INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES

693-705

Authors: Ganesh Kumar Bhatt* Ashish Rawat, Preeti Kothiyal

In today’s world about 74% of drugs are taken orally and are found not to be as effective as desired in the present scenario. So to overcome or to improve such character transdermal drug delivery system was emerged in form of transdermal patches. Transdermal drug delivery represents the most rapidly advancing areas of novel drug delivery. To overcome the difficulties of drug delivery through oral route easier way was introduced known as transdermal drug delivery system for example poor bio-availability, first pass metabolism and sometime responsible for rapid blood level. The present study was carried out to develop transdermal patches of prazosin hydrochloride with different ratio of HPMC (hydroxyl propyl methyl cellulose), EC (ethyl cellulose) by solvent casting method. Propylene glycol 3% is used as a plasticizer and Span 80 as permeation enhancer. The recognition of drug and the possible drug polymer relations were studied by FTIR spectroscopy. Formulated transdermal patches were evaluated with regard to physicochemical characteristics (thickness, folding endurance etc.) and In-vitro permeation studies were performed using Franz diffusion cell. The figures obtained from in- vitro permeation studies was treated by different conventional mathematical models (zero order, first order, Higuchi and Korsmeyer- peppa’s) to determine the release mechanism from the transdermal patches formulations. Selection of a appropriate release model was based on the values of R2 (correlation coefficient), k (release constant) obtained from the curve fitting of release data. It was found that all the formulations follow the first order kinetics. The regression coefficients (R2) for the all formulations F1 to F4 of Higuchi plot was found to be almost linear. Keywords: Transdermal patches, prazosin hydrochloride, Permeation enhancer, In-vitro permeation study.

706-712

Authors: Tushar V. Ahire1*, Avish D. Maru1, Mitesh P. Sonawane1, Prasad S. Bhamare1, Kiran B. Erande2

Albendazole oral jellies using suitable natural and synthetic polymer as gelling agent with different concentrations. The benefits of these prepared jellies are increased bioavailability by-passing first pass metabolism. jellies were prepared by dispersing the gelling agent in water. Physical characteristics, pH, in vitro % drug release kinetics, content uniformity, spreadability, viscosity, IR spectral analysis, and stability studies were conducted.The prepared jellies of Albendazole found to be stable and there has no significant change in physical appearance, pH, viscosity etc. Thus, the study confirmed that the Albendazole oral jelly can be used as a possible alternative to recently available oral formulations. The prepared formulations are free from sugar crystals. Among the prepared formulation, formulation F2 (96.21%) and F10 (98.44%) respectively released in 30 min. was found to be promising. Stability studies, pH, viscosity, spreadability, on the promising. IR spectroscopic studies indicate that there were no drug-excipients interactions. keywords: Albendazole jellies, gelling agents , etc.

728-733

Authors: Dr. S. S. Thakare*, Mr. S. P. Kakad

A method is presented for the synthesis of selective derivatization of quinazoline by controlling the temperature and solvent concentration, 2,4-dichloro-7-nitroquinazoline reacted with different amines to form the selective 2-chloro-Nalkyl-7-nitroquinazolin-4-amines by chloro amine reaction, The products have been characterized through the usual chemical transformations, IR, NMR and mass spectral analyses. Keywords: Quinazoline derivative, 5, 6 dichloride 7-nitro quinazoline, chloro amine coupling, dihydroxy compound

750-755

Authors: Y.Sirisha*1, Udaya Chandrika. P2, Dr. A. Srinivasa Rao3

In the present research work Frovatriptan drug was formulated as Fast dissolving Thin oral films by solvent casting method. Triptans are a class of anti migraine drugs which are formulated to give rapid relief from migraine attacks. Previously prepared in the form of tablets which has certain disadvantages so are formulated as films which disintegrate rapidly within in seconds in the mouth without need of water. The films were prepared by employing Frovatriptan drug, Hydroxy Proipyl Methyl Cellulose (HPMC E5) as polymer, Isopropyl alcohol was employed as solvent, Propylene glycol as plasticizer, Mannitol as diluents and aspartame as sweetening agent. The films were evaluated for parameters like Weight uniformity, Morphological properties Thickness uniformity, Folding endurance, Surface pH, Drug content uniformity test, In-vitro disintegration test, In-vitro dissolution studies which were found to be satisfactory. Among all the formulations F8 has found to be the best formulation with a disintegration time of 12sec and 100% of cumulative drug release within in 20min. Thus it indicates that Frovatriptan is highly suitable to be formulated as Fast dissolving thin oral films for their rapid release and immediate treatment of migraine attack. Keywords: Frovatriptan, HPMC E5, Maltodextrin, Mannitol, Propylene glycol, Aspartame.

759-766

Authors: Naresh Kshirasagar* Sriram Pavani, D Adukondalu, J.Kishan Pavani

Naratriptan hydrochloride, a piperidine derivatives selective agonist of serotonin, binds with high affinity to 5-HT1B and1D receptor (Hydroxy Tryptamine) has oral bioavailability in men 63% and women 74% due to hepatic first metabolism. The present investigation is to development of naratriptan sublingual films, allowing easy of drug dissolution in oral cavity, thus by passing first pass metabolism and to produce rapid onset of action. Sublingual films were prepared by solvent casting method. Low viscosity grade HPMC E5, HPMC E15, HPMC E50 (Hydroxy Propyl Methyl Cellulose) were used in combination also as film forming polymer with different ratios, PEG 400 (Poly Ethylene Glycol) is used as plasticizer, mannitol and aspartame were used as sweetener, to decrease the disintegrating time of formulation sodium starch glycolate was used as disintegrating agent. Mint is used as cooling agent, all the films formulation (A1-A4, B1-B4, C1-C4, and D1-D4) was evaluated for their thickness weight variation, assay, folding endurance, surface pH, in-vitro disintegration. Disintegration time showed by the formulation was found to be in range of 21-48 sec. B1 showed 99.89% of drug dissolved within 10 sec, the film showed an excellent stability for 1 month when stored at 40ºC and 75% RH (Relative Humidity) in stability chamber. Key words: Naratriptan, Sublingual films, solvent casting method, stability chamber

566-572

Authors: Vinaykumar Medisetti1 , Ganga rao Battu2 , Ravindra. S3 , Sandhya R.S3 , R.V.Subbarao3

Shikakai fruit used as herbal shampoo and also used in traditional medicine to treat jaundice, constipation and skin problems. The literature survey on this plant revealed that poor scientific studies are carried out to discover new therapeutic entities. The results of the antibacterial screening of aqueous extract of the leaves of Acacia concinna revealed that it has significant antibacterial activity against gram positive and gram negative tested bacterial strains. The maximum antibacterial activity of aqueous extract was exhibited against E.coli and the maximum inhibition was observed with gram positive organism, Micrococcus luteus. The aqueous extract of Acacia concinna showed that significant anthelimentic activity when compared to piperazine citrate at the tested concentration of 5mg/ml. The plant extract contains along with inert chemical constituents also possess multiple of active therapeutically active constituents which are responsible for greater therapeutic activity then the single active constituent of synthetic medicine in the case resistant microorganism strains. Keywords: Shikakai, Acacia concinna, Anthelmintic activity, Antibacterial activity

582-585

Authors: A. Rajeshkanna1*, D. Prabhakaran2 , M. M. Senthamilselvi3 , N. Muruganantham4 , S. Solomon5

Our present investigation is focused on the anticancer activity of the compound isolated from the ethyl acetate fraction of flowers of Datura stramonium against human liver cancer HePG2 cell line by MTT assay using in-vitro method. The CTC50 value of the sample was 131.53 μg/ml against liver cancer HePG2 cell lines. Significant results were observed there by explaining the use of this plant in the traditional system of medicine. Keywords: MTT assay, anticancer activity, Datura stramonium, Liver cancer HePG2

586-593

Authors: Nabil A. F. Alhemiary1*, Ahmed N. Al-Hakemi

Two rapid, simple, sensitive and selective spectrophotometric methods have been developed for the quantitative estimation of Valacyclovir hydrochloride in pharmaceutical formulations and different human body fluids (Blood and urine). The proposed methods were based on the reduction of the nitro group to amino group of the drug. The resulting amine was then subjected to proposed methods. Method A was based on the formation of oxidative coupling reaction between the corresponding drug and brucine – NaIO4 to form violet colored chromogen at 543 nm. Method B was based on the oxidation followed by coupling with 3- methyl-2-benzothiazolinonehydrazone (MBTH) in presence of ferric chloride (FeCl3) to form green colored chromogen at 644 nm. The procedures described were applied successfully to the determination of the compound in their dosage forms and body fluids. Beer’s law is obeyed over the concentration ranges of 5–110 μg/mL and 3–45 μg/mL for brucine and MBTH, respectively, with correlation coefficients of 0.9968 and 0.9990, and molar absorptivity 0.4642× 104 and 0.9761 × 104 L/mol. cm for method A and method B, respectively. The analytical parameters such as apparent limits of detection (LOD) and quantification (LOQ) were also reported for two methods. Keywords: Spectrophotometry; Oxidation reaction; Valacyclovir hydrochloride; Pharmaceutical.

606-612

Authors: V. Jayasankar Reddy*, K.Ramesh Reddy

Proniosomes are one of the important novel drug delivery carriers of various drug molecules. Aceclofenac potent analgesic anti inflamatory agent used for the treatment of inflammation. The main objective of the study was to develop proniosomal containing aceclofenac for transdermal delivery using different ratios of cholesterol and nonionic surfactants in order to achieve a sustained release of drug on topical administration. Proniosomes were prepared by using slurry method and evaluated for for angle of repose, entrapment efficiency, thickness, folding endurance, % moisture loss and absorption, drug content and in-vitro diffusion studies. As the concentration of the cholesterol decreases the entrapment efficiency decreases due to the low vescile size formation. The in-vitro diffusion and kinetic analysis were done for proniosomal patches. It showed the release of 51.28% at 8th hr and fitted into Zero order and follows non-fickian diffusion mechanism. The best formulation(F6) was composed of cholesterol and surfactant in the ratio of 1:2 showed the better sustain action. from the study it was observed that proniosomal transdermal patches are very stable and promising sustained delivery system for Aceclofenac. Key Words: Proniosomes, Aceclofenac, Cholesterol, Surfactant.

619-626

Authors: V. Jayasankar Reddy*, K.Ramesh Reddy

The present research was formulation and evaluation of Esomeprazole buccoadhesive tablets, Bioadhesion may be defined as the state in which two materials, at least one of which is biological in nature, are held together for extended periods of time by interfacial forces. In the pharmaceutical sciences, when the adhesive attachment is to mucus or a mucous membrane, the phenomenon is referred to as mucoadhesion amongst the various routes of drug delivery, oral route is perhaps the most preferred to the patient and the clinician alike. Transmucosal routes of drug delivery (i.e., the mucosal linings of the nasal, rectal, vaginal, ocular, and oral cavity) offer distinct advantages over peroral administration for systemic drug delivery. These advantages include possible bypass of first pass effect, avoidance of presystemic elimination within the GI tract and depending on the particular drug, a better enzymatic flora for drug absorption. . Tablets were evaluated their compatibility studies by using FT-IR, micrometrics properties, post formulation characters such as hardness, thickness, friability, content uniformity, Ex vivo mucoadhesive strength and in-vitro dissolution studies. Key Words: Esomeprazole, Trans mucosal, Buccoadhesive, Mucoadhesion.

637-643

Authors: Narender Boggula* , Narender Bojjala, Thriveni Mandula, Shangati M Priyanka, Krishna Mohan Chinnala

The study was carried out to ascertain the anti bacterial properties present in different extracts of dried scale leaves of Aerva lanata. The Anti bacterial testing of leaves extract Aerva lanata was evaluated by Agar well diffusion method using gram positive bacteria like Staphylococcus aureus, Bacillus subtilis, gram negative bacteria like Escherichia coli, Klebsiella pneumoniae. Amongst the test extracts, the results suggested that, Chloroform, Ethanol extracts of leaves showed significant antibacterial activity compared with standard drug. Keywords: Aerva lanata, Gentamycin, Flavonoids, Anthraquinons

651-655

Authors: Nisrat Jahan

Glycyrrhiza glabra, licorice or yastimadhu belong to the family Febaceae. For years the plant is used in clinical purposes due to it’s several pharmacological activities. Ayravedic system consigns this plant in various preparations. Licorice possesses many therapeutical activity like antioxidant, anti-inflammatory, expectorant, tonic, diuretic, laxative, sedative, antipyretic, antimicrobial, antidiabetic and so on. The present assessment has been carried out to approximate antioxidant, antimicrobial and antidiabetic activities of plant by reviewing different journal and related articles, that might be helpful to give a thorough comprehension on licorice. Key words: yastimadhu ,anti-inflammatory, expectorant, tonic, diuretic, laxative.

662-671

Authors: M.Naga Ganesh1,3* , Y. Madhsudan Rao 2 ,T.Varun Reddy3 , P.Deepika3 , U.Krishna Charan3

The present investigation is aimed to formulate floating gastroretentive tablets containing Dipyridamole tabletsusing a sublimation material. The effect of the amount of HPMC K100M on swelling and eroding of the tablets was determined. The water-uptake and erosion behavior of the gastroretentive tablets were highly dependent on the amount of HPMC K100M The water-uptake increased with increasing HPMC K100M concentration in the tablet matrix. The weight loss from tablets decreased with increasing amounts of HPMC K100M. Camphor was used as the sublimation material to prepare gastroretentive tablets that are low-density and easily floatable.Floating properties of tablets and tablet density were affected by the sublimation of camphor. Prepared floating gastroretentive tablets floated for over 24 hrs and had no floating lag time. However, as the amount of camphor in the tablet matrix increased, the crushing strength of the tablet decreased after sublimation. The release profiles of the drug from the gastroretentive tablets were not affected by tablet density or porosity. From the Formulation, Kinetic, FTIR and DSC Studies indicated that the drug was stable in the tablets. HPMC K100M can be used as a rate controlling polymer by appropriate selection in different ratios. The release of the drug from a matrix tablet was highly dependent on the polymer concentrations. Key words: Gastroretentive Dipyridamole tablets floating tablets,Sublimation method.

393-398

Authors: D. Suresh Reddy, E. Yashaswini, A. Ashok Kumar*

Objective: To develop a simple and a cheap UV spectrophotometric method for the quantitative estimation of Atomoxetine Hydrochloride in capsules and validate as per ICH guidelines. Method: The optimized method uses 0.05N HCl as a solvent for the estimation of assay of Atomoxetine Hydrochloride in tablets at a wavelength of 225 nm. Results: The developed method resulted in Atomoxetine Hydrochloride exhibiting linearity in the range 5- 40μg/ml. System precision, intra day and inter day precisions were exemplified by relative standard deviation of 1.39%, 1.547% and 1.063%. Percentage Mean recovery by absolute method was found to be in the range of 90‐110%, during accuracy studies. The limit of detection (LOD) and limit of quantitiation (LOQ) for Atomoxetine hydrochloride were found to be 154ng/ml and 467ng/ml respectively. Conclusion: A simple and a cheap UV spectrophotometric method was developed and validated for the quantitative estimation of Atomoxetine Hydrochloride in tablets as per ICH guidelines and hence it can be used for the routine analysis in various pharmaceutical industries. Keywords: UV, Atomoxetine Hydrochloride, method development, validation.

406-409

Authors: U. S. Jijith 1,2,*, C. R. Sudhakaran Nair 1 , K. Pramod

The plant Anamirta cocculus Wild is used in traditional and folk medicine for various diseases. Thus the study was aimed to carry out preliminary pharmacological screening for its cardiovascular effects. The effect of the extract on perfused blood vessels of frog and perfused frog heart was studied. The extract produced vasodilator effect and decrease cardiac output in perfused blood vessels of frog. The extract showed a depressant effect on perfused frog heart. The action was not blocked by atropine. It also blocked the action of adrenaline on heart. The results of the study indicated that the extract might have antiarrhythmic activity. Keywords: Anamirta cocculus, cardiovascular effect, pharmacological screening.

415-422

Authors: M. Sujatha Kumari*, K. Naga Lakshmi, T. V. V. N. V. L. Prasanna, K. Swapna, A. Swarna Jyothi, T. Prasanthi

The present study was based on Diabetes, its cure using natural herbs over allopathic drugs. Diabetes occurs world-wide and the incidences of both type 1 and type 2 diabetes are rising; it is estimated that, in the year 2000, 171 million people had diabetes, and this is expected to double by 2030. Despite the use of advanced Allopathic drugs for the treatment, use of herbal remedies is gaining higher importance because of Allopathic drugs have drawbacks and limitations. Natural herbs have been highly esteemed source of medicine throughout the human history. They are widely used today indicating that herbs are a growing part of modern high-tech medicine. The herbal drugs with anti diabetic activity are extensively formulated commercially because of easy availability, affordability and less side effects as compared to the synthetic anti diabetic drugs. The World Health Organization (WHO) has listed 21,000 plants, which are used for medicinal purposes around the world. A list of medicinal plants with proven anti diabetic and related beneficial effects and of herbal drugs used in treatment of diabetes is compiled. Thus, this review article undertake the attempt for providing updated information on the type of diabetes and herbal formulations which will enhance the existing knowledge of the researchers. Keywords: diabetes ; Allopathic drugs; Natural herbs; antidiabetic activity.

429-434

Authors: Kolhe Mahesh Hari*, Bhusal Ramesh Dattatraya, Hajare Pranit Pandurang.

Accurate, specific, precise and robust TLC Densitometric method have been developed for simultaneous estimation of Metoprolol Succinate (METO) and Hydrochlorothiazide (HCTZ) in tablet dosage form. The chromatographic separation was performed on precoated silica gel TLC 60 F254 plates using Toluene: Methanol: Ethyl acetate: Glacial acetic acid (7: 1.5: 1: 0.5 v/v/v/v) as mobile phase. This system was found to give compact bands for Metoprolol Succinate and Hydrochlorothiazide (RF values 0.15 and 0.35 respectively). Densitometric analysis of Metoprolol Succinate and Hydrochlorothiazide were performed at 230 nm. Regression analysis data for the calibration plots were indicative of good linear relationships between response and concentration over the range 1000-5000 ng/band for Metoprolol Succinate and 500-2500 ng/band for Hydrochlorothiazide. An approach of forced degradation study was successfully applied for the development of a stability-indicating method for estimation of Metoprolol Succinate and Hydrochlorothiazide in the presence of its degradation products. The method was validated as per ICH guidelines for accuracy, precision, LOD, LOQ and robustness.

444-449

Authors: Tamizhazhagan V*, Pugazhendy. K

Aquatic ecosystem monitoring has been carried out in India based on either chemical or biological analysis. Diatoms constitute a fundamental link between primary (autotrophic) and secondary (heterotrophic) production and form a vital component of aquatic ecosystem. Particularly PH, Temperature, at the same time remaining parameters of salinity, O2 and Co2 observation was slightly changed due to some pollutes. So in this study will be given supporting to the future study among the fresh water ecosystem balance. Key words: Physio-Chemical, Natural Pond, Culture Pond,

456-461

Authors: Bharathi KN, * Vidyashree N and Raju HV

Bytteneria herbaceae is a profusely branched prostrate herb. Traditionally different part of this plant is used for the treatment of cholera, diarrhoea and asthma, but lack scientific evidence. Hence, in the present study aqueous and ethanolic extracts of Bytteneria herbaceae was evaluated for antiasthmatic activity in rats by studying its effect on mast cell stabilization and isolated goat tracheal chain preparation. In mast cell stabilizing activity male albino rats of Wistar strain weighing 150-200 g were divided into eight groups of six animals each. Except group I (Control), all animals were sensitized by 0.5ml of sheep serum and 0.5ml of triple antigen containing diphtheria, tetanous toxoid and B.pertusis organisms. Group I and II rats received vehicle, group III – VI rats were treated with aqueous and ethanolic root extracts of Bytteneria herbaceae 200 and 400 mg/kg.b.w.p.o., respectively, group VII and VIII rats were treated with standard prednisolone and disodium chromoglycate 10 and 50 mg/kg i.p. respectively. Treatment was given once daily single dose for 14 days. On 14th day intestinal mesentery was isolated under anesthesia and stained with 0.1% toluidine blue. Numbers of intact and degranulated mast cells were counted under high‐power microscope (45X). Antagonism of extracts was recorded against histamine induced contraction on goat tracheal chain preparation. Results were expressed as mean ± SEM and analyzed by one way ANOVA, followed by Tukey’s multiple comparison test. Aqueous and ethanolic extracts of Bytteneria herbaceae root significantly (P<0.001) reduced the mast cell disruption and increased intact mast cells dose dependently. Ethanolic extract was significantly (P<0.001) more potent than aqueous extract. In isolated goat tracheal chain preparation extracts of Bytteneria herbaceae antagonized the histamine induced contraction irreversibly and was dose dependent. Antiasthmatic activity of Bytteneria herbaceae was due to the presence of active constituents such as flavonoids, steroids, carbohydrates and tannins. Results of the study substantiate traditional use of Bytteneria herbaceae in the treatment of asthma. Keywords: Bytteneria herbaceae; Antiasthmatic; Prednisolone; Mast cell; Sodium cromoglycate; Antihistaminic.

492-507

Authors: M. Prasada Rao*, K. Leelavathi, N. Chandreshta, V. Sowjanya, I. Sireesha, I. Rajani, V.V. Naga Premi

An isocratic reverse phase liquid chromatography (RP-HPLC) method has been developed and subsequently validated for the determination of Capecitabine in Bulk and its pharmaceutical formulation. Separation was achieved with a Develosil (ODS-MG-5; 100 x 4.6mm I.D; particle size 5 μm) Column and buffer Methanol (450:550) v/v as eluent and purified water, methanol and acetonitrile(600:350:50)v/v as diluent at flow rate 1.0 mL/min and the Column temperature was 40°C. The described method of Capecitabine is linear over a range of 6 μg/mL to 30 μg/mL. The method precision for the determination of assay was below 2.0% RSD. Key words: Capecitabine, RP-HPLC, Develosil ODS-MG-5.

516-521

Authors: Mukund Handral1 , Abin Joy*1 , Chaitra N1 , Shivakumar Kasabi

The main aim of the study was to carry out and investigate the Antiosteoporotic activity of ethanolic root extract of Rubia cordifolia (EERC) in Methylprednisolone acetate (MPA) induced osteoporotic rats. Acute oral toxicity was performed according to OECD guidelines 425 in albino mice and extract was found to be safe upto 2000 mg/kg. All the rats were randomly divided into 5 groups (n=6 each). Group I (normal control) received water for injection s.c., Group II MPA (0.2 mg/kg, s.c) positive control, Group III was MPA (0.2 mg/kg, s.c) + standard drug Alendronate (200 µg/kg, p.o), Group IV& V received EERC (200 mg/kg & 400 mg/kg, p.o) + MPA (0.2 mg/kg, s.c) respectively and treated for 4 weeks. The serum biochemical markers revealed dose dependent restoration of calcium, ALP and TRAP which was significant (P<0.0001) when compared to MPA control. Similarly, the findings from bone biomechanical parameters also found to have significant changes, where bone mechanical strength (P<0.0001) and bone mineral content was also significantly increased (P<0.0001) by improving calcium absorption and enhanced osteoblastic activity nearly to normal levels in rats treated with EERC. Furthermore, SEM data of femur bones of EERC (200 and 400 mg/kg) treated rats showed reduced pore formation and improved bone compactness. All these results significantly indicate a possible antiosteoporotic activity of EERC. In addition, further studies are required to determine the active components that are responsible for its antiosteoporotic activity. Keywords: Rubia cordifolia, Methylprednisolone (MPA), Osteoporosis, Biochemical parameters, Ash content, Scanning electron microscopy (SEM).

536-545

Authors: Prasad S. Bhamare* , Mitesh P. Sonawane, Rajendra K. Surawase

Valsartan is Angiotensin-II receptor antagonist used in anti-hypertensive drug. The present study is deals with formulation, optimization, evaluation of Sustained release Valsartan matrix tablet. The SR tablets were Prepared by direct compression method and formulated using different natural gums.ratios, formulation such as F1-F9. Gums like Xanthan gum and guar gum were used. Compatibility of drug with various excipients was studies. The compressed tablet were evaluated and showed compliance with Pharmacopoeial limits. The concentration of Xanthan gum and Guar gum were different in all formulations (F1-F9). All the formulations were evaluated for pre-compression parameters and weight variation, Hardness,friability, drug content, invitro dissolution studies. The formulation ‘F9’ was found to be optimized formulation. It shows results for all evaluation parameters such as weight variation 320.14±0.42%, Friability 0.30%, Swelling index 85%, drug content 98.91±0.32%, and in-vitro dissolution study 99.91±2.1% at the end of 15 hrs. keywords: Valsartan, Guar Gum, Xanthan Gum, Sustained Release Matrix Tablets, etc.

552-559

Authors: Bassey S. Antia*, Emmanuel E. Essien, Nimmong-uwem S. Peter

Lagenaria siceraria (Molina) Standl. is a vegetable food, also used as a traditional medicine. The present study was designed to investigate the flavonoids, total phenolics and antioxidant activities of seed oils extracted from six cultivars of Lagenaria siceraria. The total phenolics, flavonoids content and antioxidant activity were measured spectrophotometrically using standard procedures. The total phenolic contents of the oils ranged from 5.2-7.0 mg gallic acid/100g and total flavonoids, 4.1-6.1 mg quercetin equivalent/100g. The seed oils (120 μg/ml) free radical scavenging activity (DPPH assay) varied between 54.1-57.8% with EC50 values of 98.0-117.0 μg/ml; metal chelating activity and EC50 values of the oils were 65.5-83.6% and 19.0-59.0 μg/ml respectively; and ferric reducing power of seed oils varied from 0.528-0.580 with EC50 values of 91.0-104.0 μg/ml. Dietary polyphenolics from Lagenaria siceraria cultivars may supply substantial antioxidants, which may provide health-promoting advantages to the consumers. Keywords: Curcubitaceae, Lagenaria siceraria, Cultivars, Polyphenolics, Antioxidant activity.

324-330

Authors: Vykuntam Uppala, N. Divya, E. Charishma, K. Harshavardan, Shyamala. M

A simple, Precised, Accurate method was developed for the estimation of Ibrutinib by RP-HPLC technique. Chromatographic conditions used are stationary phase Kromosil150mm x 4.6 mm, 5 ,Mobile phase0.1% OPA: Acetonitrile in the ratio of 40:60and flow rate was maintained at 1ml/min, detection wave length was 296nm, column temperature was set to 30oC and diluent was mobile phase Conditions were finalized as optimized method. System suitability parameters were studied by injecting the standard six times and results were well under the acceptance criteria. Linearity study was carried out between 25% to150 % levels, R2 value was found to be as 0.999. Precision was found to be 1.01 for repeatability and 1.50 for intermediate precision. LOD and LOQ are 0.394µg/ml and 1.194µg/ml respectively. By using above method assay of marketed formulation was carried out 100.55% was present. Degradation studies of ibrutinib were done, in all conditions purity threshold was more than purity angle and within the acceptable range. Key Words: HPLC, Ibrutinib, Method development. ICH Guidelines.

340-347

Authors: Dr. Ananda Kumar, P. Renuka, K. Ashok Babu, K.V.S.L Prasanna, V. Rajya Lakshmi

The Chronopharmacotherapy the drug administration is synchronised with circadian rhythms Formulation development of Microspheres is more reliable formulation as compare to single type dosage formulation due to it avoids dose dumping, as per required drug release profile is achieved For microspheres many polymers are used such as albumin, gelatine, starch, Eudragit, Polyacrylamide (“PAM”) these material loading capacity is high. Micro sponges which are Spherical are called as micro-balloons. Due to its hollow structure it shows good floating properties. In these systems use of Carbon-dioxide (CO2) as gas generating system which are used for floating purpose. The objective of present investigation is to prepared and evaluate a floating pulsatile drug delivery system of Aceclofenac. The strategy adopted for microspheres containing Aceclofenac as a material were prepared by emulsion solvent diffusion technique. Drug and polymer were mixed in dichloromethane and ethanol at 1:1 ratio. The drug and polymer solution were poured in water 50% W/V polyvinyl alcohol maintained at 30-40 C and the solution was stir at 500rpm using mechanical stirrer, The microspheres obtain were washed repeatedly with water until free from poly vinyl alcohol. The developed formulations were evaluated yield of floating microspheres particle size and shape, drug entrapment efficiency in-vitro evolution of floating ability, in-vitro drug release study. On the basis of these evolution parameters it was found that optimised floating pulsatile release formulation F7 showed higher drug entrapment efficiency floating time 6.8 minutes and the drug and polymer 32 1:3 ratio the particle size was increased. Key Words: Chronopharmacotherapy, Floating pulsatile drug delivery, Aceclofenac.

351-357

Authors: P. Shaniya, NJR. Hepsebah, MD. Khasim, A. Ashok Kuma

The article aims at developing simple dissolution method for Eplerenone immediate release tablets by UV spectroscopy and validate as per ICH guidelines. The optimized dissolution method includes 0.1N HCl as dissolution media, apparatus as USP Type 2 Paddle, rpm as 100, temperature of dissolution media as 37±0.5ºC, dissolution volume as 500ml, dissolution time point as 1 hour, working concentration of standard and sample as 10µg/ml and a detection wavelength of 245 nm.The developed method resulted in Eplerenone exhibiting linearity in the range 2.5-20μg/ml. System precision and intra-day precision are exemplified by relative standard deviation of 0.695% and 0.933% respectively. Method was found to be rugged/inter day precise as %RSD was found to be 1.507%. Percentage Mean recovery was found to be in the range of 90-110 % by absolute method during accuracy studies. Hence it can be concluded that effective dissolution method by UV spectroscopy is developed and validated which can be applicable in various pharmaceutical industries. Keywords: Eplerenone, Dissolution method, UV, Validation.

368-373

Authors: Patel Nidhi1*, Patel Sweta1 , Jain Hitesh1 , Upadhyay Umesh1

Osmotically controlled oral drug delivery systems utilize osmotic pressure as energy source for the controlled delivery of drugs. The aim of the present study is to formulate and evaluate controlled porosity osmotic tablets of Losartan Potasssium. Losartan Potassium is used in hypertension. Core tablets were prepared by direct compression technique using mannitol, fructose and NaCl as osmogens and Avicel PH101 as filler. The osmotic tablet contains pore forming water soluble additives in the coating membrane, which dissolve after coming in contact with water, resulting in formation of an in-situ micro porous structure. The core tablets were coated by dip coating using cellulose acetate as a coating agent with PEG 400 and PEG 6000 as water soluble pore former and dibutyl pthalate as plasticizer. The formulations were evaluated for precompression and postcompression parameters. The batch F8C2 containing Fructose as an osmogen and 20 % PEG 6000 as a pore forming agent showed the 91.25 % drug release for 12 hrs. Keywords: Antihypertensive, Losartan Potassium, Osmotic, PEG 6000, Semi Permeable Membrane.

195-201

Authors: Hassan Ali Al-Saadi1 , Hadi Rasool Hasan AL-Masoodi2 and Zainab Hekmat Abed Kamona3

Male infertility one of the most common health problems with psychological and social effects. This study aims to investigate the effects of the antisperm antibodies(ASA) on the macroscopic and microscopic parameters of seminal fluid in some infertile males.The percent of ASA type G (IgG), and (IgA) were measured on the surface of sperms, macroscopic and microscopic examination of seminal fluid have been measured for infertile patient resorting to Institute of Embryo Research and Infertility Treatment, Al-Nahrain University, and in the laboratories of Al-Hussain Hospital /Kerbala. Throughout period then March to August 2011. (419)seminal fluid spaceman are collected from infertile patient and measurement the percentage of (IgG&IgA) antisperm antibody to (38) sperm agglutination specimen from infertile patient and comper with (12) fertile men as control group. The results were showed a significant effect (P< 0.05) of IgG and IgA on a liquefaction time, percentage of progressive motility, sperm agglutination, and round cells on compared with control group. These results showed a significant decrease (P<0.05) in the percentage of rapped progressive motility (Grade A) in all groups.A significant increase (P<0.05) in sperm agglutination and round cell in all groups. Positive correlation with sperm agglutination, morphologically abnormal sperm percent and round cells. A significant increase (P<0.05) in liquefaction time in the second and the third group. Key words:ASA,MAR test,IgA,IgG,seminal fluid

209-218

Authors: Singireddy Anandam, Srilakshmi N, P Sobhita Rani

The present involves the preparation and evaluation of floating microspheres using Famotidine as a model drug for prolongation of the gastric retention time. The microspheres were prepared by the Ionotropic gelation method using different polymers i.e., HPMC K4M, HPMC K100M and Carbopol. The prepared microspheres were evaluated for particle size, buoyancy, entrapment efficiency. In Vitro drug release studies were performed and the drug release kinetics was evaluated using the linear regression method. Data obtained for floating microspheres of famotidine showed good buoyancy and prolonged drug release. The average particle size was in the range of 526µm to 644µm. % drug entrapment efficiency ranged from 62.35% to 97.24%. Diffusion was found to be the main release mechanism. Among all formulations F9 formulation was found to be satisfactory in terms of excellent micromeritic properties,% yield, drug entrapment efficiency, % buoyancy and In-vitro drug release in a sustained manner over an extended period of time for 12 hours. Thus the prepared microspheres proved to be a potential candidate as a microparticulate controlled release drug delivery device in this era. Keywords: Famotidine, Floating Microspheres, Gastric Retention Time, Buoyancy, Entrapment Efficiency and Invitro drug release

227-233

Authors: Patel Nidhi1* , Chaudhary Anamika1 , Soni Twinkle1 , Sambyal Mehul1 , Jain Hitesh1 , Upadhyay Umesh1

Oral drug delivery is the most convenient option as the oral route provides maximum active surface area among all drug delivery system for administration of various drugs. The attractiveness of these dosage forms is due to awareness to toxicity and ineffectiveness to drugs when administered by oral conventional method in the form of tablets and capsules. An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug to a specific organ or tissue and controlling the rate of drug delivery to the target site. Oral Sustained release (SR) / Controlled release (CR) products provide an advantage over conventional dosage forms by optimizing bio-pharmaceutics, pharmacokinetic and pharmacodynamics properties of drugs in such a way that it reduces dosing frequency to an extent that once daily dose is sufficient for therapeutic management through uniform plasma concentration providing maximum utility of drug with reduction in local and systemic side effects and cure or control condition in shortest possible time by smallest quantity of drug to assure greater patient compliance. The present article contains brief review on various formulation approaches for controlled release drug delivery system. Keywords: Controlled drug delivery system, Drug release mechanism, Modified Release, Sustained Release

240-251

Authors: Muhammad Razi Ullah Khan1,2, Syed Muhammad Aun2,3, Muhammad Arsalan3 , Saeed Ur Rasid Nazir 1 , Farah Abdul Khaliq3 , Sana Ilyas3 , Sadia Kanwal3 , Sadia Hassan3 , Ayub Fareed3 , Rana Mobeen3 , Mehwish Alam

Increasing numbers of complementary and alternative medicine (CAM) practitioners are interested in evidence-based medicine (EBM). Researchers are in need of further information regarding the current status of CAM practitioner’s knowledge and use of EBM. A high prevalence of CAM use has been documented worldwide in children and adolescents with chronic illnesses. Only a small number of studies, however, have been conducted in the Pakistan. Primary aim of survey was performed to estimate and explore the use of alternative medicine in patients with different diseases among all age groups. A questionnaire survey was distributed in different hospitals (n =2000) in rural and urban area. Total 500 patients were observed out of which 48.66% were male and 51.34% were female. The 48% of the patients were literate while 52% patients do not know how to read or write. It was found in this study that 42.07% of population is getting allopathic treatment, 32.81% towards herbal treatment and 23.69% towards homeopathic treatment among the patient taking allopathic treatment almost 51.48% were male and 48.76 % female. The urban population almost 52.84% male and 47.16% female were using allopathic mode of treatment. While 44.52% male and 55.48% female in rural population were taking allopathic treatment In case of herbal treatment percentage ratio of rural and urban population was 31% and 19% respectively among male patients. Among females 30% patient belong to urban region while 20% patients were from rural areas 37% male and 29% female patients were taking homeopathic treatment in urban areas. In rural areas among the patients taking homeopathic treatment almost 21% patients were female while 13% patients were male Almost 60% patients agreed that they were getting required outcome of medicine however 40% patients feel that they were getting no effects in the start of these therapies Analysis of general health appearance of patients showed that almost 19% were in very good health condition. Almost 44% patients had good health while 12% were in satisfactory look. The ratio of patients suffering poor health was found to be 25%. Along with being more educated and reporting poorer health status, the majority of alternative medicine users appear to be doing so not so much as a result of being dissatisfied with conventional medicine but largely because they find these health care alternatives to be more congruent with their own values, beliefs, and philosophical orientations toward health and life. Key Words: Complementary and alternative medicine, Evidence based medicine, Qualitative study, Questionnaire, Barrier

265-270

Authors: Nasitha I A, K. Krishnakumar, Dineshkumar. B

Hydrogel products constitute a group of polymeric materials, the hydrophilic structure of which renders them capable of holding large amounts of water in their three-dimensional networks. Extensive employment of these products in a number of industrial and environmental areas of application is considered to be of prime importance. As expected, natural hydrogels were gradually replaced by synthetic types due to their higher water absorption capacity, long service life, and wide varieties of raw chemical resources. Literature on this subject was found to be expanding, especially in the scientific areas of research. However, a number of publications and technical reports dealing with hydrogel products from the engineering points of view were examined to overview technological aspects covering this growing multidisciplinary field of research. The primary objective of this article is to review the literature concerning classification of hydrogels on different bases, its merits and demerits. It also involved technologies adopted for hydrogel production and its application in drug delivery. Key words: Hydrogel, drug delivery, cross-linking.

275-282

Authors: SB Shirsand * , V Jonathan, Shilashri, R T Gumate

Objectives: The aim of the present work was to prepare and evaluate fast dissolving tablets of furosemide with a view to enhance patient compliance and minimizes the side effects. Methodology: In this study, fast dissolving tablets of furosemide were formulated by direct compression method using such as pectin of mango peel (mangifera indica ) was used as natural disintegrants and crospovidone as a synthetic superdisintegrant in different ratios with directly compressible mannitol (Pearlitol SD 200) as a diluent to enhance the mouth feel. The prepared formulations were evaluated for hardness, friability, drug content, in vitro dispersion time, wetting time, water absorption ratio, in vitro drug release studies, stability studies and excipients interaction studies. Results: Among all the formulation, the formulation (FMP3) containing 8% w/w pectin of mango peel (mangifera indica ) is the overall best formulation (t50% 5.2 min) based on in vitro drug release studies. Stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05). Conclusion: From the above studies, it can be concluded that fast dissolving tablets of Furosemide can be prepared using different natural super disintegrant for faster dispersion and disintegration in the mouth. Keywords: Fast dissolving tablets, Furosemide, Crospovidone, mangifera indica, Natural disintegrants.

288-293

Authors: Kanika Barik, Shweta Sao and Dharmendra K. Pariha

Madagascar periwinkle Catharanthus roseus is an important tropical medicinal plant, found as a popular ornamental plant in gardens and homes across the warmer parts of the world, also known as “an anticancerous drug yielding plant” is a tropical and subtropical plant belonging to the family Apocynaceae. The plant accumulates an array of diverse compounds comprising over 130 different MIAs. It is a seasonal to perennial garden plant and the exclusive source of the anticancer drugs vincristine and vinblastine. Apart from these, its leaves and roots hyper-accumulate the other terpenoid indole alkaloids, which are required for the economic production of pharmaceutical molecules vindoline, catharanthine, ajmalicine and serpentine. the plant have been used for various other medicinal valued like anti-diabetic, anti-ulcer, anti-bacterial, anti-oxidant and antidiarrheal properties. The review describes phoarmacological applications and phytochemicals of C. roseus. Key words: Alkaloids, antioxidant, antibiotic, anticancer, Catharanthus roseus, Vincristine, Vinblastine.

300-304

Authors: Niraj Khatri Sapkota1 , Kailash Chandra Swain2

B-12 (cobalamin) is a complex molecule in which a cobalt atom is contained in a corrin ring, an important organic cofactor essential for the neurological and hematological integrity, strictly found in non-vegetarian diets and milk products, long run abstinence of these ingredients in diet results into its deficiency exhibiting neurological clinical manifestation which is, in general not seen but with strict long term deficiency such as in strict vegetarian leads to the clinical manifestation such as weakness, paraesthesia and numbness. Management of this manifestation can be done with vitamin B12 supplements or encouraging consuming the synthetic form of the vitamin, meat and egg that is rich source of Vit.B12, therefore this short review will focus to disclose the mechanism and management that correlates the effect of long term deficiency of Vitamin B12. Key words: vitamin, non-vegetarian diets, par-aesthesia, neurology.