• Applied Chemistry for Engineering
• /
• v.28 no.6
• /
• pp.679-684
• /
• 2017

Hydrated liquid crystalline vesicles incorporating a edge activator, which confers flexibility to the vesicle membranes, were prepared and niacinamide was encapsulated in them. The formation of liquid crystalline phases and their thermal phase transitions were investigated by polarized optical microscopy and differential scanning calorimetry (DSC), respectively. Droplet sizes of the vesicles were reduced to several tens of nanometers by incorporating edge activators, such as sodium deoxycholate, lysolecithin, or polysorbate 80. The amount of niacinamide permeated into a pig skin increased greatly using the hydrated liquid crystalline vesicles compared to the case where niacinamide was applied in an aqueous solution state. The vesicles incorporating 10% sodium deoxycholate increased the amount of niacinamide permeated nearly four times. These results suggest that edge activators are effective in improving the skin permeability of vesicles.

• Journal of Pharmaceutical Investigation
• /
• v.34 no.3
• /
• pp.185-192
• /
• 2004

The objective of this study was to evaluate the effects of surfactant type and concentration upon dissolution rates of carbamazepine from an immediate-release tablet. The dissolution media used in this study were aqueous solutions containing 0.1-2% sodium lauryl sulfate, cetyltrimethylammonium bromide, or polysorbate 80. The solubility of carbamazepine in the dissolution media was determined at first. A dissolution study was then conducted by using the USP dissolution apparatus II (paddle method) with an agitation rate of 75 rpm. Aliquots of the dissolution media were taken at predetermined time intervals, and the amount of carbamazepine dissolved was measured spectrophotometrically at 285 nm. The dissolution data obtained were fitted into a biphasic exponential equation with four parameters. Excellent correlations were observed between the experimental data and the theoretical ones predicted by the equation. This equation permitted the calculation of $T_{50%}$ (the time required for dissolving 50% of carbamazepine) under various experimental conditions. Differentiation of the equation also led to the attainment of dissolution rates at dissolution time points. The addition of a surfactant to an aqueous solution led to increasing the solubility of carbamazepine by 3- to 12-folds, depending upon its type and concentration. This event also resulted in enhancing the magnitude of a sink condition during the dissolution study. As a result, the dissolution rate of carbamazepine was affected by the aqueous surfactant concentration in a proportional manner. Subsequently, $T_{50%}$ values declined rapidly, as the surfactant concentration increased. Such effects were observed in decreasing order of sodium lauryl sulfate, cetyltirmethylammonium bromide, and polysorbate 80. These results clearly demonstrated that it was possible to tailor a dissolution rate and $T_{50%}$ of carbamazepine by manipulating the type and concentration of a surfactant. Relevant information would be beneficial to setting up dissolution specifications for poorly water-soluble drug products.

• Archives of Pharmacal Research
• /
• v.29 no.11
• /
• pp.1055-1060
• /
• 2006

The objective of this study was to formulate itraconazole semisolid dosage forms and characterize their physicochemical properties. Itraconazole and excipients such as polysorbate 80, fatty acids, fatty alcohols, oils and organic acids were melted at $160^{\circ}C$. The fused solution was then cooled immediately at $-10^{\circ}C$ to make wax-like semisolid preparations. Their physicochemical attributes were first characterized using differential scanning calorimetry, Fourier transform infrared spectroscopy and nuclear magnetic resonance spectrometry. The solubility of itraconazole in semisolid preparations and their dispersability in the simulated gastric fluid were also determined. Our semisolid preparations did not show any distinct endothermic peak of a crystalline form of itraconazole around $160-163^{\circ}C$. This suggested that it was changed into amorphous one, when it was formulated into semisolid preparations. In addition, the distinctive functional peaks and chemical shifts of itraconazole were well retained after processing into semisolid preparations. It could be inferred from the data that itraconazole was stable during incorporation into semisolid preparations by the hot melt technique. In particular, itraconazole semisolid preparations composed of polysorbate 80, fatty acids and organic acids showed good solubility and dissolution when dispersed in an aqueous medium. It was anticipated that the semisolid dosage forms would be industrially applicable to improving the bioavailability of poorly water-soluble drugs.

• Korean journal of food and cookery science
• /
• v.10 no.1
• /
• pp.8-12
• /
• 1994

The effects of small molecule amphiphiles(SMA) at 1.5 and 15% levels were compared with or without heating to 65$^{\circ}C$ and cooling pretreatment in modified reduced-calorie cake systems. The SMA used were monoglycerides(MG), sorbitan monosterate(SMS), VanallR polysorbate 60(PS60), surose ester(SE) F10, F70, and F160, Low batter specific gravities with high cake voumes were noted with the high levels of treated SMS, MG, and SE F10 and F70 or cakes with treated low levels of SEF160, F70 and PS 60. Cake volumes with the treated low levels of SEF160, F70, and PS 60 were comparable to cake volumes when using an untreated high level of Vanall$\^$R/.

• Applied Chemistry for Engineering
• /
• v.30 no.4
• /
• pp.415-420
• /
• 2019

To investigate the effect of nonionic surfactant and emulsion stabilizer on O/W emulsions, various emulsion formulations with different types of nonionic surfactants and emulsion stabilizers were prepared and their rheological properties were compared. In this study, polysorbate 60 (Tween 60), PEG-60 hydrogenated castor oil (HCO 60), octyldodeceth-16 (OD 16), and ceteareth-6 olivate (Olivem 800) were used as hydrophilic nonionic surfactants, whereas cetyl alcohol, glyceryl monostearate, and stearic acid as emulsion stabilizers. Phase separation occurred only in the emulsion formulation with octyldodeceth-16 and all other emulsion formulations maintained a stable phase. The viscosity, hardness, and creaminess of emulsion formulation using a mixture of ceteareth-6 olivate and cetyl alcohol were the highest, and the emulsified droplet size was also the largest. These results are due to the formation of a network structure texture with the development of a large amount of liquid crystal in the O/W emulsion. In this formulation, the value of elastic modulus was large and the thixotropic behavior, in which the viscosity varies with the history of external force, was observed.

• YAKHAK HOEJI
• /
• v.26 no.4
• /
• pp.231-237
• /
• 1982

The transformation kinetics between polymorphs of sulpiride and the effect of additives on the transformation kinetics were studied. The results could be summarized as follows. 1. Transformation kinetics of the polymorph form I to form II in water suspenion was first order type and transformation rate constant at $25^{\circ}C$ is $2.61{\times}10^{-2}min^{-1}$, the half life of form I was about 27 minutes and the activation energy for transformation was 21.35 Kcal/mole. 2. Glycerine and coloring agents increased the rate of transformation., In the case of polysorbate 80, the rate constant increased in proportion to the concentration of polyserbate 80. Simple syrup showed no effect 3n transformation kinetics.

• Korean Journal of Biological Psychiatry
• /
• v.3 no.1
• /
• pp.83-87
• /
• 1996

The effects of disulfiram implantation therapy have three components : placebo, pharmacological, and psychological effects, However, considering the fact that there is no reported DER(disulfiram-ethanol reaction) in placebo implanted patients and the absorption of implanted disulfiram is not sufficient to produce DER, the major effect of disulfiram implantation is psychological rather than placebo and pharmacological one, Recently, there have been great efforts to develop a new farm of disulfiram which could exert a real pharmacological effect through the heightened bioavailability, To illustrate several examples, there are copolymer consisting of disulfiram and polymer such as polyethylene glycol and PLGA(polyglycolic-co-L-lactic acid) and depot in which disulfiram is dissolved into saline solution containing 5% w/v carboxymethylcellulose or 0.1% polysorbate 80. On the other hand, there has been a continuous research about Me-DTC, an active metabolite of disulfiram, which inhibit ALDH (acetaldehyde dehydrogenase) more potently even at a smaller amount than disulfiram. In the future. In is hoped to develop a new form of disulfiram with high bioavailability at a small amount.

• Journal of Pharmaceutical Investigation
• /
• v.5 no.2
• /
• pp.57-62
• /
• 1975

It was many differances to evaluate of the effect of excipients on colour fading in FD & C Yellow No.5 by use Tintometer and nearly is not effective in FD & C Red No. 2. When we observed colour fading in suger coating formulations by tintometer, FD & C Red No.2 was appeared to follow zero order reaction and FD & C Yellow No. 5 was not follow zero order reaction or first order reaction. Also, we could know the tendency of colour fading by visible spectrum, but it was net suitable method for this experiment more than by tintometer. The relative colour fading effect of the surfactants(Polysorbate) was as follows: Tween 60> Tween 80> Tween 20. In addition to, Benzalkonium chloride was reacted with FD & C Yellow No.5, so the stronger colour was appeared. On the other hand, the weaker colour was appeared in FD & C Red No.2. While, the sunscreening agents was not almost effective in colour fading of FD & Yellow No. 5 and FD & C Red No. 2.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.33 no.3
• /
• pp.159-163
• /
• 2007

The relationship between texture and rheological properties of mascara(oil-in-water emulsion) was analyzed in this study. The final mascara product and gelling agents(2.0 wt%) used therein, such as hydroxyethylcellulose(HC), carboxymethylcellulose(CMC), hectorite, sodium magnesium silicate (SMS), hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer(HS), and polyacrylate 13/polyisobutene/polysorbate 20 (PPP), were measured for rheological properties. As a result, HS and PPP showed the highest adhesiveness which were related to the volumizing effect of mascara. The viscosities of HC, SMS, and HS were measured at the stress range of $1{\sim}1,000s^{-1}$. SMS, with the lowest storage modulus range of $100{\sim}1,000s^{-1}$, affected the mascara in terms of smooth texture. The results of this study suggest that the rheology of gelling agents used influences the final texture of the mascara.

• Journal of Pharmaceutical Investigation
• /
• v.27 no.4
• /
• pp.271-277
• /
• 1997

Because omeprazole(OMP) is very unstable in aqueous condition, $OMP-{\beta}-CD$, the inclusion complex of OMP and ${\beta}-cyclodextrin({\beta}-CD)$ was made and physicochemical properties of it were compared with those of OMP. Skin permeability of OMP and $OMP-{\beta}-CD$ in propylene glycol vehicle and the reciprocal action of ${\beta}-CD$ with various enhancers were examined through hairless mouse. Adhesive patches were prepared with polyisobutylene and the skin permeability and stability of OMP were investigated. The inclusion complex showed higher solubility and lower partition coefficient than OMP itself. DMSO, 1-methyl 2-pyrrolidone and sodium cholate had an enhancing effect. However ethanol and polysorbate 80 hardly showed the enhancing effect of OMP. When sodium lauryl sulfate and sodium cholate as enhancer were added in patch, the former case showed higher permeability of OMP.