ABSTRACT

Plants have been an important source for developing drugs since time immemorial. Various medicinal herbs are indigenous to the Indian subcontinent and Asparagus is one such plant. Asparagus racemosus Willd., more commonly known as Shatavari, has been traditionally used in many systems of medicine such as Ayurveda, Unani and Siddha. It has been used for decades as a galactogogue, uterine tonic, adaptogen, and rejuvenator. Also it has been used to mitigate symptoms of peptic ulcer, as an immunostimulant, hepatoprotective, and aphrodisiac. In addition, several other health benefits of this wonder plant, such as antidepressant, antiamnesic, antianxiety, hypolipidemic, antidiabetic, and anticonvulsant effects have been discovered in the recent years. In this article, an effort has been made to comprehensively enumerate all the health benefits of A. racemosus, known so far.

Keywords: Asparagus racemosus, Shatavari, Galactogogue, Immunostimulant, Hepatoprotective, Uterine relaxant.

ABSTRACT

Cubosomes are bicontinuous cubic liquid crystalline phases formed by the self-assembly of polar lipids, monolein, in water. They offer unique physicochemical properties than the other common colloidal delivery systems such as liposomes and nanoparticles. The article reviews about definition of cubosomes, advantages and disadvantages, composition and different production and characterization techniques. Moreover, there is an emphasis on the importance of cubosomes for the effective delivery of anticancer drugs.

Keywords: Cubosomes; monolein; anticancer; production; characterization.

ABSTRACT

The area of pharmaceuticals and synthetic organic chemistry continued to remain dependent on the heterocyclic compounds due to their wide array of properties both biological and synthetic. However, their extensive clinical use as medicinal drugs and their synthetic applications has been prompting the chemists to develop new structural triazole derivatives. Benzotriazole is benzene fused azole derivative exhibiting tremendous application in medicinal and synthetic chemistry. Benzotriazole bearing compounds possess various activities such as anticancer, antifungal, antibacterial, antitubercular, antiviral, antioxidative, antiparasitic, antioxidative. Also, the versatility and usefulness of benzotriazole methodology in synthesis protocol has grown from an obscure level to extreme popularity, since benzotriazole moiety can easily be introduced into a molecule by variety of reactions, thus allowing numerous transformations, and finally its stability and ease of removal at the of the reaction sequence.  In this review, we briefly describe the development of new benzotriazole compounds having wide range of applications during the period of 2011 to 2016.

Keywords: Benzotriazole, antibacterial, antimicrobial, peptide, hydrazides.  

ABSTRACT

Thiophene an important heterocyclic nucleus has been established as the potential scaffold entity in the largely growing chemical world of heterocyclic compounds possessing agrochemical, dyes and potent pharmacological characteristics. The present review, provide a broad view of the synthetic routes of 2-aminothiophenes and further explore their biological profiles and synthetic utility. The knowledge of various synthetic pathways and the diverse physicochemical parameters of 2-aminothiophenes draw the special attention of medicinal chemists to produce combinatorial library and carry out exhaustive efforts in the search of lead molecules.

Keywords: 2-Aminothiophene, heterocycles, biological activity, fluorescence, synthon.

ABSTRACT

The transdermal route of drug delivery overcomes many of the limitations associated with the more common oral and parenteral routes. Micro needles are micronized needles made from biodegradable polymer, ranging from 25 to 2000 µm in height, made up of variety of the material and shape. Advantages associated with micro needles are ease of use, controlled drug delivery, avoidance of first pass metabolism and lack of pain. However, transdermal drug delivery is limited due to the barrier provided by our skin known as stratum corneum which is the outermost non-viable layer of the epidermis. Microneedles were developed with the advantage that these can deliver the drug in a non- invasive painless manner and along with this overcome stratum corneum. The upper layer of the skin is penetrated by the microneedles without reaching the nerve, there by delivering drug transdermally in a painless manner. The present poster discusses the various fabrication techniques of micro needles using microelectromechanical system the design, material consideration and the application of micro needles in transdermal drug delivery system.

Keywords: Controlled drug delivery, Microelectomechanical system, Micro needles, Transdermal drug delivery system.

ABSTRACT

Diabetes mellitus  is a chronic disease that is characterized by inadequate pancreatic insulin secretion or poor insulin directed mobilization of glucose by target cells. Population affected with diabetes has increased from 108 million in 1980 to 422 million till date. So, it is clearly evident that the rate is alarming and diabetes has now become a global problem. Diabetes is seventh leading cause of death globally. Insulin therapy in diabetes is the commonest and the most effective therapy. Conventional methods like subcutaneous or the oral route are having several shortcomings like the pain and invasion associated with injections, oral degradation of insulin, infection, etc. Among all the demerits hypoglycemia is the major issue especially nocturnal hypoglycemia as the patient cannot monitor the level of glucose at night. To overcome these detriments there is a need for insulin delivery through novel technologies.  Many novel technologies have been proposed like the painless smart patch, Clicksoft microinjection device, pens, pumps, modified oral delivery oral delivery, inhaled insulin, etc. for the delivery of insulin.  Many other novel devices and routes are being developed. This review discusses the glimpse of these novel technologies with their pros and cons.

Keywords: Diabetes Mellitus, Insulin, Smart Patch, Clicksoft microinjection device, Afrezza.

ABSTRACT

Melt granulation has gathered increasing interest in the pharmaceutical industry for the concept of utilizing a molten liquid as a binder. Melt granulation process is currently applied in the pharmaceuticals for the manufacture of variety of dosage forms and formulation such as immediate release and sustained release pellets, granules and tablets. This technique has been used for improving bioavailability of poorly water soluble drugs. The review article gives updates about the latest developments in technology behind use of melt granulation process. Article deals with in depth basic information about granule growth mechanisms during melt granulation. The article also provides an insight to Equipments and factors influencing the melt granulation process & its applications to improve the dosage form characteristics which are utilized for industrial production.

Keywords: Melt granulation, Bioavailability, Binder.

ABSTRACT

Alzheimer’s disease is a degenerative brain disease and the most common cause of dementia. Dementia is also caused by other diseases and conditions. it is characterized by decline in memory , language , problem solving and other cognitive skills that effects a person’s ability to perform everyday activities. This decline occurs because nerve cells (neurons) in parts of the brain involved in cognitive function have been damaged and no longer function normally , In Alzheimer’s neuronal damage eventually affects parts of the brain that enable a person to carry out basic bodily functions such as walking and swallowing . People in the final stages of the disease are bed-bound and required around  the-clock care .Alzheimer’s disease is ultimately fatal.¹

Keywords: Alzheimer’s disease, brain disease, dementia, memory, nerve cells, walking , neuronal damage , cognitive skills

ABSTRACT

When gels and emulsions are used in combined form the dosage form are referred as emulgel. Also there has been incredible interest for the utilization of novel polymers and drug molecules. A one of the feature of topical drug delivery is the immediate availability of the skin as  target organ for diagnosis and treatment. Among the different group of semisolid planning, the utilization of gel has extended both in cosmetics and in the pharmaceuticals. Although Gel has many advantages, there is many limitation in delivery of hydrophobic drugs, so to overcome this limitation an emulsion base novel approach is being most used. That is emugel system used so that even a hydrophobic moiety can enjoy the unique properties of gels and having characteristics of dual control release i.e. emulsion as well as gel. The formulation is prepared by various polymer which behave as an emulsifer and thickening agent because of gelling capacity of these compounds give rise to stable emulsions and creams by diminishing surface and interfacial pressure while in the meantime expanding the thickness of the aqueous phase. In order to understand the potential of emulgel as delivery vehicles, this review gives an overview of the ideal properties, formation, and characterization of emulgels. So this can be use as analgesics and antifungal drugs, as superior topical drug delivery systems over present conventional systems available in market.

Keywords: Emulgel, Cosmetology, Hydrophobic Drug, Polymer, Chronic Skin Diseases.

ABSTRACT

Targeted drug delivery systems deliver the drug to the site of action. Colon Targeted drug delivery is considered as one of the most convenient pathway for the delivery of the drugs or therapeutic agents and used in the treatment of the local diseases. Microencapsulation is widely used in the pharmaceutical and other sciences to mask taste/odors, prolong release, impart stability to drug molecules, improve bioavailability, and as multiparticulate dosage forms to produce controlled or targeted drug delivery. Microencapsulation is the process in which small droplets or particles of liquid or solid material are surrounded or coated by a continuous film of polymeric materials. Microencapsulation system offers potential advantages over the conventional drug delivery systems. In this present article various technologies for the preparation of microcapsules for the purpose of colon targeted drug delivery systems are reviewed.

Keywords: Colon Targeted Drug Delivery, Approaches, Microcapsules, Technologies, Evaluation.

ABSTRACT

Bauhinia variegata Linn widely used in folk medicine for varied purposes to treat different kinds of pathologies particularly diabetes, infections, pain and inflammation owing to the presence of numerous phytochemicals residing in the plant. The chemical constituents isolated so far from the plant are β-sitosterol, kaempferol-3-glucoside, tannins, carbohydrates, amides, reducing sugars, vitamin C, crude protein, fibers, calcium, phosphorus, quercetin, rutin, quercitrin, apigenin, apigenin- 7-O-glucoside, heptatriacontan-12, 13-diol and dotetracontan-15-en-9-ol. Different parts of Bauhinia variegata like leaves, bark and flowers have significant antioxidant activity. Bauhinia variegata can be considered as a model herbal drug for experimental studies including free radical induced disorders like cancer, diabetes, atherosclerosis etc.

Keywords: Bauhinia Variegata, Antidiabetic, Antioxidant, Flavanoids, Diabetes.

ABSTRACT

Childhood vaccination is our primary method to promote public health. Concerns and controversies about vaccination and vaccine safety had led some parents to decline recommended vaccination of their children ⁴.This study systematically reviewed the literatures on controversies in childhood immunization ². The objective of our study is to assess the controversies and risk benefit ratio of vaccination from the available data ⁴.  Data resources were collected from existing articles, electronic citations and existing reviews. Supportive to some personal beliefs of parents and their trust to other systems of medicine like homoeopathy there are reports of ill effects of vaccines(poliomyelitis by oral polio vaccine, encephalitis by measles vaccine) . Some other disorders had also been reported with or without evidence. But most of the studies concludes that the benefits of immunization far outweighs risk. The risk of many diseases and mortality rate had decreased in present era due to vaccination. A dramatic example of the benefits generated by vaccination is evident in the context of diphtheria. During the 1930s an average of 61,000 cases of the disease were experienced each year in England and Wales, resulting in the deaths of approximately 3,000 individuals ³ .Studies shows that after taking immunisation ,during the first three years and nine months of the 1980s there were 15 notified cases of diphtheria and only one death. Poliomyelitis routine immunisation for infants has been pursued in England and in the 1980s only 10 cases of acute poliomyelitis have been notified to the authorities from an average of 2827 notified cases in 1956.  Educating parents about vaccine preventable diseases as well as the vaccines may be one of the ways to impart the importance of vaccines to the health of their child ¹.

Keyword: Poliomyelitis, Acute encephalitis

ABSTRACT

“Non-conventional” synthetic method has shown broad applications as a very efficient way to accelerate the course of many organic reactions, producing high yields, higher selectivity and lower quantities of side products consequently easier work-up and purification of the products.  One-pot two-component condensation of 1-formamidino-5-ethylformamidonothicarbamide (llla) with various isocyano-dichlorides (Xla-g) were carried out in presence of lemon juice as a biocatalyst respectively to synthesize a novel series of 2-substitutedimino-4-amino-6-ethylformamidino-1,3,5-thiadiazines (Xlla-g) which are either to unknown. The structures were confirmed by conventional chemical characterization, elemental analysis and spectral studies.  

Keywords: Lemon Juice, various isocyanodichlorides, 1-formamidino-5-ethylformamidonothicarbamide.

ABSTRACT

Drug-protein interactions are important since most of the administered drugs are extensively and reversibly bound to albumin and drug is transported mainly as a complex with protein.  The interactions between quercetin and Egg albumin was analyzed by fluorescence resonance energy transfer theory. According to this, the average binding distance between quercetin and egg albumin was obtained.

Keywords: FRET, Egg albumin, quercetin, fluorescence.

ABSTRACT

Last three decades enormous work has been carried out on computational chemistry. The projects given for discovery of New Chemical Entities by these methods and gets a safe, potent drug molecule. However, the commercial output for the pharmaceutical company with these methodologies is negligible. Most of the drugs discovered in medicinal chemistry are accidentally. Thus synthesis of focused compound libraries and their pharmacological screening by efficient methods becomes powerful tool for drug discovery. But some additional points are required to move towards aryloxypropanolamines As 1-Aryloxy-3-(N⁴-substituted piperazinyl) propan-2 OLS (aryloxypropanolamines) shows β-adrenergic receptor antagonist activity (β-blockers), these chemical entities are applicable in management of various diseases due to their therapeutic effects. The main clinical indications of β-blockers are in the area of cardiovascular diseases, such as hypertension, angina pectoris, myocardial infarction and cardiac arrhythmias^1-4. However, some β-blockers readily access the brain because of their lipophilicity and can influence some central nervous system functions. Therefore, Propranolol has been used for the treatment of anxiety syndromes, prophylaxis of migraine headaches, schizophrenia, alcohol withdrawals and tremors^5-8. Looking at the biological profile of various aryloxypropanolamines (also Enciprazine) molecule, synthesis of various derivatives of Enciprazine having different aryloxy moiety and amine moiety (by taking different N- alkyl/aryl substituted piperazine) was planned to get safe, potent or new activity molecules.

Keywords: QSAR, Principles of QSAR, QSAR models, QSAR model Validation

ABSTRACT

A rapid, sensitive, precise, and accurate HPLC method coupled with a photodiode array detector was developed, optimized, and validated for the estimation of everolimus in bulk and tablet dosage forms. The chromatographic separation was achieved using a kromosil C8 column (200 mm × 4.6 mm i.d., 5 μm particle size) at 30°C temperature. The isocratic mobile phase consisted of 0.1M dipotassium hydrogen phosphate and methanol (60:40, v/v). The mobile phase was delivered at 1.0 ml/min and the analyte was monitored at 277 nm. The method was successfully validated in accordance to International Conference on Harmonization. The retention time of everolimus was found to be 3.496 min, and the calibration curve was linear in the concentration range of 50-150 μg/ml (R² = 0.9992). The limit of detection and the limit of quantitation were found to be 0.109 μg/ml and 0.364 μg/ml, respectively.  The proposed method is accurate (percent recoveries were in the range of 99.56-100.09%) and precise (percent relative standard deviation - 0.047 %). No chromatographic interferences from the tablet excipients and components of mobile phase were found. The proposed method was found to be suitable for the quantitative determination of everolimus in tablet dosage forms.

Keywords: Everolimus, Afinitor, HPLC, validation, analysis

ABSTRACT

The creation of genetic variability through the use of chemical mutagenic factors which increase the frequency of in vitro mutations to okra is not very frequently mentioned in scientific literature. This is why we have undertaken this study on the assessment of the in vitro regeneration in okra subject to the action of two chemical mutagens: Diethyl sulphate and Dimethyl sulphate. With a 0.1 ppm concentration, Diethyl sulphate had a low stimulative effect on the regeneration of okra in vitro, while this mutagen inhibited in vitro regeneration to some extent for 0.2 ppm and 2 ppm concentrations. On the other hand, the chemical mutagen Dimethyl sulphate resulted in an obvious decrease in the percentage of regenerated neoplantlet for all the three concentrations, but for the 2 ppm concentration in particular, and this negative effect was also seen in the case of the multiplication rate, through subculture. Moreover, the strongly mutagenic action of Dimethyl sulphate was also suggested by the appearance of a larger number of chromosome aberrations in the meristematic tissues of okra grown in vitro under the influence of this chemical mutagen, compared to Diethyl sulphate. Thus, in the case of okra culture in vitro, Dimethyl sulphate is a stronger mutagen compared to Diethyl sulphate and, hence, this one can be used to induce mutagenicity to okra, and any mutations may be speculated for the modern and quick improvement of this significant species, both at a nutritional and therapeutic level.

Keywords: Diethyl sulphate, Dimethyl sulphate, mutagen, okra.

ABSTRACT

Hypothyroidism is emerging as one of the global health issues. The analysis of the symptomatology of Hypothyroidism in the light of Ayurvedic principles reveals that the pathogenesis and manifestations of hypothyroidism occurs due to dysfunction of Agni. The trial drug Triphladya Guggulu, cited in Yogaratnakara for the management of Gandamala, contains Deepana, Pachana, Anulomana and Vatakapha shamaka drugs, targeting the Agni which is the main seat of pathogenesis. Pharmacognostical & Analytical study of Triphaldya Guggulu has been carried out for the evaluation of its efficacy in Hypothyrodism. On pharmacognostical study, Starch grains & fibres of Shunthi, Black debris of Maricha, Epidermal cells with Oil Globules & stone cells of Pippali, Sclerides of Haritaki & Vibhitaki, Trichoma of Vibhitaki, Tannin content of Haritaki, Fibres & silica deposition of Amalaki, Prismatic crystals & stone cells of Kanchnara were identified. Analytical study showed 10 spots at 254 nm and 11 spots at 366 nm.

Keywords: Hypothyroidism, Triphladya Guggulu, Gandamala, Pharmacognosy.

ABSTRACT

The objective of the present research work is to develop and validated analytical method for the determination of Darunavir in pure and tablet dosage form. A simple, rapid, precise, selective and accurate novel RP-HPLC method was developed and validated for separation and determination for the Darunavir in pure and tablet dosage form. Darunavir was analyzed by Zodiac C_18, (250×4.6mm, 5µ), Shimadzu LC-20AT Prominence Liquid Chromatograph and mobile phase constituted of Triethylamine buffer: Acetonitrile (60:40 v/v). The pH of the buffer was adjusted to 4.5 with diluted ortho-phosphoric acid. The flow rate of mobile phase was 1.0 mL/min and the analysis was performed using UV-Visible detector at 260nm. The Darunavir was eluted with in 6 min and retention time was showed 2.753 min. The developed assay method was validated by the guidelines of ICH Q2R1.The method was found to be linear in the drug concentration range of 20 µg/mL -100 µg/mL. The value of correlation coefficient was found to be 0.999. Method was found good percentage recovery it indicate the method is highly accurate. The method has been successfully applied for determination of Darunavir in pharmaceutical dosage form in regular quality control analysis.

Keywords: Darunavir, validation, Linearity, Accuracy and Robustness.

ABSTRACT

A simple, precise, and rapid high performance liquid chromatography (HPLC) method for the determination of ketoconazole level in human plasma using itraconazole as an internal standard (IS) was developed and validated. 0.25 ml plasma samples containing ketoconazole were mixed with 15 µg of the IS. After adding 0.25 ml acetonitrile, the mixture was vortexed for two minutes and then centrifuged for 10 minutes at 16000 rpm at room temperature. The clear supernatant was transferred into an auto-sampler vial, and 100 µl was injected into the HPLC system with a run time of 10 min. The compounds of interest were efficiently separated on 4.6 x 150 mm, Symmetry Shield ^TMRP₁₈ 5-µm steel column, using a Guard Pak pre-column module with    Radial-Pak C₁₈ 5-µm insert, and detected using Waters 2475 multi λ fluorescence detector with an the excitation and emission wavelengths set at 260 and 375 nm, respectively. The mobile phase consisted of 0.02 M potassium dihydrogen phosphate (pH = 6.0, adjusted with 0.1 M sodium hydroxide) and acetonitrile (40:60, v:v), and was delivered at a flow rate of 1.0 ml/min. No interference from blank plasma or commonly used drugs was observed; and the detection limit of ketoconazole was 0.1 µg/ml. The relationship between ketoconazole concentration in plasma and peak area ratio of ketoconazole /IS was linear (r² ≥ 0.9979) in the range of 0.1– 20 µg/ml. Intra- and inter-day coefficients of variation (CV) were ≤ 8.1%  and  ≤ 9.7%, respectively, with corresponding biases of ≤ -13% and ≤ 0.9%, respectively. Mean extraction recovery of ketoconazole and IS were ≥ 85% and 92%, respectively. Using the method, ketoconazole was found to be stable for 48 hrs at -20°C (≥ 95%) in processed samples and for 8 weeks at -20°C (100%) in unprocessed samples.

Key words: Ketoconazole, Itraconazole, Human plasma, HPL

ABSTRACT

To develop and validate a simple, precise, accurate and stability indicating UV method for estimation of faropenem sodium. UV, HPLC and many more experiment were carried out by taking single drug and also by combining with other drug. However, such type of studies was not reported. In the developed methods for analysis and stress degradation,  faropenem sodium was found to have the absorbance maxima at 300nm. Method A involved method development and validation and method B involved forced degradation study. In these methods methanol was used as a solvent. Linearity was observed in the concentration range of 10-50µg/ml. validation experiments were performed to demonstrate system suitability, specificity, precision, linearity, accuracy, robustness, LOD and LOQ as per International Conference on Harmonization guidelines. Furthermore, stability studies of faropenem sodium were carried out under acidic, alkali, oxidation and thermal degradation as per stability indicating assay methods. The result of analysis have been validated and recovery studies were carried out using a standard addition method by adding specific amount(80%,100% and 120%) and show recovery studies in range(99.34-101.24)%. The proposed method can be successfully applied for method development, validation and stability study of faropenem sodium.

ABSTRACT

Lisinopril dihydrate (LSP) primarily used in the treatment of hypertension, congestive heart failure and heart attack. Floating matrix tablets of LSP prepared with a view of prolonging gastric residence time with a controlled release mechanism to achieve improved patient compliance, least side effects, better drug therapy and all aspects of an ideal drug delivery system. Floating matrix tablets were prepared by  wet granulation technique using  varying concentrations of different grades of gel forming polymers like HPMC K100, HPMC K15, HPMC K4M with sodium bicarbonate as gas generating agent and evaluated for the physico-chemical parameters, floating lag time, total floating time, in vitro dissolution study and swelling studies. The physico-chemical properties of all the formulations were found to be within the prescribed official limits. FTIR study reveals that there was no interaction between drug and excipients. The amount of drug released from various FDDS formulations was found to be in the order of HPMC K100M > HPMC K15M > HPMC K4M. From among all the formulations, the formulation LF-9 with 30% HPMC K15M showed the best result in terms of the required lag time (82±5 sec) and floating duration of 12 h and releasing 99.5% of the drug in 12 h and is considered as the ideal formulation. The dosage form can control the release, avoid dose dumping and extend the duration of action of a drug with prolonged floating time.

Keywords: Lisinopril Dihydrate, Floating matrix tablet, HPMC K100, HPMC K15, HPMC K4M

ABSTRACT

Indian medicinal plants are gaining popularity in treating several diseases. Due to the plants availability and less side effects people are showing more interest in Indian medicinal plants than other source of medications. The current review is a latest and wide-ranging analysis of ethnomedical information, pharmacological uses and phytoconstituents of Bougainvillea glabra. Traditionally, the plant is conveyed for the management of helminthiasis, diabetes and respiratory tract illnesses such as cough, cold & bronchitis. It has been proved several pharmacological activities like analgesic, antipyretic, anti-inflammatory, antibacterial, antidiabetic, antiulcer, antidiarrhoea and antilipidemic. Major phytoconstituents like terpenoid, carbohydrate, fatty acids and flavonoids have been reported in this plant. This helps in supporting the plant for future studies and uses on different disorders faced due to various reasons. Further investigation and research is still required for the plant to explore various medicinal properties.

Keywords:  Bougainvillea glabra, medicinal properties, phytoconstituents, antibacterial activity, uses.  

ABSTRACT

A novel tridentate chelating ligand, (2Z,2Z)-3,3-dimethyl-2-(2-(2-oxoindolin-3-ylidene)hydrazono)butanoic acid and its Co(II), Ni(II), Cu(II) and Zn(II) complexes were synthesized and characterized by elemental analyses, spectral (vibrational, electronic, ¹H NMR, ¹³C NMR and mass) and thermal studies. The interaction of ligand and complexes with calf-thymus DNA (CT-DNA) has been extensively studied using absorption, emission, viscosity and thermal denaturation studies with E. coli DNA. The DNA cleavage ability of ligand and metal complexes were tested using plasmid pBR322 DNA by gel electrophoresis method.

Keywords: Isatin; Pyruvic acid; Transition Metal Complexes; DNA Binding and Cleavage Studies.

ABSTRACT

A convenient two-step method for the preparation of β³-amino acids is described.  This paper describes an efficient and straightforward two-step synthetic sequence leading in excellent yields to a relatively inaccessible lipophilic β³-amino acids with antimicrobial potential  from easily available starting materials. Schmidt reaction of substituted piperidin-4-ones with HN₃ generated in situ afforded the corresponding diazapinones. Acid hydrolysis of chosen diazapinones yielded β³-amino acids. Selective cleavage of only the lactam bond is achieved using 4N HCl-MeOH (1:1) mixture   leading to the formation of N-alkyl β³-amino acids in quantitative yields. synthesized  aminoacids are subjected to antimicrobial activity for gram positive, gram negative bacteria, fungi. compounds  3e & 3h  possess excellent antimicrobial and antifungal activity comparable to standard streptomycin and ketoconazole. Therefore obtained β³-amino acids serves as a scaffold for  synthetic  antibiotics  as they have desired structural moieties necessary for antibiotic action. Further refinement of  the β³-amino acids  using  either conjugation or structural modification or incorporation of these aminoacids into synthetic peptides would bring about excellent antimicrobial activity.

Keywords: Mannich reaction, Piperidin-4-ones, Schmidt reaction, Diazapinone, Acid hydrolysis, β-amino acids

ABSTRACT

The solution studies the proton – ligand stability constant pK and metal ligand stability constants logk of binary (1:1) complexes of Cu(II), Co(II), Cd(II) and Ni(II)  with substituted thiocarbamido phenols have been studied at 0.1 M ionic strength in  70% ethanol-water mixture by Bjerrum method as adopted by Calvin and Wilson. It is observed that Cu(II), Co(II), Cd(II) and Ni(II) metal ions form 1:1 and 1:2 complexes with ligands (L1 & L3). The information acquired was used to estimate and compare the values of proton –ligand stability constant (pK) and metal-ligand stability constants (logk). The effects of substituents were studied from the evaluated information (pK and logk).

Keywords : Substituted thiocarbamidophenols, stability constant, pH-metry

ABSTRACT

A simple, specific, accurate, precise and sensitive RP- HPLC method has been developed for the rapid estimation of Ganciclovir in bulk and its formulations. The chromatographic separation was carried on Grace smart RP-18 column (250 x 4.6 mm, 5 μm), using Methanol: Citrate buffer (0.05M) at PH-5.2 with KOH 70:30 (v/v) as mobile phase, at a flow rate of 1.0 ml/min.  The detection was carried out at 254 nm and drug eluted with a retention time of 2.982 min. Beer’s law was obeyed in the concentration range of 10-60μg/ml with correlation coefficient 0.999. The method has been validated according to ICH guidelines for specificity, linearity, accuracy, precision, robustness, ruggedness, LOD and LOQ. The method was found to be specific, accurate, and precise, robust, rugged and sensitive. The developed method was good linearity, novel, rapid for the estimation of Ganciclovir in bulk and capsule dosage form. Thus it can be employed for the routine analysis.

Keywords: Ganciclovir , RP-HPLC, Validation, Citrate buffer.

ABSTRACT

To describe the various adverse donor reactions and determine the frequency of their occurrence in whole blood donors.  A retrospective review of all the no of donor Reactions reports of 19 blood banks of Kerala from 01/01/2014 to 31/12/2015 was done. The total number of donations were 246092(94.34%) and the Donors rejected were 14752(5.66%) 1174(0.48%) had an adverse reaction of which 999(0.41%) were vasovagal related and 175(0.07%) were needle injuries. Donor safety is an essential prerequisite to increase voluntary blood donation. AE analysis helps in identifying the blood donors at risk of AE, applying appropriate motivational strategies, pre-donation counseling, care during and after donation, developing guidelines and hemovigilance programme in countries with limited resources. Strict adherence to the rules is essential to ensure donor safety.  Also  it would have detrimental effects on return of donors for subsequent donations and rate of complications resulting in long-term morbidity and disablement is not negligible.

Keywords: Blood Donors, Blood Donations, Adverse Reactions

ABSTRACT

An accurate, precise and sensitive HPLC system is used to determination of Lidocaine-HCl in vial dosage form as parenteral solution (intra-muscular), to compare with two Lidocaine-HCl form; commercial formulations and standard Lidocaine-HCl high purity as a test formulation. Lidocaine-HCl concentrations were analyzed by a HPLC-UV System (λ = 254 nm) at 25 ^o C. The separation was achieved using the Ion Pac Ercus C18 RP-Column; 5µm, (250×4.5 mm id). The mobile phase consisted of acetonitrile/ water (20/80) with 5% acetic acid at pH 3.4. The method was found to be linearity in the range (0.1 to 0.5) µg/ml (n = 5) with R² ≥ 0.9987, also, the recoveries were range within 96.0-100%. The detection limit of quantification (LLOQ) was 0.01645 µg/ml and lower limit of detection (LLOD) 0.00521 µg/ml. showing average intra assay and inter-assay coefficients of ± RSD % about 0.526 %. The standard Lidocaine-HCl drug eluted at a flow rate of 1.0 ml/min. The results of recoveries, ± RSD, and statistical parameters obtained in this study, clearly indicated that the HPLC–UV system offer a successfully and excellent method for the separation and determination of Lidocaine-HCl in the commercial drugs.      

Keywords: Lidocaine-HCl as parenteral solution (intra-muscular) and Standardized, HPLC- UV System.   

ABSTRACT

Bilayer mucoadhesive buccal patches of lamotrigine were prepared by solvent casting technique using different polymers like PVA, PVP K30, pullulan, carbopol and HPMC 5cps. These formulations were prepared and evaluated for various parameters like weight variation, visual inspection, content uniformity, surface pH, bioadhesive strength, in-vitro and ex-vivo diffusion studies. It was found that F3 (PVA 3% and PVP K30 2%) and F4 (PVA 4% and PVP K30 1%) formulations showed good physical, mechanical properties and sustained drug release profile of about 85% and 80% in 8 hours. The formulation was found to follow zero order model dependent kinetics with Fickian diffusion. Ex-vivo diffusion studies were conducted using Franz diffusion cell. Ex vivo diffusion studies were conducted using goat buccal mucosa. The formulations containing PVA and PVP K30 in 3:2 and 4:1 ratio and 10% of PG as a plasticizer was found to be optimized which showed 66% and 60% of drug release in 8 hours. These formulations have shown bioadhesive strength of 0.06N and 0.09N and good bioadhesion time up to 6-7 hours respectively. These formulations were found to be zero order model dependent kinetics with anomalous transport as release mechanism. Lag time, cumulative amount permeated/area, flux and permeability coefficient for optimized formulations were found to be 30 & 40 min, 1336 & 1212 µg/cm², 2.18 &  2.24 µg/cm²/min and 639x10^-4 & 904x10^-4 cm/min respectively.

Key words: Mucoadhesive patches, lamotrigine patches, bilayered patches, diffusion studies.

ABSTRACT

The studies were intended to investigate the possible antihyperlipidemic effect of tulsi and cinnamon oil in high cholesterol diet induced hyperlipidemic rats. Tulsi and cinnamon oil were evaluated for antihyperlipidemic activity using high cholesterol diet induced hyperlipidemia model in male Wistar albino rats(200-250g). A comparison was also made between the action of tulsi(0.5 mg/kg b.w) and cinnamon oil extracts(1.8mg/200g b.w) and antihyperlipidemic drug atorvastatin (0.18mg/200g). Parameters assessed were body weight, total cholesterol, triglyceride, HDL-C, LDL-C.  The results of the study are represented by mean ± SEM. Statistical significance of data was assessed by one way analysis of variance (ANOVA) followed by a comparison between different groups using “Tukey - Kramer” test. Oral administration of 0.5 mg/kg of tulsi oil with dist. water and Cinnamon oil of 1.8 mg/200g suspended in tween80 solution exhibited significant reduction (p ˂ 0.01) in serum biochemical parameters total cholesterol, triglycerides, low density lipoprotein (LDL), very low density lipoprotein (VLDL)  and increase in high density lipoprotein (HDL) levels in hyperlipidemic rats of HC diet model  compared to hyperlipidemic positive control. The results demonstrated that tulsi and cinnamon oil extracts possessed significant antihyperlipidemic activity.

Keywords: Tulsi oil, Cinnamon oil, Atorvastatin, High cholesterol diet, Hyperlipidemia.

ABSTRACT

Herbal medicines are generally available as a mixture of more than one plant constituent. It is important to quantify the maximum possible number of markers in such herbal formulations by which the quality of the formulations may be assessed. TLC densitometric methods were developed using High performance thin layer chromatography for the quantification of the three marker compounds, umbelliferone, β-sitosterol and methoxsalen, from the polyherbal tablet formulation. Solvent systems were optimized to achieve best resolution of the marker compounds from the other components of the sample.  From the various solvent systems tried, the one containing toluene: ethyl acetate: methanol: formic acid (3: 3: 0.2: 0.8) gave best resolution of umbelliferone (R_f=0.35), β-sitosterol (R_f=0.47) and methoxsalen (R_f=0.6) in the presence of the other compounds in the polyherbal tablet sample and enabled the quantification of the marker compounds. The methods were validated in terms of precision, repeatability and accuracy. The method was found to be suitable for the quantification of these marker compounds in polyherbal formulation.

Keywords: densitometric, umbelliferone, β-sitosterol and methoxsalen.

ABSTRACT

To evaluate the obstetrical complications and neonatal outcome of teenage pregnancies in comparison with older group. This study was carried out in Al Sader teaching  hospital in misan city in  2015.This study included 100 primigravida women aged 10-19 year as a case group & 100 primigravida women aged 20-25 year as a control group admitted to labour ward during the period of study, all women received  standard labour management including history & complete general & obstetric examination. Both groups were compared for the presence of any pregnancy complication & the mode of delivery, Neonatal outcome. Excel 2010 is used for statistical analysis teenage pregnancy accounts for 15% of the total pregnancies. In adolescent age group most of the pregnancies occur between 16-19 years (41%) & (2%) for those aged <15 years. The adolescent employers are lesser than the employers of control group (5% vs. 11%). Higher maternal & neonatal complications in case group compared with control group and as follows :preterm 6% vs. 2% , anemia 21% vs. 7%, LBW 9% vs. 4% , admission to NICU 15% vs. 6% .

ABSTRACT

The present study describes screening for antimicrobial and anthelmintic activity of the petroleum ether and alcoholic extracts of Corchorus depressus Linn. (Tiliaceae). The plant has been used in the traditional Indian system of medicine as an antibacterial, antifungal and anthelmintic drug, as a tonic, cooling medicine in fevers; its mucilage is prescribed in gonorrhea. Root is rubbed on stone and smeared over forehead to get relief in migraine; extract of plant is applied as a paste in healing of wounds. The HPLC chromatograms of the methanolic extract shows a single large peak with a retention time 6.451 min along with other components.  The Anthelmintic activity was studied on adult Indian earthworms, ‘Pheretima posithuma’. The methanolic extract produced more significant Anthelmintic activity than petroleum ether extract and the activities are comparable with the reference drug Piperazine citrate. The methanolic whole plant extract exhibited significant anti bacterial, antifungal activity, comparable to the standard drug tetracycline. The present study confirms the folklore claim of the plant utilized for its antimicrobial activity

Keywords: Antimicrobial; Anthelmintic; HPLC; Tetracycline; Piperazine citrate.

ABSTRACT

Present report is the successful synthesis, spectral characterization and in-vitro antimicrobial evaluation of a series of azomethine and novel 2-azetidinone derivatives. Two cyanoethylated tertiaryaminobezaldehydes A and B were prepared by cyanoethylation of the corresponding aromatic primary amines followed by formylation in presence of POCl₃ and DMF. These cyanoethylated tertiaryaminobenzaldehydes on condensation with different aromatic primary amines afforded azomethines SB1-SB14, which on cyclization with chloroacetylchloride and triethylamines in 1,4-dioxan gave new 2-azetidinone BL1-BL14. All compounds were prepared by reported methodology and characterized by elemental analysis, FT-IR and ¹HNMR data. Further screened in-vitro for antimicrobial activity against S. aureus, B. subtilis, P. vulgaris, E. coli, A. niger and A. fumigatus. Most of the compounds showed significant activity against tested pathogens. The work shows the emergence of a new series of compounds in the field of antimicrobials.

Keywords: 2-Azetidinones, azomethines, antimicrobial activity, cyanoethylation, formylation, tertiaryaminobenzaldehydes.

ABSTRACT

P. integrifolia Synonym(s): Premna serratifolia L . (Verbenaceae)  deciduous shrub a member of Brihatpanchamula groups of dashmula, known as Agni-manth, in Sanskrit; malbau in Malaysia, Common beach plant distributed along the coasts and islands of tropical and subtropical Asia, Africa, Australia and the Pacific. It contains sterols,  flavonoids apigenin, luteolin and alkaloids- Premnine, Ganiarine and Ganikarine.. Advances in microscope technology like Scanning Electron Microscope have increased the accuracy and capabilities of microscopy as a mean of botanical identification. The objective of this work to provide set of SEM histological characters that may serve as standard for identification. That helps for establishment of botanical biomarkers based on the major microscopic features observed in P.integrifolia stem. Secondly physicochemical parameter like moisture content, ash value, extractive value, crude fibre content were evaluated. Phytochemical screening of extracts PI-AK (chloroform extract of P.integrifolia) and PI-ET(Ethyl acetate  extract of P.integrifolia)  were performed. HPTLC fingerprinting of PI-ET extract marked qualitatively with Apigenin and Luteolin simultaneously as standard at Rf 0.39 and 0.29 respectively in mobile phase Toluene: Ethyl acetate :Formic acid (6:4:0.15),scanned at 367nm. Premnine HCl was used for biomarker for fingerprinting of PI-AK extract at Rf 0.59 at 283nm.  Stability of PI-ET in solution and over plate with time was checked shows persistent chromatogram. Stability during chromatography checked with 2D chromatogram shows all zone in diagonal line. This research work focused for Apigenin , Luteolin bioflavonoid   and Premnine HCl alkaloid  as biomarker for standardization of  P.integrifolia  as one of ‘Dashmul’.

Keywords:  Premna integrifolia, Apigenin , Luteolin, Dashmula, , Premnine HCl

ABSTRACT

New Chemical Entities (NCEs) were designed using information from pharmacophore profile of known anticonvulsants. Binding affinities of designed NCEs were studied on gamma-aminobutyric acid (GABA-alpha) using docking studies. Two Dimensional (2D) Quantitative Structure–Activity Relationship (QSAR) studies were performed for correlating the chemical composition of triazolethione analogs and estimation of their anticonvulsant activity using Multiple Linear Regression (MLR) Analysis.  ADMET properties were also predicted. These four basic strategies (pharmacophore mapping, QSAR, docking & ADMET screening) were implemented to evaluate the performance of derivatives. Although predicted Ki through QSAR model showed significant mild activity for GABA. Conclusively compounds, 2, 6, 7, 8, 9, 10, 11, and 20 were observed to be most feasible to activate GABA for anticonvulsant activity.

Keywords: ADMET; Anticonvulsant; Docking; Epilepsy; GABA; Pharmacophore; QSAR; Triazolethione.

ABSTRACT

The use of different solvents to extract plant materials is to obtain component of utmost activity for the management of various disease conditions. Cocoa powder was subjected to different menstruum (aqueous, ethanol, n-hexane and chloroform) to remove inert materials and obtain pure active components whose effect was determined. Diabetes was induced in forty female Albino rats divided randomly into five groups, each consisting of eight rats, using 120mg/kg body weight alloxan. Different extracts of the powder were administered orally for twenty one days at a dose of 200mg/kg each except in the diabetic untreated group. Fasting blood sample was collected from the tail vein daily to determine the blood glucose concentration. On 22^nd day, fasting blood samples were collected from all the rats for lipid profile estimation. Results showed a significant decrease (P<0.05) in the blood glucose level in ethanol extract-treated diabetic group compared with the others and a decrease in plasma TC, TG, and LDL-C in the extract-treated groups when compared with the diabetic untreated group. The reduction in lipid profile was significant (p<0.05) in ethanol extract when compared to other extracts. Conclusively ethanol extract of cocoa powder exhibited significant antihyperglycemia, hypolipodemia, and reduction in LDL-C.

Key words: Cocoa powder, diabetes mellitus, blood glucose, lipid profile, atherogenic index.

ABSTRACT

Sleep-disordered breathing (SDB) was first described in the medical literature in 1936.Obstructive sleep apnoea/hypopnoea syndrome (OSAHS) is the most common type of SDB, affecting 4% of men and 2% of women aged 30–65 years with a total population prevalence of 1–2%.There are many associations between cardiovascular diseases and sleep disordered breathing (SDB).The objective of the study is to determine the prevalence, risk factors, and severity for sleep disordered breathing in patients with cardiac disorders. A Prospective, Observational, Comparative Study on the Relationship between Sleep Disordered Breathing [SDB] and Cardiac Disorders was conducted in the Cardiology Department of a hospital in Coimbatore. The data was collected during ward rounds and severity of SDB measured with the help of two questionnaires: Epworth Sleepiness Scale and Stop-Bang questionnaire. A total of 93 cases with various cardiac disorders were analyzed. The results indicated that males (69.8%) were predominantly more than females (30.1%) in the study. The study shows that (31.1%) patients were observed with Ischemic Heart Disease condition, (31.1%) patients with Ischemic Heart Disease/Systemic Hypertension, (10.7%) patients had Systemic Hypertension as major diagnosis. Assessment using Epworth scale shows that (30.1%) patients had moderate risk, (27.9%) patients with severe risk and (24.7%) were having mild risk. Assessment using Stop- Bang shows that (49.4%) had intermediate risk, followed by (32.2%) patients with high risk and (18.2%) with low risk. The results demonstrated an increased risk for sleep disordered breathing in cardiac disorders.

Keywords: OSAHS, SDB, Stop-Bang Questionnaire, Epworth Sleepiness Scale

ABSTRACT

In this study, in vitro antimicrobial activity of Polyherbal cream comprising of various plant herb extracts of leaves viz. Aloe barbadensis, Calendula officinalis, Lawsonia inermis, Carica Papaya and Azadirachta indica along with tridax procumbens as a key Plant was evaluated. Polyherbal formulations (F1 & F2) were designed and developed as ointment based semisolid cream. Disc diffusion method and agar well diffusion method were used for in vitro antibacterial and antifungal screening for both the formulations. Zone of inhibition were observed as a measure of investigation. The Formulation-1 (F1) showed efficient zone of inhibition at concentration of 4% than the formulation-2 (F2) at lower concentration 2% of tridax procumbens. In antifungal screening, the compound showed significant zones of inhibition against tested fungi.

Keywords: Antimicrobial activity, Antifungal activity, Polyherbal cream.

ABSTRACT

A simple, sensitive, selective and rugged liquid chromatography coupled with mass spectrometry (LC/MS/MS) method for quantification of Diltiazem and its metabolites, N-desmethyl Diltiazem, desacetyl Diltiazem in human plasma was developed and validated. The chromatography was developed using Luna 5 μ, C18, 100×4.60 mm column having a mobile phase of Acetonitrile: 0.1 % formic acid (85:15 % v/v). The flow rate was 0.5 ml/min at a column temperature of 50 ± 5º C. Electron spray ionization technique in positive mode was selected to improve the selectivity and sensitivity required for this application. The retention times of Diltiazem, desmethyl Diltiazem, desacetyl Diltiazem were 2.5, 2.0 and 2.5 minutes respectively. The method was validated for linearity, precision, accuracy, specificity, sensitivity, matrix effect, dilution integrity, ruggedness, injection reproducibility and stability. Calibration curves during the course of validation were found to be linear for Diltiazem, desmethyl Diltiazem, desacetyl Diltiazem in the ranges of 0.604-603.902, 0.303-303.274 and 0.299-299.489 ng/mL with correlation coefficient ≥ 0.9969, 0.9958 and 0.9970 respectively and by using a 1/x2 weighted least square regression analysis of standard plots associated with ten point calibration standards. The precision and mean accuracy were within the acceptable limits.  

Keywords: Diltiazem; desmethyl Diltiazem, desacetyl Diltiazem; LC/MS/MS; Validation.

ABSTRACT

A new, simple, accurate and sensitive method was developed for the quantification of two potential genotoxic impurities 1-(2-methyl-5-nitro-phenyl)guanidine nitrate and  N-(2-methyl-5-nitro-phenyl)-4-(3-pyridyl)pyrimidin-2-amine at low level (2 ppm) in Imatinib using liquid chromatographic mass spectrometry. The chromatographic separation was achieved on Kromasil 100-3.5-C18 (150 x 2.1) mm column with gradient programme and elution was monitored by mass spectrometer in selective ion monitoring mode using electrospray ionization. The LOD and LOQ values found to be 0.2 ppm and 0.6 ppm for both the impurities with respect to the test concentration 5 mg/ml. The method was linear (r²>0.99), precise (RSD<2%), accurate and well within acceptable ICH limits.

Keywords: Potential genotoxic impurities, Imatinib, LC-MS, Selective Ion Monitoring (SIM), Threshold of Toxicological Concern (TTC)

ABSTRACT

The genus Euphorbia is unique, which covers highly reputed medicinal plants useful in various treatment of diseases like asthma, bronchitis, hay fever, cancer and inflammation. The present study includes comparative pharmacognostic and phytochemical standardization of aerial parts of two Euphorbia species i.e. E. hirta L. and E. thymifolia L. The comparisons of both species were carried out by various standardization parameters such as macroscopy, microscopy, powder study, leaf constant, physicochemical analysis, mineral content, qualitative and quantitative phytochemical screening and TLC study. The results of the present study showed various distinguished characters in two species which could serve as an indicator for authentification and identification of E. hirta and E. thymifolia based on their standardization parameters.

Keywords: Euphorbia hirta, Euphorbia thymifolia, pharmacognostic, phytochemical and standardization.

ABSTRACT

Objective of this research work was to employ advanced analyzing technique like ICP-OES in evaluating the potassium content of the entire plantain fruit. Often the skin part of the fruit is removed before using it. The analysis revealed that the potassium content of plantain (Musa paradisiaca) is much (800 mg/gm) more than it was believed (400 mg/gm) to have. Though the skin part of the fruit constitutes only 10-15 %, almost 50 % of potassium content comprised in the skin. (Around 1500mg/gm Potassium in together with peel and pulp). .Effect of different cooking methods of ripe and raw are also evaluated. Heavy Potassium loss, approximately 50 %, observed in boiling and 15-20 % Potassium loss observed in steaming. The findings of this work can be incorporated in formulating a proper diet for patients with hypokalemia and hyperkalemia Advanced ICP-OES methods for elemental analysis increases the specificity and sensitivity of the results.

Keywords: ICP-OES, potassium content, Musa paradisiaca, hypokalemia, hyperkalemia

ABSTRACT

The main objective of this study was to perform pharmacological evaluation of Stay-On Power Capsules in Rats namely the aphrodisiac activity. The present investigation deals with Pharmacological Studies (Mating behaviour study, mating performance test, Hormonal analysis, Reproductive organ and spermal analysis) of Stay-On Power Capsules in Rats administered orally by gavage to rats in accordance with the schedule Y of drugs and Cosmetic Act (2005). The acute toxicity study of Stay-On Power Capsules was done by up and down method. After the completion of acute toxicity studies, three different doses were selected for aphrodisiac activity such as 150, 300, and 600 mg/kg. Volume of oral administration was 1 ml/100 g of animals. Animals were randomly divided into five groups with six animals per group. Group I represented the control animals treated with normal water only; Groups II, III, and IV were treated with oral suspension of Stay-On Power Capsules at 18:00 h, at doses of 150, 300, and 600 mg/kg, respectively; and Group V served as a positive control treated with Sildenafil citrate of 5 mg/kg body weight. All the treatments were continued for 3 weeks only. Daily administration of Stay-On Power Capsules for 3 weeks to male rats resulted in a dose dependent increase in the mating performance as compared to the control group. The Stay-On Power Capsules at the dose of 150, 300, and 600 mg/kg showed 52.66%, 63.83%, 71% mating performance, respectively, against 38.33% of the control group, whereas the standard showed 79.66% mating performance. The Stay-On Power Capsules had significantly increasing (**P < 0.01) effect on testosterone, LH, and FSH concentration in the serum in comparison to the control group. Oral administration of Stay-On Power Capsules for 3 weeks has been found to be relatively safe and effective in Mating behaviour study, mating performance test, Hormonal analysis, Reproductive organ and spermal analysis in rats.

Keywords: Mating behaviour study, mating performance test, Hormonal analysis, Reproductive organ and spermal analysis

ABSTRACT

A simple reverse phase specific and selective high performance liquid chromatographic method for determination of Exemestane in Exemestane tablets has been developed and validated with Isocratic elution and UV detection. Chromatographic separation was achieved by using Hypersil, C-18, 150 X 4.6mm, 5µ column with a mixture of Acetonitrile and Purified water in the ratio of 35:65, filter and degas the mobile phase same is used as diluent. Detection was at 249 nm. By this method all known and unknown Impurity & Degradation products are well separated from Exemestane main peak.  Peak purity factor for Exemestane peak is not less than 99.0%. Both the Precision (System Precision, Method Precision, Intermediate Precision) and Linearity were within acceptable range. Response was a linear function between concentration and area of peak over the   range from 50% to 150% of assay concentration for Exemestane. It can be concluded that the Exemestane Peak is found to be degraded more in acid, alkali and peroxide stress condition. Exemestane Peak purity factor was more than 99.0% and all degradation product formed were well separated from Exemestane Peak. By this it was found that this method is robust and system suitability test was established and related parameters are recorded. This method is validated hence this method can be used for routine analysis of stability sample.

Keywords: High performance liquid chromatography, Exemestane, stability, Precision and peak purity.

ABSTRACT

In the present investigation efforts were made to develop Misoprostal loaded microspheres to obtain a desirable drug release profile by Ionic gelation method using hydrophilic polymers and cross linking agent to decrease the gastric irritation and to enhance the drug penetration. Microspheres were prepared by using sodium alginate and calcium chloride in different ratios.  All the microspheres were evaluated for particle size, percentage yield, drug entrapment efficiency, stability studies and for in vitro release kinetics and found to be within the limits. Among all the formulations S7 was selected as optimized formulation based on the physico chemical properties and drug release studies. In vitro drug release study of formulation S7 showed 97.17% drug release up to 12h in a controlled manner, which is essential for an anti ulcer therapy. The innovator Misoprostal marketed product shows the drug release of 95.23 in 1 h. The drug release of optimized formulation S7 followed zero order release and Higuchi kinetics indicating diffusion controlled drug release. FT- IR study showed no drug excipient interaction takes place.

Keywords: Misoprostol, sodium alginate, microspheres, scanning electron microscopy, release order kinetics.

ABSTRACT

In India, many indigenous plants are used in herbal medicine to cure diseases and heal injuries. Major pharmaceutical companies are currently conducting extensive research on plant materials gathered from the rain forests and other places for their potential medicinal value. Toddalia asiatica (L.) Lam. (Rutaceae) is widely used as a folk medicine in India. The roots are used in the treatment of indigestion and influenza and the leaves to treat lung diseases and rheumatism. The root and its bark have been used to treat fever, malaria, cholera, diarrhoea and rheumatism ¹. Despite the use of this plant for such purposes, there is little information on the biochemical composition of Toddalia asiatica.  L.Var . floribunda.. This work is therefore aimed at documenting the biochemical compositions of Toddalia asiatica. L. Var . floribunda. From the earlier reports qualitative phytochemical results reveals that the methanolic stem extract of Toddalia asiatica.L. contain secondary metabolites like  Alkaloids, Flavonoids, Saponins, Steroids, Glycosides, Tannins. From the quantification result of various biochemical and phytochemical constituents like carbohydrates, proteins, total ascorbic acid, phenols, tannins and flavanoids content, it was noted that alkaloid found to be the highest with phenol as the next active constituents among the secondary metabolites in the stem. From the results it reveals Toddalia asiatica has the potential to be represented as an effective biochemical and therapeutic constituent for the future use in the medical field.

Keywords:  Toddalia asiatica, ascorbic acid, alkaloids, phenols, tannins, flavanoids.

ABSTRACT

A reverse phase HPLC method is developed for the determination of Azilsartan medoximil and chlorthalidone in pharmaceutical dosage forms. Chromatography was carried out on a C₁₈ column 4.6 x 100mm, 5µm, Make: BDS using a mixture of potassium Di hydrogen ortho phosphate buffer and acetonitrile (35:65 v/v) as the mobile phase at a flow rate of 1.0 ml/min. Detection was carried out at 273 nm . The retention time of Azilsartan Medoxomil and Chlorthalidone was 2.59±0.1 mins and 3.85±0.5 min respectively. The linearity was observed In range of 2.5-15 µg/ml and 10-60 µg/ml with a correlation coefficient of Azilsartan medoximil and chlorthalidone were 0.996 and 0.999.the proposed method was validated for its linearity, accuracy, precision and robustness. The proposed method was found to be simple, rapid, accurate and precise. It was found to be economical and suitable for simultaneous determination of Azilsartan Medoxomil and Chlorthalidone in pharmaceutical dosage form.

Keywords: HPLC, Azilsartan medoximil and Chlorthalidone, Estimation, Tablets.

ABSTRACT

The aim of the present study was to evaluate the effect of Chromolaena odorata (C.odorata) and Boerhavia erecta (B.erecta) on lipid peroxidation and antioxidants in Lead acetate-induced Nephrotoxicity in male Wistar rats. The rats of the nephrotoxicity control group 2 were administered lead-acetate 10mg/kg body weight, intraperitoneally in 3 days once for 15 days. In nephrotoxicity rats, Oral treatment with C.odorata, B.erecta at a daily dose of (500 mg/kg b.wt) and silymarin (25 mg/kg b.wt) groups (3, 4 and 5) for last 15 days. The Lead-acetate-induced rats showed increase in the level of lipid peroxidation and decreased levels of superoxide dismutase, catalase, glutathione peroxidase and reduced glutathione in serum and kidney. Oral treatment with C.odorata, B.erecta and silymarin in nephrotoxicity induced rats showed significantly decrease in the levels of kidney and serum lipid peroxidation and significant (p<0.05) increase in the levels of superoxide dismutase, catalase, glutathione peroxidise and reduced glutathione in kidney and serum. The study results revealed that C.odorata, B.erecta ameliorates kidney damage in lead-acetate induced nephrotoxicity, by maintaining lipid peroxidation and antioxidants levels by its free radical scavenging effects on lead-acetate induced nephrotoxicity rats.

Keywords: Lipid peroxidation, antioxidants, Chromolaena odorata , Boerhavia erecta.

ABSTRACT

“Non-conventional” synthetic method has shown broad applications as a very efficient way to accelerate the course of many organic reactions, producing high yields, higher selectivity and lower quantities of side products consequently easier work-up and purification of the products.  One-pot two-component condensation of 1-formamidino-5-ethylformamidonothicarbamide (llla) with various isocyano-dichlorides(Xla-g) were carried out in presence of lemon juice as a biocatalyst respectively to synthesize a novel series of 2-substitutedimino-4-amino-6-ethylformamidino-1,3,5-thiadiazines (Xlla-g) which are neither to unknown. The structures were confirmed by conventional chemical characterization, elemental analysis and spectral studies.  

Keywords: Lemon Juice, various isocyanodichlorides, 1-formamidino-5-ethylformamidonothicarbamide

ABSTRACT

A simple, selective, linear, precise and accurate HPLC method was developed and validated for rapid assay of Oxazepam in Bulk and Pharmaceutical tablet Formulation. Isocratic elution at a flow rate of 1.0 ml/min was employed.  The chromatographic analysis was performed on a ODS 5 μm (4.6 mm x 15 cm) or equivalent column at ambient temperature. The mobile phase consisted of Methanol: Water in the ratio of 65:35v/v. The UV detection wavelength was 230nm and 100µl sample was injected. Flow rate was found to be 1.0.  The retention time for Oxazepam was identified. The Average percentage recovery of the method was in the range of 0.5.  The method was validated as per the ICH guidelines. The method was successfully applied for routine quality control analysis of pharmaceutical formulation.

Keywords: Oxazepam, HPLC, UV detection, Recovery, Precise.

ABSTRACT

A Quantitative High Performance Thin Layer Chromatography (QHPTLC) method was developed for the estimation of ‘Candana’ (Santalum album), one of the herbal ingredients present in the Ayurvedic polyherbal formulation ‘Padoladi Ghritham’. For this, both the methanol extracts of ‘Candana’ crude drug and Padoladi Ghritham were run using a mobile phase Chloroform : Isopropyl alcohol : Toluene (8:1:1, v/v/v) on a silica G 60 F₂₅₄ stationary phase. Methanol extract of Candana  gave a spot with R_f value of 0.76. The methanol extract of Padoladi Ghritham also gave a spot with R_f value of 0.76. The chemical equivalency of these two spots was revealed by the same pattern of the UV spectrum with a λ_max of 290 nm. Then the estimation was done graphically by preparing Quarter Standard, Half Standard, Normal Standard, and Double Standard of the formulation. A calibration plot was drawn between the concentration of standards and peak area of the reference spots. The concentration of Candana in the samples was found from the corresponding AUC obtained for the reference peak of the samples. A regression coefficient of 0.989 was obtained. The developed QHPTLC method is a simple and accurate one and can be used as a tool for the quantification of each ingredient in a polyherbal formulation.

Keywords: QHPTLC, Santalum album, Padoladi Ghritham, AUC, Regression Coefficient.

ABSTRACT

Infections caused by protozoa of the genus Leishmania are a major worldwide health problem with high morbidity and mortality in developing countries especially Sudan. The incidence of the disease has amplified since the emergence of AIDS. Since the discovery of the first drugs for Leishmaniasis treatment (i.e., pentavalent antimonials), up to now the search for substances with antileishmanial activity, without toxic effects, and able to overcome the emergence of drug-resistant strains still remains as the current goal. Moreover, in the absence of a vaccine there is a crucial need for effective drugs to replace/supplement those in current use. The plant kingdom is undeniably treasured as a source of new medicinal agents.   A thorough review of the literature on Sudanese plant extracts of natural origin either showing antileishmanial activity or expected to have, depending on the phytochemical screening is presented in this article. The review include 12 plants, their geographical distribution, the parts utilized, the type of extract, and the organism tested. The level of activity exhibited by the extracts depended largely on the type of solvent used for the extraction and the plant part used. Tannins demonstrated to be the key element of the antileishmanial properties and it is highlighted as potential source through the search for new Sudanese antileishmanial medicinal plants. The array of Sudanese medicinal plants that have demonstrated antileishmanial activity suggests that the hope to discover novel antileishmanial drugs is high.

Keywords: Leishmania, Sudanese medicinal plants, Tannins

ABSTRACT

Liquisolid technique is a new approach for delivery of drugs through oral cavity. This technique is suitable for poorly or water insoluble drugs and also for immediate or sustained release formulations. The technique is based upon the admixture of drug loaded solutions or liquid drug with appropriate carrier and coating materials to convert into acceptably flowing and compressible powder. The selection of non-toxic hydrophilic solvent, carrier, coating excipients and its ratios are independent of the individual chemical entities. Indirectly its leads to enhancement of bioavailibity. Liquisolid tablet of drug Tacrolimus were prepared by using PG, PEG 200, PEG 400, glycerin, Tween 80 and Span 80, as non volatile liquid vehicle, respectively. Tacrolimus is an immunosuppressive drug, which have poor water solubility and low bioavailability, so it is suitable for liquisolid technique. Also Tacrolimus is having daily dose 5-10 mg once a daily. FTIR and DSC studies reveal that there was no possible interaction between drug and tablet excipients. All the formulation was evaluated for disintegration time, hardness and friability time, in-vitro dissolution study.

Keywords: Tacrolimus, Evaluation, Designed, Direct compression, Liquisolid technology.

ABSTRACT

Type 2 diabetes occurs when the body becomes resistant to insulin or doesn't make enough insulin. The major treatment approach for diabetes is the use of synthetic drugs and insulin. However the side effects associated with the use of synthetic agents attracts the attention of drug discovery professionals to search an effective treatment using natural products. Malaysian plants and herbs have been used as medicinal agents and studies have proved their significance in the treatment of diabetes.  As the fruits of Gnetum gnemon (family: Gnetacea) locally known as melinjo are traditionally used to control diabetes by Malaysian and Indonesian tribes, the present study was aimed to evaluate the folklore claim about G. gnemon fruits to treat diabetes. Hexane extract (GGHE), chloroform extract (GGCE), ethanol extract (GGEE) and water extract (GGWE) were obtained by successive extraction using soxhlet extractor. The preliminary phytochemical analysis was carried out to perceive phytoconstituents in G. gnemon extracts. Diabetes was induced in albino rats by single dose of streptozotocin (60 mg/kg b.wt. i.p.) followed by nicotinamide (120 mg/kg b.wt. i.p.). Streptozotocin-induced diabetic rats were separately treated with GGHE, GGCE, GGEE and GGWE at dose of 400 mg/kg b.wt. and standard drug, glibenclamide (10mg/kg) respectively by oral administration for 14 days and antidiabetic potential of the extracts were assessed. Prelimary phytochemical screening showed the presence of flavonoids, terpenoids, phenolic compounds and tannins. Oral administration of diabetic rats exhibited significant (P<0.001) antidiabetic activity. Various serum parameters such as glucose, triglyceride, total cholesterol, HDL, LDL, VLDL, bilirubin, total protein, urea, creatinine and uric acid were significantly (P<0.001) restored in the GGEE treated animals compared with diabetic rats and normal control. Histological study supported the protective effect of G. gnemon on pancreas in GGEE treated animals. The results illustrate G. gnemon to be a promising alternative for diabetes mellitus management, thus supporting its folklore claim.

Keywords: Gnetum gnemon fruits, diabetes, extracts, antidiabetic