• Journal of Pharmaceutical Investigation
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• 제38권2호
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• pp.105-110
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• 2008

Indapamide (4-chloro-N-(2-methyl-1-indolinyl)-3-sulfamoyl-benz-amide) is an oral antihypertensive diuretic agent indicated for the treatment of hypertensive. The diuretic and natriuretic effects are mainly due to the structure of o-chlorobenzenesulfonamide. The objective of this study was to formulate sustained release indapamide granules and assess their formulation variables. Granules were prepared by fluid bed coating method and consist of drug layer and membrane layer. The granules were coated with HPC and ethyl cellulose along with plasticizer dibuthyl sebacate. The release of indapamide depended on the type of Eudragit such as RS and NE 30 D used in the formulation controlled release layer. These results obtained clearly suggest that the sustained release oral delivery system for indapamide could be designed with satisfying drug release profile approved.

• Journal of Dental Anesthesia and Pain Medicine
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• 제18권5호
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• pp.287-294
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• 2018

Mandibular third molar extraction is commonly performed in dental clinics. However, the optimal method of anesthesia has not been established for this procedure. The conventional inferior alveolar nerve block is the most widely used method. However, its success rate is not high and it may lead to complications, such as aspiration and nerve injury. Therefore, various anesthesia methods are being investigated. Articaine has been proven to be efficacious in a number of studies and is being used with increasing frequency in clinical practice. In this review article, we will briefly review various local anesthesia techniques, anesthetics, and a computer-controlled local anesthetic delivery (CCLAD) system, which reduces pain by controlling the speed of drug injection, for mandibular third molar extraction.

• Journal of Pharmaceutical Investigation
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• 제18권1호
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• pp.5-8
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• 1988

Physical properties of oral adhesive tablets prepared with four kinds of gums for topical or systemic drug delivery were investigated. Oral adhesive tablets containing 5mg of brilliant blue(BB) were prepared from direct compression. Viscosity of 2% gum solutions, water absorption, fracture resistance, stickiness of tablets, and dissolution of BB in pH 6.8 dissolution medium were tested. Acacia showed good stickiness and fracture resistance, and tragacanth showed good retarding effect on the release of BB from tablets. Therefore, tablets with varing ratios of acacia and tragacanth were prepared and their physical properties were examined. In conclusion, it was possible to obtain some adequate properties by compounding acacia and tragacanth.

• Journal of Periodontal and Implant Science
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• 제51권1호
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• pp.53-62
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• 2021

Purpose: This study aimed to evaluate the clinical and microbiological efficacy of adjunctive local delivery of minocycline (Periocline^®) in patients receiving supportive periodontal therapy (SPT) after initial treatment. Methods: The participants were 16 men and 8 women (age, 20-65 years) who had at least 15 natural teeth, underwent SPT for more than 1 year due to chronic periodontitis, had 4 or more periodontal pocket sites deeper than 5 mm, and showed >25% gingival bleeding on probing (BoP). They were randomly assigned to the test and control groups. In the test group, mechanical debridement and local antibiotic delivery were performed for all periodontal sulci/pockets; in the control group, mechanical debridement and saline irrigation were performed. In patients who underwent SPT for more than 1 year, clinical and microbiological examinations were performed at baseline and 1 and 3 months after SPT. The clinical examination included an assessment of the periodontal pocket depth, clinical attachment level, plaque index, and BoP. Microbial tests were performed using real-time polymerase chain reaction; the relative ratios of Porphyromonas gingivalis and Fusobacterium nucleatum were determined. Results: Both groups showed significant improvements in clinical parameters at 1 and 3 months from baseline; there were no significant changes between months 1 and 3. Intergroup differences were insignificant. The microbiological analysis revealed no significant differences in P. gingivalis and F. nucleatum ratios across time points. While intergroup differences were insignificant, there was a tendency for the P. gingivalis and F. nucleatum ratios to decrease in the test group. Conclusions: Mechanical debridement in patients receiving maintenance therapy resulted in clinically significant improvement; the effectiveness of additional local delivery of antibiotics was not significant. The ratios of P. gingivalis and F. nucleatum showed a tendency to decrease in the test group, although it was not significant.

• Molecules and Cells
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• 제42권11호
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• pp.755-762
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• 2019

Despite decades of research into colorectal cancer (CRC), there is an ongoing need for treatments that are more effective and safer than those currently available. Lactic acid bacteria (LAB) show beneficial effects in the context of several diseases, including CRC, and are generally regarded as safe. Here, we isolated a Lactobacillus rhamnosus (LR)-derived therapeutic protein, p8, which suppressed CRC proliferation. We found that p8 translocated specifically to the cytosol of DLD-1 cells. Moreover, p8 down-regulated expression of Cyclin B1 and Cdk1, both of which are required for cell cycle progression. We confirmed that p8 exerted strong anti-proliferative activity in a mouse CRC xenograft model. Intraperitoneal injection of recombinant p8 (r-p8) led to a significant reduction (up to 59%) in tumor mass when compared with controls. In recent years, bacterial drug delivery systems (DDSs) have proven to be effective therapeutic agents for acute colitis. Therefore, we aimed to use such systems, particularly LAB, to generate the valuable therapeutic proteins to treat CRC. To this end, we developed a gene expression cassette capable of inducing secretion of large amounts of p8 protein from Pediococcus pentosaceus SL4 (PP). We then confirmed that this protein (PP-p8) exerted anti-proliferative activity in a mouse CRC xenograft model. Oral administration of PP-p8 DDS led to a marked reduction in tumor mass (up to 64%) compared with controls. The PP-p8 DDS using LAB described herein has advantages over other therapeutics; these advantages include improved safety (the protein is a probiotic), cost-free purification, and specific targeting of CRC cells.

• 약학회지
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• 제41권1호
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• pp.30-37
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• 1997

In order to formulate a controlled release system for oral drug delivery, the microcapsules were prepared in w/o emulsion containing cefaclor as a water-soluble model drug by th e method of interfacial polycondensation. Gelatin wis selected as a suitable polymer for interfacial polycondensation. Gelatin solution containing drug was emulsified in an organic phase under mechanical stirring. After emulsification, terephthaloyl chloride was added as cross linking agent, followed by mechanical stirring, washing and drying. Physical characteristics of microcapsules were investigated by optical microscopy, scanning electron microscopy and particle size analysis. Mean particle sizes of gelatin microcapsules were, in the range, of about 20~50 ${\mu}$m. The microcapsules were in good apperance with spherical shapes before washing, but were destroyed partially after washing and drying, even though some microcapsules were still maintained in their shapes. Contents of cefaclor in the microcapsules were calculated by UV spectrophotometry after 3 days extraction with pH 4 carbonate buffer solution. The effects of cross linking time. pH. concentration of cross-linking agent, and temperature on drug release kinetics have been discussed extensively.

• KSBB Journal
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• 제23권5호
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• pp.408-412
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• 2008

본 연구에서는 당뇨병치료제인 로시글리타존약물를 생분해성 PLGA 나노입자에 봉입시킴으로서 위장흡수율과 물에 대한 용해도를 증가시키기 위한 나노제제 개발에 기반을 두고 있다. 특히 제조조건에 따라 형태 및 크기가 조절가능한 나노입자를 제조하고자 하였고, 실험결과 Emulsion-evaporation방법을 사용하여 100-150 nm 크기의 고른 입자분포를 가진 나노입자를 제조하였다. 다양한 농도의 약물 존재하에서 나노입자를 제조함으로서 1%까지의 약물이 80% 이상의 봉입율로 제조될 수 있음을 확인하였다. 또한 나노입자의 크기는 PVA양을 조절하면서 크기분포를 제어하였다. 36시간 동안의 용출실험 결과 초기 약간의 Burst effect가 있었으나 36시간동안 일정하게 약물이 용출되어 나옴을 확인하였다. 앞으로의 연구를 통해, 고효율의 경구제제용 당뇨병치료제 운반체 개발에 중점을 둘 예정이다.

• Journal of Pharmaceutical Investigation
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• 제20권2호
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• pp.89-95
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• 1990

Ethylcellulose-PEG 4000 film coated on core tablets was investigated as a potential drug delivery system for the controlled release of chlorpheniramine maleate (CPM). The kinetic analysis of the release data indicated that CPM release followed a diffusion-controlled model, where the quantity released per unit area is proportional to the square root of time. The effect of the film composition, CPM concentration, plasticizer concentration and CPM solubility on the release characteristics were examined. The release rate constant increased as CPM concentration increased. It also increased as the PEG 4000 content in the film increased above 10%(w/w), however, it decreased as the PEG 4000 content increased in the concentration range below 10%(w/w). The release rate constant was not affected by the coated weight on the core tablet. The film-coated tablets which contain CPM only in the coated film layer seemed to be a potential oral drug delivery system for the controlled release of CPM.

• Journal of Ginseng Research
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• 제47권6호
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• pp.694-705
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• 2023

Panax ginseng Meyer is a traditional Chinese medicine that is widely used as tonic in Asia. The main pharmacologically active components of ginseng are the dammarane-type ginsenosides, which have been shown to have anti-cancer, anti-inflammatory, immunoregulatory, neuroprotective, and metabolic regulatory activities. Moreover, some of ginsenosides (eg, Rh2 and Rg3) have been developed into nutraceuticals. However, the utilization of ginsenosides in clinic is restrictive due to poor permeability in cells and low bioavailability in human body. Obviously, the dammarane skeleton and glycosyls of ginsenosides are responsible for these limitations. Therefore, improving the oral bioavailability of ginsenosides has become a pressing issue. Here, based on the structures of ginsenosides, we summarized the understanding of the factors affecting the oral bioavailability of ginsenosides, introduced the methods to enhance the oral bioavailability and proposed the future perspectives on improving the oral bioavailability of ginsenosides.

• Journal of Pharmaceutical Investigation
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• 제24권2호
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• pp.73-83
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• 1994

Applications of liposomes as a drug carrier for the oral delivery of poorly-absorbable macromolecular drugs have been limited, because of their instability in gastrointestinal environments including pH, bile salts, and digestive enzymes. Two polysaccharides, dextran(DX) and pullulan(PL), were introduced to the preformed liposomes in order to enhance the stability. Palmitoyl derivatives of polysaccharides, palmitoyldextran(PalDX) and palmitoylpullulan(PalPL), were synthesizd and introduced to the liposomes during preparation for the same purpose of stability. The effects of these polysaccharides coating were evaluated basically by physical properties of particle size distribution and optical microscopy, then compared with uncoated liposomes by the observations of both in vitro stability and in vovo absorption characteristics. The geometric mean diameters of polysaccharide-coated liposomes were greater than that of uncoated liposome, showing the outermost polysaccharide-coated layer under the optical microscopy. In vitro stabilities of uncoated or polysaccharides-coated liposomes were measured by turbidity changes in various pH buffer solutions containing sodium choleate as bile salts. While uncoated liposome was very sensitive to bile salts, polysaccharides-coated liposomes were stable in relatively higher concentrations of sodium choleate, giving the results of better stability of PalDX- and PalPL-coated liposomes than that of DX- and PL-coated liposomes. After liposomal encapsulation of acyclovir(ACV), an antiviral agent as a model drug, it has been administered orally to rats as dose of ACV 40 mg/kg. Plasma concentrations of ACV were assayed by HPLC and analyzed by model-independent pharmacokinetics. Pharmacokinetic parameters of Cmax, tmax, and [AUC] have been compared.