• Archives of Pharmacal Research
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• v.28 no.8
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• pp.977-982
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• 2005

The aim of this study was to compare two formulations of film-coated pellets containing c1arithromycin after single oral dose study in healthy male volunteers. Two formulations with different coating polymers were prepared: formulation-1 (F-1) was prepared by incorporating three kinds of pH-dependent gradient-release coated pellets into capsules and formulation-2 (F-2) was prepared by coated with an insoluble semiosmotic film. Release profiles of filmcoated pellets were evaluated using paddle method under different conditions. Pharmacokinetic profiles of these formulations were obtained in three healthy male volunteers and compared to commercially available immediate release (IR) tablets. The relative bioavailability based on the $AUC_{0-24h}$ was found to be $96.2\%\;and\;58.7\%$ for F-1 and F-2 compared with IR, and the $T_{max}$ was delayed.

• Journal of the Korean Academy of Child and Adolescent Psychiatry
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• v.32 no.1
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• pp.10-16
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• 2021

Objectives: The aim of this study was to compare the compliance, efficacy, and satisfaction associated with methylphenidate and atomoxetine for treating attention-deficit/hyperactivity disorder (ADHD). Methods: The subjects were 44 patients who met the Diagnostic and Statistical Manual of Mental Disorder-5 diagnostic criteria for ADHD and were treated with methylphenidate or atomoxetine. The methylphenidate formulations included immediate release (IR), extended release (ER), and osmotic-controlled release oral delivery system (OROS). Patients and parents reported the average number of days per week the medication was taken. Efficacy was assessed using the ADHD Rating Scale. Satisfaction with medication scale (SAMS)-parent report form and SAMS-self-report form were used to evaluate parents' and patients' satisfaction, respectively. Results: Patients and parents were more satisfied with methylphenidate than with atomoxetine. There were no significant differences in the compliance with and efficacy of methylphenidate and atomoxetine. Compliance with methylphenidate IR and ER was markedly lower than that with OROS methylphenidate or atomoxetine. Conclusion: Methylphenidate OROS formulation can be considered a suitable option given its high rates of compliance, satisfaction, and efficacy.

• The Journal of Internal Korean Medicine
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• v.21 no.1
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• pp.156-161
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• 2000

The unripe fruit of Poncirus trifoliata Raf has been used for the treatment of allergic disease. Recently it was reported that the fruit inhibits passive cutaneous anaphylaxis and histamine release at mast cell. Type I immediate hypersensitivity of anaphylactic type is caused by released mediate chemical at mast cell. Histamine is also known as one of potent mediate chemical. Also release of mediate chemical is affected by specific stimulation of IgE combined with mast cell. Activation of mast cell is known to be stimulated by compound 48/80 and inhibited by increase of cAMP. In this experiment, the effect of water extract of Poncirus trifoliata Raf fruit (PT) on a histamine release, cAMP concentration and IgE production was measured. Compound 48/80 was administrated to the mouse peritoneal cell which was pretreated with PT. PT dosedependently inhibited histamine release at peritoneal mast cell and the serum level of histamine induced by compound 48/80. PT also instantly increased cAMP level of peritoneal mast cell right after it was added and the level gradually decreased. Production of IgE induced by antigens at mouse peritoneal cell was inhibited by PT. The IgE synthesis is induced by IL-4 and it is known that lipopolysaccharide(LPS) plus IL-4 cause an increase in IgE secretion by murine B cells. The effects of PT inhibited the production of IgE activated by LPS plus IL-4 at human U266B1 cells. These results indicate that PT has antiallergic activity by Inhibition of IgE production from B cells and histamine release by increase of cAMP.

• Biomolecules & Therapeutics
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• v.19 no.2
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• pp.248-254
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• 2011

Biotransformation of pharmacologically inactive lactone prodrug simvastatin (SV) into pharmacologically active simvastatin ${\beta}$-hydroxy acid (SVA) exhibits inter-species differences due to variations in amount and activity of esterase enzymes. In this study, we investigated the pharmacokinetics (PK) of SV and its metabolite SVA following oral doses of SV from controlled-release (CR) tablets and immediate-release (IR) tablets in rodent and canine animal models that features different esterase activity. In rat PK study, no SV was detected in plasma for both formulations due to rapid hydrolysis of SV into SVA by plasma esterase. Besides, no significant differences in PK parameters of SV or SVA were observed between both species. In dog PK study, the relative oral bioavailability of CR tablets in terms of SV was 72.3% compared to IR tablets. Regarding formulation differences in dogs, CR tablets exhibited significantly lower $C_{max}$ (p<0.05), and higher $T_{max}$ (p<0.01) and MRT (p<0.01) for both SV and SVA compared to IR tablets. Accordingly, CR tablets of SV with prolonged drug release profiles in both species might be a potential candidate for a more effective delivery of SV with reduced side effects. Besides, similar PK parameters of SV and SVA in both species despite variation in enzyme activities suggested involvement of equally potent biotransformation pathways in these animal species.

• Archives of Pharmacal Research
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• v.29 no.6
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• pp.514-519
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• 2006

A simple HPLC method using UV detection was developed and validated for the determination of levodropropizine (LDP) In dog plasma. The sample was prepared for injection using a liquid-liquid extraction method with 1-phenypiperazine as the internal standard. The mobile phase was methanol - diethylamine solution (0.05 M) (20:80, v/v, pH adjusted to 3.0 with $H_3PO_4$) with a detection wavelength of 240 nm. The limit of quantitation (LOQ) of LDP in a biological matrix was determined to be 25.25 ng/mL. The calibration curve was linear across the concentration range of 25.25 to 2020 ng/mL. The intra-day and inter-day precision values (CV%) were within 7% and accuracy (R.E. %) was within 6% of the nominal values for medium (252.5 ng/mL) and high (2020 ng/mL) LDP concentrations. For the LDP concentration at the LOQ, the intra-day and inter-day precision and accuracy were within 20% and 10%, respectively. The average absolute recovery for LDP was 70.28%. This method was successfully used to analyze plasma samples in a steady-state bioavailability study of a newly developed sustained-release LDP tablets (SR) using immediate-release tablets (IR) as the reference. The relative bioavailability of the SR was determined to be $106.3\;{\pm}\;12.8%$ (n=6). The $C_{max}$ of the SR was significantly lower (p<0.05), and the $t_{max}$ was significantly longer than that of the IR (p<0.05). The results of ANOVA and two one-sided tests indicated that the SR exhibited acceptable sustained release properties and was bioequivalent to the IR.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.18 no.1
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• pp.506-512
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• 2017

The purpose of this study was to improve release rate and bioavailability of nateglinide formulation. Polymorphism selection and particle size control were performed to enhance formulation dissolution rate, and a pH modifier was included in the formulation to overcome pH-dependent solubility of nateglinide. The enhanced dissolution rate was characterized by using a dissolution test. The results showed that H-type raw material had a higher dissolution rate than that of B-type raw material. There was 6.2% difference in dissolution between the two materials at 60 min. With regard to particle size, raw material with a $1.13{\mu}m$ particle size showed a 20% faster release rate than that of raw material with a $2.28{\mu}m$ particle size. Furthermore, fumaric acid was included in formulation as a pH modifier. That addition produced a greater than 50% improvement in dissolution rate. In conclusion, dissolution rate of nateglinide can be enhanced by optimizing its polymorphism and particle size; moreover, a synergistic effect on the enhancement of dissolution rate is obtained by including fumaric acid, a pH modifier, in the formulation.

• The Journal of the Korean dental association
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• v.54 no.5
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• pp.348-355
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• 2016

Ideal autogenous or allogenic bone graft materials should provide 1) stabilization of blood clot, 2) scaffolds for cellular proliferation and differentiation, 3) release of osteogenic growth factors, 4) appropriate resorption profile for remodeling of new bone. Teeth, especially dentin, mostly contain hydroxyapatite and type I collagen which are similar to bone, and could be valuable graft material. Clinically teeth are used as calcined or demineralized forms. Demineralized form of dentin can be more effective as a graft material. But a conventional decalcification method takes time and long treatment time may give negative effects to various osteogenic proteins in dentin. Author used a new clinical method to prepare autogenous teeth, which could be grafted into the removal defects immediately after extraction using vacuum ultrasonic system. The process could be finished within two hours regardless of the form (powder, chip or block). Teeth were processed to graft materials in block, chip, or powder types immediately after extraction. It took 120 minutes to prepare block types and 40 minutes to prepare powder. Clinical cases did not show any adverse response and the healing was favorable. Rapid preparation of autogenous teeth with the vacuum ultrasonic system could make the immediate one-day extraction and graft possible.

• International Commerce and Information Review
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• v.8 no.4
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• pp.71-88
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• 2006

This article want to discuss on comparative research between CHIPS and Fedwire as the cross-border payment systems which America have and use at present. CHIPS is a New York-based automated private-sector clearing facility for large-dollar transfers. It is a central switch communication and settlement system whose 53 participating banks exchange same-day payment messages over dedicated communication lines linking each one to the CHIPS central computer. On January 22, 2001, CHIPS introduced immediate finality for payment released from the CHIPS queue. Unlike the Fedwire system, The CHIPS system is not a real-time gross settlement system. Instead, CHIPS is hybrid system that uses a computer program to select payment order in a queue for release to the receiving bank. CHIPS are governed by CHIPS Rules and Administrative Procedures. Fedwire system is a nationwide electronic fund-transfer system facilitating same-day transfers throughout the United States. It is a gross settlement system providing immediate credit to the receiving bank's master account. Communicating between a Federal Reserve Bank and Fedwire users can be either on-line or off-line. Fedwire transfers are governed by Subpart B of Regulation J, issued by the Federal Reserve Board, which incorporates U.C.C. Article 4A but preempts or supersedes any of its inconsistent provisions.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.12 no.1
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• pp.1-17
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• 1999

Shinisan has been used for treatment of allergic disease in Oriental Medicine. However, its effect in experimental models remains unknown. The mast cell plays a pivotal role in initiating allergic response by secreting intracytoplasmic granular mediators such as histamine. The present report describes an inhibitory effect of Shinisan on mast cell-mediated immediate type allergic reactions. Topical application of compound 48/80 can induce an ear swelling response in normal ($WBB6F_1-+/+$) mice but not in the congenic mast cell-deficient $WBB6F_1-W/W^v$ mice. Shinisan inhibited concentration-dependently mast cell-dependent ear swelling response induced by compound 48/80. Shinisan inhibited concentration-dependently passive cutaneous anaphylaxis induced by anti-dinitrophenyl (DNP) IgE in rats by topical application. Shinisan also inhibited concentration-dependently the histamine release from the rat peritoneal mast cells by compound 48/80 or anti-DNP IgE. Moreover, Shinisan had a significant inhibitory effect on compound 48/80-induced systemic anaphylactic reaction. These results indicate that Shinisan inhibits immediate-type allergic reactions by inhibition of mast cell degranulation in vivo and in vitro.

• Natural Product Sciences
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• v.8 no.4
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• pp.177-182
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• 2002

The effect of aqueous extract of Sanguisorba officinalis L. (Rosaceae) root (SOAE) on the immediate-type allergic reactions by anal therapy was investigated. SOAE (0.01 to 1 g/kg) dose-dependently inhibited systemic anaphylaxis induced by compound 48/80 in mice. When SOAE was pretreated at the same concentrations with systemic anaphylaxis, the plasma histamine levels were reduced in a dose-dependent manner. SOAE (0.1 and 1 g/kg) also significantly inhibited local anaphylaxis activated by anti-DNP IgE. SOAE (0.001 to 1 mg/ml) dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE. The level of cyclic AMP (cAMP) in RPMC, when SOAE (1 mg/ml) was added, transiently and significantly increased compared with that of basal cells. These results provide evidence that anal therapy of SOAE may be beneficial in the treatment of allergic diseases.