Permeasi Transdermal Losartan in Vitro Dari Larutan Dengan Variasi Kadar Losartan Dan Propilen Glikol

Losartan is an angiotensin receptor antagonis which has low oral bioavailability (0.25-0.35). Transdermal drug delivery system is needed as one solution for this low oral bioavailability drug. Propilen glikol (PG), as enhancer, is frequently added in transdermal dosage form. This research was purposed to explore the effect of PG as losartan permeation enhancer in various concentration of potasium losartan (k-los). The research was carried out in vitro using vertical tipe difusion cel for 4 formulas, i.e. 2% potasium losartan (k-los) :15% PG (F1), 10% k-los :15% PG (F2), 2% k-los :20% PG (F3), and 10% k-los: 20% PG (F4) using citric buffer pH 5 as donor medium, while PBS pH 7,4 was used as receptor medium. The dorsal skin of white wistar male rat was used as membrane. HPLC with UV detector was used to determine the concentration of k-los appear in receptor compartment. The results show that increasing of k-los concentration from 2% to 10% can increase the flux if PG concentration is 20%, but it does not have any significant effect to the flux if the PG concentration is 15%. Increasing PG concentration from 15% to 20% decrease the flux permeation in k-los concentration of 2%, and does not have any significant effect in concentration of k-los of 10%. The lag time permeation does not has any significant differencess. It means that PG as enhancer in the concentration above 15% doesn't have any adventages

Formulasi Matriks Transdermal Pentagamavunon-0 dengan Kombinasi Polimer Pvp K30 dan Hidroksipropil Metilselulosa

Transdermal delivery system is one of the delivery system for Pentagamavunon-0 (PGV-0) to avoid the high intensity of first pass metabolism of PGV-0 in peroral route. The purpose of this research was to optimize the formula of PGV-0 transdermal matrix with a combination of PVP K30 and HPMC polymers.The simplex lattice optimization approach of the transdermal matrix formulas was performed by using Design Expert 7.1.5 software. The visual appearance, weight, thickness, moisture content, moisture uptake, folding endurance, drug content, and dissolution efficiency of the release profil of PGV-0 from the matrix for 6 hours were evaluated as responses to determine optimum formula of matrix. The result showed that a combination of PVP K30 and HPMC polymers had a significant influence on the visual appearance, moisture content, and dissolution efficiency of PGV-0. Combination of 1.98% of PVP K30 and 4.52% of HPMC as the optimum formula could produce homogeneous and flexible matrix with moisture content of 3.21%. The dissolution efficiency was 9.11%, indicating that 101.93 µg of PGV-0 was released from the optimum formula during 6 hours

Pengaruh Medium Dissolusi Dan Penggunaan Sinker Terhadap Profil Disolusi Tablet Floating Aspirin

Disolusi merupakan faktor penting dalam pelepasan dan pengembangan sediaan obat. Selain sifat fisika kimia obat, formulasi, dan fabrikasi sediaan; kondisi uji disolusi juga mempengaruhi profil disolusi termasuk jenis medium dan model alat uji. Tujuan penelitian ini adalah untuk mengetahui pengaruh medium disolusi dan penggunaan sinker terhadap profil disolusi tablet floating aspirin. Tablet dibuat dengan metode cetak langsung dengan bahan tambahan Methocel K4M CR, NaHCO3, Ethocel, Aerosil, dan dikalsium fosfat anhidrat. Tablet diuji disolusi menggunakan alat disolusi USP apparatus 2 dengan pengaduk dayung. Medium disolusi yang digunakan yaitu simulated gastric fluid (SGF) tanpa pepsin pH 1,2 dan HCl 0,1 N. Uji disolusi dengan SGF tanpa pepsin pH 1,2 dilakukan dengan dan tanpa sinker. Suhu percobaan 37 ± 0,5 °C dan kecepatan pengadukan 60 rpm. Cairan sampel diambil pada menit ke-15, 30, 45, 60, 90, 120, 180, 240, 300, 360, 420, dan 480. Serapan sampel diukur dengan spektrofotometer UV pada λ 280 nm. Hasil uji disolusi menunjukkan bahwa perbedaan medium yaitu HCl 0,1 N dan SGF tidak mempengaruhi DE480, kinetika, dan mekanisme disolusi tablet floating aspirin. Penggunaan sinker pada medium SGF mempengaruhi DE480, kinetika, dan mekanisme disolusi. Kurva disolusi tablet floating aspirin pada medium HCl 0,1 N, SGF dengan dan tanpa sinker mengikuti kinetika orde I dan mekanisme disolusi menurut model Korsmeyer-Peppas, Weibull, Hopfenberg, dan Hixson-Crowell. Model Higuchi juga sesuai untuk profil disolusi tablet floating aspirin dalam medium SGF dengan sinker. Kata kunci: tablet floating aspirin, medium disolusi, sinker, profil disolusi ABSTRACK Dissolution is an important factor in the release and development of drug dosage form. In addition to physical and chemical properties of the drug, formulation, manufacturing process; the conditions of dissolution test also affect the profile of dissolution including the type of medium and test equipment models. The purpose of this study was to determine the influence of the dissolution medium and the use of sinker on dissolution profile of aspirin floating tablet. The tablets were made by direct compression method with Methocel K4M CR, NaHCO3, Ethocel, Aerosil, and dicalcium phosphate anhydrous as excipients. The in vitro dissolution study was determined using USP apparatus 2 (paddle method), 900 mL dissolution medium at 37 ± 0.2 °C and 60 rpm. The dissolution test using HCl 0.1 N and simulated gastric fluid (SGF) pH 1.2 as medium with and without a sinker. Aliquouts of 5 mL was taken out at intervals of 15, 30, 45, 60, 120, 180, 240, 300, 360, 420, and 480 minutes. The samples were analyzed by UV-Vis spectrophotometer at 280 nm. The result indicated that the difference of medium (HCl 0.1 N and SGF pH 1.2) does not affect DE480, kinetics, and mechanism of dissolution. The use of sinker in SGF affects DE480, kinetics, and mechanism of dissolution. The profile of dissolution of aspirin floating tablets in 0.1 N HCl and SGF pH 1.2 (with and without sinker) follow first-order kinetics and mechanism of dissolution according to Korsmeyer-Peppas, Weibull, Hopfenberg, and Hixson-Crowell models. Higuchi model was also suitable for dissolution profile of aspirin floating tablet in the SGF pH 1.2 with sinker. Keywords: floating tablet of aspirin, medium of dissolution, sinker, profile of dissolutio

Validasi Metode HPLC Untuk Penetapan Aspirin Dan Asam Salisilat Dalam Plasma Kelinci (Lepus Curpaeums) Secara Simultan

Aspirin is a nonsteroidal anti-inflammatory drug which also has the effect of antiplatelet for stroke prevention. Aspirin inside human body is very easy to break down into salicylic acid as the main metabolite. The aim of this study is to develop and validate the method for determinating aspirin and salicylic acid concentration in plasma by HPLC. Method validation including system suitability test, linearity test, determination of LOD and LOQ, recovery, accuracy and precision. Concentration of analytes in blood is measured by HPLC using benzoic acid as internal standard, with condition Purospher column Endcapped Star RP-18 (250 x 4.6 mm id, 5 m), acetonitrile : buffer phosphate 20 mM pH 2.5 (30:70 v/v) as mobile phase, injection volume 20 mL, flow rate 1.5 mL/minute, and UV-Vis detector λ 230 nm. The results showed that the proposed method meets the requirements of system suitability and good linearity (r > 0,990) with LOQ (aspirin = 0.024 mg/mL, salicylic acid = 0.336 mg/mL) and LOD (aspirin = 0.007 mg/mL, salicylic acid = 0.101 mg/mL). The method of analysis provides recovery of 85-115 %, accuracy and precision in accordance with the requirements for bioanalytical with CV < 5 %. Therefore, the proposed method is applicable to determine of aspirin and salicylic acid concentration in plasma

Optimization Of Mixing Temperature And Sonication Duration In Liposome Preparation

Liposomes are a delivery system used in pharmaceutical products and cosmetics. Liposomes have many advantages such as increase stability and efficacy, can be targeted to reduce toxicity and increase accumulation at the target site and are biocompatible. Preparation of liposomes can be done by conventional or new methods which are still being developed. Conventional methods often require a long time and organic solvents which may be toxic. Heating (Mozafari method) is one of the new methods developed in the manufacture of liposomes without organic solvents. Mixing temperature can affect the physical properties of liposomes. The particle size has become one of the important physical properties because it affects the absorption of the drug. Sonication is an easy method of choice in reducing the size of liposomes. Optimization of mixing temperature and duration of sonication in liposomes' preparation using new heating methods and sonication were performed by factorial design with 2 factors and 3-levels to obtain optimal liposome size. Data were analyzed with two-way ANOVA. The results showed that both mixing temperature and sonication duration significantly affect liposome size, but the interaction was not statistically significant. Data analysis also showed that mixing temperature, sonication, and their interaction do not affect the polydispersity index of liposome. Results showed the optimum mixing temperature and sonication duration that can produce liposomes with size below 100 nm is at 60°C for 30 minutes

The Comparison Of Extraction Method And Solvent Variation On Yield And Antioxidant Activity Of Brassica Oleracea L. Var. Capitata F. Rubra Extract

Red Cabbage (Brassica oleracea L. Var. Capitata f. rubra) has a high anthocyanin content therefore it can be potential as a natural antioxidant. In this research, the antioxidant activity of the red cabbage extract was evaluated quantitatively with a spectroscopy method using DPPH reagent to obtain the value of IC50 . This research was divided into 2 stages. First, the influence of solvent variant to the extract yield of red cabbage powder and the maximum wavelength (λ) using a maceration protocol. The kind of solvent (70%, 80%, 95%, and 96% of ethanol) with addition 3% of citric acid. Second, the influence of extraction methods in neutral condition to the antioxidant activity. The results show the red cabbage powder maceration with 96% ethanol solvent (acid condition) exhibits the highest yield. The fresh red cabbage soxhletation with 96% ethanol (neutral condition) exhibits 288,5 nm maximum wavelength (λ) and 168,78 mg/mL of IC50 value