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Volume -6 Issue -2


Articles

ROLE OF GLUCARPIDASE IN PREVENTION AND MANAGEMENT OF HIGH DOSE METHOTREXATE TOXICITY
ROLE OF GLUCARPIDASE IN PREVENTION AND MANAGEMENT OF HIGH DOSE METHOTREXATE TOXICITY Pages 1 - 10

AVINASH KHADELA

Abstract: Methotrexate is prominently used drug in many disease conditions ranging from rheumatoid arthritis in low-dose and leukemias in high-dose. This high-dose methotrexate (HDMTX) has been widely used for oncology pa-tients, with considerable precautions such as vigorous hydration, urine alkalinization, and leucovorin therapy. However, in spite of taking precautionary measures, many patients are developing HDMTX-induced renal insuf-ficiency, which ultimately ends up with delayed methotrexate (MTX) elimination and persistent elevation in se-rum methotrexate concentrations. Consequently, it leads to increase in the methotrexate toxicity and deterio-rates the patient current condition. To encounter this issue, glucarpidase (an enzyme, carboxypeptidase G2) is an enzyme which instantly inactivates MTX. It hydrolyzes methotrexate into two inactive non-toxic metabolites, and provides an alternative non-renal pathway for methotrexate clearance in patients with renal insufficiency while receiving treatment that contains HDMTX. This article illustrates the evidence from the published articles on HDMTX and glucarpidase to provide effective management strategies for the patients who are receiving chemotherapy containing HDMTX. Glucarpidase is considered to be safe for the patients having intact kidney function if given along with excessive hydration, leucovorin pharmacokinetically guided therapy, and urinary alkalizing agents. Therefore, precise diagnosis of delayed methotrexate clearance and renal insufficiency play a vital role for the management of toxicities induced by MTX. Particularly, the sudden rise in creatinine levels or exponentially decreases in urinary output after high dose MTX administration leads to an emergency like situa-tion. Carboxypeptidase G2 reduces the plasma methotrexate concentration, only if it is administered as soon as possible with concomitantly providing excessive hydration and extended use of pharmacokinetically guided leu-covorin therapy to curtail MTX toxicity.


Keywords: Glucarpidase, High-dose Methotrexate, Leucovorin, Renal dysfunction

In-vitro Antibacterial activity of Methanolic Extract of Perquatina nigrescens (Afzel.) Bullock. Leaves and Thevetia peruviana (Pers) Schums. Roots
In-vitro Antibacterial activity of Methanolic Extract of Perquatina nigrescens (Afzel.) Bullock. Leaves and Thevetia peruviana (Pers) Schums. Roots Pages 11 - 17

Adeyemi Sherif, Oladele Ogunsola, Pass Chijindu, Ibrahim Afonja, Mutiyat Odebisi-Omokanye, Kafayat Ahmed, Ramar Krishnamurthy

Abstract: Ethnobotanical Investigation has revealed that the roots of Thevetia peruviana and leaves of Parquetina nigrescens are being used to treat bacterial diseases. Phytochemical screening revealed the presence of alkaloids and terpenoids in both species. Agar well diffusion method was employed in the sensitivity test of the studied ethnobotanicals. Different concentrations (50, 100, 200 and 300mg/ml) of extracts of T. peruviana roots and P. nigrescens leaf extracts were employed against E. coli, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus and Streptococcus mutans. All the organisms showed highest and lowest levels of inhibitions at 300mg/ml and 50mg/ml respectively. Leaf extract of P. nigrescens showed relatively more activities than the root extract of T. peruviana against the tested organisms. The Minimum Inhibitory concentration of both extracts also showed considerable activity at (50,100 and 200) mg/ml while the growth of the microorganisms was unrestrained at 25mg/ml.


Keywords: Bacteriostatic, Thevetia peruviana, Parquetina nigrescens, Microorganisms, Phytochemicals

Archives


Volume -6 Issue -1
Conference Proceedings of "International Conference on Nanotechnology and its application to Ocular Drug Delivery Systems, 28 - 30th Jan 2019"
Conference Proceedings of "International Conference on Nanotechnology and its application to Ocular Drug Delivery Systems, 28 - 30th Jan 2019" Pages 1 - 62

Maliba Pharmacy College Uka Tarsadia University,

Volume -5 Issue -2
Volume -5 Issue -1
Volume -4 Issue -2
Volume -4 Issue -1
Volume -3 Issue -2
Determination of 2-amino-4-chlorophenol (related substance) in marketed formulations of Chlorzoxazone by RP-HPLC
Determination of 2-amino-4-chlorophenol (related substance) in marketed formulations of Chlorzoxazone by RP-HPLC Pages1 - 7

Praful Dedhiya, NIPUNA PATEL, RUCHI VVAS, DINESH SHAH, SHAILESH SHAH

Abstract: Chlorzoxazone is one of the most frequently prescribed drugs in the treatment of muscle spasm in combination with NSAIDs. It is reported to undergo hydrolysis in alkaline medium to form 2-amino-4-chlorophenol, which is considered a significant related substance as per USP. Various regulatory authorities like ICH, USFDA, Canadian Drug and Health Agency are emphasizing on the purity requirements and the identification of impurities in active pharmaceutical ingredient (API) as well as in pharmaceutical formulations. To this aim, various marketed formulations were assessed with special attention to identification and quantification of 2-amino-4chlorophenol by using compendial reversed phase high performance liquid chromatography method. The use of a 250 × 4.6 mm, 5 µm particle size, C18 column with 70:30:1 %, v/v/v water: acetonitrile: acetic acid as isocratic mobile phase at flow rate 1.5 ml/min enabled separation of the drug from its related substance. UV detection wasperformed at 280 nm. The method was verified for specificity, linearity, precision and accuracy. The related substance peak was well resolved from drug peak. The linearity of the method was satisfactory over the range 400-2000 ng (correlation coefficient 0.9993). The limits of detection for 2-amino-4-chlorophenol and Chlorzoxazone were 5 and 10.94 ng respectively. The limits of quantitation for 2-amino-4-chlorophenol and Chlorzoxazone were 20 and 33.14 ng respectively. Recovery of Chlorzoxazone ranged from 99.90-100.67%. The method was successfully applied to marketed formulations of Chlorzoxazone for quantitative analysis of Chlorzoxazoneand 2-amino-4-chlorophenol.


Keywords: High Performance Liquid Chromatography, Chlorzoxazone, related substance, 2-amino-4chlorophenol

Chemo-sensitivity and Determination of Optimum Exposure Time of Nitrous Acid for Growth and YieldofDigitaria exilis(Haller)
Chemo-sensitivity and Determination of Optimum Exposure Time of Nitrous Acid for Growth and YieldofDigitaria exilis(Haller) Pages8 - 13

Animasaun A, MUSTAPHA OT., OYEDEJI S., YUSUF KA.

Abstract: In this study, we assessed chemo-sensitivity of Digitaria exilis to nitrous acid in term of growth and yield to determine the mutagenic effects and optimum exposure time for desirable mutagenesis that may be utilize in the crop improvement. We exposed dried seeds of D. exilis to 0.1 M nitrous acid for varying time of 2, 4, 6, and 8 hours while 0 hrseeds were used as control.Theseeds were sown andeffectsof exposure timewere studiedon the quantitative and qualitative characters. Results showed germination and seedling survival decreased with increased in exposure time. Data analysis revealed that 6 and 8 hr of treatment negatively affect plant height, number of leaves, tiller/plant, and leaf length. Though, all exposure time induced significant early maturity, however, 6 and 8 hr exposure produced low seed set and grain yield. The performance of the chemical treated plants was optimal for4 hrexposure time which produced best agronomic traits, a degree of variability and improved yield. Also, erect plants were obtained with 2 and 4 hr treatment which is a promising trait for mechanical harvesting of the crop. This study concluded that 4 hr of exposure of D, exilis to 0.1M nitrous acid could be utilized in inducing variability and improvement of the crop in a breeding programme.


Keywords: Chemosensitivity,Digitaria exilis, Exposure time, Nitrous acid

Effects of enhancers with biofertilizer on the better Wheat (Triticum aestivum)growth
Effects of enhancers with biofertilizer on the better Wheat (Triticum aestivum)growth Pages14 - 18

Nita Naik, AVANI PANDYA, ANOOP MARKANDE

Abstract: Pot experiments were conducted with the objective to evaluate the effect of different fertilizers and fertilizer amendments on growth of wheat plant and soil properties. Seeds were treated in different combinations of biofertilizer with urea and neem-coated urea. Combined application of biofertilizer with urea gave highest results for growth properties such as shoot and root fresh weight, dry weight, yield and yield attributes. For soil phosphorus and potassium content combined application was most beneficial while for Nitrogen content application of urea and neem coated urea was most effective. Application of biofertilizer in combination with urea increased the efficiency of applied nitrogen fertilizer as it shows increase in NPK content of soil. Amendment of biofertilizer with urea could compensate for nutrient deficiency and higher rates of chemical N fertilization.


Keywords: Biofertilizer; neem; urea;wheat

Inhibition study of Caesalpinia crista on corrosion of mild steel in hydrochloric acid
Inhibition study of Caesalpinia crista on corrosion of mild steel in hydrochloric acid Pages19 - 25

G Malik, K. CONTRACTOR, V. CHAMPANERI, NIL DESAI, K. DESAI

Abstract: In this study, we report inhibition effect of Caesalpinia crista fruit on corrosion of mild steel in hydrochloric acid using weight loss measurements and electrochemical techniques. The inhibition efficiency of Caesalpinia crista was found to vary with concentration, temperature and immersion time. Good inhibition efficiency I.E.% was recorded in acid solution. The inhibition efficiency was found to be more than 90% in 1 M HCl solution of 5 mM inhibitor concentration. The adsorption study of these compounds on mild steel surface found to obey Temkin’s adsorption isotherm. The activation energy values and values of free energy of adsorption indicated physical adsorption on mild steel surface. The potentiodynamic polarization results showed that the compound studied was mixed type inhibitor.


Keywords: Mild steel, Caesalpinia crista, corrosion, inhibition effect, hydrochloric acid. adsorption

Development and validation of HPTLC method for simultaneous estimation of Lercanidipine Hydrochloride and Enalapril Maleate in their synthetic mixture
Development and validation of HPTLC method for simultaneous estimation of Lercanidipine Hydrochloride and Enalapril Maleate in their synthetic mixture Pages26 - 33

Sandesh Lodha, SHAILESH SHAH, RICHA SHAH, DINESH SHAH, GAJANAN KALYANKAR, KUNJAN BODIWALA, PINTU PRAJAPATI, KARISHMA PATEL, RUCHI VVAS

Abstract: A precise and accurate HPTLC method has been developed for simultaneous estimation of Lercanidipine Hydrochloride and Enalapril Maleate in its synthetic mixture. The chromatographic separation was performed on aluminum plates pre-coated with silica gel 60F254 using toluene:n-butanol:formic acid in proportion of 6:4:1 v/v/v as mobile phase and densitometrically scanned at 224 nm wavelength. The Rf values were found to be 0.34 ± 0.02 and 0.55 ± 0.02 for Enalapril Maleate and Lercanidipine Hydrochloride respectively. The linearity range for bothLercanidipine Hydrochloride and Enalapril Maleate were found to be 400 –800 ng/band with correlation coefficients of 0.9979 and 0.9961 respectively. The method was validated for linearity, precision, accuracy as per ICH guidelines. The method was applied for simultaneous estimation of Lercanidipine Hydrochloride and Enalapril Maleate in its synthetic mixture. The assay results were found to be 99.48 ± 0.25% and 99.34 ± 0.15% for Lercanidipine Hydrochloride and Enalapril Maleate.


Keywords: Lercanidipine, Enalapril, HPTLC, Simultaneous

Development and characterization of Methotrexate loaded PEGylated gold nanoparticles
Development and characterization of Methotrexate loaded PEGylated gold nanoparticles Pages34 - 41

Sonia Pandey, ARPAN DESAI, ARTI GUPTA, ARPAN DESAI, ARTI GUPTA

Abstract: Cancer is a disease characterized by uncontrolled multiplication and spread of abnormal forms of the body's specific cells. The aim of these studies was to synthesize, characterize and evaluate the efficacy of PEGylated gold nanoparticles. Gold nanoparticles were synthesized by chemical reduction method. The anti-cancer drug Methotrexate (MTX) was encapsulated by the AuNPs by non covalent adsorption. The particle size, PDI, zeta potential, % drug bound, % drug content of optimized PEGylated gold nanoparticles were found to be 19.79 nm, 0.703, -6.73, 78.38 % ± 0.75 and 97.03 % ± 2.904 respectively. The proficiency of MTX loaded PEGylated gold nanoparticles in inhibiting the proliferation of breast cancer cells MCF-7 as compared to the free drug and Methotrexate loaded gold nanoparticles is demonstrated based on MTT assay. Notably, MTX loaded PEGylated gold nanoparticles was found to have 30% higher cytotoxicity on MCF-7 cells compared with an equivalent dose (0.5 µg/µL) of free MTX and Methotrexate loaded gold nanoparticles. Taken together, all results unveil that MTX loaded PEGylated gold nanoparticles could be more effective than free drug and Methotrexate loaded gold nanoparticles for cancer treatment.


Keywords: Cancer, Methotrexate, gold nanoparticle, PEGylation, Cell viability

Volume -3 Issue -1
Development and validation of HPTLC method for simultaneous estimation of Fenofibrate and Rosuvastatin in tablet dosage
Development and validation of HPTLC method for simultaneous estimation of Fenofibrate and Rosuvastatin in tablet dosage Pages1 - 7

Gajanan Kalyankar, VRUNDA GHARIYA, KUNJAN BODIWALA, SANDESH LODHA, SHRIKANT JOSHI

Abstract: A sensitive, specific and precise high performance thin layer chromatographic method for simultaneous estimation of Fenofibrate (FEN) and Rosuvastatin (RSV) has been developed and validated. The method employed aluminium plates pre-coated with silica gel 60F254 as the stationary phase. The solvent system consisted ofToluene: Chloroform: n-butanol:Formic acid (6:2:1.5:0.5, v/v)which was found to give compact and dense spots for FEN and RSV (Rf value 0.73 ± 0.02 and 0.43 ± 0.02 respectively). Densitometric analysis of both drugs was carried out in the absorbance mode at 261 nm. The method was validated with respect to linearity, specificity, precision, limit of detection, limit of quantification and recovery. The linear regression analysis data for the calibration plots showed a good linear relationship with r2 , 0.9983 for FEN in the concentration range of 100-500 ng/spot and 0.9973 for RSV in the concentration range of 100-500 ng /spot. The LOD and LOQ for FEN were found to be 23.52 and 71.29 ng/spot respectively and for RSV, 15.68 and 47.05 ng/spot respectively. Assay results for tablet formulation were found to be 99.27 ± 1.52 % and 100.48 ± 0.69% of label claim for FEN and RSV respectively. The proposed method was found to be accurate, precise and specific and can be used for routine analysis of FEN and RSV in their combined dosage form.


Keywords: Fenofibrate (FEN), Rosuvastatin (RSV) andmethod validation

Formulation and Evaluation of Co-Processed MCC Core Pellets and Confirm Its Application in Layering of Drugs with Different Solubility
Formulation and Evaluation of Co-Processed MCC Core Pellets and Confirm Its Application in Layering of Drugs with Different Solubility Pages8 - 17

Hetal Patel, KAWALPREET KAUR, KETAN RANCH, SHAILESH SHAH, MUKESH GOHEL

Abstract: Context: Microcrystalline cellulose (MCC) is an excellent excipient for production of core pellets by extrusion spheronization. Drug layering onto the MCC core pellets in a fluidized bed processor is an industrial applicable and scalable approach. However, it causes slow release rate of poorly water soluble drugs from the pellets. Objective: The aim of this work is to prepare and evaluate co-processed MCC core pellets using extrusion spheronization technique and to confirm utility of this core pellets into development of various drug layered pellets with acceptable mechanical properties and drug release profile. Materials and methods: Co-processed excipient pellets composed of MCC, crosscarmellose sodium and sodium bicarbonate were prepared by extrusion spheronization technique and evaluated for morphology, yield, bulk density, tapped density, Carr’s index, Hausner’s ratio, pellet size analysis, porosity, friability, and dispersion time. Ascorbic acid, atazanavir, isoniazid, efavirenz, eprosartan mesylate and nimesulide were used as model drugs with different solubility. Drugs were layered onto the core pellets into fluidized bed processor and drug layered pellets were evaluated for bulk density, tapped density, Carr’s index, Hausner’s ratio, pellet size analysis, porosity, friability, dispersion time, drug content and in vitro drug release. Results and discussion: Core as well as drug layered pellets exhibit adequate morphological, flow and mechanical properties. All drug layered pellets consisted of co-processed excipient core pellets showed significant increment in drug release rate compare to drug layered pellets consisted of MCC core pellets. Conclusion: Co-processed MCC core pellets can be used to coat variety of drugs with greater accuracy and consistency in drug layering.


Keywords: Microcrystalline cellulose, drug layering, fluidized bed processor, porosity, dissolution

Qualitative and quantitative phytochemical analysis of Heterophragma quadriloculare (Roxb.) K. Schum. leaves
Qualitative and quantitative phytochemical analysis of Heterophragma quadriloculare (Roxb.) K. Schum. leaves Pages18 - 25

Bhavikkumar Satani, VILAS SURANA, SHAILESH SHAH, SHRI MISHRA

Abstract: Objectives: Heterophragma quadriloculare (Roxb.) K. Schum. (HQ) is belonging to Bignoneace family. This plant has been traditionally utilized as anti-diabetic, antifungal, antiseptic and in skin disease like toe sores and chilblain. Since, scientific documentation is not well available it was thought of interest to develop scientific database for HQ leaves. With this respect we have attempted qualitative and quantitative evaluation of various phytochemicals from HQ leaves.
Methods:Successiveextracts ofHQ leaves have been analyzed by qualitativechemical tests and TLC. HPTLC fingerprints have also been developed for all extracts. Lupeol and ursolic acid have been identified and simultaneously estimated in petroleum ether extract of HQ leaves. Amount of secondary metabolites i.e. alkaloids, tannins, phenolics and flavonoids, have been estimated using reported methods.
Results: Carbohydrates, proteins, aminoacids, fats, alkaloids, steroidal compounds, flavonoids, terpenoids, tannins and phenolics were found in HQ leaves. By HPTLC method, 0.50 % and 0.93 %w/w of lupeol and ursolic acid have been observed in HQ leaves respectively. Percentage yield of alkaloid rich fraction was found to be in the range of 0.03-0.78 % w/w at different pH.Alkaloid rich fraction prepared at pH 10 was found to be best asper % yield and TLC profile. HQ leaves have been found to contain3.14 %,4.03%and 4.09 % w/w oftannins, phenolics and flavonoids respectively.
Conclusions: This report can create the way for further identification and isolation of phytoconstituents especially alkaloids and terpenoids. Chromatographic fingerprint can also serve the purpose of drug standardization. The work can be further extended for drug discovery and drug development by isolation and characterization of phytoconstituents.


Keywords: Heterophragma quadriloculare (Roxb.) K. Schum, Phytochemical profile, Quantitative phytochemical analysis, HPTLC fingerprinting, Alkaloid, Secondary metabolite

Development and validation of HPTLC method for estimation of Teneligliptin Hydrobromide Hydrate in tablet dosage form
Development and validation of HPTLC method for estimation of Teneligliptin Hydrobromide Hydrate in tablet dosage form Pages26 - 33

Sandesh Lodha, KARISHMA PATEL, SUNNY PATEL, SHREYA PATEL, KUNJAN BODIWALA, SHAILESH SHAH, GAJANAN KALYANKAR

Abstract: A stability indicating HPTLC method was developed and validated for estimation of Teneligliptin hydrobromide hydrate in tablet dosage form. Chromatographic separation was performed on aluminium plates pre-coated with silica gel 60 F254aluminium plate using the mobile phase butanol : water : glacial acetic acid (6:2:2 v/v/v) and densitometrically scanned at 245 nm. The Rf value for Teneligliptinhydrobromidehydratewas found to be 0.65. The solvent system was able to separate Teneligliptin hydrobromide hydrate and its degradation products formed under acidic condition. Developed HPTLC method was validated as per ICH guideline Q2(R1). The linear regression analysis data for the calibration plots showed a good linear relationship with r2 =0.998in the concentration range of 250-1250ng/band forTeneligliptinhydrobromide hydrate. Percent recovery of drug was found in the range of98.58–99.24%by developed method. Limit of detection and limit of quantitation werefound to be 60.50 ng/band and 183.36 ng/band for Teneligliptin hydrobromide hydrate, respectively. Developed method was applied for estimation of Teneligliptin hydrobromide hydrate in tablet dosage form and assay result was found to be 98.34±0.31%.


Keywords: High Performance Thin Layer Chromatography, Teneligliptin hydrobromide hydrate, Stability indicating method

Volume -2 Issue -2
Comparative study of Phototherapy only and Phototherapy plus Phenobarbitone in treatment of Neonatal Jaundice - An Observational Study
Comparative study of Phototherapy only and Phototherapy plus Phenobarbitone in treatment of Neonatal Jaundice - An Observational Study Pages1 - 10

Tamanpreet Mayall, KIMSHUK MODI, BHAVIN VVAS

Abstract: Objectives: The study was intended to compare the effectiveness of phenobarbitone and phototherapy combination over phototherapy alone in treatment of neonatal jaundice.
Materials and methods: A total of 47 neonates were enrolled in this observational study,of which 17 were ra ndomised to Group 1 and were given only phototherapy. Sixteen neonates were placed in Group 2 and were given phototherapy plus phenobarbitone. Fourteen neonates were excluded from the study. Phototherapy was started in neonates with total serum bilirubin =13 mg/dl. Phenobarbitone was given in a dose of 5 mg/dl/day in two divided doses. Various parameters were evaluated regarding demographics, maternal data, physical examination, laboratory data and treatment. Statistical Package for Social Sciences (SPSS; Chicago, IL, USA) program was used for statistical analysis.
Results: The demographics, maternal data and hematologic data were not statistically different (p>0.05) between both the groups. The percentage decrease in total serum bilirubin was 26.06% and 31.06% for Group 1 and Group 2, respectively (p=0.105). However, the rate of decrease of bilirubin was 0.09 mg/dl/hr and 0.16 mg/dl/hr in Group 1 and Group 2, respectively (p=0.004). The mean total duration of phototherapy was 103.57 hr and 76.41 hr in Group 1 and Group 2, respectively (p=0.019). The most prevalent risk factor was low birth weight, followed by ABO incompatibility and infection.
Conclusion: combination of phototherapy plus phenobarbitone is effective in decreasing the duration of phototherapy, thereby decreasing the adverse effects that may occur due to longer duration of phototherapy. The combination also reduces the hospitalization stay thus decreasing the overall cost.


Keywords: Neonatal Jaundice; Phenobarbitone; Phototherapy

Application of Box-Behnken Design in Optimization of Ibuprofen Ternary Solid Dispersion
Application of Box-Behnken Design in Optimization of Ibuprofen Ternary Solid Dispersion Pages11 - 19

Furqan Maulvi, ASZAD BODA, ANKITA DESAI, HARSH CHOKSI, KETAN RANCH, DINESH SHAH

Abstract: The objective of present investigation was to enhance the dissolution rate of ibuprofen by preparing its ternary solid dispersion (SD) using solvent evaporation method. Box-Behnken design was used to scrutinize the combined effect of three independent variables on percentage drug release and flow property of ternary solid dispersion. The independent variables selected were Starcap 1500 (X1), Polyethyleneglycol4000 (X2) and drug: polymer ratio (X3), whereas percentage drug release after 10 minutes (Q10) and angle of repose (AR) were selected as dependent variables. The transformed values of the independent and dependent variables were subjected to multiple regressions analysis to establish full and reduced second order polynomial equations. Using Design of Expert Software the levels of independent variables was predicted [64.65 % Starcap 1500 (X1 = 1), 10.35 % Polyethylene glycol 4000 (X2 = 0.4) and 25.00 % drug, i.e. 1:3 ratio of ibuprofen: polymer mixture (X3 = 0.50)] for maximized response of Q10 (81.68 ± 4.22 %) with good flow property (angle of repose = 31o63” ± 1o06”). Dissolution profile of optimized ternary solid dispersion was significantly improved in comparison to pure drug. In conclusion, Box-Behnken design demonstrated the application in predicting the values of independent variables for optimization of ibuprofen ternary solid dispersion.


Keywords: Box-Behnken Design, Solid dispersion, Ibuprofen, Starcap 1500, Polyethylene glycol4000.

Development and validation of HPTLC method for simultaneous estimation of Olmesartan medoxomil and Cilnidipine in their combined pharmaceutical dosage forms
Development and validation of HPTLC method for simultaneous estimation of Olmesartan medoxomil and Cilnidipine in their combined pharmaceutical dosage forms Pages20 - 27

Praful Dedhiya, CHAITALI PATEL, RENU CHAUHAN, GAJANAN KALYANKAR, RUCHI VVAS, SHAILESH SHAH

Abstract: An accurate, specific and precise HPTLC method has been developed for the simultaneous estimation of olmesartan medoxomil and cilnidipine in their combined pharmaceutical dosage form. The chromatographic separation was performed using aluminium plate precoated with silica gel 60 F254 as stationary phase and toluene: methanol: chloroform (6: 3: 2, v/v/v) as mobile phase. The quantification was carried out at 257 nm. The Rf values were found to be 0.26 ± 0.02 and 0.67 ± 0.02 for olmesartan medoxomil and cilnidipine respectively. The linearity was observed in range of 400-1200 ng/spot for olmesartan medoxomil and 200-600 ng/spot for cilnidipine. The correlation coefficient (R2) was found to be 0.9928 and 0.9987 for olmesartan medoxomil and cilnidipine respectively. The method was validated for precision, accuracy, LOD and LOQ as per ICH guidelines. The method was applied for simultaneous estimation of olmesartan medoxomil and cilnidipine in their combined pharmaceutical dosage form. The assay results were found to be 99.60% ± 0.15 for olmesartan medoxomil and 98.30% ± 0.16 for cilnidipine of percentage label claim of their combined pharmaceutical dosage form.


Keywords: High Performance Thin Layer Chromatography, olmesartan medoxomil, cilnidipine

Volume -2 Issue -1
Development of HPTLC Method for Simultaneous Estimation of Paracetamol and Flupirtine Maleate in their Combined Tablet Dosage Form
Development of HPTLC Method for Simultaneous Estimation of Paracetamol and Flupirtine Maleate in their Combined Tablet Dosage Form Pages1 - 7

Kajal Mahajan, Renu Chauhan, Shailesh Shah, Dinesh Shah

Abstract: A simple, accurate and precise high-performance thin layer chromatographic method for simultaneous estimation of paracetamol and flupirtine maleate in their combined tablet dosage form has been developed. A simple, accurate and precise high-performance thin layer chromatographic method for simultaneous estimation of paracetamol and flupirtine maleate in their combined tablet dosage form has been developed. The method employed thin layer chromatographic aluminium plates pre-coated with silica gel 60F254 as the stationary phase and toluene: acetone: triethylamine (6:4:0.5 v/v/v) as mobile phase. Chromatographic analysis was carried out in the reflectance/absorbance mode at 250 nm. The method was validated with respect to linearity, specificity, accuracy, precision, limit of detection and limit of quantitation and applied for analysis of paracetamol and flupirtine maleate in combined tablet dosage form. The Rf values were found to be 0.27 ± 0.02 and 0.47 ± 0.02 for paracetamol and flupirtine maleate, respectively. The linear regression analysis data for the calibration plots showed a linear relationship in the concentration range 975 - 2275 ng/band with correlation coefficient 0.9990 for paracetamol and 300 - 700 ng/band with correlation coefficient 0.9963 for flupirtine maleate. The proposed method can be applied for routine analysis of tablets containing flupirtine maleate and paracetamol in combination.


Keywords: Paracetamol,Flupirtine maleate

Statistical Process Control as a Tool to Control Weight Uniformity of Tablets.
Statistical Process Control as a Tool to Control Weight Uniformity of Tablets. Pages8 - 15

Hetal Patel, Chirag Desai, Anil Thaker

Abstract: Quality of a product can be controlled at two distinct phases of manufacturing process: Post-process control and In-process control. Post process control is a postmortem study and leaves no scope for improvement as the entire batch has been produced; whereas in-process control provides surveillance and feedback for keeping processes in control and hence provides scope for improvement. Aim of the present work was to apply statistical control tool such as control charts and frequency distribution curve to weight variation of tablets which is the main In Process Quality Control (IPQC) variable affecting the dosage variation. Limitations of Pharmacopoeial specifications for weight variation test and current practice in industries which needs reference have been highlighted. Cipium tablets were prepared by wet granulation method. The tablets were collected from both the sides of double rotary compression machine in small groups in the order of compression and weighed individually at every half an hour. Pharmacopoeial compliance for weight variation was checked and Mean, Range and SD charts were plotted which were used to check the state of the process. Inspection of the control charts indicated that some disruption of uniformity occurred during the compression but Pharmacopoeial compliance was observed.


Keywords: Statistical Process Control (SPC), Control charts, Frequency Distribution Curve (FDC)

Mutagenic role of Artificial Ultraviolet (UV-C) Irradiation on the Growth and Yield of Tomato (Solanum Lycopersicon L.)
Mutagenic role of Artificial Ultraviolet (UV-C) Irradiation on the Growth and Yield of Tomato (Solanum Lycopersicon L.) Pages16 - 20

Abdulkareem A, Mustapha T, Garuba T., Kasture A., Oyeyiola B.

Abstract: Effects of artificial ultraviolet (UV-C) radiation (254nm) on the growth and yield of Solanum lycopersicon (tomato) accession NGB 01301 were studied. Viable seeds were irradiated with handheld UV lamp (model UVGL- 55; Science company, USA) for 0, 10, 20, 30, 40, 50 and 60 min. Treated seeds were sown in plastic buckets at the screened house of the Botanical garden of the University of Ilorin, Nigeria in five replicates. Quantitative data were obtained at maturity, 20 WAS (Weeks After Sowing) and subjected to Analysis of variance using SPSS 16.0 for Windows. Highest germination (93.33%) was obtained in 30 min treatment and the lowest (63.33%) in 10 min exposure. Maximum plant height (53.37 cm) was recorded in 10 min while the least (47.60cm) was in 60 min treatment. Petiole length was highest (2.40 cm) in treatment for 10min, treatment with 50 min produced least petiole length (1.37±0.26 cm). With respect to leaf parameters, optimum performance was recorded in 30 min treatment. However, highest performance in response to UV irradiation with respect to petiole length, number of branches and leaf number occurred in 10 min treatment. Among the exposure time evaluated, 30 min produced early maturing plants with highest fruit yield.


Keywords: Mutagenic, Ultraviolent light, radiation, treatment, Solanum lycopersicon.

Development and Validation of HPTLC Method for Simultaneous Estimation of Budesonide and Levalbuterol Hydrochloride in their Combined Pharmaceutical
Development and Validation of HPTLC Method for Simultaneous Estimation of Budesonide and Levalbuterol Hydrochloride in their Combined Pharmaceutical Pages21 - 28

Pintu Prajapati, Bhavin Marolia, Kunjan Bodiwala, Jatinkumar Vadodariya, Shailesh Shah

Abstract: An accurate, specific and precise HPTLC method has been developed for the simultaneous estimation of Budesonide and Levalbuterol hydrochloride in their combined pharmaceutical dosage form. The chromatographic separation of Budesonide and Levalbuterol Hydrochloride was performed using aluminium plate precoated with silica gel 60 F254 as stationary phase and toluene: methanol : triethylamine (7 : 3 : 0.2, v/v/v) as mobile phase. The quantification was carried out at 275 nm. The Rf values were found to be 0.38 ± 0.02 and 0.61 ± 0.02 for Levalbuterol Hydrochloride and Budesonide respectively. The linearity was observed in range of 200-1000 ng/spot for Budesonide and 500-2500 ng/spot for Levalbuterol Hydrochloride. The correlation coefficient (R2) was found to be0.9930 and 0.9960 for Budesonide and Levalbuterol Hydrochloride respectively. The method was validated for precision, accuracy, LOD and LOQ as per ICH guideline. The method was applied for simultaneous estimation of Budesonide and Levalbuterol Hydrochloride in their combined pharmaceutical dosage form. The assay results were found to be 99.12%± 0.36 for Budesonide and 98.99%±0.47 for Levalbuterol Hydrochloride of percentage label claim of their combined pharmaceutical dosage form.


Keywords: High Performance Thin Layer Chromatography,Budesonide,Levalbuterol Hydrochloride.

Development and Validation of Stability Indicating HPTLC Method for Estimation of Bosentan Monohydrate in Tablet Dosage Form
Development and Validation of Stability Indicating HPTLC Method for Estimation of Bosentan Monohydrate in Tablet Dosage Form Pages29 - 35

Bhavin Marolia, Shailesh Shah, Kunjan Bodiwala, Pintu Prajapati, Hemakshi Jariwala

Abstract: A sensitive, accurate, and precise stability-indicating HPTLC method has been developed for the estimation of Bosentan monohydrate in the presence of its degradation products. The drug was subjected to acidic, alkaline, oxidative and photo-degradation conditions. The method employed Chloroform: methanol: ammonia solution (8.5: 1.5: 0.1 v/v/v) as a mobile phase and Silica Gel G 60 F254 TLC plates as stationary phase. Quantitatively the spots were scanned at 270 nm. The Rf Value of drug was found to be 0.49 ± 0.02. The linearity was obtained in range 200 – 1000 ng/spot. The LOD and LOQ were found to be 17.42 ng/spot and 54.43 ng/spot respectively. The percentage recovery was found in the range of 98.90 – 100.30%. One degradation product was separated in each acidic, photolytic and oxidative condition; two degradation products were separated in alkaline degradation condition by HPTLC method. The method was validated according to the ICH guidelines Q2 (R1). The developed method was successfully applied for quantitative analysis of Bosentan monohydrate in its marketed formulation.


Keywords: Bosentan monohydrate(BST),HPTLC,Stability Indicating Method,Forced Degradation Study

Volume -1 Issue -1
The P-type ATPase Mediates Copper Tolerance in Klebsiella pneumoniae IFCu4 Strain Isolated from South Gujarat Industrial Effluents.
The P-type ATPase Mediates Copper Tolerance in Klebsiella pneumoniae IFCu4 Strain Isolated from South Gujarat Industrial Effluents. Pages1 - 7

Prasant Kumar, Jigna Patel, Bishun Prasad, Rushabh Shah

Abstract: South Gujarat is one of the heavily industrial based regions in India rendering a man-polluted environment. Industrial effluent samples were used to isolate copper tolerant bacteria. The isolate IFCu4 tolerated copper (CuSO4) at 28 mM in minimal media. The isolated strain was identified as Klebsiella pneumoniae through16S rRNA gene sequencing and the sequence was submitted to NCBI database (Accession number: KF496212). The strainIFCu4 (Klebsiella pneumoniae)alsopossesses the integral inner membrane copper-transporting P-type ATPase, which was confirmed by polymerase chain reaction with specific primers for copA gene. The presence of copA gene encoding copper-transporting P-type ATPase contributes in removal of excess Cu (I) from the cytoplasm to protect microorganisms from copper-mediated toxicity at high concentrations; hence it is proposed that the isolated strain has potential role in bioremediation.


Keywords: Copper, Klebsiella pneumoniae, copA

Development and Validation of Stability Indicating HPTLC Method for Estimation of Acenocoumarol in Tablet Dosage Form.
Development and Validation of Stability Indicating HPTLC Method for Estimation of Acenocoumarol in Tablet Dosage Form. Pages8 - 15

Mitali Patel, Bhavin Marolia, Shailesh Shah

Abstract: The project involves development and validation of stability-indicating HPTLC method for the estimation of Acenocoumarol in the presence of its degradation products. Acenocoumarol was subjected to alkaline, acidic, oxidative, thermal (dry heat) and photo-degradation conditions. The drug was spotted on precoated silica gel G 60 F254 TLC plate using Toluene: Isopropyl Alcohol: Methanol (9.0: 1.0: 0.5) as a mobile phase. The drug was scanned at 290 nm. The Rf value of acenocoumarol was found to be 0.50 -+ 0.03. The linearity was obtained in the range of 200 - 1000 ng/spot. The LOD and LOQ were found to be 26 ng/spot and 78.80 ng/spot respectively. The percentage recovery was found in the range of 98.36 - 101.28%. One degradation product was separated in acidic condition; two degradation products were separated in each oxidative and photolytic degradation conditions by HPTLC method. The drug was found to be stable when subjected to alkaline hydrolysis and under thermal (dry heat) conditions. The developed method was applied for quantitative analysis of Acenocoumarolin marketed formulation.


Keywords: Acenocoumarol(ACC),HPTLC, Stability Indicating Method, Forced Degradation Study

Effect of Timolol Maleate Concentration on Uptake and Release from Hydrogel Contact Lenses using Soaking Method
Effect of Timolol Maleate Concentration on Uptake and Release from Hydrogel Contact Lenses using Soaking Method Pages16 - 22

Furqan Maulvi, Tejal Soni, Dinesh Shah

Abstract: This paper investigates the effect of timolol maleate concentration in soaking solution on uptake and delivery of drug through hydrogel contact lenses using soaking method for ocular drug delivery. Contact lenses were soaked in four different concentrations of timolol maleate (100 g/ml, 200 g/ml, 500 g/ml and 1 mg/ml) for 12 hours. After the loading period, lenses were placed in vials containing 2 ml of simulated tear fluid and the release of drug into solution at 34 C was monitored for 24 hours. Contact lenses demonstrated significant uptake, but no significant effect was found on sustaining drug release and duration (p > 0.05) with increasing concentration of drug in soaking solution, confirmed by mathematical model and release kinetic data. Contact lenses were able to release the drug within therapeutic window for few hours only. Thus soaking method was not found to be effective for daily release through hydrogel contact lenses, suggesting the need for a novel technology to produce therapeutic contact lenses for daily use.


Keywords: Soaking method, Timolol maleate, Hydrogel contact lenses, Mathematical model.

Development and Validation of pH Independent Spectrophotometric Method for Determination of Pravastatin Sodium in Dosage Forms.
Development and Validation of pH Independent Spectrophotometric Method for Determination of Pravastatin Sodium in Dosage Forms. Pages23 - 28

Kunjan Bodiwala, Pintu Prajapati, Bhavin Marolia, Ishwarsinh Rathod, Shailesh Shah

Abstract: Aim: A simple, sensitive and pH independent spectrophotometric method has been developed for the determination of pravastatin sodium in pharmaceutical formulations. Methods and Material: The method is based on the measurement of absorbance at isosbestic point. Isosbestic point for pravastatin sodium was observed at 249 nm and absorbances were measured at same wavelength. Results: The method is found to be linear in the range of 2.5-30 g/mL for pravastatin sodium with R2= 0.9996 (n=5). The proposed method is simple, rapid and gives accurate and precise results. Market formulations of pravastatin sodium were analyzed with the proposed method. Results obtained are in good agreement with the labeled amount of pravastatin sodium (100.62 -+ 0.63, n=3) in tablet dosage forms. Conclusions: The proposed method can be satisfactorily applied for estimation of Pravastatin sodium in pharmaceutical dosage form. The method can also be applied for estimation of Pravastatin sodium in aqueous medium irrespective of pH of solution.


Keywords: UV spectrophotometry, Isosbestic point, pH independent, Pravastatin sodium

Green Efficient Synthesis of Aryl Thioamides Using Ultrasound: A Comparative Study.
Green Efficient Synthesis of Aryl Thioamides Using Ultrasound: A Comparative Study. Pages29 - 33

Bhavin Patel, Dipen Desai, Jignesh Raval

Abstract: Expeditious greener approach for the synthesis of aryl thioamide derivatives is reported. The synthetic strategy involves the reaction of aromatic carboxylic acids and thiourea in presence of Ammonium cerric nitrate as a catalyst with or without the help of ultrasound. A comparative study was done between both the synthetic methodologies. It was found that the high yield of the product in shorter reaction time was achieved in ultrasound technique.


Keywords: Sonication, arylthioamide, Ammonium cerric nitrate.

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