International Journal of Pharmaceutical Sciences and Drug Research

136-143

Authors: Nadeem Siddiqui*, M. Faiz Arshad, Waquar Ahsan, M. Shamsher Alam

Thiazoles displayed broad range of biological activities and found in many potent biologically active molecules such as Sulfathiazol (antimicrobial drug), Ritonavir (antiretroviral drug), Abafungin (antifungal drug) and Tiazofurin (antineoplastic drug). So far, modifications of the thiazole ring have proven highly effective with improved potency and lesser toxicity. The present review highlights the recently synthesized thiazoles possessing important biological activities.

154-157

Authors: Srivastava Shikha1, Mishra Nidhi1, Misra Upama2*

Bacopa moniera, a traditional Ayurvedic plant, used for centuries as a memory enhancing, anti-inflammatory, analgesic, antipyretic, sedative and antiepileptic agent. The plant, extract and isolated bacosides (the major active principles) have been extensively investigated in several laboratories for their different biological activities. In addition researchers have evaluated the anti-inflammatory, cardio tonic and other pharmacological effects of Bacopa monniera preparations/exracts. Therefore, in view of the important activities performed by this plant, research is an on going process over Bacopa monniera.

164-171

Authors: Sanjeev Kumar1, Chander Parkash2, Pradeep Kumar3, S. K. Singh4*

Mefenamic acid (MFA), a potent non-steroidal anti-inflammatory drug (NSAID), has a low oral bioavailability due to poor aqueous solubility and insufficient dissolution. In order to improve the same, various techniques were employed viz., evaporative precipitation into aqueous solution (EPAS), spherical agglomeration (SA) and solid dispersion using solvent evaporation and melt mixing. The formulations were characterised by differential scanning calorimetry (DSC) and X-Ray powder diffractometry (XRD) and were investigated for drug content studies, solubility studies, in vitro study and in vivo evaluation of anti-inflammatory activity. The formulations of MFA prepared by spherical agglomeration technique have satisfactory good drug content and the formulations with SLS and HPMC show a significant increase in solubility in case of SA technique. In case of solid dispersion, all carriers show improvement in the dissolution rate of the drug The DSC studies show no change in the polymorphism in most of the formulations The XRD studies of the formulations show no change in their crystalline form. The formulation containing HPMC & SLS as drug carrier show better anti-inflammatory effect with comparison to pure drug confirming the improved bioavailability of this drug.

176-179

Authors: Sanja S. D.1*, Sheth N. R.2, Joshi D. M.1, Golwala D. K.3, Patel Dhaval4, Raval M. K.2

In the present study, methanolic extract of Ipomoea reniformis herb (MEIR) in acute, subacute and chronic models of inflammation was assessed in rats. Administration of MEIR (200, 400 mg/kg, p.o.) exhibited significant anti-inflammatory activity. In acute inflammation as produced by Carrageenan 59.55 % and 64.04 % protection was observed. While in subacute anti-inflammatory models using formaldehyde-induced hind paw edema (after 1.5 h) 38.36 % and 47.95 % and in chronic anti-inflammatory model using cotton pellet granuloma 15.02 % and 19.19 % protection from inflammation was observed. MEIR did not show any sign of toxicity and mortality up to a dose level of 1000 mg/kg, p.o. in rats. The results obtained suggest that the methanolic extract of Ipomoea reniformis herb (MEIR) is endowed with effective anti-inflammatory activity mediated via either by inhibition of cyclooxygenase cascade and by blocking the release of vasoactive substances (histamine, serotonin and kinins). These findings seem to justify the use of the plant in traditional Indian medicine in the treatment of inflammation, including arthritic conditions.

183-187

Authors: Nimish Pathak1*, Priyanshee Gohil1, Natawar Bhai Patel1, Sanjay Kasture2, Nirruddin Jivani3, Yagnik Bhalodia3

Localized bone loss in the form of bone erosions and peri-articular osteopenia constitutes important signs for the diagnosis of rheumatoid arthritis. In the present study, the effect of Albizia lebbeck Methanolic extract (AL) on the bone erosion turn over was studied by analyzing various markers of bone erosion like histological and radiological analysis of the joints in Freund’ complete adjuvant induced- arthritis in rats. The anti-arthritic activity of methanol extract of the bark of Albizia lebbeck (Mimosaceae) was evaluated against Freund’s complete adjuvant induced- arthritis induce arthritis model in rats. Arthritis was induced in rats by injecting 0.1ml of Freund’s complete adjuvant containing 6 mg of heat killed mycobacterium tuberculosis in 1ml paraffin oil into the left hind paw of the rat intradermally. AL (200 mg/kg, 400 mg/kg, 600 mg/kg body weight/day) was administered orally for 12 days. On 21st day of experiment, the histopathological and radiological observation was carried out along with rheumatoid factor and arthritic index. It can be concluded that Albizia lebbeck Methanolic extract (AL) possesses strong anti-arthritic property by modulating bone erosion.

191-194

Authors: Appia Krishnan G.1*, Rai V. K.2, Nandy B. C.2, Meena K. C.2, Dey S.2, Tyagi P. K.2¬¬, Tyagi L. K.3

The present study was designed to evaluate the preliminary phytochemical investigation of Aerva lanata Linn. (Family, Amaranthaceae), and anti-diabetic effect of Arial parts of plant Aerva lanata Linn. in normal and Alloxan induced diabetic rats. Ethanolic extract of Arial part of Aerva lanata Linn. were evaluated for four weeks treatment for hypoglycemic activity in diabetic albino rats; at doses of 50,100 and 200 mg kg -1 body weight ,its effects on the blood glucose and other biochemical parameters like cholesterol, urea, creatinine, billirubin and SGPT in Alloxan induced diabetic rats were investigated. Diabetes was introduced by single tail-vein injection of Alloxan (60 mg kg -1). Oral administrations of Aerva lanata Linn. extract to diabetic animals up to four weeks; dose dependently reduced the blood glucose level, which is comparable to standard dose of Metformin. Significantly decreased in body weight was observed with diabetic control, which was partially restored upon administration Aerva lanata Linn. extract (50, 100, 200 mg kg -l). Alcoholic extract of Arial part of A. lanata Linn. also altered other biochemical parameters level. It was concluded from the results that the alcoholic extract of A. lanata Linn. possesses anti-diabetic effect in experimental animals.

203-206

Authors: Maulik Suthar*, Rakesh Patel, Kalindi Hapani, Avani Patel

The fruits of Embelia ribes reported to contain mainly benzoquinone derivatives such as Embelin (2, 5-dihydroxy-3-undecyl-2, 5-cyclohexadiene-1, 4-benzoquinone). Chemical structure of Embelin is having quite resemblance with the structure of natural Coenzyme Q10 (ubiquinones) and the role of this is well defined in various biochemical protective mechanism. Aim of the present study was to evaluate the antifungal activity of Embelia ribes (Myrsinaceae) plant extracts using standard in vitro antifungal susceptibility test methods like NCCLS M27- A2 protocol (The National Committee for Clinical Laboratory Standards , USA) and EUCAST (European Committee for Antifungal Susceptibility Tests). Values of the MIC50 obtained by NCCLS method revealed that Methanol extract and Embelin exhibited lowest MIC50 values against C. albican (183) which was 120 mg/L. Embelin's MIC50 values were below 700 mg/L for C. albican, C. tropicalis, C. parapsilosis, C. albidus and A. flavus. Diethyl ether extract, petroleum ether extract, methanol extract and embelin obtained MIC50 in range of 300-700 mg/L against C. albican and C. parapsilosis. Petroleum ether extract showed lowest MIC50 values for C. parapsilosis (250 mg/L); C. laurintis (360 mg/L); I.orientalis (180 mg/L) and A. fumigatus(170 mg/L).

63-70

Authors: Jagan Mohan Kandukuri, Venkatesham Allenki*, Chandra Mohan Eaga, Vasu Keshetty, Kiran Kumar Jannu

Multiparticulates are discrete particles that make up a multiple unit system. Although pellets have been used in the pharmaceutical industry for more than four decades, with the advent of controlled release technology, that the full impact of the inherent advantages of pellets over single unit dosage forms have been realized, not only has focused on refining and optimizing existing pelletization techniques, but also focused on the development of novel approaches and procedures for manufacturing of pellets. The present review outlines the manufacturing and evaluation of pellets. The manufacturing techniques include layering, cryopelletization, freeze pelletization, extrusion spheronization and hot melt extrusion have been discussed. Characterization of pellets is discussed with reference to the particle size distribution, surface area, porosity, density, hardness, friability and tensile strength of pellets.

74-79

Authors: K.P.R. Chowdary1, K. Sree Deepthi2, Y. Srinivasa Rao2*

Mucoadhesive microcapsules of indomethacin were prepared by an emulsification-ionic gelation process employing sodium carboxy methylcellulose, methylcellulose, Carbopol and hydroxy propyl methyl cellulose along with alginate and the microcapsules were evaluated for release kinetics and ulcerogenic activity. The resulting microcapsules were discrete, free flowing, multinucleate, monolithic and spherical. Microencapsulation efficiency was 41-70 % and relatively high with alginate-sodium carboxymethylcellulose. Indomethacin release from these mucoadhesive microcapsules was found to be slow and extended over longer periods of time and depended on the composition of coat and size of the microcapsules. Drug release was diffusion controlled and followed first order kinetics. Alginate-methyl cellulose and alginate-sodium carboxymethylcellulose microcapsules were found suitable for oral controlled release. The microcapsules exhibited good mucoadhesive property in the in vitro wash-off test. Release from some microcapsules fulfilled the official (USP 23) drug release test-2 requirement of indomethacin extended release capsules. A 62-80 % reduction in ulcerogenic activity was observed with these microcapsules when compared to pure drug indomethacin.

83-84

Authors: Dinesh Kaushik1, Satish Sardana1, D. N. Mishra2*

The present investigation was aimed to develop a new formulation containing chemically cross-linked guar gum microspheres loaded with 5-fluorouracil for targeting of colorectal cancer. The emulsification polymerization method involving the dispersion of aqueous phase of guar gum in castor oil was used to prepare spherical microspheres. Cytotoxicity analysis on HT-29 human colon cancer cell lines indicated that 5-FU loaded guar gum microspheres leads to sustained releases of drug and thus delayed apoptosis over a long period of time. In this way, 5-fluorouracil loaded guar gum microspheres have shown promising results in the management of colorectal cancer, warranting thorough in vivo study for scale up technology.

91-99

Authors: Nandy B. C.a,b*, Gupta R. N.a, Rai V. K.b, Das S.c, Tyagi L. K.d, Roy S.e, Meena K. C.b

In the present investigation, we prepared Atenolol (1.5 % w/w) solution and various polymer formulations by incorporating the tween-20 or L-menthol, as a penetration enhancers and its effect on permeation of the drug through the excised abdominal rat skin were used to examined by using the vertical Franz-type diffusion cell. The physicochemical interactions between Atenolol and various polymers were investigated by performing the assay, ultra violet absorption maxima, Fourier transform infrared spectroscopy and it was further confirmed by thin layer chromatography studies, from which drug did not show any evidence of interaction with the polymers. We found that, L-menthol was superior than tween-20 to iontophoresis [current density applied 0.5 mA/cm2 and 90:10 (on: off) ratio], in enhancing the transdermal permeation of Atenolol; it enhanced the flux of Atenolol by more than 2-folds, comparison to the preparations without penetration enhancer via passive diffusion, and 3 folds increased using iontophoresis alone with a shorter lag time. Atenolol also showed good stability in gel formulations. The basic parameters like % loading dose released at the end of the study, permeation coefficient and steady state flux (Jss) were calculated and showed statistically significant difference (p<0.05). The results indicated that suitable iontophoretic delivery with desired permeability could be appeared and the cumulative amount-time curves were suitable to fit by a zero order equations which indicated a steady state permeation rate or sustained effect could be achieved from hydrogel; when it is combined with penetration enhancer, L-menthol. The results demonstrate that the semisolid gel formulations are more applicable than solution as a transdermal iontophoretic delivery system to administer clinically. Electrically assisted transdermal delivery of Atenolol significantly increased transport compared to passive delivery. Also, rapid and modulated delivery was shown to be feasible by programming the electrical parameters.

103-106

Authors: R. K. Gupta1*, U. K. Singh2, S. Kumar2, B. Moothan3

A simple, precise and reproducible reverse phase, isocratic high performance liquid chromatographic method was developed and validated for the quantitative determination of sodium valproate in bulk and enteric coated tablet dosage form. The quantification was carried out using a Nova-pack phenyl, 4µm, 150 mm × 3.9 mm i.d. column, with a mobile phase consisting of acetonitrile: buffer (30:70, v/v) (pH 2.5) at a flow rate of 1.2 ml/min and UV detection at 210 nm. The method was validated for specificity, linearity, accuracy, precision, limit of detection, limit of quantification, robustness and solution stability. The linearity of the proposed method was investigated in the range of 50-1500 µg/ml (r = 0.9999). Mean inter- and intra-assay relative standard deviations (RSD) were less than 2.0 %. The proposed method was successfully applied for the analysis of sodium valproate in bulk and pharmaceutical dosage forms. Also, the method was extended for determination of sodium valproate release from in-vitro dissolution studies.

110-112

Authors: Guno Sindhu Chakraborthy*, Vidhu Aeri1

Extracts of leaves and stems of Chlorophytum borivilianum were subjected to preliminary phytochemical screening and in-vitro antimicrobial studies. The results of the preliminary investigation revealed the presence of alkaloids, glycosides, steroidal nucleus, saponins and tannins in both parts. The methanolic extract of leaf and stems part were investigated for antimicrobial activity using agar disc diffusion method. Six clinical strains of human pathogenic microorganisms, comprising 3 Gram +ve, 1 Gram -ve and 2 fungi were utilized in the studies. The leaf extract of Chlorophytum borivilianum displayed overwhelming concentration dependent antimicrobial properties, inhibiting the growth of Staphylococcus aureus and Bacillus cereus, far above that of ampicillin used in a concentration of 1.0 g/ml. The extract was less sensitive to 2 Gram -ve bacteria in the assay. In antifungal assay, the growth of Aspergillus niger and Candida albicans, were inhibited in the same manner comparable to voriconazole the reference drug used in the study. The methanol extract of stem also displayed a concentration related antibacterial activity, inhibiting the growth of S. aureus comparable to ampicillin at 1.0 g/ml. The extract was least active against Escherichia coli with a mild activity at 1.0 g/ml. The extract exhibited weak activities against C. albicans as well as A. niger. Both plant parts seem to justify their ethno medical uses.

116-118

Authors: Akanksha D1*, Vikas G1, Neetesh K. J1, Shailendra S2, Neelam B1, Dinesh K. J1

Present investigation was to develop novel ointment formulation in combination of natural wound healing agent curcuma longa, which is reported to possess wound healing and anti-bacterial activities. Combination of neomycin sulphate and curcuma longa is good rational, where curcuma longa produces synergistic wound healing effect with neomycin sulphate. Formulations containing fixed concentration (0.5 %) of neomycin sulphate and 3 %, 4 % and 5 % of curcuma longa were prepared. To assess the efficacy of formulations anti-bacterial activity, rheology, stability, spreadability and other physical characteristics were evaluated. The results obtained were encouraging and formulation containing neomycin sulphate (0.5 %) with 5 % of curcuma longa was found better than other formulations.

121-123

Authors: Guno Sindhu Chakraborthy*

Plants are the best source of active secondary metabolites which are beneficial to mankind. Many plant origin drugs have been reported with biological properties like Analgesic, Anti-inflammatory, Antioxidant, hypoglycemic agents and many more. The successive extracts of Aesculus indica leaves were screened for in vitro antioxidant properties using the standard procedures. The successive extracts such as petroleum ether, ethyl acetate, methanol and water and 50% crude methanol extracts exhibited IC 50 values of respectively in DPPH and respectively in nitric oxide radical inhibition assays. The values are comparable with the standards such as ascorbic acid and quercetin. The Aesculus indica leaves are showing significant antioxidant activity.

6-8

Authors: Kaushik D.1*, Khokra S. L.1, Kaushik P.1, Saneja A.1, Sharma C.2, Aneja K.R.2, Chaudhary B.1, Koshy S.3

The present study was designed to evaluate the analgesic and antimicrobial activities of ethanolic extract of leaves of Mitragyna parvifolia plant (Rubiaceae) family. The analgesic activity was carried out on swiss albino male mice by Eddy’s hot plate and Acetic acid induced writhing test. The extract showed only moderate analgesic potential in acetic acid induced writhing test at all the test doses while the extract at the dose of 500 mg/kg (P<0.01) showed strong analgesic activity comparable to standard drug Diclofenac sodium (50 mg/Kg, i.p.) in hot plate method. The extract in different concentrations was also tested for antibacterial activity using agar well diffusion method. The extract significantly inhibited S. aureus and showed some degree of inhibition against P. aeruginosa and E. coli.

13-18

Authors: Sanjay Dey1, Bhaskar Mazumder1, J. R. Patel2*

The aim of this study was to investigate the effect of DMSO on the permeation of acyclovir in the form of topical gel formulations. Different formulations were prepared containing carbopol 934P, acyclovir (1 % w/w) and selected concentration of DMSO (0 to 10% w/w) to evaluate drug content, spreadibility, pH, viscosity, and in-vitro permeation through mouse epidermis and porcine skin. FTIR spectrometry was used to investigate physical state of drug in the gel formulations. The mechanisms of drug permeation were evaluated by FTIR spectrophotometer and histopathological studies. The carbopol 934P gel was found to contain 95.62 to 98.89 % of acyclovir and spreadibility was found in the range of 10.75 to 11.75 g.cm/sec. The pH of all formulations was found near to the skin pH value. The viscosity of the formulations was found inversely proportional with drug permeation. A maximum permeation flux of acyclovir (463.42±36.41µg/cm2.h) through porcine skin was observed with an enhancement ratio of 1.55, when DMSO was incorporated at a concentration of 10%w/w in gel system. The FTIR spectra revealed the absence of drug-polymer interaction. From FTIR spectroscopy and histopathological studies it was evident that the permeation of acyclovir, across mouse and porcine skin, were increased in presence of DMSO which can be attributed to the partial extraction of lipids in the stratum corneum. The results suggest that DMSO may be useful for enhancing the skin permeability of acyclovir from transdermal therapeutic system containing carbopol 934P gel as reservoir.

24-27

Authors: Nikhil K. Sachan1*, Yatindra Kumar2, Seema Pushkar1, R. N. Thakur2, Sudhir S. Gangwar2, V. K. Kalaichelvan3

The present investigation aims to examine the diabetic potential of the plant Ficus racemosa in normal and alloxan induced diabetic rats. The bark extract with water, petroleum ether and with alcohol were screened for blood glucose lowering activity and the alcoholic extract having better therapeutic potential was prepared through Soxhlet extraction for further study. Alcoholic and aqueous extract of bark of Ficus racemosa at a dose of 400 mg/Kg was given to normal and alloxan induced diabetic rats and the blood samples taken from the retero-orbital plexus vein were analyzed for blood glucose level as per standard protocol with available kits through Auto-analyzer. The comparison of blood sugar level as per model schedule showed that in normal group the ethanolic extract, at a dose of 400 mg/Kg intra-peritoneal, the blood glucose lowering 28.66 % while in aqueous extract given group it was 25.90 %. In alloxan induced diabetic rats decrease in blood glucose level in aqueous and ethanolic extract group was found to be 27.01 % and 45.03 % respectively. In conclusion, the ethanolic extract of Ficus racemosa reflected anti-diabetic potential through its glucose lowering activity in experimental animals. It supported the folklore claim of anti-diabetic activity of the plant.

32-35

Authors: Jani Rupal1*, Jani Kaushal2, Setty C. Mallikarjuna.3, Patel Dipti1

Aceclofenac is a potent anti-inflammatory analgesic agent indicated for acute and chronic treatment of rheumatoid arthritis, ostio arthritis, and onkylosing spondylytis. Aceclofenac is poorly water soluble and may show dissolution limited absorption. Solid dispersions (SDs) of Aceclofenac in PEG-6000, PVP were prepared by solvent evaporation method. The solid dispersion was characterized for physical appearance, solubility and IR. FTIR study reveled that drug was stable in SDs. Solubility of Aceclofenac from SDs increased in distilled water. The drug content was found to be high and uniformly distributed in the all formulation. Dissolution of drug increased from all the solid dispersion. Dissolution of Aceclofenac increased with increase in the proportion of carriers (1:1, 1:5, and 1:9). Of both the carriers used, dissolution of the drug was more in PEG 6000 based SDs. It is concluded that dissolution of the Aceclofenac could be improved by solid dispersion and PEG 6000 based solid dispersions were more effective in the enhancing the dissolution.

43-45

Authors: Choudhary B.1*, Goyal A.1, Khokra S. L.2, Kaushik D.2

A simple, accurate and reproducible HPLC method have been developed for simultaneous estimation of Diclofenac sodium and rabeprazole from their tablets formulations. A phenomenex C18 (Luna) column of length 250×7.5 mm with particle size of the stationary phase 5 µm and S mobile phase potassium dihydrogen phosphate buffer (pH adjusted to 7.5 with 1 M sodium hydroxide) and acetonitrile in the ratio 60: 40 were used in this study. Retention time was found to be 9.20 min and 6.40 min for Rabeprazole and diclofenac sodium respectively. While that for internal standard as domperidone was 11.87 min at a flow rate of 2ml / min. Linearity was found in the concentration range of 10-50 µg /ml for both the drugs in this method. The results of analysis have been validated statistically and also by recovery studies.

51-54

Authors: Rai V. K.1*, Pathak N.1, Bhaskar R.2, Nandi B. C.1, Dey S.1, Tyagi L. K.3

The purpose of this research is to prepare Raloxifene Hydrochloride immediate release tablet by wet granulation technique. In order to obtain the best, optimized product six different formulations were developed. Different filler, binder, disintegrant and lubricant were taken as variables. Weight variation, thickness, hardness, friability, disintegration time, in-vitro release and pharmaceutical assay were studied as response variables. Sticking was observed when the formulation containing stearic acid and sodium stearyl fumarate. However, in the remaining four formulation containing magnesium stearate, no sticking was observed. The formulation NP061 was selected as an optimized product. The different physical properties and in-vitro release profile showed best comparable with reference product. Optimization has proven as an effective tool in product development.