatin-loaded chitosan nanoparticles were prepared with different concentration of cross-linking agent (glutaraldehyde) by emulsion interfacial reaction method. The formed nanoparticles were characterized in terms of size and morphological characteristics by scanning electron microscopy (SEM) and transmission electron microscope (TEM). Spherical and regular nanoparticles with the size range of 100-250nm were formed. Atorvastatin encapsulation efficiency of nanoparticles was found to be highest in ANP3, followed by ANP2 and ANP1. The in vitro release of atorvastatin was studied by membrane diffusion technique. The resulted cumulative percentage of drug released for ANP1, ANP2 and ANP3 were 60.08%, 34.81% and 20.39% respectively. Through this study, the nanoparticles preparation technique has shown to be a promising approach for enhancing the dissolution of hydrophobic drugs like atorvastatin calcium. The application of this novel delivery system offers good therapeutic potential in the management of hypercholesterolemia and dyslipidemia.
Preparation, Characterization and in vivo Evaluation of Felodipine Solid-Lipid Nanoparticles for Improved Oral Bioavailability
Authors: V Kishan , Gondrala Usha Kiranmai , Dudhipala Narendar
Published: August 2020

Felodipine is an antihypertensive drug with poor oral bioavailability due to the first pass metabolism. For improving the oral bioavailability, felodipine loaded solid lipid nanoparticles (SLNs) were developed using trimyristin, tripalmitin and glyceryl monostearate. Poloxamer 188 was used as surfactant. Lipid excipient compatibilities were confirmed by differential scanning calorimetry. SLN dispersions were prepared by hot homogenization of molten lipids and aqueous phase followed by ultrasonication at a temperature, above the melting point. SLNs were characterized for particle size, zeta potential, drug content, entrapment efficiency and crystallinity of lipid and drug. In vitro release studies were performed in 0.1N HCl and phosphate buffer of pH 6.8 using dialysis method. Pharmacokinetics of felodipine-SLNs after oral admini-stration in male Wistar rats was studied. The bioavailability of felodipine was increased by 1.75 fold when compared to that of a felodipine suspension.
Formulation and Evaluation of Buccoadhesive Tablets of Losartan Potassium
Authors: Singh Sudarshan , Shyale S S , Jadhav A
Published: August 2020

The present investigation is concerned with formulation and evaluation of buccoadhesive tablets containing antihypertensive drug, Losartan Potassium to avoid the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. The tablets were prepared by wet granulation method. Nine formulations were developed with varying concentrations of polymers like hydroxypropylmethyl cellulose K100 and Guar gum. The tablets were tested for hardness, friability, weight variation, content uniformity, surface pH, swelling index, ex vivo mucoadhesive strength, in vitro drug dissolution study and ex-vivo permeation study. FTIR and DSC studies showed no evidence on interactions between drug and excipients. The in vitro release of Losartan Potassium was performed under sink conditions. The mucoadhesive strength of formulation F9 was found to be 0.14307 N. The swelling index of formulation F9 was found to be 87%. The formulation F9, containing 25 mg of losartan potassium exhibited 6 h sustained drug release of 96% with desired therapeutic concentration. The in vitro release kinetics studies revealed that all formulations fits well with zero order kinetics followed by Korsemeyer-Peppas model and the mechanism of drug release is Non-Fickian diffusion. Based on the results of ex vivo mucoadhesive strength and swelling index studies formulation F9 was selected as optimized formulation and subjected for stability study. Short-term stability studies on the promising formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics.
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.
Antioxidant Activity and Phenolic Content of Eight Mediterranean Fruit Juices
Authors: Al Asaad Nour , Al Diab Dima
Published: August 2020

Antioxidants play an important role in health and disease by reducing oxidative damage. In this study, eight local Mediterranean fruit juices (orange, grapefruit, blackberry, black mulberry, black sweet cherry, strawberry, pomegranate and red grape) were assessed for their total phenolic content and antioxidant activity. These fruits are known for their health effects and antioxidant properties which can be attributed to their phenolic compounds. Total phenolic content was determined according to Folin-Ciocalteu method. The highest in content was black mulberry juice with amounts from 4.24 gGAE/Ljuice to 11.03 gGAE/Ljuice, while the lowest was red grape juice with amounts from 0.35 gGAE/Ljuice to 0.64 gGAE/Ljuice. Antioxidant activity was subsequently determined using Ferric Reducing Antioxidant Power (FRAP) assay and reducing power assay. Black mulberry juice had the highest antioxidant activity, while red grape juice had the lowest antioxidant activity. The study indicates that black mulberry juice is the richest source of phenolic compounds and provides the highest antioxidant potential compared with other fruit juices in this study