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STUDI KOMPARATIF PREDIKSI PROFIL ADMET OBAT SINTETIS DENGAN SENYAWA AKTIF TANAMAN HERBAL ANTIMALARIA MELALUI PENDEKATAN IN SILICO Rima Rasida; Pinanga, Yangie Dwi Marga; Anjar Hermadi Saputro; Damayanti, Sophi
Acta Pharmaceutica Indonesia Vol. 49 No. 2 (2024)
Publisher : School of Pharmacy Institut Teknologi Bandung

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Abstract

Resistance to antimalarial drugs has become a global challenge in achieving the target of malaria eradication. To address this issue, effective and safe alternative treatments are urgently needed. This study compares the ADMET profiles (absorption, distribution, metabolism, excretion, and toxicity) of synthetic antimalarial drugs with active compounds derived from herbal sources using an in-silico approach. The analyzed herbal compounds, including piperine, kaempferol, berberine, quassin, and limonin, demonstrated high intestinal absorption (>30%), good water solubility, and sufficient skin permeability. In the distribution analysis, kaempferol exhibited high volume distribution due to its lipophilic interactions with body tissues, although most compounds were unable to penetrate the blood-brain barrier. The herbal compounds piperine and kaempferol inhibited metabolic enzymes CYP2C19 and CYP1A2, whereas synthetic drugs tended to act as substrates. Regarding excretion, piperine served as a renal OCT2 substrate, while pyrimethamine exhibited low clearance. Toxicity assessments revealed that herbal compounds generally exhibited better toxicity profiles compared to synthetic drugs, with limonin showing the lowest acute and chronic toxicity. These findings suggest that herbal active compounds hold significant potential for development as alternative antimalarial agents, particularly in addressing drug resistance. This study highlights the importance of further developing herbal-based drugs through in silico approaches to enhance the efficacy and safety of malaria therapy. Keyword : malaria drug resistance, active herbal compounds, ADMET, In silico
Development and Validation of Analytical Method for Piperine in Phytopharmaceutical Product Containing Cabe Jawa Fructus by HPLC Galih, Wening; Permana, Benny; Damayanti, Sophi
Indonesian Journal of Pharmaceutical Science and Technology Vol 12, No 1 (2025)
Publisher : Indonesian Journal of Pharmaceutical Science and Technology

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.24198/ijpst.v12i1.46348

Abstract

Cabe Jawa fruit (Retrofractii fructus) has empirically known to have effects such as anti-inflammatory and analgesic due to the presence of piperine. The maximum daily dose for piperine is 0.300–0.540 mg/kg/person/day. A reliable analytical method is required to ensure that phytopharmaceutical preparation is safe. This study developed and validated a piperine analysis method using phytopharmaceutical samples containing Cabe Jawa. A Shimadzu prominence HPLC SIL-20A Prominence autosampler and an X-Bridge C18 column (5 m x 250 mm x 4.6 mm) were used in the research devices. The OFAT method optimised the mobile phase, instrument systems, and sample preparation. The instrument system was optimized for acetonitrile:1% glacial acetic acid (48:52), 40°C, and a 1 mL/min flow rate. Each solid and liquid sample was prepared using the multilevel methanol dilution and water-dichloromethane liquid-liquid extraction (LLE) method. The results of validating the analytical procedures for solid and liquid samples were LOD and LOQ of 1.290 g/mL and 4.300 g/mL, 1.310 g/mL and 4 g/mL, respectively. Precision: 0.157% and 1.174%. Accuracy for three different concentrations were 94.232±1.050%, 95.387%±0.176%, and 96.272±1.043%; 88.801±0.428%, 89.473 ±0.252%, and 89.338 ±0.052% respectively. The analysis of the sample's piperine revealed that this method met the criteria for the validation parameters.