International Journal of Pharmaceutical Chemistry and Analysis

6-9

Authors: Rahul Hotwani,Singla Bhavika*,Akshaya N Shetti

Introduction: In India agriculture is the primary occupation of the people. With most of the population working in the fields, snakebite becomes a chief occupational hazard and a medical emergency. In India, more than 20,00,000 snake bites reported annually, of which 35,000-50,000 people die and Maharashtra alone contributes more than 2000 deaths each year. Thus this study is aimed to know the clinic-epidemiological pattern of snake bite in rural Maharashtra. Aims and Objectives: To study clinical and epidemiological characteristics found in patients presenting with snakebite in rural tertiary care unit. Design: Descriptive Cross Sectional study. Material and Methods: The study was conducted between 25/05/2017 to 10/09/2017 after obtaining institutional ethical clearance. A total of 70 patients were participated in study. Set questions were asked to the patient to know the clinic-epidemiological characteristics of snake bite. Statistical analysis: The data was analyzed and expressed in terms of percentage. Results: Patients with various age groups got admitted during the study period. Maximum number of (38) patients are in 21 to 40 yrs. Majority of patients were females were 36(51.4 %). Majority of patients (31) were farmer. Most of the patients were working in the farm 47(67.1%) while they had bite. Maximum bites are seen in patients right lower limb 22(31.2%). The most common vehicle used was two-wheeler 38(54.2%). Out of 70 patients admitted in hospital, 36(51.4) patients suffered with vasculotoxicity. 14(20%) patients brought snakes after killing to the hospital for identification. 22(31.4%) patients out of 70 took primary treatment in primary health care center. Out of 27 patients 5 patients required ventilator support who suffered with neurotoxic type of snake bite. We observed no mortality among 70 patients admitted with snake bite. Conclusion: Regular public health programs educating about prevention, pre–hospital management, early and safe transfer of the victim to the hospital should be done.

14-23

Authors: Manoj Kumar Katual*,Gurfateh Singh,S L. Harikumar

The major focus of the present investigation is to enhance the solubility and dissolution rate of Rosuvastatin Calcium. Preaparation of Solid dispersions of Rosuvastatin Calcium by using Vitamin E TPGS, A.Marmelos, and Gum Karaya as carriers in different ratios through solvent evaporation method. As Solid dispersions have been traditionally used effective techniques to improve the dissolution properties and bioavailability of poorly-soluble drugs. The model drug selected Rosuvastatin Calcium, which is BCS class-II drug with anti-hyperlipidemic potential. The reported bioavailability from oral route of drug is only 20%. So aim of current study is to improve the solubility and dissolution rate of a poorly water-soluble drug Rosuvastatin Calcium, by solid dispersion technique. Physical mixtures and solid dispersions were prepared using Vitamin E TPGS, MGK & natural polymers A.Marmelos in different to drug to carrier ratios, dispersions were prepared by solvent evaporation technique. Prepared formulations were characterized in solid state by FTIR analysis, powder X-ray diffraction, Scanning electron microscopy and in-vitro dissolution study. The aqueous solubility of Rosuvastatin Calcium was favored by presence of both the polymers. Solid state characterizations indicated the Rosuvastatin Calcium was present in amorphous form and entrapped in polymer matrix. In contrast to the very slow dissolution rate of pure Rosuvastatin Calcium, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. Solid dispersion prepared with TPGS showed maximum 91.19% Drug release. The best formulation of solid dispersion selected and subjected to fast dissolving tablets. The mixtures of solid dispersion and excipients were evaluated for pre-compression parameters. After then fast dissolving tablets were prepared by direct compression technique. The formulated tablets were evaluated by post compression parameters. In-vitro drug release performance of the developed formulations was investigated. Followed by that, the release mechanism of the formulations was also studied by applying various kinetic models. The overall results revealed that the formulated fast dissolving tablets complied with the standards and exhibited satisfactory performance in terms of drug release and other related parameters.

165-178

Authors: A K Mohiuddin*

Extemporaneous compounding takes place in community and hospital pharmacies. There are usually specialist compounding pharmacies in major towns and cities, but any pharmacy may undertake compounding as long as they have appropriate facilities according to state-based legislation (e.g. allocated clean bench, specific compounding equipment). Although development is a continuous process, companies are customizing features to meet the majority of patient needs, but the very nature of the process cannot meet all patient needs. The risk-benefit ratio of using traditionally compounded medicines is favorable for patients who require specialized medications that are not commercially available, as they would otherwise not have access to suitable treatment. However, if an FDA-approved drug is commercially available, the use of an unapproved compounded drug confers additional risk with no commensurate benefit. Published reports of independent testing by the FDA, state agencies, and others consistently show that compounded drugs fail to meet specifications at a considerably higher rate than FDA-approved drugs. Compounded sterile preparations pose the additional risk of microbial contamination to patients. In the last 11 years, three separate meningitis outbreaks have been traced to purportedly ‘sterile’ steroid injections contaminated with fungus or bacteria, which were made by compounding pharmacies. The 2012 outbreak has resulted in intense scrutiny of pharmacy compounding practices and increased recognition of the need to ensure that compounding is limited to appropriate circumstances. Purpose of the Study: The article aims to physico-chemical and economic considerations before compounding; factors and quality control issues; compounding support, training, chemical supplies, types of compounding (specially in hospital and ambulatory care compounding). It should aid to practice the extemporaneous preparation of basic and advanced formulations including pharmacopoeial and non-pharmacopoeial formulations encountered in pharmacy practice, together with requisite documentation, labeling, packaging and counseling requirements. Along with this, they have to study the analysis of formulations and their components and relate these to the clinical performance of medicines. This will help them to investigate, evaluate and report the physical characteristics of formulations including release kinetics and relate these to quality control and preformulation requirements; relate the application of quality control, quality assurance and the principles of good manufacturing practice to regulation of medicine production in home and abroad. Outline: Background; Introduction; Compounding Factors; Types of Compounding; Identifying Errors and Cause; Types of Compounding; Risk Management

123-129

Authors: A. V. Ganokar*,S U. Bhoyar,N S. Raut,K R. Gupta

The challenges in the field of chromatographic separation mainly fast and efficient separation for variety of samples has led to the changes in particle size, improvement in packing material design, development of synthetic method has provided the possibility of fabricating silica nanoparticle with different sizes in nanometer ranges. In present review, we have tried to show the journey of silica particle over the years and changes in the size, surface, internal pore size and packings. Their applications especially the mesoporous nanoparticles have also been mentioned.

133-140

Authors: Dhara R. Patel*

The present work describes a simple, accurate and precise Stability indicating RP-HPLC method for the estimation of Capecitabine (CPT) in bulk and pharmaceutical formulation. The Mobile phase used was Acetonitrile: Water (60: 40v/v) with 1ml/min. flow rate and 240nm was used as a wavelength maximum. The C18 HS (250 X 4.6) mm, 5 µm column was used as a stationary phase. The method was validated as per the ICHQ2 Guidelines. The retention time of CPT was found to be 3.3 min. A linear response was observed in the range of 10-50 ?g/mL with a regression coefficient of 0.999. The LOD and LOQ were found to be 1.43?g/mL and 4.34?g/mL respectively. This method can be used for the determination of CPT in quality control of API and dosage form without interference of the excipients, impurities and degradation products and hence can be used as stability indicating assay method. CPT was subjected to degradation under different stress conditions recommended by ICH viz acid, alkali, photolytic, dry heat and oxidative condition. The samples so generated were used for degradation studies including degradation kinetic study using the developed method. The degradation pathway of CPT was found to be acid hydrolysis and temperature exceeding 100°c. The degradation kinetic study shows that the acid hydrolysis, alkaline hydrolysis and oxidative degradation of the CPT follow first order kinetic.

144-146

Authors: M P. Shinde*,Aishwarya Patil,A. P. Bendale,S. P. Narkhede,A G. Jadhav

Tenofovir alafenamide is a nucleic acid analogue that is used for treatment of HIV infection and Hepatitis B. As compared with the other prodrug of tenofovir, tenofovir alafenamide is having less side effects, it is Steady in plasma and then quickly changed over into tenofovir once inside cells. The main aim and objective of present study was to perform the stability indicating studies as defined under ICH Guideline Q1A R2) by using UV spectrophotometer. According to ICH guidelines, of temperature, time, photo degradation, acid/base are the factors which are responsible for formation degradation product of a drug. UV-Vis spectroscopy method was intiated to study and compute the amount of drug in the presence of degradation products. The method was developed by using water as diluents and ? max was 260nm. Linearity was established for in the range of 2-10 ?g/mL with regression coefficient of 0.9912. The drug was subjected to acid, alkali and neutral hydrolysis, oxidation degradation conditions. The limits of detection (LOD) and quantification (LOQ) were calculated and found to be 1.43 ?g/mL and 4.33?g/mL, respectively. The method was found to be simple, economic and less time consuming as compared to other analytical techniques.

151-155

Authors: Sruthi K,Prasanth S.S*,Kamarunnisa K,Drisya N.K,Ashyam K

A fourier transform infrared (FTIR) spectrometric method was developed for the rapid, direct determination of levosulpiride in different pharmaceutical products.1-3 The universal ATR spectra were recorded and used for this study. Multiple linear regression (MLR) where a restricted set of absorption band is used for calibration beer-lambert law was used for data processing. A recovery of 98.5% of levosulpiride from the tablet dosage form with a correlation coefficient of 0.996 was obtained. The aim of this study was to develop a FTIR spectrophotometric procedure for the analysis of levosulpiride in raw material and tablets. The linear regression equation for levosulpiride was calculated to be y=189.04+152.39*x where x and y are concentration and integrated peak area respectively. The method had excellent reproducibility for the standard of 50 mg, 49.5 ±1.02 mg (n =6). The recovery test is an experimental design to verify the relationship between the amount of substance added and the amount quantified by this assay. In this test the observed concentrations of pure levosulpiride in the powdered tablets were not significantly different from the stated concentrations by student's t test, p = 0.05% (100.04 ± 1.49%, n = 3) the method gave rise to linear data in the range 2-50. Mg with accuracy and precision in the range 0.77-3.2%. Therefore, this FTIR-spectrophotometric assay was accurate, and may be recommended for the simple quantification of levosulpiride.

59-66

Authors: D. P. Kawade, A.V. Hadke

Pain and inflammation are simultaneous responses in bacterial infections. In current clinical practice, the agents like antimicrobial drug are prescribed concurrently. A POCl3 catalyzed, efficient, one-step and solvent-free synthesis of novel thieno [2, 3-d] pyrimidin-4(3H)-one derivatives from 2-amino-4,5-substitutedthiophene-3-carbonitrile has been developed using various aliphatic acid under conventional heating and microwave irradiation. The formation of compounds was confirmed using elemental analysis and spectroscopic techniques like FTIR, 1H NMR and Mass spectroscopy. All synthesized compounds have been screened for their antimicrobial activity against Escherichia coli (Gram –ve strain), Bacillus subtilis (Gram +ve strain) for antibacterial activity and antifungal activities against Aspergillus niger and Candida albicans. The result showed that synthesized compounds exhibit weak, moderate and good antimicrobial activity. It was observed that the compounds 2a, 2c, 2d, 2e, 2f, 2g, 2j and 2k showed good antimicrobial activity whereas compounds 2b, 2i, 2j showed significant antimicrobial activity compared with standard drug Streptomycin and Amphotericin B respectively.

74-83

Authors: M. Prasada Rao, B. Rama Rao, M. Srikanth

To develop a new, simple, sensitive, accurate, and economical analytical methods for the estimation of related compounds in Cefixime formulations. Validate the proposed methods in accordance with USP, EUROPE and ICH guidelines for the intended analytical application. Identify whether the given sample is Cefixime by IR spectroscopy and solubility test. To determine the wavenumber in cm-1 (reciprocal to wave length region) of given sample by Infrared Spectroscopy. To determine the moisture content present in the given sample of Cefixime by Karl Fischer method. Find out the assay and related substances (impurities) of given Cefixime by using the validated method with help of High performance Liquid Chromatography. Estimate the amount of Residual solvents by Gas Chromatography. The tests were performed as per the requirements of EUROPE monograph for Cefixime.

89-93

Authors: Nita Yadav, Anju Goyal

Optical methods through ultraviolet-spectrophotometer were developed and justification was done to validate the method for quantitative determination of aliskiren in its tablet formulation. Wavelengths for different methods were chosen by running selected sample in spectrum mode of the instrument, it was 279 nm; absorbance maxima for zero order technique, 289 nm; peak minima for first order derivative technique and between 269 nm and 289 nm for AUC technique using distilled water as reference. After studying linearity graph, working concentration range selected for method I, method II and method III was in between 25 to 150 µg mL-1. R2 value equal to 0.999 confirmed a better correlation between concentration and absorbance. Percentage purity of aliskiren in tablet formulation was found in between 98.54-100.36 which was very close to label claim. Validation following ICH guidelines was done to justify the results obtained through method I, method II and method III. The percentage of the standard drug recovered in recovery study for all the three techniques were within the limit and were in between 98.61-101.66. The percentage relative standard deviation in precision study was less than 2 for all the techniques. From the observed data it can be said that the developed methods can be utilized for quantitative estimation of aliskiren in tablet formulation.

100-105

Authors: Tilotma Sahu, Bina Gidwani, Abhishek Kumar

The objective of the study was to increase the bioavailability of selected drug rosuvastatin by preparing complex of drug with ghee. Dissolution study was done by using paddle apparatus USP type 2 and permeation study was performed by everted intestinal method. The different ratios of complexes were prepared by solvent evaporation method and evaluated. The complexes were Rosuvastatin calcium with native ghee complex(1:1 to 1:5), rosuvastatin calcium with oxidized ghee complex (1:1 & 1:5), and complex with adsorbate rosuvastatin calcium with MCC and oxidized Ghee complex (1:1:1) and rosuvastatin calcium with aluminum magnesium silicate and oxidized ghee complex (1:1:1). In dissolution study of rosuvastatin calcium the percentage drug release was in the range from 35% at 15 minutes and 98% within 90 minutes; while in case of rosuvastatin calcium with native cow ghee and oxidized cow ghee, the % drug releases decreased to93% to 52% at 90 minutesand 93% to 55% at 90 minutes respectively. Thus the prepared complexes sustained the dug release. The permeation study showed that in the presence of ghee the permeation of rosuvastatin showed 96% release at 105 minutes and 93% at 75 minutes. Results of dissolution study proved that complexation with oxidized ghee led to maximum increase in bioavailability as compared to native ghee.

7-11

Authors: Supriya Sharma, Yeshwant Deshmukh, Priya Ann Sam, Urmila Salve.

Objective: To compare the efficacy of olanzapine and risperidone in the treatment of positive and negative symptoms of schizophrenia. Materials and Methods: The study was conducted in MGM medical college Navi Mumbai between October 2012 to September 2014. The study included 110 patients of schizophrenia. The positive and negative symptoms were assessed with the help of the PANSS (positive & negative symptom score) scale. Results: We observed that the mean percentage reduction in score in the positive scale of PANSS was 48.74% in the risperidone and 49.40% in the olanzapine group .The negative score reduced by 56.32% in the Risperidone group and by 61.59% in the olanzapine group on the PANSS. Conclusion: olanzapine was superior to risperidone in controlling the positive as well as negative symptoms of schizophrenia clinically but the results were not statistically significant.

16-23

Authors: Paul Jacob, Beena Thomas, Neethu Santhosh.

Thiadiazole derivatives are reported to have various biological activities including antihyperlipidemia. In the present study a series of N-phenyl-1, 3, 4-thiadiazol-2-amine derivatives were designed using various softwares like Molinspiration, Schrodinger etc. The derivatives with optimum properties were synthesized and characterized using FT-IR, 1HNMR and MASS spectroscopy. In vivo screening for antihyperlipidemic activity in triton X-100 induced models showed moderate activity in comparison with standard.

31-38

Authors: Devangi K. Patel, Amit J. Vyas, M. N. Noolvi, Ashok B. Patel, Nilesh K. Patel.

A simple, specific, precise, accurate and economic isocratic RP-HPLC method was developed for the simultaneous determination of Ambroxol hydrochloride, Levocetirizine hydrochloride, Phenylephrine hydrochloride and Paracetamol in bulk and tablet dosage form. A reverse phase Nucleosil C18 column (250 mm x 4.6 mm x 5 µm) with mobile phase consisting of Methanol: Sodium Phosphate dibasic anhydrous Buffer (65:35 V/V) having (pH of buffer 7.0 ± 0.02 adjusted with ortho phosphoric acid) was used. The flow rate was 1.0 mL/min and the effluents were monitored at 230 nm. The retention times of Paracetamol, Levocetirizine hydrochloride, Phenylephrine hydrochloride and Ambroxol hydrochloride were found to be 3.117, 4.925, 6.217 and 12.308 min. respectively. The method was validated in terms of linearity, range, specificity, accuracy, precision and robustness. The proposed method was successfully applied for the estimation of paracetamol, levocetirizine hydrochloride, phenylephrine hydrochloride and ambroxol hydrochloride in combined tablet dosage form.

43-51

Authors: Bebee Pathare, Vrushali Tambe, Dnyaneshwari Waichal, Rahul Chanshetti, Rohini Pujari.

Objective: To investigate the potential of novel polymer isolated from fruit Artocarpus heterophyllus for mucoadhesion and sustained release action. Microspheres containing Lornoxicam formulated using isolated polymer offered a suitable, practical approach to achieve a prolonged therapeutic anti-inflammatory effect by continuously releasing the medication over extended period of time. Materials and Methods: D-Optimal design was applied to optimize the fruit polymer and sodium tripolyphosphate concentration which was used as a cross-linking agent. Result: Fruit polymer and sodium tripolyphosphate concentration has significant impact on % entrapment efficiency, mucoadhesivity, and in vitro release. Differential scanning calorimetry and infrared spectroscopy results indicates that no interaction between drug and excipients. Polynomial models were validated using one way ANOVA and results indicated that isolated fruit polymer and sodium tripolyphosphate used have significant effect on selected response (p<0.05). Contour plots and three dimensional response surface curves were drawn. In vivo studies were carried out for the optimized formulation. Furthermore, the pharmacokinetic parameters of the Lornoxicam microspheres showed constant release with minimum fluctuation in plasma drug concentration. The in vivo pharmacokinetic studies clearly demonstrate that microspheres of Lornoxicam shows sustained release action for 24 hrs. Conclusion: From the result of the present work, it was concluded that preparation of Lornoxicam loaded microspheres by ionic gelation technique using novel isolated polymer from fruit of Artocarpus heterophyllus might be promising approach for sustained release mucoadhesive formulations.