• Bulletin of the Korean Chemical Society
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• 제35권11호
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• pp.3188-3194
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• 2014

Compound K (CK) was formulated as polymeric micelles (PM) using Pluronic$^{(R)}$ F-127 to enhance the oral absorption of CK, an intestinal bacterial metabolite of ginseng protopanaxadiol saponin. The physicochemical properties of Ck-loaded PM were characterized and an in vitro transport study using the Caco-2 cell system as well as an in vivo pharmacokinetic study using SD rats was carried out. The hydrodynamic mean particle size of CK-loaded PM (CK-PM) was $254{\pm}23.45nm$ after rehydration and the drug loading efficiency was ca. 99.9%. The FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy data supported the presence of a new solid phase in the PM. The $P_{app}$ value of in vitro Caco-2 cell permeation of CK-PM and the oral absorption of CK was enhanced about 1.2-fold and 2.6-fold compared to CK suspension, respectively, showing that the present PM formulation enabled an enhancement of oral CK absorption.

• Archives of Pharmacal Research
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• 제18권6호
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• pp.427-433
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• 1995

A microscopic mass balance approach has hsown that the initial saturation (Is), absorption number (An), dose number (Do), and dissolution number (Dn) are four fundamental dimensionless parameters that can be used to estimate the fraction dose absorbed (F)l of suspensions of poorly soluble drugs in humans. The dissolution number of a drug increases with decreasing its particle size. The effect of micronization on F for suspensions was investigated in terms of Dn. About 90% of maximal F can be achieved at $Dn{\approx}2$. Increasing the solubility of a drug results in better oral absorption through increasing Dn and decreasing the solubility of a drug results in better oral absorption through increasing Dn and decreasing Do. The fractions dose absorbed of digoxin, griseofulvin, and benoxaprofen agree with predicted F values sorbed by reducing particle size, while absorption of drugs with high Do and low Dn is limited by solubility and requires higher solubility to enhance the fraction dose absorbed in addition to micronization. Solubility at the physiological pH should be used for the estimation of the fraction dose absorbed.

• 한국임상약학회지
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• 제3권1호
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• pp.61-70
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• 1993

A new cephalosporin derivate, cefazolin phthalidyl ester(CFZ-PT) was synthesized to improve oral absorption and bioavailability of parent drug by esterification of sodium cefazolin(CFZ). Partition coefficient studies showed that CFZ-PR is more lipophilic than CFZ. The pharmacokinetic characteristics of CFZ-PT and CFZ preparations were compared following oral administrations of these compounds to rabbits. The analysis of CFZ in plasma was conducted by HPLC method. The ester compound was not detected in plasma following oral administration of CFZ-PT was increased by yielding 3.5-fold bioavailability rather than CFZ. From the results of this experiment, it was concluded that CFZ-PT could be a novel prodrug of CFZ which can improve the oral bioavailability of CFZ.

• 약학회지
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• 제24권1호
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• pp.11-14
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• 1980

In order to increase the gastro-intestinal absorption of cephalexin, a new cephalexin phthalidyl ester was synthetized. Comparative studies of cephalexin phthalidyl ester in the gastro-intestinal absorption were conducted after oral administration in rabbits. The amounts of cephalexin in plasma were determined by a fluorometric method. Cephalexin phthalexin phthalidyl ester could not be identified in plasma, but only cephalexin was found by TLC method. In comparison with cephalexin, cephalexin phthalidyl ester produced much higher plasma levels of cephalexin than did cephalexin itself after its oral administration in rabbits.

• Journal of Pharmaceutical Investigation
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• 제25권1호
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• pp.1-7
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• 1995

After oral administration of various drinking solutions, the initial absorption rate of water through gastrointestinal tract of the rabbits was evaluated using tritinated water $(^3H_2O)$ as a marker to develop the sports drinking beverage for Korean people. The polynomial curve fitting over 20 min was performed using computer program to obtain the initial absorption rate of water from the tangent line of the fitted equation because initial absorption rate of water was more critical compared to elimination rate during exercise. The amount of water absorbed was increased but a large variation was observed among testing preparations in a small study group $(2{\leq}n{\leq}6)$. The initial absorption rate of water from isotonic sports drinking beverages was statistically significant when compared to hypertonic cola but was not significant when compared to hypotonic solutions (potable water and barley water). In case of hypertonic sports dringking beverages (i.e. Takeda), initial absorption rate of water was not improved and efficient when compared to other isotonic sports dringking beverages. The initial absorption rate of water from prescribed isotonic sample solution containing electrolytes, carbohydrates, and vitamins was not statistically significant when compared to other isotonic drinking beverages but showed similar absorption profile. It was obvious that isotonic solutions simultaneously containing electrolytes, vitamins and carbohydrates (sugar and glucose) had a tendency to increase the initial absorption of water compared to hypotonic (potable water and barley water) and hypertonic preparations (orange juice and cola). Although statistical significance of initial absorption rate of water between isotonic sports drinking beverages and hypotonic potable and barley water was not observed, unlike the hypertonic solutions, isotonic sports drinking beverages may aid not only to replenish loss of water, electrolytes and other nutrients during the exercise but also to prevent dehydration and muscle fatigue, resulting in improved physical performance in an exhausted condition.

• 지역사회간호학회지
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• 제29권3호
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• pp.382-392
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• 2018

Purpose: The purpose of this study is to investigate effects of an oral self-care program on oral dryness and oral health related quality of life in the elderly. Methods: The current research design isa nonequivalent control group protest-posttest design with two groups of elders from two different senior centers in D city. Tools for the research include paper of salivary absorption (WF41-1850, Whatman, Germany), 6 items for subjective oral dryness and OHIP-14 for oral health related to quality of life. The data were analyzed to test three hypotheses by using the SPSS 22.0 program. Results: The three hypotheses were significantly accepted. The subjective oral dryness score was lower in the experimental group than in the control group (t=-2.45, p=.022). Salivary absorption was higher in the experimental group than in the control group (t=3.83, p<.001).Oral health related quality of life was better in the experimental group than in the control group (t=-2.11, p=.044). Conclusion: The oral self-care program has appeared to be effective on oral dryness and an oral health related quality of life in the elderly. Therefore, it can be suggested that the oral self-care program is applicable as an intervention program motivating the elderly to maintain oral health.

• Journal of Pharmaceutical Investigation
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• 제25권4호
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• pp.323-330
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• 1995

Ceftezole pivaloyloxymethyl ester(CFZ-PV) was synthesized to improve oral absorption and bioavailability of parent drug by esterification of ceftezole(CFZ) with chloromethyl pivalate. The successful synthesis of CFZ-PV was conformed by spectroscopic analysis. Partition coefficient studies showed that CFZ-PV is more lipophillic than CFZ. The pharmacokinetic characteristics of CFZ-PV and CFZ were compared following oral administrations of these compounds to rabbits. The amount of CFZ in plasma was determined with an HPLC method. The ester compound (prodrug) was not detected in plasma following oral administration of CFZ-PV, and although CFZ-PV had not microbiological activity in vitro, the plasma taken after oral administration of CFZ-PV had microbiological activity. From above observations, it was noted that CFZ-PV is rapidly hydrolyzed to CFZ in the body. And the oral absorption of CFZ-PV was increased by yielding 2-fold bioavailability rather than CFZ. Therefore, CFZ-PV could be a novel prodrug of CFZ which can improve the oral bioavailability of CFZ.

• Environmental Analysis Health and Toxicology
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• 제31권
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• pp.16.1-16.9
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• 2016

Objectives Banha-sasim-tang (BST), which consists of seven different herbs, is one of the most popular herbal formulae for treating gastrointestinal disorders in Eastern Asia. The commonly used herbal medicine is often co-administered with other therapeutic drugs, which raises the possibility of herb-drug interactions and may modify the clinical safety profile of therapeutic drugs. Methods We investigated the potential herb-drug interactions between BST extract and midazolam (MDZ) in mice. The area under the plasma concentration-time curve (AUC) of MDZ and 1'-hydroxymidazolam (1'-OH-MDZ) was evaluated for both oral and intraperitoneal administration of MDZ, following oral administration of BST (0.5 and 1 g/kg). Results It was found that the AUC of MDZ and 1'-OH-MDZ was lower in case of oral administration of MDZ. Administration of BST extract was not associated with hepatic cytochrome P450 activity. BST extract induced a strong reduction in pH and it has been reported that oral mucosal absorption of MDZ is lower at low pH. The decreased absorption rate of MDZ might be caused by the ingredients of BST and may not be related to other factors such as increased excretion of MDZ by P-glycoprotein. Conclusions The altered pharmacokinetics of midazolam caused by co-administration with BST in vivo could be attributed to a decrease in pH and subsequent reduction of MDZ absorption rate.

• Journal of Pharmaceutical Investigation
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• 제12권2호
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• pp.45-53
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• 1982

The effects of mixture of tween 20 and span 20 or span 80 on griseofulvin absorption in rabbit were studied. The plasma concentration of griseofulvin in blood samples was determined by high pressure liquid chromatographic procedure. Griseofulvin suspension with 0.05% surfactant increased mostly drug absorption and produced about two times higher plasma level of griseofulvin than that of the suspension with 1% and 0.1% surfactant. Surfactants with H.L.B. value 4.3 resulted $2.74{\mu}g/ml$ of maximum plasma levels of griseofulvin at 18 hours after its oral administration and surfactants with H.L.B. value 16.7 resulted $0.56{\mu}g/ml$ of peak plasma levels of griseofulvin at 1 hour after its oral administration.

• Archives of Pharmacal Research
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• 제20권5호
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• pp.480-485
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• 1997

The absorption profile of phenytoin Na emulsion were examined compared to that of phenytoin suspension after oral administration in the rat. The corn oil-in-water emulsion, particle size of $184{\pm}$57.8 nm, was prepared using a microfludizer, and phenytoin Na added by shaft homogenizer. The phenytoin emulsion or suspension, 100 mg/kg, were intubated intragastrically using oral dosing needle and blood samples were withdrawn via an indwelling cannula from the conscious rat. Plasma concentrations of phenytoin were measured with HPLC using phenacetin as an internal standard. The plasma concentration versus time data were fitted to a one compartment open model and the pharmacokinetic parameters were calculated using the computer program, Boomer. The phenytoin plasma concentrations from the emulsion at each observed time were about 1.5-2 times higher than those from the suspension, significantly at time of 5, 6 and 7 hr after administration. The absorption $(k_a)$ and elimination rate constant $(k_e)$ were not altered significantly, however the AUC increased from 65.6 to $106.7{\mu}ghr/ml$ after phenytoin suspension or emulsion oral administration, respectively. From an equilibrium dialysis study, the diffusion rate constant $(k_{IE})$ was considerably higher from the phenytoin Na emulsion $(0.0439 hr{-1})$ than phenytoin suspension $(0.0014 hr{-1})$.