• Archives of Pharmacal Research
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• 제29권11호
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• pp.1055-1060
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• 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.

• Journal of Pharmaceutical Investigation
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• 제35권3호
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• pp.207-224
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• 2005

The objective of this study was to explore the principles of SUPAC-SS and its regulatory application in handling postapproval changes to nonsterile semisolid dosage forms. The types of postapproval changes that SUPAC-SS described were modifications in formulation (components and composition), batch size, manufacturing equipment & process, and the site of manufacturing. SUPAC-SS defined the levels of postapproval changes and what chemistry, manufacturing, and control tests should be conducted for each change level. The guidance also specified several occasions the manufacturers should perform in vitro release test (Franz cell diffusion test) and/or in vivo bioequivalence test. Finally, SUPAC-SS classified appropriate filing forms to be used in supporting postapproval changes. It was crystal clear that SUPAC-SS helped maintain the safety and quality of approved semisolid dosage forms when they were subject to certain postapproval changes. The availability of SUPAC-SS made contributions to reducing regulatory burdens of the industry, as well as expediting the postapproval process of regulatory agencies. This study also shed light on the background of relevant pharmaceutical sciences that the SUPAC-SS guidance adopted. Finally, the KFDA and the industry were strongly urged to implant a similar guidance in handling postapproval changes to semisolid dosage forms available in the Korean marketplace.

• 약학회지
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• 제59권2호
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• pp.70-76
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• 2015

A Softgel is an oral dosage form for medicine similar to capsules and softgel dosage form offers several advantages over other oral dosage forms, such as delivering a liquid matrix designed to solubilize and improve the oral bioavailability of a poorly soluble compound as a unit dose solid dosage form, delivering low and ultra-low doses of a compound. This study aimed to qualify a proprietary vegetable soft capsule which contains modified starch and carrageenan as capsule shell components compare to the conventional gelatin softgel. Four kinds of samples were prepared with vegetable and gelatin capsule shell, respectively. Morphology of capsule shell, mechanical strength of capsule, and hygroscopic properties were studied for comparing the quality attributes of softgel. Short-term stability against heat and moisture was also investigated in this study. Vegetable capsule shell showed better mechanical strength, physical stability and disintegration time for temperature and humidity than those of conventional gelatin capsule shell with four different filling materials used frequently as soft capsule form. Conclusively, this vegetable capsule shell polymer system can replace easily gelatin-shell systems and additionally allows encapsulation of lipid fills at high temperatures that are semisolid or solid-like at room temperature.

• Korea-Australia Rheology Journal
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• 제15권2호
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• pp.55-61
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• 2003

The steady shear flow properties of vaseline generally used as a base of the pharmaceutical dosage forms were studied in the consideration of wall slip phenomenon. The purpose of this study was to show that how slip may affect the experimental steady-state flow curves of semisolid ointment bases and to discuss the ways to eliminate (or minimize) wall slip effect in a rotational rheometer. Using both a strain-controlled ARES rheometer and a stress-controlled AR1000 rheometer, the steady shear flow behavior was investigated with various experimental conditions ; the surface roughness, sample preparation, plate diameter, gap size, shearing time, and loading methods were varied. A stress-controlled rheometer was suitable for investigating the flow behavior of semisolid ointment bases which show severe wall slip effects. In the conditions of parallel plates attached with sand paper, treated sample, smaller diameter fixture, larger gap size, shorter shearing time, and normal force control loading method, the wall slip effects could be minimized. A critical shear stress for the onset of slip was extended to above 10,000 dyne/$\textrm{cm}^2$. The wall slip effects could not be perfectly eliminated by any experimental conditions. However, the slip was delayed to higher value of shear stress by selecting proper fixture properties and experimental conditions.

• Archives of Pharmacal Research
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• 제11권3호
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• pp.185-196
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• 1988

The inflence of hydrophilic vehicles on percutaneous absorption rate of griseofulvin was studied using intact skin of full thickness of hairless rat. The in vitro absorption rates were used as the characteristics for deciding the optimum formula of ointment vehicles. The optimum formula of vehicle compositions for maximum absorption rate was obtained from the polynomial regression equation and the two graphical techniques, contour graph and partial derivative graph. It was composed of sodium lauryl sulfate (1.65 W /W%), white petrolatum (16.5 W /W%), propylene glycol (12.0 W /W%), and stearyl alcohol (19.6W /W%). The experimental value obtained from the optimum formula and the prediction value were 33.99 and 33.87 ${\mu}g/\sqrt{min}$, respectively. From these results, it was believed that optimum formula for semisolid dosage forms could be obtained from the application of the optimization technique used in this study.

• Archives of Pharmacal Research
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• 제19권3호
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• pp.183-190
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• 1996

There are a wide variety of semi-solid ointments used for healing the skin diseases, whose therapeutic and skin penetration abililties may greatly differ from one another depending on the compositions of ointment vehicles. A computer optimization technique was applied to obtain the optimum formula of o/w type ointment giving the in vitro maximum absorption rate through hairless rat skin membrane. Some of the formulations were selected to find out a relationship between skin penetration of ointment and its Theological characteristics. The experimental value of absorption rate obtained from the ointment by optimum formula agreed well with the theoretical value obtained from a polynomial regression analysis, Three kinds of ointments selected among 15 formulations were obtained with a concentric cylinder type rheometer (Model; Rheolab SM-HM Physica, Germany) at 20, 30, 40 and $50^{\circ}C$ for rheograms of rhelolgical properties of o/w type ointments. As the temperature was raised, all products showed a decrease in both shear stress and yield values. The higher skin penetration, the lower shear stress showed.

• Journal of Microbiology and Biotechnology
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• 제27권4호
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• pp.739-746
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• 2017

As alternatives to antibiotics in livestocks, probiotics have been used, although most of them in the form of liquid or semisolid formulations, which show low cell viability after oral administration. Therefore, suitable dry dosage forms should be developed for livestocks to protect probiotics against the low pH in the stomach such that the products have higher probiotics survivability. Here, in order to develop a dry dosage forms of probiotics for poultry, we used hydroxypropyl methylcellulose phthalate 55 (HPMCP 55) as a tablet-forming matrix to develop probiotics in a tablet form for poultry. Here, we made three different kinds of probiotics-loaded tablet under different compression forces and investigated their characteristics based on their survivability, morphology, disintegration time, and kinetics in simulated gastrointestinal fluid. The results indicated that the probiotics formulated in the tablets displayed higher survival rates in acidic gastric conditions than probiotics in solution. Rapid release of the probiotics from the tablets occurred in simulated intestinal fluid because of fast swelling of the tablets in neutral pH. As a matrix of tablet, HPMCP 55 provided good viability of probiotics after 6 months under refrigeration. Moreover, after oral administration of probiotics-loaded tablets to chicken, more viable probiotics were observed, than with solution type, through several digestive areas of chicken by the tablets.