Pemanfaatan produk herbal di Indonesia semakin berkembang sejak tahun 2008. Daun kumis kucing (Orthosiphon stamineus), rimpang temulawak (Curcuma xanthorrhiza), dan herba pegagan (Centella asiatica) memiliki khasiat dalam mengatasi hipertensi ringan, namun masih memiliki rasa yang kurang enak. Oleh karena itu, pada penelitian ini dilakukan pengembangan produk herbal yang inovatif berupa granul yang dibuat dengan metode granulasi kering dengan pengisi Maltodextrine dan Spray Dried Lactose (SDL). Pada formula 1 menggunakan Maltodextrine, formula 2 menggunakan SDL, dan formula 3 menggunakan kombinasi dari kedua pengisi (1:1 w/w). Tujuan penelitian ini adalah untuk menentukan pengaruh jenis pengisi terhadap mutu fisik granul herbal. Data mutu fisik dianalisis statistik menggunakan metode oneway ANOVA (α = 0,05). Hasil penelitian menunjukkan bahwa pengisi maltodextrine memberikan mutu fisik (terutama pada sifat alir granul) yang lebih optimal apabila dibandingkan dengan menggunakan pengisi spray dried lactose atau kombinasi keduanya.
Objective: This research aims to prepare cocrystal of acyclovir (ACV)-nicotinamide (NCT) by solvent evaporation with a variation of solvent (ethanol, glacial acetic acid, and HCl 0.1 N) to improve the bioavailability of ACV as an antiviral drug. Methods:Cocrystal were developed by solvent evaporation with 1:1 molar fraction, using variation of solvent such as ethanol, glacial acetic acid, and HCl 0.1 N. Further, the prepared ACV-NCT cocrystal were characterized for differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), and in vitro dissolution.Results: DSC thermogram showed that ACV-NCT cocrystal in ethanol and glacial acetic acid exhibited new endothermic peak at 221.16°C and 216.40°C, whereas no peaks were found for HCl 0.1 N. PXRD diffractogram showed that ACV-NCT cocrystal in ethanol exhibited new diffraction peaks at 2θ 5.9°; 9.2°; dan 13.3°, whereas no peaks were found for glacial acetic acid and HCl 0.1 N. FT-IR characterization of ACV-NCT cocrystal in ethanol showed disappearance of transmission peaks at 3373/cm indicating the loss of NH bands of NCT. Furthermore, C=O of ACV and NCT were observed at 1693/cm, and 1666/cm indicated a formation of hydrogen bonding between ACV and NCT. SEM micrographs showed that cocrystals have a different shape compared to ACV and NCT. DE 15 showed that there was a significant increase of ACV-NCT cocrystal dissolution rate in ethanol compared to the physical mixture and ACV. Conclusion:The study concludes that ACV-NCT cocrystal in ethanol were successfully formed and the dissolution rate of ACV can increase significantly (α=0.05).
The development of oral dissolving film (ODF) of atenolol is an attempt to enhance convenience and compliance for geriatric patients suffering from hypertension. Film former is the most essential component in ODF that determines the physical characteristic and drug release. In this study, three different types of film former including HPMC E5 4% (w/v), 5% (w/v), CMC-Na 3% (w/v), 4% (w/v), and Na-alginate 2.5% (w/v), 3% (w/v) were optimized in Formula 1 (F1) to Formula 6 (F6), respectively. A solvent casting method was employed to develop ODF of atenolol. The films formed by HPMC E5 produced a smooth and flexible surface, whereas CMC-Na and Na-alginate produced gritty textured films. Satisfactory results were obtained from several physical parameters such as film thickness, folding endurance, swelling index, and disintegration time. The homogeneity, drug content, and dissolution properties of ODF with HPMC exhibited better characteristics than the other formulas. Formula 1 exhibited the highest drug release compared to the other ODFs. The molecular docking results showed that there was a hydrogen bonding between atenolol and film formers which was also supported by the FTIR spectrum. The findings of this study suggest that HPMC E5 is the most favorable film former for ODF of atenolol.
Asiklovir (ASV) merupakan antiviral dengan bioavailabilitas oral yang rendah oleh karena sifat kelarutannya yang kurang baik. Pembentukan kokristal farmasi merupakan salah satu modifikasi padat yang dapat digunakan untuk meningkatkan kelarutan. Nikotinamida (NKT) merupakan bahan koformer berupa vitamin larut air yang memiliki potensi untuk berikatan dengan ASV membentuk kokristal ASV-NKT. Pembentukan kokristal secara umum dapat dilakukan dengan metode penguapan pelarut, akan tetapi kurang efisien dalam pembuatan skala besar. Oleh karenanya, telah dikembangkan beberapa metode lain yaitu metode grinding dan slurry. Kokristal ASV-NKT selanjutnya dibentuk menggunakan tiga metode yang berbeda yaitu penguapan pelarut, grinding dan slurry serta dianalisis menggunakan difraksi sinar-x serbuk, Differential Scanning Calorimeter (DSC) dan uji disolusi in vitro. Pengujian menggunakan difraksi sinar-x serbuk dan DSC menunjukkan adanya pembentukan fase padat baru yaitu kokristal walaupun belum menunjukkan hasil yang optimal. Akan tetapi, pembentukan kokristal ASV-NKT metode penguapan pelarut dan slurry memberikan efek peningkatan disolusi ASV pada media dengan pH 6,8. Peningkatan disolusi tersebut tidak didapatkan pada pembentukan kokristal ASV-NKT dengan metode grinding. Oleh karenanya dapat disimpulkan bahwa pembentukan kokristal ASV-NKT mendapatkan hasil lebih optimal dengan menggunakan metode penguapan pelarut dan slurry dibandingkan metode grinding.
Antioxidants are compounds to resist free radicals. The natural antioxidant group that is currently being developed is the flavonoid group, one of which is quercetin. Quercetin has a low solubility, so it can be increased by reducing the particle size. This study aims to determine the differences that are influenced by the combination of chitosan polymer and sodium tripolyphosphate as matrix forming quercetin microparticles on the physical characteristics of the results made using the orifice ionic gelation method. The resulting preparation showed a particle size of 1326.33 nm; 3497.33 nm; and 6000 nm at various concentrations of 0.2% chitosan and 0.1%; 0.2%; and 0.3% sodium tripolyphosphate, respectively. The Fourier Transform Infrared (FTIR) results showed that there was no change in the marker group on quercetin and an ionic bond was formed between chitosan and sodium tripolyphosphate. The X-ray Diffractometer (XRD) results showed that the crystalline structure of quercetin changed to become more amorphous. Although the Scanning Electron Microscope (SEM) results, it is seen that the quercetin microparticles produced are needle-shaped, especially when the concentration of sodium tripolyphosphate is increased. Based on the results of these physical characteristics, it can be proven that the microparticle was formed at various concentrations of the polymer concentration combination with the best characteristics are on 0.2% chitosan and 0.1% sodium tripolyphosphate concentration.
PREPARATION OF ACYCLOVIR-ISONICOTINAMIDE COCRYSTAL BY SOLVENT EVAPORATION METHOD WITH METHANOL AND ISOPROPANOL. Acyclovir is a nucleoside synthetic analog antiviral group used in the treatment of Herpes simplex virus (HSV-1 & HSV-2) and Varicella zoster virus (VZV). Acyclovir has low water solubility, so it needs to be modified in the form of cocrystal with isonicotinamide. This study aims to obtain the physical characteristics produced by acyclovir-isonicotinamide cocrystal (1:1) made through the solvent evaporation method with methanol and isopropanol. The crystalline formed is characterized by DSC, PXRD, FT-IR and SEM. The characterization results showed the presence of new crystals that formed between acyclovir-isonicotinamide in methanol and isopropanol solvents. Thermograms showed sharp exothermic peaks at 183.31°C and 186.24°C. The diffractogram showed a new peak at 2θ = 5.19 and 5.82. The spectrum showed a shift in wavelength in the cocrystal formed. The cocrystal has a different morphology compared with parent drug and coformer on analysis using SEM. This research shows that acyclovir can form cocrystal with isonicotinamide by solvent evaporation method with methanol and isopropanol.
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