• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.401-409
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• 2009

Ketrorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug (NSAID) is required repeated administration due to its short blood half-life. To avoid dose-dependent side effects of KT, sustained-release pellets containing KT were prepared by coating with Eudragit$^{(R)}$ RS 100 and Eudragit$^{(R)}$ NE 30D. The in vitro and in vivo drug release behavior of KT from Eudragit$^{(R)}$ RS 100 and NE 30D coated pellet (SR-A), Eudragit$^{(R)}$ RS 100 coated pellet (SR-B) and conventional commercial immediate-release tablet (IR) was investigated. KT from SR-A and SR-B was slowly released over several hours, whereas IR showed rapid initial release in vitro. The pharmacokinetic study in vivo was performed by oral administration in beagle dogs. 5 mg IR was administered 3 times at intervals 5 hr. Five milligrams of IR was administered 3 times at intervals of 5 hr and 15 mg of SR-A and SR-B did once. After administering IR, KT concentration in blood showed high peak- trough fluctuation and stomach ulcer were discovered. On the other hand, SR-A and SR-B sustainedly released KT and reduced the occurrence of stomach ulcer. There sustained-release pellets will be effective system to minimize dosedependent of side effect and improve patient compliance.

• Korean Chemical Engineering Research
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• v.46 no.2
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• pp.205-210
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• 2008

Poly(D,L-lactide-co-glycolide) (PLGA) has been widely used as carriers in controlled release delivery systems due to its biodegradability and relatively good biocompatibility. However, Release pattern of carriers fabricated using PLGA have disadvantage an initial burst within a few days, lag time several days and then sudden release changes. To solve these problems of PLGA, we fabricated PLGA wafer including monomer. Also, drug release behavior restraint sudden burst effect using recrystallization of PLGA. Recrystallized PLGA was characterized the morphological difference by SEM and in vitro release behavior measured by HPLC. The PLGA molecular weight analyzed to recognize monomer influence during degradation process of polymer using GPC. In this study, drug release duration cut short up to three days and was eliminated the lag time based on the bulk erosion.

• Polymer(Korea)
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• v.29 no.5
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• pp.468-474
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• 2005

PLGA and PCL copolymers initiated by carbitol as drug carriers were synthesized by ring-opening polymerization of L-lactide (LA), glycolide (GA), and $\varepsilon-caprolactone(\varepsilon-CL)$. Implantable wafers were simply fabricated by direct compression method after physical mixing of copolymers and bovine serum albumin-fluorescein isothiocyanate (BSA-FITC) as a model protein drug. The release amounts of BSA-FITC from wafers were determined by fluorescence intensity using the fluorescence spectrophotometer. Also, the release behavior of BSA-FITC on wafers was controlled by adding the additives such as collagen, small intestinal submucosa (SIS), poly(vinyl pyrrolidone) (PVP), and poly(thylene glycol) (PEG). The wafer prepared by PLGA and PCL exhibited slow release within $10\%$ for 30 days. But, those prepared by a variety of additives exhibited the controlled BSA release patterns with a dependence on the additive contents. furthermore, the wafers containing natural materials such as collagen and SIS showed more zero-order release profile than that with synthetic materials such as PVP and PEG. It was confirmed that the release of BSA from implantable wafers could be easily controlled by adding natural additives.

• Journal of Pharmaceutical Investigation
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• v.21 no.1
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• pp.51-55
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• 1991

Porous spheres composed of natural waxes and inorganic materials containing vitamin E acetate as a drug were prepared by impregnation method. Furthermore, the amount of vitamin E acetate entrapped in the spheres and the release rate of vitamin E acetate from the spheres were studied. The impregnation of vitamin E acetate was carried out by dipping the spheres in vitamin E acetate solutions. Entrapment mechanism of vitamin E acetate could be expressed in terms of Langmuir's adsorption isotherm. The amount of vitamin E acetate entrapped in porous spheres was influenced by the structure and concentration of the polymer used in vitamin E acetate solutions, and the concentration of vitamin E acetate. Release characteristics of vitamin E acetate from the spheres were investigated by withdrawing samples periodically and analyzing them by spectrophotomer.

• Journal of Pharmaceutical Investigation
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• v.32 no.2
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• pp.95-101
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• 2002

Matrix tablets of nifedipine (NP) were prepared with Eudragit, diluent (lactose or Ca. phosphate) and Mg. stearate employing two different preparation methods (wet granulation and direct compression) to develop its sustained-release dosage forms. The effects of various formulation factors on the dissolution rate of the drug were investigated. Dissolution test was studied in pH 6.8 phosphate buffer containing 1% sodium lauryl sulfate using the paddle method. Formulation factors were the type and content of Eudragit, the type of diluent and the tablet preparation method. The optimum formula of NP matrix tablet, which resulted in a similar dissolution profile to that from Adalat Oros used as a reference, was 30 mg NP, 10% Eudragit RS, 2% Mg. stearate and an adequate quantity of lactose to yield 500 mg weight using the wet granulation method.

• Journal of Pharmaceutical Investigation
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• v.19 no.2
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• pp.63-69
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• 1989

Dissolution characteristics of indomethacin (IMC) from hydrophobic polymer solid dispersions were investigated. IMC-polyvinyl chloride (PVC) and IMC-ethylcellulose (EC) solid dispersions were prepared. The dissolution patterns of pure IMC, IMC-PVC and IMC-EC solid dispersions prepared at various ratios (1:1, 1:3, 1:5, 1:9 and 1:19 w/w), and those of corresponding physical mixtures were compared. It was found that the dissolution rates of IMC from solid dispersions with PVC or EC decreased in the order of 1:1>1:3>1:5>1:9>1:19 as the drug to polymer ratios decreased. Also the dissolution rates of IMC from EC solid dispersions increased according to flow rate, but PVC solid dispersions were not affected significantly. After all, PVC and EC matrices could be applied in sustained-release preparation of IMC.

• Bulletin of the Korean Chemical Society
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• v.7 no.3
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• pp.213-217
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• 1986

A series of copolypeptides of glutamic acid and leucine have been synthesized by N-carboxy-${\alpha}$-amino acid anhydride procedure and cast to form injectable microparticulate monolithic devices in which indomethacin was physically dispersed. With these devices, various release properties and possible clinical application were studied. The release rate of the drug had a close relationship with the monomer composition of the copolymer matrix as well as the environmental pH condition. The monolithic device of glutamic acid/leucine = 50/50 was found to be the most promising one as a ploymeric delivery system of indomethacin. The intrinsic viscosity of this copolymer was 4.35 dl/g and the release rate was 18.5${\mu}g/g/day$.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.424.2-424.2
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• 2002

The in vivo release characteristics of rhGH-loaded PLGA microsphere prepared using a double emulsion process from hydrophilic 50:50 poly(D.L-lactide-co-glycolide) (PLGA) polymers were analyzed. This formulation showed particle size of ca 53.1$\mu\textrm{m}$ with high drug incorporation efficiency. To investigate in vivo release kinetics without the interference of formation of antibodies to rhGH in the experimental animals, the animals were immunosuppressed by treatment with Cyclosporin. (omitted)

• The Journal of Pediatrics of Korean Medicine
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• v.20 no.1
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• pp.109-135
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• 2006

Objective : In the present study, the author tried to investigate whether six oriental medical prescriptions named gamisingitang (SGT), gamijungtang (IJT), gamicheongpyetang (CPT), galhwengchihyosan (CHS), chwiyeontong (CYT), sigyoungcheongpyetang (SCPT) significantly affect mucin release from cultured hamster tracheal surface epithelial (HTSE) cells. Methode : Confluent HTSE cells were inetabolically radiolabeled with $^{3}H-glucosamine$ for 24 hrs and chased for 30 min in the presence of drugs aforementioned, respectively, to assess the effect of each drug on $^{3}H-mucin$ release. Possible cytotoxicities of effective drugs were assessed by measuring lactate dehydrogenase(LDH) release. Additionally, total elution profiles of control spent media and treatment sample (CPT, CHS, SCPT and CYT) through Sepharose CL-4B column were analysed and effect of CPT, CHS and CYT on MUC5AC mRNA expression in cultured HTSE cells were invsetigated. Results : (1) SGT and IJT did not affect mucin release without cytotoxicity; (2) CPT, SCPT and CHS significantly stimulated mucin release from cultured HTSE cells, with significant cytotoxicity; (4) CPT, CHS, SCPT and CYT chiefly affected the 'mucin' release and did not affect significantly the release of the releasable glycoproteins with less molecular weight than mucin. This result suggests that the four herbal prescriptions specifically affect the release of mucin ; (5) CTP and CHS did not significantly affect the expression levels of MUC 5AC mRNA, however, CYT significantly inhibit the expression levels of MUC 5AC mRNA. Conclusion : CYT can decrease the synthesis of mucin at gene level in cultured HTSE cells.

• Archives of Pharmacal Research
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• v.28 no.4
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• pp.493-501
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• 2005

Effect of solvents on physical characteristics and release characteristics of monolithic acetaminophen (APAP) hydroxypropylmethylcellulose (HPMC) matrix granules and tablets were examined. Various types and amounts of solvents were employed for granulation and coating. APAP and other excipients were mixed and were then wet-granulated in a high-speed mixer. The dried granules were then directly compressed and film-coated with low viscosity grade HPMC. As the amount of water increased, the size of granules also increased, showing more spherical and regular shape. However, manufacturing problems such as capping and lamination in tableting occurred when water was used alone as a granulating solvent. The physical properties of HPMC matrix granules were not affected by the batch size. The initial release rate as well as the amount of APAP dissolved had a tendency to decrease as the water level increased. Addition of nonaqueous solvent like ethanol to water resulted in good physical properties of granules. When compared to water/ethanol as a coating solvent, the release rate of film-coated HPMC matrix tablets was more sensitive to the conditions of coating and drying in methylene chloride/ethanol. Most of all, monolithic HPMC matrix tablet when granulated in ethanol/water showed dual release with about $50\%$ drug release immediately within few minutes followed by extended release. It was evident that the type and amount of solvents (mainly water and ethanol) were very important for wet granulation and film-coating of monolithic HPMC matrix tablet, because the plastic deforming and fragmenting properties of material were changed by the different strengths of the different solvents.