Optimasi Hidroksipropil Metilselulosa dan Carbopol terhadap Moisture Content dan Laju Pelepasan Patch Ibuprofen In Vitro (Optimization of Hydroxypropyl Methylcellulose and Carbopol for Moisture Content and Release Rate of Ibuprofen Patch In Vitro)

Ibuprofen is non steroidal antiinflammatory drug (NSAID) of the propionic acid class which is widely used for the treatment of rheumatoid arthritis. Ibuprofen patch is an effective approach evading ibuprofen's adverse effect in the GI tract and first pass effect. The function of polymer is to control the drug release from the patch. The aims of this study were to determine the effect of hydroxypropyl methylcellulose (HPMC) K4M and carbopol 934 combination on the moisture content (MC), in-vitro drug release, and to obtain the optimum formula of those polymers. Ibuprofen patch were prepared into three formulas based on simplex lattice design with the ratio of HPMC K4M : carbopol 934, that were 1 : 0, 0.5 : 0.5, and 0 : 1. Design expert software was used to obtain the optimum formula of both polymers. The results of this study showed that patch with HPMC K4M : carbopol 934 (0.5 : 0.5) gave the best MC and the in-vitro drug release. The optimum formula was HPMC K4M and carbopol 934 with the ratio of 0.5 : 0.5. Keywords: ibuprofen, patch, HPMC, carbopo

PENGARUH PERBEDAAN CHEMICAL PENETRATION ENHANCER PADA PENETRASI TRANSDERMAL PATCH PROMETAZIN HCL

This research aims is to create a promethazine HCl patch transdermal drug delivery systems with the most excellent penetration. Transdermal drug delivery can be efficiently used for the active agents which undergo rapid first pass metabolism and oral absorption is often disrupted by nausea and vomiting, hence the transdermal patches of promethazine HCl were prepared by using different penetration enhancers,  propylene glycol, oleic acid and isopropyl alcohol. The prepared formulations were evaluated for thickness, weight variation, moisture content, drug content, morphology, and in vitro permeation studies. The patch morphology studies were performed by Scanning Electron Microscopy (SEM). The amount of promethazine HCl transfered by propylene glycol  25.77 ± 3.0396 ug, isopropil alcohol 25.758 ± 2.9022 ug and oleic acid 25.017 ± 8.1300 ug. The penetration of promethazine HCl patch with oleic acid enhancer, produce the highest penetration than isopropil alcohol and propylene glycol. there was no difference in penetration using propylene glycol and isopropyl alcohol. Oleic acid is the best enhancer for preparations patch containing promethazine HCl although the amount of promethazine HCl contained is the least. The whole formulations comply with the  patch dosage requirement

FORMULA OPTIMIZATION OF ORALLY DISINTEGRATING TABLET CONTAINING MELOXICAM NANOPARTICLES

Meloxicam is one of oxicams anti-inflamatory drugs that are effective to relieve toothaches, arthritis, dysmenorrhea, and fever. Meloxicam in this study was milled with High Energy Milling (HEM) method to obtain its nano size and then direct compression method was used to produce Orally Disintegrating Tablet (ODT). ODT is designed to be rapidly dissolved on the tongue within a minute. It can be administered without water or chewing and may improve the bioavailability and effectiveness of the drug, and increase the patient’s adherence. The present study aimed to understand the effects of Ac-Di-Sol and Kollidon CL as superdisintegrants, that were used separately or in combination, on the characteristics of nanoparticles meloxicam ODT. It was also to obtain the best proportion of combination between Ac-Di-Sol and Kollidon CL that can produce the optimum formula of meloxicam ODT. The effects of single or combined superdisintegrants were evaluated using Simplex Lattice Design (SLD). Ac-Di-Sol (X1) and Kollidon CL (X2) were the independent variables, while the dependent variables were friability (Y1), disintegrating time (Y2), wetting time (Y3), and percent meloxicam release after 60 seconds (Y4). Optimization of five nanoparticle meloxicam ODT formulas was conducted using Design Expert 7.1.5. The combination of Ac-Di-Sol 4.05mg (X1) and Kollidon CL 10.95mg (X2) in 150mg nanoparticles meloxicam ODT can produce optimal ODT characteristics. After verification there was no difference between predicted value and observed value with p value > 0.05

Optimasi Tween dan Propilen Glikol dalam Self-Nanoemulsifying Drug Delivery System VCO-Minyak Daun Kemangi

Basil (Ocimum basilica) contains active compounds of essential oils that have volatile properties, so it will affect its antibacterial activity. SNEDDS was chosen as a delivery system to increase essential oil stability. The purpose of this study was to determine the effect of tween 80 concentration, propylene glycol, and their interactions in VCO on SNEDDS of basil leaf oil on response and to determine the antibacterial activity with optimum characteristics. Optimization of tween 80 and propylene glycol was conducted using the VCO oil phase with a factorial design method using design expert software 11 with the response used, namely% transmittance and emulsification time. Verification and characterization were carried out including organoleptic, pH, particle size, particle distribution, then tested for antibacterial activity. The results showed that an increase of tween 80 concentration and a decrease of propylene glycol would increase the transmittance value and decrease the emulsification time. There was no interaction effect between the two. Prediction software design expert 11 showed optimum formula with a clear yellow color appearance, the distinctive odor of basil oil, has an average pH of 6.81 ± 0.03, an average particle size of 19.7 ± 0.16 nm, a particle distribution with an average PDI average of 0.163 ± 0.05. The optimum formula with a concentration of 30 μl has activity against S. thypi with an average inhibition zone diameter of 17.21 ± 1.01 mm

Optimasi Hidroksipropil Metilselulosa dan Mentol pada Sediaan Gel Dispersi Padat Ibuprofen–Polietilenglikol dengan Metode Desain Faktorial (Optimization of Hydroxypropyl Methyl Cellulose and Menthol in Ibuprofen Gel Solid Dispersion-Polyethyleneglycol usi

Ibuprofen is included in non-steroidal anti-inflammatory drug (NSAID) which is used for the treatments of arthritis and inflammation. Ibuprofen gel is an effective approach evading ibuprofen's side effect in GI tract and first pass effect. The aims of this study was to determine the effect of HPMC and menthol combination on viscosity, penetration flux and to obtain the optimum formula.The gel evaluations were organoleptic testing, pH, viscosity, spreadibility test, assay of ibuprofen gel, and in vitro penetration rate. In vitro penetration testing used the paddle type dissolution tester. Furthermore ibuprofen which penetrated through rat skin were analyzed by UV-Vis spectrophotometer. Ibuprofen gel were prepared into four formulas based on factorial design and the data were analyzed using design expert trial 9.0.3. The viscosity testing of F1, Fa, Fb, and Fab were 183.30 ± 14.433,261.67 ± 16.07, 158.33 ± 7.637, and 310.0 ± 13.23 dPa.s. The in vitro penetration rate of F1, Fa, Fb, and Fab were 0.7225, 0.6716, 1.5587 And 1.0702 µg/cm2.minutes. It can be concluded that Fb has the optimum formula.   Keyword: optimization, HPMC, menthol, factorial design &nbsp

Optimasi Komposisi Polietilen Glikol dan Lesitin sebagai Kombinasi Surfaktan pada Sediaan Nanoemulsi Kafein (Optimization of Polyethylene Glycol and Lecithin Composition as Surfactant Combination in the Caffeine Nanoemulsion)

Caffeine is one of alkaloids that have the potential to skin cancer treatment. Caffeine is hydrophilic with log-P value of 0.07 that makes difficult to penetrate to the stratum corneum. Nanoemulsion is one of system which made to increase drug penetration. Oneof the important component in the nanoemulsion is a surfactant that acts as a unifier between the oil and water phases to form one phase that isotropic and thermodynamically stable. The presence of lipophilic component in the surfactant can affect the skin barrierdisturb, thus increasing penetration. The aims of this study was to find the best composition of the PEG-400 and lecithin as surfactant combination to obtain a nanoemulsion that is safe, stable, and increasing penetration of caffeine. The experiment was conducted using a factorial design method which observed responses of flux value and viscosity deviation. The viscosity deviation and flux were analyzed using Design Expert 10.0 trial to determine the optimal formula of caffeine nanoemulsion. The results obtained optimal formula of nanoemulsion that has composition of PEG-400 as 32% and lecithin as 7% . Prediction of viscosity deviation and flux value of optimal formula was 0,034 cP and 0.514 μg cm-2min-1.Keywords: caffeine, nanoemulsion, PEG-400, lecithin&nbsp

Optimasi Asam Glikolat dan Asam Sitrat dalam Krim Tabir Surya Kombinasi Titanium Dioksida, Avobenzone dan Octyl Methoxycinnamate

Ultraviolet (UV) radiation is the main cause of sunburn and skin cancer. The adverse effects of UV radiation are solved by sunscreen as protection for longer outdoors. In this study, optimization of glycolic acid and citric acid in sunscreen cream combination of titanium dioxide, avobenzone, and octyl methoxycinnamate were investigated using simplex lattice design method. The sunscreen cream evaluation includes physicochemical testing (organoleptic, homogeneity, emulsion type, spreadability, viscosity, and pH) and sunscreen effectiveness (SPF, % erythema transmission, and % pigmentation transmission). The value of physicochemical testing are 5,96 cm - 6,3 cm of  spreadability testing; 83,33 dPa.s – 108,33 dPa.s of viscosity testing; 4,06 – 4,67 of pH testing. The value of sunscreen effectiveness are 9,79 – 13,35 of SPF testing; 4,55x10-06 - 0,15x10-06% of % erythema transmission; 5,77 – 7,16 % of % pigmentation transmission. The optimum formula was obtained by combining glycolic acid 2% and citric acid 0% with a desirability value of 0,649

Pengaruh Propilen Glikol dalam Patch Dispersi Padat Ketoprofen terhadap Karakteristik Fisika Kimia dan Laju Penetrasinya

  Ketoprofen is a non steroid anti-inflammatory drug (NSAID) used as analgesic and anti-inflammation. This research had been done by ketoprofen patch preparation and evaluations aiming to enhance its penetration through the skin using propylene glycol as penetration enhancer. Evaluations included homogenity testing and FTIR for ketoprofen solid dispersion and organoleptic, weight uniformity, thickness, folding endurance, surface pH, moisture content, and penetration rate assay of ketoprofen patch. Penetration rate was determined by paddle type dissolution and the sample was analyzed by spectrophotometry UV-Vis. The value of moisture content and penetration rate were analyzed by One Way ANOVA with confidence level of 95 %. The value of moisture contents were F0 1.17 ± 0.0551 %; F1 1.27 ± 0.0208 %; F2 1.33 ± 0.08 %; and F3 1.43 ± 0.0208 %. The penetration rates of ketoprofen were F0 0.5258 ± 0.0191 µg/cm2.minute; F1 0.6935 ± 0.0613 µg/cm2.minute; F1 0.6935 ± 0.0613 µg/cm2.minute; and F3 1.1260 ± 0.0850 µg/cm2.minute. It can be concluded that the formula with propylene glycol 150 mg/patch can deliver the best penetration rate and moisture content that were fullfill the requirements.   Keywords: ketoprofen, patch, propilen glikol, penetratio enhancer, solid dispersion &nbsp

Optimasi Komposisi Polietilen Glikol dan Lesitin sebagai Kombinasi Surfaktan pada Sediaan Nanoemulsi Kafein (Optimization of Polyethylene Glycol and Lecithin Composition as Surfactant Combination in the Caffeine Nanoemulsion)

Caffeine is one of alkaloids that have the potential to skin cancer treatment. Caffeine is hydrophilic with log-P value of 0.07 that makes difficult to penetrate to the stratum corneum. Nanoemulsion is one of system which made to increase drug penetration. One of the important component in the nanoemulsion is a surfactant that acts as a unifier between the oil and water phases to form one phase that isotropic and thermodynamically stable. The presence of lipophilic component in the surfactant can affect the skin barrier disturb, thus increasing penetration. The aims of this study was to find the best composition of the PEG-400 and lecithin as surfactant combination to obtain a nanoemulsion that is safe, stable, and increasing penetration of caffeine. The experiment was conducted using a factorial design method which observed responses of flux value and viscosity deviation. The viscosity deviation and flux were analyzed using Design Expert 10.0 trial to determine the optimal formula of caffeine nanoemulsion. The results obtained optimal formula of nanoemulsion that has composition of PEG-400 as 32% and lecithin as 7% . Prediction of viscosity deviation and flux value of optimal formula was 0,034 cP and 0.514 µg cm-2min-1.   Keywords: caffeine, nanoemulsion, PEG-400, lecithin &nbsp

Optimasi Jumlah Etil Selulosa dan Kecepatan Pengadukan dalam Preparasi Hollow Microspheres Kaptopril

Captopril is an Angiotensin-Converting Enzyme inhibitor (ACE Inhibitor) used for the treatment of hypertension. It has been reported that the duration of antihypertensive action after a single oral dose of captopril is only 6–8 h, specific absorption in the stomach, stable at acidic pH and degraded at high pH. These indicate a promising potential of the captopril hollow microspheres system as an alternative to the conventional dosage form. The preparation method used in this study is non-aqueous solvent evaporation. This study aims to determine the amount of ethyl cellulose (EC) and stirring speed to produce hollow microspheres having entrapment efficiency (EE), buoyancy and particle size maximum. Determination of the optimum hollow formula microspheres captopril uses a design factorial of two factors at two levels. The factors used in this study were the amount of EC and stirring speed, while the observed response was EE, buoyancy and particle size. The chosen optimum formula will be verified and characterized (yield, SEM, FT-IR). Formula AB was the optimum formula with EE 90.68%, buoyancy 81.52% and particle size 267.10µm. The verification obtained results in accordance with the prediction of the Design-Expert software. The characterization results obtained a yield value of 98.33%, with a spherical shape, uneven surface morphology, and hollow core. The results of FT-IR analysis showed that there was no interaction between the drug and polymer used in the formulation