ABSTRACT

The current concept of good manufacturing practices (GMP) emphasizes that the quality of pharmaceutical products should be constructed during the overall process cycle. Quality control department plays an important role in the quality-by- design (QbD) concept since it demands the acquisition of in-process reliable analytical data. Quality control department should demonstrate the quality of their results and their fitness for purpose by giving a measure of the confidence that can be placed on the results. One useful measure of this is measurement uncertainty. The present article covers the sources, reasons and evaluation of measurement uncertainty.

Keywords: Measurement uncertainty, quality by design, quality control, coverage factor, confidence level.

ABSTRACT

Sirka (vinegar) is used since thousands of years for flavouring, preserve foods and therapeutically. Vinegar is derived from the French word vin aigre, meaning “sour wine”. It is prepared with the help of an organism called Ummul khal (mother of vinegar) which play a key role in fermentation. Fermentation made from any fermentable carbohydrate source, dates, apples, grapes, sugar cane, honey, malt, grains, whey etc. In Unani medicine, the term sirka is commonly applied for Sirka angoori (vinegar of grapes) which is used both internally as well as externally due to its Saree-al-nufooz (rapidly diffusible), muhallil (resolvent), qabiz (astringent) properties in many diseases. In vinegar 4-5% of hydrogen acetate is found which is called as Jauhare Sirka. In India, the most commonly used and prepared sirka is of Aab e neeshkar (Sugarcane juice) or of Jaggery called as Sirka Qandi.

Keywords: Sirka; Vinegar; Saree-al-nufooz; Unani medicine.

ABSTRACT

Xylopia aethiopica  (Annonaceae), commonly called negro pepper, African pepper, Guinea pepper and spice tree, is an ever green aromatic tree growing up to 15-30 m high. It is a native to the low land rain forests and moist fringe forests in the savanna zones and coastal regions of Africa. Folklore medicine claimed it to be useful as abortifacients, ecbolics as well as in the treatment of diarrhoea, dysentery; stomach disorder, menstrual disorder, naso-pharyngeal infections, arthritis, rheumatism, infections, among others. This present article is a collection of up to date information regarding the ethnopharmacology, phytochemistry, Pharmacology and Toxicological studies carried on  Xylopia aethiopica by different researchers (authors).

Keywords: Xylopia aethiopica, essential oil, ethno-medicine, phytochemistry, antimicrobial, anti-infertility.

ABSTRACT

Green synthesis of nanoparticles is eye catching area of nanoscience and nanotechnology. It involve development of clean, biocompatible, non-toxic and eco-friendly methods for nanoparticles synthesis as compared to conventional method like physical and chemical which are often toxic. In the  present scenario variety of nanoparticles with well-defined chemical compositions, sizes and morphology have been synthesized using different microorganisms and their applications in various cutting-edge technological areas have been explored. This review highlights the recent developments of the biosynthesis mechanisms of different types of nanoparticles using bacteria. Nanoparticles have been used in diagnosis, treatment, drug delivery, medical device coating, wound dressings, medical textiles, contraceptive devices, anti-fungal, anti-inflammatory etc. Future prospects for synthesis of nanoparticles using bacteria have also been discussed.

Keywords: Nanotechnology, Nanoparticles, Microorganisms, Drug delivery, Diagnosis.

ABSTRACT

Biomarkers are considered as tremendous gift of modern biomedical sciences to improve the outcome for people with cancer by enhancing detection and treatment approaches.  Biomarkers could include a broad range of biochemical entities, such as nucleic acids, proteins, lipids, small metabolites, as well as whole cells or biophysical characteristics of tissues. Detection of biomarkers can be accomplished by a wide variety of methods, ranging from biochemical analysis of blood or tissue samples to biomedical imaging. The primary focus of this review article is to find out the role of biomarkers as invaluable tools for cancer; specially breast and cervical cancer detection, diagnosis, patient prognosis and treatment selection. Besides, the future trend of biomarker development for these two types of cancer is also discussed.

Keywords: Biomarker, Cervical cancer, Breast cancer, Diagnostics, HPV.

ABSTRACT

Pharmacovigilance is defined as the pharmacological science that is relating to the detection, assessment, understanding, prevention of adverse effects, particularly the long term &short term adverse effects of medicines. The Pharmacovigilance is the important and integral part of clinical research. This article describes and discusses the aims, objectives, role, need for the Pharmacovigilance, different Pharmacovigilance programme, various Pharmacovigilance methods, Pharmacovigilance reporting and functioning.

Keywords: Pharmacovigilance, adverse effects, clinical research

ABSTRACT

The major goal of any drug delivery system is to supply a therapeutic amount of drug to the target site in the body, in order to achieve desired drug concentration. Colon targeted drug delivery system involves the targeting of drug to colon and is used for the treatment of various diseases related to colon like inflammatory bowel disease, colon cancer, crohn’s diseases etc. Targeting to colon directly reduces the need of higher dose, dosing frequency, incidence of side effects and cost effective treatment can also be achieved. Colon was considered as “BLACK BOX” and generally absorption of most drugs occur in upper G.I region. Lack of digestive enzymes and delayed gastric emptying, has given the idea to design colon specific drug delivery system. This review article compares the different approaches to colon targeted drug delivery like pH and time dependent, prodrug, microbial triggered and pulsatile drug delivery system etc. Beside these different new approaches were also used for colon targeting like pressure controlled, osmotic controlled drug delivery systems are highly effective.

Keywords: colon targeted drug delivery, pH sensitive, Pressure controlled, osmotic controlled. Microbial triggered.

ABSTRACT

Poor aqueous solubility of drugs is a major limiting factor with many new drugs in their successful launch in market in spite of their potential pharmacokinetic activity. Poorly water soluble drugs are becoming a problem in terms of obtaining satisfactory dissolution within the gastro intestinal tract, which is necessary for good bioavailability. Poorly water-soluble drugs are associated with slow drug dissolution followed by slow absorption leading eventually to inadequate and variable bioavailability. Various approaches to overcome the poor aqueous solubility of drugs have been investigated like solid dispersion, spherical agglomeration, nanoparticles, nanosuspensions, nanomorphs, nanocrystals, micronization, polymorphism, co-solvency, pH adjustment, use of surfactants, microemulsion, complexation. In this article, the basic approaches for enhancement of solubility and dissolution of poorly water-soluble drugs have been reviewed with literature-based examples of the formulation options for poorly water-soluble compounds and their practical applications to the industrial practices.

Keywords: Solubility, Dissolution, Techniques.

ABSTRACT

Nanotechnology plays a major role in the medical field for treating various pathological conditions, but the field of nanoimmunology has not developed to full extent. This paper presents about the role of nanoparticle in treatment of allergy. Mast cells and peripheral blood basophils are the cells mainly responsible for allergy. When a foreign particle enters the body, the immune system is activated and they produce certain molecules (mostly immunoglobulins, IgE). Histamines are also produced by the mast cells which affect the local areas, thus, stimulating the production of immunoglobulins. This review explains how allergies can be cured by using buckminster fullerenes (buckyballs). The fullerene attaches with mast cells and basophils, and then inhibits activation of IgE receptor. However, the major disadvantage of using buckyballs is its toxicity. Fullerene molecules in water form oxygen free radicals which in turn react with the lipid molecules present in the cell membrane. The lipid molecules form free radicals which lead to rupture of cell membrane on interacting with water present outside the cell. But the toxicity can be reduced by surface modifications. Therefore the surface of buckyballs can be modified on reaction with 24 OH groups and 3 COOH groups to reduce toxicity. The COOH and OH side groups make the buckyball derivatives more water soluble. Therefore they are less likely to form clumps. The advantages of using fullerenes is that it does not have side effects that certain anti-allergic drugs have and is highly effective in reducing allergic responses.

Keywords: Allergy, Mast Cells, histamine, Buckminster Fullerene, Immunoglobulins.

ABSTRACT

Creature models are urgent for comprehension the system of neuropathic painand improvement of powerful treatment for its ideal administration. A battery of neuropathic torment models has been produced to reproduce the clinical agony conditions with different etiology. The present audit thoroughly examines the procedure, behavioural adjustments, limits, and focal points of around 40 diverse creature models of neuropathic pain alongside their changes. Improvement of these models has helped tremendously in understanding the interminable pain and underlying fringe and focal pathogenic instruments. Moreover, scrutinize has brought about the improvement of new helpful operators for neuropathic agony administration, and the preclinical information acquired utilizing these creature models have been progressively meant powerful torment administration in clinical setup likewise. As every creature model has been made with particular strategy and results have a tendency to change to a great extent with the slight progressions identified with strategy, along these lines, it is vital that information from distinctive models ought to be accounted for and deciphered in the connection of the particular torment model.

Keywords: Neuropathic pain, Animal models, Model specification

ABSTRACT

Medication activities might be enhanced by creating new medication conveyance frameworks; one such detailing being a mucoadhesive framework. These frameworks stay in close contact with the absorption tissue, the mucous layer, discharging the medication at the activity site prompting expanded bioavailability for both local and systemic impacts. Throughout the last few decades, the application of mucoadhesive polymers in nasal medication conveyance frameworks has picked up enthusiasm among pharmaceutical researchers as a method for advertising dose structure residence time in the nasal cavity and in addition for enhancing closeness of contact with absorptive membrane of the natural framework. Also, the upgraded paracellular absorption after the swelling of the mucoadhesive polymers on the nasal layers gives a critical path to the assimilation of the macromolecules through the nasal cavity. This review explained a few parts of mucoadhesion identified with the nasal medication conveyance framework. On the first check, the theories of the attachment of mucoadhesive polymers to the mucosa epithelium are described. Also, the attributes and application of a few generally utilized mucoadhesive polymers as a part of nasal medication conveyance are introduced. The mucoadhesive polymers have gigantic potential for the conveyance of therapeutic macromolecules, qualities, and immunizations through the nasal cavity with upgraded bioavailability.

Keywords: Mucoadhesion,Mucoadhesive polymers,Nasal medication,Absorption enhancers

ABSTRACT

Obeticholic acid is a pharmaceutical agent under development used especially to treat liver and gastrointestinal disorders. Its chemical structure is 6 α-ethyl-chenodeoxycholic acid (Figure1). It is a semi synthetic bile acid analogue. In human drug studies, Obeticholic acid is the first farnesoid X receptor agonist and at present, this drug is under phase-II and phase-III clinical trials. Various clinical studies were conducted by using this drug Obeticholic acid to assess the safety and efficacy. In this article, we reviewed the different studies available on Obeticholic acid and its therapeutic use in diseases like non alcoholic steatohepatitis, primary biliary cirrhosis, bile acid malabsorption and portal hypertension.

Keywords: Obeticholic acid, 6 α-ethyl-chenodeoxycholic acid, Farnesoid X receptor agonist.

ABSTRACT

A simple, sensitive, accurate and specific stability-indicating high-performance liquid chromatographic method was developed and validated for the estimation of clopidogrel bisulphate in bulk. In the present study, extensive testing of clopidogrel bisulphate in different stress conditions were carried out as per the ICH guidelines Q1A (R2). The system consisted of a pump (Shimadzu, prominence, LC20AD), with 20µl sample injector, along with a PDA (Shimadzu, prominence, SPDM20A) detector at a wavelength of 254nm. Data was compiled using Shimadzu LC Solution software. The degraded products formed under various stress conditions were separated successfully from the drug by using a PHENOMENEX C8 Column (150 x 4.6mm, 5µm) with binary gradient conditions. Acetonitrile: phosphate buffer of pH 2.0 was used as mobile phase at flow rate of 1.2ml/min. Clopidogrel bisulphate was exposed to various stress conditions like oxidation, hydrolysis, photolysis and neutral decomposition. Clopidogrel bisulphate, which was found to degrade considerably in acidic, photo and oxidative conditions, was found to be stable in alkaline and neutral conditions. Apart from the formation of minor degraded products under accelerated conditions, the drug was reasonably stable in solid state. A good linear relationship over the concentration range of 150-500µg/ml was shown. Validation of the method was carried out as per the ICH guidelines. The method developed was found to be precise, accurate, specific and selective. Clopidogrel bisulphate showed degradation in 5M Hydrochloric acid at 80^oC, in 3% hydrogen peroxide for 5min the drug showed around 35% of degradation, when exposed to sunlight for 15 min, formed around 25-30% of degradation products. Statistical analysis shows that the method is reproducible and selective for the estimation of clopidogrel bisulphate in dosage form.

Keywords: Clopidogrel bisulphate, HPLC, stability parameters, stress conditions.

ABSTRACT

For more patient compliance there is a great demand for novel dosage form. Fast dissolving drug delivery system offers a solution for the patients who prefer oral route of drug administration without difficulty in swallowing. Fast dissolving films offers the simplest route of administration which is not painful and which do not require water for swallowing. Chlorpheniramine maleate is the First Generation alkyl amine antihistamine and used to relieve symptoms of allergy, hay fever, and common cold. These symptoms include rashes, watery eyes, itchy eyes/nose/throat/skin, cough, runny nose, and sneezing. In present study the aim was to formulate and evaluate fast dissolving films of Chlorpheniramine maleate. The films was prepared by solvent casting method, the superdisintegrants Crospovidone (2,4,6,8,10% w/w) and Microcrystalline Cellulose (5,10,15,20,25% w/w) were used in different concentrations with HPMC & PVA as a film forming base. Along with polymers and superdisintegrants the plasticizer PEG, mint flavor and sucrose were used in preparation of films. The formulated films were evaluated for thickness measurement, weight variation, folding endurance, disintegration time, in vitro drug release. It was concluded that the films containing Crosspovidone shows better drug release and less disintegration time as compared to the films containing Microcrystalline Cellulose.

Keywords: Fast dissolving films, Chlorpheniramine maleate, Compliance, superdisintegrants

ABSTRACT

Medicinal herbs are significant sources of chemotherapeutic drugs and play a vital role in the prevention and treatment of cancer. Mentha pulegium L. from Labiatae family was traditionally used as an anticancer agent. In this study, aerial parts including leaves of this plant were extracted by methanol and fractionated extracts have been produced by petroleum ether, ethyl acetate, acetone, methanol and distilled water. For the purpose of cytotoxic evaluation of methanolic extract and its fractions on human ovary carcinoma cells (C13), human hepatocarcinoma cells (HepG2) and human lung carcinoma cells (A549), clonogenic assay was performed. Briefly, 200 cells were seeded in each well of 6 well plates in RPMI 1640 with 10% FBS media. After 24 hours incubation, 0-50μg/ml of methanolic extract and its fractions were exposed to the cells. Finally, colonies with more than 50 cells were counted after 7 days. In each case, a control row was set by the exposure of cells to compounds-free solvents. LC₅₀ values were calculated using nonlinear regression analysis on Graphpad prism^® software. The result showed that the methanolic extract and its fractions are cytotoxic on all three studied human carcinoma cell lines at different degrees. Human ovary carcinoma cell line (C13), which is resistant to many other chemotherapeutic agents (e.g. cisplatin), is the most sensitive cell line to methanolic extract and its fractions compared to two other cell lines. Further complementary cellular and animal studies are recommended for these anticancer candidates.

Keywords: Cancer, Mentha pulegium, Clonogenic assay, Cytotoxicity, C13, HepG2, A549

ABSTRACT

Andrographis paniculata (Kalmegh, family: Acanthaceae) is used extensively in the Indian traditional system of medicine as a hepato-protective and hepato-stimulative agent. Osmotic drug delivery systems are the best amongst promising strategy based reliable drug delivery systems employed for controlled drug delivery. Floating drug delivery systems is one of the important approaches to achieve gastric retention to obtain sufficient drug bioavailability. Pre-formulation studies are the first step in the rational development of dosage form of a drug substance. Different quantities of cetosteryl alcohol ranging from 50 mg to 200 mg have been checked for floating lag.

Keywords: GRDDS, floating osmotic capsule, Andrographis paniculata, hepatoprotective

ABSTRACT

In 2013 world health organization concluded that approximately around 35.0 million people have been infected with HIV and about 1.5 million people have died of AIDS. Most of the people infected with HIV particularly African regions. World health organization continuous to bear the burnt of HIV epidemic in sub Saharan African region like Zimbabwe. This country is experiencing one of the harshest HIV/AIDS epidemics in the world .So according to performance of ART program estimated that percentage of eligible adulates 76.9% and children’s around 46.12 % in 2013. The statistical information about Global economic environment in ARV business has continued to grow in the generic-accessible market. So it is an essential need for quality assured ART’s with proper regulatory control and evolution procedures. In this paper work it involves how will the Anti Retroviral generic drugs filing have been processed based on Medicinal Control Authority of Zimbabwe [MCAZ].

Keywords: HIV/AIDS, ART, MCAZ.

ABSTRACT

Aegle marmelos, a plant having tremendous therapeutic potential, the importance seems largely due to its medicinal properties and all the parts viz. roots, leaves, fruits, bark and seeds are used for curing human ailment. In the present investigation, the anticlastogenic potential of hydromethanolic Aegle marmelos (AM) leaves extract has been evaluated using in vivo Micronucleus assay in Swiss albino mice. Cyclophosphamide (CP), a well known mutagen was given intraperitoneal (i.p.) injection at the dose of 50 mg/kg bodyweight (b.w.). AM leaves extract at the doses of 450, 675, 900 mg/kg b.w. provided protection when given 24 hrs. prior to CP administration. In CP treated animals, a significant induction of micronucleus was recorded and in different AM extracts supplemented groups, a dose dependent significant decrease in CP induced clastogenicity was observed which was statistically significant (p<0.05) as compared to the cyclophosphamide group. It was also observed that Aegle marmelos leaves extract alone could not induce micronuclei formation at the test dose of 450 mg/kg b.w. Thus, the study revealed the antigenotoxic potentiality of AM leaves extract against CP induced micronuclei formation.

Keywords: Cyclophosphamide, Antigenotoxic, Anticlastogenic, Micronucleus, Intraperitoneal.

ABSTRACT

In the present study a series of 20 histone deacetylase 8 (HDAC8) inhibitors were used for generation of pharmacophore. A five features pharmacophore with one hydrogen bond acceptor (A), two hydrogen bond donors (DD) and two ring aromatics (RR) was developed and used for searching compound database. A statistically significant atom based 3D QSAR model was built by selecting best pharmacophore hypothesis ADDRR.3 with R² = 0.9821 for training set of 14 molecules and Q²= 0.7314, RMSE= 0.1709, Person-R= 0.9061 for test set of 6 molecules. These parameters indicate that the model is a good predictive model. Docking study of known inhibitors as well as hits resulted after data base searching having fitness score ≥ 1 was performed. Docking analysis shows the important residues in the active site of receptor are Zn-388, TYR-306, HIS-142, PHE-152, PHE-208, GLY-151, and HIE-180. The XP glide score of highest active compound 1 and lowest active 20 are -11.73 and -6.036 respectively, which corroborated with experimental activity. On the basis of pharmacophore matching, predicted activity and docking interactions 5 novel chemical scaffold (Code No: CACPD2011a-0001275680, CACPD2011a-0000573705, CACPD2011a-0001843791, CACPD2011a-0000300107, CACPD2011a-0000291783) are reported as potent HDAC8 inhibitors.

Keywords: Pharmacophore, Virtual screening, atom based 3D QSAR, HDAC8 inhibitors, Docking.

ABSTRACT

The aim of the present work was to formulate and evaluate in situ gelling system of levofloxacin hemihydrate. Levofloxacin hemihydrate is an antibacterial agent which exhibits rapid pre-corneal elimination and poor ocular bioavailability when administered in the form of conventional ophthalmic solutions like eye drop. To overcome this, an attempt has been made to formulate pH induced in situ gelling system of levofloxacin to provide sustained release of drug. Polymeric carriers that undergo sol-to-gel transition upon change in pH. The levofloxacin hemihydrate in situ gelling system formulated by using polyox in combination with hydroxyl propyl methyl cellulose (HPMC K4M) which acted as viscosity enhancing agent. The developed formulation was stable, non-irritant and provided sustained release over 8-hour period and can be a viable alternative to conventional eye drops. The formulations were found to be non-irritating.

Keywords: Ophthalmic drug delivery system, pH induced, in situ gel, Levofloxacin hemihydrate

ABSTRACT

A rapid, specific and accurate stability indicating liquid chromatographic method compatible with Mass Spectrophotometer has been developed for Aliskiren Hemifumarate. The LC method is carried out on a Hypersil BDS C8 150*4.6 mm maintained at 25°C. The mobile phase consisted of 0.1 M ammonium acetate adjusted to pH 6.5±0.05 and mixed with Methanol in ratio of 375:200 v/v. A gradient programme used with acetonitrile with flow rate of 1.0 mL/min, with ʎmax 278 nm. The chromatographic separation is obtained with Aliskiren retention time at about 18 minutes and it is linear in the range 1 – 4 ppm ( 0.05% - 0.2 % of Test concentration). The specificity and stability-indicating capability of the method are proven through degradation studies, which also showed that, there is no interference of degradation products and peak due to excipients with main peak.  Developed method was used for identification of Aliskiren Lactose adduct impurity. The method partially validated for its intended use and can be applicable for stability study.

Keywords: Aliskiren Hemifumarate, Aliskiren Lactose adduct, mass spectrophotometer.

ABSTRACT

The present study was an attempt to prepare and evaluate Zolmitriptan 9 different oral disintegrating tablets using superdisintegrants like SSG, Crospovidone and Croscarmellose sodium. Formulations were evaluated for their micromeretic properties and post compression studies and found to be within the limits. Based on the disintegrating time and dissolution studies F9 was found to be best formulation. It was found that the sodium starch glycolate is much more effective than the other super disintegrating agents in the preparation of Zolmitriptan oral disintegrating tablets. DSC and FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation.

Keywords: Zolmitriptan, ODT’s, SSG, Crospovidone, Croscarmellose sodium.

ABSTRACT

RP-HPLC method has been developed for the quantitative estimation of Propranolol hydrochloride and Etizolam using C 18 column and a mobile phase consisting of Methanol and Water in the ratio 70:30. The mobile phase was pumped at a rate of 1ml/min and detection was carried out at 281.5 nm(iso-absorptive point). The linearity was found to be in range of 5-50µg/ml and 0.5-5µg/ml with regression coefficient (r²=0.999, and r²=0.997) for Propranolol hydrochloride and Etizolam respectively. The peaks obtained were sharp having baseline separation with a retention time of 2.35and 6.57min for Propranolol hydrochloride and Etizolam respectively.The LOD was found to be at the concentration of0.1µg/ml and 0.025µg/ml for Propranolol hydrochloride and Etizolam respectively. The percentage recovery was found to be 98.5% to 100.58% for Propranololhydrochloride and 95% to 106.6% for Etizolam. The method was validated statistically.

Keywords: Propranolol hydrochloride, Etizolam,  RP-HPLC.

ABSTRACT

Development of pH sensitive zolmitriptanin-situnasal gel was aimed to improve absorption and patient compliance. In the present research work, mixture of Carbopol 940 and Hydroxypropylmethylcellulose K100 were used to confer pH sensitive gelation property. Different formulation was prepared by varying the concentrations of Carbopol 940 and HPMC K100.These formulations were evaluated for parameters like pH, drug content, viscosity, mucoadhesive strength, gel strength, in-vitro drug release, in-vitro permeation and drug excipients compatibility. In this formulation the release profile depend on the concentration of Carbopol 940 and HPMC K100. A 3² factorial design was applied to see the effect of variables Carbopol 940 (X₁) and HPMC K100 (X₂) on the various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. The results of the F-statistics were used to select the most appropriate model. Formulation containing Carbopol 940 (0.1%) and HPMC K100 (0.2%) was found to be optimum. The study indicate that the formulation was effective in providing in-vitro release of drug and the mucoadhesive formulation.

Keywords: Anti-migraine, Carbopol 940, HPMC K100, In-situ Gelling system.

ABSTRACT

This research has focused on the incorporation of the thiadiazole moiety into versatile pyridine ring because of their biological properties. In order to explore the possibilities of some altered biological action author envisaged that by designing the Schiff base derivatives of 1, 3, 4-thiadiazole moiety may exhibit anticancer properties. These novel 1,3,4-thiadiazole Schiff base compounds have been synthesized by microwave-assisted synthesis and screened for their cytotoxicity on HeLa, HepG2 and MCF7 cancer cell lines.The key intermediate 2-(4-fluorophenyl)pyridine-3-carboxylic acid was obtained by hydrolysing the ester 3 in presence of KOH and methanol.Thus obtained compound 4 was treated with thiosemicarbazide and phosphorous oxychloride and cyclized in microwave inorder to get the intermediate 5-[2-(4-fluorophenyl) pyridin-3-yl]-1, 3, 4-thiadiazol-2-amine. The amine 5 was reacted with different aldehydes (a-h) in presence of catalytic amount of acetic acid and obtaineda series of novel Schiff base derivatives 6a-6h. These compounds were characterized by MS, ¹H-NMR,IR and elemental analysis. Most of the compounds in this series have exhibited moderate cytotoxicity onall the three human cell lines at different concentrations, but two compounds 6f and 6h showed good inhibition towards liver carcinoma cell lines having IC₅₀ of 23.8µMand 13.4µM respectively.

Keywords: carcinoma cell, thiadiazole

ABSTRACT

The field of Ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. The most frequently used dosage forms i.e. ophthalmic solutions and suspensions are compromised in their effectiveness by several limitations, leading poor ocular bioavailability. In situ hydrogels are instilled as drops into the eye and undergoes a sol to gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic in situ gel of Moxifloxacin HCl a fluoroquinolone antibiotic. Poloxamer 407 a temperature sensitive gelling agent was employed for the formation of in situ hydrogel along with sodium alginate as a mucoadhesive polymer. In-situ gel was evaluated for various parameters like appearance, pH, drug content, gelling capacity, gel strength, bioadhesion, viscosity, In-vitro drug release, isotonicity, sterility, antifungal activity, ocular irritancy and stability studies. The gel strength, bioadhesion and isotonicity shown quality parameter for ophthalmic formulation. The optimized formulation containing 10% w/v poloxamer 407 and 0.1% w/v sodium alginate have shown 96.84% drug release up to 8 hrs. This is sufficient for antibacterial activity. Drug release kinetic study shown that a Korsmeyers-peppas is the best-fit model. This study found that an optimized formulation having improved viscosity and better mucoadhesive property may improve the bioavaibility of ocular administration of moxifloxacin HCl in in-situ gel form and can be alternative to the conventionally administered oral formulation and effectively used to prolong residence time.

Keywords: Poloxamer 407, Thermoreversible technique, Antibacterial activity

ABSTRACT

Nasal mucosa has been considered as a potential administration route to achieve faster and higher levels of drug absorption because it is permeable to more compounds than the gastrointestinal tract. It is an attractive route of administration due to lack of pancreatic and gastric enzymatic activity, neutral pH of the nasal mucus and less dilution by gastrointestinal contents. In-situ gel forming systems have been developed to prolong the nasal residence time of a drug and improve nasal bioavailability. Fexofenadine hydrochloride is one of the most widely used drugs for allergic rhinitis. It is an anti-histaminic and is available in oral dosage forms. The present work is aimed at designing a gel formula for nasal administration. To enhance therapeutic effect of the nasal formulation of fexofenadine hydrochloride pH sensitive polymers were used. Xanthan gum and Carbopol 934 were selected as independent variables in the factorial design. Solubility of the drug in the formulation was enhanced by using Tween 80. Evaluation parameters of the formulation like pH, clarity; rheological study both formulation i.e. solution and performed gel, gelling time, drug content, in-vitro drug diffusion study, stability studies were performed. The formulations so designed shall enhance bioavailability of drug and offer better therapeutic outcomes, offer aesthetically appealing dosage form to increase patient compliance and shall overcome side effects and limitations of other dosage forms of marketed preparations.

Keywords: Nasal drug delivery, Fexofenadine Hydrochloride, pH sensitive, gels.

ABSTRACT

Cancer, a disease characterized by uncontrolled proliferation of cells that have transformed from the normal cells of the body and is one of the major causes of death in developed and developing nations. Presently available treatment method, chemotherapeutic agents, suffers from drawback of toxicity such as bone marrow suppression, alopecia and vomiting. Its not within the reach of common man. Therefore challenging task is to identify quick and novel methods which can be of therapeutic value in human cancers. Plants have a long history and important role as a source of effective anti-cancer agents. Hence in the present study, one of the traditionally used plant, M.minuta was screened for cytotoxicity. Successive solvent extraction was carried out and the petroleum ether, chloroform, ethyl acetate, alcoholic and aqueous extracts of M.minuta were prepared. Extracts were subjected to Brine shrimp lethality assay and it was observed that % mortality increased gradually with the increase in concentration of the test samples. Ethyl acetate and alcoholic extracts which showed better cytotoxicty were further screened for their cytotoxicity towards breast cancer cell lines using MTT cell viability assay. In the same, ethyl acetate extract was found to be significantly cytotoxic towards cell lines compared to that of alcoholic extract which may be due to higher amount of phenolic compounds present in them. The results obtained in this study further supported the traditional usage of the drug and the activity of drug can be attributed to major bioactive phytochemical class; poly phenolics, present in the drug.

Keywords: Marsileaminuta, cytotoxicity, phenolics, MTT assay, Brine shrimp

ABSTRACT

To develop and validate a simple, accurate & precise Spectrophotometry methods for simultaneous estimation of Gatifloxacin (Gati) and Loteprednol (Lote) in their combined pharmaceutical dosage form. Two simple, accurate, precise U.V Spectroscopy methods have been developed. First method was based on Simultaneous equation method. Here 286 nm was selected for the estimation of Gatifloxacin and 220 nm was selected for the estimation of Loteprednol. Second method was developed was second order derivative method, here Gatifloxacin was measured at 265.60nm ZCP of Loteprednol and 228.84 was selected for Loteprednol at ZCP of Gatifloxacin. Gatifloxacin and Loteprednol showed linearity in the range of 3-15μg/ml and 5- 25μg/ml in Simultaneous Equation method as well for second order derivative method. Correlation coefficient for Simultaneous estimation method is 0.9936 & 0.9968 whereas for Second order derivative it is 0.9986 & 0.9977 Both methods were validated by validation parameters and it show result where lie within its acceptance criteria as per ICH Q2 (R1) guideline. Hence, it can be successfully used for the routine analysis of Gatifloxacin and Loteprednol in their combined pharmaceutical dosage forms.

Keyword: Gatifloxacin, Loteprednol, 0.1N NaoH and Validation parameter.

ABSTRACT

For the estimation of tolterodine tartrate a new simple and accurate visible spectrophotometric method was developed. The proposed method was based on the formation of yellow-orange colored complex results from complete mixing of tolterodine tartrate, methyl orange and chloroform, which shows the maximum absorption at the wave length 417 nm. The linear relationship between the absorbance and the concentration of tolterodine tartrate was in the range of 20 – 120 µg/ml with a correlation coefficient = 0.997. This new method has offered a determination of tolterodine tartrate drug without any interference with excipients indirectly with a high accuracy for the analytical results. The method was found to be simple, economic, accurate and reproducible and can be used for routine analysis of tolterodine tartrate in bulk and in pharmaceutical formulation.

Keywords: Tolterodine tartrate, methyl orange, tolterodine tartrate tablets, colorimetry.

ABSTRACT

5-(7-bromo-5-chloro-3-methylbenzofuran-2-yl)-1-phenyl-1H-pyrazole-3-carbohydrazide 1 underwent a series of hetero-cyclization reactions with different chemical reagents such as triethylorthoformate, acetic acid in phosphorous oxychloride, benzoic acid in phosphorous oxychloride,  N,N’carbonyldiimidazole in dioxane, carbon disulphide in pyridine to afford substituted 1,3,4-oxadiazoles 2, 3, 4, 5 and 6 respectively.  Extending the reaction of 6 with 4-(2-chloroethyl) morpholine hydrochloride afforded 7. The structures of the newly synthesized compounds were established on the basis of spectral analysis such as IR, ¹H NMR, ¹³C NMR and Mass spectral data. The synthesized compounds were screened for their antimicrobial activity against two gram positive and gram negative bacteria and a fungus and found to possess good activity against selected strains.

Keywords: Pyrazole-3-carbohydrazide, 1,3,4-oxadiazole, 1,3,4-oxadiazol-one, 1,3,4-oxadiazole-thione

ABSTRACT

Microsponges are tiny, uniform, micro-porous polymeric beads and spherical in shape. It has the interconnected voids. The particle size of it ranges between 5-300μm. The porous surface of non-collapsible structure of microsponges helps to deliver the active ingredient in controlled manner. Diclofenac Sodium is a Non-steroidal anti-inflammatory drug. The plasma half-life of Diclofenac is 1-2 hrs which increases the dosing frequency and this drug also causes the gastrointestinal irritation. Therefore the purpose of present investigation was to design suitable controlled release Diclofenac Sodium microsponges which can reduce the dosing frequency and gastric irritation. In the present work, Diclofenac Sodium loaded eudragit microsponges were prepared using quasi emulsion solvent diffusion method. Different drug: polymer ratios were used to formulate the microsponges. The compatibility of the drug with polymer was established. Surface morphology of the microsponges was examined using scanning electron microscopy. Production yield, loading efficiency, particle size analysis, and in-vitro release studies were carried out. In-vitro release study showed that the release of drug was in controlled manner and it was increased with increase in drug to polymer ratio up to certain limit.

Keywords: Microsponges, Diclofenac Sodium, Eudragit RS100, Controlled release, Quasi- emulsion.

ABSTRACT

The objective of the present work was to formulate and characterize a Gastro retentive drug delivery system (GRDDS) for Clopidogrel Bisulphate to improve bioavailability and to minimize the side effects such as gastric bleeding and drug resistance development. Clopidogrel floating tablets were prepared by direct compression technique by using HPMC K-100M(Hydroxy Propyl Methyl Cellulose), PEO(polyethylene oxide POLYOX WSR 303) and Carbopol 971P as release retarding agents in different concentrations. Sodium bicarbonate and microcrystalline cellulose (MCC) were used as gas generating agent and diluents respectively. Studies were carried out on floating behavior and influence of polymer type on drug release rate. All the formulations were subjected to various quality control and in-vitro dissolution studies. All the formulations followed first order kinetics, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release. As per Korsmeyer-Peppas equation, the release exponent “n” ranged 0.381-0.561 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. The release rate of Clopidogrel was found to be affected by the type and concentration of the polymer used in the formulation. As the concentration of the polymer was increased, the drug release was found to be retarded. Based on the results, Clopidogrel floating matrix tablets prepared by employing HPMCK100M at concentration 35% w/w (F9) was the best formulation with desired in-vitro floating time and dissolution. The FT-IR and DSC studies revealed that there was no interaction between drug and excipients.

Keywords: Clopidogrel bisulfate, Gas generating system, floating matrix tablets, in-vitro buoyancy.

ABSTRACT

A Chiral liquid chromatographic (LC) method was developed for the enantiomeric resolution of Mirabegron(R)-2-(2-aminothiazol-4-yl)-N-(4-(2-(2-hydroxy-2-phenyl ethyl) amino) ethyl) Phenyl acetamide, adrenoceptor agonist bulk drugs. The enantiomers of mirabegron were resolved on a Chiralpak IF (250mm x 4.6mm, 3.0µm) column using a mobile phase system containing n-Heptane, methyl tertiary butyl ether, methanol and ethanol amine in the ratio of (30:28:42:0.1v/v/v/v). The resolution between the enantiomers was found not less than 4.0.  The presence of methyl tertiary butyl ether and ethanol amine in the mobile phase has played an important role in enhancing chromatographic efficiency and resolution between the enantiomers. The developed method was extensively validated and proved to be robust.  The limit of detection and limit of quantification of (S) enantiomer were found to be 0.2µgmL^-1 and 0.6 µgmL^-1 respectively for 15µl injection volume. The percentage recovery of (S) enantiomer was ranged from 98.5 to 102.5 in bulk drug samples of mirabegron. Mirabegron sample solution and mobile phase were found to be stable for at least 48hrs. The proposed method was found to be suitable and accurate for the quantitative determination of (S)-enantiomer in bulk drugs.

Keywords: Mirabegron‎, enantiomer‎

ABSTRACT

The present study investigates the anti-inflammatory activity in ethanolic extract of Canthium Parviflorum using carrageenan induced paw edema in albino rats. The medicinal values of the Canthium Parviflorum have been mentioned ancient literature as useful in disorders of inflammation. Dried leaves of Canthium Parviflorum powdered and extracted with ethanol using soxhlet apparatus. The anti-inflammatory activity was done by carrageenan induced hind paw edema method using plethys mometer. Diclofenac is used as a standard drug. The significant inhibitory activity shown by the leaf extract of Canthium Parviflorum (125, 250, and 375 mg/kg) over a period of 4h in carragenan-induced inflammation was quite similar to that exhibited by the group treated with diclofenac sodium. The highest percentage inhibition activity was found in the dose of 375 mg/kg with the mean percentage inhibition of 23.45% after 4 hours of extract administration.

Keywords: Canthium Parviflorum, Leaf ethanolic extract, Diclofenac Sodium, Anti-inflammatory activity, Carrageenan induced paw edema.

ABSTRACT

A simple isocratic RP-HPLC method was developed for the estimation of Lurasidone in bulk and pharmaceutical dosage forms by using Waters (Alliance) HPLC (2695 series) System operated with Empower software-2. The optimized chromatographic conditions were found to be buffer of 0.05% Trifluroacetic acid in 0.01 M Potassium dihydrogen orthophosphate solution, mobile phase of buffer and acetonitrile in the ratio 60: 40, Inertsil ODS, C₁₈, 150mm x 4.6mm, 5µ particle size HPLC column at temperature of 30°C, 20 µL of injection volume, 1.0ml/min flow rate and UV detector with detection wavelength 231nm. Retention time and peak area of standard or sample were found to be 5.428min or 5.431 min. and 4128545 or 4126122 respectively. System precision and method precision were found to be less than 2.0%. The method was found to be linear within the limits 2.5-15.0µg/ml with good correlation coefficient 0.9999. The percent of recovery (accuracy) was found from 99.34 to 99.97%. Ruggedness and robustness studies were carried out and the results were found to be satisfactory. Stability of Lurasidone was studied under the different stressed conditions and found to be stable (96.37-93.55%). The % of assay of different dosage of Latuda tablets was found between 99.68 -100.18%. The proposed method was found to be sensitive, precise, accurate, linear, rugged and robust, and applied for the analysis of pharmaceutical formulations and percent of assay was evaluated, hence the proposed method can adopt for the routine analysis in any quality control laboratory.

Keywords: Lurasidone, RP-HPLC, Latuda, Validation, Assay and Quality control.

ABSTRACT

Amitriptyline and chlordiazepoxide in bulk and formulation were estimated by stability indicating reverse phase high performance liquid chromatographic method. For the proposed method the chromatographic conditions are C18 column (250mm×4.6mm i.d., 5µ particle size), mobile phase was mixture of acetonitrile and triethylamine buffer pH 2.5 at a ratio of 30:70. The injection volume was 20µl with a flow rate 1.0ml/min at a ambient temperature. The wave length selected was 220nm and retention times were found to be 4.55 and 5.893mins for amitriptyline and chlordiazepoxide respectively. Amitriptyline shows linear curve at a concentration range of 5-20µg/ml and for chlordiazepoxide the linearity was obtained for the concentration range of 1.8-6.4µg/ml and regression coefficient was found to be 0.997 and 0.999 for amitriptyline and chlordiazepoxide. The limit of detection  and limit of quantification for amitriptyline was found to be 0.02µg/ml and 0.05µg/ml and for chlordiazepoxide was found to be 0.01µg/ml and 0.03µg/m. amitriptyline and chlordiazepoxide shows recoveries were ranged  from 99.98% – 100.08 % and 99.96%- 100%respectively. The method was performed based on ICH guidelines. In the detection of these drugs degradation products were not interfered and the method was considered as new stability indicating method.

Keywords: Amitriptyline, Chlordiazepoxide, Method development and Validation, Stability indicating assay, forced degradation study.

ABSTRACT

The indoor air environment can potentially place patients at greater risk than the outside environment because enclosed spaces can confine aerosols and allow them to build up to infectious levels .It becomes imperative to undertake a study of the microbiological air quality of the airborne micro-flora in the environments of two major hospitals, Ruby Hall Clinic and Jehangir in Pune- India. In Jehangir hospital Staphylococcus aureus (15.74%) was found to be the most common organism. The correlation between the location of sampling and concentration of Staphylococcus aureus showed patient room (65±3)> neonatal ward (22±1.41)> intensive care unit (22±2.82)> operating room (16±1.73)> the main entrance of the hospital (0±0).  While Staphylococcus aureus (25.2%), followed by coagulase negative Staphylococcus (21.78%) and M. luteus (16.28%) were found to be the most common in a Ruby Hall hospital. The correlation between the location of sampling and concentration of Staphylococcus aureus in Ruby hall hospital , showed patient room (45±4.24)> intensive care unit (22±2.82)> neonatal ward (12± 2.80)> operating room (8±1.41)> the main entrance of the hospital (3±2.85). Aspergillus spp., Penicillium spp., Rhizopus spp. and Alternaria spp. were isolated in both hospitals. Maximum bacterial rates were detected in the patient rooms, while minimum bacterial rates were detected in the operating rooms and neonatal wards. The time of visit showed higher microbial rates in hospital.

Keywords: Air sampling, airborne microflora , bacteria, Fungi

ABSTRACT

The aim of this investigation was to develop and optimize Metformin Hydrochloride matrix tablets for sustained release application. The sustained release matrix tablet of Metformin Hydrochloride was prepared by wet granulation technique using Tamarind pulp polysaccharide. The polysaccharides obtained after extracted from natural source and evaluated for their colour, viscosity and pH. The prepared tablet was evaluated for their hardness, friability, drug content, In vitro dissolution, swelling studies. In vitro drug release profiles of Metformin Hydrochloride Tablet using Tamarind pulp polysaccharide formulation release of drug from the Tablet exhibited a sustained & controlled pattern over an extended time period. .The tablet formulation TF-1 was found to release the drug of about 95% after 12 hrs, The tablet formulation TF-5 was found to release the drug of about 70% after 12 hrs, thus concluded to have sustained drug release for longer period of time in sustained and controlled pattern when compared to other tablet formulations. Using Higuchi’s Model and the Korsmeyer equation, the drug release mechanism from the sustained release tablets was found to be Anomalous (non-Fickian) diffusion. Compatibility study confirmed that interactions do not exist between the drug and polymer.

Keywords: Metformin Hydrochloride, Tamarind pulp Polysaccharide, matrix tablet, Sustained Release. Swelling index.

ABSTRACT

Microwave assisted solvent free synthesis of cyclohexenone and indazole derivatives were carried out by chalcones derived from different acetophenones and 1-naphthaldehyde. Structures of the compounds have been characterized by IR, ¹H NMR, Mass spectrometry and elemental analysis. All the synthesized indazole derivatives were screened for antibacterial activity and are found to posses moderate to good activity against some species of bacteria.

Keywords: 1-napthaldehyde, chalcones, cyclohexenone, indazole, antibacterial, microwave irradiation.

ABSTRACT

The present investigation is mainly on the synthesis, characterization and determination of some properties of new compound cetylpyridinium hexafluorosilicate for his potential use as caries-preventive and antibacterial agent. Hexafluorosilicate of the composition (C₂₁H₃₈N)₂SiF₆ was separated as crystalline product of interaction of hexafluorosilicic acid with the methanol solution of cetylpyridinium chloride. This complex was characterized by elemental analysis, IR, ¹H and ¹⁹F NMR, mass-spectrometry, differential thermal analysis, and solubility data. The IR spectral data indicates on absence of noticeable distortion of the symmetry of SiF₆^2– anion with regard to O_h. The studied compound is characterized by the predicted tendency to hydrolyze in dilute aqueous solutions with the formation of silica and fluoride anions.

Keywords: Hexafluorosilicate, IR spectra, NMR, solubility, hydrolysis.

ABSTRACT

To develop a fast and sensitive  UV spectrophotometric method for the quantitative estimation of Formaldehyde in Rivastigmine tartrate drug substances and validate as per ICH guidelines. The method was based upon the observation, that a characteristic colourresults upon addition of  solution of Pentane-2,4-dione , also known as acetylacetone . In acetic acid and ammonium acetate buffer condition, acetylacetone and formaldehyde react to form dimethyl pyridine. Dimethyl pyridine is slightly yellow and its absorption maximum in aqueous solution is λ 420 nmin Rivastigmine tartrate drug substance.The developed method resulted in Formaldehyde exhibiting linearity in the range 0.975 to 234 µg/g. The Intraday and interday precision is exemplified by relative standard deviation of 0.562 % and 0.757%. Percentage Mean recovery was found to be in the range of 98‐101%, during accuracy studies. The limit of detection (LOD) and limit of quantitiation (LOQ) were found to be 1.3 µg/g and 3.9 µg/g respectively.The present work was aimed to develop a visible spectrophotometric method, which is simple, sensitive, accurate and cost effective to evaluate the quality of the bulk drugs.

Keywords: UV Spectrophotometry, Formaldehyde, Rivastigmine Tartrate, Method development, Validation.

ABSTRACT

Antimicrobial prophylaxis in cardiac surgery has been demonstrated to lower the incidence of postoperative infection. Inappropriate antimicrobial prophylaxis, as inappropriate selection of the antimicrobial agent or dosing regimen, can increase the prevalence of antibiotic resistant strains, prolong hospital stay, cause postoperative infection, and negatively affect an institution’s pharmacy budget for antibiotics. To assess the current postoperative prophylactic antibiotic protocols applied in the cardiac surgeries department in Ain Shams University teaching hospitals with respect to others and to international guidelines for antimicrobial prophylaxis practice in cardiac surgery. Total of 320 paediatric and adult patients who were admitted for cardiac surgery to Ain Shams University teaching hospitals from September 2012 till March 2013.The antimicrobial prophylaxis indication, choice, duration, dose, dosing interval, and timing appropriateness were assessed against 3 international guidelines using a pre-tested, structured clinical data collection form. All patients were monitored daily during their inpatient stay until discharge. Data regarding surgery duration, mechanical ventilation duration, intensive care unit stay, postoperative stay and total hospital stay were obtained. Adherence to all antimicrobial prophylaxis guidelines was not achieved for any study patients. A statistical significant difference for the mechanical ventilation duration, intensive care unit stay, postoperative stay and total hospital stay were found concerning both the paediatrics and the adults between the infected and non-infected group. Study findings indicate that adherence to international guidelines for antimicrobial prophylaxis is far from optimal in cardiothoracic department at Ain Shams University teaching hospitals, leading to the inappropriate administration of many antibiotics.

Keywords: Prophylactic Antibiotic, Antibiotic Resistance, Nosocomial Infection, Clinical Pharmacy.

ABSTRACT

This study was conducted to determine the effect of foliar salicylic acid (SA) applications on vegetative growth, physiological and biochemical constituents of Vigna radiata (L.)Wilczek. SA was applied at five different concentrations (50ppm, 100ppm, 150ppm, 200ppm 250ppm) during the growth period of 7 and 15 days old Vigna seedlings. Growth parameters such as shoot and root lengths, shoot and root fresh weights and dry weights and physiological and biochemical constituents such as photosynthetic pigment composition, total soluble sugar, free amino acid and total phenols were recorded from treated and control plants on 10 and 18 days after sowing. From the experiment done all of five doses of SA application produce considerable increase in plant growth, physiological and biochemical constituents compared to the control. The optimal concentration for increased overall plant growth was found to be at 100ppm. As compared to Chlorophylla, Chlorophyllb was found to synthesize more which could be ascribed to change in the stoichiometry of PSII to PS I. Thus, the present work confirms the promotory effects of SA on overall growth, pigment synthesis and other biochemical constituents in Vigna radiata.

Keywords: Vigna radiata, salicylic acid, vegetative parameters, physiological and biochemical constituents.

ABSTRACT

The main aim of the study was to assess the role of grape seed extract in gamma radiation-induced impact on delayed type hypersensitivity (DTH) response to oxazolone in Swiss albino mice. Eight groups each of ten have been used. Four groups have exploited to assess the effect of grape seed, gamma radiation and both on the induction of contact sensitivity and four other groups have been utilized to evaluate the effect of grape seed, gamma radiation and both on the elicitation of contact hypersensitivity. In each group, one was used as a control, the second received 2 Gy gamma irradiation 24 hr before the induction or the elicitation phase using the mouse ear swelling test (MEST). Third group was maintained on oral grape seed extract (0.1%), and a fourth was maintained on grape seed extract (0.1%) and received with total body irradiation (2Gy). At the end of the experiment sera from all groups were tested for total antioxidant and dismutase activities and gamma interferon level. Data showed that exposure to gamma irradiation had a negative impact on DTH response to oxazolone whether the exposure was before the elicitation or the induction phase. Data also showed that radiation was associated with a significant mounting of serum total antioxidant, dismutase activity, gamma interferon. Grape seed extract was able to restore the DTH response of irradiated mice to the control value. This was associated with a decline in serum total antioxidant, dismutase activity and gamma interferon in comparison to gamma irradiated animals.

Keywords: ionizing radiation- delayed type hypersensitivity- grape seed extract – interferon gamma- oxazolone.

ABSTRACT

The present work aims to study the effect of ethyl extract stem bark of Khayasenegalensis on the lipid profile of rat hepatocytes. For this, a sub-chronic gavage was performed on batches of 8 Wistar rats received 3 respectively, by oral administration of the extract at doses 2.5 mg / kg; 5mg / Kg; 10mg / Kg; 25mg / Kg; 50mg / Kg; 100mg / kg and 200mg / kg body weight for 14 days (control group received instead of the extract of Khayasenegalensis of distilled water) and isolation of hepatocytes was made after killing rats. Then, all the lipids (phospholipids and neutral) were extracted and separated by thin layer chromatography on two different plates. TLC of lipids (phospholipids and neutral) revealed an appearance of membrane lipids in the dose of 5 mg / kg; 10mg / Kg; 25mg / Kg; 50mg / Kg; 100mg / kg and 200mg / kg compared to control, while in the dose of 2.5 mg / kg there was no significant change compared to the control. The appearance of neutral lipids is only degradation of the phospholipids and the phospholipids provides that Khayasenegalensis lysed membrane of hepatocytes, which leads to the dispersion of the phospholipids. So it was only after dispersion, these lipids have started to deteriorate in neutral lipids. Where the administration of ethyl extract of trunk bark khayasenegalensis high dose may cause necrosis of liver cells, thus at high doses is toxic Khayasenegalensis. And the most efficient to mitigate the risk of toxicity are those doses less than or equal to 2.5 mg / Kg.

Keywords: Khayasenegalensis, phospholipids, neutral lipids, CCM, necrosis.

ABSTRACT

Chalcones are a category of compounds consisting of two aryl rings linked by an α,β-unsaturated ketone moiety. The synthesized compounds CEA and CMA were evaluated for antimicrobial activity by disc diffusion method. The antibacterial and antifungal activity was evaluated against Moraxella, Enterobacter, Pseudomonas aeruginosa (bacterial strains), Candida albicans, A.niger and Trichophyton (fungal strains) using Erythromycin (for bacteria) and Ciprofloxacin (for fungi) as the standard drugs. The structure of synthesized compounds has been elucidated by IR, ¹H, ¹³C NMR and elemental analysis.

Keywords: Chalcone, antibacterial, antifungal, Nystatin and ciprofloxacin.

ABSTRACT

Etravirine is a non-neucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV. One of the major problems with the Etravirine is its low solubility, which results into poor bioavailability after oral administration. Therefore, solid dispersions (SDs) of Etravirine were prepared by two methods, Hot-melt extrusion and Spray drying technique using various carriers like Polyvinyl Caprolactam-Polyvinyl Acetate-Polyethylene Glycol Graft Copolymer (Soluplus), Hypromellose 2.5 cPs, PEG 6000, Amino Methacrylate Copolymer (Eudragit EPO) & Copovidone (Kollidon VA64) and Povidone (Kollidon 30) to increase its aqueous solubility. Faster and high drug release was found in the SDs prepared by hot melt extrusion (HME) with soluplus in the ratio of 1:3 as compared with spray drying technique (SDT) using drug substance, Soluplus and Microcrystalline cellulose (Avicel PH105) in the ratio of 1:2:0.5. There is 3 fold increases in the solubility of Etravirine prepared by HME & SDT compared with pure drug substance. HM3 and SDT4 are finalized as optimized formulations prepared by HME & SDT based on their solubility, drug substance content and in vitro drug dissolution studies. FT-IR, DSC and XRD of SDs by HME & SDT showed a change in crystal structure toward an amorphous form of Etravirine. The obtained results suggested that developed Etravirine SDs by HME & SDT has potential for oral delivery and might be an efficacious approach for enhancing the therapeutic potential of Etravirine.

Keywords: Etravirine, HIV, Hot-melt extrusion, Spray drying, Soluplus.

ABSTRACT

A simple, specific, accurate and precise reverse phase high performance liquid chromatographic (RP-HPLC) method was developed with high sensitivity for determination of Valsartan and Hydrochlorothiazide drugs in combined dosage forms. The separation was achieved on Zorbax CN (25 cm x 4.6 mm, 5 µm) at flow rate of 1.8 ml/min with 70: 30 mixture of phosphate buffer: acetonitrile (pH 6) as the mobile phase. The quantification was achieved with PDA detector at 265 nm. The injection volume was 20 μl. The retention times of Valsartan and Hydrochlorothiazide were 6.04 min and 2.27 min, respectively. The method was validated for linearity, precision, specificity, robustness and recovery according to the ICH guidelines. The linearity of response for Valsartan and Hydrochlorothiazide were assessed by analysis of five independent levels of calibration curve in range of 20-100 µg/ml and 2-10 µg/ml respectively. The recovery data was between 98.77-99.73% and 98.75-100.56% for Valsartan and Hydrochlorothiazide respectively. The limit of detection and quantification for Valsartan were 0.98 and 2.97μg/ml respectively and for Hydrochlorothiazide were 0.18 and 0.57μg/ml, respectively. The method was found to be simple and highly sensitive and can be useful in the routine quality control of Valsartan and Hydrochlorothiazide in bulk manufacturing and pharmaceutical dosage forms.

Keywords: Valsartan, Hydrochlorothiazide, RP-HPLC, validation, system suitability.

ABSTRACT

Aim of this study is to give an enlightment on pharmacognosy and in-vitro antioxidant activity of Among them E. littorale leaf, G. sylvestre leaf and M. charantia fruits which are used as antidiabetic drug in India since ancient time. These plants traditionally used in diabetes, liver disorders, fever and inflammation. The antioxidant activity was measured by DPPH method.

Keywords: Anti oxidant, E. littorale,  E. littorale leaves, G. sylvestre leaf and M. Charantia fruits