• Title/Summary/Keyword: oral delivery

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Development of Controlled Release Oral Drug Delivery System by Membrane-Coating Method-II-Correlation Between Acetaminophen Concentrations in Plasma and Sativa Samples of Man- (피막법에 의한 경구투여용 제어방출 제제의 개발-II-사람에 있어서 아세트아미노겐 혈장 중 농도와 타액 중 농도와의 상관성-)

  • Shim, Chang-Koo;Kim, Mi-Ae;Lee, Min-Hwa;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.20 no.1
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    • pp.29-33
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    • 1990
  • Plasma and saliva concentrations of acetaminophen (AAP) were determined at various time points by HPLC after oral administration of AAP tablets (AAP 500 mg) to four healthy male Korean subjects. Saliva concentrations (S) of AAP were significantly correlated with plasma AAP concentrations (P). The S/P ratio of AAP was calculated to be 1.05 (r =0.944, $p<10^{-6}$) for all the data points from the subjects. It showed a little intersubject variation and ranged from 0.89 to 1.46 in each subject. Bioavailability parameters such as AUC, $C_{max}$ and $T_{max}$ which are usually obtained from the plasma concentration data will be predictable approximately by saliva concentration data. Saliva seems to be very convinient and useful samples for the preliminary studies of bioavailability and bioequivalence of AAP preparations, since it can be collected frequently without any painful venipuncture to the subjects, that is inevitable in plasma sampling. Evaluation of the bioavailability of a preparation by saliva samples will reduce the cost, time and safety risk greatly in developing a new drug delivery system for AAP.

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Development of Controlled Release Oral Drug Delivery System by Membrane-Coating Method-III- Preparation of Theophylline Tablets and Pharmacokinetic Evaluation in Man- (피막법에 의한 경구투여용 제어방출제제의 개발-III-테오필린함유 제어방출제제의 제조 및 사람의 타액중 농도로부터의 평가-)

  • Shim, Chang-Koo;Kim, Chong-Kook;Lee, Min-Hwa;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.22 no.3
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    • pp.205-210
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    • 1992
  • In order to develop a controlled-release oral drug delivery system (DDS) of theophylline (TP), microporous membrane-coated tablets were prepared and evaluated in vitro and in vivo. Rapidly water-soluble core tablets of TP (300 mg) were prepared by wet granulation and compression technique, Then the core tablets were spray-coated with polyvinylchloride (PVC) in which micronized sucrose particles were dispersed. Effect of formula compositions of coating suspensions on the pharmaceutical characteristics such as membrane strength and dissolution was investigated in vitro. The membranes remained unbroken in pH 1.2 buffer at $37^{\circ}C$ at least for 2 hours after the disintergration test. TP was released from the coated-released tablets at a zero-order rate over 8 hours. The release at pH 1.2 and 4.0 was similar in rate but a little more rapid than that at pH 6.8. The coated tablets were administered to three healthy male volunteers and their saliva profiles of TP were compared with those from the commercial sustained release TP tablets such as Slobid and Asconthin. Saliva TP concentrations from the coated tablets were successfully sustained over 48 hours after the dosing and were comparable to those of the commercial sustained-release tablets. The membrane-coating technique is very simple and does not need any sophisticated equipments. In this respect, the membrane-coated tablets may be superior to the commercial sustained-release tablets and this technique is worth adopting by the pharmaceutical industries.

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EVIDENCE OF SUSTAINED RELEASE OF CHLORHEXIDINE ADDED TO ACRYLIC RESIN : PRELIMINARY INVESTIGATION OF A POTENTIAL DRUG DELIVERY SYSTEM (아크릴릭 레진에 혼합된 클로르헥시딘의 방출 : 새로운 방법의 약물송달시스템을 위한 예비실험)

  • Choi, Yeong-Chul;Lee, Eun-Yeong;Lee, Jin-Yong
    • Journal of the korean academy of Pediatric Dentistry
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    • v.25 no.2
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    • pp.259-267
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    • 1998
  • For more than two decades, many investigators have tried a variety of methods for delivering antimicrobial agents to the oral cavity with the objective of eliminating mutans streptococci. In the belief that the effectiveness of chemotherapy might be improved by a more effective delivery system, the intention of the present study was to exploit a new drug delivery system delivering chlorhexidine to the oral cavity. The vehicle delivering chlorhexidine tested in this study was self-curing acrylic resin(polymethyl methacrylate). The powder of the acrylic resin was polymerized with the 5 different liquid preparations, in which $Chlorzoin^{(R)}$ was mixed with five different monomer/Chlorzoin ratios immediately prior to the polymerization, in a stainless steel mold ($40mm{\times}40mm{\times}2mm$). A total of 50 cured resin specimens were divided into 5 groups according to the different monomer preparations. Every specimen was soaked in an airtight container filled with distilled water (100 ml) and then kept in an incubator at $37^{\circ}C$. The solutions (0.8 ml) were collected from the container at every 24 hours, and the amount of released chlorhexidine in the solutions was measured in an ultraviolet spectrophotometer at 250nm. The container was refilled with distilled water every after measurement. This procedure was repeated for 14 days. It was found that chlorhexidine was continuously released from all of the 50 specimens during the experimental period. And it was noted that the pattern of chlorhexidine release was a type of sustained-release preparation, that is, the amount of the released chlorhexidine at the first day in all 5 groups was high (p<0.0001), and then the release was decreased during the rest of the experimental period (p<0.001).

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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.

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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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.

Inducing apoptosis by the inhibition of c-myb in oral squamous carcinoma cell line, KB cell

  • Lee, Jung-Chang;Moon, Hyun-Ju;Lee, Young-Hee;Jung, Ji-Eun;Sharma, Manju;Jhee, Eun-Jung;Yi, Ho-Keun
    • International Journal of Oral Biology
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    • v.32 no.4
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    • pp.127-133
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    • 2007
  • Oral squamous cell carcinoma (OSCC) is the most common malignancy and is a major cause of worldwide cancer mortality. The proto-oncogene c-myb plays an important role in regulation of cell growth and differentiation, and it is expressed at high levels in hematopoietic cells and many other types of cancers. However, the function of c-myb is not well known in OSCC. The present study aimed to reveal the function of c-myb and to test the alternation of cell growth and signaling by c-myb in OSCC. In this study, c-myb and dominant-negatibe myb(DNmyb) were expressed in an adenovirus-mediated gene delivery system to KB cells. The over-expressed c-myb brought increased cellular proliferation compared with control cells. However, DN-myb infected KB cells showed significant reduction of cell growth and enhanced induction of apoptosis to activate PARP and caspase 9. c-myb induced increase of IGF-I, -II and IGF-IR expressions while DN-myb down-regulated these expression. Activation of ERK and Akt/PKB pathway was shown only in c-myb transduced cells. These findings suggest that the role of c-myb in cell growth of oral cancer cells is partially mediated through the modulation of IGFs, ERK and Akt/PKB. From this results, DN-myb is strongly recommended as a curable gene for the treatment of c-myb dependent malignancies such as OSCC.

Basic Understanding of Transcutaneous Electrical Nerve Stimulation

  • Jung, Jae-Kwang;Byun, Jin-Seok;Choi, Jae-Kap
    • Journal of Oral Medicine and Pain
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    • v.41 no.4
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    • pp.145-154
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    • 2016
  • Transcutaneous electrical nerve stimulation (TENS) is one of the representative physiotherapical modalities used for the treatment of various musculoskeletal disorders by the application of electrical stimuli. In dental practice, it has long been used in the treatment of acute and chronic orofacial pain conditions including temporomandibular disorders. TENS is the delivery of therapeutic electrical stimuli with a variety of electrical intensity, frequency and duration to stimulate peripheral nerve through surface electrodes with various form and placement. While controversy still remains over the clinical effectiveness and application of TENS, basic understanding of its electrical properties and the expected biological reactions is important to increase the therapeutic effect and decrease the risk of possible side effects. This review, therefore, focuses on basic understanding of TENS including its underlying mechanisms and stimulation parameters.

Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process

  • Rhee, Yun-Seok;Lee, Jae-Hwi;Lee, Beom-Jin;Park, Eun-Seok
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.103-112
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    • 2010
  • Pellets, which are multiple-unit dosage systems, have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. This review focuses on the current status and explores extrusion-spheronization technique with special attention to controlled-release application of pellets including coated pellets for delayed release formulations, coated pellets for colon delivery, coated pellets for sustained drug delivery, sustained-release matrix pellets, pellets compressed into tablets, bioadhesive pellets, floating pellets, and pelletization with solubilization techniques.

Active components delivery rate from acrylic resin maxillary surgical obturator: Part I

  • Al-Kaabi, Arshad;Hamid, Mohammed A.
    • Advances in materials Research
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    • v.9 no.2
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    • pp.109-114
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    • 2020
  • The purpose of this study was to observe the trend of compounds release from acrylic resin oral prosthesis when used for drug delivery as well as a restoration. In this study, 10 specimens of heat-cured polymethylmethacrylate material were prepared and loaded with methylene blue biological stain. The specimens were then submerged in vials with 5 ml distilled water for 24 hours. The extraction procedure continued for 4 days, each day the specimens were immersed in another 5 ml distilled water vial. All extracted solutions were analyzed by visible light spectroscopy for absorbance comparison. The statistical results showed that the absorbance values were significantly different in the first day of extraction than the following days. However, there was no statistical difference among the 2nd, 3rd and 4th days of extraction. Biological stain loading to acrylic resin at the mixing stage, and then after extraction in distilled water, showed a burst release during the first day followed by a constant release during the following few days.