• Journal of Pharmaceutical Investigation
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• 제31권1호
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• pp.37-41
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• 2001

Various characteristics of polyethylene oxide (PEO) are useful for drug delivery systems. In this study, PEO was used as a sustained release matrix system containing cefatrizine propyleneglycol (Cefa-PG) which is a new semi-synthetic broad-spectrum and orally active cephalosporin. Five kinds of sustained release matrix tablets were formulated with various content of PEO and other ingredients. And three types of matrix tablets were formulated of which compositions were the same but the hardness was different. It was found that PEO content influenced drug release rate. Increasing PEO content, the drug release rate from matrix tablets was decreased. In addition, Avicel, one of the ingredients of matrix components, changed the drug release from the sustained release PEO matrix tablets. With increasing Avicel content, the rate of drug release was increased. For the effect of hardness of matrix tablets, the rate of drug release is decreased with increasing hardness. In comparison of bioavailability parameters after oral administration of Cefa-PG PEO matrix tablets and general Cefa-PG capsule in beagle dog, the sustained release PEO matrix tablets is more useful than a general dosage form. $AUC^{0-12}$ of the sustained release PEO matrix tablet and the general dosage form was 1.16 and 0.644 respectively.

• Journal of Pharmaceutical Investigation
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• 제41권2호
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• pp.83-90
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• 2011

Main objectives of this study were to investigate the effects of a lubricant, magnesium stearate, as blended in a hydrophilic matrix tablet and to identify significant factors using a tablet ejection force and a swelling property. The characteristics of tablet ejection were evaluated with three different compression forces (30, 40, and 60 MPa) and two controlled factors, amount of magnesium stearate and its mixing time. A hydrophilic model drug (terazosin HCl dihydrate) was regarded as a default factor. Tablet swelling was also evaluated. The optimal amount of PEG compared to PEO was set to be 88.50% w/w. As the amount of magnesium stearate was varied from 0.79% to 2.20% w/w, the amount of PEO and PEG was adjusted to meet the tablet's total weight while maintaining the ratio between the two excipients constant. As the mixing time of magnesium stearate was increased, the tablet ejection force and the swelling property were decreased. As the amount of magnesium stearate was increased, the tablet ejection force and the swelling property were decreased since the increased mixing time and the amount of magnesium stearate induced hydrophobic properties of the matrix tablet more effectively. The ejection force of the tablet increased as a result of increase in the compression force, which means that the breaking of tablet/die-wall adhesion energy was also increased when the compression energy was increased. The results gavea valuable guide how to choose suitable amount of the lubricant with processing conditions for the development of hydrophilic matrix formulations.

• 한국산학기술학회논문지
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• 제16권11호
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• pp.7838-7843
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• 2015

본 논문에서는 제 2형 당뇨병의 1차 선택약으로 사용되는 메트포르민 염산염이 통상적으로 1일 1000mg~2000mg의 고용량으로 투여되고 동시에 매우 높은 수성용해도를 가지므로 1일 1회 복용을 위한 약물방출제어시스템에 다량의 서방성 부형제를 필요로 하여 제형의 크기가 커져 복용이 어려운 문제점이 있다. 따라서 이를 개선하고자 상대적으로 수성용해도가 낮은 새로운 메트포르민 산부가염을 합성하여 서방성 정제에 적용하여 메트포르민의 방출을 확인하고자 하였다. 이를 위해 메트포르민 염산염을 원료로 하여 NaOH하에서 메트포르민 base를 만들고 여기에 산부가염을 반응시켜 6개의 새로운 메트포르민 산부가염들을 합성하였다. 또한 이들의 수성용해도를 측정하여 메트포르민 염산염에 비해 현저히 낮은 수성용해도를 가지는 메트포르민 스테아린산염을 확인하였고 메트포르민 서방성 제형에 적용하여 실제 약물의 방출제어에도 용출시험 결과, 12시간에서 약 2배의 약물방출제어 효과를 확인하였다. 결론적으로 새로운 메트포르민 산부가염을 통해 서방성 부형제의 양을 줄여 제형의 크기를 줄임으로써 보다 높은 환자의 복약순응도를 기대할 수 있을 것이다.

• 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.

• 섬유기술과 산업
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• 제8권2호
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• pp.183-191
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• 2004

의약품의 원재료인 약물은 사용 목적과 환자에 따라 정(tablet)이나 주사액과 같은 형태를 가지고 이를 제형(dosage form)이라 하고, 이런 형태의 물체를 제제(pharmaceutical preparations)라 한다. 신약이 대거 출현한 1950년대는 새로운 제형을 개발하는 물리약제학(physical pharmacy)이 활발히 연구되었다. 신약들은 당시의 기술로는 생체 내에서의 작용 등에 대한 명확한 자료와 근거 없이 약효가 있을 것으로 추정되었다. 그러나 분석기술과 기기의 발달로 약물의 체내 정량기술이 발달하면서 약물동태 학 (pharmacokinetics)이나 생물 약제학(biopharmaceutics)이 발달하여 약물의 체내 동태를 경시적으로 추적하는 일이 가능해졌다. (중략)

• 분석과학
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• 제30권1호
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• pp.32-38
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• 2017

In attempt to contribute in official monographs of Korean Pharmacopoeia, an HPLC method was developed and fully validated for the determination of tolperisone hydrochloride in tablets which have never been published in other forgein Pharmacopoeia. Analysis was carried out in an ODS column ($250{\times}4.6mm$ I.D., $5{\mu}m$) with common solvents include acetonitrile and ammonium hydrophosphate buffer as mobile phase. The assay was validated according to International Conference on Harmonization (ICH) guidelines. The method has good linearity in the range of $5-200{\mu}g/mL$ tolperisone. Intra-day precision varied between 0.04 and 0.10 %. Relative standard deviations of inter-day precision ranged between 0.43 and 1.24 % for peak area. The percentage recovery of the tolperisone ranged between 99.8 and 101.2 % in material. Recoveries in tablets were ranged between 98.7 and 100.8 %, thus confirmed the suitability of method for estimation of tolperisone hydrochloride in tablet dosage form.

• Journal of Pharmaceutical Investigation
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• 제26권3호
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• pp.187-192
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• 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
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• 제22권4호
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• pp.281-287
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• 1992

Omeprazole (OMZ) is very unstable in acidic solution, which selectively inhibit the release of the gastric juice in the gastric mucosa, In order to stabilize (OMZ) in oral solid dosage form, the enteric-coated microcapsules and compression-coated OMZ tablets containing lysine or arginine as stabilizer were prepared and their dissolution and stability test were performed. The haif life of OMZ microcapsules containing arginine was 194 days at $30^{\circ}C$ and OMZ was completely released in 60 min. The half-lives of enteric coated and non-coated compression-coated OMZ tablets with lysine were 292 and 95 days at $30^{\circ}C$, respectively. The half-lives of enteric coated and non-coated compression-coated tablets with arginine were 1752 and 293 days at $30^{\circ}C$, respectively, and OMZ were released completely in 20 min in the 2nd fluid of K.P.VI. Consequently, the enteric-coated compression-coated OMZ tablets with arginine as stabilizer provided a good formulation for oral solid dosage form.

• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.219-223
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• 1997

Terfenadine, antihistaminic drug, is poorly soluble in water. The purpose of this study is to investigate the possibility of using $terfenadine-{\beta}-cyclodextrin$ inclusion compound, instead of terfenadine, as the active substance of solid dosage form by improving the solubility, dissolution and anti-histaminic activity of terfenadine. The solubility and binding characteristics of $terfenadine-{\beta}-cyclodextrin$ complex in pH $1.2{\sim}6.8$ were investigated. Furthermore, the preparing method of $terfenadine-{\beta}-\;cyclodextrin$ inclusion compound was setting up and its physico-chemical characteristics such as DSC curve, solubility, dissolution and anti-histaminic activity were investigated. In conclusion, the solubility of terfenadine was increasing ${\beta}-cyclodextrin$ and with the decreasing pH. $Terfenadine-{\beta}-cyclodextrin$ inclusion compound, whose yield is almost 100%, was prepared by neutralization method. This inclusion compound was 200-times as soluble as terfenadine in pH 1.2-6.8. In addition, it had the faster dissolution and anti-histaminic activity than terfenadine. Therefore, it is used to the active substance of solid dosage form such as tablet and capsule in stead of terfenadine.

• 한국근적외분광분석학회:학술대회논문집
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• 한국근적외분광분석학회 2001년도 NIR-2001
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• pp.4111-4111
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• 2001

When a drug is prepared in a tablet, the active component represents only a small portion of the dosage form. The other components of the formulation include materials to assist in the dissolution, antioxidants, coloring agents and bulk fillers. The tablets are tested using approved testing methods usually involving separation and subsequent quantification of the active component. Tablets may also be tested by near-Infrared Reflectance spectrometry (NIRS). In the present study, based on NIRS and multivariate calibration methods, a novel and precise method is developed for direct determination of ascorbic acid in vitamin C tablet. Two different tablet formulations were powdered in three different sizes, 63-125 ${\mu}{\textrm}{m}$, and examined. Spectral region of 4750-4950 $cm^{-1}$ / was used and optimized for quantitative operations. Partial least squares (PLS) and multiple linear regression (MLR) methods were performed for this spectral region. The results of optimized PLS and MLR methods showed that reproducibility increase with decreasing grain size and standard error of calibration (SEP) of less than 1% w/w of ascorbic acid and a correlation coefficient of 0.998 can be achieved. The PLS method showed better results than MLR. Seven overdose and underdose samples (prepared in the laboratory to match marketed products) were tested by proposed and iodometric standard methods. A correlation between NIRS predicted ascorbic acid values and iodomet.ic values was calculated ($R^2$=0.9950). Finally, the direct analysis of individual intact tablets in their unit-dose packages (Blistering in aluminum and PVC foils) obtained from market were also carried out and a correlation coefficient of 0.9989 and SEP of 0.931% w/w of ascorbic acid were achieved.