• Proceedings of the PSK Conference
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• 2003.10a
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• pp.50-53
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• 2003

Aceclofenac (AFC) as a model has poor solubility in water, resulting in lower dissolution rate and bioavailability. A solid dispersion (SD) is one of effective methods to enhance the solubility or dissolution rate of various poorly water-soluble drugs. Polyvinylpyrrolidone (PVP) that is a nontoxic, water-soluble and generally applicable pharmaceutical excipient has been widely used as a carrier in the preparation of solid dispersions. (omitted)

• Journal of Life Science
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• v.28 no.4
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• pp.472-477
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• 2018

Pravastatin sodium is a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor used in the treatment of hypercholesterolemia by reducing cholesterol biosynthesis. Pharmaceutical excipients of commonly used including water, diluents, stabilizers, disintegrants, lubricants and colorants, and were identified for compatibility. All tests were performed by means of physical mixture of pravastatin and the excipients, which were placed in a press-through-pack (PTP) and incubated under accelerated conditions ($40^{\circ}C$ and 75% relative humidity) for 3 months. The blends of pravastatin with all excipients developed white, off white, and light brown powders, which showed no changes upon visual analysis. Accelerated conditions changed the degradation profile of pravastatin calcium in the HPLC system when mixed with different excipients. Although most excipients can have minor effects on pravastatin stability, the major degradation product from pravastatin was lactone. Low-level interaction (assay and impurity) was induced by all excipients except for microcrystalline cellulose and croscarmellose sodium. These excipients increased lactone impurity in 3 months by as much as 0.22% and 0.18% respectively. The total mixture slightly increased the lactone impurity (by 0.43% in 3 months) of pravastatin. There was no change in the assays of all excipients. These results will be helpful in studying tablet size reductions for convenience of use.

• Journal of Pharmaceutical Investigation
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• v.36 no.4
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• pp.239-243
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• 2006

Due to the development of new dosage forms and the improvement or pharmaceutics, the pharmaceutical excipients have become more specified and diverse, and the reclassification on them became necessary. Also with the increasing interests on the kinds and usage amount, related provisions, and evaluation of the pharmaceutical excipients, the systemic and effective control of them was in its demand. Therefore, in this research, we provided the following information on excipients: the type, amount and specification. In order to provide the information, we investigated, analysed and summarized the excipients that are approved by KFDA and published $\ulcorner$Handbook of Pharmaceutical Excipients$\lrcorner$). This handbook is expected to be used as a reference in the development of the pharmaceutics and evaluation in them. As the importance of excipients in pharmaceutics are increasing, IPEC which consist of IPEC-America, IPEC-Europe and JPEC, PDG and ICH have tried to make an international harmonization on excipient. This current status was not an exception to Korea, therefore, the result of this research is expected to make a progress in the evaluation on the excipients to an advanced level.

• Polymer(Korea)
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• v.36 no.1
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• pp.1-8
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• 2012

In this study, we employed hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta}$-CD) as an excipient to produce poly(lactic-$co$-glycolic acid) (PLGA) fine particles by a supercritical fluid process, called aerosol solvent extraction system (ASES), and investigated the effect of HP-${\beta}$-CD content on the morphology of the particles. The influence of HP-${\beta}$-CD on the drug release characteristics of paclitaxel-loaded PLGA particles was also evaluated. Fine particles were obtained when the HP-${\beta}$-CD content in PLGA/HP-${\beta}$-CD mixtures was greater than 40% and 30%, respectively, for PLGA(75:25) and PLGA(50:50), whereas a film-like precipitate was obtained for lower HP-${\beta}$-CD content. The release rate for paclitaxel loaded PLGA(75:25)/HP-${\beta}$-CD particles was found to increase with HP-${\beta}$-CD content.

• YAKHAK HOEJI
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• v.29 no.3
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• pp.124-129
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• 1985

A dissolution characteristics of phenylbutazone deposited on Avicel and dibasic calcium phosphate by solvent deposition method were studied. The solvent deposition was confirmed by scanning electron microscopy. Avicel was superior to dibasic calcium phosphate as excipient in dissolution rate. Total amount of phenylbutazone dissolved from Avicel deposition system at 30minutes were enhanced 1.2-1.6 times compared with physical mixtures of them. The dissolution rate of 10% solvent deposition system was highest and that of 75% solvent deposition system was lowest in Avicel system and dibasic calcium phosphate system. Dissolution profile of commercial products was dependent on manufacturing conditions and dissolution rate of 10% Avicel system was greater than that of commercial products.

• Korean Journal of Veterinary Research
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• v.48 no.1
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• pp.27-32
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• 2008

The present study was carried out to develop a sustained release implantable formula of bovine somatotropin (SRIF-BST) and to examine its sustained release effect. The SRIF-BST was produced by coating a solid pellet, which was comprised of BST and an excipient, made of a biodegradable polymer and poloxamer, which are capable of regulating the rate of BST release. The coated membrane of SRIFBST was observed with a field emission scanning electron microscope. The thickness of the coated membrane was approximately $1{\mu}m$, and the pore sizes of the coated membrane surface were below $10{\mu}m$. In dissolution test, the release duration of the SRIF-BST maintained for 10 days, whereas the release duration of the control BST formula maintained for 3 days. In weight gain assay and tibia test of hypophysectomized rats, the release duration of the SRIF-BST treated group was 12 days and the net weight gain was 53.16 g, also the tibia length and strength of the SRIF-BST treated group was increased 10.5% and 23.1% compared with those of the control group, respectively.

• Journal of Pharmaceutical Investigation
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• v.29 no.2
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• pp.117-126
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• 1999

Differential scanning calorimetry(DSC) was used as a screening technique for assessing the compatibility of some drugs with excipients. On the basis of DSC results, interaction of ibuprofen with PVP K40 was found and eutectic formations with PEG 6000 or magnesium stearate were demonstrated. Fenoprofen Ca was found to interact with PEG 6000. Naproxen showed interactions with PEG 6000, PVP K40, PVPP and Mg stearate. Interactions of tiaprofenic acid with PVP K40 or PVPP were found and eutectic formations with PEG 6000 or Mg stearate were observed. Bisoprolol hemifumarate, metoprolol tartrate and penbutolol sulfate were found to interact with lactose.

• Journal of mucopolysaccharidosis and rare diseases
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• v.1 no.1
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• pp.15-18
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• 2015

Biopharmaceuticals, with their ability to treat many unmet needs, are seen as promising medications in diabetes mellitus, growth hormone deficiency, chronic renal failure, cancer, and rheumatoid arthritis. However, almost all biopharmaceuticals should be administrated by injection; IV, IM, and SC. In addition, these treatments are long term, and patients should receive frequent injections for many years. Patient compliance is therefore of critical importance to ensure treatment benefits. Therefore, the goal of drug product development should be focused on improving patient compliance by reducing injection-associated pain as well as stable formulation development. This review will suggest the kinds of factors that should be considered to minimize injection pain with regard to formulation, device, and injection procedures focused on SC injections.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.225.1-225.1
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• 2003

Purpose. Paclitaxel has demonstrated significant activity in clinical trials against a wide variety of tumors. The clinical application of Taxol$\^$\ulcorner/, a commercial product of solubilized paclitaxel with co solvents of ethanol and Cremophor, however, has been limited largely by hypersensitivity of the excipient. The aim of this study was to formulate paclitaxel-loaded lipid nanodispersions (Px-LN) for i.v. administration without toxic excipients, and to evaluate in vitro characteristics and in vivo pharmacokinetic behaviors. (omitted)

• Journal of Pharmaceutical Investigation
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• v.31 no.2
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• pp.81-87
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• 2001

The purpose of this study was to investigate the effect of additives on the powder characteristics of peonja dry elixir. Peonja dry elixirs were prepared with various amounts of dextrin using a spray-dryer, and their powder characteristics such as flow, cohesion and compressibility were evaluated as an angle of repose, cohesion index and compressibility index, respectively. Their powder characteristics were not significantly different from one another, indicating that the hydrophilic dextrin, a base of dry elixir hardly affected their powder characteristics. Peonja dry elixirs were prepared with 10% dextrin and various amounts of additives such as mannitol (hydrophilic excipient), sodium lauryl sulfate (surfactant), colloidal silica (hydrophobic excipient) and HPMC (polymer), respectively, and their angle of repose, cohesion index and compressibility index were measured. The powder characteristics of peonja dry elixirs prepared with mannitol were not significantly different from one another, indicating that the mannitol scarcely improved the powder characteristics of peonja dry elixirs. The angle of repose and cohesion index of peonja dry elixirs significantly decreased with increasing amount of sodium lauryl sulfate to 0.3% followed by no significant changes in them. The cohesion index of peonja dry elixir significantly decreased with increasing amount of colloidal silica. The angle of repose and cohesion index of peonja dry elixir significantly decreased with increasing amount of HPMC to 0.3% followed by an abrupt increase in them. However, the compressibility index of peonja dry elixir significantly increased with increasing amount of HPMC to 0.3% followed by an abrupt decrease in them. Our results suggested that a small amount of sodium lauryl sulfate, colloidal silica and HPMC improved markedly the powder characteristics of peonja dry elixirs due to forming stronger and less hygroscopic shell of peonja dry elixirs. Among the peonja dry elixirs studied, the peonja dry elixir prepared with 0.3% sodium lauryl sulfate and 0.3% HPMC had the lowest angle of repose of $27^{\circ}$ and cohesion index of 37.8%, and the highest compressibility index of 38.7%, respectively. Thus, sodium lauryl sulfate and HPMC appear to be promising additives for peonja dry elixir, if used in adequate amounts.