• Title/Summary/Keyword: solubility test

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Improvement of Dissolution rate of Felodipine Using Solid Dispersion and its Sustained Release Oral Dosage Form (고체분산체에 의한 펠로디핀의 용출율 개선과 서방성 경구제제)

  • Gil, Young-Sig;Hong, Seok-Cheon;Yu, Chang-Hun;Shin, Hyun-Jong;Kim, Jong-Sung
    • Journal of Pharmaceutical Investigation
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    • v.32 no.3
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    • pp.185-190
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    • 2002
  • To improve the solubility of poorly water-soluble drug and to develop a sustained release tablets, the need for the technique, the formation of solid dispersion with polymeric materials that can potentially enhance the dissolution rate and extent of drug absorption was considered in this study. The 1:1, 1:4, and 1:5 solid dispersions were prepared by spray drying method using PVP K30, ethanol and methylene chloride. The dissolution test was carried out at in phosphate buffer solution at $37^{\circ}C$ in 100 rpm. Solid dispersed drugs were examined using differential scanning calorimetry and scanning electron microscopy, wherein it was found that felodipine is amorphous in the PVP K30 solid dispersion. Felodifine SR tablets were prepared by direct compressing the powder mixture composed of solid dispersed felodipine, lactose, Eudragit and magnesium stearate using a single punch press. In order to develop a sustained-release preparation containing solid dispersed felodipine, a comparative dissolution study was done using commercially existing product as control. The dissolution rate of intact felodipine, solid dispersed felodipine and its physical mixture, respectively, were compared by the dissolution rates for 30 minutes. The dissolution rates of felodipine for 30 minutes from 1:1, 1:4, 1:5 PVP K30 solid dispersion were 70%, 78% and 90%. However, dissolution rate offelodipine from the physical mixture was 5% of drug for 30 minutes. Our developed product Felodipine SR Tablet showed dissolution of 17%, 50% and 89% for 1, 4, and 7 hours. This designed oral delivery system is easy to manufacture, and drug releases behavior is highly reproducible and offers advantages over the existing commercial product. The dissolution rate of felodipine was significantly enhanced, following the formation of solid dispersion. The solid dispersion technique with water-soluble polymer could be used to develop a solid dispersed felodipine SR tablet.

Development of Self-microemulsifying Drug Delivery System for Enhancing the Bioavailability of Atorvastatin

  • Jin, Shun-Ji;Cho, Won-Kyung;Park, Hee-Jun;Cha, Kwang-Ho;Park, Jun-Sung;Koo, Ja-Seong;Wang, Hun-Sik;Kim, Jeong-Soo;Kim, Min-Soo;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.41 no.2
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    • pp.103-109
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    • 2011
  • The objective of the study was to prepare self-microeulsifying drug delivery system (SMEDDS) incorporating atorvastatin calcium and evaluate its properties and oral bioavailability. Solubility of atorvastatin in various vehicles was determined. Pseudo-ternary phase diagrams were constructed to identify the good self-emulsification region. The droplet size distributions of the resultant emulsions were determined by dynamic light scattering measurement. The mean droplet size of chosen formulation (20% ethyl oleate, 40% tween-80, 40% Carbitol$^{(R)}$) was $23.4{\pm}1.3$ nm. The SMEDDS incorporating atorvastatin calcium appeared to be associated with better performance in dissolution and pharmacokinetic studies, compared with raw atorvastatin calcium. In dissolution test, the release percentage of atorvastatin from SMEDDS mixture could rapidly reach more than 95% within 3 min. Oral $AUC_{0{\rightarrow}8hr}$ values in SD rats was $1994{\pm}335\;ng{\cdot}hr/mL$, which significantly increased (P<0.05) compared with raw atorvastatin calcium. The SMEDDS formulation was relatively stable when stored at $4^{\circ}C$ during 3 months. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin, by the oral route.

Immediate Drug Release Enhancement of Nateglinide Using Fumaric Acid (푸마르산을 이용한 나테글리니드 함유 속방출형 제형의 약물방출 개선에 관한 연구)

  • Lee, Sung-Hoon
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.18 no.1
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    • pp.506-512
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    • 2017
  • The purpose of this study was to improve release rate and bioavailability of nateglinide formulation. Polymorphism selection and particle size control were performed to enhance formulation dissolution rate, and a pH modifier was included in the formulation to overcome pH-dependent solubility of nateglinide. The enhanced dissolution rate was characterized by using a dissolution test. The results showed that H-type raw material had a higher dissolution rate than that of B-type raw material. There was 6.2% difference in dissolution between the two materials at 60 min. With regard to particle size, raw material with a $1.13{\mu}m$ particle size showed a 20% faster release rate than that of raw material with a $2.28{\mu}m$ particle size. Furthermore, fumaric acid was included in formulation as a pH modifier. That addition produced a greater than 50% improvement in dissolution rate. In conclusion, dissolution rate of nateglinide can be enhanced by optimizing its polymorphism and particle size; moreover, a synergistic effect on the enhancement of dissolution rate is obtained by including fumaric acid, a pH modifier, in the formulation.

Effect of Fluoride and Laser on Artificial Caries-like Lesion Formation in Bovine Enamel (불소 및 레이저가 우치법랑질의 인공우식병소에 미치는 영향)

  • Kim, Jae-Gon;Baik, Byeong-Ju;Ju, Hoon;Yun, Hyun-Du
    • Journal of the korean academy of Pediatric Dentistry
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    • v.24 no.3
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    • pp.660-677
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    • 1997
  • The purpose of this study was to examine the morphological characteristics and combined effects of fluoride application and laser irradiation on artificial caries-like lesion formation in bovine enamel. Enamel specimens were divided into five experiment group and placed in no-treatment(group C), APF application alone(group F), laser irradiation alone(group L), APF application before laser irradiation (group FL), and APF application after laser irradiation(group LF) on artificial caries-like lesion. Sound enamel was used as a control group. The ultrastructural changes and physical effects of the fluorided and lased enamel has been investigated by using SEM, enamel solubility and microhardness test as well as distributions of calcium, phosphorus and fluoride in internal enamel by using EPMA. The following results were obtained. 1. In the all experiment groups, the amounts of dissolved calcium of enamel surfaces significantly decreased according to increasing exposure time of acid solution than control group(P<0.001). Group L showed higher than that group FL and LF in 30 and 60min(P<0.05). 2. The microhardness values of enamel surface in the control group was highest than that in the other experiment groups. Group F, L, FL and LF were significantly increased than group C(P<0.001). The enamel surface treated with APF produced deposites of numerous small globules and lased enamel showed a cracker-like appearance with microcrack and small pore. Numerous deposits were infiltrated in the fissured portion of enamel treated with APF after laser irradiation. 4. In the case of APF application alone, the elevation of the fluoride profile can be seen within $5{\mu}m$ of the outermost layer and a similar profile observed in the specimen treated with APF before laser irradiation. However, the specimen treated with APF after laser Irradiation showed a large elevation within $10{\mu}m$ of the outermost layer of the enamel. 5. The higher Ca/P ratios were observed in $10{\mu}m$ depth of lased and fluorided enamel when compared to the sound and carious enamel. The fluoride content decreased rapidly with distance from enamel surface, in the group F, fluoride concentration was significantly higher than that in the group C, L, FL, LF and control group according to increasing enamel depth (P<0.05).

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Effects of Solvent-Based Dilution Condition on CNT Dispersion in CNT/Epoxy Composites (용매를 이용한 에폭시 희석 조건이 CNT 에폭시 복합재료 내 CNT 분산도에 미치는 영향)

  • Kwon, Dong-Jun;Shin, Pyeong-Su;Kim, Jong-Hyun;Lee, Hyung-Ik;Park, Jong-Kyoo;Park, Joung-Man
    • Composites Research
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    • v.29 no.4
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    • pp.125-131
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    • 2016
  • In case of CNT mixing with epoxy, epoxy matrix needs to be diluted. This work studied the effect of the dilution condition of epoxy on CNT dispersion. The optimum solvent condition using acetone and DMF was found via mechanical and solubility methods which affects, the epoxy performance. The dispersion using acetone was better than the DMF and thus higher mechanical properties. Four mixing types of CNT particle were performed. To verify the effects of each step between dilution and dispersion, the dispersion between epoxy and CNT was evaluated via the electrical resistance and optical methods. The optimum dispersion was obtained via mechanical test and thermal analysis by DSC. Among four types, the best was to disperse CNT after epoxy and hardeners were diluted respectively.

Inhibitory Effects of β-Cyclodextrin-Helenalin Complexes on H-TERT Gene Expression in the T47D Breast Cancer Cell Line - Results of Real Time Quantitative PCR

  • Ghasemali, Samaneh;Nejati-Koshki, Kazem;Akbarzadeh, Abolfazl;Tafsiri, Elham;Zarghami, Nosratollah;Rahmati-Yamchi, Mohamad;Alizadeh, Effat;Barkhordari, Amin;Tozihi, Majid;Kordi, Shirafkan
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.11
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    • pp.6949-6953
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    • 2013
  • Background: Nowadays, the encapsulation of cytotoxic chemotherapeutic agents is attracting interest as a method for drug delivery. We hypothesized that the efficiency of helenalin might be maximized by encapsulation in ${\beta}$-cyclodextrin nanoparticles. Helenalin, with a hydrophobic structure obtained from flowers of Arnica chamissonis and Arnica Montana, has anti-cancer and anti-inflammatory activity but low water solubility and bioavailability. ${\beta}$-Cyclodextrin (${\beta}$-CD) is a cyclic oligosaccharide comprising seven D-glucopyranoside units, linked through 1,4-glycosidic bonds. Materials and Methods: To test our hypothesis, we prepared ${\beta}$-cyclodextrin-helenalin complexes to determine their inhibitory effects on telomerase gene expression by real-time polymerase chain reaction (q-PCR) and cytotoxic effects by colorimetric cell viability (MTT) assay. Results: MTT assay showed that not only ${\beta}$-cyclodextrin has no cytotoxic effect on its own but also it demonstrated that ${\beta}$-cyclodextrin-helenalin complexes inhibited the growth of the T47D breast cancer cell line in a time and dose-dependent manner. Our q-PCR results showed that the expression of telomerase gene was effectively reduced as the concentration of ${\beta}$-cyclodextrin-helenalin complexes increased. Conclusions: ${\beta}$-Cyclodextrin-helenalin complexes exerted cytotoxic effects on T47D cells through down-regulation of telomerase expression and by enhancing Helenalin uptake by cells. Therefore, ${\beta}$-cyclodextrin could be superior carrier for this kind of hydrophobic agent.

Effect of Xylanase on Performance and Apparent Metabolisable Energy in Starter Broilers Fed Diets Containing One Maize Variety Harvested in Different Regions of China

  • O'Neill, H.V. Masey;Liu, N.;Wang, J.P.;Diallo, A.;Hill, S.
    • Asian-Australasian Journal of Animal Sciences
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    • v.25 no.4
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    • pp.515-523
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    • 2012
  • The objective of this study was to investigate the variability in broiler performance, apparent metabolisable energy (AME) and ileal digestible energy (IDE) between five different maize samples fed with and without xylanase at 16,000 U/kg. Various in vitro characterisations were conducted to determine if any could predict performance or AME. Samples of the maize were harvested in five diverse regions and fed individually in a mash diet as follows (g/kg): test maize 608.3; soya bean meal (SBM) 324.1; poultry fat 25.2; salt 4.6; met 2.6; lys 1.6; thr 0.5; limestone 9.7, dical 18.4; vit/min 5.0; CP 210 and ME (kcal/kg) 3,085. The diets were fed to 720 broilers with 6 replicates, each containing 12 birds per treatment, from 0 to 18 d of age. Maize samples were analysed for starch, protein, crude fibre, fat, protein solubility index (PSI) and vitreousness using near infra red reflectance spectroscopy (NIR). They were also assayed using an in vitro starch digestibility method. The results showed that there was no effect of harvest region on the feed intake (FI), body weight gain (BWG) or feed conversion ratio (FCR) of the broilers over the 18 d period (p = 0.959, 0.926, 0.819 respectively). There was an improvement in all parameters with the addition of xylanase (FI p = 0.011; BWG and FCR p<0.001). There was a significant positive effect of xylanase on IDE, AME, IDE Intake (IDEI) and AME intake (AMEI) (p<0.0001 in all cases). Although there was no significant effect of maize source, there was a strong trend towards variability in IDE (p = 0.066) and AME (p = 0.058). There were no significant correlations (p<0.05) between any proximate or physiochemical values and any performance or AME values. This may suggest that none of those selected were suitable predictors for performance or AME. The broilers performed well according to the breed guidelines, with slightly increased FI, increased BWG and similar FCR prior to the addition of xylanase. When FCR and BWG were analysed with FI as a covariate, xylanase addition remained significant suggesting that the improvement in BWG and FCR was driven by an increase in digestibility and nutrient availability.

Properties and Gas Permeability of PEBAX Composite Membrane Containing GO (GO를 함유한 PEBAX 복합막의 성질과 기체투과도)

  • Lee, Seul Ki;Hong, Se Ryeong;Lee, Hyun Kyung
    • Membrane Journal
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    • v.28 no.4
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    • pp.233-242
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    • 2018
  • To study gas membrane using GO (graphene oxide), the PEBAX [poly(ether-block-amide)]-GO polymer composite membrane was prepared by adding GO to PEBAX. Through this composite membrane, gas permeation characteristics for $H_2$, $N_2$, $CH_4$, and $CO_2$ were studied. As a result of the gas permeation test, the permeability of $N_2$, $CH_4$, and $CO_2$ to PEBAX-GO composite membranes gradually decreased as the GO content increased. On the other hand, the gas permeability of $H_2$ increased with the increase of GO content, and it was 21.43 barrer at the GO content of 30 wt%, which was about 5 times higher than that of PEBAX membrane. This is because the GO was easier to operate with a fast and selective gas transport channel for $H_2$ than other gases. The increased selectivity ($H_2/N_2$) and selectivity ($H_2/CH_4$) were influenced by the diffusion selectivity by the permeate gas size. The increased selectivity ($CO_2/N_2$) and selectivity ($CO_2/CH_4$) were more influenced by the solubility selectivity due to the affinity of $CO_2$ and GO for -COOH.

Studies on the Development of Hydrangea and Stevia as a Natural Sweetening Products (천연감미료(天然甘味料) 자원식물(資源植物) Hydrangea 및 Stevia의 개발(開發)에 관(關)한 조사연구(調査硏究))

  • Chung, Myung-Hyun;Lee, Myung-Yul
    • Korean Journal of Pharmacognosy
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    • v.9 no.3
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    • pp.149-156
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    • 1978
  • The result of the study about the cultivation, the constituents, the sweetenity, and the development of preparations of Stevia and Hydrangea are as follows: 1. Hydrangea thrived at $200{\sim}1,400m$ above the sea-level, and the good ones were brought up at $600{\sim}1,200m$. 2. The good ones which belonged to the genera of Hydrangea were produced in the damp, dark and cold place. 3. The growth and cultivated yield of Stevia was not significantly influenced by the acidity of the soil. 4. The best season was May and June for propagation of Stevia by cutting method. 5. The growth rate of Stevia and Hydrangea was really good in the sandy fertile soil, but in the mucotic soil it was not suitable. 6. The extraction and separation of phyllodulcin by solvent had many difficulties, because it was very soluble in water, ethanol, ether, petroleum ether, acetone and benzene, etc. 7. The solubility of stevioside on the solvent was as follows: It was very soluble in water and methanol, slightly soluble in ethanol and acetone, and insoluble in ether, petroleum ether and chloroform. 8. The alkaloid reaction by Mayer reagent in Hydrangea extract was positive. 9. The ashification rate of Stevia was 8.66% to 8.72% and that of Hydrangea 17.02% to 17.04%. 10. The tannin of Stevia leaf was 7.80% to 7.88% and its of Hydrangea decreased 9.46% to 6.08% by fermentation. 11. The percent rates in minimum concentration-occurring sweetness in sugar, glycyrrhiza methanol extract, Hydrangea water extract, Stevia leaf water extract, decoction of Stevia's leaf, decoction of Stevia's stem were as follows: 1.2, 0.1, 0.1, 0.2, 0.4, 0.01, 0.1, 0.6. and sweetenity ratios of those were 1, 12, 12, 6, 3, 64, 12, 2, 12. It was very meaningful to develop preparations of stevia as stevioside, micronized powder, water extract, methanol extract and compound teas and in Hydrangea, water extract, methanol extract, single tea, and compound teas were less meaningful. 13. The genera of Hydrangea which is natural species in Korea was positive in phyllodulcin-identification test, but it was not available to make the sweet tea because of having a little content.

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Effects of Different Milling Methodes on Physico-chemical Properties & Products (제분방법이 쌀가루 및 제품의 특성에 미치는 영향)

  • Kum, Jun-Seok;Lee, Sang-Hyo;Lee, Hyun-Yu;Kim, Kil-Hwan;Kim, Young-In
    • Korean Journal of Food Science and Technology
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    • v.25 no.5
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    • pp.546-551
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    • 1993
  • Rice flour obtained by four different milling methods, Pin mill. Colloid mill, Micro mill, and Jet mill, were used to investigate physico-chemical properties and product. Crude fat, ash, and protein contents of rice flours between different milling methods were similar. Blue value, amylose content, and damaged starch which related to properties of rice flour were reduced in the order that of Jet mill, Micro mill, Colloid mill, and Pin mill. Water absorption index, water solubility index, and water retention capacity increased as damaged starch increased. Hardness of gel(15%) is the highest value for Pin mill. The finer granules (Jet mill) had lower gelatinization onset(To) and peak(Tp) than any other rice flours. Those result are simillar with amylogram properties. Enthalpy of gelatinization increased as damaged starch increased. Jet mill had the highest score (p<0.05) of overall test in sensory evaluation and good paste properties.

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