IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
DECEMBER 2015
1

EVALUATION OF ANTICANCER POTENTIAL OF IPOMOEA RENIFORMIS CHOIS (CONVOLVULACEAE) LEAVES AGAINST EHRLICH ASCITES INDUCED CANCER IN MICE

Dr. S.B. Bothara1*, Santosh Kumar Vaidya2
1Department of Pharmacology, Shri Bhagwan College of Pharmacy, Aurangabad, Maharashtra, India.
2Department of Pharmacology, CU Shah Pharmacy College, Wadhwan city, Gujarat, India.

Abstract

The present study was carried out to evaluate the antioxidant and antitumor activity of methanolic and aqueous extract of leaves of Ipomoea reniformis has (IPR) against Ehrlich ascites carcinoma (EAC) in mice. The antioxidant activity of Alcoholic and Aqueous extract of leaf of Ipomoea reniformis were carried out by DPPH and lipid per oxidation anti-oxidant assay. It is comparatively studied on the basis of EC50 value with reference to EC50 value of ascorbic acid. The EC50 value of standard, Alcoholic and Aqueous extract of Ipomoea reniformis were found 2.278, 2.392, 2.951 and 66.45, 68.11, 100 by DPPH and lipid per oxidation anti-oxidant assay respectively. For the anticancer potential of Ipomoea reniformis chois. (Convolvulaceae) leaves evaluated against Ehrlich Ascites Carcinoma induced cancer in mice. The EAC cells were maintained in Swiss albino mice, by intraperitoneal (i.p.) transplantation in every 9 days. The ascetic fluid was collected by syringe and the tumour cell count was performed in a neubauer chamber (haemocytometer) and 2 x 106 cells/per ml was obtained by dilution with normal saline. EAC cells of 9 days old were used for the screening study.72 Swiss albino mice were divided into six groups (n = 12) mentioned food and water ad libitum. All the animals in each groups except Group-I, received EAC cells (2×106 cells/mouse i.p.). This was taken as day ‘0’. Group-I served as normal saline control (5 ml/kg i.p.), Group-II served as EAC control. 24-h after EAC transplantation, Group-III received reference drug 5-FU (20 mg/kg i.p) for nine consecutive days and Group-IV to Group VI received plant extract by oral rout for nine consecutive days respectively. Twenty-four hours of last dose and 18 h of fasting, 6 animals of each group were sacrificed by cervical dislocation to measure antitumor, hematological and biochemical parameters, the rest were kept with food and water adlbitum to check mean survival time and percentage increase in life span of the tumor host and results of hematological, biochemical and antitumor were studied respectively. All the studied parameter reveals the Alcoholic and Aqueous extract of Ipomoea reniformis having potent antioxidant and anticancer potentials.

2

FORMULATION AND EVALUATION OF TIZANIDINE HYDROCHLORIDE MOUTH DISSOLVING FILM

Vishal A. Suryawanshi1*, Mitesh P. Sonawane1, Parag K. Rane1, Mayur V. Chinchore1, Bharti S. Borse2
1Department of Pharmaceutics, Loknete Dr. J. D. Pawar College of Pharmacy, Manur, Tal- Kalwan, Dist- Nashik (423501), Maharashtra, India.
2Department of Pharmacognosy, M. G. V. Pharmacy College, Panchavati, Nashik-3.

Abstract

Tizanidine Hydrochloride is widely used in the treatment of multiple sclerosis spastic diplegia back pain or certain injuries to the spine or CNS, Tizanidine Hydrochloride has been found to be effective other antispasmodic drug and has superior tolerability to that baclofen and diazepam. The present study is deals with formulation, and evaluation of Tizanidine Hydrochloride mouth dissolving films. Tizanidine Hydrochloride is one of the drug which is used in the treatment of above The mouth dissolving films was prepared by using solvent casting method. The concentration of Sodium alginate, Glycerol, Tween 80 were kept constant in all formulations (F1-F4) and varying concentration of all the formulations were evaluated for surface pH, weight uniformity, folding endurance, drug content, disintegration time, in-vitro dissolution studies. The formulation ‘F3’ was found to be optimized formulation. It shows results for all evaluation parameters such as weight variation 84.56±0.22 mg, surface pH 6.10 ±0.45, folding endurance > 100, drug content 84.10±0.20%, disintegration time 28±0.50 sec, and in-vitro dissolution study 63.71 % at the end of 5 min. From all of observation we can conclude that the formulation F3 shows better results.

3

IDENTIFICATION AND CHARACTERIZATION OF UNKNOWN IMPURITIES IN RACTOPAMINE HYDROCHLORIDE ACTIVE DRUG SUBSTANCE

S. Natarajan1*, B. K Kempegowda2
1Bharathiar University, Coimbatore, Tamil Nadu- 641 046, India.
2Maharani’s Science College for Women, Mysuru, Karnataka 570005. India.

Abstract

This research articles focus on identification and characterisation of unknown impurity that is present in theRactopamine hydrochloride (RHCL) an Active drug substance(API). The various regulatory guidelines emphasise to identify the unknown impurities present in the drug substances and drug product and therefore it is very important to identify and characterise these impurities. The unknown impurity present in the drug substance was synthesized in the laboratory and it was further purified by the preparatory HPLC(PHPLC).The purified impurity taken for Characterisation by Mass spectrometry(MS),UV Profile,NMR.The investigational reports concludes that impurity present in the drug substance is Dimer of RHCL. The peaks of the dimers were well separated from the other known impurities. The extensive analytical investigations clearly indicates that the impurities with retention time of 1.2 and 1.24 isO-[β-Hydroxy- β-(4-hydroxyphenyl)ethyl] Ractopamine Analogue-1/Analogue-2 which is another dimer Impurity of the RHCL.This impurity is not reported in any monographs or by any drug manufacturers.

4

COMPARATIVE STUDY OF THERAPEUTIC OUTCOMES OF MONTELUKAST AND SERATRODAST IN ASTHMA

Dr. Mohd Ilyaz1*, Dr. Ashfaq Hasan2 , Syeda Sanober Ghazaal3, Shama Noor3, Rumaisa Sahar3, Sana Fatima3
1HOD-Department of Pharmacy Practice, Deccan School of Pharmacy, Hyderabad-500001,Telangana.
2HOD- Pulmonary Medicine, Owaisi Hospital and Research Centre, Hyderabad,Telangana
3Student (PHARM.D) Deccan School of Pharmacy, JNTU-H, Hyderabad-500001, Telangana.

Abstract

Asthma is characterized by hyperresponsivness of tracheobronchial smooth muscles to a variety of stimuli resulting in narrowing of air tubes, often accompanied by increased secretion, mucosal edema and mucus plugging. There is also a disturbing trend of alarming increase in asthma incidences world wide affecting majority of population. . Asthma is treated by Long acting Controller medications like inhaled corticosteroids, beta-2 agonists, mast cell stabilizers, anticholinergics, leukotriene modifiers and Short acting - Reliever medications like beta-2 agonist, oral corticosteroids, anticholinergics. Hence there is a need of a new drug (such as Thromboxane receptor antagonist ) which is therapeutically more efficient than the commonly prescribed medication in management of Asthma. In our study the patients were divided in two groups and prescribed Montelukast and Seratrodast respectively, and their progress was evaluated. We concluded that Seratrodast is more efficient therapeutically than Montelukast in managing Asthma by comparing the FEV1 values and SGRQ scores.

5

RELATIONSHIP BETWEEN SURGICAL STRESS AND SERUM CORTISOL LEVEL: A COMPARATIVE STUDY AMONG ELECTIVE AND EMERGECIVE SURGERY

Dr. R Venkata Ramudu1, Dr. T Giridhar2, T Mahendra3, K Goutham Reddy3, R Rohith3
1Department of Psychiatry, Rajiv Gandhi Institute of Medical Sciences, Kadapa, India.
2Department of General Surgery, Rajiv Gandhi Institute of Medical Sciences, Kadapa, India.
3Department of Clinical Pharmacy, P RamiReddy Memorial College of Pharmacy, Kadapa, India.

Abstract

The aim of our study is to examine the relationship between surgical stress and serum cortisol levels in patients undergoing surgeries and to find out any difference in hormonal response between either type of surgical procedures; elective and emergency. A total number of 90 male subjects of ages between 20-50 years have participated in our study. The total 90 subjects were divided into three groups (I,II,III) each group consisting of 30 subjects and the groups B,C were again divided to three subgroups (A,B,C). Subgroups A (preoperative blood samples were collected 1- hour before surgery), B (postoperative blood samples were collected 1-hour after the end of the surgery) and C (postoperative blood samples were collected 24-hours after surgery). Serum cortisol level was estimated by using the invitro-immunolytic test. Statistical analysis were done by paired, unpaired‘t’ test and regression analysis methods. The preoperative mean serum cortisol concentration in elective surgical cases was almost parallel to that of healthy control. Conversely, in the emergency surgeries, a significantly increased mean cortisol level were observed (I vs IIIA and IIA vs IIIA; P < 0.05). The serum cortisol concentrations were increased both in elective and emergency surgeries but the extent of increase was more noticeable in emergency surgeries (IIB vs IIIB; P < 0.05). Consequently, our study concludes that there is a clear relationship between the surgical stress and the serum cortisol levels in patients undergoing either surgerical procedures (elective or emergency) and there was a high increase observed in emergency type of surgery.

6

AN EMPHASIS ON NAIL INFECTION

Priyanka Rajendra Kajale*, Supriya Rajendra More, Swati Gokul Talele, Anil Jadhav
Sandip Institute of Pharmaceutical Sciences, Nashik.

Abstract

Nails are the remarkable piece of body, other than it’s a dead tissue it likewise have part in serving the human excellence. It secures the fingertip and tissues from wounds further more upgrades the exact developments of distal digits, however it has additionally been reviled with numerous ailments and afflictions including genuine contaminations. Most regular sorts are of Fungal or Yeast diseases bringing about Onychomycosis and in the event that it is left untreated, the nail plate may separate from the nail cot. Other diseases incorporate Paronychia, Tinea Unguis, and Pseudomonas bacterial contamination.Various diseases associated with nail infection are Fungal & Yeast Infection, Paronychia, Pseudomonas bacterial disease, Tinea Unguis, Onychatrophia, Melanonychia, Onychomycosis, Hematoma,etc. This particular review focus on treatment & diseases related to nail. One of the most recent and advanced treatment to treat contagious contaminations of nails is Ozone treatment yet it is not habitually utilized and unreasonable. Like others body parts nails likewise obliged a decent wellspring of supplements to keep up their appearances and wellbeing, Vitamin A, Vitamin D and calcium help in keeping up dampness substance of nails and maintain a strategic distance from fragility, besides this Protein further more unsaturated fats like Linoleic acids are additionally crucial.

7

DEVELOPMENT OF RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION AND VALIDATION FOR ATORVASTATIN AND FENOFIBRATE IN BULK AND TABLET DOSAGE FORM

Patil Khushabu, Narkhede Swapnal, Navade Varsha, Sapkale Pabodh, Dr. Deshmukh Tushar
Shellino Education Society’s, Arunamai College of Pharmacy, Mamurabad, Jalgaon.

Abstract

In the present study, a simple, selective, precise and accurate HPLC method was developed and validated for the simultaneous estimation of atorvastatin and fenofibrate in bulk and its formulations. The mobile phase consists of a mixture of acetonitrile and water (0.05% OPA) in the proportion 75:25. The HPLC analysis of atorvastatin and fenofibrate was carried out at a wavelength of 248nm with a flow rate of 1ml/min. The linear regression analysis data for the calibration curve showed a good linear relationship with a regression coefficient 0.997 and 0.998 respectively. The linear regression equation was y = 45.06x + 4.177 and y = 28.06x + 213.1. The developed method was employed with a high degree of precision and accuracy for the analysis of atorvastatin and fenofibrate. The method was validated for precision (% RSD 1.50 & 0.14 resp.), accuracy (99.97%) ruggedness, (% RSD 0.28 and 0.48 resp.) robustness, repeatability (% RSD 1.93), LOD(%RSD 0.14 and 0.39 resp.) and LOQ (%RSD 0.48 and 1.19 resp.). From the results we can conclude that this method is better for the estimation of atorvastatin and fenofibrate in bulk and its tablet formulation.

8

IMPORTANCE OF SUPERCRITICAL FLUID EXTRACTION TECHNIQUES IN PHARMACEUTICAL INDUSTRY: A REVIEW

Bhusnure O.G1*, Gholve S.B.1, Giram P.S.2, Borsure V. S.3, Jadhav P.P.1, Satpute V. V.3, Sangshetti J N4
1Channabasweshwar Pharmacy College (Degree), Department of Quality Assurance, Latur (MS), India.
2Channabasweshwar Pharmacy College (Degree), Department of Pharmacology, Latur (MS), India.
3Channabasweshwar Pharmacy College (Degree), Department of Pharmaceutics, Latur (MS), India.
4Y. B. Chavan College of Pharmacy, Aurangabad, Department of Quality assurance, Aurangabad. (MS).

Abstract

The pharmaceutical industry is facing many challenges: Invention of new drugs and improvement of the therapeutic drug efficacy against numerous pathologies, meanwhile supporting a continuous effort to move to environment-friendly processes and reducing the use of potentially harmful solvents. As Nature is almost an unlimited source of active substances, a great interest is paid to concentrate them or to remove undesired compounds, using mainly extraction with organic solvents or water or ethanol/water mixtures, depending on the polarity of the targeted molecules. However, for the past three decades, important R&D works about supercritical fluid technology have been dedicated to natural products processing, leading to some very well-known applications to food products like coffee and tea decaffeination or hops resins extraction, but also to manufacturing phytopharmaceuticals/ nutraceuticals; in fact, carbon dioxide, used pure or added with ethanol, presents the definitive advantages to be a green, abundant and cheap solvent perfectly adequate to process food or pharmaceutical products from natural feed stocks at a temperature near to ambient, although it does require a sophisticated equipment designed for high pressure operation, generally up to 300 or 350 bar. But, natural product needs a natural solvent And for non-polar compounds extraction, there is no alternative to supercritical carbon dioxide. Supercritical Fluid Extraction (SFE) referring to fluid-solid extraction and Supercritical Fluid Fractionation (SFF) - referring to fluid-liquid fractionation are also widely investigated for purification of natural or synthetic active products (for instance, elimination of toxic residues). Moreover, Supercritical Fluid technology is very attractive for manufacturing innovative therapeutic particles, either of pure active compounds or mixtures of excipient and active compounds. In fact, it is important to notice that optimized drug formulation and delivery improve therapeutic efficacy of the drug, reduce adverse effects and bring better comfort to the patient. In comparison to conventional Liquid extraction technique, supercritical fluid extraction is much rapid, due to the low viscosity and high diffusivity of the supercritical fluid. Extraction procedure can be made more selective by controlling the density of the medium. Releasing of the pressure, leads to the change of the phase, that is supercritical fluid returns to the gaseous phase and evaporate, leaving behind the extracted material or constituent. Carbon dioxide is the most widely used supercritical solvent for the extraction procedure.

9

IN VITRO SYNERGISTIC ANTIBACTERIAL EFFECT OF METHANOLIC EXTRACTS OF SYZIGIUM AROMATICUM WITH AMPICILLIN AND TETRACYCLINE

Shiji Thomas*1, Fathimathu Zuhara K1, Thara K M2
1Department of Life Sciences, University of Calicut, Kerala- 673635, India.
2Department of Biotechnology, University of Calicut, Kerala- 673635, India.

Abstract

The inevitable development of drug resistance among bacterial pathogens prompted the search for alternative therapeutic methods. The combination therapy of plant antimicrobial compounds with antibiotics seems to be promising. The present study focuses on the synergistic effect of various extracts of Syzygium aromaticum (Linn.) in combination with ampicillin and tetracycline. Preliminary antibacterial investigations were carried out using extracts prepared from dried clove buds using four different solvents of increasing polarities (chloroform, methanol, ethanol and water). The antibacterial activity against different bacterial strains was analysed by agar well diffusion assay, determination of Minimum Bactericidal Concentration and time kill assay. Checkerboard assay and time kill assay of combinations of clove extract with the antibiotics was performed to demonstrate synergistic interactive effects of the drugs. The methanolic extract of clove was subjected to qualitative phytochemical screening for identification of various classes of active chemical constituents such as phenols, flavonoids, saponins, terpenoids, glycosides and alkaloids. Methanolic extract was also subjected to phytochemical compound analysis through RP-HPLC profiling. Clove (methanol) extract enhanced the antimicrobial activity of both ampicillin and tetracycline against Staphylococcus aureus, Methicillin resistant Staphylococcus aureus and Pseudomonas aeruginosa. Clove (methanol)-tetracycline combination proved to be the most effective combination against the MRSA strain used in the present study. The results suggest that extracts of Syzygium aromaticum (Linn.) could be employed to enhance the antibacterial activity of various antibiotic formulations.

10

FLUORESCENT, ANTIMICROBIAL AND PHYTOCHEMICAL ANALYSIS OF BARK OF “CHARAIGORH” (VITEX PEDUNCULARIS WALL.) FROM LATEHAR, JHARKHAND

Raphael R. Marandi*, Dr. S. John Britto
The Rapinat Herbarium and Centre for Molecular Systematics, St. Joseph’s College (Autonomous), Tiruchirappalli, Tamil Nadu, India.

Abstract

Vitex peduncularis Wall., belonging to Lamiaceae family, is commonly called as ‘Charaigorh’ by the several ethnic groups of Jharkhand. According to the local traditional healers, the bark is used against snake bites, hypertension, psoriasis, kidney disease, anaemia, retained placenta, postpartum haemorrhage, sciatica, leucorrhoea, dysmenorrhea, kala-azar, encephalitis, rheumatoid arthritis, cancerous wounds, black water fever, malarial fever and ordinary fever. Leaf decoction is used against articular arthritis, hypotension and eczema. Phytochemical investigations of the ethanolic extract of the bark revealed the presence of high concentrations of alkaloids, flavonoids, steroids, terpenoids, cardiac glycosides, phenols, tannins and free amino acids. The prominent bioactive compounds identified are cis-3-Hexenoic acid, Cyclooctane, n-Hexadecanoic acid, 2-Nitrothiophene, 3-Methyl-2-butenoic acid, 2,6-Dimethyl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one and N-(3-Methoxyphenyl) 2,2- dimethylpropanamide. The bark also exhibited a good antibacterial activities. The findings validate the ethnomedicinal uses of the bark against several diseases.

11

IMPACT OF CLINICAL PHARMACIST ON DRUG RELATED PROBLEMS

A. Chandrakanth1, Mrs. P. Alekhya. Dr. U. Kishan, Dr. B.V.S Lakshmi
1Department of Pharmacy Practice, Malla Reddy College of Pharmacy, Maisammaguda, Secunderabad, Telangana.
2Department of General Medicine, Malla Reddy Hospital, Suraram, Rrangareddy Dist, Telangana.

Abstract

BACKGROUND: Drug related problems can be defined as any event or circumstance involving the drug treatment, which actually or potentially interferes with the patient in achieving an optimum outcome of medical care. MATERIALS AND METHODS: A prospective, observational and interventional study was carried out in the general medicine department of a tertiary care hospital. A total of 250 subjects admitted or treated between January-2015 to June-2015 were included in the study according to the study criteria. Patient data and prescription details were recorded and analyzed accordingly. Drug related problems (DRPs) were identified, patients were counseled about drug related problems and suitable clinical pharmacist recommendations were suggested to the clinical team in an attempt to prevent and/or resolve drug-related problems. RESULTS AND DISCUSSION: During the study period, a total of 250 patients were analyzed and found 154 DRPs in 52 patients. The most common DRP was found to be drug-drug interactions, 29 (55.79%), and most of them were moderately significant. The most common drug related problems was found to be drug interactions(55.79%)followed by adverse drug reaction(17.30%),and failure to receive drugs(13.46%), On identification of the DRPs necessary interventions were made in which frequently recommended intervention was drug duration change(28.8%), mostly for moderately significant interactions, followed by drug schedule and frequency change (23.07%)for ADR and major drug-drug interactions, then drug discontinuation(19.23%) for drugs prescribed for no indication, then drug addiction(11.53%). The acceptance rate of pharmacist recommendation was high 28.84% and the remaining 55.76% were not accepted. CONCLUSION: The study demonstrated that clinical pharmacist interventions were successful in identifying and rectifying the different types of drug related problems. Thus, the Clinical pharmacists function as catalysts in the multidisciplinary team highlighting the task of making a holistic assessment of drug therapy.

12

SPECTROPHOTOMETRIC DETERMINATION OF OLMESARTAN MEDOXOMIL USING SODIUM NITROPRUSSIDE AS CHROMOGENIC REAGENT

K. Sandhya Rani*, K. Raghu Babu, M. Srividhya
Department of Engineering Chemistry, AU College of Engineering (A), Andhra University, Visakhapatnam, Andhrapradesh, India.

Abstract

A simple, sensitive and cost effective visible spectrophotometric method was developed for the estimation of Olmesartan medoxomil in bulk and dosage forms. The method is based on the formation of purple red colored species with sodium nitroprusside –acetaldehyde reagent exhibiting maximum absorption at 552 nm. Beer’s law obeyed in the concentration range of 4 - 20 μg/ml. commercially available tablets were analysed, the results obtained by the proposed method were in good agreement with the labeled amounts. These methods are reproducible with an accuracy of ±1 %.

13

CIRCADIAN RHYTHMS AND THEIR ABNORMALITIES

Rahul Taneja, Dr. Ghanshyam Das Gupta*
Department of Pharmaceutical Research Div. ASBASJSM College of Pharmacy, Ropar, Punjab, India.
IK Gujral Punjab Technical University, Jalandhar.

Abstract

Pulsatile drug delivery system is the new approach to overcome patient non-compliance over commercially used dosage forms. These techniques also help in treating the disorders based on circadian paradigm. In this article, an attempt has been made to discuss the Chronotherapeutics approach to increase the efficiency of pharmacotherapy is the administration of drugs at times at which they are most effective and best tolerated. Biological plays a pivot role in the tolerance to any medicine given for the treatment of any disorder. This system enables the active drug for target action and inflated bioavailability with increased pharmacokinetic as well as pharmacodynamics profile of active moiety and also stated all the techniques involved in pulsatile system with their brand name. Various disease are discussed which is affected by circadian rhythm such as Cardiovascular disease, Diabetic, Alzhemier Disease, Parkinson’s Disease, Bronchial Asthma and Rheumatoid Arthritis. The author attract an attention to establish an importance of marketed pulsatile drug delivery technique in medical simultaneously in pharmaceutical Research & Development and the various disease associated with the pulsatile system of the body.

14

FORMULATION STRATEGIES FOR TASTE-MASKING OF CHEWABLE TABLETS

Bhusnure O.G.1, Shaikh F.E., Sugave B.K., Kavale B.S., Sayyed R.A., Hucche B.S.
Channabasweshwar Pharmacy College (Degree), Maharashtra, India.

Abstract

Chewable tablets which are required to be broken and chewed in between the teeth before ingestion. These tablets are given to the children who have difficulty in swallowing and to the adults who dislike swallowing. These tablets are intended to disintegrate smoothly in the mouth at a moderate rate either with or without actual chewing, characteristically chewable tablets have a smooth texture upon disintegration, are pleasant tasting and leave no bitter or unpleasant taste. Many active pharmaceutical ingredients (API) inherently possess a bitter taste. Nearly 20% of American adults surveyed complained of bad aftertastes or struggling to swallow when trying to take medication. If a medication is not palatable, the patient may opt to discontinue it. Failure to take medication as prescribed leads to increased morbidity, mortality, and potentially avoidable healthcare costs exceeding US$100 billion annually in the US alone. While objectionable taste may be one of several reasons for poor adherence, every measure that minimises these reasons helps. With a recognised impact on patient healthcare outcomes and costs, the European Medicines Agency (EMA) has released guidelines promoting the development of medicines for paediatric use. The US FDA is promoting similar initiatives. Taste-masking is incredibly important for paediatric populations as well as Geriatric patients. Firstly, children are 3-4 times as sensitive to tastes as adults, with increasing tolerance to bitter tastes with age. Secondly, children, particularly infants, are unable to rationalise ingestion of an unpalatable medicine. The most popular oral dosage forms include liquids, powders, granules, orally disintegrating tablets (ODT), and chewable tablets. Each one has pros and cons, depending on the target age group. Liquids, powders, and granules provide the greatest flexibility in dosing, provided there is a simple way to meter the powders. For solid oral dosage forms like orally disintegrating tablets and chewable tablets, break-lines can be included in the tablet design to adjust dosing. As a result, chewable tablets has seen an increased interest from the pharmaceutical industry in taste-masking technologies.

15

ENHANCEMENT OF SOLUBILITY AND RATE OF IN VITRO DRUG RELEASE PROFILES OF POORLY SOLUBLE TICAGRELOR BY SOLVENT EVAPORATION SOLID DISPERSION TECHNIQUE

K. Ramesh*1&3, B. Chandra Shekar2, P. Khadgapathi3

1Research Scholar, Pharmaceutical Sciences, JNTUH, Hyderabad, Telangana - 500072, India.

2Principal, Bomma Institute of Pharmacy, Allipuram, Khammam (D), Telangana - 507318, India.

3Executive Director, Hetero Labs Ltd, IDA, Jeedimetla, Hyderabad, Telangana - 500055, India.

Abstract

Ticagrelor is acts by interacting with platelet P2Y12 ADP receptor and prevent platelet activation. It is prescribed for reduction of rate of thrombotic cardiovascular events in patients suffering from acute coronary syndrome like unstable angina, non-ST or ST elevation myocardial infarction. Appearance of Ticagrelor is off-white to pale pink colored crystalline powder. It is belongs to BCS class IV molecule, poorly soluble and permeable. The absolute bioavailability of Ticagrelor is in range 30%-42%. The rate of drug release is a crucial and limiting step for drugs with low gastrointestinal solubility and low permeability for oral drug bioavailability. Among the different solubility enhancement techniques, solid dispersion of poorly soluble drug (s) in a hydrophilic carrier has been proven to be one of the most promising strategies for augmenting solubility and bioavailability. Hence, solubility and thereby in vitro drug release profiles were improved by formulating solid dispersions in hydrophilic polymers by solvent evaporation technique. There was an appreciable enhancement in solubility of Ticagrelor in solid dispersions as compared to solubility of plain drug substance. The rate of in vitro drug release from TSE8 was found to be similar and from TSE13 was on higher side against drug release profiles of BRILINTA® 90 mg Tablets in pH 3.0 Phosphate buffer with 0.2% Tween 80. The percentage of crystallinity of Ticagrelor has been reduced significantly within solid dispersion (TSE13), it has been confirmed by p-XRD. It can be concluded that solid dispersion by solvent evaporation might be an efficacious strategy for augmenting the therapeutic potential of Ticagrelor.

16

REVIEW ON PEPTIDOMIMETICS: A DRUG DESIGNING TOOL

Manish Kumar Pathak*1, Vibhu Jha1, Nem Kumar Jain2, Nikhil Shrivastava2, Nisha Yadav1, Deepayan Purukayastha1
1Department of Pharmaceutical Chemistry, School of Pharmacy, ITM University, Gwalior, M. P., India.
2Department of Pharmacology, School of Pharmacy, ITM University, Gwalior, M. P., India.

Abstract

Peptides show great pharmaceutical potential as active drugs and diagnostics in several clinical areas such as endocrinology, urology, obstetrics, oncology, etc. and as functional excipients in drug delivery systems to overcome tissue and cellular membrane barriers because availability of huge amounts of genomic and proteomic data can contribute for research in this area. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signalling, especially in living systems. The design of peptidomimetics can be viewed from several different perspectives and peptidomimetics can be categorized in a number of different ways. Study of the vast literature would suggest that medicinal and organic chemists, who deal with peptide mimics, utilize these methods in many different ways. This manuscript is an endeavour to discuss a variety of methodologies and strategies to develop and establish systematic tools for transformation of peptides into peptidomimetics or further into small drug-like molecules and their pharmacological activities having significance in modern drug design.

17

A REVIEW - FORMULATION & DEVELOPMENT OF ORODISPERSIBLE TABLET

Pradip Sonwane M*, Dr. Bhusnure O.G, Gaikwad V, Sayyed Sarfaraz Ali, Garkal Atul, Kamble Santosh
M. Pharmacy, CB Pharmacy College, Latur-413512.

Abstract

The oral route of drug administration is the most important method for administering drugs for systemic effects. Except in certain cases the parenteral route is not routinely used for self administration, e.g. insulin. The topical route of administration has only recently been employed to deliver drugs to the body for systemic effects. The parenteral route of administration is important in treating medical emergencies in which the subject is comatose or cannot swallow. Nevertheless it is probable that at least 90% of all drugs used to provide systemic effects are administered by the oral route. Oral route is presently the gold standard in the pharmaceutical industry where it is regarded as the safest, most economical and most convenient method of drug delivery resulting in highest patient compliance. Oral delivery of active ingredients include a number of technologies, many of which may be classified as Orodispersible tablets (ODTs). Usually, elderly people experience difficulty in swallowing the conventional dosage forms like tablets, capsules, solutions and suspensions because of tremors of extremities and dysphagia. In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. ODTs systems may offer a solution for these problems. Advancements in the technology arena for manufacturing these systems includes the use of freeze drying, cotton candy, melt extrusion, sublimation, direct compression besides the classical wet granulation processes. This has encouraged both academia and industry to generate new orally disintegrating formulations and technological approaches in this field. This article attempts at discussing the ideal characteristics, advantages and disadvantages, formulation aspects, formulation technologies and future potential of ODTs.

18

STUDY ON PRESCRIBING PATTERN AND UTILIZATION OF ANTIBIOTICS IN IN-PATIENTS OF THE MEDICINE DEPARTMENT OF A TERTIARY CARE TEACHING HOSPITAL, DAVANGERE, KARNATAKA

Chaitanya Kumar T1, Pappachan B1, John A1, Raj A A1, Sushilkumar PL1,2, Dr. Baishnab S1, Muneerudeen J1, Dr. Basavarajappa A P3
1Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka.
2R K University, Rajkot, Gujarat.
3Bapuji Pharmacy College, Davangere, Karnataka.

Abstract

The purpose of this study was to assess the prescribing pattern, utilization and rationality of antibiotics utilization in the patients.A retrospective observational study of the antibiotic prescription was carried out in the medicine department of a tertiary care teaching hospital, Davangere. 175 case records of the patients were identified, assessed, evaluated and analyzed for the rational use of antibiotics for a period of 6 months.In a total of 175 prescription, 73(41.7%) prescriptions were prescribed with single antibiotic, 69 (39.4%) and 24 (13.7%) prescriptions were given 2 and 3 antibiotics respectively and 9 (5.1%) prescriptions were given with 4 antibiotics. In majority of the prescriptions Cephalosporins were prescribed, 98 (56%) were treated with combination therapy and 77 (44%) were treated with monotherapy. In this study minor DDI’s were found to be more (11). Parenteral antibiotic formulations were mostly used than oral formulations. Out of 323 prescribed antibiotics 134 were Cephalosporins, among them, Ceftriaxone were prescribed to 105 (78.3%) patients, Cefixime was prescribed to 17 (12.6%) and Cefotaxime to 12 (8.9%).It was concluded that study provides insights into the patterns of antibiotic use and rationalizing prescribing practices. The active participation of clinical pharmacists in the clinical ward rounds and documentation of pharmacist observation on prescription in patient case sheets is highly recommended for safety drug monitoring.

19

OCIMUM SANCTUM (TULSI), EXCELLENT SOURCE OF PHYTOCHEMICALS

Rangita Tanwar*, Prof. Amiya Pahare, Dr. S. M. A. Naqvi
Guajarati Science College Indore (M.P.)
Swami Vivekananda Career Guidance Scheme, Dept. of Higher Education Govt. of M.P.
Islamia Karimia Science College Indore (M.P.)

Abstract

Phytochemicals are secondary metabolites, which are produced by medicinal plant. In Pharmacological studies, Ocimum sanctum is considered as important medicinal plant. It is commonly known as tulsi, belongs to family Lamiaceae. In traditional system of medicine, different parts (leaves, stem, flower, root, seeds and even whole plant) of Ocimum sanctum Linn. Have been recommended for the treatment of bronchitis, malaria, diarrhea, dysentery, skin disease, arthritis, eye diseases, insect bites and so on. The major aim of present study was to investigate the phytochemical screening of Aqueous and Methanolic extracts of Ocimum sanctum Leaves. Aqueous and Methanolic extracts were prepared and subjected to phytochemical screening in which the secondary metabolites were confirmed based on tests of coloration and precipitation. The leaves have shown the presence of all the phytoconstituents like carbohydrate, alkaloids, glycosides, phenolic compounds tannins, and flavanoids etc. Among the both extracts used, the methanolic extract of Ocimmum sanctum leaves was found to have accountable number of phytoconstituents. The results of the above studies support the use of this plant for human and animal disease therapy and the importance of the ethno-botanical approach as a potential source of bioactive substances.

20

ETHNO-MEDICINAL USE AND PHARMACOLOGICAL ACTIONS OF SOME OF THE DOMESTICALLY USED INDIAN SPICES – A REVIEW

Nisreen Husain1, Bhawana Pandey2
1Department of Zoology, Govt. Dr. W.W. Patankar Girls’ PG. College, Durg (C.G.).
2Department of Microbiology, Bhilai Mahila Mahavidyalaya, Bhilai, Durg (C.G.).

Abstract

A wide variety of plants commonly growing around us in the surrounding environment have been known for their medicinal values and traditional uses since ages. Their remarkable antioxidant properties and healing abilities provide health care to human beings. This helps in prevention of many chronic diseases and delay in early ageing. Thus, the medicinal plants form the major part of not only the traditional medicinal systems but also in modern pharmaceuticals. The present review focuses on the ethno-medicinal use and pharmacological actions of some of the very commonly used spices from the Indian homes, viz., Pepper, Cardamom, Clove, Cumin and Fenugreek seeds. All these plants are used for the cure of different diseases.

21

DEVELOPMENT AND APPLICATION OF LIQUID CHROMATOGRAPHIC METHOD FOR SIMULTANEOUS DETERMINATION OF CLARITHROMYCIN, TINIDAZOLE AND LANSPRAZOLE IN FIXED TABLET DOSAGE FORMS

Dr. Nemala Appala Raju, Mr. J. Raghu Ram, Dr. V. Kiran Kumar, Dr. Tulliballi Shyam
Sultan–Ul–Uloom College of Pharmacy, Hyderabad, Telangana State, India.
Unity College of Pharmacy, Bhongir, Nalgonda Distrtict, Telangana State, India.
Dr.Samuel George Institute of Pharmaceutical Sciences, Tarlupadu Road, Markapur-523 316.

Abstract

Anti H.pylori therapy consists of combination of antimicrobials like amoxycillin or clarthromycin and nitroimadazoles. Eradication of H.pylori concurrently with H2 blocker /PPI therapy of peptic ulcer has been associated with faster ulcer healing and lower relapse rate. Heligo® is a fixed-dose combination tablet kit containing Combipack containing 2 capsules of Lansoprazole 30 mg, 2 tablets of Clarithromycin 250 mg & 2 tablets of Tinidazole 500 mg. It is indicated for Eradication of H.pylori infection in patients with duodenal ulcers, gastric ulcer, chronic active gastritis and gastric non-nodgkin lymphoma of MALT. Chromatographic separation of the three drugs was achieved by using a gradient elution at a flow rate of 1.0 mL/min on Inertsil ODS 3V C18 column (250m×4.6mm, 5μm particle size, 100Å pore size) at ambient temparature. Mobile phase containing 0.2% Ortho-phosphoric acid in 1000 ml of water and 4 grm of Hexane sulphonic acid adjust pH: 2.5 with dilute KOH: Methanol (30:70 v/v). UV detection at 205nm was employed to monitor the analytes. A linear response was observed in the range of 25–275 μg/ mL for Clarithromycin, 62.2–746.4 μg/ mL for Tinidazole and 8.5-102 μg/ mL Lansaprazole. Limit of detection (LOD) for Clarithromycin, Tinidazole and Lansaprazole were 12.5 μg/mL, 0.622 μg/mL, and 1.75μg/mL respectively. Limit of quantification (LOQ) for Clarithromycin, Tinidazole and Lansaprazole were 37.5 μg/mL, 1.86 μg/mL and 5.1μg/mL respectively. The present study demonstrates the applicability of chromatographic method to develop a new, sensitive and robust RP-HPLC method for the simultaneous quantitative determination of three acive pharmaceutical ingredients in fixed pharmaceutical dosage form.

22

NANOGEL: A VERSATILE TARGETED DRUG DELIVERY SYSTEM

Miss.Vishakha S. Bidwai, Mr. Pranit S. Rane, Mrs. Swati G. Talele, Dr. Anil Jadhav
Sandip Institute of Pharmaceutical Sciences, Nashik, India.

Abstract

Nanogels are nanosized hydrogel particles formed by physical or chemical cross-linked polymer networks. The porous nanogels have been finding application as anti-cancer drug and imaging agent reservoirs. The advantageous properties of nanogels related to the ability of retaining considerable amount of water, the biocompatibility of the polymers used, the ability to encapsulate and protect a large quantity of payload drugs within the nanogel matrix, the high stability in aqueous media, their stimuli responsively behavior potential, and the versatility in release drugs in a controlled manner make them very attractive for use in the area of drug delivery. Nanoparticle-based medication can enhance the viability and security of certain anticancer medications. Nanogels based materials have high drug loading capacity, biocompatibility, and biodegradability which are the key points to design a drug delivery system effectively. A targeted nanogel can encapsulate a wide range of drug chemotypes, including biological, small molecule, and cytotoxic agents; display targeting ligands and polymeric coatings on the surface; enhance drug retention within the nanogel core after photo-cross-linking; and retain therapeutic activity after lyophilization allowing for prolong storage. This study shows that the curcumin is a multi-functional and pharmacologically safe natural agent having anti-inflammatory, anti-oxidative and anti-tumor properties.

23

PROSPECTIVE OBSERVATIONAL STUDY OF ASTHMA AND ITS MANAGEMENT

Bincy .T. Abraham, Sreeja .P .A, Anusreeraj .R .S, Divya .V, Haritha .S .B.
Department of Pharmacy Practice, Grace College of Pharmacy, Palakkad, Kerala, India.

Abstract

Asthma is an inflammatory disorder of the airways and lung tissue that varies in nature and severity overtime. It imposes a significant increase in the global prevalence, morbidity, mortality and economic burden over the past 40 years. The Study was carried out at Paalana Institute of Medical Science over a period of five months from July 2014 to December 2014. During the entire study period, a total of 90 patients were included of these, 54% were male and 46% were female. It is evident from the study that male population are more prone to asthma as compared to the females. Demographic analysis of data reveled that the most prominent age group were ‘41-50’ and ‘61-70’ years and both comprises of 25.5%. Out of the 90 cases, most patients identified and diagnosed as chronic OAD is accounted by 44.4% followed by acute exacerbation of OAD, which is about 35.5%. Since asthma patients often require more than one drug for control of symptoms hence multiple drug therapy were used. Overall drug therapy used in asthma management showed that the most commonly prescribedantiasthmatic drug were Corticosteroids 100% followed by combination of anticholinergic and short acting β2 agonist 94%, antibiotics 87% and methyxanthines 83% etc. In Corticosteroid therapy, systemic, IV as well as inhalers techniques were usedThus the present study will be more beneficial in improving asthma knowledge as well as current therapy awareness in the medical community.

24

ISOLATION, SPECTROSCOPIC CHARACTERIZATION AND SCREENING OF ANTIMICROBIAL ACTIVITY OF ISOLATED COMPOUNDS FROM LEAVES AND SEEDS OF CORDIA OBLIQUA AGAINST SOME ORAL PATHOGENS

Reenu Yadav1, Govind Mohan1, Ankur Choubey2, Udit N. Soni3, Jay Ram Patel3
1NIMS University, Jaipur (RJ).
2VNS Institute of Pharmacy, Bhopal (M.P.)
3Oriental College of Pharmacy, Bhopal (M.P)

Abstract

Development of bacterial resistance to presently available antimicrobial agents and their side effects has necessitated the search for new antimicrobial agent. Hence, here we searched for alternative and natural phytochemicals from plants used in traditional medicine are considered as good alternatives to synthetic chemicals. We report here the antimicrobial effect of various extracts and isolates from Cordia obliqua on oral pathogenic strains by zone of inhibition assay Cordia obliqua seeds and leaves extracts were evaluated for antimicrobial activity against some oral pathogenic strains of Gram-positive (Streptococcus mutans, S.mitis and S. sanguis) and Gram-negative (A. actinomycetemcomitans, P. gingivalis and B. forsythus) bacteria and fungal stain (Candida albicans) . The use of methanolic extract and isolated compounds from Cordia obliqua seeds and leaves as a potential antimicrobial agent in prevention and treatment of oral infections and diseases has been suggested. Methanolic extracts of the seed and leaves of the plant produced good inhibition zones against the test organisms, and ethyl acetate fraction of the extract shown significant significant activity

25

DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE DELIVERY SYSTEM OF LOSARTAN POTASSIUM

Shaikh Siraj*, Molvi Khurshid .I
Ali-Allana College of Pharmacy, Akkalkuwa Dist Nandurbar (MH), India.

Abstract

The objective of the study was to design and develop Gastroretentive dosage form for Losartan potassium using floating bioadhesive tablet approach with Polyox Wsr 1105 & HPMC K 4M polymers & sodium bicarbonate & citric acid as gas generating agents to reduce floating lag time. Optimization study was carried out by using 32 factorial design to prepare formulations. Vit E is added as a antioxidant for development of this gastroretentive dosage form of Losartan potassium by using Polyox to avoid stability risk associated with Polyox .The concentration of polymers was considered as independent variables whereas Swelling index, bioadhesive strength, % drug release at 10 hrs, of the tablets were utilized as dependent variables .Tablets were prepared by direct compression method. The prepared tablets were thoroughly evaluated for physical properties, floating, swelling, bioadhesive and in vitro release behaviors .The optimized F4 gastroretentive batch, gave floating lag time of 21±2 sec and with in vitro dissolution of 98.71 % in 12 hrs with appropriate bioadhesive property. After stability studies, no significant change was observed in floating lag time, bioadhesive strength, total floating duration and drug release rates. These results suggest that this floating bioadhesive gastroretentive dosage form is a promising approach for the oral delivery of Losarten potassium by improving its Gastric residence time for better management of hypertension.

26

FORMULATION DEVELOPMENT OF ROPINIROLE HYDROCHLORIDE MICROEMULSION FOR INTRANASAL DELIVERY

Shubhrajit Mantry1*, Anna Balaji2
1Institute of Pharmaceutical Sciences and Research Center, Bhagwant University, Ajmer, Rajasthan- 305004, India.
2Pathfinder Institute of Pharmacy Education & Research, Beside Mamnoor Camp, Khammam Road, Warangal, India.

Abstract

Objective: In the present day, an attempt was made to formulate and evaluate self-emulsifying Drug Delivery System of Ropinirole Hydrochloride for better treatment of Parkinson’s disease by improving its solubility profile and drug release of Ropinirole Hydrochloride from its formulations in conventional buffers. In general, Ropinirole Hydrochloride has bio availability of less than 50% because of its extensive first pass metabolism. It is very poorly available at the site of action for fast and immediate treatment. Thus formulated self-Emulsifying system of Ropinirole Hydrochloride avoids first pass metabolism and being more soluble and formation of fine, uniform microemulsion it shows better release profile in conventional buffers. Material and Methods: Experiments were performed with Ropinirole Hydrochloride as a drug, Sesame Oil, Sunflower Oil, Castrol oil, Elainic Acid (Oleic Acid), Tween 80, Tween 20, Span 20, Span 80, Methanol, Polyethylene glycol 400, Glycerin as surfactant and co-surfactant. Result: For the formulations F1 to F10 diffusion studies i.e. % Cumulative drug release vs. time (mins) were performed and its % cumulative drug release for all formulations was in between 83.57% to 99.93%in pH 6.6 buffer. Out of Ten formulations F2 showed the maximum % cumulative release of 99.93%. Conclusion: A series of emulsifying formulations were prepared with varying concentrations of Oil, Smix and water. Concentration of Castrol oil was varied from 4-70% (w/w) as an oil phase, Smix from 40-8% (w/w) which includes both Tween 80 and PEG 400 and water concentration which is varied in a concentration of 56-22% (w/w). Total of the Oil, Smix and water added up to 100% in each mixture. Each formulation was homogenized with the heat up to 45-50oC. Those compositions having % transmittance more than 70%.

27

FORMULATION AND EVALUATION OF A NEW LIPOSOMAL DRUG-IN-ADHESIVE PATCH FOR TRANSDERMAL DELIVERY OF SUMATRIPTAN SUCCINATE

M. Srujan Kumar1*, Anna Balaji2
1Institute of Pharmaceutical and Research Center, Bhagwant University, Ajmer, Rajasthan, India-305004.
2Pathfinder Institute of Pharmacy Education and Research, Warangal, Telangana, India-506005.

Abstract

The transdermal route of drug delivery has gained great interest of pharmaceutical research, as it circumvents number of problems associated with oral route of drug administration. In this study a transfersomal gel was fabricated using liposome-based nano carrier transfersome. Transfersomes as ultra-sfigurabile liposomes are prepared by rotary evaporation method with the composition of soyalecithin as lipid and propylene glycol as surfactant. Sumatriptan was selected as model drug for the treatment of migraine. Migraine is a chronic disease and the first line agents useful in treatment include NSAID’S and triptans .In recent years, most of the triptans have been designed to deliver the drug in the form of transdermal application to avoid gastrointestinal irritation, to overcome first pass effect and to maximize the drug concentration at the site of action. The present study describes the effect of sonication on size of transfersomes for future fabrication of transfersome into Lipo-drug-In-Adhesive Patch. Transfersomes were evaluated for vesicle size; polydispersity index, zeta potential, SEM, entrapment efficiency and transfersomal gel were evaluated for In Vitro Diffusion Studies. Optimized formulation of transfersomes are further are further fabricated into patch system. The prepared formulations were evaluated for various parameters like thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, in vitro drug release, in vitro permeation, kinetic modeling, adhesion properties and stability studies. Formulation T1 showed desirable permeation of about 99.15 at the end of 12 hours with transdermal flux of 9.288 (μg/cm2/h) and permeability coefficient 1.54 (cm/h) Patch system might follow zero-order kinetics as it was evident by correlation coefficients R2 (0.924), better fit than first order R2 (0.783) and Higuchi model R2 (0.991).