bluuebunny/crossref_metadata_2025 huggingface dataset:
Development of RP-HPLC Method for the Quantitative Estimation of Ofloxacin and Ornidazole in Combined Liquid Oral Dosage Forms
Authors: Menezes Cylma , G Varun , B Shyamkumar , N Reema
Published: August 2020

A simple, efficient and reproducible reversed phase high performance liquid chromatographic (RP-HPLC) method for the quantitative estimation of ofloxacin and ornidazole in bulk and in combined liquid oral dosage form has been developed and validated. The separation was carried out using thermohypersil phenyl column (250 mm × 4.6 mm, 5 μm) as stationary phase with isocratic flow and phosphate buffer (adjusted to pH 2.4 with ortho phosphoric acid): acetonitrile (87:13 v/v) as mobile phase. Mobile phase was maintained at a flow rate of 1.0 ml/min and UV detection was carried out at 294 nm. The retention time of ofloxacin and ornidazole was 10.40 and 5.69 min, respectively. All calibration curves showed good linear correlation coefficients within the tested limits (r2 > 0.9995). The linear dynamic range was 10-100 µg/ml and 25-250 µg/ml for ofloxacin and ornidazole respectively. Percentage recoveries for ofloxacin and Ornidazole were 100.48 % and 99.84 % respectively. All the analytical validation parameters were determined and found in the limit as per the International Conference on Harmonization (ICH) guidelines, which indicates the validity of the method. The validated method is also found to be accurate, precise and robust for the quantitative estimation of ofloxacin and ornidazole in combined liquid oral dosage forms.
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.
Development and Validation of Stability-indicating RP-HPLC Method for Coumarin Assay in Bulk Drugs and Pharmaceutical Products
Authors: Prabu S. Lakshmana , Thiyagarajan S , Balan P , Suriyaprakash T N K , S P Sharavanan
Published: August 2020

A simple, economic, selective, precise, rapid and reproducible stability indicating HPLC method for the analysis of coumarin (CMN) in bulk drugs and from pharmaceutical formulation has been developed and validated. Separation was achieved on a symmetry C18 column using a mobile phase consisting of a mixture of methanol:water in the ratio of (70:30%v/v) at a flow rate of 1ml/min with detection at 276 nm. Linear regression analysis data for the calibration revealed a good linear relationship between response and concentration in the range 2 μgml-1 to 14 μg ml1 of CMN; the correlation coefficient was 0.999. The LOD and LOQ were 30 and 100 ng ml-1 respectively. The method was validated for accuracy, precision, recovery, reproducibility, specificity, robustness and degradation studies. The statistical analysis showed the method to be precise, reproducible, selective, specific and accurate for analysis and estimation of coumarin in bulk drugs and pharmaceutical dosage forms.
Formulation and Evaluation of Solubility Enhanced Ciprofloxacin
Authors: Thakur R S , Nayaz A , Koushik Y
Published: August 2020

In the case of solubility limited absorption, creating supersaturation in the GI fluid is very critical as supersaturation may provide great improvement of oral absorption. The techniques to create the so-called supersaturation in the GI fluid include microemulsions, emulsions, liposomes, complexations, polymeric micelles, and conventional micelles. Ciprofloxacin was chosen because it is practically insoluble in water; hence its salt form is used commercially, which is soluble in water. The objective of the present investigation was to enhance the solubility of Ciprofloxacin by formulating it into microemulsion system. For this purpose, initially, surfactant and cosurfactant were selected based on their HLB value, followed by pseudo-ternary phase diagrams to identify the microemulsion existing zone. Different formulations were developed and evaluated for pH, conductivity, in vitro release and stability. Solubility study was performed for optimized formulation. The pH of the designed formulations varied from 6.02-7.04. This was ideal and near blood pH 7.4. Conductivity data indicated that the microemulsion was of the o/w type. In vitro release of optimized formulation(FM3) was 95.2% as compared to pure drug 46.61% after 90 min and marketed product(salt form) 93.9%. Hence, by formulating into microemulsion, the solubility of ciprofloxacin is significantly enhanced.
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.
Drug-Excipient Interaction during Formulation Development, in vitro andin vivo Evaluation of Gastroretentive Drug Delivery System for Nizatidine
Authors: V Kishan , Reddy Ramireddy Amarnath , Bomma Ramesh
Published: August 2020

The present investigation dealswith the development and evaluation of floating tablets of nizatidine to prolong the gastric residence time, increase local delivery of drug to the H2-receptor of the parietal cell wall to reduce stomach acid secretion. The drug-excipient compatibility studies were conducted by using FTIR, DSC and visual observations. Citric acid inclusion in formulations resulted in incompatibility and the composition was modified to eliminate the problem of incompatibility. Floating matrix tablets of nizatidine were developed by direct compression method using hydroxypropyl methylcellulose (HPMC K4M) and polyox WSR 1105 alone as release retardants and sodium bicarbonate as a gas-generating agent. Alleleven formulations exhibited satisfactory physicochemical characteristics andin vitro buoyancy. Formulations F6 and F10 exhibited controlled and prolonged drug release for 10 h with zero order release. Formulation (F10) was selected as optimized formulation based on physicochemical properties and in vitro drug release and was used inradiographic studies by incorporating BaSO4. The radiographic studies were conducted in comparison with plain controlled release tablets. These studies revealed that gastric retention time of floating and plain controlled release tablets in fasting state were 2 ± 0.86 h and ≤ 0.5 h respectively in human volunteers. Gastric retention time of floating and plain controlled release tablets in fed state were 5.33 ± 0.57 h and 1.66 ± 0.28 h respectively in human volunteers. In conclusion, optimal floating matrix tablet for nizatidine with desired in vitro buoyancy, in vivo gastric retention time and prolonged release could be prepare
An Overview of Optimization of Spherical Crystallisation Process
Authors: Bhagat N B , Yadav A V , Mastud P R , Khutale R A
Published: August 2020

In this article we describe the optimizing parameters in the process of spherical crystallisation. Particle engineering of active pharmaceutical agents is an innovative area of research in pharmaceutical industry because of several advantages. Spherical crystallization is one of the particle engineering technique in which drug directly gets crystallized and agglomerated into spherical shape. The spherical crystals can be obtained by different methods like solvent change, Quasi-emulsion droplet, ammonia diffusion and neutralisation. The optimization of process of spherical crystallization is important for obtaining the ideal spherical crystal agglomerates. It includes stirring rate, selection of solvent, pH, temperature etc. which affects on the physico-chemical properties of crystals. These optimizing parameters play its specific role in formation of spherical crystals. Stirring rate affects the shape as well as size of the final agglomerates and solvent selection helps in the formation of maximum amount of agglomerates in the system. The factors like pH and temperature should be maintained in case of drugs which show polymorphism. Apart from this, several others physical phenomenon or parameters like interfacial tension and rate of crystallisation are also important for thorough optimization of process.
Comparative Evaluation of Isoniazid and Rifampicin Dispersible Tablets Prepared by Direct Compression and Sublimation Methods
Authors: Bolmal Uday , Pandey C K , Phatarpekar V , Dhople N G , Kotha Rajkumar
Published: August 2020

Dispersible tablets are gaining popularity over conventional tablets due to its increased popularity for administration to pediatric and geriatric patients as it provides quick onset of action and ease of administration. An attempt had been made, to develop dispersible tablet of isoniazid and rifampicin combination by direct compression and sublimation method, to increase the bioavailability of the anti-tubercular agents as well to provide the local delivery in the case of oral tuberculosis. Formulation F1 to F8 (2% and 4% w/w of different superdisintegrants (crospovidone, pregelatinized starch, croscarmellose sodium and sodium starch glycolate) formulated by direct compression method. The formulations containing 4% of superdisintegrants (F2, F4, F6, and F8) were selected as optimized and hence 4% of superdisintegrants were used for sublimation method (F9 to F12). The effects of sublimating material (camphor) on drug release profile and disintegration property were evaluated. Studies on two different methods showed sublimation method as a better alternative as its formulations rapidly disintegrates, disperse and shows faster drug release (in 14 min) in comparison to direct compression (in 20 min). Pre-compression parameters of formulation blends indicated good flow properties and compressibility. Simultaneous estimation was performed for calculation of drug content and % drug release. In vitro release data analysis revealed 90% drug release. F9 formulation (sublimation) showed best anti-tubercular activity. F2, F9 formulations were found to be stable even after 90 days. Hence it is evident from this study that fast dissolving tablets could be a promising delivery system for isoniazid and rifampicin with improved drug availability and better patient compliance.
Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles
Authors: Gupta Dilip Kumar , Razdan B K , Bajpai Meenakshi
Published: August 2020

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.
Development and Validation of Derivative Spectroscopic Method for Simultaneous Estimation of Cefadroxil and Probenecid
Authors: Mehta Pratik S , Patel Pratik R. , Parmar Rajesh R , Modasiya M M K , Shah Dushyant A
Published: August 2020

A novel, simple, accurate, sensitive, precise and economical derivative spectroscopic method was developed and validated for the determination of cefadroxil and probenecid in synthetic mixture. First order derivative spectroscopy method was adopted to eliminate spectral interference. The method obeys Beer’s Law in concentration ranges of 4-36 μg/ml for cefadroxil and of 5-25 μg/ml of probenecid. The zero crossing point for cefadroxil and probenecid was 260 nm and 237.8 nm respectively in 0.1N HCl. The method was validated in terms of accuracy, precision, linearity, limits of detection, limits of quantitation. This method has been successively applied to synthetic mixture and no interference from the synthetic mixture’s excipients was found.
Formulation and Evaluation of Gastroretentive Nanoparticles of Repaglinide
Authors: Jamkar P M , Gujar K N , Nemmaniwar S B , Kulkarni N B
Published: August 2020

Controlled drug release system is one of the most favourable technique of novel drug delivery system owing to its reproducibility and ease of formulation. Nanotechnology is very useful for controlling the drug release and thus improving the pharmacokinetic and pharmacodynamic properties of the drug. The technique improves patient compliance by reducing both dose and the frequency of administration and thus minimizing the local as well as systemic toxic effects. The aim of the present research work was to formulate and evaluate gastroretentive nanoparticles of Repaglinide, an anti-diabetic drug by using the ionotropic gelation method. Repaglinide has a very short half-life of 1 hour with bioavailability 56%. Sustained release mucoadhesive nanoparticles of Repaglinide were prepared to increase the drug residence time in gastrointestinal tract and thus improving the bioavailability of drug. The mucoadhesive nanoparticles were prepared by using chitosan and sodium alginate as polymers; calcium chloride as the crosslinking agent. Different formulations were prepared with varying concentrations of chitosan and sodium alginate in order to achieve the optimum particle size and maximum encapsulation efficiency. The particle size of nanoparticles was found to be in the range of 300 nm to 756 nm. Drug encapsulation efficiency ranged between 56% to 80% with controlled drug release upto 88% in phosphate buffer pH 7.4 and 75% drug release in 0.1N HCl in 12 hrs. FT-IR and DSC studies showed that the drug and polymers were compatible. The results of swelling study and bioadhesive strength indicated that optimized formulation exhibited excellent mucoadhesive properties
Development and In vivo Bioavailability Evaluation of Sumatriptan Succinate Buccal Tablets
Authors: Singh Sudarshan , Savaliya Dharmesh , Shah D. Suresh , Bothara B Sunil
Published: August 2020

In the present investigation an attempt has made to design mucoadhesive buccal tablets of sumatriptan succinate to improve its bioavailability. The mucoadhesive buccal tablets were prepared by wet granulation procedure using different concentration of polycarbophil and hydroxy propyl methyl cellulose K4M alone. Compatibility study of drug and polymer were performed by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Precompression property of sumatriptan succinate was evaluated to check the suitability of compression method. Postcompressional parameters such as weight variation, hardness, thickness, surface pH, in vitro drug release, ex vivo bioadhesion time, ex vivo mucoadhesive strength, ex vivo permeation study and in vivo bioavailability study of optimized formulation were evaluated. FTIR spectroscopy and DSC study revealed that there was no possible interaction between drug and polymers, because no major change in peaks were obtained. The precompression parameters were in acceptable range of pharmacopoeial specification. The surface pH of the tablets was in the range of salivary pH (6.5 to 7.5) and tablets showed good ex vivo bioadhesion time up to 10 hr which indicated good adhesive capacity of tablets. The in vitro release of optimized formulation obeyed zero order kinetics with non-Fickian anomalous diffusion mechanism. The percentage relative bioavailability of sumatriptan succinate from optimized buccal tablets was found to be 152.76 %. Buccal tablets of sumatriptan succinate were successfully prepared with improved bioavailability.
Phytochemical Evaluation and Screening of Cardiotonic, Antibacterial and Anthelmintic Activities of Sida cordifolia L.
Authors: Kumar Sarella Prakash Nathaniel , L.K. Kanthal , S Durga , D Achutha Rama Raju , K Satyavati
Published: August 2020

Several herbs are traditionally used in the treatment of a variety of ailments particularly in the rural areas, where herbal medicine is mainly the source of health care system. Many of these herbs havenot been assessed for safety or toxicity to tissue or organs of the mammalian recipients. An attempt is made to prove the efficacy of Sida cordifolia Linn., (a traditional medicinal plant chosen on the basis of ethnomedical knowledge) for its Cardiotonic, Antibacterial and Anthelmintic activities. Sida cordofolia Linn., is used traditionally, inter alia, in the treatment of various infections, asthma, diarrhoea, heart and stomach disorders. Cardiotonicactivity is performed using isolated Frog Heart Perfusion Technique. Antibacterial activity of the whole plant extracts were assessed by Agar well diffusion method against the strains of Bacillus subtilis, Escherichia coli, and Staphylococcus aureus. Anthelmintic activity was studied against Pheretima posthuma. Phytochemical screening of powdered plant material revealed thepresence of some secondary metabolites such as alkaloids, saponins, tannins, glycosides and flavonoids. Results indicated that methanol, chloroform, aqueous extracts have significant cardiotonic activity but less than standard drugs. Methanol and Aqueous extracts showed high antibacterial activity and anthelmintic activity than the standard drugs. In a nutshell, we can conclude that the methanol and aqueous fractions of Sida cordifolia Linn., had a profound antibacterial and anthelmintic effect eventhough it possessed very significant cardiotonic activity. This validates its continuous usage in ethnomedicine. This plant could be developed into cheap, safe and culturally acceptable standardized herbal products and may serve as asource of new molecules for broad-spectrum antimicrobial and anthelmintic agent.
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.
RP-HPLC Method for Simultaneous Estimation of Ciprofloxacin and Phenylephrine in Combined Dosage Forms
Authors: Patel Harsh B , Patel Paresh U
Published: August 2020

A new, simple, rapid, selective, precise and accurate gradient RP-HPLC method has been developed for simultaneous estimation of Ciprofloxacin and Phenylephrine Hydrochloride in combined dosage form. The separation was achieved by using Thermic Hypersil C column (250 mm x 4.6 mm, 5 µm particle size) coupled with a guard column of same material, in mobile phase Acetonitrile: Methanol: Phosphate Buffer pH 6 (10: 65: 25, v/v/v). The flow rate was 1.0 ml/min and the separated drugs were detected using UV detector at the wavelength of 220 nm. The analysis was performed at room temperature (37 ± 2 ºC). The retention time of Ciprofloxacin and Phenylephrine Hydrochloride was noted to be 6.63 and 4.49 min, respectively, indicative of rather shorter analysis time. The method was validated as per ICH guidelines. The calibration curves were linear (r2 > 0.9980) over a concentration range from 0.5 – 4.0 μg/ml and 2.0 – 5.5 μg/ml for Ciprofloxacin and Phenylephrine Hydrochloride, respectively. The relative standard deviation (RSD) was < 2.0% and the mean recovery was 100.51 ± 0.34 and 100.81 ± 0.80 for Ciprofloxacin and Phenylephrine Hydro-chloride, respectively. The proposed method was found to be accurate, reproducible, and consistent. It was successfully applied for the analysis of these drugs in marketed formulations and could be effectively used for the routine analysis of formulations containing any one of the above drugs, or a combination, without any alteration in the chromatographic conditions.
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.
Formulation and Evaluation of Nanosuspension Formulations of Ramipril using Hydrophilic Polymers
Authors: Nerker Pankaj P , Mahajan Hitendra , Deore Sagar , Ige Pradyumn
Published: August 2020

Nanosuspensions provide convenient formulations for improving the bioavailability and drug delivery. The objective of the investigation was to develop stable nanosuspension formulation of ramipril, with minimum surfactant concentration that could improve its solubility, stability and oral bioavailability. Ramipril is a potent antihypertensive drug, which act by inhibiting the angiotensin-converting enzyme. Nanosuspension was developed by antisolvent precipitation followed by high-pressure homogenization using hydrophilic polymers such as HPMC E5, HPMC E15, PVP K30, PVP K25, and PVA. The resulting nanosuspension was transformed into dry powder by freeze-drying process. Among all five formulations a formulation was choosen on the basis of results obtained from comparative study between different polymers based nanosuspension formulation of ramipril. The nanosuspension prepared was then evaluated for particle size, polydispesivity index, zeta potential, entrapment efficiency, saturated solubility study, scanning electron microscopy, differential scanning colorometry, and X ray diffraction. The combination of soya lecithin and pluronic F-68 as stabilizers yield nanosuspension with the smallest average particle size. The formulation of ramipril based on HPMC E 15 (Formulation B) shown enhanced dissolution rate. In which more than 60% of the drug was dissolved in the first 20 min compared to less than 25% of the pure drug within the same time period. The increase in the in vitro dissolution rate, nano size may favourably affect bioavailability.
Formulation and Evaluation of Orally Disintegrating Tablets of Lamotrigine
Authors: Singh Sudarshan , Shyale S S , Karade P
Published: August 2020

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.
Simultaneous Determination of Dextromethorphan and Promethazine in Pharmaceutical Syrups by Rapid HPLC Method
Authors: Trefi Saleh
Published: August 2020

A simple, precise and accurate method is validated for the simultaneous determination of two nitrogenous compounds dextromethorphan hydrobromide and promethazine hydro-chloride, which are commonly used as active ingredients in pharmaceutical syrups. The chromatographic conditions comprised of a classical C8-type stationary phase (250 × 4.6 mm, 5 μm) with a mobile phase consisting of 3 g of sodium lauryl sulfatein a mixture of 400 ml of water and 600 ml of acetonitrile along with 0.5 g of ammonium nitrate as additional agent. The solution pH 2.0 was adjusted with glacial acetic acid. The flow rate was 1 ml/min; the detection was carried out at 280 nm under temperature of 25o. The retention time of dextromethorphan was 8.5 min and 9.9 min for promethazine. The method was validated for specificity, accuracy, precision and linearity. The results indicate that the drugs are susceptible to photo-degradation. All the peaks of degraded products were resolved from the two active pharmaceutical ingredients with significant different retention times.
Formulation and Evaluation of Fish Oil-based Rizatriptan Microemulsion for Intranasal Migraine Treatment
Authors: Upadhye Kanchan P , Senpal Divya , Nimbalwar Minakshee , Dixit Gouri
Published: August 2020

In the present study microemulsion based intranasal gel of rizatriptan using fish oil was prepared for treatment and management of migraine to sustain the drug release and improve the drug residence time in nasal cavity. Fish oil is reported to have antimigraine activity hence it has been used in the present formulation along with cremophore EL as surfactant and Transcutol P as co-surfactant. The pseudoternary phase diagram plotted with these components shown the microemulsion existence region in ratio of (1:9-9:1) surfactant and co-surfactant. The optimized micro-emulsion contained fish oil (45.29%), cremophore E/transcutol P (2:1) and was characterized for pH (6.3±0.02), viscosity (114 ± 3.00cp), % transmittance (99.5 ± 1.01), refractive index (1.335±0.01),). The prepared microemulsion gels were optimized and characterized for in-vitro studies, pH, drug content, rheological studies and stability study. The release of rizatriptan from micro-emulsion gel prepared from carbopol 934 (98.01%) was found to be higher and prolonged than plain gel. Thus, microemulsion based gel was able to prolong drug releaseand improve drug residence time in the nasal cavity.
Recent Advances in Nanotechnology based Tubercular Chemotherapy
Authors: Dureja Harish , Khatak Sunil
Published: August 2020

Tuberculosis (TB) is a more prevalent granulomatos bacterial infection, which remains the world’s second most common cause of death due to infections of Mycobacterium tuberculosis (M.Tuberculosis). A number of characteristics of mycobacterium makes there disease chronic and necessitate prolonged treatment. The emergence of multi-drug-resistance (MDR) stains of M.Tuberculosis makes its necessary for the development of effective combinations of either first-line or second-line drugs or discovery of new safe and effective drug molecules and also implements other modalities of treatment. A number of novel carrier-based drug delivery systems incorporating the traditional and newer anti-tubercular agents have been shown incredible promise to target the site of action, reduce dosing frequency and enhance drug bioavailability with the objective of improving patient compliance. Nanoparticulate system have unique and comparatively more effective drug delivery carriers, including liposomal-mediated drug delivery, polymeric nanoparticles/microparticles, solid lipid nanoparticles, nanosuspensions, nanoemulsions, niosomes, dendrimers, Metal/cyclodextrin inclusion complexes and other nanosystems exploiting the extraordinary properties of matter at the nanoscale. Nanoparticles shown significant improvements in diagnosis, treatment and prevention and provide the flexibility of selecting the invasive and non-invasive route of delivery for chemotherapy of tuberculosis. This manuscript have been made to highlight and overviews the present WHO estimated burden of tuberculosis globally, recent discovery of safe and effective newer anti-tubercular drug moleculesfor MDR and XDR tuberculosis, first and second line anti-tubercular drugs loaded novel nanoparticle carriers for chemotherapy and development of solid lipid nanoparticles as an alternative drug carriers for tubercular chemotherapy.
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.
Solubility Enhancement of Hydrochlorothiazide using a Novel Drug-Drug Solid Dispersion Technology
Authors: Sonpal Rakshit N , Shelat Pragna , Lalwani Anita
Published: August 2020

Fixed dose combination (FDC) is commonly used in pharmaceuticals to reduce pill burden and optimize the drug therapy. The recent advancements in combinatorial chemistry often lead to drugs with low aqueous solubility. Many FDC’s contain at least one drug with suboptimal physicochemical properties like BCS class II drugs for which its poor aqueous solubility may often be a limiting factor to its bioavailability. Considering the above fact, a novel drug – drug solid dispersion has been developed in present study, wherein a poorly soluble drug hydrochlorothiazide has been solid dispersed in a hydrophilic drug, Metoprolol tartrate with which it is available as a FDC. Hydrochlorothiazide was solid dispersed in Metoprolol tartrate in ratios as available in market and also in conventional carrier mannitol by melting method. Physical mixtures of the two drugs and hydrochlorothiazide and mannitol were also prepared in the same ratio. Physical mixture did not show any signs of incompatibility in the FTIR study. In vitro dissolution study showed that t90% was less for solid dispersion (SDMT4) as compared to pure drug and physical mixture of the two drugs and so was selected for further study. The SDMT4 batch was then subjected to DSC analysis and XRD study, where the results suggested amorphization of hydro-chlorothiazide. Tablets were prepared from the SDMT4 batch and the in vitro release profile was compared to marketed formulation of hydrochlorothiazide. Tablets were subjected to accelerated stability analysis for 6 months at 40 °C and 75 % RH and were found to remain stable. Pharmacokinetic analysis was carried out with pure drug and SDMT4 and relative bioavailability was estimated to be 1.21. Thus a novel concept where in one drug is solid dispersed in other was hypothesized and proved. The concept can be explored for many such FDC’s.
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.
Preventive Measures and Treatment of Drug Resistant Malaria
Authors: Gupta Dilip Kumar , Razdan B. K. , Bajpai Meenakshi
Published: August 2020

Malaria is mostly a preventable but devastating parasite disease widely prevalent in underdeveloped countries. Malaria is a vector-borne infectious disease caused by the protozoan Plasmodium parasites. The annual incidence of malaria is about 515 million people and malaria mortality accounts for nearly 3 million people, the majority of whom are young children in sub-Saharan Africa. Malaria is widespread in tropical and subtropical regions, including parts of the Americas, Asia, and Africa. Due to climate change and the gradual warming of the temperate regions the future distribution of the malaria disease might include regions which are today seen as safe. Currently, malaria control requires an integrated approach comprising of mainly prevention, including vector control and the use of effective prophylactic medicines, and treatment of infected patients with antimalarial drugs. The antimalarial chloroquine, which was in the past a mainstay of malaria control, is now ineffective in most malaria areas and resistance to other antimalarial drugs is also increasing rapidly. Artemisinin-based Combination Therapies (ACTs) are now generally considered as the best current treatment for uncomplicated Plasmodium falciparum malaria. Such combination therapies are currently recommend by the World Health Organization because of widespread resistance of the disease to conventional drug therapies, such as chloroquine, sulfadoxine, pyrimethamine and amodiaquine, has increased. ACTs are the most effective drug treatments currently. ACTs produce a very rapid therapeutic response to malaria and should be adopted worldwide
Formulation and Comparative Evaluation of Transdermal Patch and Proniosomal Gel of Ropinirole, An Anti-Parkinson’s Drug
Authors: Shah Hardik A. , Patel Disha R. , Sonpal Rakshit N. , Prajapati Paresh A. , Patel Madhabhai M.
Published: August 2020

The conventional multidose antiparkinson’s therapy leads to re-emergence of Parkinson’s symptoms, due to fluctuations in serum levels of drug. Ropinirole HCl is a drug used to treat Parkinson’s disorder and it is suitable drug candidate for transdermal delivery due to its small molecular size, optimum log P and low oral bioavailability due to first pass metabolism. The combination of Different HPMC grades with PVP K 30 was used to formulate transdermal matrix by solvent Evaporation Method. A 32 full factorial design was used for optimization in which grade of HPMC (X1), % concentration of PVP K30 (X2) were selected as independent variables while t90% was taken as dependent variables. Further Proniosomal gel was also formulated using coacervation phase separation method. Formulated transdermal patch was evaluated for their folding endurance, tensile strength and t90%. Proniosomal gel was evaluated for their vesicle size, morphological analysis was done by Scanning Electron Microscopy. Both transdermal patch and Proniosomal gel were compared for their Flux, t90 %,CombinationofHPMC K 100M with PVP K30 Showed Highest drug retention which was confirmed by stastical analysis using factorial design. Gel formulation with Span 60 showed good polydispersitivity with particle size distribution of 0.497 µm. comparative flux showed that Proniosomes have better flux on other hand transdermal patch are retaining drug for more time.Present work showed possibility to formulatetransdermal patch and proniosomal Gel to attain desired release of Ropinirole HCL up to 24hr. It is possible to use different blend of HPMC and PVP K30, Proniosomal gel can also be used for sustain release of drug with sufficient lipophilic characters