• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.303.1-303.1
• /
• 2003

Excipients of the drug products can sometimes affect the rate and extent of drug absorption. The changes in components or composition of them can also affect the pharmacological activity. So the quantity of excipients to be changed, the new excipients and atypically large amount of commonly used excipients should be considered as bioequivalence studies. (omitted)

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

• Analytical Science and Technology
• /
• v.34 no.2
• /
• pp.46-55
• /
• 2021

Evaluation of drug-excipient compatibility is one of the basic steps in the preformulation of pharmaceutical dosage forms. Some reactive excipients have been known so far which may cause stability problems for drug molecules in pharmaceutical dosage forms. The aim of this study was to evaluate drugexcipient compatibility of gliclazide with some common pharmaceutical excipients, known for their ability to incorporate in drug-excipient interactions. Binary mixtures were prepared using lactose, magnesium stearate, polyvinylpyrrolidone, sodium starch glycolate, polyethylene glycol 2000 and dicalcium phosphate. Based on the results; gliclazide was incompatible with all tested excipients; but not with dicalcium phosphate. DSC (Differential Scanning Calorimetry) results were in accordance with HPLC (High Pressure liquid chromatography) data and were more predictive than FTIR (Fourier Transform Infrared Spectroscopy). Drug and reactive excipients incompatibility was fully discussed and documented. It is advisable to avoid incompatible excipients or carefully monitor the drug stability when incorporating such excipients in final formulation designs.

• Journal of Pharmaceutical Investigation
• /
• v.33 no.1
• /
• pp.67-71
• /
• 2003

Drug excipients are material used in the formulation of pharmacologically active drugs. They have a variety of roles including dilutents/fillers/bulking agents, binders/adhesives, propellant, disintegrants, lubricants/dlidants, colors, flavors, coating agents, polising agents, fragrance, sweeteening agent, polymers and waxes. Excipient should be inert or inactive and does not interfere with the test. Nowadays within industry there has been a recent surge of interest in novel excipient for novel dosage forms. The purpose of the review is to introduce the administration systems of drug excipient about kinds, matters to be attended to change of excipients.

• Journal of Pharmaceutical Investigation
• /
• v.29 no.3
• /
• pp.185-191
• /
• 1999

The polymeric films containing drug and various excipients were fabricated using aqueous-based $Eudragit^{\circledR}$ RS 30D dispersions. The diffusional behaviors and mechanism of the fabricated polymeric film were investigated using Keshary-Chien diffusion cell. The melatonin was used as a model drug. The diffusion behaviors of drug through the fabricated polymeric films were highly dependent on drug concentration in donor part, polymer contents and drug concentration, and the types of plasticizers and solubilizers. The fabricated polymeric films containing excipients and solubilizers could be applied for the controlled release of poorly water-soluble drug and for the preparation of drug-containing latex films for topical or oral drug delivery.

• Journal of Pharmaceutical Investigation
• /
• v.23 no.4
• /
• pp.231-254
• /
• 1993

These days, it is not uncommon that a same kind of drug is circulated globally. However, the qualities of excipients used in the same drug have to be sometimes different depending on the different requirements in the qualities stipulated by each country. For a supplier of pharmaceutical excipients, it is generally necessary to carry out different tests on the same kind of testing criteria depending on the country of destination. Thus, the discrepancies between compendium requirements of pharmaceutical excipients create severe problems in various area of industrial activities. The decision of the United States Pharmacopoeia, European Pharmacopoeia and Japanese Pharmacopoeia Commissions to harmonize the requirements is a unique chance for the industries to overcome these problems. On the other hand, discrepancies of general test methods and requirements in each monograph of pharmaceutical excipient between the compendia valid at present are in most cases extensive. Consequently their harmonization needs a lot of detailed work requiring strong support from the industry. Based on these circumstances, pharmaceutical excipients councils have been established first in U.S.A. and successively in Europe and in Japan to contribute to the harmorization process. We should like to review here the progress since the Orlando Conference in 1991 and comment about the matters at issue with regard to the international harmonization of pharmaceutical excipients.

• Archives of Pharmacal Research
• /
• v.28 no.5
• /
• pp.604-611
• /
• 2005

Polyethylene glycol (PEG) 6000-based solid dispersions (SDs), by incorporating various pharmaceutical excipients or microemulsion systems, were prepared using a fusion method, t o compare the dissolution rates and bioavailabilities in rats. The amorphous structure of the drug in SDs was also characterized by powder X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). The ketoconazole (KT), as an antifungal agent, was selected as a model drug. The dissolution rate of KT increased when solubilizing excipients were incorporated into the PEG-based SDs. When hydrophilic and lipophilic excipients were combined and incorporated into PEG-based SDs, a remarkable enhancement of the dissolution rate was observed. The PEG-based SDs, incorporating a self microemulsifying drug delivery system (SMEDDS) or microemulsion (ME), were also useful at improving the dissolution rate by forming a microemulsion or dispersible particles within the aqueous medium. However, due to the limited solubilization capacity, these PEG-based SDs showed dissolution rates, below 50% in this study, under sink conditions. The PEG-based SD, with no pharmaceutical excipients incorporated, increased the maximum plasma concentration (C$_{max}$) and area under the plasma concentration curve (AUC$_{0-6h}$) two-fold compared to the drug only. The bioavailability was more pronounced in the cases of solubilizing and microemulsifying PEG-based SDs. The thermograms of the PEG-based SDs showed the characteristic peak of the carrier matrix around 60$^{\circ}C$, without a drug peak, indicating that the drug had changed into an amorphous structure. The diffraction pattern of the pure drug showed the drug to be highly crystalline in nature, as indicated by numerous distinctive peaks. The lack of the numerous distinctive peaks of the drug in the PEG-based SDs demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix of the amorphous structure. The utilization of oils, fatty acid and surfactant, or their mixtures, in PEG-based SD could be a useful tool to enhance the dissolution and bioavailability of poorly water-soluble drugs by forming solubilizing and microemulsifying systems when exposed to gastrointestinal fluid.

• Journal of Pharmaceutical Investigation
• /
• v.26 no.3
• /
• pp.187-192
• /
• 1996

The matrix tablet containing sodium alginate and $CaHPO_4$ can release drugs in a controlled fashion from hydrogel with gelling and swelling due to their interaction as water penetrates the matrices of the tablet. The purpose of this study was to evaluate release characteristics of the matrix tablet varying the amount of sodium alginate, $CaHPO_4$ and other excipients such as chitosan, hydroxypropyl methylcellulose (HPMC) and $Eudragit^{\circledR}$ RS100 in the simulated gastric and intestinal fluid. The practically soluble ibuprofen was used as a model drug. The release profiles of matrix tablet in the gastric fluid as a function of sodium alginate/$CaHPO_4$ ratio was not pronounced because of low solubility of drug and stability of alginate matrices. However, release rate of drug from the matrix tablet in the intestinal fluid was largely changed when sodium alginate/$CaHPO_4$ ratio was increased, suggesting that the ratio of sodium alginate/$CaHPO_4$ was an important factor to control the gelling and swelling of the matrix tablet. The incorporation of other excipients into the matrix tablet also influenced the release rate of drug. The chitosan and HPMC decreased the release rate of drug. No release of drug was occurred when $Eudragit^{\circledR}$ RS100 was added into the tablet. The retarded release of matrix tablet when excipients were added resulted from the hindrance of swelling and gelling of the matrix tablet containing sodium alginate and $CaHPO_4$. The hardness and bulk density of the matrix tablet was not correlated with release rate of drug in the study. From these findings, the ratio of sodium alginate and $CaHPO_4$ in the matrix tablet in addition to incorporation of excipients could be very important to control the release rate of drug in dosage form design.

• Journal of Pharmaceutical Investigation
• /
• v.12 no.3
• /
• pp.74-87
• /
• 1982

To evaluate the pharmaceutical aspects of solvent deposition method where drug is solvent deposited on the surface of excipients, a study has been made on dissolution characteristics of indomethacin solvent deposited on lactose and potato starch. In a solvent deposition system, the drug-to-excipient ratio and kind of excipient effect much on dissolution rates of indomethacin. The experimental results are as follows: 1) Lactose was shown to be superior to potato starch as excipients in indomethacin solvent deposited. 2) Total amount of indomethacin dissolved from solvent deposition systems at 30 minutes were enhanced about 5 to 23 times compared with that of pure indomethacin. 3) Increased dissotion amount of indomethacin from the solvent deposition systems were observed to be alike in the systems where the drug-to-excipient weight ratios were 1 : 5, 1 : 7 and 1 : 10.

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