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

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The Anti-proliferation Assay of Bioactive…………

Proceeding International Conference on Pharmacy and Advanced Pharmaceutical Sciences 63

PROCEEDING

The International Conference on Pharmacy

and Advanced Pharmaceutical Sciences

Yogyakarta, Indonesia, 2009

Editors :

Pudjono

Hilda Ismail

Ronny Martien

Triana Hertiani

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Proceeding International Conference on Pharmacy and Advanced Pharmaceutical Sciences Yogyakarta, Indonesia, 2009

64

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.

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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

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Proceeding I nternational Conference on Pharmacy and Advanced Pharmaceutical Sciences Yogyakarta, I ndonesia, 2009

ii

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.

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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.

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

th

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

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iv

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

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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

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

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65

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: [email protected]

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

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

I n t r odu ct ion

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.

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Esti Hendradi, et al.

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 . 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

Table 2. The form ulat ion of diclofenacsodium preparat ion.

Com pound Concent rat ion

Carbom er 940 0.1000 g 0.1000 g

TEA 0.2 m L 0.2 m L

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123

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:

Ep ( % ) =















Ct

Cf

Ct

x 100% ...( 1)

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 CO2 in 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

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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=

x

q

= [ Dt ( 2A- Cs) Cs ]1/ 2_{...( 2)} 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.

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125 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

I 74.60

75.32± 0.68

I I 75.14

I I I 76.23

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.

Form ula Observat ion

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.

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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.

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127

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

g/ cm2/ m inut e½ and form ula of t he niosom e syst em was 73.062.01g/ cm2/ m inut e½. 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

Bij u, S.S., Talegaonkar S., Mishr a P.R. And Khar R.K., 2006. Vesicular Syst em s: An Overview. I ndian J. Pharm Sci,68 ( 2) : 141- 153

Budavari, S., 1996. The Merck I ndex 12t h. 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. Res., Vol. 18, No.5, p.209- 219.

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.

Pat el, Rakes P., 2005. Niosom e : An Unique Drug Delivery Syst em, ht t p: / / pharm ainfo.net. Tanggal akses 11 Novem ber 2008