CHARACTERIZATION OF PHARMACOKINETICS OF 2-((3-(CHLOROMETHYL)BENZOYL)OXY) BENZOIC ACID IN RATS BY USING HPLC-DAD METHOD

Objective: A new compound of salicylic acid derivative, namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CBB), was synthesized to find a compound exhibiting higher analgesic activity and smaller ulcer irritation than acetylsalicylic acid (ASA). Therefore, this study aimed to investigate the pharmacokinetics of this new compound in rats, following a single dose oral administration of 3CBB (45 mg/kg BW). Methods: Plasma samples of 9 healthy rats were collected before and up to 3 h after its oral administration, following an 18 h fasting period. Plasma concentrations of 3CBB were determined using a validated HPLC-DAD assay. Pharmacokinetic parameters were determined using the compartment model technique. All experiments were carried out in triplicate. Results: The pharmacokinetic parameters of 3CBB obtained were as follows: Tmax= 28.9±1.1 min, Cmax = 0.57±0.02 µg/ml, AUCtotal = 66.3±1.0 µg min/ml, Kel = 0.018±0.002 min-1, and T1/2el = 39.4±3.9 min. The long elimination half-life and low Cmax indicated that 3CBB was extensively distributed in the deep and very deep tissues. This confirmed the unique and special characteristics of a highly lipophilic compound like 3CBB (log P = 3.73). Conclusion: 3CBB demonstrated a slower onset of action and longer elimination time from the body compared to ASA. Thus this new compound is a potential candidate to be developed as a new drug

Perbandingan Aktivitas Antibakteri 4-Metilpiperazin-N-Karbonil Ampisilin dengan Ampisilin Terhadap Micrococcus luteus dan Escherichia coli

Piperacillin has antimicrobial action but it is not absorbed from gastrointestinal tract Therefore, it needs structure modification to increase its absorption while keeping its antimicrobial action. The 4-methylpiperazin-N-carbonyl ampicillin was the product of reaction between ampicillin and 4-methylpiperazin-N-carbonyl chloride using Schotten Baumann method. The aim of this research was to compare the antibacterial activity between 4-methylpiperazin-N-carbonyl ampicillin and ampicillin. The comparison test of antibacterial activity was done with Kirby-Bauer disk diffusion susceptibility method on Mueller-Hinton agar which had been inoculated with Micrococcus luteus and Escherichia coli. Based on orientation studies, concentration of 4-methylpiperazin-N-carbonyl ampicillin and ampiCillin were 0.5 ppm against Micrococcus luteus and 500 ppm against Escherichia collin order to get visible zone of inhibition. The results showed that 4-methylpiperazin-Ncarbonyl ampicillin had lower antibacterial activity than ampicillin which was showed by its zone of inhibition which was lower compared to ampicillin in inoculated agar media of Micrococcus luteus and Escherichia coli

Komunikasi Ilmiah di Perguruan Tinggi pada Era Perpustakaan 4.0

Komunikasi Ilmiah di Perguruan Tinggi pada Era Perpustakaan 4.

Influence of various concentrations of PVP K-30 as a binder on the physical quality of cerme (Phyllanthus acidus) leaves extract tablet

A Study on the influence of tablet formulae containing cerme leaves extract using PVP K-30 as a binder in the concentrations of 2% (formula A), 3% (formula B), 4% (formula C) on the physical quality of tablet has been conducted. Cerme leaves extract was obtained by percolation method employing ethanol 96% as a solvent. Tablets were prepared by wet granulation method and the physical quality of resulting granules was evaluated including moisture content, repose angle, flow rate, and compressibility. Granules were then compressed to yield tablets of 650 mg. in which each tablet contains 449 mg of dry extract of cerme leaves. The physical quality of resulting tablets was evaluated including weight uniformities, hardness, Friability, disintegration time, dissolution, and a comparative qualitative determination of chemical contents of cerme leaves extract by TLC (Thin Layer Chromatography) in various samples commencing from viscous extract until tablet dosage form. The hardness, friability, disintegration time. and dissolution data were evaluated using completely randomized design ANOVA with a level of confidence of 95% and subsequently followed by LSD (Least Significant Difference) test. It can be concluded that cerme leaves extract could be formulated as a tablet and met the physical quality requirements of tablet. There no significant differences on the hardness and dissolution of three formulae tablets (Fcalc < Ftable). On the other hand. The friability and disintegration time of three formulae tablets differed significantly (Fcalc < Ftable). Formula A was the selected one owing ot its shortest disintegration time and highest economic value (least binder concentration)

Amilum kulit pisang (Musa paradisiaca) Agung sebagai bahan pengikat tablet.

lnvensi ini berhubungan dengan pembuatan amilum dari kulit pisang (Musa paradisiaca) agung serta pemanfaatannya daiam bidang farmasi sebagai bahan tambahan sediaan tablet. Keunggulan pisang (Musa paradisiaca) agung yaitu memiliki ukuran buah yang besar dan panjang (34-36 cm) dengan bobot 10-20 kg/tandan; kulit buah yang tebal sehingga tahan disimpan 3-4 minggu setelah petik dan iJ'lemiliki rasa buah yang manis. Pisang (Musa paradisiaca) agung banyak digunakan sebagai bahan pembuatan kripik pisang, dengan 1agian kulitnya dibuang. Amilum kulit pisang (Musa paradisiaca) agung yang diperoleh, digunakan sebagai pengikat pacta tablel \assa tablet yang dihasilkan memenuhi persyaratan berdasarkan nilai Carr's index dan Hausner ratio, serta tablet dengan mutufisik yang \suai dengan persyaratan kekerasan, kerapuhan, dan waktu hancur tablet

Characterization Of Pharmacokinetics Of 2-((3-(Chloromethyl)Benzoyl)Oxy) Benzoic Acid In Rats By Using Hplc-Dad Method

Objective: A new compound of salicylic acid derivative, namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CBB), was synthesized to find a compound exhibiting higher analgesic activity and smaller ulcer irritation than acetylsalicylic acid (ASA). Therefore, this study aimed to investigate the pharmacokinetics of this new compound in rats, following a single dose oral administration of 3CBB (45 mg/kg BW). Methods: Plasma samples of 9 healthy rats were collected before and up to 3 h after its oral administration, following an 18 h fasting period. Plasma concentrations of 3CBB were determined using a validated HPLC-DAD assay. Pharmacokinetic parameters were determined using the compartment model technique. All experiments were carried out in triplicate. Results: The pharmacokinetic parameters of 3CBB obtained were as follows: Tmax= 28.9±1.1 min, Cmax = 0.57±0.02 μg/ml, AUCtotal = 66.3±1.0 μg min/ml, Kel = 0.018±0.002 min-1, and T1/2el = 39.4±3.9 min. The long elimination half-life and low Cmax Conclusion: 3CBB demonstrated a slower onset of action and longer elimination time from the body compared to ASA. Thus this new compound is a potential candidate to be developed as a new drug. indicated that 3CBB was extensively distributed in the deep and very deep tissues. This confirmed the unique and special characteristics of a highly lipophilic compound like 3CBB (log P = 3.73)

Influence of various concentrations of PVP K-30 as a binder on the physical quality of cerme (Phyllanthus acidus) leaves extract tablet

A Study on the influence of tablet formulae containing cerme leaves extract using PVP K-30 as a binder in the concentrations of 2% (formula A), 3% (formula B), 4% (formula C) on the physical quality of tablet has been conducted. Cerme leaves extract was obtained by percolation method employing ethanol 96% as a solvent. Tablets were prepared by wet granulation method and the physical quality of resulting granules was evaluated including moisture content, repose angle, flow rate, and compressibility. Granules were then compressed to yield tablets of 650 mg. in which each tablet contains 449 mg of dry extract of cerme leaves. The physical quality of resulting tablets was evaluated including weight uniformities, hardness, Friability, disintegration time, dissolution, and a comparative qualitative determination of chemical contents of cerme leaves extract by TLC (Thin Layer Chromatography) in various samples commencing from viscous extract until tablet dosage form. The hardness, friability, disintegration time. and dissolution data were evaluated using completely randomized design ANOVA with a level of confidence of 95% and subsequently followed by LSD (Least Significant Difference) test. It can be concluded that cerme leaves extract could be formulated as a tablet and met the physical quality requirements of tablet. There no significant differences on the hardness and dissolution of three formulae tablets (Fcalc < Ftable). On the other hand. The friability and disintegration time of three formulae tablets differed significantly (Fcalc < Ftable). Formula A was the selected one owing ot its shortest disintegration time and highest economic value (least binder concentration)

Evaluation of analgesic and antiplatelet activity of 2-((3-(chloromethyl) benzoyl)oxy)benzoic acid

Acetylsalicylic acid is used as a non-steroidal anti-inflammatory drugs (NSAID) and antiplatelet agents by inhibiting cyclooxygenases. However, therapy using acetylsalicylic acid could induce gastric bleeding and cause other gastrointestinal toxicity. The aim of this study was to demonstrate the synthesis of a new compound bearing salicylic acid residue namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid, to analyze its potential as a ligand for human cyclooxygenase-2 (COX-2) receptor, to evaluate its toxicity level and its effectiveness for analgesic and antiplatelet agent compared with acetylsalicylic acid. Synthesis of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid was conducted by microwave irradiation. The purity of this compound was evaluated with TLC, IR, NMR, and EDS spectroscopy. The chemical characterization and docking studies against human COX-2 (PDB:5F1A) was performed in-silico. The acute oral toxicity assay was performed under OECD guidelines. The analgesic activity study was performed by plantar and writhing test on animal model. For anti-platelet activity study, we performed tail-bleeding assay and flow cytometry based platelet aggregation assay. We could successfully synthesize a pure white crystalline 2-((3-(chloromethyl)benzoyl) oxy)benzoic acid. In-Silico G-Score result of those compounds gives us preliminary hint of the potential affinity of this compound as a ligand for COX-2 receptor (PDB: 5F1A). Acute toxicity and microscopic gastrointestinal assessments indicated non-observable harmful toxicity parameters. The plantar response time of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid treated groups showed a significant increment (P < 0.01), and the nociceptive response in writhing test demonstrated a significant dose-dependent decrement. This indicated that its analgesic activity was better than acetylsalicylic acid. The platelet aggregation of 2-((3-(chloromethyl)benzoyl) oxy)benzoic acid was lower than its controls, indicating an aggregation inhibition pattern. The animals treated with 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid gave a longer bleeding time. Overall, this study demonstrated a successful synthesis of pure 2-((3- (chloromethyl)benzoyl)oxy) benzoic acid. We postulated that this compound was better than acetylsalicylic acid, exhibiting excellent analgesic and antiplatelet activity with no toxicity impact

Evaluation of analgesic and antiplatelet activity of 2-((3-(chloromethyl) benzoyl)oxy)benzoic acid

Acetylsalicylic acid is used as a non-steroidal anti-inflammatory drugs (NSAID) and antiplatelet agents by inhibiting cyclooxygenases. However, therapy using acetylsalicylic acid could induce gastric bleeding and cause other gastrointestinal toxicity. The aim of this study was to demonstrate the synthesis of a new compound bearing salicylic acid residue namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid, to analyze its potential as a ligand for human cyclooxygenase-2 (COX-2) receptor, to evaluate its toxicity level and its effectiveness for analgesic and antiplatelet agent compared with acetylsalicylic acid. Synthesis of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid was conducted by microwave irradiation. The purity of this compound was evaluated with TLC, IR, NMR, and EDS spectroscopy. The chemical characterization and docking studies against human COX-2 (PDB:5F1A) was performed in-silico. The acute oral toxicity assay was performed under OECD guidelines. The analgesic activity study was performed by plantar and writhing test on animal model. For anti-platelet activity study, we performed tail-bleeding assay and flow cytometry based platelet aggregation assay. We could successfully synthesize a pure white crystalline 2-((3-(chloromethyl)benzoyl) oxy)benzoic acid. In-Silico G-Score result of those compounds gives us preliminary hint of the potential affinity of this compound as a ligand for COX-2 receptor (PDB: 5F1A). Acute toxicity and microscopic gastrointestinal assessments indicated non-observable harmful toxicity parameters. The plantar response time of 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid treated groups showed a significant increment (P < 0.01), and the nociceptive response in writhing test demonstrated a significant dose-dependent decrement. This indicated that its analgesic activity was better than acetylsalicylic acid. The platelet aggregation of 2-((3-(chloromethyl)benzoyl) oxy)benzoic acid was lower than its controls, indicating an aggregation inhibition pattern. The animals treated with 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid gave a longer bleeding time. Overall, this study demonstrated a successful synthesis of pure 2-((3- (chloromethyl)benzoyl)oxy) benzoic acid. We postulated that this compound was better than acetylsalicylic acid, exhibiting excellent analgesic and antiplatelet activity with no toxicity impact

Pemanfaatan Kulit Pisang Agung Semeru Sebagai Bahan Pengikat Tablet.

Menurut Peraturan Menteri Kesehatan Republik Indonesia Nomor 87 Tahun 2013, tentang Peta Jalan Pengembangan Bahan Baku Obat, amilum merupakan salah satu target bahan baku obat yang akan dikembangkan dalam jangka menengah (3-5 tahun). Kulit pisang Agung Semeru, yang diperoleh dari sentra pengolahan keripik pisang di Kabupaten Lumajang, Jawa Timur, merupakan limbah organik yang belum dimanfaatkan sehinggga belum memiliki nilai ekonomis yang baik. Kandungan amilum yang ada dalam kulit pisang Agung Semeru dapat dimanfaatkan sebagai bahan pengikat pada pembuatan tablet. Pada penelitian ini dibuat amilum dari kulit pisang Agung Semeru yang digunakan sebagai bahan pengikat untuk membuat bahan ko-proses orally disintegrating tablet (ODT). Bahan ko-proses ODT mengandung laktosa monohidrat dan Avicel PH101 sebagai pengisi tablet, amilum kulit pisang Agung Semeru sebagai pengikat tablet, sodium starch glycolate (SSG) sebagai penghancur tablet, dan manitol sebagai pemanis, dibuat dengan metode granulasi basah. Dilakukan pengamatan terhadap mutu fisik granul dan tablet bahan ko- proses. Hasil penelitian menunjukkan amilum kulit pisang Agung Semeru dapat digunakan sebagai pengikat tablet dan dapat menghasilkan bahan ko-proses ODT yang memiliki sifat alir dan kompaktibilitas yang baik. Formula optimum diperoleh dengan menggunakan konsentrasi amilum kulit pisang Agung Semeru 3,35% dan konsentrasi SSG 4,473%, yang memberikan respon teoritis Carr’s index 19,594%, Hausner ratio 1,242, kerapuhan tablet 0,585%, kekerasan tablet 2,124 kp, waktu hancur tablet 116,964 detik, waktu pembasahan 59,836 detik, dan rasio absorpsi air 59,6