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.
Getah Jarak Tintir (Jatropha multifida Linn.) yang berasal dari famili Euphorbiaceae diketahui memiliki kandungan fenolik dan flavonoid yang berpotensi sebagai antioksidan alami. Penelitian ini bertujuan untuk mengetahui kandungan metabolit sebagai antioksidan, interaksi senyawa metabolit sekunder dalam getah jarak tintir dengan enzim tirosinase, dan mengaplikasikannya dalam bentuk sediaan. Metode pengujian antioksidan dilakukan dengan metode DPPH dan pengujian aktivitas inhibitor enzim tirosinase dilakukan dengan in silico metode molekular docking. Formulasi hand and body cream getah jarak tintir dibuat dalam tiga formula yaitu F0 (basis krim sebagai kontrol), F1 (basis krim dengan 100×IC50 serbuk getah jarak tintir), F2 (basis krim dengan 200×IC50 serbuk getah jarak tintir). Hasil penelitian menunjukkan bahwa senyawa yang mempunyai afinitas kuat dalam menghambat enzim tirosinase yaitu Multifidol dengan nilai ∆G sebesar -6,01 kkal/mol dan KI sebesar 39,37 nM. Hasil pengujian antioksidan dari hasil freeze drying serbuk getah jarak tintir menunjukkan nilai IC50 sebesar 8,33 µg/mL yang termasuk kategori sangat kuat. Persen inhibisi pada krim F1 (konsentrasi zat aktif 8,33 µg/mL) dan F2 (konsentrasi zat aktif 16,4 µg/mL) berturut-turut adalah 25,08% dan 50,57% yang termasuk kategori sangat kuat dan berpotensi sebagai alternatif krim pemutih. Kata kunci: Getah jarak tintir, molecular docking, krim, antioksidan, DPPH The sap of Jarak Tintir (Jatropha multifida Linn.) from the family Euphorbiaceae was known to contain phenolic and flavonoid compounds that have the potential as natural antioxidants. This study aimed to determine the content of metabolites as antioxidants, the interaction of secondary metabolites in Jatropha sap with tyrosinase enzymes, and to apply them in a dosage form. The antioxidant test method was carried out using the DPPH method and the tyrosinase enzyme inhibitory activity was tested using the molecular docking in silico method. The hand and body cream formulation of the sap was made in three formulas, namely F0 (cream base as control), F1 (cream base + 100×IC50 of the sap powder), F2 (cream base + 200×IC50 of the sap powder). The results showed that the compound that has a strong affinity to inhibit the tyrosinase enzyme is Multifidol with a ∆G value of -6.01 kcal/mol and a KI of 39.37 nM. The freeze-drying of the sap powder had the potential as an antioxidant with an IC50 value of 8.32 g/mL which was categorized as very strong activity. The percentage of inhibition in F1 cream (active substance concentration 8.32 g/mL) and F2 (active substance concentration 16.4 g/mL) were 25.08% and 50.57%, respectively, included in the very strong category and have potential to be alternative whitening cream. Keywords: the sap of Jarak tintir, molecular docking, cream, antioxidant, DPPH
Introduction: The formation of co-crystal is widely studied to obtain more favourable physicochemical properties than the pure active pharmaceutical ingredient (API). The co-crystal formation between an anti-fungal drug, fluconazole (FLU), and tartaric acid (TAR) has been investigated and its impact on mechanical properties has also been studied. Methods: The co-crystal of FLU-TAR (1:1) molar ratio was prepared by ultrasound-assisted solution co-crystallization (USSC) method with ethanol as the solvent. Polarization microscopy was used to observe the crystal morphology. Meanwhile, powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) methods were used to characterise the co-crystal formation. The mechanical properties of the co-crystal, such as flowability and tablet-ability, were compared with pure FLU. Results: Photomicroscopes revealed the unique crystal morphology of the USSC product was different from the two starting components. The typical PXRD pattern was shown by the USSC product, which indicated the formation of FLU-TAR co-crystal. In addition, the DSC thermogram revealed 169.2°C as the melting point of the FLU-TAR co-crystal, which is between the melting points of FLU and TAR. It indicates that FLU-TAR co-crystal has better flowability and tablet-ability than pure FLU. Conclusion: FLU-TAR co-crystal is one of the alternative solid forms for a raw material in pharmaceutical tablet preparation because it has better mechanical properties than pure fluconazole.
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.
Pati merupakan salah satu disintegran sediaan tablet yang berfungsi menghancurkan tablet sehingga zat aktif dapat dilepaskan. Tujuan penelitian ini untuk memanfaatkan pati hasil pregelatinasi dari buah sukun (Artocarpus altilis (Parkinson ex F.A.Zorn) Fosberg) sebagai bahan penghancur pada tablet eritromisin stearat (ERS). Penelitian diawali dengan mengidentifikasi kemampuan pati pregelatinasi buah sukun (PPBS) dengan melakukan uji swelling power dari pregelatinasi pati pada suhu 0, 60, 70, 80 dan 90oC. Pati yang memiliki swelling power yang paling baik dipilih sebagai bahan penghancur pada tablet ERS. Dalam penelitian ini dibuat 4 formula, yaitu F1 (ERS tunggal), F2 (ERS-PPBS, 9:1), F3 (ERS-PPBS, 7:3) dan F4 (ERS-PPBS, 1:1). Tablet dikempa langsung dengan alat kompaktibilitas (hydrolic press), selanjutnya tablet dievaluasi kekerasan, kerapuhan, kompaktibilitas dan waktu hancur tablet serta dikarakterisasi dengan scanning electron microscopy (SEM). Hasil penelitian menunjukkan bahwa penambahan pati pregelatinasi buah sukun dapat menurunkan nilai kekuatan tarik (tensile strength) campuran massa kempa. Fotomikrograf SEM menunjukkan penambahan pati pregelatinasi buah sukun dapat mencegah terjadinya sintering pada tablet ERS. Tablet campuran ERS-PPBS dapat meningkatkan waktu hancur dari pada tablet ERS tunggal. Waktu hancur paling cepat terjadi pada F4 yaitu pada 0,45±0,06 menit. Hasil ini mengindikasikan bahwa pati pregelatinasi buah sukun dapat mencegah terjadinya fenomena sintering dan meningkatkan waktu hancur tablet eritromisin stearat.
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