International Journal of Pharmaceutical Sciences and Drug Research

134-143

Authors: Amal Kumar1*, Bhaswat S. Chakraborty2

Polychemotherapy and intermittent monochemotherapy regimens in metastatic breast cancer were examined in a meta analysis that included both tumor response rate and toxicities. Randomized controlled studies (conducted during 1990-2008) comparing monochemotherapy and poly-chemotherapy in advanced breast cancer patients were selected from electronic databases. Meta-analysis for response rate and toxicities [nausea and vomiting, toxic death, alopecia and reduced white cell count (WCC)] was performed using the Mantel-Haenszel method. The heterogeneity among the trials was assessed through a χ2 statistic, I2 and visual inspection of the forest plots. Analysis of eligible studies reveals statistical significant difference in response rate (OR 0.72, 95% CI 0.65-0.79), nausea and vomiting (OR 0.80, 95% CI 0.67-0.59), Alopecia (OR 0.75, 95% CI 0.64-0.88) and reduced WCC (OR 0.55, 95% CI 0.48-0.62) which favours polychemotherapy except toxic death (OR 0.87, 95% CI 0.58-1.29). There was marked evidence of heterogeneity in all end points except toxic death. This meta analysis shows the superiority of efficacy but not of safety of polychemotherapy over that of a single agent. However, the choice of treatment should be based on the response to the therapy, toxicity, patient preference, presence of metastases or imminent complications requiring aggressive and rapid tumor control.

149-152

Authors: Gopalakrishnan S1*, Vadivel E2

The bark of Bauhinia tomentosa L. is used wildly used for the treatment of varies ailments such as inflammation, wound, dysentery, skin diseases and for microbial infections. In the present study the ethanolic extract of the bark of Bauhinia tomentosa L. has been subjected to Gas Chromatography-Mass Spectrometry (GC-MS) analysis, while the mass spectra of the compounds found in the extract was matched with the National Institute of Standards and Technology (NIST) library. GC-MS analysis revealed the presence of fourteen phytochemical constituents, These compounds were identified by comparing their retention time and peak area with that of literature and by interpretation of mass spectra. The major chemical constituents are 4-(Benzyloxy)-1-methoxy-2-(3,7-dimethylocta-2,6-dienyl)-benzene (10.88%), Levodopa (6.39%) and (9E, 12E) - Methyl octadeca-9,12-dienoate (5.68%) which possess many biological activities. Hence these studies pave a platform to screen many bioactive components for wound healing.

157-165

Authors: Meetali M. Chaphekar*, Purnima D. Hamrapurkar

The concept of Quality by design (QbD) has recently gained importance in the area of analytical method development and involves understanding of the critical factors and their interaction effects by a desired set of experiments. So, the present work describes the development of Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) method by QbD approach using Design of Experiments and subsequent validation for analysis of Vildagliptin in bulk drug and its pharmaceutical formulation. An efficient experimental design based on systematic scouting of all three key components of the RP‐HPLC method (Buffer pH, Organic Phase-% acetonitrile, Organic Modifier-Methanol) is presented. The significance and interaction effects of these parameters on the response variables (Retention time and tailing factor) were evaluated through statistical analysis tools like Analysis of Variance (ANOVA) and plots which revealed the final chromatographic conditions of the method. The developed method was validated and Forced degradation studies were also carried out in order to determine the stability-indicating nature of the method. The chromatographic separation was achieved on Jasco CrestPack RP C18 (250 × 4.6 mm, 5μ) column using Buffer (pH 6): Acetonitrile: Methanol (70:10:20 v/v) as mobile phase and detection was done using Photo-Diode Array (PDA) detector at 210 nm. The developed method of Vildagliptin is linear over a range of 5-15μg/ml having correlation coefficient R2 value as 0.999. The %RSD for precision and accuracy of the method was found to be less than 2%. Forced Degradation studies revealed that the method was found to be stability-indicating. The results showed that the proposed method is suitable for the precise and accurate determination of Vildagliptin in bulk and its formulation.

170-173

Authors: Vineeta V. Khanvilkar*, Rupali R. Kothekar

A simple, rapid and economic UV spectrophotometric method has been developed and validated using a solvent 0.1N HCl to determine Dextromethorphan hydrobromide content in bulk and two different pharmaceutical solid dosage formulations, lozenges and chewable tablets. At the pre-determined λmax of 278 nm, it was proved linear in the range of 5.0-30.0 µg/ml and exhibited good correlation coefficient (R2=0.9993) and excellent mean recovery (101.37-100.76%) and (100.66-101.17%) for lozenges and chewable tablets respectively. This method was successfully applied to the determination of Dextromethorphan hydrobromide content in lozenges and chewable tablets and the results were in good agreement with the label claim. The method was validated as per ICH guidelines for linearity, precision, accuracy, specificity, LOD and LOQ. The obtained results proved that the method can be employed for the routine analysis of Dextromethorphan hydrobromide in bulks as well as in the pharmaceutical formulations.

182-188

Authors: Bipul Nath*, Tushar Kanti Roy

The objectives of present investigation is to evaluate the compatibility of Atorvastatin calcium with immediate release excipients and to optimize the tablet which release is best comparable with innovator product by varying different super disintegrants. Various excipients used were sodium starch glycollate, cross carmellose sodium, cross-povidone, lactose, micro crystalline cellulose, mannitol, sodium lauryl sulfate, magnesium stearate, and stearic acid. Thermal characterization of the drug was done by DSC and FT-IR. From the DSC studies, the excipients such as microcrystalline cellulose (Avicel 101), magnesium stearate, mannitol, sodium lauryl sulfate were found to have physical interactions with Atorvastatin. Immediate release tablet was prepared by direct compression method and its release profile was compared with the marketed IR tablet. The prepared tablet have conform the pharmacopoeial limit for hardness, thickness, friability, weight variation and content uniformity. Formulation F11 containing two super disintegrants have shown the disintegration time less than 25 sec and better dissolution than all other formulations releasing more than 80% of the drug after 20 minutes. Kinetic data reveals that the drug release follows best order by Higuchi model, followed by korsemeyer peppas, zero order and first order mechanisms. The results of accelerated stability studies as per ICH guidelines indicated that the tablet was stable as there were no any significant physical changes after the study.

75-82

Authors: Mallikarjuna Gouda M1*, Ramakrishna Shabaraya A2

In the present investigation planned to study the less explored sterculia gum as matrix carrier of Budesonide to colon. Developed the formulations from B1 to B4 contains alone sterculia gum and its proportion increased gradually in the formulation. The formulations B5 to B10 contain the sterculia gum in combination with Eudragit S 100 and the hydrophilic, hydrophobic polymer. The budesonide core in coat matrix tablets was prepared by direct compression method. The powder bed of the formulations is evaluated for pre compressional characteristics like bulk density, tapped density, compressibility index and angle of repose. The compressed budesonide core in coat matrix tablets were evaluated for post compressional characteristics like thickness, diameter, hardness, disintegration, friability and to understand the drug release pattern and to correlate the in vivo condition, the in vitro dissolution performed in three different gastro intestinal pH at 1.2, pH 7.4 and pH 6.8 with and without 4% rat cecal content. The in vitro dissolution results of formulations ascertain that sterculia gum alone in formulation uncontrolled the drug release in first 5 hrs and carried lesser amount of drug to colon. The formulations B8 in the first 5 hours released 4.3% and carried the larger amount of drug to colon and in absence of rat cecal content released 90% and in presences of 4% rat cecal content released 99% of drug, indicating the sterculia gum undergoes enzymatic degradation and this formulation is considered as potential in targeting the budesonide to colon in the local ulcerative colitis.

87-90

Authors: Kamanashis Das1*, Md. Yasin1, Ishrak Jahan1, Tahira Akter1, Saiful Islam2, Md. Sagir Mia3

In order to prepare the sustained release tablet with levo-salbutamol sulphate we have used these excipients methylcellulose, PVPK30, magnesium stearate, talc, isopropyl alcohol, microcrystalline cellulose, lactose, HPMCK100, HPMCK4M. Here our approach was for making the sustained released matrix tablet by two ways, one is to make the tablet granules floating and the second one is by retarding the release of the levo-salbutamol sulphate from the matrix. We have already discussed the relationship with delaying the gastric transit time and the active drug absorption, if the tablet granules are floating in our introduction part. Since the above mentioned excipients are floating in nature so formulations with those excipients are supposed to be floating. We also showed a list of excipients those are used in the preparation of floating tablets. Now the second observation which was the release rate, among the three different formulations (mentioned in the introduction) we found different types of release. Since our objective is to prepare a sustained released tablet which will give a prolong release time, in that prospect two among the three formulations were disqualified (though we have not done the kinetic study). We observed desired effect in the formulation-2 during the preparation of experiment.

98-102

Authors: Krushnkumar Karangiya1*, Jatin Upadhyay2

In present study the new series of 3-(Aryl)-5-[4-(2, 4-Dichlorophenylmethoxy)-3-methoxyphenyl]-4, 5-dihydro pyrazoline (2a-k) and 3-(Aryl)-5-[4-(2, 4-Dichlorophenylmethoxy)-3-methoxyphenyl]-4, 5-dihydroacetyl pyrazoline (3a-k) derivatives were synthesized from various substituted 3-Methoxy-4-(2, 4-Dichlorophenyl methoxy) chalcones (1a-k). The new chalcones were synthesized using various acetophenones with newly synthesized aldehyde of vanillin analog by Claisen-Schmidt condensation. Characterization of pyrazoline derivatives have been established on the basis of IR, NMR, Mass and elemental analyses. The derivatives were screened for their in vitro antimicrobial Screening.

111-116

Authors: Mehul K. Bhatt1*, Nehal Shah2

Hygrophila salicifolia (Family: Acanthaceae) is an erect herb, nearly glabrous, mainly whole herb used as raw material in medicine. The aim of present investigation was to evaluate acute toxicity, in vitro urolithiatic and diuretic activity of methanolic extract of Hygrophila salicifolia, whole herb. Methanolic extract of Hygrophila salicifolia was administered to experimental rats orally at 2000 mg/kg p.o. The acute toxicity of the extract was evaluated as per OECD guideline 420. The LD50 of the extract was found to be between 2000-5000 mg/kg p.o. Urolithiatic activity was determined for all extracts using Conductometric titration and crystal growth inhibition. Methanolic extract of Hygrophila salicifolia was administered to experimental rats orally at doses 300 & 500 mg/kg p.o. Furosemide (10 mg/kg) was used as positive control. The diuretic potential of the extracts was evaluated by measuring urine volume, Diuretic index, Lipchitz value, Saliuretic index, Na+/K+ ratio and excretion of sodium-potassium content. The present study provided quantitative and qualitative basis for explaining non toxicity, urolithiatic and diuretic potential of methanolic extract of Hygrophila salicifolia.

121-127

Authors: Abhay R. Shirode*, Arpita P. Nath, Vilasrao J. Kadam

A new isocratic simple and rapid reverse phase high performance liquid chromatographic (RP-HPLC) method was developed and successively validated for the estimation of ziprasidone hydrochloride monohydrate (ZHM). In this newly developed method chromatographic separation of ZHM was achieved on a Hemochrom-Intertsil C18-5U column (250 × 4.6) mm within a short runtime of 6.5min using mobile phase containing HPLC grade water (pH adjusted to 3.0 with glacial acetic acid AR) and methanol in the ratio of 45:55% v/v. ZHM was estimated with UV detection at 317nm and it was found to be eluted at 4.8min. The above mentioned method was validated as per International Conference on Harmonization (ICH) guidelines with respect to accuracy, precision, linearity, lower limit of detection (LOD) and lower limit of quantitation (LOQ) and robustness. The method was found specific for ZHM and linear (r2 =0.998) over concentrations ranging from 2 to12μg/ml. The method was found statically accurate (mean recovery = 100.46%), precise with both intra-day and inter-day relative standard deviation (RSD) values < 1.0% and robust. The obtained results concluded that the proposed RP-HPLC method is convenient, reliable and useful in routine analysis for estimation of ZHM in its bulk form and dosage form.

7-12

Authors: Sridevi Gowripattapu*, S. Madhavi Latha

The objective of the present investigation was to design suitable sustained release tablet formulation of Nateglinide by using different polymers such as hydroxy propyl methyl cellulose K15M, xanthan gum, guar gum as release rate retarding polymers. The tablets were prepared by direct compression technique. Nateglinide is used as anti diabetic drug. The objective of the treatment is to achieve hypoglycemia, by using an ideal dosage regimen. The sustained release formulation provides extend duration of action in therapeutic range without reaching toxic levels as in the case of conventional dosage forms. The real formulation trails are carried from F1 to F9 in which Drug: Polymer ratio was set as 1:9 respectively. The prepared formulations F1 to F9 were evaluated for pre and post compression characteristics, along with the in vitro dissolution Studies. It was found that the release of drug from F1, F2, and F3 gave the better release than other formulations. In these three formulations F2 showing highest release following first order kinetics. From the Higuchi plot good correlation coefficient was observed showing diffusion mechanism. From the peppas plot it was observed that the release model was non fickian anomalous. The release rate was decreased as polymer concentration increased so it shows that increase in diffusion length of polymer decreases the release rate.

21-29

Authors: Ndatsu Yakubu1*, Umaru Alhassan Mohammed2

The total flavonoid contents of the various coagulated tofu and the hepatoprotective potential of all tofu flavonoid extracts were investigated. Tofu was prepared from locally sourced coagulants (steep water, alum, lemon, and lemon peel ash extract). Total flavonoid contents of all coagulated tofu were investigated as established in vitro flavonoid assay. The hepatoprotective activities of tofu flavonoid extracts against acetaminophen-induced hepatic cell toxicity in rats was also investigated in this study. The activity was analyzed by assessing the levels of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) and lactate dehydrogenase (LDH). The concentrations of the serum sugar, total protein, albumin, and cholesterol as well as prothrombin time (PT) of experimental rats with histopathological analysis were also conducted. The range of the total flavonoid contents of tofu was 4.3-6.4 mg/g. Tofu flavonoid extracts significantly reduced the activities of serum AST, ALT, ALP, and LDH; total cholesterol, and sugar levels, but total protein and albumin concentrations increased compared to acetaminophen-intoxicated rats. Also, the prothrombin time prolongation of serum in acetaminophen intoxicated rats was reduced. Histology of the liver tissue demonstrated that tofu flavonoid extracts inhibited the acetaminophen-induced hepatic cell necrosis, decreased inflammatory cell infiltration and accelerated hepatocellular regeneration. Therefore, all tofus exhibited high total flavonoid contents, and the tofu supplement in human diets is highly recommended as it can be used as a functional food to prevent liver injuries.

37-42

Authors: DH Geetha*, Indhiramuthu Jayashree, M Rajeswari

To investigate the anti-diabetic activity of Elaeocarpus serratus fruit in streptozotocin-induced (STZ) diabetic rats. The dose-dependent effects of 30days oral treatment with ethanol extracts of fruit (200 and 400 mg/kg) of E. serratus on body weight, blood glucose level, total protein, albumin, liver marker enzymes and carbohydrate metabolizing enzymes were evaluated in STZ-induced diabetic rats. Oral administration ethanolic extract of fruit of E. serratus showed significant restoration of the body weight and decrease in the blood glucose level, liver marker enzymes (ALT, AST ALP) and carbohydrate metabolizing enzymes were observed in diabetic rats. These results suggest that fruit extract of E. serratus has valuable anti-diabetic activity in STZ-induced diabetic rats which is comparable to the standard drug glibenclamide and hence might be of use in the management of diabetes.

50-56

Authors: Afagnigni Alian Désiré1*, Nyegue Maximilienne Ascension1, Ndoye Foe Chantal Florentine2, Voundi Olugu Steve1, Fonkoua Marie Christine3, Etoa Francois-Xavier1

Dissotis multiflora leaves are commonly used in the Cameroon traditional medicine to heal infectious diseases without solid scientific basis. This study aimed to investigate the phytochemical screening, in vitro antibacterial activity, phenol content and antioxidant activity of its ethanolic leaves extracts. Antibacterial test was assessed by agar well diffusion and microdilution methods against seven clinical isolates species namely Enterobacter cloacae, Klebsiella pneumoniae, Escherichia coli, Shigella flexneri, Proteus mirabilis, Salmonella typhi and Bacillus cereus. Total phenol content was determined by the Folin-Ciocalteu test while antioxidant activity was evaluated by DPPH, FRAP and ABTS methods. The phytochemical screening revealed the presence of phenols, tannins, alkaloids, saponins, anthraquinons, steroids and flavonoids. Extract inhibited the growth of all species tested with inhibition zone diameter ranged from 10.33 ± 1.24 mm (Klebsiella pneumoniae) to 28 ± 2.94 mm (Shigella flexneri) and MIC varying between 97.65µg/ml (Salmonella typhi) and 781µg/ml (Bacillus cereus and Enterobacter cloacae). Total phenol content was found to be 813.68 ± 1.27 mg ascorbic acid equivalent/g of dry material. The scavenging kinetics of DPPH by Dissotis multiflora extracts shows a steady state at 60 minutes while EC50 was 0.7 × 103 g/mol in DPPH. FRAP assay shows a reducing power of 7 ± 0.35 mg ascorbic acid equivalent/g of dry material. ABTS assay displayed an inhibition percentage of 93.269% at 4.54µg/ml. These results justify the use of Dissotis multiflora in traditional medicine to heal diarrhea and can be use as potential biomolecules reservoir.

65-67

Authors: Chandra Shekhar Sharma1*, Shashank Shekher Mishra1, Hamendra Pratap Singh1, Neeraj Kumar2

Cancer is a serious health problem that recognized as a group of diseases involving uncontrolled cell growth. Majority of cancer chemotherapeutic agents have serious toxicity profile. Due to this use of these agents are limited. Therefore, it is essential requirement for developing new chemotherapeutic agents to devoid toxicity. In this research work, we study the pharmacokinetic, toxicity and bioactivity profile of few selected chemotherapeutic agents by In silico method. These research investigations provide the lead for the development of new cancer chemotherapeutic agents with lesser toxicity and more effectiveness.

444-450

Authors: Valenčáková, A.*, Dziaková, A., Hatalová, E.

Gene therapy of cancerous diseases provides new means of curing patients with oncologic illnesses. There are several approaches in treating cancer by gene therapy. Most commonly used methods are: cancer immunogene therapy, suicide gene therapy, application of tumor-suppressor genes, antiangiogenic therapy, mesenchymal stem cells used as vectors, gene directed enzyme/prodrug therapy and bacteria used as anti-cancer agents. Cancer gene immunotherapy uses several immunologic agents for the purpose of explaining effective anti-tumor immune response. Another method is suicide gene therapy, based on introducing viral or bacterial agents to tumor cells, allowing the conversion of a non-toxic compound to a lethal medication. The application of intact suppressor genes to cancer cells will avert their neoplastic behavior and will induce tumor regression. Inhibition of angiogenesis is also a promising strategy for treating oncologic patients. Mesenchymal stem cells can also be used as vectors in targeted gene therapy. An increasing list of experimental evidence shows, that therapeutically modified mesenchymal stem cells in “gene directed enzyme/prodrug therapy” can attack cancer tissue can kill tumor cells, cancer stem cells included. Bacteria are used as anti-cancer agents independently of in combination with conventional therapeutic methods.

456-464

Authors: P. K. Gupta1*, D. S. Rathore1, G. Mohan1, J. K. Pandit2

The transdermal delivery of Diclofenac diethylamine has attracted considerable interest in recent years due to a lot of significant properties. Transdermal delivery system exhibits very poor permeation through the skin. Thus, an attempt was made to enhance the transdermal permeability of drug using nanoemulsion as vehicle. The main objective of this study was to develop a potential of nanoemulsion formulation for transdermal delivery of Diclofenac diethylamine for inflammatory disease. Transdermal patches were prepared using solvent evaporation technique. In this investigation, the transdermal patches (control) and nanoemulsion containing transdermal patches were prepared, compared and characterized for different physicochemical parameters (moisture content, moisture uptake folding endurance, in-vitro drug release). The optimized batch was also subjected for in-vivo anti-inflammatory study, pharmacokinetics (Cmax, Tmax and AUC) study and skin irritation study. The physical evaluation indicated that the prepared batches were smooth, flexible and translucent. The transdermal patch having 1:5 ratio of polyvinyl pyrrolidone and ethyl cellulose, exhibited a 1.7 fold increase in skin permeation compare to Diclofenac diethylamine patch. Nanoemulsion containing transdermal patch showed a significant increase in permeation parameters such as steady state flux (Jss); 0.061 mgcm-2hr-1 and permeability coefficient (Kp); 0.025 cmhr-1, when compared to the control. The mean Cmax of drug for optimized transdermal patch (TD) and nanoemulsion transdermal patch (NETD) was 2.56µg/ml and 3.42µg/ml, respectively. The in-vivo studies revealed a constant plasma concentration of drug for long period. Thus, results indicated that the nanoemulsion containing transdermal patches can be a promising tool for enhancing the percutaneous delivery of Diclofenac diethylamine.

474-477

Authors: Rachita Chengappa1*, Mangala Rakaraddi2, Asim Mustafa Khan3, Veena Narayanan1, Jijin Mekaddath4, Krupashankar Rangaswamy1

Antibiotics form an intergral part in the management of odontogenic infections. Streptococci group of bacteria have been implicated as one of the important causative agents in dental caries and dental abscess. The objective of this study was to determine the sensitivity and resistance of pathogenic facultative anaerobic streptococci to various routinely used antibiotics in odontogenic infections and also to determine appropriate empirical antibiotic therapy for the orofacial infections of odontogenic origin. Primary culture was performed for duration of 48 hours with the samples obtained from the patient. A lawn culture from the primary culture was made and antibiotic sensitivity testing was done using commercially available antibiotic disks by disk diffusion method. Standard strain of Streptococcus mutans (MTCC 497) was subjected to susceptibility testing by the above mentioned method. Poor susceptibility was seen in amoxicillin (18.4%), amoxicillin clavulanic acid (14.3%), and erythromycin (26.5%). Maximum resistance was noted for metronidazole (89.8%). High susceptibility was observed in tetracycline (67.3%), streptomycin (61.2%) and ciprofloxacin (44.9%). Low resistance was also exhibited by gentamycin (22.4%) and doxycycline (40.8%). Streptococcus mutans (MTCC 497) too showed similar results as that of the test samples. Due to the evolving resistance to all major antimicrobial agents used for treatment of odontogenic infections, antibiotic susceptibility testing is important to direct therapy. Antimicrobial susceptibility helps in monitoring the changing patterns of resistance and can be useful for empirical treatment of odontogenic infections.

484-488

Authors: Pavan Kumar Kothapuvari1*, Swati Rawat2, Darna Bhikshapathi3

A simple, precise, rapid and accurate RP-HPLC method was developed for the percentage drug release estimation of Eletriptan Hydrobromide in oral film dosage form. Eletriptan Hydrobromide is used to treat severe migraine headaches and it’s associated to nausea and sensitivity to light. Eletriptan Hydrobromide oral films were prepared by solvent casting method. It is available in market as conventional tablets (Relpax). An Xterra RP18 (150 × 4.6 with 5 microns particle size) and the mobile phase, consisting of KH2PO4 and triethylamine in water adjusting the pH-7.0 with o-phosphoric acid: acetonitrile in ratio of 98:2 v/v & acetonitrile: methanol HPLC Grade (80:20 v/v) was used as mobile phase in isocratic mode. The flow rate was 1.0 mL/min and the effluents were monitored at 225 nm. The retention time was 7.0 minutes and the detector response was linear in the concentration of 6.60-99.02µg/mL for Eletriptan Hydrobromide. The respective linear regression equation being Y = 11447 X + 5508 for Eletriptan Hydrobromide. The Limit of Detection (LOD) and Limit of Quantification (LOQ) were not applicable for dissolution parameter. The method was validated by determining its accuracy, precision, linearity and system suitability. The results of the study showed that the proposed RP-HPLC method is simple, rapid, precise, linear and accurate, which is useful for the routine estimation of percentage drug release of Eletriptan Hydrobromide in oral film dosage form.

493-497

Authors: Sharav A. Desai1*, Vipul P. Patel2, Dhara V. Patel3

The medicinal and pharmaceutical importance of currently available thrombolytic agents like urokinase, t-PA, streptokinase, staphylokinase and others, demonstrated repeatedly since 1970s, however sometimes they cause undesirable side effects like bleeding and allergic responds. The present findings reports isolation, screening and identification of soil bacterium for production of fibrinolytic enzyme. Samples for the study were collected from different locations were first screened for proteolytic activity using skimmed milk agar plate and lastly fibrin plate method was used to evaluate fibrinolytic activity. The strain capable of producing fibrinolytic protein was identified as Bacillus Spp. Using both Bergery’s manual of systemic bacteriology and biochemical characterization simultaneously. Selected strain was than subjected to the process of fermentation using basal media for 5 days, 37°C and at 180rpm. Protein content and fibrinolytic activity were measured by Biuret method using bovine serum albumin as standard and fibrinolytic assay respectively. Three stage purification was done, that includes salting out with ammonium sulphate, followed by gel filtration chromatography and finally separated by RP-HPLC, proteins were eluted in peaks with a retention time of 2.092, 3.188, 5.178, 7.295, and 11.32 minutes. The fraction with retention time 7.295 minutes shows a maximum activity. The enzyme found to be having an optimum pH between 7.0 and 7.5. Enzyme is also stable at the optimum pH and found to lose its activity on higher side of acidity or alkalinity. It is more active at 40°C and is stable at 37°C to 43°C with slight modification in activity.

384-394

Authors: Dinesh Kaushik*, Pankaj Kumar, Satish Sardana

The objective of this study is to prepare a formulation of Azithromycin which increase the oral bioavailability as well as increased solubility and dissolution rate. In the present study nine formulations were formulated by using the three different polymers and varying the concentration of PEG and also varying the rotation speed of the stirrer. Results of preformulation studies like melting point 117°C, UV spectroscopy and FTIR studies showed that the drug was pure. The spherical and rough surface of F9 viewed through SEM. In-vitro dissolution study had shown satisfactory results. On the basis of release data and graphical analysis formulation F8 and F9 showed a good controlled zero order release profile.

401-406

Authors: Abdul Malik P.H*, S Satyanandam, Sunil Murala

In the present work, an attempt has been made to formulate pH-induced in-situ gel as an ophthalmic drug delivery system. In situ gels are made from polymers that exhibit phase transition due to physicochemical change in the environment. They can be conveniently dropped as a solution into the conjuctival sac in the eye. Upon contact with the lacrimal fluid, the polymer changes its conformation to form a gel. This delivery system has the ease of administration similar to an opthalmic solution and has a long retention time because of the gel formation. Different polymers for preparing pH induced in-situ gels have been evaluated. The topical application of ophthalmically active drugs to the eye is the most prescribed route of administration for the treatment of various ocular diseases. It is generally agreed that the intraocular bioavailability of topically applied drugs is extremely poor. Upon instillation of an ophthalmic solution; most of the instilled volume is eliminated from the pre-corneal area. This loss is mainly due to drainage of the excess fluid by the nasolacrimal duct or elimination of the solution by tear turnover, which will results in poor ocular bioavailability. Lomefloxacin is member of the fluoroquinolone class of antimicrobial drugs. It is active against a wide range of gram positive and gram negative organisms.

412-416

Authors: Somara Sasikala1*, Siddamsetty Lakshminarasaiah1, Malepati Dhananjaya Naidu2

This study was conducted to evaluate the therapeutic effect of methanol extract Centella asiatica leaves by assaying the activities of diagnostic markers (aminotransferases) in the streptozotocin induced diabetic rats. The rats were divided into five groups with 6 rats in each group. The methanol extract of Centella asiatica leaves was orally administered at a dose of 300 mg/kg body weight (b.w), and glibenclamide was administered at a dose of 5 mg/kg b.w. The effect of methanol extract of Centella asiatica leaves on total protein and the activities of diagnostic marker enzymes aspartate aminotransferase (AST), alanine aminotransferase (ALT) were examined in the liver and kidney of control and experimental rats. The result showed a significant (p < 0.001) decrease in total protein concentration and increase in AST and ALT activities in the liver of diabetic rats whereas the levels were unaltered in the kidney of diabetic rats. The daily oral treatment of methanol extract of Centella asiatica leaves to diabetic rats for 30 days reversed the above changes in a significant (p < 0.001) manner. From our observations, we conclude that methanol extract of Centella asiatica leaves was able to restore the altered activities of aminotransferases. The obtained results were compared with glibenclamide, a standard antidiabetic drug. These results indicate that oral treatment with methanol extract of Centella asiatica leaves may be used to alleviate the liver functions impairment associated with diabetic condition.

421-424

Authors: Saurabh Kumar Sinha*

Some new Schiff bases of 4-aminopyridine were synthesized and evaluated for antiamnesic and cognition enhancing activity. In the current study to further understand the mechanism of action of these derivatives we have evaluated in-vitro acetycholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. Enzyme kinetics and docking studies were performed for all compounds to observe their nature of inhibition. The IC50 value of synthesized compounds showed maximum activity of compound 4APg compared to standard drug donepezil and rivastigmine whereas its kinetic analysis of enzyme inhibition demonstrated non-competitive inhibition for both enzymes AChE and BChE. The docking study confirmed their consensual interaction with AChE and BChE active sites justifying the experimental outcome.