Papers by Sachin Pishawikar
Zenodo (CERN European Organization for Nuclear Research), Jul 11, 2023
Sibutramine, {1-[1-(4-chlorophenyl) cyclobutyl]-3-methylbutyl} dethylamine is potent serotonin an... more Sibutramine, {1-[1-(4-chlorophenyl) cyclobutyl]-3-methylbutyl} dethylamine is potent serotonin and norepinephrine inhibitor. Pharmacologically it acts as antihypertensive and antiobesity agent via its secondary (M1) and primary (M2) amine metabolites. In present work an attempt has been done to develop a simple, rapid, precise and accurate isocratic reversed-phase HPLC method for the determination of sibutramine. As a novelty along with validation of developed method as per ICH guidelines, a QbD approach has been applied. As critical quality attributes related to analytical method have been identified and optimized more robustness and accurate method HPLC method has been developed. Slection of column, composition of mobile phase and flow rate were identified as critical quality attributes where by selection of KYA TECH HIQ Sil C18 (4.6 mm × 250 mm) 5µm column, Acetonitrile: water in composition 80:20 v/v as mobile phase with flow rate 1mL/min was done. The λmax was detected as 239 nm. The linearity range of the proposed method was found to be in the range of 10-50 µg/ml (r = 0.999). The limits of detection was 0.081 µg/ml and the limits of quantitation were 0.172 µg/ml respectively.
Journal of current pharma research, Nov 15, 2010
An attempt has been made to develop an economic, sensitive and reproducible colorimetric method f... more An attempt has been made to develop an economic, sensitive and reproducible colorimetric method for quantitative estimation of Aceclofenac from bulk drug and in pharmaceutical formulations. The first method employs Ferric chloride reagent in presence of hydrochloric acid and Potassium ferricyanide to form greenish complex with Aceclofenac. The concentration of Aceclofenac over a range of 10-60 µg/ml was found sufficient for obeying Beer's law in the stated range. The second method employs Ferric ammonium sulphate reagent in presence of hydrochloric acid and Potassium ferricyanide to form greenish complex with Aceclofenac. The concentration of Aceclofenac over a range of 10-50 µg/ml was found sufficient for obeying Beer's law in the stated range. The drug was determined in the presence of tablet excipients, concentration range in first method of 10-60 ug ml-1 and mean recoveries are 99.92 ± 0.16 and 100.88 ± 0.55 and concentration range in second method of 10-50 ug ml-1 and mean recoveries are 100.79 ± 0.087 and 99.36 ± 0.23 respectively for two formulations. Simplicity, ease of operation and short time required for analysis makes the method useful for routine analysis of Aceclofenac in bulk as well as in tablet formulation.
International research journal of pharmacy, Dec 28, 2010
Lamivudine (LMV), Zidovudine (ZDV) and Nevirapine (NVR) are used in combination for treatment of ... more Lamivudine (LMV), Zidovudine (ZDV) and Nevirapine (NVR) are used in combination for treatment of HIV I. The present work deals with method development for simultaneous estimation of these drugs in tablet dosage form by UV spectrophotometry. A new simple, accurate and sensitive method for simultaneous estimation of lamivudine, zidovudine and nevirapine from tablet formulation has been developed. The method employs combination of zero order and first order derivative spectroscopy. Estimation of nevirapine was done in zero order derivative mode at 310 nm where zidovudine and lamivudine do not show any interference. Estimation of zidovudine was done in first order derivative mode at 270 nm where lamivudine and nevirapine shows zero crossing points. Estimation of lamivudine is done in zero order derivative mode at 271 nm by correcting the absorbance interferences due to zidovudine and nevirapine. Absorbance interferences of zidovudine and nevirapine calculated from their absorptivities. The results of analysis validated statistically and recovery studies showed satisfactory results. Thus the method is accurate and reproducible and can be employed for routine analysis of these drugs from tablet dosage forms.
International journal of pharma and bio sciences, 2012
Strontium ranelate is used for treatment of osteoporosis. The present work deals with method deve... more Strontium ranelate is used for treatment of osteoporosis. The present work deals with method development for estimation of Strontium ranelate in bulk dosage form by UV spectrophotometry. A new simple, accurate and sensitive method for estimation of Strontium ranelate from bulk dosage form has been developed. The method employs zero order derivative spectroscopy. Estimation of Strontium ranelate was done in zero order derivative mode at 323 nm and obeyed Beer’s law in the range of 4&28 (g/ml . The results of analysis were validated statistically as per ICH guidelines and recovery studies showed satisfactory results. Thus the method is accurate and reproducible and can be employed for routine analysis of the drug from bulk dosage forms.
Asian Journal of Research in Chemistry, 2010
Lamivudine (LMV), Zidovudine (ZDV) and Nevirapine (NVR) are used in combination for treatment of ... more Lamivudine (LMV), Zidovudine (ZDV) and Nevirapine (NVR) are used in combination for treatment of HIV I. The present work deals with method development for simultaneous estimation of these drugs in tablet dosage form by UV spectrophotometry. A new simple, accurate and sensitive method for simultaneous estimation of lamivudine, zidovudine and nevirapine from tablet formulation has been developed. The method employs combination of zero order and first order derivative spectroscopy. Estimation of nevirapine was done in zero order derivative mode at 310 nm where zidovudine and lamivudine do not show any interference. Estimation of zidovudine was done in first order derivative mode at 270 nm where lamivudine and nevirapine shows zero crossing points. Estimation of lamivudine is done in zero order derivative mode at 271 nm by correcting the absorbance interferences due to zidovudine and nevirapine. Absorbance interferences of zidovudine and nevirapine calculated from their absorptivities. ...
Indian Journal of Pharmaceutical Sciences, 2008
Shinde, et al.: Spectrophotometric analysis of cefuroxime Axetil A simple rapid spectrophotometri... more Shinde, et al.: Spectrophotometric analysis of cefuroxime Axetil A simple rapid spectrophotometric method has been developed for estimation of cefuroxime axetil from bulk drug and tablet dosage form by using 1-nitroso-2-napthol and sodium hydroxide. The method is based on the formation of yellow-orange coloured complex of drug with 1-nitroso-2-napthol having absorbance maxima at 424 nm. The Beer's law is obeyed in the concentration range of 10-50 µg/ml of the drug but more precisely it obeys in the range of 10-30 µg/ml. The slope and intercept values are 0.0101 and 0.0838, respectively. Results of analysis of this method were validated statistically and by recovery studies. The method is applied to the marketed tablet formulation. Result of analysis of tablet formulation given as percentage of label claim ±standard deviation is 99.17±1.57. The precision and accuracy was examined by performing recovery studies and was found to be 99.50±1.82. Sandell's correlation coeffi cient is calculated as 0.4434. The developed method is simple, sensitive and reproducible and can be used for routine analysis of cefuroxime axetil from bulk and tablet dosage form..
Solid lipid microparticles (SLMs) loaded with ketoprofen were prepared by single emulsion-solvent... more Solid lipid microparticles (SLMs) loaded with ketoprofen were prepared by single emulsion-solvent evaporation method, in which glyceryl monostearate and Tween 80 were employed. The particle size was found to be 99.80±2.1μm. Microparticles observed by scanning electron microscope (SEM) showed spherical shape. The entrapment efficiency (EE %) and drug loading capacity (DL %) were found to be 72.60±1.6 % and 17.98±0.7% respectively. Results of stability evaluation showed relatively long term stability after storage at 4˚C for 3 months. The in-vivo study revealed slightly better per cent inhibition of pain i.e. 74% in comparison with 68% produced by plain drug.
Asian Journal of Pharmaceutics, 2008
Areverse phase high performance liquid chromatography (RP-HPLC) method for the simultaneous estim... more Areverse phase high performance liquid chromatography (RP-HPLC) method for the simultaneous estimation of amlodipine and metoprolol in marketed formulation is developed. The determination was carried out on a Kromasil C18 (250 x 4.6 mm, 5 μm) column using a mobile phase of 0.02 M phosphate buffer solution: acetonitrile (70:30v/v, pH 3.0). The flow rate was 1.0ml/min with detection at 221 nm. The retention time for amlodipine was 2.57 min and for metoprolol 4.49 min. Amlodipine and metoprolol showed a linear response in the concentration range of 10-110 μg/ml. The correlation co-efficient (‘r’ value) for amlodipine and metoprolol was 0.9991 and 0.9992, respectively. The results of analysis have been validated statistically and by recovery studies. The percentage recoveries obtained for amlodipine and metoprolol ranges from 100.04 to 100.57%.
Journal of pharmaceutical research international, Mar 26, 2022
Strontium ranelate is used for treatment of osteoporosis. The present work deals with method deve... more Strontium ranelate is used for treatment of osteoporosis. The present work deals with method development for estimation of Strontium ranelate in bulk dosage form by UV spectrophotometry. A new simple, accurate and sensitive method for estimation of Strontium ranelate from bulk dosage form has been developed. The method employs zero order derivative spectroscopy. Estimation of Strontium ranelate was done in zero order derivative mode at 323 nm and obeyed Beer’s law in the range of 4-28 µg/ml. The results of analysis were validated statistically as per ICH guidelines and recovery studies showed satisfactory results. Thus the method is accurate and reproducible and can be employed for routine analysis of the drug from bulk dosage forms.
Synthesis of new antimicrobial compounds is need of the hour due to prevalence of resistance to a... more Synthesis of new antimicrobial compounds is need of the hour due to prevalence of resistance to antibacterial agents. Different pharmacological activities like, anticancer, antimicrobial, antifungal, anticonvulsant, antimalarial, analgesic and anti-inflammatory are shown by mannich bases and thiosemicarbazide individually. Synthesis of mannich bases was done using aldehyde, ketones and amines having aliphatic, aromatic, cyclic and heterocyclic nature. Synthesized mannich bases were condensed with thiosemicarbazide to form noval mannich bases of thiosemicarbazide as mutual pro-drugs. Spectral analysis was done using IR and H-NMR. Docking analysis performed on the DNA polymerase enzyme (PDB ID 2v4q) showed strong hydrophobic interaction between carbon atom of ketone and amino acids phenylalanine, tyrosine and threonine, charged interactions with aspartine and Vanderwall’s interactions with phenylalanine, aspartine, lysine alanine and threonine, In vitro testing was done using BHI( bra...
The Indian Pharmacist, 2006
Talc is a known adsorbent, has lubricant and antisticking properties in powder form and therefore... more Talc is a known adsorbent, has lubricant and antisticking properties in powder form and therefore can be proposed as a flow promoter and lubricant in tablet formulations. The objective of this study was to elucidate the comparative adsorption of diclofenac sodium and diltiazem hydrochloride onto talc. Freundlich and Langmuir adsorption isotherms, two commonly used models for adsorption, showed that diclofenac sodium was adsorbed weakly while diltiazem hydrochloride was significantly adsorbed onto the surface of talc. This variation in adsorption may be due to weak or no interaction of diclofenac sodium while significant interaction of diltiazem hydrochloride with negatively charged silicate anions of talc. Therefore, the combination of talc with diclofenac sodium could reduce its bioavailability to a lesser amount than that of diltiazem hydrochloride.
High-Throughput Screening (HTS) is an approach to drug discovery that has gained widespread popul... more High-Throughput Screening (HTS) is an approach to drug discovery that has gained widespread popularity over the last two decades and has become a standard method for drug discovery in the pharmaceutical industry. Progress from traditional one-compound-at-a time approach, low throughput screening to high throughput screening involving fully automated robotic systems, enables testing of large numbers of compounds daily for different activities in miscellaneous areas of biology. HTS reveals screening of more than 100,000 samples per day. Compared to traditional drug screening methods, HTS is characterized by its simplicity, rapidness, low cost, and high efficiency. Identification of good hits using HTS can minimize the time span of drug discovery noticeably. However, synthetic chemistry for lead optimization and the low throughput of secondary assays for defining the crucial pharmacological properties of active compounds, limits the overall rate of identification of candidate molecules...
Asian Pacific Journal of Tropical Medicine, 2014
To develop and validate a simple, accurate and precise colorimetric method using Bougainvillea sp... more To develop and validate a simple, accurate and precise colorimetric method using Bougainvillea spectabilis (B. spectabilis) bract color previously not exploited for estimation of amide group containing drugs i.e. lidocaine and ranolazine in pharmaceutical formulations. Methods: Methanolic extract of B. spectabilis was prepared and evaluated for stability of its color at different pH and temperature for a period of 3 weeks. The accuracy and reliability of the proposed method was ascertained by evaluating various validation parameters like linearity, precision, limit of detection, limit of quantitation and specificity according to International Conference on Harmonization guidelines. About 0.5% of B. spectabilis bract color was added to the working standard solutions of the drugs separately and after formation of color complex, and absorbances were noted at 418 nm. Results: For color complexes of lidocaine and ranolazine, linearity was found to be in the range of 4 to 24 and 5 to 25 µg/mL respectively. The % relative standard deviation was found to be within specification limits. Presence of lone pair of electron on nitrogen of amide group of both drugs shows basic nature, contributed in formation of color complex between amide and the color pigment obtained from B. spectabilis bracts. Conclusions: It can be concluded that the method is simple, accurate, economic, and rapid hence can be employed for routine analysis.
Pharmaceutical Methods, 2011
A Simultaneous determination of Olmesartan Medoxomil (OLM) and Amlodipine Besylate(AML) by first ... more A Simultaneous determination of Olmesartan Medoxomil (OLM) and Amlodipine Besylate(AML) by first order derivative spectrophotometric method has been developed in combined dosage form. The method is based on measurement of absorbance at 226 nm as wavelengths for quantification of OLM where no interference due to AML was observed similarly absorbance at 241 nm is selected for quantification of AML, where OLM did not interfere with the estimation of AML. The system obeyed Beers law over the concentration of 2 to 32 µg ml-1 for OLM and 2 to 20 µg ml-1 for AML.respectively. The proposed method was validated and can be used for analysis of combined dosage tablet formulation containing Olmesartan medoxomil and amlodipine besylate. Interday and intraday studies showed repeatability of the method.
Arabian Journal of Chemistry, 2017
Mannich bases and thiosemicarbazide individually show antimicrobial, antifungal, anticonvulsant, ... more Mannich bases and thiosemicarbazide individually show antimicrobial, antifungal, anticonvulsant, antimalarial, analgesic and anti-inflammatory type of varied pharmacological activities. The novelty of the present work is the synthesis of mannich bases of thiosemicarbazide as mutual prodrugs. In step-1, mannich bases are synthesized using aldehyde, ketones and amines with aliphatic, aromatic, cyclic and heterocyclic nature. In step-2, the synthesized bases were condensed with thiosemicarbazide to form mannich bases of thiosemicarbazide. Structural characterization of synthesized compounds was done using IR, mass and H-NMR spectroscopy. The compounds were screened for anti-fungal activity using BHI (brain heart infusion) broth dilution method against Candida albicans and Apergillus niger. Docking of synthesized compounds was done on CYP51A1, P45014DM (Lanosterol 14 a-demethylase enzyme) using Vlife MDS 3.5 to conform the mechanism of antifungal activity. Docking study showed a strong hydrophobic interaction between amino acid residues Arganine (ARG141), Glutamine (GLU146), Leucine (LEU54), Lycine (LYC227), and Threonine (THR147) with the carbon of ketone, nitrogen of amine and sulfur of thiosemicarbazide. Strong Vander wall's interactions are also observed with the carbon of ketone, nitrogen of amine and sulfur of thiosemicarbazide. Analogs with aromatic and substituted aromatic aldehydes showed least activity, while analogs with aliphatic aldehyde, ketones and amines showed greater activity in C. albicans compared to A. niger. Analogs having morpholine as amine showed comparable activity in both. Compounds K 17 , K 18 , K 19 , and K 20 have shown comparable highest activities.
and review articles in less time without much delay in the developing field of Pharmaceutical and... more and review articles in less time without much delay in the developing field of Pharmaceutical and Biological sciences. One week from the date of manuscript submission author gets the decision of acceptance and if accepted the manuscript will be processed within 3 weeks (approx.) for publication.
Asian Journal of Research in Chemistry, 2012
A simple, accurate, sensitive and reliable method have been developed for the determination of Gl... more A simple, accurate, sensitive and reliable method have been developed for the determination of Glibanclamide in bulk and Pharmaceutical formulation using extract of Beta vulgaris root. Phytochemical investigation shows presence of betanin group of compounds which have polyphenolic nature similar to synthetic dyes like methyl orange, bromocresol green etc. which are commonly used as colouring agent to form a colour complex with amide group containing compounds in developing visible spectroscopic method of analysis. In present work a successful attempt has been done to develop a colorimetric method for estimation of glibanclamide by forming a stable colour complex using extract of Beta vulgaris root on the basis of amide linkage present in glibanclamide. The absorbance of the pale yellow colored complex was measured spectrophotometrically at 533 nm against reagent blank. From Calibration graphs Beer's law is followed in range of 2 to 20μg/ml with correlation coefficient 0.999587, ...
Mannich bases and thiosemicarbazide individually show varied pharmacological activities like anti... more Mannich bases and thiosemicarbazide individually show varied pharmacological activities like anticancer, antimicrobial, antifungal, anticonvulsant, antimalarial, analgesic and anti-inflammatory. By using mutual prodrug concept, first mannich bases were synthesized using aldehyde, ketones and secondary amines with aliphatic, aromatic, cyclic and heterocyclic nature using mannich reaction and then condensed with thiosemicarbazide to form mannich bases of thiosemicarbazide as mutual prodrug. Structural characterization of synthesized compounds was done using IR and H-NMR. Complexicity in the structure of reactants lead to change in reaction time, temperature and % yield of final product. The compounds were screened for anti- microbial activity using Escherichia Coli (8739) Staphylococcus aureus (25923), anti-fungal activity using Aspergillus niger (16404), Candida albicans (10231) using BHI (brain heart infusion) broth dilution method and anti tubercular activity by micro plate Alamar ...
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Papers by Sachin Pishawikar