The Pharmaceutical and Chemical Journal

6-15

Authors: Kapoor D, Vyas RB, Lad C, Patel M, Sharma S

In the current exploration a novel oral drug delivery system was developed utilizing the concepts of controlled release and mucoadhesiveness. Mucoadhesion is a topic of current interest in the design of drug delivery systems. Mucoadhesive microspheres exhibited a prolonged residence time at the site of application or absorption and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved and/or better therapeutic performance of drugs. Nizatidine microspheres were equipped by emulsification-ionic gelation technique using mucoadhesive polymers such as Carbopol 934P, Hydroxypropyl methylcellulose (HPMC K15M) and Carboxy methyl cellulose with a rate controlling polymer sodium alginate. The arranged formulations were subjected to particle size and shape analysis, % drug entrapment efficiency, in vitro floatability, swelling rate, in vitro mucoadhesion test and in vitro drug release kinetics. The primed microspheres were discrete, spherical with a mean particle size in the range of 478±0.99μm to 640 ±2.67 μm. Entrapment efficiency was found to be in the range of 59.56±0.99 to 79.90± 1.78%. Formulations containing Carbopol 934P showed amplified in vitro mucoadhesion compared to formulations with Hydroxypropyl methylcellulose and CMC. In vitro drug release for all the formulations in 0.1N HCl was diffusion controlled progressively over a period of 12 h and followed First order kinetics. The in vitro drug release mechanism was nonfickian type controlled by swelling and relaxation of polymer. There was no noteworthy alteration in physico-chemical characteristics of the microspheres stored at diverse storage condition after 3 months of stability study. The fabricated system has the twofold advantages of being gastroretentive, to augment oral bioavailability and releasing drug in a controlled manner, to diminish the required frequency of administration thereby promoting patient compliance.

24-32

Authors: Sheikh S. Ahmad, Saaleha Mahboob Khan, Amna Butt

Medicinal usage of plants is one of the superior characteristic on which mankind is dependent upon since ages. Plants are being used for the treatment of various diseases of humans and animals. The Changa Manga Forest is designated as National Park located in Kasur, District. It consists of vast biological panorama, constituting many plants of the medicinal values. The purpose of this study was to preserve native traditional knowledge of plant’s usage, promotion of awareness and its significance to the domestic and international entrepreneur, identifying the flora, density and conservation of species. Ethno-medicinal survey was conducted in the periphery of the Changa Manga. The survey identified many plants at study site. Some of them including their medicinal values are Ageratum conyzoid, Anaglis arvensis, Coronopus didymus, Cannabis sativa, Fumairia officianalis, Oxalis corniculata, Sonchus oleraceus, Rumex crispus, Euphorbia heliscopia, Prosopis cineraria, Mentha spicata etc .They are used by the indigenous people for the treatment of ulcers, dysentery, eye problems, burns, malaria, insomnia, hepatitis, cough, cholera, insect stings, gastric problems respectively. Plants like Capparis deciduas Cleome Viscosa, Suaeda Fruticosa, Malvastrum coromendelianum are present in few numbers, but surpassing medicinal values, highlighting the need of conservation. Responsiveness of the botanist is required to focus on the sustainable use, conservation and management strategies are required for valuable medicinal species so that sustainable production, with the balanced ecosystem and development may lead the country to sustainable income and other welfare.

42-46

Authors: Shahnaz Sultana, Mohammed Ali, Kamran J Naquvi

The fruits of Lycium chinense Miller (Solanaceae) possess emmenagogue, diuretic, antipyretic and hepatoprotective properties and are used to stimulate the immune system, to increase hormonal growth, to improve blood circulation and eye sight and to cure morning sickness. Phytochemical investigation of a chloroform extract of the fruits gave two new aliphatic esters, characterized as n-butanyl n-octadec-9,12-dienoate (n-butanyl linoleate,1) and n-tridecanyl n-octadec-9,12-dienoate (n-tridecanyl linoleate, 2) and two new fatty acids identified as cis,cis,cis –n-octacos-5,8,11-trienoic acid (4) and cis-n-octacos -11-enoic acid (5) and along with a known saturated fatty acid, arachidic acid (3). The structures of these phytoconstituents have been elucidated on the basis of spectral analysis and chemical reactions.

54-61

Authors: Kapil Tak, Gaurav Bhardwaj, Y.S. Tanwar, R.P.S. Rathore, Kuldeep Choudhary

The drug chosen for the present investigation, Metformin hydrochloride, is an orally active antidiabetic agent. It is effectively used in the treatment of non-insulin dependent diabetes mellitus (NIDDM) Type II. It is more appropriately referred to as antihyperglycemic agent and found to be well-tolerated and safe even on chronic use. The objective of this study was to design and evaluate oral sustained drug delivery system for metformin hydrochloride using hydrophilic polymers such as HPMC K4M and HPMC K100M. Four batches were prepared by using HPMC K4M in drug: polymer ratio of 5:1, 6:1, 7:1, 8:1 and four batches using HPMC K100M in ratios of 5:1, 6:1, 7:1, 8:1. Further formulations were modified by varying the ratios of diluents i.e. F9, F10, F11, F12 to check the effect of diluents on drug release. Matrix tablets were prepared by wet granulation method and were evaluated for weight variation, drug content, friability, hardness, thickness, and in-vitro dissolution. Among the formulations studied, formulation F6 containing HPMC K100M (6:1) showed sustained release of drug for 24 hrs with cumulative percent drug release of 98.11%, similar to that of the research listed drug. The kinetic treatment showed that the optimized formulation follow first-order kinetic with release exponent (n) 0.711 and having good stability as per ICH guidelines. The matrix formulation F6 showed sustained release of metformin hydrochloride by the diffusion mechanism.

8-16

Authors: AbdAlwadood H. Elbadawi

The study reports modeling of laminar film condensation of horizontal flat plate with hot vapor film exists above the plate with higher temperature (saturation temperature). In this study mathematical expressions for film thickness, velocity and temperature profile were obtained analytically. Models confirm that velocity and temperature depend on the distance from plate center (x), from plate surface (δ) and depend also on Ra and Ja numbers.

22-29

Authors: Jigna Zankat, Mayank Bapna, Jigisha Patel

A simple, rapid, accurate and precise RP-HPLC method was developed and validated for simultaneous estimation of Azilsartan medoxomil and Amlodipine besylate in synthetic mixture. The chromatographic separation was carried out on Hypersil ODS C18 column (250×4.6 mm; 5µ) with mixture of 0.2% ortho-phosporic acid in water :acetonitrile (35:65% v/v) as a mobile phase; at a flow rate of 1.0 mL/min. UV detection was performed at 232 nm. The retention time was found to be 5.496 min and 3.255 min for Azilsartan medoxomil and Amlodipine besylate, respectively. Calibration plots were linear over the concentration range of 80.3-120.5 µg/mL and 20.2-30.2 µg/mL of both Azilsartan medoxomil and Amlodipine besylate, respectively. The method was validated for linearity, accuracy, precision, recovery, repeatability, LOD and LOQ. The proposed method was successfully used for quantitative analysis of Azilsartan medoxomil and Amlodipine besylate used for hypertension. No interference from the components of pharmaceutical dosage form was observed. Good percentage recovery and low relative standard deviation confirm the suitability of the proposed method for routine estimation of Azilsartan medoxomiland Amlodipine besylatein tablet dosage form.

41-51

Authors: Sheikh S Ahmad, Amna Butt, Summra Erum, Beenish Malik, Asma Jabeen

Plants which endowed medicinal values are held at the highest rank in folk medicinal systems throughout the world. The locally suggested remedies and the ethno-botanical knowledge for this purpose, whether it’s traditional or modernized, have its roots into the belief in folk medicinal knowledge of the particular region. This study was conducted at Gatwala forest park (GFP), Faisalabad, Pakistan. The method adopted for documentation of indigenous knowledge was based on semi-structured interviews and direct observations. The present study gathered the indigenous knowledge of local inhabitants and about the use of herbaceous plants they collected from GFP. A total of 40 herbaceous plants belonging to 19 families were recorded as medicinal plants at the study site. Most of the plants we found were used for the treatment of common cold, sore throat, abdominal infections, skin disorders, hepatic diseases, eye ailments, stomach problems, fever, cough, chest congestion, asthma, joint pains. Along with their ethno-medicinal uses their occurrence was also recorded as very common, common, fairly common and scarce. This appraisal has documented the inventory of important medicinal plants of GFP by giving due weight age to the indigenous folk knowledge of the local inhabitants.

6-13

Authors: Radha Chaudhary

The photo chromic behavior of Hexacyanoferrate in phthalein system was observed spectrophotometrically. Hexacyanoferrate (II) ejects electrons, which abstracts H+ from indicator molecule and this molecule of the indicator changes into their quinonoid form which is coloured.

25-30

Authors: Akshay V Patel, Gaurav Bhavsar, Jai Singh Vaghela, Navin Kapadiya

A simple, rapid, and precise reversed-phase liquid chromatographic method is developed for determination of paracetamol, aceclofenac, and chlorzoxazone in their ternary mixtures of commercial pharmaceutical preparation. This method uses C18 (Phenomenex) (150mm×4.6mm), 5 μm analytical column. Mobile phase is Methanol: Disodiumhydrogen orthophosphate (ph-3, 0.05M) 65:35 v/v. The instrumental settings are at a flow rate of 1.5 ml/min; the column temperature is 20°C, and detector wavelength is 271 nm. The sample concentrations are measured on weight basis to avoid the internal standard. The method is validated and shown to be linear. The correlation coefficients for paracetamol, aceclofenac, and chlorzoxazone are 0.9993, 0.9994, and 0.999 respectively. The recovery values for paracetamol, aceclofenac, and chlorzoxazone found 98.86%, 99.67%, and 99.51%, respectively. The relative standard deviation for six replicates is always less than 2%. This HPLC method is successfully applied to the quantitative analysis of the title drugs in tablets.

41-50

Authors: Gajendra Singh Rathore, Yuvraj Singh Tanwar, Anshu Sharma

Skin acts as a major target as well as a principle barrier for topical drug delivery. The greatest challenge for dermal delivery is stratum corneum, and in order to improve its permeability, new formulation approaches have been investigated. The main requirement for topical anti-fungal treatment is that the drugs should penetrate into skin layers to ensure effective drug concentrations following topical administration. Types of the formulations as well as the physicochemical characteristics of drug molecules are effective parameters in topical delivery of drugs. Antifungal drugs should reach effective therapeutic levels in the viable epidermis after dermal administration. The drug of choice for topical fungal disease is Fluconazole. Fluconazole has a broad spectrum of activity that includes both dermatophytes and yeasts. The drug is particularly effective in the treatment of mucosal and cutaneous forms of candidiasis. Vesicular system (Liposomes and ethosomes) entrapped in Gel is one of the most promising approaches for topical delivery of active substances and has potential for new opportunities for topical application of Fluconazole in the fungal infections.

59-68

Authors: Kamble Ravindra K, Chetan S Chauhan, Kamble Priyadarshani R, Jitendra S Rajawat, Gajendra S Rathore

The present research was aimed to design controlled release suspension formulation of BCS class I drug Tramadol hydrochloride a centrally acting synthetic analgesic. Complexes of indion 244 ion-exchange resin and tramadol hydrochloride, a model drug, were prepared using a batch method. The prepared resinate complexes were microencapsulated by o/o solvent evaporation technique. These microcapsules were then formulated into the suspension dosage form to get the controlled release of drug for extended period. The resinate microcapsule suspensions were evaluated for the flow properties, drug content and in vitro drug release. Dry powder suspensions shown excellent flow properties and the in vitro drug release showed a significant sustained drug release up to 12 hours. The stability studies were performed as per ICH guidelines for the dry and hydrated forms of suspensions. The results obtained clearly evident that the dry powder suspensions are best suitable for the storage conditions and gives better physical and chemical stability.

9-16

Authors: Devesh Kapoor, Ruchi B Vyas, Chaitali Lad, Manish Patel, Basant Lal, Ruchi Parmar

The objective of the current research work was to explore the potential of emulgel in enhancing the topical delivery of piroxicam. Emulgel formulations of piroxicam were prepared using three types of gelling agents: Carbopol 934, Xanthan gum and HPMCK15M. Based on solubility studies Tween-80 and Span-80 as emulsifiers and propylene glycol as co-surfactant were selected for preparation of emulgel. The persuade of the type of the gelling agent on the drug release from the prepared emulgel was investigated. The mentha oil is used as permeation enhancer. The formulated emulgel were characterized for their physical appearance, pH determination, viscosity, spreadability, in vitro drug release, ex vivo drug release, skin irritation test, anti inflammatory activity, analgesic activity and stability studies. All the prepared formulations showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity and pH value. In-vitro release study demonstrated diffusion controlled release of piroxicam from formulation up to 8 h. The drug release profile exhibited zero order kinetics.

25-27

Authors: Puneet Sudan, Tapan Behl, Shaveta Sharma, Swati Sabharwal

The efficacy and potency of Hibiscus sabdariffa (HS) in the treatment of risk factors associated with various cardiac and hypertensive disease is presented in this paper. Anthocyanins found in abundance in Hibiscus sabdariffa sepals are generally considered the phytochemicals responsible for the antihypertensive and hypocholesterolemic effects. Decoctions and infusions of sepals and tender leaves are used in whole world in the treatment of hypertension, hyperlipidemia and various cardiovascular ailments with no reported adverse events or side effects, except for possible adverse hepatic and renal effects at increased doses ie more than 5000mg/kg/day. The daily consumption of extract produced from Hibiscus sepals significantly decreases systolic blood pressure (SBP) and diastolic blood pressure (DBP) in adults with pre to moderate essential hypertension and type 2 diabetes. The studies revealed that effectiveness of extract is equivalent to Captropril, but less effective than Lisinopril. This comprehensive body of evidence suggests that extracts of Hibiscus sabdariffa sepals are promising in the treatment of hypertension and hyperlipidemia in diabetes -II patients. For the study, 60 volunteers suffering from diabetes with mild hypertension were recruited. But volunteers were devoid of any kind of medication for hypertension, hyperlipidemia or high cholesterol levels. The patients were randomly grouped into two groups HT and BT and asked to drink infusions of Black tea (BT) and HT (Hibiscus tea) twice a day for a month. Their BP was measured uniformly at regular intervals. The mean of Systolic BP decreased from 134.4±11.8 mmHg to 112.7±5.7mm Hg with HT after one month; whereas in case of BT group measure changed from 118.6±14.9 to 127.3±8.7 mm Hg.

5-13

Authors: Upadhyay Uma, Rathore KS

The aim of the current study is to design a sustained release matrix tablet of metformin HCl to maintain plasma level of drug for prolong period of time. Metformin HCl is antihyperglycemic agent used in the treatment of type II Non insulin dependent diabetes mellitus. Sustained release formulation of metformin HCl prolong drug absorption in the upper GI tract and permits once daily dosing in patient with type II diabetes mellitus. This newer formulation may enhance patient compliance compared to conventional immediate release metformin HCl. Metformin HCl present significant challenges due to its poor inherent compressibility, high dose and high water solubility. So matrix tablet of metformin HCl is formulated by different combination of matrix forming polymers such as hydroxypropyl methylcellulose and hydroxylpropyl cellulose by direct compression method. PVPK30 is used as a binder. Magnesium stearate and micro crystalline cellulose are used as a lubricant and filler respectively. Drug and polymer compatibility study is done by IR spectroscopy. The formulated powder mixture is evaluated for precompression parameters such as bulk density, tapped density, angle of repose, compressibility index and Hausner’s ratio for determining flow properties of mixture. Prepared tablets are subjected to post compression parameter such as hardness, thickness, weight variation, friability and drug content. All formulations showed compliance with pharmacopoeial standards. No physicochemical interaction is found between drug and polymers in IR spectrums. It would be desirable in dissolution study that formulation containing lower concentration of polymer will earlier drug release.

20-25

Authors: Raman Kr. Verma, Rishabh Kapoor, Shailendra Kr. Gupta, Rahul R.Chaudhari

Potassium Permanganate (KMnO4) is an oxidizing agent widely used throughout the water industry. It has an effect on the development of a disinfection strategy by serving as an alternative to pre-chlorination or other oxidants at locations in a treatment plant where chemical oxidation is desired for control of color, taste, odor and algae. Potassium Permanganate when exposed in extreme quantity can react with human tissue and causes similar effect as that of acid, it can also cause severe eye irritation on contact and possible burns, may cause chemical conjunctivitis and corneal damage. The objective of this study is to evaluate the ability of activated charcoal to retain Potassium Permanganate ions (K+ and MnO4-) through adsorption in an aqueous solution. On the laboratory scale length of unused bed and equilibrium concentration was found out keeping in mind various parameters like effect of temperature, effect of concentration of adsorbate and flow rate of adsorbate for the removal of KMnO4 ions from water. The isotherm data was verified with the Langmuir adsorption isotherm as well as Freundlich adsorption isotherm equations.

32-33

Authors: Chandan Kumar, Priyanka Gaur, Dr. Sandeep Bhattacharya

The wealth of latest data and knowledge relating to epigenetics obtained in recent years highlights a vibrant future for epigenetics research. It involves the integration of high-throughput sequencing technologies and the means to maintain and manipulate the large amount of data produced by sequencing epigenomes. As more epigenetic markers are associated with specific diseases and tools can be developed to diagnose patients and gauge the severity of disease. There is also great concern in therapeutic epigenetics many drugs, such as DNA methyltransferase inhibitors and histone deacetylase inhibitors are already used in cancer treatment. It is a very exciting time to study epigenetic, and this field of research has the potential to completely transform medicine and greatly improve human lives.