• Journal of Pharmaceutical Investigation
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• 제23권4호
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• pp.231-254
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• 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.

• 분석과학
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• 제34권2호
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• pp.46-55
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• 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
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• 제36권4호
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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.

• Journal of Pharmaceutical Investigation
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• 제40권4호
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• pp.237-244
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• 2010

This study investigated basic material properties and compressibility of commonly used pharmaceutical excipients. Five classes of excipients are selected including starch, lactose, calcium phosphate, microcrystalline cellulose (MCC), and povidone. The compressibility was evaluated using compression parameters derived from Heckel and Kawakita equation. The Heckel plot for lactose and dicalcium phosphate showed almost linear relationship. However, for MCC and povidone, curves in the initial phase of compression were observed followed by linear regions. The initial curve was considered as particle rearrangement and fragmentation and then plastic deformation at the later stages of the compression cycle. The Kawakita equation showed MCC exhibited higher compressibility, followed by povidone, lactose, and calcium phosphate. MCC undergoes significant plastic deformation during compression bringing an extremely large surface area into close contact and facilitating hydrogen bond formation between the plastically deformed, adjacent cellulose particles. Lactose compacts are consolidated by both plastic deformation and fragmentation, but to a larger extent by fragmentation. Calcium phosphate has poor binding properties because of its brittle nature. When formulating tablets, selection of suitable pharmaceutical excipients is very important and they need to have good compression properties with decent powder flowability. Material properties tested in this study might give a good guide how to select excipients for tablet formulations and help the formulation scientists design the optimum ones.

• Journal of Pharmaceutical Investigation
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• 제40권6호
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• pp.367-372
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• 2010

Rabeprazole sodium (RPN) is known to be very unstable at acidic condition or some acidic pharmaceutical excipients such as acrylic acid polymer (carbomer 934) with carboxylic acids. Thus, degradation mechanism of binary blends of rabeprazole with pharmaceutical excipients in a solid state without using solvents at three different ratios (3:1, 1:1 and 1:3) was investigated using Fourier transform infrad (FTIR) spectroscopy. Alkalizer (MgO), neutral hydroxypropymethylcellulose (HPMC 4000) were also tested for comparison. The binary blends were stored under accelerated conditions ($40^{\circ}C$/75% relative humidity) for two weeks. The concentration of thioether rabeprazole from the binary blends with acidic carbomer 934 increased as the rabeprazole concentration decreased. In addition, the degradation half-life of rabeprazole as well as the relative peak area ratios obtained from FTIR spectra of S=O stretching at $1094.1\;cm^{-1}$ decreased consistently as the fraction of carbomer 934 increased due to its sensitivity between the basic benzimidazole nitrogen and carboxylic acid group of carbomer 934. The physical appearance also turned into strong brown color in the presence of carbomer 934. In contrast, there were no significant changes in the degradation kinetics of rabeprazole with MgO and HPMC 4000 in a solid state. This present study demonstrated that the solid-state compatibility test with the aid of HPLC chromatographic and FTIR spectral analyses could offer a valuable methodology to select suitable pharmaceutical excipients and to elucidate the degradation mechanism of RPN for drug formulations at the early formulation stages.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.303.1-303.1
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• 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)

• 생명과학회지
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• 제28권4호
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• pp.472-477
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• 2018

Pravastatin은 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) 환원효소 억제제이며, 혈청 콜레스테롤 농도를 낮추어 심혈 관계 위험성 및 사망률을 감소시킨다. 이번 연구는 부형제, 안정화제, 붕해제, 활택제, 착색제로 사용되는 첨가제들 및 pravastatin과의 적합성 연구를 위해 진행되었다. 모든 첨가제들과의 혼합은 PTP 포장으로 포장되어 가속시험장치($40^{\circ}C/75%$ Relative Humidity)에서 3개월 동안 진행하였다. 가시적인 시험결과로는 백색의 가루 또는 밝은 갈색으로 변화는 없었다. 모든 첨가제들과 pravastatin 혼합 시 pravastatin 함량 및 순도에 있어 아주 적은 수준으로 영향을 주었으며, 그 중 pravastatin의 lactone 함량의 변화가 조금 있는 첨가제로는 microcrystalline cellulose 및 croscamellose sodium이었다. 초기의 pravastatin의 lactone 함량과 비교 시 약 0.22% 및 0.18%로 증가하였고 모든 첨가제들과의 전체 혼합 시도 3개월에서 lactone 함량이 0.43%로 증가하는 것을 확인 하였다. 이번 연구 결과들은 복용편리성을 위한 pravastatin 정제 크기 감소 연구에 크게 기여 할 것으로 판단된다.

• Journal of Pharmaceutical Investigation
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• 제33권1호
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• pp.67-71
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• 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.

• 대한약침학회지
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• 제25권4호
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• pp.317-325
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• 2022

Polymers are the major constructive material of pharmaceutical formulations that play a prime role in designing effective drug-delivery systems and releasing drugs at their sites of application. Polymers are composed of multiple repeating units of high molecular mass components with attendant properties. Most synthetic polymers are non-biocompatible, expensive, and extremely inclined to deliver adverse impacts. Meanwhile, edible polymers obtained from natural sources have gained remarkable recognition for their promising use in modern medicine. Moreover, polymers derived from natural sources are generally preferred due to certain of their unique features such as abundant availability, biocompatibility, nontoxicity, economical, safe, and effective functions that fit the purpose. Polysaccharides including starch, cellulose, hemicellulose, pectin, and mucilage are identified as a major class of naturally obtained molecules that have a substantial role as functional polymers. This review summarizes the potential role of polysaccharides derived from vegetable sources such as adhesives, anticaking agents, binders, disintegrants, emulsifiers, film-framing agents, and thickeners. This is simply an opportunity to abandon synthetic excipients that hurt our bodies and think back to nature from where we originate.

• Journal of Pharmaceutical Investigation
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• 제12권3호
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• pp.74-87
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• 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.