METHOD DEVELOPMENT AND VALIDATION OF FAST DISSOLVING TABLET OF RAMIPRIL BY HPLC METHOD

Objective: The Objective of present work is method development and validation of HPLC method for the quantitation of Ramipril in Fast dissolving tablet (FDT).Methods: A stable, linear, rapid, accurate and selective HPLC method has been developed for the quantification of Ramipril in FDT using buffer and acetonitrile: methanol (60:40 v/v) ratio in combination as mobile phase and at the flow rate of 1 ml/minute at λmax 210 nm. Chromatographic separation was performed on Shimadzu SPD-20A, SD-M10 AVP-Shimadzu, an ODS C-18 Kromacil (250 mm × 4.60 mm) column used as stationary phase. The quantitation of Ramipril done by HPLC, parameters studied were retention time, linearity, accuracy, precision, detection limit, quantitation limit and stability.Results: Linear regression analysis data show a good linear relationship between response and concentration in the range of 5-30 µg/ml; detection carried out at λmax210 nm; the linear regression equation for Ramipril was Y=10327x+72877; R²=0.998. The retention time of the Ramipril was 2.910 min. Percent recoveries obtained for Ramipril was 99.58-100.15%. LOD and LOQ value was 0.802µg/ml and 1.4µg/ml for Ramipril respectively.Conclusion: The result suggested that proposed method gives good peak resolution of Ramipril within short analysis time (<10 min) and high percentages of the recovery shown that method is free from interference of excipient present in the formulation. The % RSD of each parameter lies below the limit of 2%, proven the suitability. The statistical analysis proved that the proposed method is precise, accurate, selective and rapid for the HPLC estimation of Ramipril.Keywords: Fast dissolving tablet, Ramipril, Accuracy, HPLC, Linearit

FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISSOLVING TABLET OF RAMIPRIL

Objective: The aim of this study was to prepare fast dissolving tablet of Ramipril by using Sodium starch glycolate, and Crospovidone as superdisintegrants to enhance the dissolution rate and the disintegration rate and evaluated for Pre and Post Compression parameter of the tablet.Methods: Fast dissolving tablet of Ramipril was prepared by direct compression technique. Fast dissolving tablet was evaluated for Pre compression parameter; bulk density, tapped density, Hausner's ratio, angle of repose and Carr's index and post compression parameter; weight variation, thickness, hardness, friability, wetting time, water absorption ratio, disintegration time and dissolution time. The UV-spectrophotometric method has been used for the quantitation of drug release of Ramipril in the Fast dissolving tablet formulation.Results: Pre and post compression parameter were evaluated. Five different batches of tablets, F1 to F5 were prepared. Bulk density and tapped density was found in the range of 0.64-0.85 g/cm3 and 0.68-0.98 g/cm3 simultaneously. The hardness, friability, wetting time, the water absorption ratio, disintegration and dissolution time were found to be acceptable according to the standard limit and compare to all formulations F4 formulation was selected as the promising formulation. All batches of fast dissolving tablet were satisfactory in term of dissolution. The cumulative percentage of drug release of F4 formulation was 90.12% after 12 min compare to other formulation.Conclusion: The result suggested that the dissolution and disintegration of Ramipril have improved considerably in batch F4 formulation as compared to rest of the formulation. The dissolution rate and dissolution rate of Ramipril can be enhanced to a great extent by the direct compression technique with the addition of superdisintegrants

Extraction and wound healing potential of Nerium Indicum M, Artocarpus Heterophyllus Lam, Murraya Koenigii L, Punica Granatum L on albino rats using burn wound model

Objective: The objective of present work was to extract the active constituents and evaluate the wound healing potential of Nerium indicum, Artocarpus heterophyllus, Murraya koenigii, Punica granatum on albino rats using burn wound model. Poly-herbal ointment and gel formulation was developed and compare with the extract of all plants. These plants has shown anti-asthmatic, anti-diabetic, anti-inflammatory, anti-microbial, anti-leukemic, anti-mycobacterial, antibacterial, antioxidant, antiulcer, antiviral, anticancer, antimalarial, anti-inflammatory and wound healing properties. Materials and Methods: Solvent extraction method has been utilized for the separation of the active constituents of interest by using 70% ethanol as a solvent. Poly-herbal ointment and gel formulations has been prepared by mixing the extract of Nerium Indicum, Artocarpus heterophyllus, Murraya koenigii and Punica granatum in different ratio with the ointment base (10-15%) contains PEG and for gel formulation Carbapol-940 base (10-15%). Burn wound model of albino rats has been utilized for the assessment of wound healing potential of the plant extract as well as developed formulations. Results and Conclusion: The studies on burn wound healing model reveals that F2 poly-herbal ointment formulation show better burn wound healing potential in comparison to all other formulations, F-1 ointment formulation as well as extracts of all plants. There was no mortality observed in the tenure of study. Discussion: These data has indicated that ointment and gel poly-herbal formulation of Nerium Indicum, Artocarpus Heterophyllus, Murraya Koenigii and Punica Granatum has been utilized for wound healing purpose and it is safer for topical application. No toxicity and mortality has been observed during the experimental tenure.  Keywords: Wound healing, Nerium indicum, Murraya koenigii, Punica granatum, Artocarpus heterophyllus, burn wound model

Design, synthesis and anticonvulsant potential of (E)-3-(5-(substituted aminomethyl)-1,3,4-thiadiazol-2-yl)-2-substituted styrylquinazolin-4-(3H)-one

Objective: The prime objective of the paper was to design and synthesize new derivatives of (E)-3-(5-(substitutedaminomethyl)-1,3,4-thiadiazol-2-yl)-2-styrylquinazolin-4(3H)-one and evaluated for their anticonvulsant potential. Material and methods: Various derivatives  of (E)-3-(5-(substitutedaminomethyl)-1,3,4-thiadiazol-2-yl)-2-styrylquinazolin-4(3H)-one derivatives has been synthesized by reacting 2-substituted benzoxazin-4-one with (E)-2-(4-Substituedstyryl)-4H-benzo[d][1,3]oxazin-4-one. All synthesized compounds have been characterized by the IR, NMR and mass spectral analysis. Proposed compounds have been evaluated for anticonvulsant potential by subcutaneous pentylenetetrazole (scPTZ) and maximal electroshock seizure (MES) model and compared with the reference drug phenytoin &carbamazepine. Result and discussion: The subcutaneous pentylenetetrazoles (scPTZ) model denotes that compounds SB-6, SB-12, SB-14 and SB-18 were found most active at anticonvulsant screening when compared with phenytoin and carbamazepine (standard drug).The most active compound of the series was SB-1, SB-4, SB-6, SB-9, SB-12, SB-14, SB-14 and SB-18. In most of the Cl and nitro group phenyl ring in position of the 1,3,4-thiadiazoles nucleus and Cl on phenyl ring of 4(3H)-quinazolinone has shown the potent activity. Keywords: quinazolinone, anticonvulsant, maximal electroshock seizure, phenytoin, carbamazepin

Extraction of Momordica charantia, Pongamia glabra and Piper nigrum: Qualitative and Quantitative assessment

Objective: The objective of present work was to evaluate the qualitative and quantitative assessment of momordica charantia, pongamia glabra and piper nigrum extract for the natural product present in them. These plants were having the rich source of alkaloid, glycoside, tannins, carbohydrates, saponins, flavonoids, proteins and amino acids and were used as anti-diabetic, anti-inflammatory, antitumor, anti-malarial and having wound healing potential. Materials and Methods: Extract of all three plants has been separated by the process of Soxhlet extraction. The extract of momordica charantia, pongamia glabra and piper nigrum evaluated for qualitative and quantitative measurement of alkaloid, glycoside, tannins, carbohydrates, saponins, flavonoids, proteins and amino acids content. Different solvent is used for the extraction of content includes petroleum ether, ethyl acetate, alcoholic and distilled water. Results and Conclusion: Preliminary Phytochemical screening was performed for extracts of Momordica charantia fruits (FMC), Pongamia glabra (LPG) and Piper nigrum fruits (FPN). Identification test on extracts was shown the sign of alkaloid, glycoside, tannins, carbohydrates, saponins, flavonoids, proteins and amino acids content. Discussion: All results indicates that extracts of Momordica charantia fruits (FMC), Pongamia glabra (LPG) and Piper nigrum fruits (FPN) having a rich source of Glycosides, alkaloid and flavonoid content. Keywords: momordica charantia, pongamia glabra, piper nigrum, glycosides, flavonoid, extraction

Development, characterization and evaluation of herbal ointment containing momordica charantia, pongamia glabra and piper nigrum

Objective: The objective of present study was the development, characterization and evaluation of poly-herbal ointment formulation of pongamia glabra, piper nigrum and momordica charantia extract. Plant derived substances and herbal medicines have recently attracted the great interest towards their versatile application. Medicinal plants are the richest source of bioactive compounds used in traditional and modern medicine. The ointment formulation of plant extract has a sound approach to develop a poly-herbal ointment. The poly-herbal ointment formulation was evaluated for its physicochemical parameters like color, odor, pH, spreadability, extrudability, consistency, diffusibility, solubility, washability and stability. Materials and methods: Extract of all three plants has been separated by the soxhlet extraction. Poly-herbal ointment has been prepared by mixing the extract of momordica charantia, pongamia glabra and piper nigrum with wool fat, Cetostearyl alcohol and paraffin. Results and conclusion: Physicochemical evaluation shows that the poly-herbal ointment fulfilled the criteria as herbal formulation and irritancy test also performed indicate the effectiveness and efficacy of prepared ointment formulations. The poly-herbal ointment formulations were also evaluated for its stability at various temperature conditions which shows no change in the irritancy, spreadability and diffusion study. Thus it could become a medium to use the medicinal properties of extracts effectively and easily as a simple dosage form. Keywords: Momordica charantia, pongamia glabra, piper nigrum, ointment, Cetostearyl alcohol

Development, characterization and evaluation of poly-herbal ointment and Gel formulation containing Nerium Indicum Mill, Artocarpus Heterophyllus Lam, Murraya Koenigii Linn, Punica Granatum Linn

Objective: The objective of present study was the development, characterization and evaluation of poly-herbal ointment and gel formulations of Nerium Indicum Mill, Artocarpus Heterophyllus Lam, Murraya Koenigii Linn, Punica Granatum Linn extract. Plant derived substances and herbal medicines have recently attracted the great interest towards their versatile application. Medicinal plants are the richest source of bioactive compounds used in traditional and modern medicine. The ointment and gel formulation of plant extract has a sound approach, The poly-herbal ointment and gel formulation were evaluated for its physicochemical parameters like color, odour, pH, spreadability, extrudability, consistency, diffusibility, solubility, washability, non-irritancy and stability. Materials and methods: Extract of all four plants has been separated by the soxhlet extraction by 70% ethanol. Poly-herbal ointment and gel formulation has been prepared by mixing the extract of Nerium Indicum Mill, Artocarpus Heterophyllus Lam, Murraya Koenigii Linn, Punica Granatum Linn with carbapol 940 for Gel formulation and PEG 2000 & PEG 600 for ointment formulation. Results and conclusion: Physicochemical evaluation shows that the poly-herbal ointment and gel formulations fulfilled the criteria as herbal formulation and irritancy test also performed to indicate the effectiveness and efficacy of prepared ointment and gel formulations. The poly-herbal ointment and gel formulations were also evaluated for its stability at various temperature conditions which shows no change in the irritancy, spreadability and diffusion study. Thus it could become a medium to use the medicinal properties of extracts effectively and easily as a simple dosage form. Keywords:  Nerium Indicum Mill, Artocarpus Heterophyllus Lam, Murraya Koenigii Linn, Punica Granatum Linn, extract, ointment, gel.    &nbsp

Wound healing prospective of pongamia glabra, piper nigrum and momordica charantia on albino rats using anemic burn wound model

Objective: The objective of present work was to evaluate wound healing potential of pongamia glabra, piper nigrum and momordica charantia using as herbal ointment formulation on albino rats using burn wound model.  All the plant has the rich source of alkaloid, glycoside, tannins, carbohydrates, saponins, flavonoids, proteins and amino acids content and were used as anti-diabetic, anti-inflammatory, antitumor, anti-malarial and having wound healing potential. Materials and Methods: Extract of all three plants has been separated by the Soxhlet extraction. Herbal ointment formulation has been prepared by mixing the extract of momordica charantia, pongamia glabra and piper nigrum with the wool fat and paraffin. Burn wound model has been utilized for the evaluation of wound healing potential. Histopathological evaluation has been also carried-out for the physical verification wound healing potential. Results and Conclusion: The studies on burn wound healing model reveals that all twelve groups showed decreased wound area on the time and there was no mortality observed in the course of study. Discussion: These studies have indicated that herbal ointment formulation of pongamia glabra, piper nigrum and momordica charantia has been utilized for wound healing and it is safer for topical application. No toxicity and mortality have been observed during the experimental tenure.  Keywords: Wound healing, momordica charantia, pongamia glabra, piper nigrum, burn wound mode

DESIGN, SYNTHESIS, AND EVALUATION OF NEW DERIVATIVE OF 1,2,4-TRIAZOLES FOR ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITY

Objective: The object of the study is to design, synthesize and biological evaluation of isoniazid derived 1,2,4-triazoles compounds.Methods: Isoniazid based 1,2,4-triazoles derivatives have been synthesized by reaction of Isoniazid with carbon disulfide in basic medium (KOH) to form Potassium dithiocarbazinate salt and reaction with hydrazine hydrate converted into 4-amino-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol. These compounds were reacted with seven different benzaldehyde to form 4-[(substituted phenyl)-methylene]-amino-5-(pyridine-4-yl)-4H-1,2,4-triazol-3-thiol (4). The final compounds were synthesized by reaction with four different acetanilide to form 4-[substituted phenyl)-methylene]-amino-3-(N-substitutedcarboxamidomethylthio)-5-(pyridine-4-yl)-4H-1,2,4-triazoles derivatives. All these compounds were characterized by IR, 1H-NMR, [13]C-NMR and elemental analysis. The antimicrobial activity was determined by the cup plate method. Acute anti-inflammatory activity determined by using carrageenan-induced rat paw edema model.Results: Series PJ-A4, PJ-A7 and PJ-A13 showed more than 90% of the zone of inhibition against both Gram positive and Gram negative organisms. The antifungal study suggested that among synthesized compounds series PJ-A4, A7, A9, A11 and A13 showed more than 90% of zone of inhibition, A2, A10 and A12 shows more than 80% of the zone of inhibition. Anti-inflammatory study data indicate that compounds PJ-A4, PJ-A8, PJ-A9 and PJ-A13 produced 70 to 76% of paw edema inhibition compare to standard drug Ibuprofen which showed 83.3% after 5 h. Conclusion: Results suggested that the isoniazid based 1,2,4-triazole derivatives have significant antibacterial, antifungal and anti-inflammatory activity

Molecular Approaches for Malaria Therapy

Malaria is a potentially fatal blood disease spread by mosquitos. Malaria is preventable, but it is more prevalent in developing countries where prevention is difficult and prophylaxis is often inaccessible. Malaria remains one of the world’s most serious public health problems, according to the World Health Organisation (WHO). The development of resistance is a current problem that poses a danger to the environment. Resistance is a current problem that could jeopardise the use of well-established and cost-effective antimalarials. The World Health Organisation recommends an artemisinin-based drug combination (ACT) to avoid or postpone the development of resistance. This book’s chapter discusses current medicines as well as potential and rational possibilities for finding new drugs to treat malady. There were also WHO recommendations for both complicated and non-complicated malaria. Other preventive measures such as ITN and IPT are listed in the manuscript in addition to routine care. While a brief overview of the vaccine tested so far has been included, there is currently no vaccine available to treat malaria