Tedjo Yuwono
Faculty of Pharmacy Universitas Gadjah Mada Yogyakarta

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THE SULPHAMETHOXAZOLE BIOAVAILABILITY OF POLYMORPH IIA IN RABBITS Siti Nurasiyah; Tedjo Yuwono
Indonesian Journal of Pharmacy Vol 12 No 4, 2001
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (96.784 KB) | DOI: 10.14499/indonesianjpharm0iss0pp205-210

Abstract

Sulphamethoxazole, a sulphonamide antibacteria, is usually combined with trimetoprime, namely cotrimoxazole, to obtain higher potency. Because of the solubility of sulphamethoxazole in water is minute, its dissolution rate would be slow. Consequently, dissolution rate become the limiting step in the absorption process. In order to overcome this problem, therefore, some polymorph forms of sulphamethoxazole were created. The previous study found a polymorph IIA crystal form, a new modified internal crystal structure of sulphamethoxazole. This study was a continuing investigation of the bioavailability of the polymorph IIA, in capsule dosage forms, in rabbits. It was evident that the bioavailability of polymorph IIA was twice of that polymorph I. The bioavailability parameter changes of polymorph I to polymorph IIA were: the AUC increased from 872 to 1,530 mg hr L-1, the peak time (tmax) increased from 2 hours to 0.9 hours, the blood plasma level peak (Cpmax) increased from 104 to 136 mg/ L-1. Key words: bioavailability, sulphamethoxazole polymorph
A COMPARATIVE BIOAVAILABILITY OF FUROSEMIDE IN SOLID DISPERSIONS FORMS Yandi Syukri; Lukman Hakim; Tedjo Yuwono
Indonesian Journal of Pharmacy Vol 12 No 1, 2001
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (86.704 KB) | DOI: 10.14499/indonesianjpharm0iss0pp28-32

Abstract

Furosemide is a poorly soluble diuretic drug, the solubility of which can be enhanced by solid dispersion with polyvinylpirolidon (PVP). The solid dispersion system was prepared by a solvent method in various ratios of 1 : 5 and 1 : 7 of the drug and PVP, respectively, in order to improve furosemide bioavailability. The bioavailability of furosemide - PVP solid dispersion was compared with pure furosemide (control) and Lasix (reference). The study was done in a cross over design with a single-dose peroral that administered to the white male rabbits (n = 6). Furosemide blood levels were determined spectrofluorometrically by an extraction method. The area under the blood concentration-time curve AUC0 - , peak blood concentration Cmax and time to reach peak blood concentration Tmax were used to compare their bioavailabilities. The solid dispersion systems produced a higher extent of bioavailability than pure furosemide (P < 0,05). On the contrary, no statistically significant difference about the extent of bioavailability between solid dispersion and Lasix (P > 0,05). Finally, furosemide – PVP solid dispersion (1 : 7) was the best formulation with the highest extent of bioavailability and bioequivalence with the Lasix formula.Key Word : Solid dispersion, solubility, dissolution, bioavailability, furosemide.
PREFORMULATION OF DICLOFENAC SODIUM SUSTAINED RELEASE BY ION EXCHANGER RESINE A. Karim Zulkarnain; Tedjo Yuwono; Sumarno .
Indonesian Journal of Pharmacy Vol 12 No 1, 2001
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (83.534 KB) | DOI: 10.14499/indonesianjpharm0iss0pp20-27

Abstract

The aim of the study was to find out a formula of granules giving a constant release of drug and also to search for the influence of pH on the drug release from the formula. One type of drug-resin complexes was used in this study ion exchanger the complex of diclofenac sodium and dowex. After 12 hours mixing the drug-resin complex was dried at 40 oC in an oven for 3 days. Afterwards, they were granulated and shieved. The particle size used were 20-40 mesh. The granules were tested for the dissolution of diclofenac sodium from the granules. The dissolution experiments were performed in a modified model of USP XX and the dissolution media used were phosphate buffer with the pHs of 5,8; 6,8 and 7.6 and the temperature was maintained at 37 oC. The amount of diug released in to the medium was assayed spectrophotometrically. The extent of dissolution was expressed as dissolution efficiency in 8 hours (DE8, % ). The results showed that the extent of dissolution of dtclofenac sodium from the granules complexed with the resin were low. The correlation between the amount of drug release from the complex and time was linier with the highest coefficient correlation having the ratio of l:5. The higher the pH values of the media, the higher the drug release from granules was. The drug release from drug-resin complex was well controlled which may be used for making a sustained release dosage form.Key Word : sustained release, diclofenac sodium, ion exchanger resin, granules