• Journal of Pharmaceutical Investigation
• /
• 제40권3호
• /
• pp.181-185
• /
• 2010

The objective of this study was to improve the extent of drug release as well as the dissolution rate of TD49, a novel algicidal agent, via the preparation of solid dispersion (SD). Among the various carriers tested, $Solutol^{(R)}$ HS15 was most effective to enhance the solubility of TD49. Subsequently, SDs of TD49 were prepared by using $Solutol^{(R)}$ HS15 and their solubility, dissolution characteristics and drug crystallinity were examined at various drug-carrier ratios. Solubili ty of TD49 was increased significantly in accordance with increasing the ratio of $Solutol^{(R)}$ HS15 in SDs. Compared to untreated powders and physical mixtures (PMs), SDs facilitated the faster and greater extent of drug release in water. Particularly, SD having the drug-carrier ratio of 1:20 exhibited approximately 90% of drug release within 1 hr. Differential scanning calorimetry (DSC) thermograms and X-ray diffraction (XRD) patterns suggested that SDs might enhance the dissolution of TD49 by changing the drug crystallinity to an amorphous form in addition to the increased solubilization of drug in the presence of $Solutol^{(R)}$ HS15. In conclusion, SD using $Solutol^{(R)}$ HS15 appeared to be effective to improve the extent of drug release and the dissolution rate of poorly water soluble TD49.

• 대한의용생체공학회:의공학회지
• /
• 제34권2호
• /
• pp.69-72
• /
• 2013

The goal of this study is to develop test method for evaluating the drug eluting properties of drug eluting stents (DES). PBS and the detergent solutions, presented by each DES manufacturer, were used for drug release of DES coated with paclitaxel, zotarolimus and everolimus. The drugs which are coating DES were not released by PBS but released by the detergent solutions, finally paclitaxel 83.38%, zotarolimus 103.85% and everolimus 115.78%. It seems that the use of the detergents is necessary in order to release the drugs because those drugs are extremely hydrophobic. In conclusion, using of detergent solutions presented by each manufacturer were suitable for evaluating the drug eluting property of drug eluting stent.

• Journal of Pharmaceutical Investigation
• /
• 제17권3호
• /
• pp.111-126
• /
• 1987

Methyl methacrylate-butyl methacrylate copolymer (MMBM)-dibutyl phthalate (DBP) films were investigated as a potential topical drug delivery system for the controlled release of nitrofurazone. The kinetic analysis of release data indicated that drug release followed a diffusion-controlled granular matrix model, where the quantity released per unit area is proportional to the square root of time. DBP of several hydrophobic plasticizers selected was found to give the highest release of nitrofurazone. However, hydrophilic plasticizers such as propylene glycol and polyethylene glycol 400 had no controlled release properties and acceptable film formation. The effects of changes in film composition, drug concentration, film thickness, pH of release medium, and temperature on the in vitro release of nitrofurazone were analyzed both theoretically and experimentally. The release rate constant (k') was found to be proportional to DBP content, pH, and the temperature of release medium, but independent of film thickness, and drug concentration in a range of 0.1-0.4% by weight. The linear relationship was found to exist between the log k' and DBP content. The release of nitrofurazone from MMBM-DBP (8:2) films was found to be an energy-linked process. Two energy terms were calculated ; the activation energy for matrix diffusion was 13.45 kcal/mole, and the heat of drug crystal solvation was 27.26-29.34 kcal/mole. Observation of scanning electron micrographs and microscopic photographs showed that the incorporation of DBP in films increased markedly the particle size of nitrofurazone dispersed in the film matrix, comparing with the fine dispersion of nitrofurazone in pure MMBM film alone.

• Journal of Pharmaceutical Investigation
• /
• 제26권3호
• /
• 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.

• 대한화학회지
• /
• 제57권4호
• /
• pp.493-498
• /
• 2013

리포솜은 표적 약물을 봉입하여 병소에 안전하게 전달할 수 있는 약물전달체로서 연구되고 있다. 그러나 일반적인 리포솜은 표적부위에서 약물방출이 제한적인 문제점이 있다. 따라서 본 연구에서는 리포솜의 안정성을 향상시키고 표적부위에서 외부 초음파로부터 약물의 방출을 극대화시키기 위하여 하이드록시아파타이트(hydroxyapatite, HA)가 코팅된 리포솜을 개발하였다. 대조군 리포솜은 인지질과 콜레스테롤을 이용하여 제조하였고, 대조군 리포솜의 표면에 칼슘 아세테이트, 포스포릭에시드, 그리고 25% 암모니아용액을 이용하여 HA를 코팅하였다. 모델 약물로는 독소루비신을 사용하였다. HA코팅 리포솜의 크기는 120 nm 이었고, 약물봉입효율은 95% 이상이었다. 30% 혈장용액 내에서 HA코팅 리포솜의 입자크기는 일정한 상태를 유지하였으며, 대조군 리포솜은 크기가 1.4배 증가하였다. 외부 초음파 자극에 의한 리포솜으로부터 약물 방출을 유도한 후, 방출된 약물의 세포 이입율은 HA 코팅된 리포솜이 3배 이상 대조군 리포솜에 비하여 증가하였다. 본 연구에서는 외부 초음파 자극에 의하여 리포솜으로부터 약물의 방출을 극대화시키기 위한 초음파 민감형 리포솜을 개발하였고, 본 제형은 표적부위에서 약물의 방출을 효과적으로 제어하기 위한 분야에 활용이 가능할 것이다.

• 약학회지
• /
• 제32권1호
• /
• pp.26-39
• /
• 1988

Eudragit $RS^{\circledR}$ polymer was used as a wall material for the microencapsulation of aspirin by a phase separation method from chloroform-cyclohexane system with 5% polyisobutylene (PIB) in cyclohexane, and microcapsules obtained were evaluated by particle size analysis, scanning electron microscopy (SEM), drug release and drug stability test. With PIB as a coacervation inducing agent, smooth and tight microcapsules with less aggregation were obtained. Below 1 : 0.3 core-wall ratio, it was possible to coat individual particle. Variation of production conditions showed that increasing the proportion of wall material, particle size and wall thickness of microcapsules and the concentration of paraffin wax in cyclohexane as a sealant sustained drug release rates effectively. SEM confirmed that larger microcapsules after drug release did not rupture into smaller particles but contained a few small pores on the surface. Aspirin release from Eudragit $RS^{\circledR}$ coated microcapsules was independent of the pH of medium, and the mechanism of drug release from non-sealed and sealed microcapsules appeared to fit Higuchi matrix model kinetics. Aspirin in the mixture of aspirin microcapsules and sodium bicarbonate was by far more stable than that in the mixture of pure aspirin and sodium bicarbonate.

• Journal of Pharmaceutical Investigation
• /
• 제24권4호
• /
• pp.251-256
• /
• 1994

Polypropylene glycol (M.W. 4000) was crosslinked and chain-extended by using triisocyanate and diisocyanate to synthesize rubbery and water swellable hydrogels. Model drugs, i.e., sodium salicylate and indomethacin were incorporated in the polymer matrices by swelling loading. The drug release rates of drugs could be regulated by varying the degrees of crosslinking and chain-extension. Whereas, no correlation was observed between the drug release profiles and the swelling behaviours of the matrices. The release of drugs from the matrices was considered to be governed by the mobility and mesh size of the polymer chains in the matrices.

• Journal of Pharmaceutical Investigation
• /
• 제21권3호
• /
• pp.149-153
• /
• 1991

Polyethylene oxide (PEO)-polymethacrylic acid (PMAA) interpenetrating polymer networks (IPN) were synthesized via radical polymerization of PMAA and simultaneous crosslinking of PEO using triisocyanate. The equilibrium swelling of PEO-PMAA IPN was determined at different pHs. The swelling of PEO-PMAA IPN, ranged from 20% to 90%, was more sensitive than that of homo polymer PMAA gel This is probably due to protonation and deprotonation of the PMAA network and interpolymer complex formation between PEO and PMAA. Several model drugs were loaded into the IPN matrices and the release mechanisms were investigated. The release of nonionizable drugs such as ftorafur and prednisolone was controlled by swelling of the matrices. However, he release of propranolol, positively charged drug, was more affected by the ionic interaction between the drug and PMAA newtork, and the interpolymer complexation.

• Macromolecular Research
• /
• 제16권1호
• /
• pp.45-50
• /
• 2008

This study examined the swelling behavior and in vitro release of a model drug, tetracycline-HCl, from alginate and alginate-polyaspartate (Alg-PASP) composite gel beads. The alginate and Alg-PASP composite beads were prepared using an ionic crosslinking method with aqueous $Ca^{2+}$. Their microporous morphology was observed by scanning electron microscopy. The swelling ratio of the beads in different media varied according to their composition, cross-linking density ($Ca^{2+}$ concentration), and pH of the aqueous medium. The in vitro release experiment of the tetracycline-HCl encapsulated beads in different media suggests that the release of the drug is governed mainly by the swelling properties of the polymer network. The presence of PASP was found to significantly influence the swelling properties and drug release profile.

• 한국재료학회지
• /
• 제33권11호
• /
• pp.458-464
• /
• 2023

In order to develop catechin patches for skin regeneration at wound sites, patches with varying concentrations of catechin and chitosan were manufactured. An optimal composition ratio was determined by adjusting the drug release rate and amount, to maximize efficiency. The catechin used in this study was extracted from green tea leaves using a solvent/ultrasonication method, and its characteristics were confirmed through Fourier transform-infrared spectroscopy (FT-IR) and high-performance liquid chromatography (HPLC) analyses. Patches were prepared with different concentrations of catechin and chitosan, and various properties were analyzed using techniques such as FT-IR, water contact angle analysis, and UV-Vis spectroscopy. It was observed that as the chitosan concentration increased, the release of catechin slowed down or almost ceased. A patch manufactured with 1.5 mg/cm² of catechin at a 1 % chitosan concentration exhibited a high initial release rate over 24 h and demonstrated cellular biocompatibility. Consequently, these patches, with tailored release characteristics based on the concentrations of chitosan and catechin, hold promise for use as drug delivery systems in wound healing applications.