International Journal of Pharmaceutical Chemistry and Analysis

101-105

Authors: M.Prasada Rao, M. Srikanth, K. Umamaheswari.

This is the present work which is a new method development and validation was carried out for the estimation of Amlodipine besylate and hydrochlorthiazide by RP-HPLC technique. The wavelength selection was made at 245 nm in various literature were having a maximum absorbance at around 240 to 250 nm. Hence the wavelength was selected at 245 nm for the detection of the compound. In this method development several trials had been carried out and reported. Leading this to the optimized chromatographic conditions for the estimation of Amlodipine besylate and hydro chlorthiazide pharmaceutical dosage form. Preliminary studies involved trying C18, columns and several mobile phase compositions for the effective separation of these drugs by using symmetry C18Hypersil-BDS column eluted with the mobile phase Degassed water and acetonitile with a flow rate of 1.0ml/ min and a detection wavelength of 245 nm with injection volume of 20 ml at ambient (25°C) temperature yielded the good results.

112-116

Authors: Pawan S. Avhad.

India is a country which is full of natural recourses on all direction of land such as snow fall on northern India, highest rainfall in northeast, hot desert on west and damp sea air on remaining costal area. Such types of climates are hardly available in any country in the world. Due to all this three seasons are observed in India, like summer, Rainy season, and winter. Because of change in climates there will be sudden growth of microorganism in atmosphere and chances to increase the illness in common people. The illness due to change in season is called as viral infections. Generally viral infections include sneezing, coughing, cold, fever, body ache etc. Depending upon the immunity of individual number of patients are cure within in few days either by oral analgesic, anticold, or basic antibiotics or by simply OTC medicines but few were treated with IV antibiotics. Majority of people complaint with sore throat, patches in throat, because of cold air entered in respiratory tract and produces running nose and irritation in throat. Number of viruses is pathogenic in human being producing a variety of syndromes. In a large majority of the cases, viral infections are not apparent or subclinical; only in some of them is a clinical disease produced. Clinical illness following a virus infection depends upon factors in the virus and the host. The very important factor in a virus is genomic alterations. The factors in the host mostly depend upon the nutritional status and the immune system. The life cycle of a virus starts with its entry into a host; it reaches the susceptible target cell, enters it, replicates and causes cell injury, and may be cell death. At any of these steps the life cycle of the virus can be aborted by various body mechanisms, mainly by the immune response. A single cough can release hundreds of droplets, a single sneeze thousands (up to 40 000) each droplet containing millions of viral particles.

59-65

Authors: Anup Sharma, Bulbul Purkait.

The morphological changes occurring because of trituration and solid dilution have been assessed by surface electron microscopy to follow medicinally active ingredients and validation of these findings became the objective of the study. Diluted Pharmaceutical agents Silica and Potassium Chloride were analyzed for comparison. The SEM presentation of the biochemic drugs support the idea that it is the unique characteristic change of the virgin drug substances produced because of trituration and solid dilution which is responsible for the changes in medicinal properties. The high intensity electron beam caused multiple fractures on softer molecules which helps distinguishing between lactose and the drug particles.

70-78

Authors: Jagadeswara Rao K, Murali Mohan SV, Rama Rao Malla.

The pharmaceutical dosage form manufacturing process use some of polymers, which contains traces of inorganic elements like Tin (Sn) content. The traces of inorganic elements were determined by using inductively coupled plasma mass spectroscopy (ICP-MS). It is a sensitive method used to determine the inorganic elements by atomic mass value. In the present study Tin (Sn) was extracted by the sample using microwave-assisted digestion with hydrochloric acid. Different validation parameters were employed to evaluate the method in terms of selectivity, specificity, method precision, accuracy, intermediate precision and standard measurement uncertainty. The mass value of tin element is 118 as per the Perkin Elmer instrument recommendations. The results indicate that this method could be used for the routine measurement of tin (Sn) in the pharmaceutical laboratories.

83-87

Authors: Sonali P. Mahaparale, Vikas Gaware.

Transdermal route of administration of drug is effective route of administration for different kind of indications. The purpose of present investigation was to develop Lornoxicam emulgel for systemic effect and to avoid side effects and minimize frequency of administration. Lornoxicam (NSAIDS) is a cox-1 and cox-2 inhibitor used in the treatment of pain, inflammations rheumatoid arthritis. Emulgel of lornoxicam was formulated using triethanolamine (5%) as solvent, carbopol 934 and carbopol 940 as gelling agents and various preservatives formulated gel was evaluated with respect to different physiochemical parameters such as ph, viscosity, Spreadability % drug content. All the prepared emulgel showed acceptable physical properties like homogeneity, colour, consistency, ph value, Grittiness, Spreadability, Extrudability % drug content. The results of in vitro drug release showed that carbopol 940 (0.4 gm) based emulgel gave better release. Also it was found that the gelling agent concentration had the most pronounced effect on the drug release from the emulgel.

30-34

Authors: Debarshi Kar Mahapatra, Santosh S. Chhajed, Ruchi S. Shivhare.

Murrayanine and chalcone are well known for their anti-diabetic potentials. The present research represents an effort is represented in which the two scaffolds were rationally integrated with an objective that the designed hybrid molecule will cumulatively produce higher pharmacological activity than their parents, and will also illustrate analogous or more pronounced activity with the marketed product. All the novel murrayanine-chalcone hybrids exhibited activity in the range of 6.27-30.87%. The molecules 3a, 3f, 3g, and 3h exhibited an effective reduction of blood glucose level (>18%). Chalcone 3g, having two lipophilic substituents at meta positions in the B-ring presented the highest anti-hyperglycemic activity (30.87% lowering of glucose level). From the study, it was evidenced that the positions of substitution and their number played an intense role in exhibiting anti-diabetic activity. A superior biological activity was observed with electrophilic halogen substituents at para and meta positions as compared to ortho position. However, a very well defined structure-activity-relationship (SAR) cannot be defined from this study. The study opened new avenues for utilizing the natural scaffolds in form of hybrids as anti-diabetic agents which may act by modulating various anti-diabetic targets. Still, further research is needed to elucidate the complete mechanism of action(s) of the synthesized hybrids.

37-42

Authors: Garima Verma, Mohemmed Faraz Khan, Wasim Akhtar, Mohammad Mumtaz Alam, Mohammad Shaquiquzzaman.

1,3,4-oxadiazoles, heterocycles bearing one oxygen and two nitrogen atoms in a five membered ring have their application in the diverse areas of medicine. Enough literature is available demonstrating antibacterial, antifungal, anticonvulsant, antiviral, antidiabetic and antimalarial potential of the moiety. Owing to their wide applications, scientists across the globe are engaged in the design and development of oxadiazole derived medicinal agents. This motif can also be traced in a number of drug molecules. Most commonly adopted method for their synthesis includes he reaction between acid hydrazides and acid chorides/carboxylic acids or direct cyclization of diacylhydrazines in the presence of different dehydrating agents like phosphorus oxychloride, thionyl chloride, phosphorus pentaoxide and polyphosphoric acid. This manuscript covers different conventional and non-conventional approaches adopted for the synthesis of 1,3,4-oxadiazole derivatives.

46-50

Authors: Aditi Malasiya, Anju Goyal.

A simple, specific, accurate, precise , rapid, robust and selective stability indicating reverse phase high performance liquid chromatography (RP-HPLC) method has been developed for assay and related substances and validated for quantification of antifungal drug with its excipients in its topical dosage form. Forced degradation study is done to determine stability of the product. The mobile phase has been used for separation consisting of ammonium acetate buffer: ACN (60:40). Column used was inertsil ODS 3V (4.6*150 mm, 5µm) with flow rate of 1.0 ml/min. Detection wavelength for luliconazole was 294 nm and for methyl paraben was 254nm. The method has been linear for both compounds at 50-150% range with r2 0.998 and 0.999 respectively. Luliconazole and methyl paraben has showed 98-102% recovery. The method have been robust under various variation with flow rate, detection wavelength and column oven temperature. The drug was exposed to stress conditions. Method resolves all degraded product as compared to luliconazole. Developed method can be used routinely for estimation of drug luliconzole with its excipient methyl paraben in dosage form and stability sample.

Page No. 5-7

Authors: Nilambari L. Darade, Yawatkar PC

Amlapitta is most common disorders in the society nowadays, due to indulgence in incompatible food habits and activities. In Brihatrayees of Ayurveda, scattered references are only available about Amlapitta. Kashyapa Samhita was the first Samhita which gives a detailed explanation of the disease along with its etiology, signs and symptoms with its treatment protocols. A group of drugs and Pathyas in Amlapitta are explained and shifting of the place is also advised when all the other treatment modalities fail to manage the condition. The present review intended to explore the important aspect of Amlapitta and its management as described in Kashyapa Samhita, which can be helpful to understand the etiopathogenesis of disease with more clarity and ultimately in its management, which is still a challenging task for Ayurveda physician.

Page No. 13-19

Authors: RP Bhole, SB Wankhede, YB Zambare, TS Wankhede

A HPTLC method was developed and validated for determination of Linagliptin in tablet formulation and in biological sample. The chromatography was performed on pre-coated silica gel 60 F254 plates using methanol: toluene 7:3 (v / v) as mobile phase. The optimized chromatographic conditions gave good peak shape with acceptable Rf value of 0.48 for Linagliptin. Method was validated as per ICH guidelines. The calibration plots were linear between 50–300 ng/ band and between 50-500 ng/ band in pure and in biological sample, respectively. Accuracy of the proposed method was evaluated by recovery studies (% recovery= 100.38% and 99.99% from tablet sample and biological sample, respectively). In stability testing, Linagliptin was found susceptible to acid hydrolysis, alkali hydrolysis and oxidation (3 % H2O2). The method was able to selectively quantitative. Linagliptin in presence of degradation products and components likely to be present in the biological matrix.

Page No. 24-26

Authors: Akshaya N. Shetti, SN Mahajan, Vaishali Kadam, Mallikarjun Reddy, Tushar Tanpure

Guillain-Barre syndrome (GBS) is also known as acute idiopathic polyneuritis. It is a neuromuscular paralysis that occurs in all the age groups and has several variants. These include demyelinating polyneuropathy, acute axonal neuropathy, Bickerstaff brainstem encephalitis, pharyngo-cervical-brachial variant, Miller Fisher syndrome and polyneuritis cranialis. Miller Fisher syndrome (MFS) is a rare variant of GBS which is observed only about 1% to 5% of all cases. The incidence of the MFS is more common in males when compared to females by a ratio of 2:1. The lower and upper age groups reported with MFS are 13 and 78 years respectively. Here we report the successful management of rare form of GB syndrome.

Page No. 193-197

Authors: Jimishaben D. Kher, Jagat Upadhyay

Uncontrolled proliferation is the hall mark of cancer and abnormal cell cycle regulation in cancer. CDK plays very important role in the control of the cell cycle and its proliferation. CDK2 is the “superstar” among the CDK family.CDK2 has cyclin A and cyclin E in its complex which the cyclin A complex require to progress through S phase regulated by phosphorylation and cyclin E require to transition from the G1 to S phase in cell cycle. Also, the mechanism of binding of CDK2 with its inhibitors as well as the changes of binding mechanisms following conformational variation of CDK2 are compared. Considering this fact, inhibition or disruption of the CDK2/cyclin complexes should be possible to suppress the hyper activation of CDK2 and hold back the infinite cell proliferation. There are main four binding site of CDK inhibitors. Competitive binding sites (site 1), Noncompetitive binding sites (site 2 and 3), Allosteric binding site (site 4). CDK inhibitors are mainly used in cancers including leukemia, melanoma, solid tumors and other types are being targeted.

Page No. 205-218

Authors: Krishna R. Gupta, Kiran Keche, Anvesha V. Ganorkar

A simple HPLC method has been developed and subsequently validated for the simultaneous determination of Eperisone hydrochloride and Diclofenac sodium. Optimum chromatographic separations among the eperisone, diclofenac sodium and stress-induced degradation products were achieved by using Waters -ODS 5 μ C18 column (250 X 4.6mm) as stationary phase with Acetonitrile and 0.05% TEA pH 3.5 (75:25% v/v) as mobile phase at a flow rate of 1.0 mL min with detection at 273 nm. ICH guidelines were used to validate the developed method. Linearity was established for Eperisone hydrochloride and Diclofenac sodium in the range of 15-75 µg/ml and 10-60 µg/ml, respectively. Eperisone hydrochloride and Diclofenac sodium were exposed to acid, base and neutral hydrolysis, oxidation and photolytic stress conditions and the stressed samples were analyzed by the proposed method. Also the kinetics of degraded sample was evaluated for all the hydrolytic conditions. As the proposed method could effectively separate the drug from its degradation products, it can be employed as stability-indicating method for the determination of instability of these drugs in combined dosage form.

Page No. 229-234

Authors: Manoj V. Girase, Monika L. Jadhav

The present study was undertaken with an objective to investigate in-vivo and in-vitro immunomodulatory potential of Cassia auriculata Linn. The methanolic extracts of flowers and roots of plant were investigated for their immunomodulatory potential by using in-vivo, oxazolone-induced cell mediated inflammation in rat’s model and various in-vitro immunomodulatory models. Methanolic extracts of both flowers and roots were screened scientifically through various activities models. The result of oxazolone-induced cell mediated inflammation, showed that methanolic flowers extract possesses immunomodulatory potential. While in in-vitro immunomodulatory models like NBT reduction assay by human PMN cells, methanolic flower extract showed dose dependent stimulation. With the same extract similar observation was recorded with phagocytosis of Candida albicans by human PMN. The methanolic flower extract also increased candidacidal activity in dose-dependent manner. The methanolic flower extract significantly induced human PMN cells chemotaxis and exhibited potent effects than positive control. Thus results of in-vitro studies clearly indicated that methanolic flower extract has immunostimulant effect, where as in in-vivo study of oxazolone-induced delayed type hypersensitivity, methanolic flower extract significantly reduced rat ear edema in dose dependent manner. The in-vitro assays, revealed that methanolic flower extract possess potent immunomodulatory activity due to its antioxidant potential. In all, results represented here indicated that Cassia auriculata, in addition to its reputed cytoprotected effects, also passes significant immunomodulatory activity. Thus the flavonoids rich methanolic flowers extract can be exploited in chronic inflammatory condition, such as rheumatoid arthritis usually in combination with conventional drugs to reduce the dose and dose related toxicities of later