Volume 3 - Issue 3

S.NO Title & Authors Name page
1
IMPACT OF CYP3A5 AND P-gp POLYMORPHISMS ON THE PHARMACOKINETIC INTER-INDIVIDUAL VARIABILITY OF A SINGLE-DOSE OF A QUETIAPINE IMMEDIATE-RELEASE TABLET: A RANDOMIZED, OPEN-LABEL, TWO-PERIOD CROSSOVER STUDY IN HEALTHY JORDANIAN VOLUNTEERS
*Sireen Abdul Rahim Shilbayeh
 Abstract                  View                 Download                 XML
This study aimed to investigate the impact of the CYP3A5 and ATP-binding cassette sub-family B member 1 (ABCB1) C3435T polymorphisms on the inter-individual variability of quetiapine pharmacokinetics in a Jordanian population. Quetiapine plasma concentrations were measured in 34 healthy Jordanian Arabic volunteers. Twenty blood samples were collected over a 24-hour period following the administration of a 25 mg immediate release tablet. The pharmacokinetic parameters were determined from the plasma concentration-time profiles using the WinNonlin® software. The CYP3A5 and ABCB1 C3435T genotypes were determined by polymerase chain reaction. With regard to the CYP3A5 polymorphism, the *3*3 genotype carriers showed consistently higher exposure index values in comparison to the non-carriers, with differences ranging from 1.34- to 1.6-fold. While, the TT genotype subjects displayed a trend toward lower exposure and higher disposition (up to 2.2-fold) indexes when compared to the CC genotype carriers. These results may provide useful data that clinicians can utilize to optimize the quetiapine dose administered to psychotic patients.
415-425
2
INFLUENCE OF SEROTONIN TRANSPORTER-LINKED POLYMORPHIC REGION (5-HTTLPR) VARAINTS ON CLINICAL OUTCOMES IN THAI PATIENTS WITH DEPRESSIVE DISORDER
*Kamolwan Tantipiwattanaskul, Duangchit Panomvana, and Verayuth Praphanphoj
 Abstract                  View                 Download                 XML
The influence of the serotonin transporter polymorphisms on fluoxetine clinical outcomes was determined in 69 Thai patients with major depressive disorder. The results indicated that patients with l/l genotype had a significantly better response to fluoxetine treatment when compared with s allele carriers either evaluated based on the Thai HRS-D scores or psychiatrist efficacy evaluation (p = 0.001). At the same time, carriers with s allele had significantly higher rate of various side effects than the l/l genotype group (p = 0.002). These preliminary data might be used to reduce or prevent adverse effects and improve prescribing efficacy for depressive patients with different genotypes.&nbsp; <br />
426-430
3
BIOCHEMICAL EFFECTS OF THE SPECTRA DOSES OF SPARFLOXACIN ON HEALTHY ALBINO RATS
*Ukpo Grace E, Adevokhai Gladys I, Ehianeta Teddy S, Ebuehi Albert OT
 Abstract                  View                 Download                 XML
The fluoroquinolones have become an increasingly popular class of antibiotics for use in a variety of infections. This study investigated the effect of the spectra doses of sparfloxacin on the clinical chemistry parameters of healthy albino rats. The rats were evenly distributed into four groups such that each group had similar mean weights. Group 1 (control group) was administered 2.0 ml of 0.9% normal saline solution throughout the experimental duration. Group 2 (sub therapeutic dose) was administered a loading dose of 0.7 mg/kg body weight by oral route on day 1 and 0.35 mg/kg body weight p.o on days 2 to 7 while Group 3 (therapeutic dose) was administered a loading dose of 0.35mg/kg body weight p.o on day 1 and 0.175 mg/kg body weight p.o on days 2 to 7. Group 4 (toxic dose) was administered a loading dose of 3.5 mg/kg body weight p.o on day 1 and 1.75 mg/kg body weight p.o on days 2 to 7. The elevated levels of alanine aminotransferase (ALT) in the sub-therapeutic group are suggestive of liver-related malfunction or injuries to the liver parenchyma.&nbsp; It can also be seen that sub-therapeutic doses of sparfloxacin has some inductive effects on the ALTs but inhibitory effects by the toxic doses. Since no elevated levels of aspartate aminotransferase (AST) were seen in the treated groups, this suggests sparfloxacin is not hepatotoxic. There was no statistical difference in the creatinine levels of the control as well as all the treated groups. Thus it can be concluded that the renal function is not affected as serum creatinine level is a more reliable indicator of renal function
431-435
4
THERAPEUTIC APPROACHES FOR THE TREATMENT OF PULMONARY HYPERTENSION
*Diana Malaeb, Fouad Sakr, Mariam Dabbous
 Abstract                  View                 Download                 XML
Pulmonary hypertension is a progressive symptomatic fatal disease. It is a diagnosis of exclusion. The main goal of therapy is to lower pulmonary arterial pressure and pulmonary vascular resistance while preserving systemic pressure. Current treatments including calcium channel blockers, endothelin-1 antagonists, prostanoids, phosphodiesterase inhibitors, and prostacyclins. These treatments are palliative, may slow the progression of the disease, relief symptoms, and improve quality of life, but do not cure it. The article reviews the current updated therapeutic treatment, pharmacological action, doses, and adverse drug reaction.
436-441
5
IMPACT OF COUNSELLING IN INHALATION TECHNIQUE (ROTAHALER) IN CHRONIC OBSTRUCTIVE PULMONARY DISEASE PATIENTS
*Sweta Shrestha, Binaya Sapkota, Anurodh Ghimirey, Rajani Shakya
 Abstract                  View                 Download                 XML
Though inhaled medications are mainstay of therapy for COPD patients, assessment and training on rotahaler technique is lacking. Aim of study was to evaluate effect of counseling in inhalation technique of COPD patients focusing on essential items using combination of video and demonstration. 54 patients meeting inclusion criteria were included. On discharge day, baseline assessment of their technique was done using 8 item checklists. Training on&nbsp;&nbsp; rotahaler technique was given using video and demonstration. Immediate assessment of technique and necessary corrections were done. Final assessment was done after two weeks using same checklist. Comparison of scores at three time points was done. Average percentage of patients obtaining perfect score in essential checklist items prior instruction and after two weeks was 44.43% and 86.4% respectively. Relatively poor technique and best technique was seen at baseline and immediately after counseling respectively which slightly deteriorated after two weeks. Regular counseling and assessment with suitable teaching aids can improve inhalation technique of COPD patients. <br />
442-449
6
ANTIDEPRESSANT ACTIVITY OF THE HERBAL EXTRACT, KHAMIRA GAOZABAN AMBRI JADWAR OOD SALIB WALA
*Humera Ishaq, Raana Mahmood, Itrat Javed, TalatTariq, Iffat Mahmood
 Abstract                  View                 Download                 XML
Khamira Gaozaban ambri jadwar ood salib wala (KGA) is a traditional medicine in Southeast Asia, used as anxiolytic, antiepileptic and nervine tonic. We have evaluated its role as an anti-depressant agent in animal models of stress. We evaluated an anti-depressant activity by forced swim and marble burying method. 96 NMRI mice were randomly divided into Control group which received saline, a standard group which received Imipramine and two test groups which were given two doses 86 mg/kg and 170 mg/kg doses of KGA with different models of treatments. Each group consisted of 6 animals irrespective of sex. Results show pronounce anti-depressant effect both in acute (One day) and sub-acute (10 days) treatment with CMS (chronic mild stress) model and one day and 15 day treatments in marble burying test. Concluding results suggest strong anti-depressant activity of KGA in different treatment patterns.
450-456
7
PAXIL, WELLBUTRIN AND AVANDIA- A PERFECT COCKTAIL OF MEDICO MARKETING MALPRACTICE
*A. Shyam Sundar
 Abstract                  View                 Download                 XML
Pulmonary hypertension is a progressive symptomatic fatal disease. It is a diagnosis of exclusion. The main goal of Pharmaceutical industries play the central role in patient care through the process of drug discovery. The noble deed of discovering magic bullets to heal mankind is often neutralized by unethical medico-marketing strategies employed by the pharmaceutical industries. Disreputable acts such as misbranding, selective reporting, data dredging, misusing continuing medical education programs to provide tailored information lead to largest healthcare fraud settlement of US$3billion in the United States by GlaxoSmithkline LLC (GSK). This article analyses the indifferent medico-marketing practices of the pharma major for their products Paxil, Wellbutrin and Avandia. Candid efforts from the regulatory bodies, pharmaceutical industries and practicing doctors are the need of the hour to combat the menace of withholding safety data, illegal marketing which eventually results in poorer patient outcomes. <br />
457-461
8
EVALUATION OF ANTIOXIDANT ACTIVITY OF METHANOLIC EXTRACT OF THE BARK OF HOLARRHENA PUBESCENS, ITS FRACTIONS AND CONESSINE
*Bina S. Siddiqui, Syed Tahir Ali, Saima Tauseef, Saira Kamal, Ghazala H. Rizwani, Sabira Begum, and Aqeel
 Abstract                  View                 Download                 XML
The present study was carried out to investigate the antioxidant effect of the methanolic extract, its alkaloidal and non-alkaloidal fractions along with petroleum ether soluble, ether soluble and ethyl acetate soluble sub-fractions of non-alkaloidal part of the bark of Holarrhena pubescens. The pure compound conessine was also tested. The activity was determined by using DPPH free radical scavenging assay at 500 &mu;g/mL for the extract and the fractions, and at 200 &mu;g/mL for conessine and the standard (ascorbic acid). The non-alkaloidal fraction was found to be more active (63% inhibition; EC50 = 250 &mu;g / mL) than the alkaloidal fraction (16% inhibition) and its polar ethyl acetate soluble fraction was found to be most active (70% inhibition; EC50 = 250 &mu;g / mL). Conessine was non-active at the concentration used.
462-464
9
MALE WISTAR RATS RESPONSE TO KEROSENE EXPOSURE THROUGH DIFFERENT ROUTES: FOCUS ON ANTIOXIDANT INDICES
*Iyanda A. Ayobola
 Abstract                  View                 Download                 XML
Due to poverty, kerosene is widely applied for the treatment of a number of ailments in Africa. The impact of kerosene on antioxidant indices is therefore determined in Wistar rats. The experimental animals were divided into four groups (n=6). Trace quantity of kerosene (0.4 ml/kg body weight) was administered through oral, dermal or combined routes. At the end of 3 weeks of daily administration, activities of the antioxidant enzymes, levels of malondialdehyde and reduced and oxidized glutathione were estimated. Levels of oxidized glutathione and malondialdehyde were significantly elevated (p&lt;0.05); while the levels or activities of reduced glutathione and reduced glutathione/oxidized glutathione ratio (p&lt;0.05) as well as all the antioxidant enzymes were significantly decreased.&nbsp; The results of this suggest that trace administration of kerosene to male Wistar rats is capable of inducing significant oxidative stress and also support the same kind of observation earlier observed in female rats. <br />
465-469
10
Application and Validation of Two Smart Spectrophotometric and a HP-TLC Densitometric Methods for Determination of Metoclopramide Hydrochloride/ Paracetamol in Raw Material and in Pharmaceuticals
*Amira M. Hegazy, Nagiba Y. Hassan, Fadia H. Metwally, Mohammad Abdel-Kawy
 Abstract                  View                 Download                 XML
Currently the anti-emetic drug metoclopramide hydrochloride (MCP-HCl) is co-formulated with paracetamol (PCM). Three simple, economic and fast methods for determination of both drugs, simultaneously and without previous separation were developed. In first method (A), a third derivative spectrophotometric method was developed. The peaks amplitudes of third derivative spectra of MCP-HCl and PCM were measured at 334.5 and 299 nm, respectively. In second method (B), a ratio subtraction spectrophotometric method was developed. The peak amplitude of first derivative spectrum of MCP-HCl was measured at 321 nm at which PCM spectrum gives zero crossing point whereas the peak amplitude of ratio subtraction spectrum of PCM was measured at 292 nm.&nbsp; Both spectrophotomertric methods were linear within concentration range of MCP- HCl; 12-60 &micro;g/mL and PCM; 35-165 &micro;g/mL with&nbsp; high correlation coefficients.&nbsp; In third method (C), HP-TLC method was developed. The mobile phase composed of methanol, chloroform and conc. ammonia solution (10: 2: 0.15) gave typical chromatogram for MCP-HCl and PCM at Rfs 0.21 &plusmn; 0.02 &amp; 0.59 &plusmn; 0.02, respectively and the UV scanning was carried out at 270 nm. The method was linear within range of MCP- HCl; 6-18 &micro;g/mL and PCM; 5-50 &micro;g/mL giving high correlation coefficients. Complete validation process of the established methods was performed according to ICH guidelines and USP requirements and gave relative standard deviation values for all the key validation parameters less than 2.00%. <br />
470-481
11
HYPOTENSIVE, SPASMOLYTIC AND SPASMOGENIC EFFECT OF CYPERUS ROTUNDUS CRUDE EXTRACT AND ITS FRACTIONS
*Mansoor Ahmad, Mahayrookh, Mehjabeen, Asif Bin Rehman, Noor Jahan and S.I. Ahmad
 Abstract                  View                 Download                 XML
The main objective of present study is to explore the hypotensive and GIT effect of traditionally important plant Cyperus&nbsp; rotudus. Aqueous extract of C. rotundus caused a decrease in mean arterial blood pressure in anaesthetized Sprague-Dawley rats in a dose dependant manner. At the dose of 3 mg/kg the MAB was found to reduce by 42.6% from its control. This fall in the MABP was statistically significant (p&lt;0.0005). The increased dose of C. rotundus (10 and 30 mg/kg) showed a less reduction in the MABP (22.3% and 10.4% respectively). The crude extract and its fractions (ethylacetate, chloroform, n-butanol and aqueous) were analyzed for its spasmogenic and spasmolytic activity in vitro, on rabbit intestine and the effects were compared with standard drugs acetylcholine, adrenaline and atropine. The crude extract of C. rotundus exhibited highly significant (70.16%) relaxing action on smooth muscles in comparison to control and standard drugs. When it was fractionated except ethylacetate fraction which showed spasmolytic action all other fraction showed very strong spasmogenic activity (chloroform 83.87%, n-butanol 77.11% and aqueous 96.5%). It was also observed that spasmolytic activity was dominant in crude extract.
482-489
12
Establishment and validation of Two Smart UV-Spectrophotometric and a Novel Spectrodensitometric Methods for Simultaneous Determination of Metoclopramide Hydrochloride/ Pyridoxine Binary Mixture in Raw Material and in Syrup
*Amira M. Hegazy, Nagiba Y. Hassan, Fadia H. Metwally, Mohammad Abdel-Kawy
 Abstract                  View                 Download                 XML
Currently the anti-emetic drug metoclopramide hydrochloride (MCP-HCl) is co-formulated with pyridoxine (VB6). Three simple, economic and fast spectroscopic methods for determination of both drugs, simultaneously and without previous separation were developed. The first method is a ratio derivative spectrophotometry. The peaks amplitudes of first derivative spectra of MCP-HCl and VB6 were measured at 318.5 nm and 327.5 nm, respectively. The second one is an isosbestic point spectrophotometry. The peaks amplitudes of MCP-HCl and VB6 spectra were measured at 321.5 and 299.5 nm, respectively. The third method is spectrodensitomerty. The mobile phase was composed of benzene, methanol, glacial acetic acid, and acetone (10: 8: 0.5: 0.5; by volume). It gave typical chromatogram for MCP-HCl and VB6 at Rfs 0.2 &plusmn; 0.02 &amp; 0.51 &plusmn; 0.01, respectively and the UV scanning was carried out at 245 nm. Complete validation processes of the established methods were performed according to ICH guidelines and USP requirements.&nbsp; All methods were linear within wide concentrations ranges with high correlation coefficients.&nbsp; The proposed methods showed high accuracy, precision and selectivity results. Relative standard deviation values for all the key parameters were less than 2.00%. <br />
490-500
13
ASSESSMENT OF PATIENT SATISFACTION ON THE SERVICES PROVIDED BY COMMUNITY PHARMACIES IN AND AROUND PULIKKAL, KERALA
*Linu Mohan P, Shamna M, Dilip C, Abin C, Sajeev V Kumar, Sheron Joseph
 Abstract                  View                 Download                 XML
This study was planned to assess the patient satisfaction on the services provided by the community pharmacies at Pulikkal Panchayath &ndash; Kerala. A questionnaire was prepared with 10 questions which is helpful to measure the patient satisfaction level on the services like, availability of drugs, time taken for billing and dispensing, approach of pharmacist, advices on current health problem / general advices on medicine, location and layout of the pharmacy refund system, counselling service on side effects. A total of hundred filled questionnaire were collected back and the analysis of answers were done. Patients expressed that they were satisfied with the availability of the medicine in most of the pharmacies, and also the time taken for billing and dispensing of medicine. 38% of respondents were satisfactory in approach of the pharmacist. The locations of all pharmacies were very much convenient to the patient. Anyway most of the patients (37%) were not satisfied on services like advices on current health problem, general advices on medicine and the counselling service on side effects of drugs. Considering all the factors overall rating of the pharmacy was good (40%).
501-509
14
PRELIMINARY PHYTOCHEMICAL SCREENING OF CYCAS CIRCINALIS (L.) AND IONIDIUM SUFFRUTICOSUM (GING.)
*Senthil Kumar Babu, Vijaya kumar Jagadesan, Selvaraj Ramasamy, Panneer Selvi Gopalsamy
 Abstract                  View                 Download                 XML
India is one of the countries richly endowed with vast species of medicinal plants. The various bioactive phytoconstituents of the medicinal plants were identified and used for many chronic ailments. Cycas circinalis L. and Ionidium suffruticosum Ging. are the two herbs which were used in Indian medicine (Siddha) for improving the fertility of male. The present study involves the preliminary physicochemical, phytochemical analysis of the above said herbs. Physicochemical analysis involving ash values such as total ash, acid insoluble ash and water soluble ash for Cycas (8.12, 0.64, and 5.2 respectively) and for Ionidium (9.76, 0.94, and 5.6 respectively). The heavy metals such as lead, cadmium, mercury and arsenic were found to be within permissible limits in both the herbs. The powdered plant material of Cycas showed presence of alkaloid, flavonoids, amino acids and triterpenoids with percent yield of 40% in ethanolic solvent whereas Ionidium showed the presence of alkaloid, flavonoids, saponins, tannins, glycosides, amino acids and triterpenoids with percent yield of 32% in ethanolic solvent.
510-513
15
PHARMACOGNOSTIC, PHYTOCHEMICAL AND PHYSICOCHEMICAL STUDIES OF CURCUMA LONGA LINN. RHIZOME
*P.V. Kadam, K.N. Yadav, F.A. Patel, F.A. Karjikar, M. K. Patidar, M.J. Patil
 Abstract                  View                 Download                 XML
In recent year there has been rapid increase in the standardization of selected medicinal plant of potential therapeutic significance. Despite the morden techniques, identification of plant drug by Pharmacognostic study is more reliable. The rhizomes of Curcuma longa reported to have good medicinal values in traditional system of medicines. The present study deals with pharmacognostic parameters for the rhizomes of Curcuma longa which mainly consist of Macromorphology, Cytomorphology, Physico-chemical constants and Phytochemical screening. This information will be of used for further pharmacological and instrumental evaluation of the species and will assist in standardization for quality, purity and sample identification.
514-520
16
METHOD DEVELOPMENT AND VALIDATION OF IRBESARTAN AND HYDROCHLORTHIAZIDE BY RP-HPLC IN BULK AND PHARMACEUTICAL DOSAGE FORM
*Ramesh Bhukya, Elizabeth Y, Dhanalaxmi K, D. Nagarjuna Reddy
 Abstract                  View                 Download                 XML
A simple, precise, accurate and rapid reverse phase high performance liquid chromatographic method had been developed for simultaneous estimation of Irbesartan (IRBE) and Hydrochlorothiazide (HCTZ) in bulk and Pharmaceutical dosage form. A Phenomex Luna C-18 column having I&rsquo;d of 150&times;4.6 mm and 5&micro;m particle size was used. The method was carried out in gradient program using mobile phase, 0.02M Potassium dehydrogenate orthophosphate: acetonitrile (60:40 v/v) adjusted to pH-3.4 using dilute ortho phosphoric acid. Flow rate was adjusted to 1.0ml/min and effluents were monitored at 224nm. The retention time obtained for Irbesartan and HCTZ was 2.59 &amp; 8.13min respectively. The calibration curves were linear in the concentration range of 100-300&micro;g/ml for Irbesartan and 50-150&micro;g/ml for HCTZ. The developed method was validated in accordance to ICH guidelines.
521-526
17
FORMULATION AND EVALUATION OF LORNOXICAM AS MUCOADHESIVE MICROCAPSULES
*Varun Sharma, Bharat Parashar, Abhisekh Chandel and Ajay Chandel
 Abstract                  View                 Download                 XML
The microencapsulation has a major role in solving the problems regarding targeting of drug to a specific organ tissue and controlling the rate of drug delivery to the target site. Microencapsulated drug delivery system plays a major role in developing oral controlled release systems. The objective of this work was to discuss how the efficiency of drug delivery can be increased and also how the release of drug and drug targeting can be improved. This work provides the thorough literature review of different techniques involved in microencapsulation and evaluation parameters of microencapsulation process. Various formulations were developed by using release rate controlling and gel forming polymers like HPMC-5 and HPMC-15. From among all the developed formulations, F3 formulation with HPMC-5 sustained the drug release for longer period of time as compared to other formulations. So, F3 formulation with HPMC-5 was selected as the best formulation. It was concluded that the release followed Zero order kinetics. Thus, best formulation satisfied physicochemical parameters and in vitro drug release profile requirements for a sustained drug delivery system.
527-533
18
METHOD DEVELOPMENT AND VALIDATION OF SIMULTANEOUS ESTIMATION OF ROSUVASTATIN AND OLMESARTAN IN BULK AND TABLET DOSAGE FORM BY RP-HPLC
*Elijabeth.Y, Ramesh.B, K.Dhanalaxmi, Nagarjuna reddy
 Abstract                  View                 Download                 XML
A simple, precise, accurate and rapid reverse phase high performance liquid chromatographic new method had been developed for simultaneous estimation of Rosuvastatin and Olmesartan in bulk and tablet dosage form. An Agilent XDB, C18 column having I&rsquo;d of 150&times;4.6 mm and 5&micro;m particle size was used. The new method was carried out in gradient program using mobile phase, 0.01M Potassium Dehydrogenate orthophosphate: acetonitrile (55:45 v/v) adjusted to pH-3.2 using dilute ortho phosphoric acid. Flow rate was adjusted to 1.0ml/min and effluents were monitored at 240nm. The retention time obtained for Rosuvastatin and Olmesartan was 2.61 and 5.13min respectively. The calibration curves were linear in the concentration range of 10-30&micro;g/ml for Rosuvastatin and 50-150&micro;g/ml for Olmesartan. The developed method was validated in accordance to ICH guidelines.
534-539
19
FORMULATION AND CHARACTERIZATION OF AMPHOTERICIN B LIPOSOMES PREPARED BY THIN FILM HYDRATION METHOD
*Arvind G, Sumit Shah, Shanmukha Mule, Prashanth P, Noveen Konda
 Abstract                  View                 Download                 XML
Amphotericin B is a polyene antifungal drug used intravenously for systemic fungal infections. Simple solution of amphotericin B is having many side effects while liposomal amphotericin B preparations exhibit fewer side-effects having similar efficacy. Various preparations of liposomal amphotericin B have recently been introduced and all of these are more expensive than plain amphotericin B. Fungisome and Abelcet are liposomal complex formulation of amphotericin B and being the latest and cheapest addition to the lipid formulations of amphotericin B. AmBisome is a liposomal formulation of amphotericin B for injection which is having less side effects as compared to all other formulations of Amphotericin B. Liposomal formulation of amphotericin B for injection, prepared by thin film hydration technique was selected in the present study. Different formulations variables (solvents ratio and pH of complex formation) and process variable (numbers of homogenization cycles) were carried out to control the impurities levels and particle size of liposomes. Formulation prepared at pH 3.0 with 1:2 solvent ratio (Methanol: Chloroform) was given least impurities. Formulation prepared at 1400 bar pressure with 15 homogenization cycles was shown desire particle size.&nbsp; The optimized formulation was exhibited more than 90% release of drug for a period of 7 days. The stability study (40&plusmn;2&deg;C/ 75&plusmn;5% RH) of the Amphotericin B liposomes was evaluated for 3 months and it was found to be stable.<br /><br />
540-547
20
FORMULATION AND IN VITRO - IN VIVO EVALUATION OF BILAYER FLOATING-BIOADHESIVE FAMOTIDINE TABLETS
*Prabha A. Singh, Amrita Narayan Bajaj, Anjali Harikrishna Singh
 Abstract                  View                 Download                 XML
Bilayer floating-bioadhesive drug delivery systems exhibiting a unique combination of floatation and bioadhesion to prolong gastric residence time were developed. Hydroxypropyl methylcellulose and sodium bicarbonate were added such that when immersed in 0.1N HCl, the tablet expands and rises to the surface and famotidine is gradually released without interference from gas bubbles. Effect of different ratios of drug: polymer on in vitro release profile was investigated. Developed tablets were evaluated for uniformity of weight, hardness, friability, drug content, buoyancy and floating lag time. Time buoyancy curve, detachment force and swelling index were evaluated. Antiulcer activity of famotidine tablets was assessed by inducing ulcers in fasted rats by ethanol and indomethacin. Measurement of gastric contents was carried out by ulcer induced pylorus liagated rats. Prepared tablets exhibited satisfactory physico-chemical characteristics. The tablet swelled radially and axially during in vitro buoyancy studies. From the buoyancy kinetic curve it was observed that bilayer tablet started floating in less than 10 minutes and remained buoyant for 12h. In vivo antiulcer studies exhibited that developed formulation showed comparable percent inhibition of ulcers to standard in both gastric ulcer models. Gastric pH was significantly reduced showing decreased acid output. Thus floating-bioadhesive systems exhibited independent regulation of buoyancy and drug release and in vivo studies showed good antiulcer efficacy confirming potential of floating-bioadhesive tablets as drug delivery system for prolonging gastric residence and enhancing local effect of famotidine.
548-555
21
FORMULATION AND IN-VITRO EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOFLOXACIN
*Satyabrata Bhanja, Parthasarathi Mishra, Sudhakar Muvvala, Arun Kumar Das
 Abstract                  View                 Download                 XML
The present study aimed to formulate and evaluate sustained release matrix tablets of levofloxacin to achieve sustained drug release with reduced side effects and improved patient compliance. Different batches of sustained release matrix tablets of levofloxacin were prepared by direct compression method using HPMC, sodium CMC and sodium alginate as polymers, Avicel PH 102 (MCC) as filler and starch as binder. The prepared tablets were evaluated for hardness, weight variation, friability, drug content uniformity, in vitro drug release, in vitro drug release kinetics and Acceralerated stability studies. It was found average hardness of the tablets to be in range 6.7&plusmn; 0.04 to 7.7 &plusmn; 0.35 kg/cm2. The friability of the prepared tablets was found in the range of 0.005&plusmn;0.034 to 0.6&plusmn;0.035 %. The uniformity of drug levofloxacin present in tablets formulation ranged from 96.84 &plusmn; 0.16 to 98.87 &plusmn; 0.34%. The in vitro drug release was studied by using pH 1.2 acidic buffer for 24 hours. Among all twelve formulations F1 to F12, the best formulation F4 was found to be 99.5% drug release in 24 hours which showed the sustained action drug release. The formulations F1 to F12 followed first order release kinetics with non fickian diffusion mechanism. <br />
556-564
22
FORMULATION AND CHARECTERIZATION OF IN SITU IMPALNT OF OCTREOTIDE ACETATE
*Prashanth P, Sumit Shah, Arvind G, Naveen Konda
 Abstract                  View                 Download                 XML
Octreotide is the acetate salt of a cyclic octapeptide. It is a long-acting octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin. The peptide drugs after oral and parental administration the poor bioavailability in the blood due to their short biological half &ndash;lives caused by their metabolic instability. so that these peptide drugs are formulated by polymeric drug delivery systems such as micro particles or implants, has been proposed enabling their sustained&nbsp; release after a residence time in the polymer which protects the peptide against enzymatic and hydrolytic influences of biological media. In the present study, In situ implants of Octreotide acetate were prepared by polymer precipitation method. PLGA is dissolved in hydrophilic solvents such as Dimethyl sulphoxide, N-Methyl 2-pyrrolidone, PEG-200 and Triacetin until the formation of a clear solution. Different formulations were prepared using different concentration of polymer i.e. 5to35 % w/w. The characterization of implant was carried out by Determination of PLGA 5050 polymer ratio by NMR, Determination of molecular weight of polymer by GPC, Viscosity of polymer solution, Sterility test, In-vitro drug release, Release kinetics and Scanning electron microscopy. The Maximum percent of drug release with minimum Initial Burst release was found in formulation (F3) with NMP as solvent. Effect of gamma irradiation on molecular weight of polymer, viscosity of polymer solution, monomer ratio of lactide and glycolide and in-vitro release after gamma radiation was studied with F3 formulation.
565-573
23
NOVEL SPECTROPHOTOMETRIC METHODS FOR THE ASSAY OF NATEGLINIDE IN PURE AND DOSAGE FORMS
*Ch. Sudheer, T.Tirumaleswara Rao, B.V.Sreenivasulu, C. Ramababu
 Abstract                  View                 Download                 XML
Two simple, sensitive and selective methods for the determination of Nateglinide in bulk and in pharmaceutical formulations were described. These methods are based on extraction of this drug into chloroform as ion-pair with basic dyes, Safranin O (SFNO) and Methylene blue (MB). The optimum conditions of the reactions of the developed methods were studied and optimized. The absorbance of the colored products was measured at 515nm for nateglinide-SFNO and 620nm for nateglinide-MB. The calibration curves obeyed the beer&#39;s law over the concentration range of 2.5-12.5&mu;g/mL for nateglinide-SFNO and nateglinide-MB with correlation (r2=0.9997 &amp; 0.9992) respectively. The results of analysis for the two methods have been validated statistically and by the recovery studies. The proposed methods were simple, sensitive and economical for the quantitative determination of nateglinide and were successfully employed for the assay in bulk and in formulations.
574-578
24
FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF LORNOXICAM
*Jyothi Rani L, K. Abbulu, Nagabushan Rao T, A Akhila
 Abstract                  View                 Download                 XML
Mouth dissolving tablets are also known as fast disintegrating, fast dissolving, fast melt, quick melt tablets. Lornoxicam is an NSAID with 100% bioavailability having a bitter taste. So by formulating it as an ODT the absorption and the bioavailability of the drug will fasten and hence the action of the drug will be faster .The mode of action of Lornoxicam is mainly by inhibition of prostaglandin synthesis (inhibition of cyclooxygeanase enzyme). So the purpose of the present work is to formulate a taste masked mouth dissolving tablet of Lornoxicam. Taste masking was done by using Eudragit (EPO 100) in different ratios. Three superdisintegrants were used namely sodium starch glycolate, crospovidone, crosscarmellose sodium. The tablets were evaluated for various parameters like hardness, friability, drug content, disintegration and in vivo dissolution. Among all the formulations F5 showed 98% drug release with in 15 min. So it was considered as best formulation.&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp; <br />
579-586
25
FORMULATION AND EVALUATION OF SUSTAINED RELEASE TABLETS OF VILDAGLIPTIN
*Vishnu P, Shireesh kiran R, Chaitanya B, Naveenbabu K, Vijayavani Ch. S.
 Abstract                  View                 Download                 XML
The purpose of this research work was to establish Vildagliptin sustained release matrix tablets of&nbsp; 50mg. Vildagliptin is an anti diabetic drug of the new dipeptidylpeptidase-4 (DPP-4) inhibitor class of drug. The tablets were prepared by wet granulation technique using different grades of Hydroxy Propyl Methyl cellulose (HPMC K 100 LV, HPMC K15M and HPMC K4M) as extended release polymer. Tablets were evaluated for different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies and FT-IR studies. The physico-chemical property of the finished product compiles with the internal specification limits. In vitro release from the formulation was studied as per the USP and IP dissolution procedure. The formulation gave a release of 98.5 % for 24 hr and the data best fitted into Higuchi model.&nbsp; From the present study it was concluded that the vildagliptin sustained release tablets can extend drug release and improve the bioavailability of vildagliptin. <br />
587-593
26
Analytical Method development and Method validation for the simultaneous estimation of Metformin HCL and Linagliptin in Bulk and tablet Dosage Form by RP-HPLC Method
*A. Janardhan Swamy, K. Harinadha Baba
 Abstract                  View                 Download                 XML
A rapid, highly sensitive, economical and accurate RP-HPLC method was developed for simultaneous estimation of Metformin HCL and Linagliptin in Bulk and Pharmaceutical Dosage form. The separation was achieved by Hypersil C18 column (250 &times; 4.6 mm, 5 &mu; particle size) with mobile phase consisting of phosphate buffer (pH 5.6, diluted with orthophosphoric acid), methanol and acetonitrile in the ratio of 40:5:55 v/v, using flow rate 1.0 mL/min and eluents monitored at 233nm .The developed method was validated as per ICH guidelines for specificity, linearity, precision, accuracy, robustness, limit of detection and limit of quantification. The retention times of Linagliptin and Metformin were 5.4 and 6.6 min respectively. The linearity was found to be in the range of 125-750 &mu;g/mL and 0.625-3.75 &mu;g/mL for Metformin and Linagliptin respectively, had regression coefficients (R2) 0.999. The proposed method was successfully applied for simultaneous estimation of both drugs in Pharmaceutical formulation.
594-600
27
A VALIDATED RP-HPLC METHOD FOR DETERMINATION OF ALISKIRIN AND AMLODIPINE IN TABLET DOSAGE FORM
*Venkata Raveendra Babu Vemula, Pankaj Kumar Sharma
 Abstract                  View                 Download                 XML
A simple, accurate, rapid, precise, specific and cost effective reverse phase high performance liquid chromatography (RP-HPLC) method have been developed and subsequently validated for simultaneous estimation of Aliskiren and Amlodipine in pharmaceutical dosage forms. Chromatography is carried out isocratically at 30&deg;C &plusmn; 0.5&deg;C on an Water&rsquo;s X-bridge C-18 column (4.6 x 150mm, 5&mu; particle size) with a mobile phase composed&nbsp; of&nbsp; acetonitrile -phosphate&nbsp; buffer&nbsp; (pH-2.5)&nbsp; (40:60, v/v)&nbsp; at&nbsp; a&nbsp; flow rate&nbsp; of&nbsp; 1.0&nbsp; mL/min. Detection&nbsp; was carried out using a PDA detector at 230 nm. Parameters such as linearity, precision, accuracy, recovery, specificity and ruggedness are studied as reported in the International Conference on Harmonization guidelines. The retention times for Aliskiren and Amlodipine are 3.8 min and 5.1 min respectively. The linearity range for Aliskiren and Amlodipine are 18.75-187.5&micro;g/ml and 1.25-12.5 &micro;g/ml respectively. The correlation coefficients for both components are close to 1. The relative standard deviations for six replicate measurements of samples in tablets are always less than 2%.
601-606
28
DEVELOPMENT AND VALIDATION OF RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF ROSUVASTATIN AND FENOFIBRATE IN BULK AND TABLET DOSAGE FORM
*S. Thukabai, V. Uma Maheshwara Rao and Muhammad Rafi Shaik
 Abstract                  View                 Download                 XML
A new precise, accurate, reliable validated method for the determination of Rosuvastatin and Fenofibrate has been developed by using reverse phase high performance liquid chromatography (RP-HPLC) in pharmaceutical dosage form. Chromatographic separation was carried out by using mobile phase 0.01M Potassium dihydrogen phosphate: methanol (55:45v/v, PH-2.6 adjusted with Orthophosphoric acid) on Agilent XDB C18 (150 x 4.6 mm, 5&#61549;) at a flow rate 1ml/min with UV detection at 220nm.The retention times for Rosuvastatin and Fenofibrate were 2.36 and 5.80 min respectively and both drugs showed good linearity in the range of 5-20 &micro;g/ml and 80-320 &micro;g/ml. The proposed method has been successfully applied to pharmaceutical formulation and was validated according to ICH guidelines and method showed good precision with percentage relative standard deviation less than 2%. The percentage recovery for Rosuvastatin and Fenofibrate was found between 99.06-100.94% and 99.12-100.95% respectively indicating the proposed method was accurate and precise.
607-612
29
FORMULATION AND EVALUATION OF LAMIVUDINE AND TENOFOVIR DISPROXIL FUMARATE IR TABLETS
*Patil Sagar Nanaji, Swati Shailendra Rawat, D. Yashwanth Kumar
 Abstract                  View                 Download                 XML
The main objective of the present study is to formulate and evaluate an immediate release tablet of Lamivudine and Tenofovir Disproxil Fumarate using different disintegrants. Lamivudine and Tenofovir Disproxil Fumarate belong to class of anti-retroviral drugs known as nucleotide analogue reverse transcriptase inhibitors. Pre formulation studies were performed prior to compression. The tablets were compressed using microcrystalline cellulose, crospovidone, crosscarmallosesodium, magnesium stearate and Aerosil. The fabricated tablets were evaluated for various micrometric properties like bulk density, tapped density, compressibility index, Hausner&rsquo;s ratio, angle of repose and post compression characteristics like thickness, hardness, friability, disintegration time and drug release. Crospovidone is found to be the better disintegrant when compared to crosscarmallosesodium in the formulation of immediate release tablets of Lamivudine and Tenofovir Disproxil Fumarate. The absorbance of Lamivudine and Tenofovir Disproxil Fumarate were screened in the UV region and the maximum absorbance was found to be 271 nm and 260nm respectively and this was used for UV analysis. Among the six different formulations developed F6 was found to be the best one with a drug release of 99.96% at the end of 30min. <br />
613-617
30
MICROANATOMICAL DEFORMATION AFTER PTZ INDUCED SEIZURE IN MICE BRAIN
*Pankaj Kalita, Manash Barthakur
 Abstract                  View                 Download                 XML
Seizure is an abnormal state of brain electrical activity. The causes of seizure are different but seizure can be induced artificially also. Present experiment was conducted on albino mice and seizure was induced by Pentamethyline tetrazole (PTZ). Duration of seizure was maintained more than half an hour. Mice were sacrificed by cervical dislocation and brain was removed. Brain was fixed in Carnoy&rsquo;s fixatives and sectioned at 5 micron thickness. Histological slide was stained in H&amp;E stain. Micro-anatomical deformation of brain was observed in treated animals. Simultaneously control group of mice was maintained in same laboratory conditioned. Loss of cellular architecture in the neocortex I remarkably observed.&nbsp; Excitatory neurotransmitter overloaded in axon terminal may be responsible for neuronal degeneration.
618-620
31
DEVELOPMENT AND VALIDATION OF NOVEL HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF CEFIXIME AND MOXIFLOXACIN IN COMBINED TABLET DOSAGE FORM
*B. Raja, A. Lakshmana Rao
 Abstract                  View                 Download                 XML
A simple, rapid, accurate and precise RP-HPLC method has been developed and validated for simultaneous estimation of Cefixime and Moxifloxacin in combined tablet dosage form. The chromatographic separation was carried out on Hypersil BDS C18 column (100 x 4.6 mm; 3 &micro;) with a mixture of phosphate buffer pH 6.0: acetonitrile (75: 25 V/V) as a mobile phase; at a flow rate of 1.0 mL/min. UV detection was performed at 293 nm. The retention times were 2.374 min and 5.776 min for Cefixime and Moxifloxacin respectively. Calibration plots were linear (r2=0.999) over the concentration range of 5-30 &micro;g/mL for both Cefixime and Moxifloxacin. The method was validated for linearity, accuracy, precision, specificity and sensitivity. The proposed method was successfully used for quantitative analysis of Cefixime and Moxifloxacin tablets. No interference from any component of pharmaceutical dosage form was observed. Validation studies revealed that the method is specific, rapid, reliable and reproducible. The high recovery and low relative standard deviation confirm the suitability of the proposed method for routine estimation of Cefixime and Moxifloxacin in pure sample and tablet dosage forms.
621-627
32
INVITRO ANTIOXIDANT ACTIVITY OF METHANOLIC EXTRACT OF SACCHARUM SPONTANEUM
*M. Sai Krishna, K. Naga Sravanthi, G. Sreenika, S. Chaithanya, M. Sudhakar
 Abstract                  View                 Download                 XML
Biomolecules can be oxidized by free radicals which results in oxidative stress. This oxidative damage has an important etiological role in aging and development of diseases like cancer, atherosclerosis, and other inflammatory disorders. Synthetic antioxidants, like Butylated hydroxyl anisole, Butylated hydroxyl toluene are good free radical scavengers. However, synthetic antioxidants can be carcinogenic. Therefore, there is an increasing interest in searching for antioxidants of natural origin. We report here the in vitro antioxidant activity of methanolic extract of S. spontaneum. The activity of S.spontaneum has been tested using various antioxidant models viz., total phenolic and flavonoid content, estimation of DPPH, nitric oxide,&nbsp; superoxide and hydroxyl radical scavenging activity at different concentrations. This study indicates significant free radical scavenging potential of S.spontaneum which may be due to the presence of high Phenolic and Flavonoid content.<br />
628-633
33
A VALIDATED STABILITY-INDICATING HPLC METHOD FOR DETERMINATION OF TICAGRELOR IN BULK AND ITS FORMULATION
*L. Kalyani, A. Lakshmana Rao
 Abstract                  View                 Download                 XML
A simple, rapid, accurate and precise stability-indicating HPLC method was developed and validated for the determination of Ticagrelor in bulk and its tablet dosage forms. Separation of the drug was achieved on Hypersil BDS C18 column (100 mm x 4.6 mm, 5 &micro;) as stationary phase with mobile phase consisting of phosphate buffer pH 3.0 and acetonitrile in the ratio of 70: 30 V/V. The method showed a good linear response in the concentration range of 22.5-135 &micro;g/mL with correlation coefficient of 0.999. The flow rate was maintained at 1.0 mL/min and effluents were monitored at 254 nm. The retention time was 3.215 min. The percentage assay of Ticagrelor was 99.9%. The method was statistically validated for accuracy, precision, linearity, ruggedness, robustness, solution stability, selectivity and forced degradation studies. The results obtained in the study were within the limits of ICH guidelines and hence this method can be used for the determination of Ticagrelor in pharmaceutical dosage forms.
634-642