• Journal of Pharmaceutical Investigation
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• v.22 no.4
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• pp.267-279
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• 1992

Microencapsulations of amoxicillin and cephalexin, using Eudragit RS, RL, E, S and L were investigated. The microcapsules were prepared by the solvent evaporation process in liquid paraffin phase, which is based on dispersion of acetone/isopropanol containing the drug in liquid paraffin. Aluminium tristearate was used as an additive for the preparation of microcapsules. The size distribution, dissolution test and observation by SEM were examined. Good reproducibility in microcapsule preparation was observed. The microcapsules obtained were spherical and free-flowing particles. The dissolution rates of amoxicillin and cephalexin from the microcapsules were considerably decreased as compared with those from amoxicillin and cephalexin powder, respectively. As the dispersing agents (aluminium tristearate) increased, the particle size of microcapsules decreased and the dissolution rate increased. In order to control the release rate of drugs, microcapsules were prepared by mixing Eudragit RS/RL or Eudragit S/L. As Eudragit RL ratio in microcapsule of Eudragit RS/RL increased, the dissolution rate increased. As Eudragit L ratio in microcapsule of Eudragit S/L increased, the dissolution rate increased. Furthermore, the release rates of drugs from Eudragit RS/L or RS/polyelthylene glycol 1540 (PEG 1540) were examined. The dissolution rate of drugs increased with increasing of Eudragit L or PEG 1540 ratio. In conclusion, the release rates of drugs from Eudragit RS/RL or RS/PEG 1540 microcapsule could be controlled, and these microcapsules will be convenient for reducing frequency of administration.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.409.3-410
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• 2002

Microencapsulations of piroxicam using the mixture of Eudragit RS with RL or Eudragit L or E or S according to Eudragit RS were carried out. The Eudragit microspheres of piroxicam were prepared by solvent method. Piroxicam and Eudragit polymer were dissoved in methylene chloride and dispersed in 0.5% pOlyvinyl alcohol solution and solvent evaporated. The average diameters of various Eudragit microspheres were from 40 to 43${\mu}{\textrm}{m}$. A good and smooth surface of microspheres observed by SEM were shown in all type of microspheres. (omitted)

• Journal of Pharmaceutical Investigation
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• v.18 no.4
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• pp.175-180
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• 1988

The role and effect of aluminum tristearate in microencapsulation were investigated based on the dispersion system of ethambutol hydrochloride in acetone-liquid paraffin. Eudragit RS was used as a wall-forming material. Eudragit RS microcapsules prepared using aluminum tristearate were uniform, free-flowing particles. The phase diagram of ethambutol hydrochloride-Eudragit RS-aluminum tristearate indicated that spherical microcapsules ranging from 250 to 1400 ${\mu}m$ in diameter could be prepared only in a very limited region. Instrumental analysis using an energy dispersive-type X-ray microanalyser and a scanning electron microscope showed that aluminum tristearate was localized near the surface of microcapsules. From these results, it was presumed that aluminum tristearate reduced the phase tension between Eudragit microcapsules and liquid paraffin. The dissolution rates of ethambutol hydrochloride from Eudragit RS microcapsules were consideraly lower than those from ethambutol hydrochloride powders and decreased as the amount of aluminum tristearate decreased.

• Polymer(Korea)
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• v.35 no.6
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• pp.520-525
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• 2011

Superporous hydrogels (SPHs) with fast swelling and superabsorbent properties are useful materials in various biomedical fields, by improving the swelling properties of conventional hydrogels based on their unique porous structure. In this study, Eudragit polymers were used as coating materials to control the swelling properties of poly(acrylic acid-co-acrylamide) based SPHs by environmental pH. The SPHs were coated with Eudragit L100 and S100 that have different pH characteristics as enteric coating materials by a dip coating method, and their pH dependent swelling behaviors were observed in various pH environments. The swelling of SPHs was inhibited at a low pH range, but significantly enhanced above a characteristic pH of Eudragit polymers. This pH dependent swelling behavior of hydrogels could be modulated by the characteristics of the enteric coating polymers.

• Korean Chemical Engineering Research
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• v.46 no.2
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• pp.222-226
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• 2008

Nanoparticles have been developed and applied for various applications to intelligently deliver bioactive materials. Herein, lactocin was processed into nanoparticles with methacrylic acid-methyl methacrylate copolymer (1:1) (eudragit L100). The eudragit polymer can protect lactocin from the stomach acid and release lactocin in the intestines. When acetone and pH 7 buffer solution were used as non-solvent and solvent, respectively, the smallest volume-average particle size (290 nm) could be obtained. Freeze drying in presence of carrageenan (dispersant) can process the particles into dried powders with minimum aggregation. SEM observation revealed the primary particles prepared based on lactocin and eudragit were of a few tens of nanometers.

• Polymer(Korea)
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• v.31 no.4
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• pp.329-334
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• 2007

Osmotic pellet system, which is one of the oral drug delivery systems, has been developed to improve manufacturing process, reduce product cost and other problems of osmotic tablet systems. Osmotic pellet is consisted of water swellable seed layer, drug layer, and membrane layer. Among them, the membrane layer plays an important role in a control of the drug release. In this work, we examined the effect of ratio for Eudragit RL and RS on the drug release behavior. Osmotic pellet with nifedipine as a model drug was easily obtained in a good yield by fluidized bed coater. Osmotic pellet showed round morphology with a range of size $1300{\sim}1500\;{\mu}m$. In the experiment of nifedipine release, the release amount increased with the increase of the ratio of Eudragit. This is due to the fact that Eudragit RL contains more hydrophilic quaternary ammonium group than Eudragit RS. Additionally, the release amount was retarded with increasing the membrane thickness. There are no differences in the release amount measured at the different pH 1.2, 6.5, 6.8, and 7.2. In conclusion, it was found that the drug release from osmotic pellets depended on the composition ratio and coating thickness of membrane layer.

• Journal of the Korean Society of Food Science and Nutrition
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• v.32 no.8
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• pp.1239-1244
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• 2003

Microcapsules were prepared by coacervation method using acetone/liquid paraffin system to control the ripening of kimchi. Eudragit E100, which was soluble at below pH 5.0 in aqueous solution, was used to make microcapsules to be sensitive to acidity of kimchi. The microcapsules with Eudragit E100 containing grapefruit seed extract (GFSE) showed the highest yield of 92.13%, the size of microcapsules was decreasing as increasing the amount of aluminium stearate, a dispersing agent. Morphology of the microcapsules determined by scanning electron microscopy showed spherical forms. GFSE, encapsulated antimicrobial agents, was quickly released at acidic buffer (pH 4,5,6) within 1 storage day. However, 70% of encapsulated GFSE in Eudragit E100 microcapsules was continuously released at pH 7 till 3 days, and it was sustained till 9 days. Characteristics of kimchi containing microcapsules of GFSE were analysed with ripening period. Decease of pH in kimchi was retarded with the added GFSE microcapsules till 2 days of fermentation, but GFSE did not affect pH in kimchi after 3 days. Total numbers of microorganisms and lactic acid microorganisms in kimchi were decreased with increasing the amount of the added GFSE microcapsules, however, the effect of controlled released GFSE from pH sensitive Eudragit E100 microcapsules was hard to detect. These results suggest the possibility of pH sensitive microcapsules for high qualify of kimchi.

• Archives of Pharmacal Research
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• v.16 no.1
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• pp.50-56
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• 1993

The microencapsulation of sodium naproxen with Eudragit. RS was studied by coacrtvation/phase separation process using Span 80 in mineral oil/acetone system. Various factors which affect the mciroencapsulation, e.g., stirring speed, and surfactant concentraction, Eudagit RS concentration and loading drug amounts were examined. For the evaluation of the prepared microcapsules, release rate, particle size distribution and surface appearance as well as in vivo test were carried out. The addition of n-hexane and freezing of microcapsules accelerated the hardening of microcapsules. The optimum concentration of Span 80 ti prepare the smallest microcapsules was the same value with the CMC of Span 80 in solvent system. When 1.5% (w/w) Span 80 was used, the smallest microcapsules were formed $(30.02\pm5.05\mu$ in diameter) belonging to the powder category showing smooth, round and uniform surface. The release of sodium naproxen was retarded by microencapsulation with Eudragit RS. The Eudragit RS microcapsules showed significantly increased AUC and MRT and deceased Cl/F in rabbits.

• Journal of Pharmaceutical Investigation
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• v.23 no.2
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• pp.103-110
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• 1993

Microcapsules(Mc) of cephalexin (CEPH), using Eudragit RS, RL, L, S and polyethylene glycol 1540, were evaluated biopharmaceutically. The area under the curve of CEPH-Eudragit RS/RL Mc administered orally once was larger than that of cephalexin powder twice every 6 hrs. Controlledrelease effectiveness and the absorption rate effectiveness, two important parameters of Vallner's method, of CEPH-Eudragit RS/RL Mc indicate that these Mc can be good sustained-release preparations. And a simple pharmacokinetic model is introduced which allows the gastric emptying and intestinal-transit rates of a drug itself and a solid-state drug contained in Mc. Decreasing $K_r$, without change in $K_a$, showed that the rate-limiting step of absorption moved from absorption step to releasestep.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.102-102
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• 1993

제1차년도 연구에서 Goto등의 방법을 응용하여 생체에 대하여 안전하고 transit 양상에 대해 재현성이 확보되는 경구용 방출조절성 마이크로캅셀을 개발 하였다. 즉 methacrylate polymer(Eudragit RS, RL, E, S 및 L)의 특성을 이용하여 B-락탑계 항생물질(amoxicillin 및 cephaiexin)을 함유하는 마이크로캅셀을 제조하는 방법을 개발하였다. 본 연구에 있어서는 제1차년도에 in vitro 실험결과 유용한 서방성 제제로 판단되는 cephalexin 함유 Eudragit RS/RL, S/L 및 RS/PEG 마이크로캅셀을 제조하여 가토에 경구투여 후 생체이용률을 평가하였다. 또한 소화관에서 약물의 방출속도 및 흡수속도등을 고려한 모델을 구축하여 약물속도론적으로 해석함으로써 실제 임상에 적용할 수 있는 유용한 경구투여용 마이크로캅셀을 개발하고자 하였다. 1. in vitro 실험 입도분포, 함량시험, 용출시험 2. in vivo 실험 1) AUC에 의한 평가 2) Vallver 등의 방법에 의한 평가 3) 약물속도론적 방법에 의한 평가 결론: 1. Eudragit 의 특성을 이용하여 유중건조법으로 40％ cephalexin 함유 Eudragit RL/RS, S/L 및 RS/PEG 마이크로캅셀을 제조할 수 있었고 각 조성비를 변화시킴으로써 약물방출을 조절할 수 있었다. 2. 약물속도론적 해석결과 마이크로캅셀제제의 Ka는 변화하지않고 Kr이 감소되는 즉, 약물흡수의 율속단계가 방출단계임을 보여주었다. 3. Eudragit RL/RS 마이크로캅셀은 제어방출 효율 및 흡수속도 효율이 우수한 서방성 제형으로 평가되었다.