Clozapine (CLO) is an effective atypical antipsychotic to control the symptoms of psychosis and schizophrenia. Clozapine has low solubility and high permeability, so it is classified as a class II in the biopharmaceutical classification system. The aim of this study was to improve the solubility and dissolution rate of clozapine by clozapine-isonicotinamide (CLO-INA) co-crystal formation. CLO-INA co-crystal was prepared by solvent-drop grinding (SDG) method using water as a solvent. Characterization of SDG result was conducted by powder X-ray diffraction (PXRD) and Fourier transform infrared (FTIR). Solubility test was performed in water at room temperature. The dissolution test was performed in 900 mL of pH 6.8 phosphate buffer solution, 50 rotation per minute of paddle rotation, and at 37±0.5 °C. The PXRD pattern of SDG result of CLO-INA has many different peaks from its parent components, and this may indicate the co-crystal formation. The solubility of the co-crystal clozapine was fifteen folds higher than pure clozapine. The dissolution rate of CLO-INA co-crystal increased in the first 10 minutes compared to pure clozapine. Percentage of clozapine dissolved after 10 minutes from CLO-INA co-crystal and pure CLO were 10.2 and 2.4%, respectively. CLO and INA can form co-crystal by SDG method that can improve the solubility and dissolution rate of clozapine.Keywords: Clozapine, Isonicotinamide, Co-crystal, Solubility, Dissolution
The formation of co-amorphous is one alternative that can be attempted to enhance the solubility of drugs. The study aimed to identify the co-amorphous formation between candesartan cilexetil (CAN) and l-arginine (ARG) and to know its effect on the solubility and dissolution rate of candesartan cilexetil. Initial prediction of co-crystal formation was undertaken by observing differences in crystal morphology between the candesartan cilexetil-l-arginine (CAN-ARG) mixture and each of its initial components due to crystallization in ethanol. The CAN-ARG co-amorphous was produced by the liquid-assisted grinding (LAG) method with the same molar ratio of the CAN and ARG mixture using ethanol as solvent. The co-amorphous formation of CAN-ARG was identified by powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) methods. The solubility and dissolution test was performed to know the impact of the co-amorphous CAN-ARG formation. The PXRD pattern of CAN-ARG of LAG result showed a very low peak intensity compared to pure CAN and ARG. The DSC thermogram of the CAN-ARG LAG result does not show any sharp endothermic peaks. The PXRD and DSC results reveal that CAN and ARG can form co-amorphous. The solubility and dissolution rate of candesartan cilexetil in co-amorphous CAN-ARG was better than that of pure CAN. It can be concluded, liquid-assisted grinding of CAN-ARG mixture is identified to form co-amorphous which has an impact on increasing the solubility and dissolution rate of candesartan cilexetil.
Pirimetamin (PIR) adalah suatu obat antimalaria dengan kelarutan yang buruk di dalam air, sehingga ketersediaan hayatinya rendah. Pembentukan ko-kristal dapat mempengaruhi kelarutan dan laju disolusi bahan aktif farmasi tanpa mengubah aktivitas farmakologinya. Tujuan dari penelitian ini adalah untuk mengetahui pengaruh pembentukan ko-kristal pirimetamin (PIR) dengan asam fumarat(FUM) terhadap kelarutan dan laju disolusi pirimetamin. Ko-kristal PIR-FUM dibuat dalam perbandingan stoikiometri ekuimolar menggunakan metode penggilingan basah dengan menggunakan campuran pelarut aseton:air(1:1). Karakterisasi ko-kristal dilakukan dengan metode difraksi sinar-X serbuk, spektrofotometri infra merah, dan mikroskopik. Uji kelarutan dan uji laju disolusi dilakukan di dalam media air dan larutan dapar pH 1,2; 4,5; dan 6,8. Pola difraksi sinar-X serbuk hasil penggilingan basah berbeda dengan pola difraksi komponen-komponen murninya yang mengindikasikan terbentuknya ko-kristal PIR-FUM. Ko-kristal PIR-FUM mempunyai kelarutan dan laju disolusi lebih tinggi daripada pirimetamin murni.
Natrium diklofenak (Na-diklofenak) adalah obat anti inflamasi non steroid yang umumnya digunakan untuk penderita radang sendi. Namun, waktu paruh yang pendek sekitar 1-2 jam menyebabkan obat diberikan berulang kali dalam interval waktu yang pendek untuk pemberian secara oral. Oleh karena itu, tujuan penelitian ini yaitu memformulasi Na-diklofenak tablet sustained release menggunakan metolose 90 SH 4000 sebagai matriks. Untuk melihat pengaruh metolose 90 SH 4000 terhadap profil disolusi Na-diklofenak tablet sustained release, metolose 90 SH 4000 ditambahkan dengan perbandingan 0% (F0), 5% (F1), 10% (F2), 15% (F3), 25% (F4). Tablet Na-diklofenak dibuat dengan metode granulasi basah. Hasil disolusi menunjukkan formula F0, F1, F2 dan F3 dapat dicapai dalam waktu 120, 240, 300 dan 480 menit, berturut-turut, namun F4 tidak mencapai disolusi selama 480 menit. Bedasarkan USP 26, hanya F3 yang memenuhi syarat disolusi tablet sustained release.
The combination formulation of tuberculosis drugs may cause interactions if drugs are given simultaneously. Rifampin (RIF) decomposes in the stomach when given concurrently with isoniazid (INH), which results in a decrease in the bioavailability of RIF. The purposed is to make INH microcapsules using HPMCP HP-50 and HP-55 coatings to prevent these interactions. The process of making INH: HPMCP HP-50 and HP-55 (2:3) microcapsules was done by using solvent evaporation method. The entrapment efficiency of INH: HPMCP HP-50 and HP-55 (2:3) were 83.21% and 91.57%, respectively. The dissolution test of INH: HPMCP HP-50 and HP-55 microcapsules met the requirements of the Indonesian Pharmacopoeia Edition V. The FTIR results showed that there was no change either in the chemical composition of isoniazid or in the coating of the microencapsulation. Scanning Electron Microscopy (SEM) showed the active substance was well coated. This study resulted in a novel formula for microcapsules INH:HPMCP HP-50 and HP-55 (2:3) which can prevent the decomposition of RIF when given together with INH with a delayed release effect so that INH will be released in the intestine.
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