The Characteristics and Release of Diclofenac Sodium of Niosome System in Carbomer 940 Gel Base Preparation (Niosome System of Diclofenac Sodium-Span 60-Cholesterol with Molar Ratio 1:5 :5) Repository - UNAIR REPOSITORY

  

PROCEEDING

The International Conference on Pharmacy

and Advanced Pharmaceutical Sciences

  

Yogyakarta, Indonesia, 2009

Editors :

  

Pudjono

Hilda Ismail

Ronny Martien

Triana Hertiani

  

Ritmaleni Published by: Faculty of Pharmacy Universitas Gadjah Mada Sekip Utara, Yogyakarta, 55281, Indonesia

ISBN : 978-979-95107-7-8

First Edition, 2010

  

No part of this publication may be reproduced, stored in a retrieval system or

transmitted in any form or by any means, electronic, mechanical,

photocopying, recording or otherwise, without the prior written permission of

the publisher, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta,

Indonesia.

No responsibility is assumed by the publisher for any injury and/or damage to

persons or property as a matter of product liability, negligence or otherwise,

or from any use or operation of any methods, products, instructions or ideas

contained in the material herein.

  Printed in Yogyakarta, Indonesia

Preface from the Editor

  

The proceeding was produced based on papers and posters presented at the

international Conference on Pharmacy and Advanced Pharmaceutical Sciences, held in

Yogyakarta, Indonesia, 5 – 6 October 2009.

The proceeding clearly reflects broad interest; from there are participants coming from

all around the world. Many contributions on Pharmaceutical Sciences there are quite a

substantial number of papers on Pharmacist role in general. The papers presented file

into a broad spectrum in Pharmaceutical sciences including Pharmacology, Toxicology,

Analytical Chemistry and Drug Design, Drugs Synthesis, Formulation of Drugs,

Pharmacy Social, Pharmacoepidemy, Traditional Medicine Natural Product Chemistry

and Phytochemistry, etc.

In addition there are substantial numbers of paper deal with professional aspect of

Pharmacist in general health care.

  

In this an opportunity, I would like to express my appreciation to the editorial team of

the proceeding who have been working hard to review manuscripts, and making the

first edition of this proceeding be possible.

I would like also to thanks to all invited speakers and presenters who participated in

the International Conference on Pharmacy and Advanced Pharmaceutical Sciences and

your contribution to this proceeding.

Finally, I hope this proceeding will give contribution to the advanced scientific research

in the field of pharmaceutical sciences Yogyakarta, July 2010 Dr. rer. nat. Pudjono, SU., Apt.

  

Organizing Committee

Steering committee

  

Prof. Dr. Marchaban, DESS, Apt (Pharmacy, UGM, INDONESIA)

Prof. Dr. Umar Anggara Jenie, M.Sc.,Apt (LIPI, INDONESIA)

Prof. Dr. Retno S. Sudibyo, M.Sc.,Apt. (Pharmacy, UGM, INDONESIA)

Prof. Dr. Syed Azhar S. Sulaiman (USM, MALAYSIA)

  

Prof. Masashi Kawaichi, Ph.D (NAIST JAPAN)

Dr. Edy Meiyanto, M.Si., Apt (CCRC, UGM INDONESIA)

Prof. Dr. Zullies Ikawati, Apt (Pharmacy, UGM, INDONESIA)

  

Chairman

Dr. Hilda Ismail, M.Si., Apt.

  

Secretary

Dr. rer. nat. Ronny Martien, M.Si

  

Treasurer

Dr. Ratna Asmah S., M.Si., Apt

Scientific Committee Prof. Dr. Sismindari, SU., Apt

  

Prof. Dr. Lukman Hakim,M.Sc., Apt

Prof. Dr. Suwidjijo Pramono, Apt.

  

Prof. Dr. Suwaldi, M.Sc., Apt

Welcome Message From the committee

  Welcome to Yogyakarta

On behalf of the Scientific and Organizing Committees, it is a great pleasure for me to welcome

all participants to Yogyakarta, to the International Conference on Pharmacy and Advanced

Pharmaceutical Science 2009. th

  

The international conference is organized by the faculty of Pharmacy UGM to celebrate its 63

anniversary and the Lustrum XII of Gadjah Mada University, as a collaboration work between

the Faculty of Pharmacy UGM with the Nara Institute of Science and Technology (Japan) and

the Universiti Sains Malaysia (Malaysia). In this conference 15 lectures within the field of

Pharmaceutical Care and Advanced Pharmaceutical Science will be given by invited speakers.

Besides, 55 posters and 75 paper will be presented in the parallels presentation sessions.

Herewith, we express our gratitude to all speakers and presenter, who would like to share

their advance knowledge in this scientific event.

  

The Organizing Committee gratefully acknowledges the Nara Institute of Science and

Technology and the Universiti Sains Malyasia, for the nice collaboration in bringing forth this

conference. A special acknowledgment is addressed to the Rector of Gadjah Mada University

and the sponsors, for all supports that make this symposium possible. Furthermore,

personally, I want to express my deep appreciation to the members of the Organizing

Committee, for the good teamwork and their great effort given in the preparation for this

symposium.

Finally, I wish all participants a scientifically rewarding and an enjoyable meeting in Yogyakarta.

Chairman Dr. Hilda Ismail, M.Si., Apt.

Remark of the Dean Faculty Assalamu’alaikum wr. wb

  Distinguished ladies & gentlemen.

First of all, on be half of the Faculty of Pharmacy Universitas Gadjah Mada, I would like come

to all of you in Yogyakarta, thank you very much for your attention to come and to attend the

international Symposium on Pharmacy and Advanced Pharmaceutical Sciences. I hope we are

all in health condition.

  Ladies and gentlemen,

The symposium is organized by the Faculty of Pharmacy UGM in collaboration with the Faculty

of Pharmaceutical Sciences Universiti Sains Malaysia and the Nara Institute of Science and

Technology Japan, and held as part to celebrate the 63th anniversary of the Faculty of

Pharmacy UGM.

In the symposium , I hope we can communicate our recently information concerning social /

clinical pharmacy and pharmaceutical sciences. I hope the symposium will be very fruitfull,

very useful for all of us .

I addres special thanks to the plenary speakers both from domestic and aboard, the oral and

poster presenters, as well as to those who come just to know the development of clinical or

social pharmacy and pharmaceutical science. Your willingness to come , to communicate and

to share your experiences is highly appreciated.

  

Special thanks also I address to my colleague the Dean of Faculty of Pharmacy USM who has

been coordinating USM students to attend this symposium. The hope is not to set up

networking between the pharmacy students of USM and UGM.

Therefore, during almost whole day discussing scientific matter related to human health and

welfare, I hope we can make a wonderful opportunity to make a scientific closer relationship

while we enjoy the cultural performances of Yogyakarta presented by our pharmacy student.

Finally, I hope that this meeting will give benefits to all of us, and we may see each other again

in a similar event in the near future.

  I look forward to thank you all for attending this event.

  Wassalamu’alaikum wa rahmatullahi wa barakatuh, Dean of Faculty of Pharmacy UGM Prof. Dr. Marchaban, DESS., Apt.

Speech of the Senior Vice Rector For Education, Research and Community Services, Gadjah Mada University

Assalamu’alaikum wa rahmatulLahi wa barakatuh

  On behalf of the Rector, I would like to welcome all of you to our campus Gadjah Mada

University and to our home town Yogyakarta. It is a great honor for me and Gadjah Mada

University to host the Two-day International Conference on Pharmacy and Pharmaceutical

Sciences that is conducted by the Faculty of Pharmacy, Gadjah Mada University. The increasing

problems and new cases of some diseases in the world, both the infectious and the

degenerative diseases, have demanded the development of medical and pharmaceutical

sciences and technologies for supporting the developments of early detection methods of the

diseases, the accurate diagnoses, as well as the appropriate and effective medications or

therapy. Pharmaceutical Science and Technology have been developing very fast within recent

years. The development trend shows using much more biotechnological approach in both

diagnose establishment and medication administrations. For examples the usage of some

serums, enzymes, hormones, vaccines, etc., and their recombinant products. The science and

technology for finding prevention method against infectious diseases or degenerative diseases

now have been developing so amazing, for example the usage of growth hormones, vaccines,

and stem cells for it.

  Gadjah Mada University has been committed to become World Class University;

therefore international networking in education, research and publication is much needed. I

really support to this international conference on Pharmaceutical Science and Technology

which can keep us in touch with the state of the art of pharmaceutical science. I do believe

that by conducting this kind of international meeting, we can get and exchange new

information and best practices on pharmaceutical science and technology, and it is very

important to inspire our young researchers and enhance our research networking

internationally. In this occasion, I would like to express my great gratitude to all the guest

speakers and speakers, who have contributed their advanced presentations in this

international conference. I also would like to extend my gratitude to the Organizing Committee

from the Faculty of Pharmacy, Gadjah Mada University, who has already successfully arranged

this international conference. I would also thank to all institutions or companies who have

sponsored and supported this conference. Finally, have a fruitful conference and enjoy Yogyakarta. Thank you

Wassalamu’alaikum wa rahmatulLahi wa barakatuh

  Senior Vice Rector for Education, Research and Community Service Gadjah Mada University Prof. Dr. Retno Sunarminingsih, M.Sc., Apt.

CONTENTS Preface from the Editor

  i

  Organizing Committee

  ii

  Welcome Message Proceeding International Conference on Pharmacy and Advanced Pharmaceutical Sciences

  iii

  From the committee Remark of the Dean Facultyi

  v v

  Senior Vice Rector For Education CONTENT

  vi Pharmacogenetics : in case of cytochrome P450 oxidases (CYPS) related to adverse drug

  1

• – 4 reactions

  Arum Pratiwi, Harianto Lim and Ronny Martien

  Interaction of turmeric and garlic extract combination against free radical scavenging

  5

• – 6 activity

  Patonah, Daryono H. Tjahjono, Elin Yulinah S. and I Ketut Adnyana

  7 Influenced of Kojic Acid and Β-Cyclodextrin on SPF Value Sunscreen Product Contained – 14 Oxybenzone and Octyl Dimetyl Paba (3:7) (In vanishing cream base formulation)

  Diana, Tristiana Erawati, Widji Soeratri and Noorma Rosita

  Isolation and Antimicrobial activity of endophytic fungi Kabatiella caulivora var B isolated

  15

• – 17 from Alyxia reinwardtii BL

  Noor Erma Sugijanto, Dian Anggraeny and Noor Cholies Zaini

  Rapid and Simple Luciferase Reporter Gene Assays for the Discovery of Peroxisome

  18

• – 24 Proliferator-Activated Re ceptor α and γ Agonists and Nuclear Factor-κB Inhibitors from Medicinal Plants.

  N. Fakhrudin, S. Vogl, P. Picker, E. H. Heiss, J. Saukel, G. Reznicek, B. Kopp, A. G. Atanasov and V. M. Dirsch

  Identification of components of essential oil from Cananga odorata which penetrated into

  25

• – 29 the rat skin /(wistar strain) in the practice of Timung (development of Timung as alternative healing)

  Mangestuti Agil, Esti Hendradi and Budiastuti

  In Vivo Antihyperglycemic Test of Albedo Durian (Durio zibethinus M) Extract on Aloxan-

  30

• – 33 Induced Diabetic White Rat (Rattus norvegicus)

  34 Effect of Pasak Bumi’s Root (Eurycoma longifolia, Jack) on Sperm Output in Rats – 37

  Farida Hayati and Mustofa

  The Influence of Arbutin 3% and Sesame Oil (3,5,7 % w/w) on SPF Values of Oxybenzon and

  38

• – 43 Padimate O (3:7% w/w) in carbomer Gel Base

  Noorma Rosita, Tristiana Erawati and Rafi Jikrona

  44 Sulochrin as α -glucosidase inhibitor lead compound – 48

  Rizna Triana Dewi, Ahmad Darmawan, Sofna D.S Banjarnahor, Hani Mulyani, Marisa Angelina and Minarti

  The Practice of Complementary Indigenous Malay Ther

  49 apies In Rural Areas: Do Users’ – 54 Attitudes, Beliefs And Perceptions Significantly Differ From Non-Users?

  Pei Lin Lua, Rohayu Izanwati Mohd Rawi, Suffian Mohamad Tajudin, Norlida Mamat and Ahmad Zubaidi Abdul Latif

  An Interventional Pilot Study: Effect Of Dark Chocolate Consumption On Anxiety Level

  55

• – 62 Among Female Nursing Students

  Sok Yee Wong, Pei Lin Lua, Rohayu Izanwati Mohd Rawi, Rokiah Awang, Ahmad Zubaidi and Abdul Latif

  The Anti-proliferation Assay of Bioactive Fraction from Curcuma zedoaria Rhizome

  63

• – 67

  Ros Sumarny, Priyosoeryanto B. P., Ietje W., Latifah K. D. and Chairul

  Studies of Sub-acuteToxicity Assay from Acorus calamus L. in Experimental Animal Models

  68

• – 71

  Banjarnahor S.D.S, Sri Hartati and Megawati

  Antioxidant Properties and Phenolics Content of Mikania scandens L.(Wild)

  72

• – 77

  Sumi Wijaya, Ting Kang Nee, Khoo Teng Jin and Christophe Wiart

  The Influence of Olive Oil Addition on Increasing of Arbutin Penetration in the Carbomer-

  78

• – 81 940’s Gel (Observation on Inhibition of Enzyme Tyrosinase Activity)

  Widji Soeratri, Tristiana Erawati, Noorma Rosita and Fahriyatul Wahyuni

  The difference of antioxidant activity of various tea (Camellia sinensis L.) methanol extract

  82

• – 88

  Wahyu Widowati, Tati Herlina and Hana Ratnawati

  Chemical Stability of Cisplatin and Ondansetron During Simulation of hemotherapy

  89

• – 94 Administration

  Yahdiana Harahap, Rizka Andalusia and Armon Fernando

  The Effects of Cassava Starch (Manihot utilissima, Pohl.) as a Binder on Physicochemical

  95

• – 98 Characteristics of Acetaminophen Tablet Formulation

  Yandi Syukri, Tri Rahayu Ningsih and M. Hatta Prabawa

  Drug Interaction Study in Hospitalized Hepatic Cirrhosis Patient in Dr. Ramelan Navy

  99

• – 102 Hospital

  Amelia Lorensia, Aziz Hubeis, Widyati and Hary Bagijo

  The Effect of Cold Storage in Krebs-Henseleit Buffer in the Viability and Metabolic Activities 103

• – 110 of Precision Cut Intestinal Slices

  Dewi Setyaningsih, AA Khan and GMM Groothuis

  The Effect Of b-Cyclodextrin And Oxybenzone-Octyl Dimethyl Paba (3:7% W/W) Addition

  On The Penetration Of Kojic Acid In Vanishing Cream (Based on Activity Inhibition of Tyrosinase)

  Diana Winarita, Tristiana Erawati, Noorma Rosita and Widji Soeratri 111

• – 116 The profile of knowledge and self-medication in handling cough symptoms by students of pharmacy at Airlangga university

  Elida Zairina, Liza Pristianty and Lestriana Kusumasari 117

• – 120 The Characteristics and Release of Diclofenac Sodium of Niosome System in Carbomer 940 Gel Base Preparation (Niosome System of Diclofenac Sodium-Span 60-Cholesterol with Molar Ratio 1:5 :5)

  121

• – 128

  Esti Hendradi, Tutiek Purwanti, Bety Nurfia Puspitarini and Bianda Ida Kurnia

  Red Betel Vine (Piper Crocatum) Essential Oil as Antituberculosis 128

• – 133

  Farida Juliantina Rachmawaty

  134 Effect of Pasak Bumi’s Root (Eurycoma longifolia, Jack) on Sperm Output in Rats – 137

  Farida Hayati and Mustofa

  The Influence of Sesame Oil Addition on Arbutin Release from Carbomer-940 Gel Bases 138

• – 141

  Hanifa Rahma, Tristiana Erawati and Noorma Rosita

  Phytochemical Screening and Determination of Antioxidant Activity of Fractions from Ethyl 142

• – 145 Acetate Extract of Phyllanthus acidus (L.) Skeels Leaf

  Hindra Rahmawati, Hesty Utami and Moordiani

  Study on Antihyperglicaemic Activitiy of Ethyl Acetate Extract of Sidaguri (Sida rhombifolia 146

• – 152 L.) Stem onAlloxan-Induced Diabetic Mice (Mus musculus L.)

  Irma Ratna K, Muktiningsih, Suhartono, Natalia Elisabeht and Muhammad Ali Zulfikar

  The Influence of Arbutin and Olive Oil as an Enhancer in Characteristic and SPF Value of 153

• – 160 Sunscreen (Combination of Oxybenzone and Octyldimethyl Paba in Carbomer 940 Gel Base)

  Josephine Paramita Ayuningtyas, Tristiana Erawati, Noorma Rosita and Widji Soeratri

  The Effect of Secondary Emollients Triethylhexanoate, Isopropyl myristate, and 161

• – 165 Propyleneglycol Isostearate on in-vitro skin penetration of tocopheryl acetate cream using Franz-diffusion cell

  Joshita Djajadisastra, Sutriyo and Fraida Aryani

  Immunomodulatory activity of Plantago major L. on IgM titer of mice 166

• – 169

  Kartini, A. Kirtishanti, Dessy, Fauziah and Isnaini

  Antibacterial activities of Aleurites moluccana (Euphorbiaceae) 170

• – 178

  Othman Abd Samah and Rasyidah Mohamad Razar

  Total synthesis and revised structure of benzophenone glucopyranosides from phaleria 179

• – 185 macrocarpa

  Phebe Hendra, Yukiharu Fukushi and Yasuyuki Hashidoko

  Influence of Tween 80 Concentration in Carbomer/ Tween 80 Aggregate on Kojic Acid

  Penetration (Observed on Inhibiting Tyrosinase Activity in Vanishing Cream) 186

• – 191

  Siti Evi Jayanti, Tristiana Erawati and Noorma Rosita

  Validation for Result Degradation of Nifedipine Residue with Thin Layer Chromatography- Densitometry and Thin Layer Chromatography-Spectrophotometry 192

• – 195

  Sitti faika and Sudibyo Martono

  Synthesis and Biological Activity Test of Antibiotic UK-3 Analogues, 2-Hydroxynicotinyl- Butyl-Serine-Ester and Its Derivatives

  196

• – 198

  Ade Arsianti, Kiyomi Kakiuchi, Tsumoru Morimoto, M.Hanafi and Endang Saefudin

  Vitamin e content in the dragon fruit Established by high performance thin layer chromatography 199

• –densitometry
• – 204

  Any Guntarti and Warsi

  Drug interaction study in hospitalized hepatic cirrhosis patient in Dr. Ramelan navy hospital

  Amelia Lorensia, Aziz Hubeis, Widyati and Hary Bagijo 205

• – 208 PGV-1 inhibits G2M phase progression in WIDr colon cancer cell

  209

  

Endah Puji Septisetyani, Edy Meiyanto, Masashi Kawaichi and Muthi’ Ikawati – 212

  Proceeding International Conference on Pharmacy and Advanced Pharmaceutical Sciences The influence of oleic acid pre-treatment on transport of epigallocathecin gallat in green 213

• – 215 tea (Camellia sinensis, L) extract Across mice skin in vitro

  Nining Sugihartini, Achmad Fudholi, Suwidjiyo Pramono and Sismindari

  Development and Production of Anti Tuberculosis Fixed Dose Combinations (FDCs) 216 Barokah Sri Utami, Syamsul Huda, Nurliya Irfiani and Badrus S.

• – 218 The Characteristics and Release of Diclofenac Sodium of Niosome System in Carbomer 940 Gel Base Preparation (Niosome System of Diclofenac Sodium-Span 60-Cholesterol with 219
• – 224 Molar Ratio 1:5 :5)

  Esti Hendradi, Tutiek Purwanti, Bety Nurfia Puspitarini and Bianda Ida Kurnia

  The Characteristics and Release of Diclofenac Sodium of Niosome System in Carbomer 940 Gel Base Preparation (Niosome System of Diclofenac Sodium-Span 20-Cholesterol with 225

• – 231 Molar Ratio 1:5 :5)

  Esti Hendradi, Tutiek Purwanti, Anditasari and Srimaryati

  An Interventional Pilot Study: Effect Of Dark Chocolate Consumption On Anxiety Level Among Female Nursing Students

  232

• – 239

  Sok Yee Wong, Pei Lin Lua, Rohayu Izanwati Mohd Rawi, Rokiah Awang and Ahmad Zubaidi Abdul Latif

  240

• – 243 Antiemetics utilization in cancer patients with high emetogenic cytotoxic drugs in two govermental hospital in indonesia

  Dyah Aryani Perwitasari and Ana Hidayati

  244

  246

  

Th e Ch a r a ct e r ist ics a n d Re le a se of D iclofe n a c Sodiu m of N iosom e

Syst e m in Ca r bom e r 9 4 0 Ge l Ba se Pr e pa r a t ion ( N iosom e Syst e m of

D iclofe n a c Sodiu m - Spa n 6 0 - Ch ole st e r ol w it h M ola r Ra t io 1 :5 :5 )

  

Esti Hendradi* , Tutiek Purw anti, Bety Nurfia Puspitarini, Bianda I da Kurnia

Department of Pharmaceutics of Faculty of Pharmacy, Airlangga University, Surabaya,I ndonesia

  

Corresponding : esti_hendradi@yahoo.com

Abst r a ct

  The present st udy was designed t o det erm ine t he charact erist ics and release of diclofenac sodium of noisom e syst em in Carbom er 940 gel base preparat ion. The com posit ions of niosom e was diclofenac sodium , Span 60 and cholest erol 1: 5: 5. Diclofenac sodium non niosom e syst em was used as a cont rol. The evaluat ion included organolept ic, pH and sodium diclofenac released t est of each form ula. The result of drug ent rapm ent efficiency of t his syst em was 73.32 0.68% . The charact erist ics of gel preparat ion showed t hat niosom al syst em increases consist ency, decreases pH of diclofenac sodium gel and also showed sim ilar it y of diclofenac sodium release com pared wit h t hat cont rol. The rat e ( flux) of

  2 ½

  diclofenac sodium release in cont rol form ula was 71.49 3.96 g/ cm / m inut e and form ula of

  2 ½

  g/ cm t he niosom e syst em was 73.06 2.01 / m inut e . I t was analysed by st at ist ic program m ed SPSS 16.0 using independent - sam ple T- t est wit h degree of believed 95% ( = 0.05) . The result showed t hat t here was not a significant difference bet ween each form ula.

  Key words: diclofenac sodium , niosom e, Span 60, Cholest erol, flux released

I n t r odu ct ion

  Diclofenac sodium is NSAI D, t he drug causes gast ric irrit at ion and undergoes hepat ic first - pass m et abolism ( 40- 50% ) ( Ganiswara,1995) . Diclofenac sodium has log P 1.13 ( Budavari et al, 2001) , so it hydrophobic com pound and has sm all solubilit y in w at er and dist ribut ion in t he gel based not well. One of t he m et hods used t o increase dist ribut ion in t he gel based by m ade vesicle, niosom e ( Choi and Maibach, 2005) . Niosom e is well docum ent ed for t ransderm al drug delivery. Niosom e syst em is unilam ellar or m ult ilam ellar vesicle where in an aqueous solut ion is enclosed in highly ordered bilayer m ade up of nonionic surfact ant wit h or wit hout cholest erol and dicet yl phosphat e ( Bij u et al, 2006) . The recent st udy, t o im prove t he released of diclofenac, a niosom e com posed of Span 60, cholest erol was prepared. The fact or t hat influence on charact erist ics include size of noisom e vesicle, ent rapm ent efficiency ( Ep) and released was am ount , t ype of surfact ant ( HLB) and it cont ain of cholest erol ( Pat el, 2005) . The research of Shahiwala and Misra ( 20 02) , niosom e m ade from act ive com pound of Nim esulid and used Span 20 - cholest erol wit h m olar rat io 1: 3: 3 has given Ep 39,00 ± 0,001% , and using m olar rat io 1: 6: 6 t he value of Ep was 91,21 ± 0,010 % .

  I n t his st udy, t he influence of niosom e syst em was m ade from diclofenac sodium , Span 60 and cholest erol wit h m olar rat io 1: 5: 5 on preparat ion charact erist ics and released of diclofenac sodium from Carbom er 940 gel base was evaluat ed.

M e t h odology M a t e r ia ls

  Diclofenac sodium was obt ained as a gift sam ple from PT Dexa Medika, Carbom er 940 ( Noveon Asia Pacific Lt d, Hongkong) , Span 60 ( Sigm a) , Cholest erol ( Sigm a) , KCl ( E.Merck) , NaCl p.a ( E.Merck) , Na HPO .12 H O p.a ( E.Merck) , KH PO p.a. ( E.Merck) . t riet anolam in was

  2

  4

  2

  2

  4

  purchased from PT. Trist ar. Com pound was used w it hout m ent ion t he specificat ion was a pharm aceut ical grade.

  Pr e pa r a t ion a n d ch a r a ct e r iz a t ion of n iosom e

  The com posit ion of niosom e syst em showed in Table 1 and t he foem ulat ion of sodium diclofenac gel preparat ions showed in Table 2.

  Ta ble 1 . The com posit ion of noisom e syst em .

  

Com pou n d M ola r Ra t io Am ou n t in 2 0 gr a m pr e pa r a t ion

  Diklofenac Sodium 1 0.2002 g Span 60 5 1.3301 g Cholest erol 5 1.2201 g

• Chloroform

  10 m L Aqua free of CO - 9 m L

  2

• PBS pH 7.4

  6 m L Niosom es were prepared by using Reverse Phase Evaporat ion Technique ( REV) . The m olar rat io of diclofenac sodium , Span 60 and cholest erol is 1: 5: 5. Drug, non ionic surfact ant and Cholest erol were weighed as indicat ed in Table 1. Cholest erol and Span w ere dissolved in chloroform , diclofenac sodium in 9 m L aquadest t han m ixed and sonificat ion at t em perat ure 4- 5 C for 16 m inut es. The m ixt ure was added 6 m L PBS pH 7.4 ± 0.05 and sonificat ion again 12 m inut es. Than t he m ixt u re was r ot avapored at 40

  C, 200 m m Hg unt il

  o

  chloroform disappeared ( + 1.5 h) and t he end evaporat ed using wat erbat h at 60 C unt il 15 m inut es t o m ake t he concent rat ed suspension of niosom e syst em . The diclofenac sodium of niosom e syst em was analy zed for per cent drug ent rapm ent by spect rophot om et ric m et hod.

  The niosom e syst em t han adding t he Carbom er gel wit h t he com posit ion as indicat ed in Table 2. Table 2. The form ulat ion of diclofenacsodium preparat ion.

  Com pound Concent rat ion Cont rol Niosom e Syst em

• Diclofenac Sodium 0.2001 g Span 60
• 1.3602 g
• Cholest erol 1.2201 g PBS pH 7.4
• 6 m L - Chloroform 10 m L Aqua free of CO
• 2 9 m L

  Tot al am ount of cont rol com ponent

• 12.344 g * 12.852 g* * - Niosom wit h EP 75%

  Carbom er 940 0.1000 g 0.1000 g TEA

  0.2 m L 0.2 m L Tot al am ount of t he cont rol aft er concent rat ed *

• Tot al am ount of niosom e syst em

  

D e t e r m in a t ion of t h e e n t r a pm e n t e fficie n cy of diclofe n a c sodiu m in t h e n iosom e

sy st e m .

  The ent rapm ent of diclofenac in t he niosom e syst em was calculat ed using equat ion 1:

  Ct  Cf    

  Ep ( % ) = x 100% ...........( 1)

  Ct  

  where, Ep : diclofenac sodium ent rapm ent in t he niosom e syst em Cf : concent rat ion of diclofenac free ( un ent rapped) Ct : t ot al concent rat ion of diclofenac sodium in t he form ulat ion of niosom e syst em .

  D e t e r m in a t ion of pH on t h e for m u la t ion

  The pH of preparat ion was done by m ixed t he preparat ion in t he aqua free of CO in

  2 rat io 1: 9. Mix well and t han t he pH of preparat ion was m easured using pHm et er.

  D e t e r m in a t ion of diclofe n a c r e le a se d fr om t h e pr e pa r a t ion .

  Perm eat ion st udy was perform ed apparat us 5 paddle over disk com plet ely wit h diffusion cell ( Figure 1) at 37C for 6 h. As a m em brane was cellophane and as donor com part m ent was filled by preparat ion of niosom e syst em in Carbom er 940 gel. As recept or solut ion was phosphat e buffer saline pH 7.4. At t he appropriat e t im e sam ple was t aken from recept or solut ion.

  A : Diffusion cham ber cont ain PBS pH 7.4 B : Paddle C : Dist ance from paddle t o diffusion m em br ane D : Diffusion cell E : Ther m om et er F : Sam ple holder Figu r e 1 . Apparat us 5- paddle Over Disk ( The USP Convent ion, 2002)

  Diclofenac concent rat ion of sam ple solut ion was m easured using Spect rophot om et er. Released of diclofenac sodium was calculat ed using equat ion 2 ( Higuchi, 1959) .

  q 1/ 2

  Q= = [ Dt ( 2A- Cs) Cs ] ...................( 2)

  x

  where, Q : flux of drug released D : coefficient diffusion of dr ug in t he based A : concent rat ion of drug in t he based Cs : solubilit y of drug in t he based t : t im e

  Re su lt s a n d D iscu ssion s The m orphology of niosom e syst em showed at t he figure 2 and 3.

  Figure 2. Morphology of noisom e syst em using light m icroscope ( Olym pus BX 41) wit h m agnify 1000X.

  Figure 3. Morphology of niosom e syst em using Scanning Elect ron Microscope ( Jeol t ipe JSM T- 100) wit h m agnify 2000X.

  The percent ent rapm ent of diclofenac sodium in t he niosom e syst em was shown at t he Table 3. Table 3. The ent rapm ent efficient ( Ep) of diclofenac sodium in niosom e syst em

  Replicat ion % Ep Mean ± SD

  74.60 I

  75.14 I I 75.32± 0.68

  76.23 I I I The organolept ic of Carbom er gel of diclofenac preparat ion showed in Table 4. Table 4.. The organolept ic of diclofenac sodium in Carbom er gel preparat ions.

  Observat ion Form ula

  Consist ency Color Sm ell Cont rol Fluidit y Whit e No sm ell Niosom e Syst em Sm oot h and Viscous Whit e Specific The pH value of f diclofenac in Carbom er 940 preparat ions were shown at Figure 4.

  Based on t he st at ist ical result of t he pH using independent T- t est t hat found t he t calculat ed ( 2,980) > t t abel ( 2,776) , it m eans t here was significant different bet ween cont rol and niosom syst em preparat ion.

  

Figu r e 4 . The pH value of diclofenac in Carbom er 940 preparat ions. Dat a were t he m ean of

t hree replicat ions  SD.

  Flux is t he m ost useful index t o evaluat e t he released of drug. The cum ulat ive am ount of drug released was plot t ed as funct ion of root t im e. From t he result of linear regression of st eady st at e condit ion I get flux at t he slope.

  Figure 5. The profile of diclofenac released from t he Carbom er 940 gel preparat ions. Dat a was t he m ean of t hree replicat ions  SD.( : Cont rol;  Niosom e Syst em ) .

  As shown in t he Figure 5, t he released profile shows t he sufficient linearit y wit h t he coefficient r was  0.98. Flux released of diclofenac sodium from Carbom er 940 gel base shown in Figure 6. I n t his Figure shown t hat t he flux released of diclofenac from preparat ion of niosom syst em diclofenac sodium : Span 60 : cholest erol wit h m olar rat io 1: 5: 5 in Carbom er 940 gel base was insignificant ly different com pared wit h t hat of cont rol. I t caused t he niosom e syst em t hat used in t he form ulat ion was wit hout separat ed t he ent rapm ent and not ent rapm ent . So t he profile was sim ilar. Beside t hat m aybe it caused t he experim ent was done only unt il 6 hours.

  Figure 6. Flux released of diclofenac from Carbom er 940 gel base. Dat a was t he m ean of t hree replicat ions  SD.

  From t he result s of t he experim ent we suggest t hat t he experim ent m ust done longer t han 6 hours and t he vesicle of niosom e is separat ed from diclofenac sodium t hat is not ent rapm ent in t he vesicle.

  As shown in t he Figure 5, t he released profile shows t he sufficient linearit y wit h t he coefficient r was  0.98.

Con clu sion

  The conclusions of t he experim ent were: 1. The drug ent rapm ent efficiency ( Ep) of t he niosom e syst em was 73.32  0.68% .

  2. The charact erist ics of gel preparat ion showed t hat niosom al syst em increase d consist ency, decreased pH of diclofenac sodium gel.

  3. The flux of diclofenac sodium release in cont rol form ula was 71.49 3.96

  2 ½

  g/ cm / m inut e and form ula of t he niosom e syst em was

  2 ½

  73.062.01g/ cm / m inut e . The st at ist ic result of t he flux of diclofenac released showed t hat t here was not a significant difference bet ween each form ula.

Re fe r e n ce s

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  t h

  Budavari, S., 1996. The Merck I ndex 12 . USA: Mer ck & CO., I NC. p. 521 Choi, M. J., Maibach, H. I ., 2005. Liposom es and Niosom es as Topical Drug Delivery Syst em s, Skin Pharm acology and Physiology 2005, J. of Pharm acol. and Biophis.

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  Ganiswarna, S. G., 1995. Farm akologi dan Terapi, Edisi I V, Jakart a: Bagian Farm akologi FKUI , hal. 207- 210, 218. Higuchi, T., 1959, Physical Chenical Analysis of Percut aneous Absorpt ion Process From

  Cream s and Oint m ent s. Pr esent ed Sept em ber 23 - 24, 1959, Sem inar, New York Cit y.

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