bluuebunny/crossref_metadata_2025_split huggingface dataset:
Effect of Permeation Enhancers on Transdermal Delivery of Venlafaxine Hydrochloride from Carbopol Gel
Authors: Ain Shabnam , Dahiya J , K Babita , Gupta V 
Published: August 2020

In this study, we investigated the effect of different permeation enhancers at different concentrations viz. oleic acid, olive oil and castor oil from transdermal gel for transdermal delivery of venlafaxine, a newer antidepressant. It is a first line drug in the treatment of depression and inhibits brain serotonin and norepinephrine neuronal reuptake. It is also used in the treatment of anxiety disorders. Transdermal delivery of venlafaxine hydrochloride may result in enhanced patient compliance by reducing the incidence of the undesirable GI problems associated with its multiple oral dosing. The differential scanning colorimetry study was used to investigate the drug-polymer interaction. The prepared gels were evaluated for several physico-chemical parameters such as drug content, spreadability, pH, viscosity and physical appearance to justify their suitability for topical use. The in vitro permeation studies were performed by using Franz diffusion cell and rat skin as a semi permeable membrane. This indicate that penetration enhancers in 5% v/w concentration enhance the permeation of venlafaxine hydrochloride but oleic acid show maximum permeation rate was 197 µg/cm2/hr as compared to olive oil (154.69µg/cm2/hr) and castor oil (175.8µg/cm2/hr). It is further optimized by increasing the concentration of permeation enhancer at levels as high as 10% v/w and 15% v/w. The result indicates that increase in the concentration of enhancer enhances the percutaneous permeation of venlafaxine. Oleic acid was found to be superior to olive oil and castor oil implying the ability of oleic acid to increase the drug diffusion by SC lipid disruption and increase partition coefficient into SC. The permeation rate of venlafaxine hydrochloride with 15% v/w oleic acid was higher (rat abdominal skin flux = 8.507 µg/cm2/h) than with 15% v/w olive oil and castor oil. These studies show promising potential of transdermal patches of venlafaxine.
Development of Solid-Self Micron Emulsifying Drug Delivery Systems
Authors: Sudheer Preethi , Y Koushik , P Satish , M S Uma Shankar , Thakur R S 
Published: August 2020

As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new pharmacologically active lipophilic compounds that are poorly water soluble and solubility is one of the most important parameter to achieve desired concentration of drug in systemic circulation for therapeutic response. It is a great challenge for pharmaceutical scientist to convert those molecules into orally administered formulation with sufficient bioavailability. Among the several approaches to improve oral bioavailability of these molecules, Self-micron emulsifying drug delivery system (SMEDDS) is one of the approaches usually used to improve the bioavailability of hydrophobic drugs. However, conventional SMEDDS are mostly prepared in a liquid form, which can have several disadvantages. Accordingly, solid SMEDDS (S-SMEDDS) prepared by solidification of liquid/semisolid self-micron emulsifying (SME) ingredients into powders have gained popularity. This article provides an overview of the recent advancements in S-SMEDDS such as methodology, techniques and future research directions.
Stability Studies of Cefepime Hydrochloride by Stability Indicating RP-HPLC Method
Authors: Raj Behin Sundara , Punitha I S R , Krishnan S 
Published: August 2020

Drug stability and compatibility are critical issues controlling accurate and appropriate delivery of drug therapy to patients. Stability is very important for antibacterial agents especially those given by intravenous route as they reach systemic circulation directly, and the clinical outcome and safety are directly correlated to drug levels in blood. The physical and chemical stability of Cefepime hydrochloride, a fourth generation cephalosporin, was determined at three different temperatures (5 °C/ 60 %RH, 25 °C/60 %RH & 45 °C/75% RH) and quantified by using a stability indicating RP-HPLC method. Decrease in drug concentration by more than 10% from initial concentration (0 time) was considered unstable (chemical instability). Change in pH by more than 1 was considered unstable (Physical instability). The drug solutions were clear and light yellow initially with intensity increasing over time, eventually becoming dark yellow for cefepime. HPLC analysis indicated that 40 mg/ml concentration of cefepime hydrochloride maintained adequate stability for 2 hours at 45°C and up to 24 hours at 25 °C and up to 7 days at 5 °C.
Formulation and In Vivo Evaluation of Mucoadhesive Buccal Tablets of Carvedilol
Authors: Shirsand S. B. , Wadageri G V , Raju S A , Kolli Gopikrishna 
Published: August 2020

In present study we studied the feasibility of preparing mucoadhesive buccal delivery systems containing carvedilol to improve drug residence time on buccal mucosa and drug dissolution rate, to circumvent the first-pass metabolism and quick drug entry into the systemic circulation. Bilayer buccal tablets of carvedilol prepared using controlled release and mucoadhesive polymers (hydroxypropyl methylcellulose 15 cps, 50 cps, K4M and Carbopol 934p) along with impermeable backing layer (ethyl cellulose). 15 formulations were developed with varying concentrations of polymers. The designed tablets were evaluated for tablet size, shape, in vitro drug release, stability studies, bioavailability studies and drug-excipients interaction (FTIR). Among the 15 formulations, F151 containing hydroxypropyl methylcellulose 15 cps (48% w/w of matrix layer), Carbopol 934p (2% w/w of matrix layer) and mannitol (channeling agent, 34.5% w/w of matrix layer) was found to be promising. Dissolution tests revealed that 84.73% of carvedilol was dissolved from the formulation F151 in 8 h along with satisfactory bio adhesion strength (5.71 g). Bioavailability studies of the promising formulation were compared with that of the oral solution. The percentage relative bioavailability of the buccal tablets was found to be 121.27%. Stability studies, on the promising formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics (p<0.05). FTIR studies show no evidence of interaction between drug and excipients. It was concluded that mucoadhesive buccal tablets of carvedilol with controlled unidirectional drug release along with satisfactory bioadhesion strength and with sufficient residence time can be successfully developed by direct compression method.
Optimization and Evaluation of Solubility-Modulated Gastroretentive Floating Matrix Tablet of Furosemide
Authors: Lalwani Anita , Bhalodiya D , Patel C , Panchal L , Shelat P 
Published: August 2020

The objective of the present study was to prepare delivery system for furosemide which has poor solubility and has specific absorption in stomach. Solid dispersion of furosemide (SD) was prepared in polyethylene glycol 6000 and characterized using differential scanning calorimetry. Floating gastroretentive tablets of the prepared solid dispersion were then prepared by wet granulation technique, using polymer Methocel K100M CR (HPMC) and sodium bicarbonate. A 32 factorial design was applied systematically to study the effect of the amount of HPMC (X1) and sodium bicarbonate (X2) on the floating lag time (YFLT) and amount of drug release at the end of 1st hr (Y60), 6th hr (Y360) and 12th hr (Y720). The solubility of SD was higher than that of drug alone and the physical mixture. The results of multiple regression analysis, when applied to responses obtained for experimental design batches, indicated that low level of HPMC and high level of sodium bicarbonate decreased the floating lag time, while the amount of drug released at all time points decreased with increase in level of HPMC. Swelling behavior of experimental design batches was studied and its relationship with mechanism of drug release was interpreted. Batch D3 came close to satisfying the drug release and floating criteria. Drug compatibility with the excipients used was ascertained using FTIR. Stability studies were carried out at recommended storage conditions and the tablets were found to be stable. Delivery system could be developed for furosemide which addressed the solubility and site specificity issues of drug.
Formulation and Evaluation of Taste Masked Oral Disintegrating Tablets of Aripiprazole
Authors: Kumar Y. Shravan , Patel Prashanthi , Ch Sravanthi , B Rashmi 
Published: August 2020

Aripiprazole is an atypical antipsychotic agent used for treatment of schizophrenia, bipolar disorder and major depressive disorders. In the present work, oral disintegrating tablets of aripiprazole were developed to enhance the patient compliance and provide rapid onset of action. The efficacy of aripiprazole is mediated through a combination of partial agonist activity at dopamine D2 and serotonin 5HT-1A receptors and antagonist activity at 5HT-2A receptors. It has a bitter taste and poor-solubility in water. Thus, the main objective of the study is to formulate taste masked oral disintegrating tablets of aripiprazole by using inclusion complex beta-cyclodextrin to achieve a better dissolution rate and further improving the bioavailability of the drug. Oral disintegrating tablets were prepared by direct compression method using super disintegrant like crospovidone, croscarmellose sodium, sodium starch glycolate and combinations of cros-povidone with croscarmellose sodium, and crospovidone with sodium starch glycolate in different concentrations. They were evaluated for the pre-compression parameters such as bulk density, compressibility, Hausner ratio and angle of repose. The prepared batches of tablets were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time, in vitro dispersion time, and in vitro dissolution profile. All these parameters were found to be satisfactory. Among all, the formulation F15 containing crospovidone 5% + cros-povidone with croscarmellose sodium 5% was considered to be the optimum formulation, which released nearly 99% of the drug in 20 minutes with a disintegration time of 10. 20 seconds. These studies indicate the viability and benefits of oral disintegrating tablets of aripiprazole.
Chemical Constituents of Adesmia Boronioides and Evaluation of their Antioxidant Activity
Authors: Muñoz Orlando , Delporte C 
Published: August 2020

As part of our ongoing research into the pharmacologically active compounds of Chilean flora, here we did phytochemical investigation of Adesmia boronioides Hook.f (fabaceae). (Papilonaceae) leaves. This effort has led to isolation and identification of liqueritigenin, isoliquiritigenin, sesamin, isodrimenin and a kaempferol glycoside, kaempferol 3-O-β-D-[galactopyranosyl (1–2) rhamnoside]-7-O –α-L-rhamnopyranoside.Compound structures were identified by 1D- and 2D-NMR experiments, mass and UV spectrometry and comparison with data from the literature. This is the first time these compounds have been isolated from this plant’s leaves.These active constituents have been studied further pharmacologically. Antioxidant properties in A. boronioides leaves were determined.
Benzophenanthridine Alkaloids from Callus Cultures of Toddalia Asiatica
Authors: Veeresham Ciddi , Chinthala Praveena 
Published: August 2020

Benzophenenathridine alkaloids nitidine and chelerythrine production from callus cultures of Toddalia asiatica was investigated. Callus cultures were initiated on Murashige and Skoogs medium fortified with different hormonal combinations. Nitidine and chelerythrine levels in callus culture extracts was analyzed by high performance liquid chromatography and was found that medium supplemented with 2,4 (0.5 mg/l) + BA (1 mg/l) accumu-lated significant amount of nitidine and chelerythrine than any other phytomormonal combination employed. An attempt was also made to compare high performance liquid chromatography and HPTLC analysis for secondary metabolite estimation. Production of secondary metabolites through callus cultures may serve as a best alternate system and optimization of media will result in improved yield of secondary metabolites.
Pharmaceutical Development and Evaluation of Reservoirtype Ciprofloxacin Ocular Insert
Authors: Jethva Jayesh K , Trivedi Chintan H , Ratanpara Sarita P , Bathwar Geeta R , Parmar Ramesh B 
Published: August 2020

Ocular inserts of ciprofloxacin hydrochloride were prepared with the aim of achieving once a day administration. Drug reservoir was prepared using sodium CMC while rate controlling membrane was prepared using Eudragit RS100 and RL100. Ocular inserts were evaluated for their physicochemical parameters like thickness, weight uniformity, drug content, percent moisture loss, and percent moisture absorption. The in vitro drug release studies were carried out using Bi-chambered donor receiver compartment model. In vitro drug release kinetic data was treated according to Zero, First, and Higuchi kinetics to access the mechanism of drug release. At the end of 24th hr, in-vitro percentage drug release was obtained for the formulations RF1 was% 46.02 and for RF5 was 98.23%. The drug release from the formulation RF5 (Eudragit RS and RL 100 (1:1)) was 98.23 % at the end of 24th hour which was available as controlled and prolonged. In Kors Meyer Peppas, n value in optimized batch (RF5) was observed 1.399 which indicated super case II transport occurs. All physical parameters evaluated were satisfactory. So formulation RF5 was selected as the best formulation.
In Silico Study of Novel Fluoroquinolones as Inhibitors of Topoisomerase IV of Acinetobacter Baumannii
Authors: Sabbagh Ghalia , Murad Thanna 
Published: August 2020

New antibacterial agents needed to treat drug resistant infections. In this study, an effective novel flouroquinolones (FQ) against Acinetobacter baumannii(A. baumannii) were identified by the in silico analysis using iGemDock v2.1 tool, where the structure of Topoisomerase IV (Topo IV) was retrieved from the Protein Data Bank (PDB). The structures of (FQ) compounds were selected from literature survey of 400 novel synthesized compounds and they were obeyed for filtration of each compound for drug-relevant properties based on “Lipinski’s rule of five. Finally a total of 150 (FQ) were docked against the enzyme PDB ID-2XKK. From this study, it was found that the compound (1)[7-{4-[(2E)-2-(5-chloro-2-thienyl)-2-(methoxyimino)ethyl] piperazin-1-yl}-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid]and the compound (2) [1-ethyl-7-{4-[(2-ethyl-1H-benzimidazol-1-yl)methyl]-3-fluoropiperazin-1-yl}-4-oxo-1,4- dihydroquinoline-3-carboxylic acid] showed the best interaction value against 2XKK enzyme, the binding energy was (-105.61 kcal/mol),(-102.58 kcal/mol) respectively, whereas the reference moxifloxacin was (-79. 33 kcal/mol). These results lead to recognize novel (FQ)s against (A. baumannii) and further in vitro studiesare needed to confirm these compounds.
Design and Development of Microparticulate Drug Delivery System of Hydrochlorothiazide
Authors: Sakhare S.S. , Mali A.K. 
Published: August 2020

Microparticles open up new vistas of research in the development of novel drug delivery systems. Microparticles are defined as particulate dispersions or solid particles with size range of 1-1000 µm. Hydrochlorothiazide (HCT), diuretic drug, is practically insoluble in water and has a solubility of 250µg/mL in 0.1 N HCl (25 °C). Presently, the improvement of drug solubility is one of the most challenging fields in pharmaceutical development, therefore, we choose hydrochlorothiazide for the micro-particulate drug delivery. Microparticles of hydrochlorothiazide were prepared by solvent evaporation technique. The prepared microparticles were evaluated for various properties. Particle size determination of microparticles by optical microscopy showed uniform size distribution. The in vitro dissolution studies of hydrochlorothiazide microparticles showed better release effect (99.45%) over a period of 60 min as compared to pure drug. Thus a successful attempt was made to formulate microparticles of this BCS class II drug which resulted in increase in dissolution properties of hydrochlorothiazide microparticles.
Cellular and Molecular Mechanisms of Neuroinflammation in Epilepsy
Authors: Reddy D. Samba , Clossen Bryan , Medi Harika 
Published: August 2020

Epilepsy affects millions of people worldwide. Epilepsy is a chronic neurological disorder characterized by recurrent unprovoked seizures. Neuronal damage and inflammation are suggested to play a central role in the pathophysiology of epileptogenesis and chronic epilepsy. There is increasing evidence that excessive inflammatory actions of the neuroimmune system may contribute to the development of epilepsy following a variety of precipitating conditions, including brain injury, prolonged seizure events or status epilepticus, brain infections, stroke, and neurotoxicity. This review describes the current status of neuroinflammation in epilepsy and the therapeutic promise of targeting the brain immune system for chronic blockade of inflammation as an effective approach for preventing the onset of epilepsy and related hyperexcitability conditions. The inflammatory reaction is mediated by microglia, astrocytes, and other brain immune cells. It is well established that proinflammatory cytokines, interleukins, and related factors are critically involved in processes linked to epileptogenesis. Consequently, a variety of targeted therapeutic approaches have been tested in experimental models of epilepsy. There are many promising pharmacological strategies for targeted modulation of neuroinflammation including microglia inhibitors, cyclooxygenase inhibitors, prostaglandin receptor antagonists, and interleukin inhibitors. Overall, current reports suggest that many key outcome parameters of hyperexcitability, epileptogenesis, and neuroprotection have been successfully inhibited by specific blockade of proinflammatory signaling in the brain
Process Validation of Lyophilized Formulation of the Anticancer Drug Topotecan
Authors: Joseph Lincy , George Mathew , Chandran Rajimol T. , Jain Saurabh Kumar 
Published: August 2020

Sterile pharmaceutical products are produced under strict compliance with good manufacturing practices (GMP). The purpose of process validation is to provide documented evidence that the pharmaceutical system that is capable of continuously supplying the clean and conditioned air with the specified quality attributes and establish its dependability of cytosterile injection facility. Topotecan (Hycamtin) is an anticancer agent that is a topoisomerase inhibitor. It is a synthetic, water-soluble analog of the natural chemical compound camptothecin. This work is aimed to establish documentary evidence to demonstrate the anticancer drug topotecan hydrochloride process validation, under defined set of operating conditions are capable of producing the finished product as per the finished product specifications. The data generated were checked, compiled, and critically reviewed based on the final results. It has been observed that all the critical process parameters and analytical results for process validation batch are well within the limits and correlated with the expected compliance parameters
Comparative Bioavailability of Cefuroxime Axetil from Tablets and Self-Microemulsifying Drug Delivery Systems in Rats
Authors: Puttachari Satish , Kalyane Navanath. V. , Duttagupta Sarbani 
Published: August 2020

Cefuroxime axetil has poor bioavailability due to low solubility. This can be surmounted by preparing the drug by self-microemulsifying drug delivery system (SMEDDS). In this study the bioavailability of cefuroxime axetil from SMEDDS and tablets was evaluated in Wistar rats. The optimized SMEDDS formulation was prepared using Labrasol®, Gelucire® 44/14 and Lutrol®E400. The formulation was evaluated for micro-emulsification properties and percent in-vitro dissolution. The HPLC method was developed and optimized to estimate the drug content in the plasma. The method was clearly separating the cefuroxime A and B polymorphs and LOD and LOQ values are satisfactory. Rats were randomized in to two groups - one group of animals were administered with SMEDDS and another with tablet formulation. At frequent intervals the blood samples were withdrawn and analysed for drug content. The pharmacokinetic parameters were calculated using PK Solve software. The calculated bioavailability and tmax from SMEDDS was 1687.06 μg/ mL.min and 50 min, respectively, whereas for tablet it was 1219.803 μg/mL.min and 62 minutes, respectively. The bioavailability of SMEDDS formulation was 1.5 times more than the marketed formulation, indicating a significant improvement in oral bioavailability. In conclusion, this study confirms that the SMEDDS formulation is a viable strategy for enhancing the oral bioavailability of cefuroxime axetil
Current Progress in the Formulation and Taste-Masking Technologies for Mouth Dissolving Tablets
Authors: A V Misal , Godage G R , Belge S. A 
Published: August 2020

Within the past one decade, mouth dissolving or fast disintegrating tablet technology has received ever-increasing demand. Mouth dissolving or fast disintegrating tablet can be defined as a solid dosage form that can disintegrate or dissolved within half-minute in the oral cavity resulting in a solution or suspension without administration of water. Mouth dissolving tablet have been formulated for pediatric, geriatric, bedridden patient or mentally ill patient and may not have access to water. Patient incompliance occurs due to bitterness of formulation. So masking the bitterness become in dispensable. To surmount this problem, several newer techniques have been developed to mask the bitter taste. Such techniques are not only masked the bitter taste but also improved the bioavailability and performance of the drug formulation. This review article focus on taste-masking techniques, conventional and advanced technologies for fast disintegrating tablet. This article also describes the properties, advantages of mouth dissolving tablets and the need for developing a better mouth dissolving tablet.
Marine Streptomyces-derived Antibacterial Compound [2, 4-Dichloro-5-sulfamoyl benzoic acid] for MRSA and VRE Strains
Authors: K. Kannabiran , Rajan Benita Mercy 
Published: August 2020

The aim of the present study was to predict the interaction of 4-dichloro-5-sulfamoyl benzoic acid (DSBA) derived from Streptomyces sp. VITBRK3 with the drug target enzymes of methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococci (VRE) strains procured from ATCC. Two proteins dihydropteroate synthetase (DPS) and dihydrofolate reductase (DFR) were chosen as drug targets. The well-known folic acid synthesis inhibitor amino salicylic acid (ASA) was taken as a positive control. AutoDock 4.2.1 was used to perform the protein-ligand docking analysis. DSBA showed least binding energy of –6.99 kcal/mol and inhibition constant of 7.5 µM and formed 8 hydrogen bonds with DFR. DSBA showed least binding energy of -5.6 kcal/mol and inhibition constant of 78.58 µM and formed 7 hydrogen bonds with DPS. ASA showed the binding energy of –4.97 kcal/mol, and inhibition constant of 225.9 µM and formed 5 hydrogen bonds with DPS protein. It showed the binding energy of –4.68 kcal/mol, and inhibition constant of 371.32 µM and formed 4 hydrogen bonds with DFR protein. DSBA has qualified CMC rule, lead like rule and Lipinski’s rule of five. The compound DSBA does not possess any carcinogenic effect in rat or mouse model. Osiris Property Explorer analysis suggested that, DSBA does not possess any major side effects and is a suitable drug candidate. Pre ADMET analysis also suggests that, the lead compound, DSBA is a suitable drug candidate. The results of this study suggest that the antimicrobial activity of DSBA against MRSA and VRE strains is due to its inhibition over bacterial cell wall folic acid biosynthesis.