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Editorial Board Yohei Kawasaki

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Research & Reviews: A Journal of Pharmaceutical Science

Contents

1. Titrimetric and Spectrophotometric Assay of Diethylcarbamazine Citrate in Pharmaceuticals using Permanganate as Oxidant Nagib A.S. Qarah, K. Basavaiah

1

2. Colloidosomes: An Inherent Rigid Vesicle with Controlled Drug Distribution Vivek P. Chavda, Moinuddin M. Soniwala, Jayant R. Chavda

12

3. Alcoholic and Aqueous Extract of Eucaluyptus Globules Posses Antimicrobial Activity and Antifungal Property Confined only to Alcoholic Extract Pushpaveni C., Rekha S., Iswar Hazarika, Vineeth Chandy

26

4. Factors Affecting Implementation of Pharmaceutical Care at Jimma University Specialized Hospital, South West Ethiopia Gebremichael Tesfay, Shibiru Tesema, Eliyas Kadi Abafita

30

5. High-Performance Liquid Chromatographic Assay of Nateglinide and its Stability Study K. Basavaiah, N. Rajendraprasad, K.B. Vinay

41


Research & Reviews: A Journal of Pharmaceutical Science ISSN: 2229-7006(online) Volume 7, Issue 3 www.stmjournals.com

Titrimetric and Spectrophotometric Assay of Diethylcarbamazine Citrate in Pharmaceuticals using Permanganate as Oxidant Nagib A.S. Qarah, K. Basavaiah* Department of Chemistry, University of Mysore, Manasagangothri, Mysore, Karnataka, India Abstract

Two titrimetric and one spectrophotometric methods are described for the determination of diethylcarbamazine citrate in bulk drug and dosage forms using permanganate as an oxidimetric agent. In method A, the drug solution in H 2SO4 is titrated directly at 80°C to a pink end-point. DEC was treated with a measured excess of standard permanganate in H 2SO4 medium, and after a contact time of 5 min, the residual oxidant back titrated with ammonium ferrous sulphate to a colorless end-point (method B). Spectrophotometry is based on the measurement of the unreacted permanganate at 550 nm after the reaction between DEC and permanganate in H2SO4 medium is ensured to be complete (method C). In all methods, the amount of permanganate reacted was related to the amount/concentration of DEC. Experimental variables associated with the assay were carefully examined and optimized for better performance characteristics. Both the titrimetric methods are applicable over 1–10 mg range and the reaction follows 1:3 and 1:4 (DEC:KMnO 4) stoichiometry in direct and indirect methods, respectively. In spectrophotometry, Beer's law is obeyed in the inverse manner, and linearity is observed in the range 2.5–30 µg ml-1 with a molar absorptivity value of 8.03×103 l mol-1 cm-1. The limits of detection (LOD) and quantification (LOQ) were calculated to be 0.12 and 0.35 µg ml-1, respectively. The methods were validated for precision and accuracy, robustness and ruggedness and selectivity. The methods were applied to the determination of DEC in tablets and suspension with satisfactory results. The accuracy of the methods was also assessed by recovery study via standard-addition procedure. Keywords: Diethylcarbamazine citrate, assay, titrimetry, spectrophotometry, permanganate, pharmaceuticals

INTRODUCTION

The World Health Organization (WHO) has called for an effort to eliminate lymphatic filariasis (LF) around the world [1]. A nematode worm (Wuchereria bancrofti) is the cause of 90% of lymphatic filariasis cases globally. Mosquito bites transmit larval nematodes (microfilariae) present in the blood stream of infected persons, and although the adult nematodes are resistant to medical treatment, human transmission in endemic regions can be stopped by administering drugs, such as Diethylcarbamazine (DEC) (Figure 1), that kill the microfilariae. DEC has had a long history of safe use in mass drug administration (MDA) LF eradication programs [2–4], and so far, W. bancrofti do not appear to have developed resistance to DEC [5, 6]. A course of treatment of 6 mg/kg per day of DEC citrate

for 12 days (daily dose around 300 mg) can significantly reduce the microfilariae count in an infected person. However, in regions where the disease is endemic, yearly drug administration to infected individuals must be continued over the adult worm lifetime of 4– 6 years to eradicate the disease. As an alternative to pill-based MDA, DEC can be administered to local populations in the form of medicated cooking salt, with DEC citrate present at 0.2–0.4% w/w, which corresponds to a daily dose of 20–40 mg DEC citrate. Local production and distribution of medicated salt fortified with DEC has proved to be a particularly effective method [7, 8] for eradicating LF from endemic regions [9, 10]. In view of its pharmaceutical importance, considerable work has been done for its

RRJoPS (2016) 1-11 © STM Journals 2016. All Rights Reserved

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Research & Reviews: A Journal of Pharmaceutical Science ISSN: 2229-7006(online) Volume 7, Issue 3 www.stmjournals.com

Colloidosomes: An Inherent Rigid Vesicle with Controlled Drug Distribution Vivek P. Chavda*, Moinuddin M. Soniwala, Jayant R. Chavda Department of Pharmaceutics, B.K. Mody Government Pharmacy College, Rajkot, Gujarat, India Abstract

Colloidosomes are hollow capsules whose shell is composed of closely packed uniform colloidal particles. To date, colloidosomes have been fabricated using colloidal assembly at liquid-liquid interfaces. This system also solves the problem of insolubility, instability, rapid degradation and widely used in specialized areas like protein delivery, gene delivery, targeting to brain, tumour targeting, etc. In the series of vascular systems, colloidosome is the advanced tool in drug delivery. Colloidosomes have a great, encapsulation efficacy with a wide control over size, permeability, mechanical strength and compatibility. Moreover, the release of larger encapsulated materials from such traditional colloidosomes relies on external triggers such as, changes in osmotic pressure or mechanical forces to crush or break open the capsule; this precludes precise control of the release response. These limitations highlight the need for a flexible technique to fabricate colloidosomes that enables both, control of the permeability to small species and a high degree of sensitivity to a release trigger. The types, properties, fabrication techniques, characterization and recent works on colloidosomes are compiled in this work. Keywords: Colloidosomes, core materials, emulsion droplets, fused colloidal particles, microcapsules

INTRODUCTION

Delivery systems are designed to protect an incorporated drug from the environment during delivery and to provide a controlled release. The goal may be either to deliver a drug locally to specific sites in the body or to prepare a drug carrier system that acts as a reservoir at the site of injection over a certain time period [1]. In recent years, a growing number of potential drugs, peptides and protein drugs have been discovered. Unfortunately, protein drugs are subjected to numerous chemical and physical instability mechanisms and rapid enzymatic degradation, while drug molecule has solubility and permeability issues; therefore, they often show low bioavailabilities and have short in vivo half-lives, thus necessitating parenteral delivery [2]. To sustain therapeutic effects, these drugs have to be administered by infusion or via frequent injections. It is obvious that there is an urgent need for suitable delivery systems capable of preserving protein stability and improving administration frequencies, and thus lessening the strain on patients. Particulate drug carriers that have been investigated for this purpose are: oil/water (o/w) emulsions, liposomes,

microparticles, and nanoparticles based on synthetic polymers or natural macromolecules [3]. Use of synthetic materials, however, often goes along with biocompatibility problems, residual solvents, and detrimental effects on the incorporated drug during the manufacturing procedure or during polymer degradation after application [4]. Therefore, alternative carrier substances have been investigated in recent years. Among them, lipidic materials have garnered growing attention. Successful drug or protein incorporation and delivery has been reported for liposomes [5], multivesicular liposome preparations [6], cubic phase gels [7], hollow lipid microparticles [8], hollow lipid microcylinders [9], microparticles [10], and solid lipid nanoparticles (SLN) for intravenous applications [11].

RRJoPS (2016) 12-25 Š STM Journals 2016. All Rights Reserved

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Research & Reviews: A Journal of Pharmaceutical Science ISSN: 2229-7006(online) Volume 7, Issue 3 www.stmjournals.com

Alcoholic and Aqueous Extract of Eucalyptus globulus Posses Antimicrobial Activity and Antifungal Property Confined only to Alcoholic Extract 1

Pushpaveni C.1, Rekha S.2, Iswar Hazarika1,*, Vineeth Chandy2

Department of Pharmacology, T. John College of Pharmacy, Gottigere, Bannerghatta Road, Bangalore, Karnataka, India 2 Department of Pharmaceutical, T. John College of Pharmacy, Gottigere, Bannerghatta Road, Bangalore, Karnataka, India

Abstract

Alcoholic and aqueous extract of leaves of Eucalyptus globulus was studied for in vitro for its antimicrobial and antifungal activity. The study was done against gram-positive bacteria (Staphylococcus aureus), gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and fungus (Candida albicans). The evaluation was done by determining its inhibition zone. Result demonstrated that alcoholic extract has broad spectrum antibacterial and antifungal activity on gram-positive bacteria, gram-negative bacteria and fungus, whereas the aqueous extract has only broad spectrum antibacterial activity. Our study confirms the antibacterial and antifungal property of E. globules. Keywords: Eucalyptus globules, anti-bacterial, amoxicillin, ciprofloxacin

INTRODUCTION

Resistances of microorganism towards conventional antimicrobial agents are a serious problem worldwide. This necessitates the search of a novel chemical agent which can substitute the conventional antimicrobial agents. Eucalyptus globules (Family: Myrtaceae) is a tall and evergreen tree native to Australia and Tasmania but successfully introduced worldwide including India [1–4]. It is one such plant which symbolizes all that is wondrous in nature because, the whole plant has been used as traditional medicine for household remedy against various human ailments from antiquity. Although, it is native to Australia, its therapeutic effect have been introduced and integrated into traditional system of medicine of India, China and Greco-Europe. In India, it is described in Ayurveda for more than 1250 preparations containing eucalyptus oil [5]. Many amongst these preparations have been successfully used in various infectious conditions. Eucalyptus oils have a history of wide application including pharmaceutical use. Moreover, report suggests that it has

antibacterial effect but proper scientific evidence is missing. Hence, the aim of our study was to investigate the antimicrobial activity of Eucalyptus globules extracts on some microbial stains.

MATERIALS AND METHODS

Plant Materials The fresh leaves of Eucalyptus globulus were collected on October 2014 from the local areas of Bangalore, India. The sample was authenticated in the research and development laboratory of Natural Remedies Pvt. Ltd., Bangalore of Karnataka State, India, by comparing the sample with authentic sample. A voucher specimen has been preserved at the laboratory for further reference. The collected fresh leaves of E. globulus were air dried over a period of two weeks and the air-dried leaves were grinded into powder. Extract Preparation Alcoholic Extract About 50 g of dried plant material were extracted with 200 ml of solvent (in the ratio of 9:1 ml distilled methanol: water respectively). The leaves were completely

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Research & Reviews: A Journal of Pharmaceutical Science ISSN: 2229-7006(online) Volume 7, Issue 3 www.stmjournals.com

Factors Affecting Implementation of Pharmaceutical Care at Jimma University Specialized Hospital, South West Ethiopia Gebremichael Tesfay, Shibiru Tesema, Eliyas Kadi Abafita* School of Pharmacy, College of Health Sciences, Jimma University, Ethiopia Abstract

Pharmaceutical care is the responsible provision of medicine therapy for the purpose of a definite outcome that improves a patient’s quality of life. It is a necessary element of healthcare and the concept implies the active participation of the patient in medicine therapy decisions and, the cooperation of healthcare providers across disciplines. This study was conducted to explore factors that affect the implementation of pharmaceutical care at Jimma University Specialized Hospital (JUSH). A prospective cross-sectional study with semistructured self-administered questionnaire was conducted and complete survey technique was used for pharmacists working at JUSH and pharmacy post-graduate students. Fifty nine questionnaires were retrieved from the respondents that make the response rate around 89.39%. Significantly more than half of the respondents (69.49%) were male and slightly more than half (55.93%) were able enough to communicate through both Amharic and Afan Oromo. Lack of space and inappropriate layout within the pharmacy was found to be the strongest challenging factor for pharmaceutical care implementation at JUSH with 50.85 and 33.89% strongly agree and agree, respectively. Even though, the feasibility of pharmaceutical care in Ethiopia health system has been assured in previous studies, it is not well implemented at JUSH yet and is found in its early stage. Lack of space, trained personnel and time were identified in this study as inhibiting factors and therefore, enough and appropriate space and, sufficient pharmacists should be employed and freed to a greater extent from performing routine tasks which could be delegated with supervision to train supportive personnel, thereby expanding professional pharmacy service. Keywords: Pharmaceutical care, Implementation, Barrier, Jimma University Specialized Hospital

INTRODUCTION

Pharmaceutical Care (PC) is widely understood as "the direct, responsible provision of medication-related care to achieve definite outcomes intended to improve the patient's quality of life”. The principal elements of PC are that it is medication related; it is care that is directly provided to the patient by pharmacist in collaboration with the patients and healthcare professionals [1]. This role requires pharmacists to apply a higher level of drug knowledge, clinical skill, and independent judgment to their work which involves designing, implementing and monitoring a therapeutic plan. The care provided is to produce definite outcomes; these outcomes are intended to improve the patient’s quality of life; and the pharmacists

who practice PC have accepted personal responsibility for their patients’ outcomes. These therapeutic outcomes are: cure of a disease, elimination or reduction of a patient’s symptoms, arresting or slowing a disease process or symptoms [2, 3]. Most of the literatures available on the evaluation of PCSs, and identified numerous barriers that impede its implementation were conducted in developed countries [4, 5]. Despite the fact that the clinical, economic and humanistic viability of PC is even more essential in resource limiting settings, there is a lack of information in relation the implementation, and its challenges, of PCSs in developing (particularly in Africa) countries and its value too [7, 8]. Although PC concept

RRJoPS (2016) 30-40 © STM Journals 2016. All Rights Reserved

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Research & Reviews: A Journal of Pharmaceutical Science ISSN: 2229-7006(online) Volume 7, Issue 3 www.stmjournals.com

High-Performance Liquid Chromatographic Assay of Nateglinide and its Stability Study K. Basavaiah1,*, N. Rajendraprasad2, K.B. Vinay3

1

2

Department of Chemistry, University of Mysore, Manasagangothri, Mysuru, Karnataka, India PG Department of Chemistry, JSS College of Arts, Commerce and Science, B.N. Road, Mysuru, Karnataka, India 3 Jubilant Generics Ltd., Nanjanagudu, Mysuru, Karnataka, India

Abstract

Nateglinide (NTG) is a D-phenylalanine derivative used in the treatment of type-2 diabetes mellitus. An accurate, sensitive and reproducible high-performance liquid chromatographic (HPLC) method has been developed and validated for the quantification of NTG in pharmaceutical samples. The drug was eluted from Inertsil ODS 3V (150×4.6 mm; 5 µm particle size) column at 30°C with a mobile phase consisting of phosphate buffer of pH 3.3 and methanol (70:30 v/v). The flow rate was 1 mlmin-1 and the UV detector was set at 210 nm to monitor the effluent. The retention behaviour of NTG as a function of mobile phase pH, composition and flowrate was investigated. Quantification was achieved by the measurement of mean peak area and the calibration curve was linear (r=0.9998) over the concentration range, 1–300 µg.ml-1. Limits of detection (LOD) and quantification (LOQ), calculated as per ICH guidelines, were 0.1 and 0.3 µg.ml-1, respectively. Intra-day and inter-day precisions expressed as RSD were <1% and the corresponding accuracies were better than 1.2% (RE). The method was also validated for robustness, ruggedness and selectivity. The method was applied to the determination of NTG in commercial tablets and the results agreed well with the label claim and those obtained by the reference method. Accuracy was also assessed by recovery test via standard-addition procedure. As part of degradation study, drug was subjected to forced degradation via acid- and base- hydrolysis, oxidation, thermolysis and photolysis, and the results revealed that the drug was degraded completely under oxidative stress condition and partly under base-induced stress condition. The drug remained intact when subjected to other stress conditions. Keywords: Nateglinide, determination, HPLC, pharmaceuticals, stress-testing

INTRODUCTION

Nateglinide (NTG), chemically known as [N(trans-4-isopropylcyclohexyl carbonyl)-Dphenylalanine] (Figure 1) [1], is a Dphenylalanine derivative lacking either a sulphonylurea or benzamido moiety and is a novel oral meal-time glucose regulator and has been approved for the treatment of diabetes mellitus [2, 3]. This meglitinide derivative works by stimulating the pancreas to release insulin by closing the ATP-dependent potassium channels. The resulting influx of calcium induces insulin secretion. It is rapidly and completely absorbed from the gastrointestinal tract and peak plasma concentration reaches at 0.5– 1.0 h. It is metabolized by cytochrome P-450

system to inactive metabolite and eliminated with half-life of 1.4 h [4].

Fig. 1: Structure of NTG. The medicinal value of NTG has prompted many researchers to develop methods for its determination in body fluids as a part of

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