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Disolusi Kapsul Dispersi Padat Piroksikam-PEG 6000 Selama Penyimpanan Binarjo, Annas; Khotimah, Husnul
Indonesian Journal of Pharmaceutical Science and Technology Vol 4, No 1 (2017)
Publisher : Indonesian Journal of Pharmaceutical Science and Technology

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (424.429 KB) | DOI: 10.15416/ijpst.v4i1.7933

Abstract

Kelarutan piroksikam yang rendah mempengaruhi laju disolusi sebagai penentu bioavaibilitas. Pembuatan dispersi padat dengan piroksikam-polietilenglikol dapan meningkatkan laju disolusinya. Tujuan penelitian ini adalah untuk mengetahui pengaruh pembentukan dispersi padat piroksikam- polietilenglikol 6000 (PEG 6000) terhadap laju disolusi kapsul piroksikam selama 1 bulan penyimpanan. Rekristal piroksikam (R) dan dispersi padat piroksikam-PEG 6000 (DP) dibuat dengan metode pelarut menggunakan campuan aseton-etanol (1:1), keduanya bersama dengan piroksikam tanpa modifikasi (P) dikapsul dan disimpan selama 1 bulan. Uji disolusi dilakukan setiap minggu. Efisiensi disolusi 60 menit (DE60), prosentase disolusi 45 menit (C45), dan waktu untuk 80% terdisolusi (t80) digunakan sebagai parameter disolusi. Kurva hubungan DE60, C45, dan t80 terhadap waktu penyimpanan dilihat slope-nya sebagai parameter stabilitas. Hasil percobaan menunjukkan bahwa Kapsul P dan DP menunjukkannilai DE60, C45, dan t80 yang stabil selama penyimpanan (slope=0, p>0.05), demikian juga nilai t80 kapsul R. Sedangkan DE60 dan C45 kapsul R selama penyimpanan terus menurun dengan slope -0,636 %/hari dan -0,171 mg/hari. Dapat disimpulkan bahwa DP yang dibuat dengan metode pelarut campuran aseton dan etanol (1:1) menunjukkan profil disolusi yang stabil selama penyimpanan 1 bulan.
STUDI PENETAPAN KADAR LOSARTAN DENGAN METODE SPEKTROFOTOMETRI DAN HIGH PERFORMANCE LIQUID CHROMATOGRAPHY (HPLC) SERTA APLIKASINYA PADA TRANSPOR TRANSDERMAL in vitro Binarjo, Annas; Nugroho, Achmad Kharis
Pharmaciana Vol 3, No 1 (2013): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (162.592 KB) | DOI: 10.12928/pharmaciana.v3i1.417

Abstract

The development of drug delivery system needs a usefull determination method ofdrug in many kind of samples. This research was purposed to develop a determinationmethod of losartan, an angiotension receptor antagonist II, from the sample of in vitrotransdermal transport. Three methods were studied, i.e. normal spectrophotometric, 1stderivative spectrophotometric, and HPLC. The spectrophotometric method wasconducted using Spectrophotometer Shimadzu tipe UV 1700 controlled by UV Probesoftware (Shimadzu), while HPLC method was performanced by Shimadzu HPLCcontrolled by LC Solution software (Shimadzu). Lichrospher RP 18 250-4 (5 µm) wasused as stationary phase and acetonitril-acetic buffer 0,01 M pH 4 (60:40) was used asmobile phase. Chromatogram was recorded using UV 223 nm and 254 nm as adetector. Some parameters of determination method performance were calculated, i.e.LOD, LOQ, recovery, systemic error, and random error. The results shown thatspectrofotometric methods did not have an enough performance parameters to use intransdermal transport of losartan, while HPLC method had LOD and LOQ 27,329 and91,098 ng/ml using UV 223 nm as detector and 36,178 and 120,590 ng/ml using UV 254nm as detector. Detector UV 223 nm was selected. This HPLC method had recovery106,405% and random error 3,71%, and could be used to determine the losartanconcentration in sample from transdermal transport in vitro.
STABILITAS FISIKA DAN KIMIA REKRISTAL DAN DISPERSI PADAT PIROKSIKAM-PEG 6000 Binarjo, Annas
Pharmaciana Vol 5, No 1 (2015): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (439.36 KB) | DOI: 10.12928/pharmaciana.v5i1.2287

Abstract

It is hoped that solid dispersion and recrystalization can solve the problem of low solubility of piroxicam.  Metastable polymorph or amorph state can be formed in solid dispersion and recrystalization preparation, leading to a better dissolution. During storage, the metastable polymorph or amorph will be changed to stable crystal, so that the dissolution will be decreased (physical instability), beside that the increasing of solubility also trigger the higher rate of decomposition (chemical instability).  This research was purposed to reveal these two instability. The research was began by preparing recrystal of piroxicam (R) and solid dispersion piroxicam-PEG 6000 (DP) by solvent method using aseton.  These preparate were stored in room temperature (25oC). The dissolution was tested after 1, 2, 3, and 4 month of storage, using dissolution efficiency for 60 minutes (DE60) as parameter, and also the drug content in bulk preparate was determined. The result showed that recrystalization and solid dispersion preparation did not decrease  the piroxicam content.  During storage, the DE60 and piroxicam content in R and DP were not changed (p>0.05). It could be concluded that R and DP prepared had a stable dissolution and purity.
FORMULASI COLD CREAM PROPRANOLOL UNTUK PENGHANTARAN TRANSDERMAL DENGAN BASIS EMULSI YANG MENGANDUNG VCO (VIRGIN COCONUT OIL) Lestari, Muji; Binarjo, Annas
Pharmaciana Vol 3, No 2 (2013): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (150.251 KB) | DOI: 10.12928/pharmaciana.v3i2.429

Abstract

Propanolol is a non-selective beta-blocker that is used widely to overcome cardiovascular disorder.Development of propranolol in transdermal delivery is necessary to avoid the first pass metabolism that reducesthe active metabolite up to 15-23% left. This study was objected to determine the effect of VCO (Virgin CoconutOil) concentration as a base and penetration enhancer of propranolol in the cold cream preparation through rat skinmembrane in vitro. Variation concentration of VCO (0%, 14%, 28%, and 42%) was added to propanolol coldcream. Transdermal in vitro study was performed using vertical type diffusion cell with PBS pH 7,4 as receptormedia. The temperature was maintained at 35ºC with a constant stirring rate at 300 rpm. The transport wasconducted for 8 hours. Flux, efficiency, and lag time were calculated as responses. The results showed that flux atvarious concentration of VCO (0%, 14%, 28%, 42%) were 12,30; 14,13; 14,52; and 23,06 -1 cm-2respectively. The transport efficiency were 6,5x10-4; 7,5x10-4; 8,1x10-4; and 1,22x10-3 % cm-2 respectively. Thelag time were 1,13; 1,26; 1,11; and 0,92 hours respectively. It can be concluded that the VCO can be used mainlyas a base in the preparation of cold cream and can increase percutaneous permeation of propranolol significantly(p <0.05). VCO concentration of 42% has the highest performance.
PENGEMBANGAN PREPARASI NANOPARTIKEL THYMOQUINONE-KITOSAN DENGAN METODE KOSOLVEN MENGGUNAKAN ISOPROPIL ALKOHOL Binarjo, Annas; Yuwono, Tedjo; Priyanti, Renny
Pharmaciana Vol 5, No 2 (2015): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (542.834 KB) | DOI: 10.12928/pharmaciana.v5i2.2363

Abstract

Thymoquinone, an active compound isolated from black cumin seeds (Nigella sativa L.), has pharmacological activity as anticancer, antiinflammatory, and immunomodulator. This compound has a volatile nature, easily oxidized, and low melting point, leading to difficulties in tablet formulation. Moreover, its low solubility in water leading to low bioavailability. Therefore, it is necessary to develop nanoparticle drug delivery systems to solve these problems. Chitosan-thymoquinone nanoparticles can be formed using sodium tripolyphosphate as cross linker by cosolven method. Chitosan solution in acetate buffer pH 4 was added to thymoquinone solution in 50%, 75%, 100% isopropyl alcohol, than sodium tripoliphosphate solution in water was added slowly in a gently stirrer.  The nanoparticle produced was characterized in its loading capacity (LC), particle morphology, particle size, and zeta potential, as well as the loading efficiency (LE) of nanoparticle. Factorial Design Optimization resulted that the best condistion is achieved by 75% isopropyl alcohol using thymoquinone level of 10 mg/mL and chitosan level of 10 mg/mL. In this condition, the nanoparticle has LC of 8.71%, LE of 76.29%, 609.8 nm in diameter and zeta potential of 137.9 mV. It can be concluded that isopropyl alcohol can help the formation of nanoparticles thymoquinone. The particle size and zeta potential is too big, therefore it is craved to modify the process by variation in thymoquinone, chitosan, and sodium tripoliphosphat concentration.
Formulasi Emulgel Minyak Biji Bunga Matahari (Helianthus annuus L.) sebagai Sediaan Penyembuh Luka Bakar Monika, Tika; Edityaningrum, Citra Ariani; Binarjo, Annas
Media Farmasi: Jurnal Ilmu Farmasi Vol 12, No 1: Maret 2015
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (193.541 KB) | DOI: 10.12928/mf.v12i1.3026

Abstract

Luka bakar merupakan suatu bentuk kerusakan atau kehilangan jaringan yang disebabkan kontak dengan sumber panas seperti api, air panas, bahan kimia, listrik, dan radiasi. Asam linoleat dan β-sitosterol merupakan senyawa aktif yang ditemukan didalam minyak biji bunga matahari (Helianthus annuus L.) yang mempunyai aktivitas dalam penyembuhan luka bakar. Penelitian ini bertujuan untuk mengetahui sifat fisik emulgel dan efek konsentrasi minyak biji bunga matahari pada sediaan emulgel terhadap aktivitas penyembuhan luka. Pada tahapan awal, minyak biji bunga matahari diidentifikasi kandungan β-sitosterol (menggunakan KLT) dan kandungan asam linoleatnya (menggunakan GS-MS). Selanjutnya minyak diformulasikan dalam emulgel dengan berbagai konsentrasiminyak biji bunga matahari yaitu F1 (3%), FII (5%), dan F III(10%). Krimdievaluasi sifat fisik meliputi pH, daya lekat, kemampuan proteksi, dan daya sebar; serta daya penyembuh luka bakar denganhewan uji marmut. Pembuatan luka bakar dilakukan dengan menggunakan solder yang telah dimodifikasi. Data yang diperoleh dianalisis menggunakan uji statistika ANOVA dan LSD dengan taraf kepercayaan 95%.  Berdasarkan penelitian ini disimpulkan emulgel minyak biji bunga matahari dapat mempercepat penyembuhan luka bakar. Semakin tinggi konsentrasi minyak biji bunga matahari, semakin tinggi aktivitasnya terhadap penyembuhan luka, serta daya sebar dan daya lekatnya. Kata kunci: minyak biji bunga matahari, emulgel, sifat fisik, asam linoleat, βsitosterol, luka bakar
Permeasi Transdermal Losartan In Vitro dari Larutan dengan Variasi Kadar Losartan dan Propilen Glikol Annas Binarjo; Akhmad Kharis Nugroho
Jurnal Kimia Valensi Jurnal Valensi Volume 4, No.1, Mei 2014
Publisher : Syarif Hidayatullah State Islamic University

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (174.262 KB) | DOI: 10.15408/jkv.v4i1.1046

Abstract

Abstrak Losartan, senyawa antagonis reseptor angiotensin II, mempunyai bioavailabilitas oral 0.25-0.35.  Bioavailabilitas yang rendah ini dapat diatasi dengan penghantaran obat secara transdermal. Enhancer sering ditambahkan ke dalam formula sediaan transdermal, misalnya propilen glikol (PG).  Penelitian ini bertujuan mempelajari pengaruh kadar propilen glikol terhadap permeasi transdermal losartan pada kadar obat yang berbeda. Penelitian dilakukan secara in vitro dengan sel difusi tipe vertikal dilakukan terhadap empat formula yaitu 2% potasium losartan (k-los) :15% PG (F1), 10% k-los :15% PG (F2), 2% k-los :20% PG (F3), dan 10% k-los: 20% PG (F4) dengan dapar sitrat pH 5 sebagai mediumnya.  Kulit punggung tikus jantan galur wistar digunakan sebagai membran, PBS pH 7,4 sebagai medium kompartemen reseptor, dan HPLC untuk pengukuran kadar k-los dalam kompartemen reseptor dengan detektor UV. Hasil penelitian menunjukkan bahwa peningkatan kadar k-los dari 2% ke 10% pada kadar PG 15% meningkatkan fluks, sedangkan pada kadar 20% tidak berpengaruh terhadap fluks.  Peningkatan kadar PG dari 15% ke 20% justru menurunkan fluks pada kadar k-los 2%, dan tidak berpengaruh pada kadar k-los 10%.  Nilai lag time tidak berbeda diantara semua fomula. Hal ini berarti penggunaan enhancer PG lebih dari 15% justru merugikan permeasi transdermal. Kata Kunci : transdermal, losartan, propilen glikol, enhancer   Abstract Losartan is an angiotensin receptor antagonis which has low oral bioavailability (0.25-0.35).  Transdermal drug delivery system is needed as one solution for this low oral bioavailability drug.  Propilen glikol (PG), as enhancer, is frequently added in transdermal dosage form.  This research was purposed to explore the effect of PG as losartan permeation enhancer in various concentration of potasium losartan (k-los). The research was carried out in vitro using vertical tipe difusion cel for 4 formulas, i.e. 2% potasium losartan (k-los) :15% PG (F1), 10% k-los :15% PG (F2), 2% k-los :20% PG (F3), and 10% k-los: 20% PG (F4) using citric buffer pH 5 as donor medium, while PBS pH 7,4 was used as receptor medium.  The dorsal skin of white wistar male rat was used as membrane.  HPLC with UV detector was used to determine the concentration of k-los appear in receptor compartment. The results show that increasing of k-los concentration from 2% to 10% can increase the flux if PG concentration is 20%, but it does not have any significant effect to the flux if the PG concentration is 15%.  Increasing PG concentration from 15% to 20% decrease the flux permeation in k-los concentration of 2%, and does not have any significant effect in concentration of k-los of 10%.  The lag time permeation does not has any significant differencess.  It means that PG as enhancer in the concentration above 15% doesn’t have any adventages. Keywords : transdermal, losartan, propilen glycol, enhancer
FORMULASI COLD CREAM PROPRANOLOL UNTUK PENGHANTARAN TRANSDERMAL DENGAN BASIS EMULSI YANG MENGANDUNG VCO (VIRGIN COCONUT OIL) Muji Lestari; Annas Binarjo
Pharmaciana Vol 3, No 2 (2013): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (150.251 KB) | DOI: 10.12928/pharmaciana.v3i2.429

Abstract

Propanolol is a non-selective beta-blocker that is used widely to overcome cardiovascular disorder.Development of propranolol in transdermal delivery is necessary to avoid the first pass metabolism that reducesthe active metabolite up to 15-23% left. This study was objected to determine the effect of VCO (Virgin CoconutOil) concentration as a base and penetration enhancer of propranolol in the cold cream preparation through rat skinmembrane in vitro. Variation concentration of VCO (0%, 14%, 28%, and 42%) was added to propanolol coldcream. Transdermal in vitro study was performed using vertical type diffusion cell with PBS pH 7,4 as receptormedia. The temperature was maintained at 35ºC with a constant stirring rate at 300 rpm. The transport wasconducted for 8 hours. Flux, efficiency, and lag time were calculated as responses. The results showed that flux atvarious concentration of VCO (0%, 14%, 28%, 42%) were 12,30; 14,13; 14,52; and 23,06 -1 cm-2respectively. The transport efficiency were 6,5x10-4; 7,5x10-4; 8,1x10-4; and 1,22x10-3 % cm-2 respectively. Thelag time were 1,13; 1,26; 1,11; and 0,92 hours respectively. It can be concluded that the VCO can be used mainlyas a base in the preparation of cold cream and can increase percutaneous permeation of propranolol significantly(p <0.05). VCO concentration of 42% has the highest performance.
PENGEMBANGAN PREPARASI NANOPARTIKEL THYMOQUINONE-KITOSAN DENGAN METODE KOSOLVEN MENGGUNAKAN ISOPROPIL ALKOHOL Annas Binarjo; Tedjo Yuwono; Renny Priyanti
Pharmaciana Vol 5, No 2 (2015): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (542.834 KB) | DOI: 10.12928/pharmaciana.v5i2.2363

Abstract

Thymoquinone, an active compound isolated from black cumin seeds (Nigella sativa L.), has pharmacological activity as anticancer, antiinflammatory, and immunomodulator. This compound has a volatile nature, easily oxidized, and low melting point, leading to difficulties in tablet formulation. Moreover, its low solubility in water leading to low bioavailability. Therefore, it is necessary to develop nanoparticle drug delivery systems to solve these problems. Chitosan-thymoquinone nanoparticles can be formed using sodium tripolyphosphate as cross linker by cosolven method. Chitosan solution in acetate buffer pH 4 was added to thymoquinone solution in 50%, 75%, 100% isopropyl alcohol, than sodium tripoliphosphate solution in water was added slowly in a gently stirrer.  The nanoparticle produced was characterized in its loading capacity (LC), particle morphology, particle size, and zeta potential, as well as the loading efficiency (LE) of nanoparticle. Factorial Design Optimization resulted that the best condistion is achieved by 75% isopropyl alcohol using thymoquinone level of 10 mg/mL and chitosan level of 10 mg/mL. In this condition, the nanoparticle has LC of 8.71%, LE of 76.29%, 609.8 nm in diameter and zeta potential of 137.9 mV. It can be concluded that isopropyl alcohol can help the formation of nanoparticles thymoquinone. The particle size and zeta potential is too big, therefore it is craved to modify the process by variation in thymoquinone, chitosan, and sodium tripoliphosphat concentration.
STUDI PENETAPAN KADAR LOSARTAN DENGAN METODE SPEKTROFOTOMETRI DAN HIGH PERFORMANCE LIQUID CHROMATOGRAPHY (HPLC) SERTA APLIKASINYA PADA TRANSPOR TRANSDERMAL in vitro Annas Binarjo; Achmad Kharis Nugroho
Pharmaciana Vol 3, No 1 (2013): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (162.592 KB) | DOI: 10.12928/pharmaciana.v3i1.417

Abstract

The development of drug delivery system needs a usefull determination method ofdrug in many kind of samples. This research was purposed to develop a determinationmethod of losartan, an angiotension receptor antagonist II, from the sample of in vitrotransdermal transport. Three methods were studied, i.e. normal spectrophotometric, 1stderivative spectrophotometric, and HPLC. The spectrophotometric method wasconducted using Spectrophotometer Shimadzu tipe UV 1700 controlled by UV Probesoftware (Shimadzu), while HPLC method was performanced by Shimadzu HPLCcontrolled by LC Solution software (Shimadzu). Lichrospher RP 18 250-4 (5 µm) wasused as stationary phase and acetonitril-acetic buffer 0,01 M pH 4 (60:40) was used asmobile phase. Chromatogram was recorded using UV 223 nm and 254 nm as adetector. Some parameters of determination method performance were calculated, i.e.LOD, LOQ, recovery, systemic error, and random error. The results shown thatspectrofotometric methods did not have an enough performance parameters to use intransdermal transport of losartan, while HPLC method had LOD and LOQ 27,329 and91,098 ng/ml using UV 223 nm as detector and 36,178 and 120,590 ng/ml using UV 254nm as detector. Detector UV 223 nm was selected. This HPLC method had recovery106,405% and random error 3,71%, and could be used to determine the losartanconcentration in sample from transdermal transport in vitro.