• Journal of Oral Medicine and Pain
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• v.42 no.3
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• pp.72-80
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• 2017

Purpose: Pilocarpine as a salivation stimulant in pill form has mostly been used to relieve oral dryness for xerostomic patients but its use may often be limited due to variable side effects from systemic absorption. Therefore, the purpose of this study was to investigate the effects of pilocarpine mouthwash on salivation according to the variable concentration and duration for healthy volunteers. Related adverse effects and subjective assessment on its effects on salivation were also examined. Methods: This study was performed as placebo-controlled, double-blind, randomized clinical trial. Thirty healthy volunteers (male=23, mean age=22.2 years) were randomly allocated to 6 groups with the different concentration of pilocarpine mouthwash (placebo, 0.1%, 0.5%, 1.0%, 1.5%, and 2.0%). The whole experiment consisted of 3 sessions according to the duration of mouthwash, i.e., 1, 3, and 5 minutes with the mean wash-out period ${\geq}2$ days between the sessions. Unstimulated whole saliva was collected before and after gargling with a mouthwash. Results: Salivation of the higher concentration groups ${\geq}1%$ significantly increased than those of lower concentration group. The application period of mouthwash did not cause any changes of salivary flow rate at the higher concentrations ${\geq}1.0%$. The lower concentrations of 0.5% and 0.1% had no effects on salivation even after 5-minute mouthwash. There was no significant difference between blood pressure and pulse rate before and after use of mouthwash. Conclusions: From the results of the current study, pilocarpine mouthwash with at least 1.0% concentration more than a minute might be clinically effective in salivation without any serious side effects. Dose of mouthwash rather than duration seems to be a critical factor to salivation.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• v.40 no.5
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• pp.225-232
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• 2014

Objectives: The purpose of this retrospective study is to find the differentiating characteristics of cystic and cystic-appearing lesions that involve the impacted mandibular third molar by analyzing panoramic radiographs and computed tomography images, and to aid the preoperative diagnosis. Materials and Methods: Eighty-one patients who had a mandibular cystic or cystic-appearing lesion that involved impacted mandibular third molar and underwent cyst enucleation were included in the study. The preoperative panoramic radiograph and computed tomography findings were analyzed in accordance to the histopathologic type. Results: Most of the cystic lesions containing the mandibular third molar were diagnosed as a dentigerous cyst (77.8%). The occurrence of mesio-distal displacement of the third molar was more frequent in the odontogenic keratocyst (71.4%) and in the ameloblastoma (85.7%) than in the dentigerous cyst (19.1%). Downward displacement was primarily observed in each group. Odontogenic keratocyst and ameloblastoma showed more aggressive growth pattern with higher rate of bony discontinuity and cortical bone expansion than in dentigerous cyst. Conclusion: When evaluating mandibular cystic lesions involving the impacted mandibular third molar, dentigerous cyst should first be suspected. However, when the third molar displacement and cortical bone absorption are observed, then odontogenic keratocyst or ameloblastoma should be considered.

• Imaging Science in Dentistry
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• v.38 no.1
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• pp.7-15
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• 2008

Purpose: This study provides comparative measurements of absorbed and effective doses for newly developed cone beam computed tomography (CT) in comparison with these doses for conventional CT. Materials and Methods: Thermoluminescent dosimeter rods (TLD rod: GR-200, Thermo Fisher Scientific Inc., Waltham, MA, USA) were placed at 25 sites throughout the layers of Male ART Head and Neck Phantom (Radiology Support Devices Inc., Long Beach, USA) for dosimetry. Implagraphy, DCT Pro (Vatech Co., Hwasung, Korea) units, SCT-6800TXL (Shimadzu Corp., Kyoto, Japan), and Crane x 3+(Soredex Orion Corp., Helsinki, Finland) were used for radiation exposures. Absorption doses were measured with Harshaw 3500TLD reader (Thermo Fisher Scientific Inc., Waltham, MA, USA). Radiation weighted doses and effective doses were measured and calculated by 2005 ICRP tissue weighting factors. Results: Absorbed doses in Rt. submandibular gland were 110.57 mGy for SCT 6800TXL (Implant), 24.56 mGy for SCT 6800TXL (3D), 22.39 mGy for Implagraphy 3, 7.19 mGy for DCT Pro, 5.96 mGy for Implagraphy 1, 0.70 mGy for Cranex 3+. Effective doses $(E_{2005draft)$ were 2.551 mSv for SCT 6800TXL (Implant), 1.272 mSv for SCT 6800TXL (3D), 0.598 mSv for Implagraphy 3, 0.428 mSv for DCT Pro and 0.146 mSv for Implagraphy 1. These are 108.6, 54.1, 25.5, 18.2 and 6.2 times greater than panoramic examination (Cranex 3+) doses (0.023mSv). Conclusion: Cone beam CT machines recently developed in Korea, showed lower effective doses than conventional CT. Cone beam CT provides a lower dose and cost alternative to conventional CT, promising to revolutionize the practice of oral and maxillofacial radiology.

• Journal of Pharmaceutical Investigation
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• v.33 no.2
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• pp.91-97
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• 2003

During the preparation of decoction from the mixture of Coptidis Rhizoma and Scutellariae Radix, insoluble copreciptate was formed. The coprecipitated product (COP) was composed of berberine and baicalin which was the active ingredient of Coptidis Rhizoma and Scutellariae Radix, respectively. COP was slightly soluble in water and could not be well absorbed after oral administration. This poor bioavailibility might be associated with its poor aqueous solubility. With the purpose of increasing the solubility and bioavailibility of COP, hydrolysis of COP by ${\beta}-glucuronidase$ was carried out. Hydrolyzed products (HOP) of COP were identified and assayed for active ingredients. The partition coefficient study, in situ absorption test, and pharmacokinetic study after oral administration were also performed. COP was found to be consisted of berberine and baicalin with molecular ratio of 1 to 1. This compound was hydrolyzed to berberine and baicalin by ${\beta}-glucuronidase$. The rate of hydrolysis was higher at higher temperature up to $50^{\circ}C$ and higher concentration of ${\beta}-glucuronidase$ up to 2500 unit under our experimental conditions. Baicalein, which is more liphophilic than baicalin, showed greater absorption in small intestine than baicalin did. The plasma concentrations of berberine and baicalein after oral administration of HOP were significantly higer than those of COP. The possible mechanism of increased bioavailibility of berberine and baicalein could be the hydrolysis of COP by ${\beta}-glucuronidase$. On the basis of the above results, it might be said that HOP should be a suitable preparation for increasing the bioavailibility of Coptidis Rhizoma and Scutellariae Radix.

• YAKHAK HOEJI
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• v.44 no.6
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• pp.578-587
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• 2000

The purpose of the present study was to design and prepare the optimum formulation for the oral administration of titrated extract of the unsaponifiable fraction of Zea mays L. (ETIZM). For this purpose, we simulated the blood concentration of ETIZM after its oral administration, changing the dissolution rate constants $(0.05{\sim}20\;hr^{-1})$. In vivo parameters, such as absorption rate constant $(k_a)$, elimination rate constant (k) and volume of distribution (Vd), were incorporated in the simulation on the basis of the experiments and literatures. When the dissolution rate constant $(k_r)$ is over $5\;hr^{-1}$, the absorption process appears to be the rate limiting step for the transport of ETIZM from the G.I. ract to the blood circulation. While less than $5\;hr^{-1}$, the dissolution rate considered to be the rate limiting step. Moreover, the optimum blood concentration was shown in the range from 1 to $5\;hr^{-1}$ of $k_r$ in the simulation. To design and prepare the tablets on the basis of the above results, 7 formula containing HPMC, PEG 4000 and PEG 6000 (1-5%, respectively) were prepared and evaluated. The tablets containing PEG 4000 (1%), PEG 6000 (1%) or PEG 4000 (5%) satisfy the optimum $k_r$ range ($1-5\;hr^{-1}$). These formulations, therefore, will be able to show the more effective blood concentration, compared with the commercial products after the oral administration.

• Journal of Pharmaceutical Investigation
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• v.24 no.2
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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.

• Biomolecules & Therapeutics
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• v.25 no.4
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• pp.452-459
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• 2017

In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability. The results showed that genistein-loaded solid lipid microparticles and nanoparticles exhibited a considerably increased drug dissolution rate compared to that of genistein bulk powder and suspension. The microparticles gradually released genistein as a function of time while the nanoparticles exhibited a biphasic drug release pattern, showing an initial burst drug release, followed by a sustained release. The oral bioavailability of genistein loaded in solid lipid microparticles and nanoparticles in rats was also significantly enhanced compared to that in bulk powders and the suspension. However, the bioavailability from the microparticles increased more than that from the nanoparticles mainly because the rapid drug dissolution rate and rapid absorption of genistein because of the large surface area of the genistein-solid lipid nanoparticles cleared the drug to a greater extent than the genistein-solid lipid microparticles did. Therefore, the findings of this study suggest that controlling the particle size of solid-lipid particulate systems at a micro-scale would be a promising strategy to increase the oral bioavailability of genistein.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1997.04a
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• pp.119-119
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• 1997

Valacyclovir is a L-valyl ester prodrug of acyclovir which is a highly effective and selective antiviral agent in the treatment of herpes virus diseases. Valacyclovir is rapidly and almost completely converted to acyclovir and increases the oral bioavailability of acyclovir three to five fold. However, the intestinal absorption mechanism of valacyclovir is not clear. If the improved absorption mechanism of valacyclovir is fully understood, it will provide a rationale of designing the amino acid ester prodrugs of polar drugs containing hydroxyl group. The main objective of our present study is to characterize the membrane transport mechanism of valacyclovir. Methods : Intestinal absorption of valacyclovir was investigated by using in-situ rat perfusion study and its wall permeability was estimated by modified boundary layer model. The membrane transport mechanism was also investigated through the uptake study in Caco-2 cells and in CHO-hPepTl cells. Results : In the rat perfusion study, the wall permeability of valacyclovir was ten times higher than acyclovir and showed concentration dependency, Valacyclovir also demonstrated a D,L stereo-selectivity with L-isomer having an approximately five-fold higher permeability than D-isomer. Mixed dipeptides and cephalexin, which are transported by dipeptide carriers, strongly competed with valacyclovir for the intestinal absorption, while L-valine did not show any competition with valacyclovir. This indicated that the intestinal absorption of valacyclovir could be dipeptide carrier-mediated. In addition, the competitive uptake study in Caco-2 cells presented that dipeptides reduced the valacyclovir uptake but valine did not. Also, in IC$\sub$50/ study, valacyclovir showed strong inhibition on the $^3$H-gly-sar uptake in CHO-hPepTl cells over-expressing a human intestinal peptide transporter. Taken together, the result from our present study indicated that valacyclovir utilized the peptide transporter for the intestinal absorption.

• The Journal of Korean Academy of Prosthodontics
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• v.30 no.4
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• pp.582-610
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• 1992

The long-term success of any dental implant is dependent upon the optimization of stresses which occur during oral function and parafunction. Especially, it has been suggested that there is an unique set of problems associated with joining an osseointegrated implant and a natural tooth with a fixed partial denture. For this particular case, although many literatures suggest different ways to avoid high stress concentrations on the bone surrounding the implant under static and dynamic loading conditions, but few studies on the biomechanical efficacy of each assertion have been reported. The purpose of this investigation was to evaluate the efficacies of clinically suggested methods on stress distribution under static load and shock absorption under dynamic load, using two dimensional finite element method. In FEM models of osseointegrated implant-natural tooth supported fixed partial dentures, calculations were made on the stresses in surrounding bone and on the deflections of abutments and superstructure, first, to compare the difference in stress distribution effects under static load by the flexure of fastening screw or prosthesis, or intramobile connector, and second, to compare the difference in the shock absorption effects under dynamic load by intramobile connector or occlusal veneering with composite resin. The results of this analysis suggest that : 1. Under static load condition, using an implant design with fastenign screw connecting implant abutment and prosthesis or increasing the flexibility of fastening screw, or increasing the flexibility of prosthesis led to the .increase in height of peak stresses in cortical bone surrounding the implant, and has little effect on stress change in bone around the natural tooth. 2. Under static load condition, intramobile connector caused the substantial decrease in stress concentration in cortical bone surrounding the implant and the slight increase in stress in bone around the natural tooth. 3. Under dynamic load condition, both intramobile connector and composite resin veneering showed shock absorption effect on bone surrounding the implant and composite resin veneering had a greater shock absorption effect than intramobile connector.

• Journal of Pharmaceutical Investigation
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• v.27 no.2
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• pp.133-137
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• 1997

Buccal absorption test of omeprazole in human was performed to determine the permeability of the drug molecule through oral mucous membrane. Oral mucosal adhesive tablets of omeprazole were prepared by compressing the omeprazole with a mixture of sodium alginate and hydroxypropylmethyl cellulose (HPMC) as bioadhesive polymers, magnesium oxide (MgO) as a stabilizer and sodium carboxymethyl cellulose (Na CMC) or cros-carmellose sodium (Ac-Di-Sol) as disintegrants. The bioadhesive force, stability in saliva and release characteristics of the tablets were evaluated. Omeprazole was absorbed about 23% in 15 min through human buccal mucous membrane. Furthermore, omeprazole was stable in saliva for more than 8 hrs when MgO was added to the tablet as the amount of 2.5 fold of omeprazole. The release rate of omeprazole was increased with increasing the amount of sodium alginate in the tablet. From these results, it is suggested that tablets composed of [omeprazole/HPMC/sodium alginate/MgO/Ac-Di-Sol and/or Na CMC (20/6/24/50/10) (mg/tablet)] are potential candidate for buccal drug delivery system.