The purpose of this study was to investigate the intestinal and nasal absorption enhancement of cefotaxime (CTX) by ion-pairing with counterions and to design an effective oral and intranasal drug delivery system for antibiotics. Counterions for absorption promotion were cationic surfactants [cetylpyridinium chloride (CP), cetrimide (CT) and benzalkonium chloride (BA)]. In the presence of counterions, the apparent partition coefficient of cefotaxime was increased depending on the molar concentration of the counterions. Anion interference was observed for ion-pairing of cefotaxime with counterions because of the counterbalance between an anion and counterions. The present study employed the in situ simultaneous nasal and intestinal perfusion technique in rats. The apparent permeabilities $(P_{app})$ of cefotaxime were $1.43{\pm}0.04{\times}10^{-5}\;cm/sec(mean{\pm}S.E)$ in the nasal cavity and 0 in the jejunum, respectively, which indicated that the intrinsic absorptivity of cefotaxime was greater in the nasal cavity than in the jejunum. When ionupairing formers were used, the decreasing order of apparent cefotaxime permeability $(P_{app},\;10^{-5}\;cm/sec)$, corrected for surface area of absorption, was as followings: $BA\;(7.50{\pm}0.36)\;>\;CT\;(4.92{\pm}0.24)\;>\;CP\;(3.01{\pm}0.17)$ in the jejunum and $BA\;(22.31{\pm}1.36)\;>\;CP\;(18.24{\pm}0.81)\;>\;CT \;(16.22{\pm}1.87)$ in the nasal cavity. The increase in permeability of cefotaxime was about 13-fold in the rat nasal cavity and was marked in the rat jejunum for ion-pairing with counterions as compared to those without ion-pairing. The damages of jejunal and nasal mucosal membrane by counterions were observed within approximately 2hrs after removal of ion-pair of cefotaxime with counterions from the nasal cavity and jejunum. These results suggest that CP can be used as an ion-pairing former in the jejunum and CP and CT can be used as ion-pairing formers in the nasal cavity for cefotaxime, as well as for poorly absorbed drugs with a negative charge due to ionization.
Most dentists are very interested in laser therapy on the intraoral soft tissue lesions because they want to accomplish the analgesic and aseptic surgery with little or no bleeding. In order to determine the difference of pain threshold according to different gingival tissues with or without inflammation, 25 patients with inflammatory periodontal disease and 10 volunteers with good general and oral health were selected as the inflamed group and the normal group, respectively. Interdental papilla, marginal gingiva, attached gingiva, and alveolar mucosa were irradiated by the contact delivery($300{\mu]m$ fiber optic, for 5 seconds) of a pulsed Nd:YAG laser(EN.EL.EN06O, Italy). And the laser power was gradually increased from 0.5W by the increment of 0.1W. The highest laser power was recorded as the first painful power when the painful gesture was recognized at first. The difference of the first painful power of laser according to different gingival tissues with or without inflammation was statistically analyzed by paired t-test in MICROSTAT program. Following results were obtained: 1. In the comparison related with the inflammation, the first painful power was significantly lower in the inflamed group than in the normal group, regardless of interdental papilla and marginal gingiva(p<0.05). 2. In the comparison related with the tissue structure, the first painful. power was significantly lower in alveolar mucosa than in attached gingiva(p<0.05). The results suggest that, for the painless therapy by a pulsed-Nd:YAG laser irradiation, the laser surgery over 2.0W of power should be necessarily accomplished under the local anethesia, and the local anesthesia should be considered according to the degree of inflammation, the tissue structure, and the purpose of laser therapy.
In this study, we prepared core-shell type nanoparticles of a poly(DL-lactide-co-glycolide) (PLGA) grafted-dextran (DexLG) copolymer with varying graft ratio of PLGA. The synthesis of the DexLG copolymer was confirmed by $^1H$ nuclear magnetic resonance (NMR) spectroscopy. The DexLG copolymer was able to form nanoparticles in water by self-aggregating process, and their particle size was around $50\;nm{\sim}300\;nm$ according to the graft ratio of PLGA. Morphological observations using a transmission electron microscope (TEM) showed that the nanoparticles of the DexLG copolymer have uniformly spherical shapes. From fluorescence probe study using pyrene as a hydrophobic probe, critical association concentration (CAC) values determined from the fluorescence excitation spectra were increased as increase of DS of PLGA. $^1H-NMR$ spectroscopy using $D_2O$ and DMSO approved that DexLG nanoparticles have core-shell structure, i.e. hydrophobic block PLGA consisted inner-core as a drug-incorporating domain and dextran consisted as a hydrated outershell. Drug release rate from DexLG nano-particles became faster in the presence of dextranase in spite of the release rate not being significantly changed at high graft ratio of PLGA. Core-shell type nanoparticles of DexLG copolymer can be used as a colonic drug carrier. In conclusion, size, morphology, and molecular structure of DexLG nanoparticles are available to consider as an oral drug targeting nanoparticles.
Kim, Young-Hwa;Lee, Yong-Suk;Park, Gee-Bae;Lee, Kwang-Pyo
Journal of Pharmaceutical Investigation
/
v.21
no.4
/
pp.215-222
/
1991
The absorption characteristics of itraconazole, which is an antifungal agent, from intestinal segments in the anesthetized rat i1l situ were investigated in order to design an effective oral drug delivery system. The pH-solubility profile of itraconazole, the rate and extent of absorption of itraconazole, the optimal absorption site(s) of itraconazole and the absorption enhancing effect of sodium cholate on itraconazole were examined in the present study. In situ single-pass perfusion method and recirculating perfusion technique using duodenum(D), jejunum(J) and ileum(I) were employed for the calculation of apparent permeability(Pe) and apparent first-order rate constant(Kobs). respectively. The results of this study were as follows; (1) Itraconazole showed appreciable aqueous solubility only at pH values of below 2.0. (2) pe(cm/sec) decreased in the following order: $D(10.24{\pm}1.78{\times}10^{-4})>J(8.86{\pm}0.79{\times}10^{-4})>I(3.78{\pm}0.13 X 10^{-4})$. (3) $Kobs(min^{-1})$ decreased in the following order: $J(17.12{\pm}3.19{\times}10^{-3})>D(13.37{\pm}0.6{\times}10^{-3})>I(11.05{\pm}0.91{\times}10^{-3})$. (4) The solubility of itraconazole markedly increased with the increase of the concentration of sodium cholate. (5) The addition of 10 mM sodium cholate significantly increased the apparent first-order rate constant of itraconazole in the ileum by a factor of 6.8.
Purpose: The aim of this retrospective study was to determine the prevalence of early implant failure using a single implant system and to identify the factors contributing to early implant failure. Methods: Patients who received implant treatment with a single implant system ($Luna^{(R)}$, Shinhung, Seoul, Korea) at Dankook University Dental Hospital from 2015 to 2017 were enrolled. The following data were collected for analysis: sex and age of the patient, seniority of the surgeon, diameter and length of the implant, position in the dental arch, access approach for sinus-floor elevation, and type of guided bone regeneration (GBR) procedure. The effect of each predictor was evaluated using the crude hazard ratio and the adjusted hazard ratio (aHR) in univariate and multivariate Cox regression analyses, respectively. Results: This study analyzed 1,031 implants in 409 patients, who comprised 169 females and 240 males with a median age of 54 years (interquartile range [IQR], 47-61 years) and were followed up for a median of 7.2 months (IQR, 5.6-9.9 months) after implant placement. Thirty-five implants were removed prior to final prosthesis delivery, and the cumulative survival rate in the early phase at the implant level was 95.6%. Multivariate regression analysis revealed that seniority of the surgeon (residents: aHR=2.86; 95% confidence interval [CI], 1.37-5.94) and the jaw in which the implant was placed (mandible: aHR=2.31; 95% CI, 1.12-4.76) exerted statistically significant effects on early implant failure after adjusting for sex, age, dimensions of the implant, and type of GBR procedure (preoperative and/or simultaneous) (P<0.05). Conclusions: Prospective studies are warranted to further elucidate the factors contributing to early implant failure. In the meantime, surgeons should receive appropriate training and carefully select the bone bed in order to minimize the risk of early implant failure.
Microspheres of felodipine, which is one of the calcium channel blocker using a mixture of Eudragi $t^{R}$ RL, L, E, and cellulose on the base of Eudragi $t^{R}$ RS were investigated. Cremopho $r^{R}$ was added to each preparation of polymers in order to increase the release of felodipine from microspheres. Felodipine-loaded microspheres were prepared by a solvent evaporation method, which is based on dispersion of methylene chloride containing felodipine and polymers in 0.5 w/v % polyvinyl alcohol solution. The average diameter based on the size distribution of the felodipine-loaded microspheres was observed to be ca. 40-55 ${\mu}{\textrm}{m}$. A good and smooth surface were showed in all types of the microspheres. The amount of felodipine loaded was over 90 w/w % in all types of microspheres. The dissolution profiles of felodipine from microspheres were similar with each type of polymer, and about a 60 w/w % of the total amount of felodipine loaded to microsphere was released within 7 hours. Dissolution rate of felodipine from the microsphere was increased by addition of Cremophor. After oral administration of the felodipine-loaded microspheres in PVA solution and felodipine alone in PEG solution to rats, respectively, the pharmacokinetic study revealed that the Tmax values of the microspheres were observed in the range of 0.67~l.0 hr while that of the felodipine solution was obtained 0.33 hr. In addition, the AUC of the microspheres at 0 to 7 hr was remarkably increased in comparison to that of felodipine solution. These results revealed that the microspheres based on Eudragit RS could be a good candidate for the controlled release drug delivery system for felodipine.e.e.e.
Jo, Deuk-Won;Kwon, Min-Jung;Kim, Jong-Hee;Kim, Young-Kyun;Yi, Yang-Jin
The Journal of Advanced Prosthodontics
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v.11
no.2
/
pp.88-94
/
2019
PURPOSE. This study was conducted to investigate patterns of adjacent tooth displacement in the posterior implant with interproximal contact loss (ICL) by 3-D digital superimposition method. MATERIALS AND METHODS. Posterior partially edentulous patients, restored with implant fixed partial prostheses before 2011 and suffered from food impaction of ICL between 2009 and 2011, were included. Two dental casts, at the time of delivery and at the time of food impaction in a same patient, was converted into 3-D digital models through scanning and superimposition was performed to assess chronologic changes of the dentition. Directions of tooth displacement were evaluated and the amount of ICL was calculated. Correlations between the amount of ICL and elapsed time, or between the amount of ICL and age after function, were assessed at a significance level of P<.05. RESULTS. A total number of 13 patients (8 males, 5 females) with a mean age of $65.76{\pm}9.94years$ and 17 areas (4 maxillae, 13 mandibles) were included in this retrospective study. Teeth adjacent to the implant restoration showed complex displacements but characteristic tendency according to the location of the arch. The mean amount of ICL was $0.33{\pm}0.14mm$. Elapsed time from function to ICL was $61.47{\pm}31.27months$. There were no significant differences between the amount of ICL and elapsed time, or age (P>.05). CONCLUSION. Natural teeth showed various directional movements to result in occlusal change in the arch. The 3-D superimposition of chronologic digital models was a helpful method to analyze the changes of dentition and individual tooth displacement adjacent to implant restoration.
Shin, Dan Bi;Lee, Jung On;Chun, Tae-Uk;Lee, Tae-Hoon
Journal of Rhinology
/
v.25
no.2
/
pp.103-107
/
2018
Pregnancy rhinitis is a relatively common condition. It is characterized by the presence of nasal symptoms, especially nasal congestion, not present prior to pregnancy, but typically present during the last 6 or more weeks of pregnancy, without other signs of respiratory tract infection or any known allergic causes, and disappearing completely within 2 weeks after delivery. Nasal saline irrigation, intranasal steroid spray, and oral antihistamines are usually recommended as the first line of treatment for rhinitis. However, most pregnant women refuse medical treatment for pregnancy rhinitis because of the fear of teratogenicity. Severe pregnancy rhinitis increases the risk of snoring, which has been suggested as having adverse effects on the fetus. In cases where the patients are unable to control their symptoms, pregnancy rhinitis can negatively affect the quality of life (QOL) as well as the pregnancy outcome. Therefore, special caution is required for determining the appropriate diagnosis and treatment modalities for pregnancy rhinitis. Here, we report for the first time, the successful treatment of pregnancy rhinitis that was unresponsive to conservative management and medical therapy by using microdebrider-assisted inferior turbinoplasty at the final stages of pregnancy, along with a review of the relevant literature.
Objective: To quantitatively analyze the effect of nicotine on orthodontic tooth movement (OTM) and bone remodeling in rats using micro-computed tomography and tartrate-resistant acid phosphatase immunostaining. Methods: Thirty-nine adult male Sprague-Dawley rats were randomized into three groups: group A, 0.5 mL normal saline (n = 9, 3 per 3, 7, and 14 days); group B, 0.83 mg/kg nicotine (n = 15, 5 per 3, 7, and 14 days); and group C, 1.67 mg/kg nicotine (n = 15, 5 per 3, 7, and 14 days). Each animal received daily intraperitoneal injections of nicotine/saline from the day of insertion of identical 30-g orthodontic force delivery systems. A 5-mm nickel-titanium closed-coil spring was applied between the left maxillary first molar (M1) and the two splinted incisors. The rate of OTM and volumetric bone changes were measured using micro-computed tomography. Osteoclasts were counted on the mesial alveolar bone surface of the distobuccal root of M1. Six dependent outcome variables, including the intermolar distance, bone volume fraction, bone mineral density, trabecular thickness, trabecular volume, and osteoclast number, were summarized using simple descriptive statistics. Nonparametric Kruskal-Wallis tests were used to evaluate differences among groups at 3, 7, and 14 days of OTM. Results: All six dependent outcome variables showed no statistically significant among group-differences at 3, 7, and 14 days. Conclusions: The findings of this study suggest that nicotine does not affect OTM and bone remodeling, although fluctuations during the different stages of OTM in the nicotine groups should be elucidated in further prospective studies.
Objectives: Post-term pregnancy is a condition associated with increased maternal and fetal complications. Administration of castor oil causes cervical stimulation by increasing the production of prostaglandins. We examined the effects of castor oil on cervical ripening and labor induction through a systematic review and meta-analysis. Methods: The search process was performed to obtain relevant articles from databases including Pubmed, Cochrane library, Scopus, Science direct, SID, Iran Medex, and Google Scholar using the English keywords of cervical ripening, post-term, castor oil, labor induction, Bishop score, and pregnancy considering all possible combinations without time constraints and their Persian equivalents from national databases. Results: A total of eight related articles from the 19 primary studies were extracted and systematically reviewed. According to a cumulative chart, the difference in the post-intervention Bishop score was statistically significant (standard mean difference [SMD]: 1.64, 95% confidence interval [CI]: 1.67-2.11, p = 0.001), indicating an effect of castor oil on increasing the Bishop score. In addition, the difference in labor induction was statistically significant after the intervention (odds ratio: 11.67, 95% CI: 3.34-40.81, p = 0.001), indicating an effect of castor oil on increasing the odds ratio of labor induction (experience of vaginal delivery). Conclusion: This meta-analysis showed that oral administration of castor oil is effective for cervical ripening and labor induction. Midwives should closely monitor pregnant women with prolonged labor and collaborate with obstetricians to employ castor oil as a safe intervention to induce cervical ripening and labor to prevent undue caesarean surgery.
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