Objective : The aim of this study was to explore co-crystallization to enhance the solubility of simvastatin (SV) as a drug of choice for hypercholesterolemia using saccharin (Sacch) as co-former. Methods: Molecular modeling of sacch against SV has been conducted by in silico using auto dock 4.2. Preparation of co-crystal has carried out by solvent evaporation (SE) using an equimolar ratio of SV and Sacch. Co-crystal of SV-Sacch was evaluated by the saturated solubility test and intrinsic dissolution test. Afterward, the co-crystal was characterized by infrared spectrophotometry (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), binary phase diagram and stability studies in storage condition 400C and relative humidity (RH) 75% for three months. Results: In silico studies showed that the interaction of SV against sacch has hydrogen bonding as molecular synthon. Evaluations of solubility and intrinsic dissolution have shown an increased in rate properties significantly of co-crystal as compared to pure SV and its physical mixer (PM). Characterizations of a co-crystal SV: sacch (1: 1) has indicated the formation of different new solid crystal phase as compared to SV, sacch, and its PM, and stable for 40 0 C and RH 75% in 3 months. Conclusion: Co-crystallization has been used to increase the solubility and dissolution rate of simvastatin and all characterization has shown the formation of co-crystal SV: sacch (1: 1).

Objective: Purpose of this research was to get the optimum formulation of Self-Nanoemulsifying Drug Delivery System (SNEDDS) of mangosteen peels and to evaluate the permeation ability of active substances in the formulation. Method: Oil phase solubility of ethanol extract, ethyl acetate extract, ethyl acetate fraction, n-hexane fraction and residue of the mangosteen peels was tested with virgin coconut oil (VCO). The formulation was designed with a simplex lattice design using Design Expert software and the permeation was tested using Franz diffusion cell. Results: Based on the results of simplex lattice design methods obtained that the optimum formulation of SNEDDS was the composition of VCO, Tween 80, PEG 400 at a ratio of 1:6,95:2,05. The results of permeation test in vitro using Franz Diffusion cell indicated that the obtained SNEDDS ethyl acetate fraction of mangosteen peels that is 96.9223% higher than without preparation SNEDDS was 18,9426 % on hour-8. The optimum physical evaluation SNEDDS optimum values obtained involved drug loading of 125mg/5 mL SNEDDS, the transmittance value of 92%, emulsification time of 65 seconds, pH of 6.35, particle size 20 nm, zeta potential -12,40 and stable for three months. Conclusion: SNEDDS can improve the diffusion rate of mangosteen peels as a model poorly water soluble drug.Various samples of mangosteen peels were screened as candidates for SNEDDS on the basis of solubility of the active compound in oils, surfactants, and co-surfactants. Simplex lattice design methods can be used to obtain optimum formulation on SNEDDS.Key words: SNEDDS, Extract, Fraction, Mangosteen Peels, Simplex Lattice Design.Key message: Novelty in this research is the utilization of waste mangosteen peels in ethanol extract, ethyl acetate extract, ethyl acetate fraction, n-hexane fraction and residue designed SNEDDS. SNEDDS designed with the simplex lattice design route topical are something new. Additionally, it appeared that diffusion for in vitro release from these SNEDDS. This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.

Esterification of citric acid (CA) with locust bean gum (LBG) was prepared by hydrochloric acid (HCl) as a catalyst and UV irradiation (254 nm) as esterification energy. This study aims to determine the best conditions of esterification. Other than that, it is to know the effect of amount HCl and UV irradiation time for the esterification process of CA with LBG. The amounts of HCl are 0.18 and 0.30 M, while the variations of UV irradiation time are 75 and 100 minutes. Polyester (CA-LBG) were characterized by Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffractometer (XRD), esterification degree, and viscosity. Parameters for determining the best conditions for esterification are esterification degree and viscosity. The best conditions of esterification were obtained by using 0.30 M mL HCl and 100 minutes of UV irradiation time resulted in CA-LBG having a value of esterification degree 9.69 % and viscosity 7.46 cPs. HCl accelerates protonation on the O atoms and the formation of positive C atoms of carbonyl groups of citric acid. The time of UV irradiation gives the longer energy for the bond formation between the positive C atoms of the carbonyl group and the O atoms of the hydroxyl group at C-6 atoms of mannose and galactose.

ABSTRAK Penerapan basa kuat sebagai bahan curing telah banyak diterapkan dalam industri gelatin komersial, namun penerapan basa lemah belum banyak dilakukan. Penerapan basa kuat sebagai bahan curing tidak ekonomis dan diduga dapat berpengaruh bagi kesehatan manusia. Penelitian dilakukan untuk mempelajari sifat-sifat gelatin kulit kambing yang diproduksi menggunakan basa lemah jenis Ca(OH) 2 dan selanjutnya dibandingkan dengan sifat-sifat gelatin komersial. Kulit kambing dari jenis Bligon (hasil persilangan kambing etawah dan kacang) jantan umur 1,5-2,5 tahun digunakan sebagai bahan baku dan Ca(OH) 2 100 g/l sebagai bahan curing. Rancangan acak lengkap pola faktorial 2x3 dengan 3 ulangan digunakan sebagai desain penelitian. Dua waktu curing (2 dan 4 hari) dan tiga konsentrasi bahan (3, 6, 9% v/v) digunakan sebagai perlakuan serta gelatin komersial (murni oleh Merck, standar pangan dan standar farmasi) digunakan sebagai kontrol. Gelatin yang diproduksi dari kulit kambing menggunakan Ca(OH) 2 memiliki sifat yang mirip dengan gelatin komersial. Kadar logam berat (Pb, Cu, dan Zn) yang dikandung dalam produk gelatin kulit kambing masih memenuhi standar yang dipersyaratkan SNI. Produksi gelatin optimum dihasilkan dari penerapan waktu curing 4 hari pada konsentrasi 9% (v/v).

Purpose: To improve the solubility of simvastatin (SV) by co-crystallization using nicotinamide (Nic) as co-crystal agent (co-former

Solidification of liquid self-nano emulsifying drug delivery system (SNEDDS) formulation is required to enhance the feasibility and flexibility for further formulation processes. This study purposed to compare the soluble and insoluble carriers namely mannitol and fumed silica, respectively on the nano-emulsion formation and physical properties. The optimized SNEDDS formulation comprising of virgin olive oil, Tween 80, and PEG 400; and meloxicam was impregnated into solid carriers e.g. mannitol and fumed silica using a freeze-drying method. The physical mixture was carried out to compare the aforementioned method. Vibrational spectroscopy, thermal analysis, and morphological characteristic, droplet size and distribution, and drug release were performed to characterize the solid SNEDDS (S-SNEDDS). The result showed that crystallization of meloxicam did not observe in the S-SNEDDS formulations, which confirmed by the vibrational spectroscopy and thermal analysis. The morphological characteristic of S-SNEDDS was similar to the native carriers. The soluble carrier did not affect the formation of the nano-emulsion compared to the insoluble carrier. In addition, the S-SNEDDS enhanced the drug release of meloxicam up to 3-4 folds increment.

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