Physical Stability Test Research Articles

Antibacterial Tests Against Acne in vitro, the Physical Stability and Patch Test using Cream Containing Ethyl p-methoxycinnamate Extracted from Kaempferia galanga L., Rhizoma

Antibacterial Tests Against Acne in vitro, the Physical Stability and Patch Test using Cream Containing Ethyl p-methoxycinnamate Extracted from Kaempferia galanga L., Rhizoma

Accelerated Physical Stability Testing of Amorphous Dispersions.

The goal was to develop an accelerated physical stability testing method of amorphous dispersions. Water sorption is known to cause plasticization and may accelerate drug crystallization. In an earlier investigation, it was observed that both the increase in mobility and decrease in stability in amorphous dispersions was explained by the "plasticization" effect of water (Mehta et al. Mol. Pharmaceutics 2016, 13 (4), 1339-1346). In this work, the influence of water concentration (up to 1.8% w/w) on the correlation between mobility and crystallization in felodipine dispersions was investigated. With an increase in water content, the α-relaxation time as well as the time for 1% w/w felodipine crystallization decreased. The relaxation times of the systems, obtained with different water concentration, overlapped when the temperature was scaled (Tg/T). The temperature dependencies of the α-relaxation time as well as the crystallization time were unaffected by the water concentration. Thus, the value of the coupling coefficient, up to a water concentration of 1.8% w/w, was approximately constant. Based on these findings, the use of "water sorption" is proposed to build predictive models for crystallization in slow crystallizing dispersions.

Impact of glucose polymer chain length on heat and physical stability of milk protein-carbohydrate nutritional beverages

This study investigated the impact of glucose polymer chain length on heat and physical stability of milk protein isolate (MPI)-carbohydrate nutritional beverages containing 8.5% w/w total protein and 5% w/w carbohydrate. The maltodextrin and corn syrup solids glucose polymers used had dextrose equivalent (DE) values of 17 or 38, respectively. Increasing DE value of the glucose polymers resulted in a greater increase in brown colour development, ionic calcium, protein particle size, apparent viscosity and pseudoplastic rheological behaviour, and greater reduction in pH, hydration and heat stability on sterilisation at 120°C. Incorporation of glucose polymers with MPI retarded sedimentation of protein during accelerated physical stability testing, with maltodextrin DE17 causing a greater reduction in sedimentation velocity and compressibility of sediment formed than corn syrup solids DE38. The results demonstrate that chain length of the glucose polymer used strongly impacts heat and physical stability of MPI-carbohydrate nutritional beverages.

Karakterisasi dan Stabilitas Fisik Mikroemulsi Tipe A/M Dengan Berbagai Fase Minyak

This research consists of formulation, characterization and physical stability of the microemulsion of water-in-oil type. On the microemulsion, VCO, palm oil, olive oil and soybean oil were used as oil phase, aqua demineralisata used as the aqueous phase, a combination of Span® 80 and Tween® 80 as a surfactant and propanol as cosurfactant. Each formula was made three times replication and determined the physical characteristics including organoleptic observations, measurements of density, droplet, viscosity, flow properties, and pH. Determination of physical characteristics was done at the beginning of the microemulsion formed and after 5 weeks storage at room temperature. The physical stability test including the centrifugation test at 10,000 rpm for 30 minutes, the freeze-thaw test for 6 cycles, and heating stability with the oven temperature of 60oC, 70oC, 80oC, 90oC and 100oC for 5 hours were done. The data were analyzed using t-Test and one-way ANOVA. Based on the characteristic and physical stability tests, it showed that microemulsion with VCO, palm oil and soybean oil had better physical characteristics and stability compared to the microemulsion with olive oil.

Vitamin A palmitate-bearing nanoliposomes: Preparation and characterization

Abstract The encapsulation of fat soluble vitamins in nanoliposomes seems to be an effective method for protecting them from light, oxygen and chemical degradation. In this study, nanoliposomes containing vitamin A palmitate were prepared from different concentrations of lecithin–cholesterol (60:0, 50:10, 40:20 and 30:30 mg) by thin-film hydration–sonication method. Fourier transform infrared spectra (FTIR) were utilized to study the possible bioactive–lipid complex formation and the results indicated that the complex between vitamin A and liposomes were formed by physical interaction. Particle size, morphology, encapsulation efficiency and physical stability tests were carried out to determine the physicochemical properties of the resulted vitamin A-bearing liposomes. The size of particles were in the range of 76–115 nm and the particle size distributions were monomodular (span=0.6–0.88). The results showed that using the highest cholesterol concentration for preparing of liposomes containing vitamin A palmitate induces lower encapsulation efficiency and 50/10 mg lecithin–cholesterol concentration was used for preparation of optimum formulation of vitamin A palmitate-loaded nanoliposomes with mean size of about 76 nm and monomodular size distribution (span=0.74) and the encapsulation efficiency was 15.8%.

Formulasi dan Uji Stabilitas Fisik Sediaan Gel Ekstrak Daun Ketepeng Cina (Cassia alata L.)

Cassia alata L. leaf contains flavonoids which have anti-inflammatory, anti-allergy, antioxidants and antifungal effects. The traditional application of it requires long preparation time so we need a formulation with more practical and durable storage is needed. Gel formulation was chosen because it is easy to dry, forming an easy to wash film layer and give a sense of cold on the skin. Gel components affect the stability of the gel. Physical stability is analyzed to ensure that the formulated gel’s quality, safety and benefits meet the specifications and survive during storage. This study aimed to create a gel formula and analysed its physical stability test of Cassia alata L. leaf extract gel. Research design adopted in this study was an experimental laboratory. Optimum gel formula determined by variations in the concentration of sodium carboxymethyl celulose (CMC-Na). Gel that meet the criteria of homogeneity, consistency, pH and spreadibility was set as the optimum formula. Physical stability of optimum formula was analyzed by organoleptic, homogeneity test, pH test, viscosity test and spredability test. Gel that meets the acceptance criteria are Cassia alata L. leaf extract gel with CMC-Na concentration of 3% those determined as the optimum formula. Stability analysis of optimum formula didn’t show any changes in pH, color, smell and taste, although it changes of the shape, viscosity and spreadibility were found. The optimum formula gel obtained by the concentration of CMC-Na 3%. results were less stable during the 8 weeks of storage at a temperature of 40°C.

Degradation of Vitamin E in Nanoemulsions during Storage as Affected by Temperature, Light and Darkness

Abstract Vitamin E (VE) nanoemulsions confront physical instabilities and chemical degradation during processing and/or storage. Therefore, thermal stability and degradation kinetics of VE in nanoemulsions fabricated using low-energy emulsification method as a function of temperature under light and in the dark were studied. Nanoemulsions had small droplet diameter (≈110 nm). The thermal degradation of VE followed the first-order kinetics with samples heated at 75°C and above presenting the highest degradation rate and short half-life (5.22 min). The degradation of VE in long-term storage fitted the Weibull model with highest degradation in nanoemulsions stored under light at 40°C. However, VE retained in nanoemulsions after certain period of time might be boosted up when nanoemulsions are stored in the dark. Results showed that the physical stability tests alone are not enough to judge the stability of VE delivery systems, as the encapsulated VE might be lost during processing and storage.

Preparation of gelatin based porous biocomposite for bone tissue engineering and evaluation of gamma irradiation effect on its properties.

Biodegradable porous hybrid polymer composites were prepared by using gelatin as base polymer matrix, β-tricalcium phosphate (TCP) and calcium sulfate (CS) as cementing materials, chitosan as an antimicrobial agent, and glutaraldehyde and polyethylene glycol (PEG) as crosslinkers at different mass ratios. Thereafter, the composites were subjected to γ-radiation sterilization. The structure and properties of these composite scaffolds were characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), mechanical properties testing (compressive, bending, tensile and impact), thermogravimetry/differential thermal analysis (TG/DTA), and physical stability test in simulated body fluid (SBF). We found that TCP rich composites showed enhanced mechanical properties among all the crosslinked composites. γ-Radiation sterilization triggered further cross linking in polymer matrix resulting a decrease in pore size of the composites and an increase in pore wall thickness with improved mechanical and thermal properties. The chemically crosslinked composite with 40% TCP followed by γ-radiation sterilization showed the smallest pore size distribution with a mean pore diameter of 159.22μm, which falls in the range of 100-350μm - known to be suitable for osteoconduction. Considering its improved mechanical and thermal properties along with osteoconduction ability without cytotoxicity, we propose this biocomposite as a viable candidate for bone tissue engineering.

ANTI-ACNE (Acne Vulgaris) EMULGEL FORMULATION of AROMATIC OIL From PATCHOULILEAVES (Pogostemoncablinbenth) Andin VITRO ANTIBACTERIAL ACTIVITY TEST Againstpropionibacterium Acnes

ANTI-ACNE (Acne Vulgaris) EMULGEL FORMULATION of AROMATIC OIL From PATCHOULILEAVES (Pogostemoncablinbenth) Andin VITRO ANTIBACTERIAL ACTIVITY TEST Againstpropionibacterium Acnes Dra. Rr. Sulistiyaningsih, M.Kes., Apt; Dra. Emma Surahman, M.Si., Apt; Puti Lenggogeni Abstract Patchouli leaves (Pogostemon cablin Benth) aromatic oil containsalcoholic patchouliwhich has antibacterial activity. This research aim is to get an effective, safe, and stable antiacne emulgel preparation from patchouli leaves (Pogostemon cablin Benth) aromatic oil especially during storage time. Concentration of patchouli leaves (Pogostemon cablin Benth) aromatic oil used in the anti-acne emulgel preparation is 0.2%; 0.3%; and 0.4% (v/v). Stages of research that has been done are materials collection, antibacterial activity test of aromatic oil, fetermination of minimum inhibitory concentration, emulgel basis selection, emulgel formulation, physical stability test including organoleptic checking, viscosity and pH measurement, antibacterial preparation activity test for 30 days of storage times and preparation safety test. Results from the research showed that all of the anti-acne emulgel preparations had good quality and didnot trigger any inflammation or irritation on the user skin. Full Text: PDF DOI: 10.15640/ijmp.v3n2a5

Uji Stabilitas Fisik Formula Krim yang Mengandung Ekstrak Kacang Kedelai (Glycine max)

Soybean extract has known for its antiaging potential. The addition of soybean extract was predicted can influence the physical stability of the cream. Therefore, this research was aimed to test the physical stability of cream contained soybean extract in different concentration (2%, 4%, 6%, and 8%). The physical stability test including the storage for eight weeks at room temperature, high temperature (40°±2°C), and low temperature (4°±2°C). Stability parameters were the organoleptic observation, pH, globul size, viscosity, and cycling test. Those four cream formula showed good stability in organoleptic, pH, globul size, viscosity, and cycling test.

Enhanced effectiveness of tocotrienol-based nano-emulsified system for topical delivery against skin carcinomas

The potent anti-proliferative and pro-apoptotic actions of tocotrienols (T3) against cancer, but not normal tissues, have been hampered by their limited systemic bioavailabilty. Recent expansive development of diverse nanoemulsion (NE) vehicles emphasized their vast potential to improve the effective dosing of different clinical and experimental drugs of lipophilic nature, such as T3. The emphasis of the present work is to develop a pharmaceutically scalable, low-energy nano-emulsification approach for optimized incorporation of T3-rich palm oil (Tocomin®), possessing anticancer activity as a potential cutaneous delivery platform for adjunctive therapy of skin carcinomas, either alone or in combination with other chemotherapeutic agents. Different Tocomin®-NEs, obtained with different homogenization strategies, were screened based on physicochemical uniformity (droplet size, charge and polydispersity) and subjected to stress physical stability testing, along with chemical content analysis (≥90% Tocomin® - incorporation efficiency). Adopted hybrid nano-emulsification of Tocomin®, correlated with highest preservation of DPPH-radical scavenging capacity of active T3 in prototype formulation, Tocomin®-NE, which effectively permeated diffusion cell membranes 4-folds higher than propyleneglycol (PG)-admixed Tocomin® control. Against two different cell models of human cutaneous carcinoma, Tocomin®-hybrid NE demonstrated significantly stronger cytotoxic profiles (p ≤ 0.01), visible in both concentration- and time- dependent manners, with at least 5-folds lower IC50 values, compared to those estimated for the closest Tocomin®-control. The proposed hybrid nano-emulsified formulation of Tocomin® provides simple and stable delivery platform, for effective topical application against keratinocyte tumors.

Uji Aktivitas Antiinflamasi Gel Ekstrak Buah Kaktus (Opuntia elatior Mill.) Pada Tikus (Rattus norvegicus L.) Yang Diinduksi Lamda Karagenan

This research is about anti inflammatory activity of cactus fruits ( Opuntia elatior Mill.) extract gel in rats ( Rattus norvegicus L.) at induced lamda carragenan in purpose to determine anti inflammatory activity, and concentration of cactus fruits extract in the gel that have an anti inflammatory activity which is equal to sodium diclofenac 1% activity, and to determine the effect of variations in the concentration of cactus fruit extract ( Opuntia elatior Mill) on the physical stability of the gel. Extract was made by remaseration method using 70% ethanol. Physical stability test was conducted based on organoleptic, pH, viscosity and homogeneity of the gel. Test on Antiinflammatory activity were divided into 5 groups of treatment. Each rats induced by using lambda carrageenan. The first group of rats was given a gel without active ingredient as a negative control, groups of 2nd, 3rd and 4th rats were given gel cactus fruit extract in concentration of 5%, 10% and 15 % respectively, and 5th groups of rats were given diclofenac sodium gel as a positive control. Diameter and volume of inflammation were measured during 6 hours with 30 minute interval. Colected data were statistically analyzed using ANOVA. The results showed that concentration of cactus fruit extract in proportion of 5%, 10% and 15% in the gel preparation showed different conditions on organoleptic observations and homogeneity even though there was no different in the pH and viscosity during 14 days of storage. The results on anti-inflammatory activity testusing concentration of 5%, 10% and 15% have a recuperation effect on inflammation Gel contining 10% of extract has anti inflammatory activity which equal to 1% of sodium diclofenac activityi.e. the percentage of diameter and volume of inflammation were 63,75% and 20,93%.

Fortification of reconstituted skim milk powder with different calcium salts: Impact of physicochemical changes on stability to processing

Reconstituted skim milk powder (RSMP) was fortified with 12.5 mM/L calcium (Ca) using soluble [Ca chloride (CChlor), Ca gluconate (CGluc) or Ca hydroxide (CHyd)] or insoluble [Ca carbonate (CCarb), Ca phosphate (CPhos) or Ca citrate (CCit)] salts. CPhos and CCit decreased heat stability moderately at 140 °C, while CCarb had no effect. Soluble salts had a pronounced destabilising effect at 140 °C due to increased ionic Ca levels. After a laboratory‐scale high‐temperature short‐time heating process, CHyd‐fortified RSMP had a lower viscosity than all other samples. CChlor and CGluc increased sedimentation during accelerated physical stability testing, with CHyd causing greater sedimentation than CChlor or CGluc.

Optimization of madecassoside liposomes using response surface methodology and evaluation of its stability

Polar compounds with large molecular weight have poor membrane permeability, liposomes can promote drugs to penetrate epidermis and remain or release at dermis. Madecassoside (MA) exhibits powerful potency in treatment of skin disorders such as wound healing, scar management, and psoriasis, but it is not easy to penetrate epidermis for its hydrophilic nature. The aim of this work is to get the optimum process conditions and evaluate physicochemical properties and physical stability of MA liposomes. In order to avoid this disadvantage and maintain long term drug storage, MA Liposomes were designed to achieve optimum preparation conditions using response surface methodology (RSM) in our experiment. The process and formulation variables were optimized by achieving maximum drug encapsulation efficiency. The optimum conditions were 0.4424g of madecassoside, 8.174 of ratio of egg yolk lecithin to cholesterol, 65s of ultrasonic time. The results of particle size, zeta potential and encapsulation efficiency of madecassoside liposomes were 293nm, −35.6mV, and 40.90%, respectively, on the basis of the above optimum conditions. According to the morphology of liposomes and encapsulation efficiency of triplicate experiments conducted at optimum conditions, MA liposomes obtained by this optimized formulation had characters of favorable repeatability and proper particle size. The physical stability tests of MA liposomes indicated that its suitable storage temperature was at 4°C with higher encapsulation efficiency.

Formulasi dan Evaluasi Mikroemulsi Antikerut Ekstrak Beras Hitam (Oryza sativa L.)

Free radicals in the body can lead to wrinkle. The use of antioxidants can prevent wrinkle. Black rice known to have an antioxidant effect. The purpose of this study is to get a microemulsion preparation of black rice extract that stable and has antiwrinkle effect. Research was started by antioxidant power test in vitro against DPPH, then the optimization of the microemulsion preparation base. The optimum base formula then formulated with black rice extract. Then tested the chemical and physical stability test, also antiwrinkle effect. The results showed that black rice extract microemulsion has composition as black rice extract of 4%, VCO of 28.8%, Croduret-50-SS of 28.8%, glycerol of 28.8%, and citrate phosphate buffer pH 3.0 of 9.6%. The antiwrinkle effectivity of black rice extract in microemulsion form was more than in emulsion form. The average decrease of wrinkle level by black rice extract microemulsion was 44.46%±19.7%, and by black rice extract emulsion was 36.6%±19.5%. Keywords: Antiwrinkle, black rice, microemulsion

Nitazoxanide Cocrystals in Combination with Succinic, Glutaric, and 2,5-Dihydroxybenzoic Acid

Combination of nitazoxanide (NTZ) with a total of 32 cocrystal formers gave cocrystals with succinic acid (NTZ-SUC, 2:1) and glutaric acid (NTZ-GLU, 1:1). Additionally, 2,5-dihydroxybenzoic acid provided a cocrystal solvate with acetonitrile (NTZ-25DHBA-CH3CN, 1:1:1). All solid phases were characterized by X-ray powder diffraction analysis, IR spectroscopy, thermogravimetric analysis, differential scanning calorimetry, and single-crystal X-ray diffraction analysis. Single-crystal X-ray crystallography revealed that NTZ and the carboxylic acid cocrystal formers were linked in all three cocrystals through the same supramolecular heterodimeric synthon, C(N)NH···HOOC. Despite having different stoichiometries, the crystal structures of NTZ-SUC and NTZ-GLU showed similarities in the supramolecular organization, both containing two-dimensional layers formed by NTZ molecules, which were further interconnected by single (NTZ-SUC) and homodimeric entities (NTZ-GLU) of the cocrystal former. Basic physical stability tests showed that cocrystals NTZ-SUC and NTZ-GLU are stable at least for one month under standardized temperature/relative humidity stress conditions but decompose within 1 h into the corresponding physical phase mixtures, when exposed to aqueous solutions simulating physiological gastrointestinal conditions. Measurement of the dissolution rates gave small increases of the intrinsic dissolution rate constants when compared with NTZ. Pressure stability tests showed that the cocrystals support higher pressures (at least up to 60 kg/cm2) than NTZ.

FORMULASI SUSPENSI DOKSISIKLIN MENGGUNAKAN SUSPENDING AGENT PULVIS GUMMI ARABICI: UJI STABILITAS FISIK DAN DAYA ANTIBAKTERI

Suspension is a dosage contain solid drug material with insoluble form and smooth. Doxycycline is an antibiotic which difficult dissolve in water. Stable doxycycline suspension during 2 week if it kept at space temperature, stable on the air but will change to be dark if it influence sunshine. The aim of the research to evaluate physical stability and ability antibacterial stability doxycycline suspension with PGA as suspending agent. Research category are: Independent variable : concentration of suspending agent (PGA), suspension holding time. Dependent variable: physical stability (sedimentation volume, viscosity, redispersibility, easy to pour, and particle size) and antibacterial of doxycycline suspension, and variabel control is temperature suspension making, create of suspension. Data collecting with measuring physical stability and ability antibacterial of doxycycline suspension. The result shows doxycycline suspension with suspending agent PGA had physical stability and antibacterial ability is good. Physical Stability test show formula 1 rate PGA 5% is formula had physical stability better than formula 2 with rate PGA 7,5% and formula 3 withrate PGA 10%. stability ability test antibacterial show formula 2 is the best in pursues Staphylococcus aureus.

Preparation, Characterization and Stability Studies of Glassy Solid Dispersions of Indomethacin using PVP and Isomalt as carriers.

The purpose of the present study was to use the solid dispersion (SD) technique to improve the dissolution rates of indomethacin (IMC). IMC solid dispersions in PVP K30 and isomalt (GALEN IQ 990) were prepared using the solvent evaporation technique and a hot melt method in weight ratios of 2, 10 and 30% (IMC:PVP). Solid dispersions and physical mixtures were characterized by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and dissolution test. Physical stability tests were also performed at different temperatures and humidity conditions. The dissolution rates of all solid dispersions were faster than those of their physical mixtures. In samples containing 2% or 10% of IMC, there were no significant differences between the dissolution rates of IMC in PVP and isomalt solid dispersions, but in samples containing 30% of IMC, the dissolution rates were higher in isomalt dispersions. The XRPD analysis showed no crystalline peaks in solid dispersions, indicating that IMC was amorphous within the carrier. The DSC results showed that an interaction occurred between the drug and the carrier in PVP and isomalt dispersions. Physical stability tests at severe storage conditions showed that the dissolution rate of IMC in PVP solid dispersions decreased, while the dissolution profile of IMC in isomalt solid dispersions did not change significantly. It was shown that the dissolution rates of IMC in PVP and isomalt solid dispersions were substantially increased compared with their physical mixtures and pure IMC.

Formulation and in vitro evaluation of transdermal drug delivery system for donepezil

The effects of different formulation variables on the transdermal absorption of donepezil were investigated. The permeation of donepezil from various pressure sensitive adhesive matrices was evaluated using flow-through diffusion cell system at 37°C. The penetration of donepezil from the matrices was found to be influenced by the nature of adhesives. 1:1 combination of acrylic rubber hybrid adhesives (Duro-Tak® 87-503A and Duro-Tak® 87-504A) provided good adhesion force and high flux of donepezil. Significant increase in flux was obtained using Brij® 30, Brij® 52, and their combination, as penetration enhancers. Manual assessment using thumb test revealed that patches containing combination of enhancers possessed good adhesive properties. The formulation containing combination of Brij® 30 and Brij® 52, each at the level of 5% v/w with 15% w/w drug load in 1:1 combination of Duro-Tak® 87-503A and Duro-Tak® 87-504A matrix was found to be the best. No significant alteration in morphology and assay values were observed during the physical and chemical stability tests conducted for the study period of 3 months.

Formulation of cefuroxime axetil oral suspension and investigation of its pharmaceutical properties.

Cefuroxime is the second generation cephalosporin, which its intravenous and oral dosage forms are available. Oral route is the selective method for administration of most of the drugs. The aim of this study was formulating 'for oral' cefuroxime axetil suspensions. Minitab (ver.15) was used to design the formulations containing 125 mg of cefuroxime in 5 ml vehicle. After selecting the acceptable preparations, physical stability tests and other tests such as dissolution rate, pH, zeta potential and viscosity measurement of formulations were performed. From all 33 formulations, only 9 were selected to further investigation. Considering no sedimentation, the sedimentation volume was determined to be 1. The degrees of flocculation were also equal to 1. All selected formulations released the drug between 81-100% in 30 minutes which was acceptable according to the USP32 criteria. The results of assay test also proved that all formulations contain the drug in acceptable range (91-106%). The viscosity curves showed that the systems were pseudo plastic and thixotrop. Designed cefuroxime axetil formulations had good qualities and could be added as a new product to Iran drug marketing.