• Title/Summary/Keyword: Oral delivery system

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Controlled Transdermal Delivery of Loxoprofen from an Ethylene-Vinyl Acetate Matrix

  • Ryu, Sang-Rok;Shin, Sang-Chul
    • Journal of Pharmaceutical Investigation
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    • v.41 no.6
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    • pp.347-354
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    • 2011
  • Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances and acidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aim of this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhanced transdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug concentration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The solubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased with increased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activation energy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dose from the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhanced controlled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetration enhancer could be useful in the development of a controlled drug delivery system.

ANALYSIS OF MINOCYCLINE IN TISSUE AND SERUM AFTER LOCAL APPLICATION OF MINOCYCLINE OINTMENT (by High-Performance Liquid Chromatography) (미노싸이클린 연고의 근육 내 투여 후 조직 및 혈중 약물농도의 분석 (High-Performance Liquid Chromatography를 이용하여))

  • Hwang, Hye-Wook;Lee, Sang-Chull;Kim, Sung-Jin
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.25 no.4
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    • pp.304-310
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    • 1999
  • This study was designed to find the effect of Minocycline loaded microcapsule applied locally to tissue by measuring drug concentration in tissue and serum by HPLC and to achieve optimal drug delivery system and duration to a specific target site. Control group were administrated minocycline intramuscularly twice a day with $0.2{\mu}g/100g$ for 1 to 10 days. In experimental group, surgical wound was created on Rt. cheek and then minocycline loaded microcapsule was applied into the space between superficial and deep layer of masseter muscle. Animals were sacrificed at 1, 3, 5, 7, 10 days after initial administration, blood was obtained from heart and right masseter muscle was excised. Blood sample was centrifuged at 3000rpm for 15min. Tissue sample was homogenized, left at room temperature for 48hr and centrifuged at 4000g for 5min. Supernatant was completely dried and dissolved in distilled water. Analysis was conducted using a ${\mu}Bondapack$ C18 column. The mobile phase was 0.2M Ammonium Oxalate/0.1M EDTA/DMF=11/4/5 solution, which was injected into the column and detected with photodiode detector at 344nm wavelength. The results were as follows : 1. This method was reliable, could be replicated and suitable for minocycline analysis in tissue as well as serum. 2. In tissue, concentration of minocycline of experimental group was higher than that of control group for 5days. 3. Except 1 day, concentration of minocycline in serum of experimental group was lower than that of control group. 4. Concentration of minocycline in tissue was much higher than that in serum. From these results, minocycline loaded microcapsule might be effective tool for local drug delivery system might be useful for treatment of infections of oral and maxillofacial region and management of infected surgical wound, minimizing systemic effects.

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The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies (이트라코나졸 마이크로스폰지의 약물 전달 시스템: 제조, 특성 및 방출 연구)

  • Cho, Young-Ho;Lee, Jong-Hwa;Kim, Hak-Hyung;Lee, Gye-Won
    • KSBB Journal
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    • v.26 no.3
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    • pp.217-222
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    • 2011
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of $Eudragit^{(R)}$ E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.

Percutaneous absorption Characteristics of Anti hyperlipidemia Gel Ointment using Fibric acid (Fibric acid를 이용한 항고지혈증 겔 연고의 경피 흡수 특성)

  • Jung, Duck-Chae;Hwang, Sung-Kwy;Oh, Se-Young
    • Journal of the Korean Applied Science and Technology
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    • v.27 no.4
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    • pp.407-414
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    • 2010
  • New biological treatments were being developed at a record place, but their potential could be compromised by a significant obstacle: the delivery of these drugs into a body. Pharmaceutical delivery is now nearly as important as product. New systems are being developed, and Drug Delivery Markets Series cover these new systems. Transdermal Delivery System(TDS) is often used as a method of drug dosage into the epidermic skin. An approach used to delivery drugs through the skin for therapeutic use as an alternative to oral, intravascular, subcutaneous and transmucosal routes. Various transdermal drug delivery technologies are described including the use of suitable formulations, carriers and penetration enhancers. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other methods of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharides, such as karaya gum and glucomannan, were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, drug contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in fibric acid(ciprofibrate) such as lipophilic drug in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate. Especially, this result suggests a possible use of polysaccharide gel ointment matrix as a transdermal delivery system of anti-hyperlipoproteinemic agent.

BIOLOGIGIC MEMBRANE FOR GUIDED BONE REGENERATION (골 재생을 위한 생물학적 유도막)

  • Hong, Jong-Rak;Kang, Na-Ra;Choung, Pill-Hoon
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.30 no.1
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    • pp.17-24
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    • 2004
  • The purpose of this study was to evaluate the stability and efficacy of biologic membrane made of freeze-dried cartilage as a barrier to facilitate guided bone regeneration in experimental non-healing bone defects in the rat mandible. Nine adult Sprague-Dawley rats (400-500g) were used in experiment. 5.0mm in diameter were created on the mandibular angle area by means of slow-speed trephine drill. In microscopic examination, dynamic immature bone forming at 2 weeks and its calcification at 4 weeks were observed. The membrane made of lyophilized cartilage taken from human costal cartilage seems to be very effective for guided bone regeneration as a biologic membrane and the scaffold for attachment of cells or local drug delivery system of growth factor, which may meet the ideal requirement of a barrier membrane and graft materials.

Plants as platforms for the production of vaccine antigens (항원 생산 기반으로서의 식물 연구)

  • Youm, Jung-Won;Jeon, Jae-Heung;Joung, Hyouk;Kim, Hyun-Soon
    • Journal of Plant Biotechnology
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    • v.37 no.3
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    • pp.250-261
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    • 2010
  • The expression of vaccine antigens in transgenic plants has the potential to provide a convenient, stable, safe approach for oral vaccination alternative to traditional parenteral vaccines. Over the past two decades, many different vaccine antigens expressed via the plant nuclear genome have elicited appropriate immunoglobulin responses and have conferred protection upon oral delivery. Up to date, efforts to produce antigen proteins in plants have focused on potato, tobacco, tomato, banana, and seed (maize, rice, soybean, etc). The choice of promoters affects transgene transcription, resulting in changes not only in concentration, but also in the stage tissue and cell specificity of its expression. Inclusion of mucosal adjuvants during immunization with the vaccine antigen has been an important step towards the success of plant-derived vaccines. In animal and Phase I clinical trials several plant-derived vaccine antigens have been found to be safe and induce sufficiently high immune response. Future areas of research should further characterize the induction of the mucosal immune response and appropriate dosage for delivery system of animal and human vaccines. This article reviews the current status of development in the area of the use of plant for the development of oral vaccines.

Alginate Beads as Controlled Release Polymeric Drug Delivery System (Alginate Bead를 이용한 고분자 약물의 제어방출형 약물수송체)

  • Hwang, Sung-Joo;Rhee, Gye-Ju;Jo, Hang-Bum;Lee, Ki-Myung;Kim, Chong-Kook
    • Journal of Pharmaceutical Investigation
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    • v.23 no.1
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    • pp.19-26
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    • 1993
  • The purpose of this paper is to explore the possible applicability of alginate beads as an oral controlled release system of polymeric drugs. Cellulase was used as a model polymeric drug. The release of cellulase from alginate beads was moderately affected by the ratio of cellulase to sodium alginate and strongly affected by $CaCl_2$ concentration. However, the release was not particularly affected by the other factors such as sodium alginate concentration and curing time. The drug was not released from alginate beads at pH 1.2, but was released continuously up to 8 hr at pH 6.8. At pH 6.8, the beads were swollen highly up to 3 hr, thereafter, were eroded into the bulk solution up to 6 hr, completely. Drug release from the beads can be caused due to diffusion and erosion of the matrix. Activity of cellulase was reduced when alginate beads containing cellulase were stored in simulated gastric juice. Further investigation would be necessary to improve the acid resistance of the beads. Since the release of cellulase as a model polymeric drug could be controlled by the regulation of the preparation conditions of alginate beads, the alginate beads may be used for a potential oral controlled release system of such polymeric drugs as polypeptide drugs.

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The relationship between social values and health system values in dental healthcare hygienist (치과병의원에 근무하는 치과위생사의 사회적 가치관과 보건의료체계에 대한 가치관의 관련성)

  • You, So-Yeon;Park, Eun-Mi;Jang, Jong-Hwa
    • Journal of Korean society of Dental Hygiene
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    • v.11 no.3
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    • pp.353-361
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    • 2011
  • Objectives : This study was to examine the social value of dental hygienists, their values about the health system and the relationship of all the related variables. Methods : The subjects in this study were 205 dental hygienists who worked in dental clinics and hospitals on Seoul. A survey was conducted from August 12 to October 15, 2010. The questionnaire consisted of nine items about general characteristics, two items about social values and 11 about values of the health system. The items related to social values and values of the health system were prepared by translating the items used in David et al's study, and the Cronbach alpha coefficient of those items respectively 0.80 and 0.76. Results : The dental hygienists got 3.94 in social values, which was above the average. In terms of values about the health care system, their values of the treatment delivery system(3.92) rated highest, followed by values of patient rights(3.79) and values of institutional restrictions(3.25). Their socal values had a closest positive correlation to their values of the treatment delivery system, and their values of patient rights had a strong positive correlation to those of the treatment delivery system and was positively correlated to those of institutional regulations as well. And there was a positive correlation between their values of the treatment delivery system and institutional regulations(r=.276). Conclusions : The above-mentioned findings illustrated that the social values of the dental hygienists had a positive correlation to their values of the health system. Therefore the kinds of educational programs that help dental hygienists to build their social values and values of the health system should be developed to improve their job efficiency as oral health experts.

Mucosal Immune System and M Cell-targeting Strategies for Oral Mucosal Vaccination

  • Kim, Sae-Hae;Lee, Kyung-Yeol;Jang, Yong-Suk
    • IMMUNE NETWORK
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    • v.12 no.5
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    • pp.165-175
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    • 2012
  • Vaccination is one of the most effective methods available to prevent infectious diseases. Mucosa, which are exposed to heavy loads of commensal and pathogenic microorganisms, are one of the first areas where infections are established, and therefore have frontline status in immunity, making mucosa ideal sites for vaccine application. Moreover, vaccination through the mucosal immune system could induce effective systemic immune responses together with mucosal immunity in contrast to parenteral vaccination, which is a poor inducer of effective immunity at mucosal surfaces. Among mucosal vaccines, oral mucosal vaccines have the advantages of ease and low cost of vaccine administration. The oral mucosal immune system, however, is generally recognized as poorly immunogenic due to the frequent induction of tolerance against orally-introduced antigens. Consequently, a prerequisite for successful mucosal vaccination is that the orally introduced antigen should be transported across the mucosal surface into the mucosa-associated lymphoid tissue (MALT). In particular, M cells are responsible for antigen up-take into MALT, and the rapid and effective transcytotic activity of M cells makes them an attractive target for mucosal vaccine delivery, although simple transport of the antigen into M cells does not guarantee the induction of specific immune responses. Consequently, development of mucosal vaccine adjuvants based on an understanding of the biology of M cells has attracted much research interest. Here, we review the characteristics of the oral mucosal immune system and delineate strategies to design effective oral mucosal vaccines with an emphasis on mucosal vaccine adjuvants.