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Journal : INDONESIAN JOURNAL OF PHARMACY

SUN PROTECTOR FACTOR (SPF) IN VITRO AND THE PHYSICAL STABILITY OF O/W CREAM OPTIMAL FORMULA FROM THE PARTITION PRODUCT OF MAHKOTA DEWA LEAVES [Phaleria macrocarpa (Scheff) Boerl] Zulkarnain, Abdul Karim; Marchaban, Marchaban; Wahyuono, Subagus; Susidarti, Ratna Asmah
Indonesian Journal of Pharmacy Vol 26 No 4, 2015
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1137.832 KB) | DOI: 10.14499/indonesianjpharm26iss4pp210

Abstract

The leaves Mahkota dewa (Phaleria macrocarpa (Scheff) Boerl) contains a benzophenoic glycoside (Phalerin) which is active for sun screen. Some formula and designed on the Simplex Lattice Design (SLD) method then its physical characteristics were investigated. The physical characteristics will be used to determine the optimum formula. In present study, the optimum formulation was evaluated to determine chemical stability and the in vitro SPF. The doses of partition product of P. macrocarpa was used 6%. The optimal formulation cream was determined by SLD version 9.0.1 with variety of Cetyl alcohol, mineral oil, and Tween 80. The difference of physical characteristics between experimental and software was analyzed using T-test, P= 95 %. The physical stability and in vitro SPF of the optimum formula was observed. he study exhibits that the combination of cetyl alchodol 9,71%, mineral oil 29%, and tween 80 3,29% was the optimum formula of o/w cream with the desirability test 0,924. The T-test result test shows that there is no significant difference (p>0.05) on physical characteristics between experimental and software prediction. During the storage, the viscosity, spread ability, adhesive ability, separation volume ratio of cream was relatively stable however the stability started to decline on the week IV in the extreme temperature. The SPF of the cream of the CFR, CPHR and CBZP partition were 21,32; 33,12 and 42,49, respectively.Keywords: Mahkota dewa, cream, optimum, SPF
Preparation and antibacterial activity of p-Anisyl ethyl fumarate and ethyl n-phenyl fumaramate ., Jumina; Zulkarnain, Abdul Karim; Mulyono, Panut
Indonesian Journal of Pharmacy Vol 16 No 2, 2005
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (189.073 KB) | DOI: 10.14499/indonesianjpharm0iss0pp116-123

Abstract

In order to generate potent C-9154 antibiotic derivatives, it has been conducted the synthesis and antibacterial activity evaluation of p-anisyl ethyl fumarate and ethyl N-phenyl fumaramate. These target molecules were chosen as the former would be a para-methoxy substituted C-9154 derivative, whereas the latter would be an example of unsubstituted C-9154 derivative bearing an amido-ester fumaric side chain.p-Anisyl ethyl fumarate was synthesized from p-anisaldehyde by reduction with NaBH4, condensation of p-anisyl alcohol with maleic anhydride, and esterification of the resulting p-anisyl maleic acid with ethanol in the presence of benzenesulfonic acid as the catalyst. These reactions gave satisfactorily yields (55-81 %) in all steps involved. In the case of ethyl Nphenyl fumaramate, this molecule was synthesized in 84 % yield through condensation of aniline with maleic anhydride, followed by esterification with ethanol in the presence of concentrated sulfuric acid.The antibacterial activity test showed that the minimum inhibition concentration (MIC) of p-anisyl ethyl fumarate and ethyl N-phenyl fumaramate towards Staphyllococcus aureus were 15 and 25 μg/mL. Interestingly, the MIC values of these two compounds towards Eschericia coliwere also 15 and 25 μg/mL respectively. Thus, the data showed that the two C-9154 derivatives obtained are sufficiently potent and possess antibacterial activities which are comparable to the antibacterial activity of C-9154 itself towards Staphyllococcus aureus (12.5 – 37.5 μg/mL) and Eschericia coli (25 – 50 μg/mL).Key words: synthesis, antibacterial activity, fumarate and fumaramate.
SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF C-9154 ANTIBIOTIC DERIVATIVES FROM VANILLIN ., Jumina; Siswanta, Dwi; Zulkarnain, Abdul Karim
Indonesian Journal of Pharmacy Vol 12 No 2, 2001
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (68.404 KB) | DOI: 10.14499/indonesianjpharm0iss0pp85-91

Abstract

This research was conducted in order to synthesize two derivatives of C-9154 antibiotic from vanillin and to evaluate their biological activities. The synthesis of these C-9154 derivatives was performed through alkylation of vanillin, preparation of the corresponding benzaldoxim, reduction of this benzaldoxim, treatment of the resulting substituted benzilamine with maleic anhydride and esterification of this C-9154 antibiotic derivative. The alkylation of vanillin was carried out using diethylsulfate and NaOH as the base to give 89% yield of ethyl vanillin. The oxim synthesis from ethyl vanillin was performed using hydroxylamine hydrochloride under alkaline condition at 50oC for 2 hours to yield 89% 4-ethoxy-3-methoxybenzaldoxim. Reduction of this benzaldoxim with metallic Na in absolute ethanol afforded 82% yield of 4-ethoxy-3-methoxybenzylamine. This benzylamine derivative was then reacted with maleic anhydride in benzene to give the acid-form of C-9154 antibiotic derivative (6) in 74% yield. Esterification of this acid conducted Jumina using absolute ethanol in the presence of concentrated sulfuric acid at reflux for 4 hours gave the ethyl ester-form of C-9154 antibiotic derivative (7) in 87% yield. Antimicrobial activity evaluation was conducted using Staphyllococcus aureus and Eschericia coli. Based on the minimum inhibition concentration (MIC) data determined using aqueous methanol as the reference, it was observed that the acid-form (6) and the ethyl ester-form (7) of C-9154 antibiotic derivative obtained respectively gave MIC values of 2000-3000 g/ml and 500-1000 g/ml respectively either towards Staphyllococcus aureus or Eschericia coli.Key words: antibiotics, vanillin, oxim, benzylamine, C-9154 derivative, antimicrobe.
SYNTHESIS AND ANTIMICROBIAL ACTIVITY EVALUATION OF ETHYL SALICYL FUMARATE AND ETHYL FURFURYL FUMARATE Jumina .; Iqbal Tahir; Abdul Karim Zulkarnain
Indonesian Journal of Pharmacy Vol 13 No 4, 2002
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (118.116 KB) | DOI: 10.14499/indonesianjpharm0iss0pp207-214

Abstract

This research was conducted in order to synthesize and investigate the antimicrobial activity of ethyl salicyl fumarate and ethyl furfuryl fumarate. These two target molecules were chosen as the former is the derivative of C-9154 antibiotic containing phenolic hydroxyl group, whereas the latter is an example of C-9154 antibiotic derivative bearing furan ring instead of benzene.Ethyl salicyl fumarate was synthesized from methyl salicylate through reduction with LiAlH4, condensation of salicyl alcohol with maleic anhydride, and esterification of salicyl maleic acid with ethanol in the presence of benzenesulfonic acid as the catalyst. These reactions gave satisfactory yields (76-92 %) in all steps involved. Similar to this procedure, ethyl furfuryl fumarate was prepared from furfural through reduction with NaBH4 followed by condensation of the resulted furfuryl alcohol with maleic anhydride and esterification of furfuryl maleic acid with ethanol in the presence of benzenesulfonic acid. Although the reduction of furfural and the condensation of furfuryl alcohol with maleic anhydride could be performed smoothly, the esterification of furfuryl maleic acid with ethanol only gave 38 % yield of ethyl furfuryl fumarate.The results of antimicrobial activity test showed that the value of minimum inhibition concentration (MIC) of salicyl maleic acid and ethyl salicyl fumarate towards Staphyllococcus aureus were 500 and 100 μg/mL, whereas towards Eschericia coli were 2000 and 4000 μg/mL respectively. In contrast, the MIC values of furfuryl maleic acid and ethyl furfuryl fumarate towards Staphyllococcus aureus and Eschericia coli were 150 and 100 μg/mL respectively.Keywords: synthesis, activity, C-9154 antibiotic, fumarate
The influence of tween 80 and polyethylen glycol 400 on piroxicam absorption from rat intestinal lumen in situ Abdul Karim Zulkarnain; Arundita Kusumawida; Triani Kurniawati
Indonesian Journal of Pharmacy Vol 19 No 1, 2008
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (191.007 KB) | DOI: 10.14499/indonesianjpharm0iss0pp25-31

Abstract

Oral drug absorption administered is highly influenced by dissolution rate, especially for poorly and insoluble drugs. Tween 80 and polyethylene glycol 400 (PEG 400) as surfactant an increase drug solubility by means of a micelle forming mechanism. The aim of the study wasto know the influence of addition and variation of Tween 80 and PEG 400 on the absorption of piroxicam from rat intestinal lumen in situ. Piroxicam solution in pH 7.5 phosphate buffer was prepared with the same concentration in three kinds based on the addition concentration of Tween 80 and PEG 400, they were 1.0, 1.5 and 2.0 % respectively. The male rats of 130-180 grams body weight fasted were for 24 hours before treatment. The rats were anaesthetized with 5x10-3 mL/g BW 40% urethan subcutaneously. Piroxicam unabsorbed fraction was measured in a spectrophotometer at 353 nm, and then calculate Papp (Appear Permeability). The data obtained were calculated according to Kolmogorov-Smirnov and one-way ANAVA then continued by a t-test (95% confidence level). Tween 80 at 10% and 1.5% increased piroxicam absorption from the phosphate buffer pH 7.5 but decreased with Tween 80 2.0%. According to Papp, thevalues were 0.3929 cm/minute (1.5% Tween 80), 0.3507 cm/minute (1.0% Tween 80) and 0.2593 cm/minute (2.0% Tween 80) respectively. PEG 400 at 2.0 % rised piroxicam absorption from the phosphate buffer pH 7.5 but no with influence PEG 400 1.5 % concentration one way ANAVA. Key words : Tween 80, Polyethylen glycol 400, piroxicam, in situ absorption