IJPAR | International Journal of Pharmacy and Analytical Research

International Journal of Pharmacy and Analytical Research

ISSN: 2320_2831

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  1. Design, synthesis, spectral analysis, antibabacterial activity of n-(3-chloro-2-oxo-4-arylazetidin-1-yl)-3 hydroxybenzofuran-2- carboxamide derivativesDownload Article

    Mohsina Abid, S. Imam Pasha
    • Article Type: Research Article
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    • Pages (518-524)
    • No of Download = 379

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    3-hydroxybenzofuran-2-carbohydrazide undergoes facile condensation with aromatic aldehydes to afford the corresponding N-arylidene-3-hydroxybenzofuran-2-carbohydrazide in good yields. Cyclo condensation of compounds with chloro acetyl chloride yields N-(3-chloro-2-oxo-4-arylazetidin-1-yl)-3 hydroxybenzofuran-2- carboxamide. The structures of these compounds were established on the basis of analytical and spectral data. The newly synthesized compounds were evaluated for their antibacterial activity.

  2. Design, synthesis, spectral analysis & antibacterial activity of thiazol- pyrimidine 5-carboxamide derivativesDownload Article

    GhazalaYasmeen S.Imam Pasha
    • Article Type: Research Article
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    • Pages (525-533)
    • No of Download = 304

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    Several fused heterocycles based on thiazolidinone derivatives were synthesized and characterized using physical properties, elemental analysis, IR and other spectral studies. New ligands i.e. 4-(2-furyl)-6-methyl-2-oxo-thiazol- pyrimidine-5-carboxamidewere synthesized by condensation reaction of thiazolidinone derivatives with phenyl hydrazine in presence of glacial acetic acid. Furthermore the antibacterial of newly synthesized fused heterocyclic compounds was examined against various microbial strains.

  3. Formulation, invitro evaluation & stability studies of the bilayered tablets of combination-glipizide (I.P) & pioglitazone (I.P)Download Article

    Romana Siddiqua, Dr.Syed Abdul Azeez Basha
    • Article Type: Research Article
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    • Pages (534-545)
    • No of Download = 576

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    The objective of present investigation was to formulate and evaluate bilayered tablets containing Pioglitazone (I.R) & Glipizide (S.R).The Bilayered tablets prepared by direct compression method. The sustained release layer is prepared by wet granulation method using synthetic and natural polymers like HPMC K4M, Ethylcellulose, and Guargum& Xantham gum. The immediate release layer is prepared by direct compression method using superdisintegrants like Crosscamellose sodium; Crosspovidone & Sodium starch glycolate (SSG). The physicochemical evaluation results for the powdered blend of all trials pass the official limits in Bulk density, Tapped density, Compressibility index, Hausner ratio, and Angle of repose. The formulated tablets were evaluated for thickness, weight variation test, hardness test, friability test and drug content. The prepared tablets exhibited satisfactory physico-chemical characteristics. The formulation (F6) having immediate release layer of Pioglitazone showed 100.8%drug release within 60min & the formulation (F4) having sustained release layer of Glipizide showed 100.1% drug release within 12 hours. The drug release from the tablets was sufficiently sustained. The kinetic modeling of in vitro dissolution profiles revealed diffusion release mechanism. The stability studies revealed no significant changes in physical and chemical properties for the optimized formulation.

  4. Synthesis of some novel benzoxazole derivatives and their antimicrobial activityDownload Article

    Akula Ganesh, D.V.R.N. Bhikshapathi
    • Article Type: Research Article
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    • Pages (546-551)
    • No of Download = 357

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    The conventional methodology was adopted to synthesize the novel substituted pyrazole derivatives from substituted chalcone derivatives as starting material. The intermediate chalconederivatives(II) were prepared from reaction between equimolar quantities of substituted Aromatic aldehydes (0.01mol) and acetophenone(I) (0.01mol) in the presence of sodium hydroxide solution(0.02mol) using ethanol as solvent. The novel pyrazole derivatives were synthesized by means of cyclization reaction between equimolar quantities of substituted chalcone intermediates (0.02 mol) and hydrazine hydrate (0.02 mol) using sodium acetate in ethanol as solvent. All the synthesized derivatives were characterized by Infrared pectroscopy(IR), Mass spectroscopy(MS) and proton nuclear magnetic resonance(1H NMR). All the pyrazole derivatives were screened for anti bacterial activity by disc diffusion method against the organisms, S.aureus and E.coli. The derivatives are also screened for Antifungal activity using Candida albicans by double dilution method on nutrient agar media. The standard drug used was Ampicillin for anti-bacterial and Ketoconazole for anti-fungal activity.

  5. Review on: Statistical designs and response surface methodology (RSM) as a tool for the optimization of HPLC MethodsDownload Article

    Ganna Anitha, Dr. V.P. Pandey
    • Article Type: Review Article
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    • Pages (552-569)
    • No of Download = 400

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    The present paper discusses the basics and exercising response surface methodology (RSM) for the optimization of HPLC methods for separation and quantification of various pharmaceuticals. The Symmetrical experimental designs: Full factorial three level design, Central composite design, Box–Benhken design, Doehlert design and Mixture design are discussed and applications of these techniques for optimization of extraction, Derivitization, quantification and determination of experimental conditions for HPLC separations are presented with recent references. The practice of mixture design for optimization of mobile phases is also summarized.

  6. Formulation and evaluation of fast dissolving lovastatin tablets by solid dispersionDownload Article

    Huma Fatima, Dr. S. Shahid Mohammed
    • Article Type: Research Article
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    • Pages (570-578 )
    • No of Download = 612

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    The Fast Dissolving Tablets of Lovastatin by solid dispersion using Eudrgit RS100 were successfully prepared by direct compression method. The physiochemical evaluation results for the powdered blend of all trials pass the official limits in angle of repose, compressibility index. The prepared tablet for immediate release also maintained the physiochemical properties of tablets such as thickness, hardness, weight variation, friability. The optimized formulation F4 contains the average thickness of 2.75 mm average hardness of 5.6 kg/ cm2, average weight variation of ± 0.5, and friability of 0.66%. The F4 formulation of Fast Dissolving Tablets of Lovastatin showed 100% drug release within 20 mins using Eudragit RS100 as carrier whereas marketed formulation showed 100% drug release in 60 mins.

  7. RP-HPLC METHOD DEVELOPMENT AND VALIDATION FOR CILOSTAZOL IN TABLET DOSAGE FORMDownload Article

    M. Swapna, M.Vijay Prakash, M.Sunil Kumar
    • Article Type: Research Article
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    • Pages (579-584)
    • No of Download = 202

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    A simple, precise rapid and economical reverse phase high performance liquid chromatographic method has been developed for the estimation of Rasagiline in tablet dosage from, using mobile phase containing Acetonitrile and Water in volume ratio (60 : 40 v/v) at a flow rate of 1.0 ml/min. An ODS C18 RP column (150 x 4.5 mm, 5 µ) was used as stationary phase. The linearity of Rasagiline was in the range of 5 – 25 µg/ml, shows a regression coefficient of 0.9997, quantification was done using UV detector at 265 nm. The retention time of the drug was found to be 4.61 min. The limit of detection and limit of quantification was 10.72 µg/ml and 32.49 µg/ml respectively. The percentage assay of Cilostazol in PLETOZ and ST1LOZ were 106.54 ± 0.663 % and 103.27 ± 0.5965 %. This proposed method is precise, accurate and rapid for determination of Cilostazol.

  8. Development and validation of septrophotometricmethods for the estimation of rasagiline in tablet doage formDownload Article

    M. Swapna, R. Pavani, M.Sunil Kumar
    • Article Type: Research Article
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    • Pages (585-589)
    • No of Download = 388

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    Two simple and sensitive spectrophotometric methods (A and B) for the determination of Rasagiline mesylate in tablet dosage form are described. In method A – UV Spectroscopic method, Distilled Water was used as solvent and shows absorption maximum at 265 nm. In the method B – UV Spectroscopic method, 0.2 N Methanolic Hydrochloric acids was used as solvent and shows absorption maximum at 211 nm. The Beer’s Law range for method A is 20 – 160 µg/ml and 4 – 20 µg/ml for method B. The linear regression for method A and B are found to be 0.9999 and 0.9998 respectively. When tablet dosage forms where analysed, the results obtained by the proposed methods are in good agreement with the labelled amount and the results were validated statistically.

  9. Formulation and evaluation of chronomodulated drug delivery system by using metaprolol succinateDownload Article

    K.Narendra Naidu, Dr.V.Kiran Kumar, S.Revathi, A.Gopi Reddy
    • Article Type: Research Article
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    • Pages (590-601)
    • No of Download = 268

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    There is an impact of circadian rhythms in the symptoms of certain diseases like cardiac diseases, arthritis, depression, ulcer, allergic rhinitis, sleep disorders etc. The human body follows the solar/ lunar adaptations known as biological clock. The biological clock follows the main rhythm known as circadian rhythm. If the circadian rhythms dysfunctions it can greatly affect the function of the brain and behavior cognition. This can be improved by the chronotherapeutics approach. The objective of the present study was to develop chronomodulated tablets of metoprolol succinate, β1- selective adrenergic receptor blocking agent. The recent interest is occur in the field of chronotherapeutics is to match the circadian rhythms of the disease for the successful treatment of disease.The impact of chronotherapeutics in the optimal treatment of diseased patients is evaluated because in this method the treatment is done at right time with right medication at right targeted site and in the right concentration. The optimized formulation is F9 and the percentage drug release of the optimized formulation is 98.77%.The tablets were prepared by the wet granulation method.

  10. Development and validation of RP-HPLC method for simultaneous estimation of allopurinol and alphalipoicacid in bulk and tablet dosage formDownload Article

    S.Revathi, A.Gopi Reddy, K.Narendra Naidu, Dr.V.Kiran kumar
    • Article Type: Research Article
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    • Pages (602-612)
    • No of Download = 900

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    A new simple ,Rapid selective , precise and accurate gradient reversed phase high performance liquid chromatographic method (RP-HPLC )method has been developed And validated for simultaneous estimation of allopurinol and alphalipoic acid in bulk and tablet dosage form. Chromatographic analysis was performed on a c-18 column (250×4.6×5 µ)at ambient temperature .the column used was as BDS in Isocratic mode, with mobile phase containing tetrabutylammoniumhydroxide buffer and acetonitrile(70:30v/v) Adjusted to Ph 6.6 with dilute orthophosphoric acid solution . The flow rate was 0.8 Ml/min and effluents were monitored at 230nm. The retention times of allopurionol and alpha lipoicacid were found to be 2.33 min and 6.32 min, respectively. The method was validated as per ICH guidelines. The recoveries of allopurinol and alpha lipoic acid were found to be 98.53 to 100.03 and 98.5 to 99.9% respectively. The proposed method was found to be accurate reproducible and consistent. It was successfully applied for the analysis of these drugs in marketed formulations and could be effectively used for the routine analysis of formulations containing any one of the above drugs or a combination, without any alteration in the chromatographic conditions.

  11. Effect of modern lifestyle on reproductive healthDownload Article

    Dr. Bhanu Pratap Singh, Dr. Om Prakash Dadhich, Dr. Deepa
    • Article Type: Research Article
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    • Pages (613-618)
    • No of Download = 282

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    Infertility defined as the inability of a couple to achieve conception after one year of regular undefended coitus. Sterility is an absolute state of failure to conceive. Conception depends on fertility potential of both male and female partner. The male is directly responsible in about 30-40%, the female in 40-50% and both are responsible in 10% cases. The remaining 10% is unexplained in spite of thorough investigations with modern techniques. The causes of infertility are wide ranging which are such as, ovulatory disorders, tubal disease, endometriosis, chromosomal abnormalities, sperm factors and unexplained infertility. Lifestyle factors have had a spectacular impact on general health and the capacity to reproduce. Some common cause of infertility related to lifestyle such as excessive smoking, alcohol intake, degrading environment, high pollution levels, changes in diet and stress etc. that affect fertility negatively both in male and female. The present topic is taken to find out the role of lifestyle factors play in the development of infertility.

  12. Formulation and evaluation of acyclovir loaded chitosan nanoparticlesDownload Article

    S.Selvaraj, V. Niraimathi and M.Nappinnai
    • Article Type: Research Article
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    • Pages (619-629)
    • No of Download = 732

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    The present study was aimed to formulate and evaluate chitosan nanoparticles containing acyclovir as potential ophthalmic drug delivery system. The topical application of acyclovir as eye ointment remains a concern for effective management of various ocular viral diseases owing to poor ocular drug bioavailability. The acyclovir loaded chitosan nanoparticles were prepared by ionic gelation of chitosan with sodium tripolyphosphate anions. Differential Scanning Calorimetry (DSC) and Fourier Transform Infra-Red (FTIR) spectroscopy measurements were carried out on the nanoparticles and on the pure acyclovir and chitosan polymer. Five different formulations were prepared and evaluated for particle size, Zeta potential, scanning electron microscopy, entrapment and loading capacity, in vitro drug release profile. All the prepared formulations resulted in nano size in 150 - 250 nm and displayed spherical shape with Zeta potential of +33.2 to +42.8 mV. The encapsulation efficiency and loading capacity were 70% - 90% and 25% - 50% respectively. The acyclovir loaded chitosan nanoparticles displayed crystallinity than acyclovir. The in-vitro release profile of acyclovir from the nanoparticles showed a sustained release of the drug over a prolonged period of 24 hrs. Kinetic release profiles of acyclovir from nanoparticles appeared to fit best with Higuchi model with zero order and the non- Fickian diffusion mechanism. The in- vitro results reveal that ocular viral infections can be inhibited by the nanoparticles more significantly than the drug in conventional dosage forms. Thus it can be conclusively stated that the acyclovir loaded chitosan nanoparticles suspension may be considered as an improved ophthalmic drug delivery system for the treatment of ocular viral infections.

  13. Determination of Terazosin by MBTH and BPB reagents using Spectrophotometric TechniqueDownload Article

    B. Ramachandra & N.Venkatasubba Naidu
    • Article Type: Research Article
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    • Pages (630-643)
    • No of Download = 368

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    A simple, sensitive, selective rapid spectrophotometric method has been developed for the determination of terazosin in pure form, pharmaceutical formulations and blood sample based on the oxidative coupling reaction with MBTH (3-methyl-2-benzothiazolone hydrazone hydrochloride- Method-A), and Ion association reaction with BPB(Bromophenol Blue-Method-B) reagents at PH_4.0 which is extractable at 620 nm (Method-A) and 410nm (Method-B) respectively. Beer’s law is obeyed in the concentration ranges 10-60 µg ml-1and 5-30 µg ml-1 for formulations, 4-24 µg ml-1 and 3-18 µg ml-1 for blood sample respectively. The developed method was applied directly and easily for the analysis of the pharmaceutical formulations and blood samples. % R.S.D was found between 0.09699%-0.38910% (Method-A), and 0.45101%-0.75718% (Method-B), respectively and recovery was found between 99.85%-99.98% (Method-A), and 98.62%-99.86% (Method-B), respectively. The proposed methods were applied successfully for the analysis of terazosin. No interference was observed from common pharmaceutical excipients.

  14. Determination of Some Minerals in Salvadora Persica StemsDownload Article

    Hanaa. S. Boshra, Yosra Tilal Osman AlRasheed El Mohammed
    • Article Type: Research Article
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    • Pages (644-649)
    • No of Download = 188

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    Salvadora persica is a well known small tree in the Middle East, Africa and India subcontinent, it one of most important chewing stick use for oral hygiene by people live in this regions. In this study chemicals analysis for some minerals showed Salvadora Persica collected from three different regions in Sudan (in center, north and west) named as sample No 1,2,3 respectively. The concentrations of four elements Sodium Na+, Potassium K+, Calcium Ca+2, and Magnesium Mg+2 were determined by atomic absorption spectrophotometer using wet digestion method, the results obtained represented presence of four elements with different values. But Sample No 1 showed highest value for Potassium 61.64± 0.025K /ppm, 144.375±0.004 for k/ppm for Sodium and 170.24±0.016 for Calcium, while highest value recorded for Sample No 3 for Magnesium 10.45 K /ppm. The concentrations of fluoride and phosphorus also were determined in the three samples by fluoride selective electrode and UV-visible spectrophotometer. The content of fluoride in samples No 2 and 3 were 3556.56 for both which is higher than sample NO 1, the phosphorus content was found 95 ppm in samples No 1 and 2 higher than sample No 3.

  15. Stability Indicating Analytical method development & Validation of 2, 4-dihydroxy-5- Fluoro Pyrimidine in bulk drugs & its Injection formulationDownload Article

    S.Imampasha, Dr. Mohd. Ibrahim, Dr. V.Murali Balaram
    • Article Type: Research Article
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    • Pages (650-657)
    • No of Download = 192

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    Stability indicating HPLC method is developed for 2,4-dihydroxy-5-fluoropyrimidine bulk drug and its formulation, all validation parameters including specificity (interference, forced degradation), Precision (system, method, intermediate), Linearity, accuracy, range ,robustness studied, forced degradation (acid, base, peroxide, water, thermal ,humidity, photo stability effect studied for 2,4-dihydroxy-5-fluoropyrimidine,Retention time was found to be 3.4minutes at the wave length of 254nm

  16. Formulation and Evaluation of Gastro retentive Bilayer Tablets-Glimepiride as Sustained Release and Lisinopril as Immediate ReleaseDownload Article

    Farhat Ansari, Dr. S. Shahid Mohammed
    • Article Type: Research Article
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    • Pages (658-669)
    • No of Download = 551

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    The Bilayer tablets containing Glimepiride SR and Lisinopril IR were successfully prepared by Wet granulation and direct compression method respectively. Various formulations were prepared and evaluated with an aim of presenting Glimepiride as sustained release and Lisinopril as immediate release for improving the patient’s compliance. The physiochemical evaluation results for the blends of all trials pass the official limits in all tests including Angle of repose, Bulk density, Tapped density, Compressibility index, and Hausner’s ratio. The prepared blend for SR layer tablets and IR layer tablets were also maintained the physiochemical properties of tablets such as weight variation, hardness, thickness, friability. The optimized formulation F9 in IR formulations contains the average thickness of 2.4 mm, average hardness of 4.9 kg/cm2, average weight of 150 mg, friability of 0.46% and disintegration time of 2 minutes. The optimized formulation F7 in SR formulations contains the average thickness of 2.64mm, average hardness of 5.9kg/cm2, average weight of 250 mg, friability of 0.52%, and optimum mucoadhesive strength. The F7 formulation of Glimepiride Sustained Release Layer releases 10.5% in 1st hour but the remaining drug release was sustained up to 24 hours and F9 formulation of Lisinopril Immediate Release showed 99.92% drug release with in 30min. With the data of kinetic analysis, F7 formulation showed best linearity in zero order plot indicating that the release of drug is independent upon concentration and the mechanism from mucoadhesive layer follows Higuchi diffusion mechanism. The dissolution study was carried out for optimized bilayer tablet and it correlates with the drug release of individual release layer formulations. Stability studies were carried out for 6 months. All physical and chemical parameters were found to be satisfactory based on the stability data.

  17. Pharmacological activity of Curcumin-Bio-Enhancer loaded polymeric loaded nanoparticles: An invitro cell line studyDownload Article

    Kathiresan Krishnasamy, Anandh Ramasamy, Ruby Philip
    • Article Type: Research Article
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    • Pages (670-673)
    • No of Download = 15

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    Clinical utility of curcumin in the treatment of cancer is restricted due to multi-drug resistance and metabolism via glucuronidation and sulfation in the liver and intestine. To overcome these limitations, we have used Curcumin and Bio-Enhancer (piperine, quercetin and silibinin) loaded polymeric loaded nanoparticles. Sulforhodamine B assay was used to evaluate the anti-cancer activity of Curcumin and Bio-Enhancer (piperine, quercetin and silibinin) loaded polymeric loaded nanoparticles in comparison with pure curcumin and positive control doxorubicin on Ovkar-3, HL60 and HEPG2 cancer cell line. Curcumin and Bio-Enhancer (piperine, quercetin and silibinin) loaded polymeric loaded nanoparticles displayed enhanced anti-cancer activity on Ovkar-3, HL60 and HEPG2 cancer cell lines than the pure curcumin. Enhanced anti-cancer activity of Curcumin and Bio-Enhancer (piperine, quercetin and silibinin) loaded polymeric loaded nanoparticles might be due to reversal of multi-drug resistance and synergistic enhancement of anti-cancer activity of curcumin by the bio-enhancers. The study concludes that the Curcumin and Bio-Enhancer (piperine, quercetin and silibinin) loaded polymeric loaded nanoparticles would significantly enhance the anti-cancer activity of curcumin in the treatment of various cancers. However, this pilot study data requires further validation using molecular level studies and clinical trials.

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