• 한국식품위생안전성학회지
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• 제37권2호
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• pp.114-120
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• 2022

본 연구에서는 체내에서 비타민 C의 지속성을 나타내기 위해 성분의 용출을 조절하는 기술이 적용된 용출조절형 비타민 C 제품과 일반적인 속방형 비타민 C 제품의 비교용출 실험을 진행하여, 일반적인 속방형 제품과 용출조절형 제품 간의 용출 양태를 비교분석 하였다. 비타민 C 정제들의 용출률을 확인하기 위해 '대한약전(제2020-88호)', '경구용의약품의 용출규격 설정 가이드라인'의 용출시험법, '건강기능식품의 기준 및 규격 고시(제2020-63호)'에 근거한 HPLC 함량시험을 수행하여 시간별 용출률을 분석하였다. 분석 결과 속방형 비타민 C 제품은 45분 이후 100% 용출이 이루어진 반면 용출조절형 비타민 C 제품은 480분(8시간) 이후에 100% 용출이 나타났으며, 용출조절형 비타민 C 제품의 60분에서의 용출률이 속방형 비타민 C 제품에 비해 더 느리게 나타나는 것을 확인하였다. 이러한 결과를 바탕으로 비타민 C를 주성분으로 한 용출조절형 정제의 개발 및 용출분석이 가능함을 확인하였다.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.555-559
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• 1997

The three different batches of an oral sustained release melatonin (MT) delivery system were prepared by aqueous-based fluid-bed coating of the sugar spheres for the evaluation of in vitro release characteristics and plasma concentration profiles in human subjects. The MT contents in 20% coated sugar spheres of three batches (B1, B2 and B3) were $3.3{\pm}0.08$, $2.4{\pm}0.1$ and $2.5{\pm}0.13$ mg per gram of coated sugar spheres, respectively. The release profiles of three different batches had a very similar fashion. However, the release profiles of three different batches had a very similar fashion. However, the release half-lives $(T_{50%})$ of MT from B1, B2 and B3 was $3.70{\pm}0.2$, $5.2{\pm}0.2$ and $4.9{\pm}0.07h$, respectively. Plasma concentration profiles of sustained release 0.2mg melatonin-loaded sugar spheres containing 10% immediate release melatonin in gelatin capsules (B1 and B2) were then evaluated in human subjects. The in vivo plasma concentration profies of the two batches (B1 and B2) were very similar each other and located between the physiological endogenous ranges. The time to reach the peak concentration $(T_max)$ was more advanced in case of B1 when compared to B2. However, there was no statistically significant difference in the maximum concentration $(C_max)$ and the area under the curve (AUC) between B1 and B2. The AUC of melatonin-loaded sugar spheres containing 10% and 20% immediate release MT in human subjects had a good linearity between dose and AUC, regardless of the fraction of immediate release MT, indicating the first order elimination process of MT within these doses. The current oral sustained release MT delivery system may be utilized to treat circadian rhythm disorders if it is proven to be more clinically useful when compared to immediate release MT.

• Journal of Pharmaceutical Investigation
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• 제23권3호spc1호
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• pp.9-18
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• 1993

Sugar spheres loaded with melatonin (MT) were coated with $Aquacoat^{\circledR}$ to control the release rate of MT over 8 hours. A zero-order release pattern over 8 hours was obtained with 20% coating on 8-10 mesh beads in USP basket dissolution studies. MT in 20% coated beads was quite stable at room temperature with less than 5% MT degraded during 6 months' storage. Dissolution profiles were also unchanged after 6 months. An oral preparation containing MT-loaded uncoated beads for immediate release and 20% coated beads with $Aquacoat^{\circledR}$ for controlled release over 8 hours was evaluated in six human subjects. When total 0.5 mg MT as low dose (immediate release portion of MT, 0.1 mg) was administered to four subjects, average peak plasma MT concentration was reached at about 600 pg/ml and maintained at about 10 pg/ml over 8 hours. Plasma MT concentration-time profiles were similar in shape to computer-simulated profiles. However, maximal plasma MT concentrations were three times greater compared to computer simulated curve. These results suggest that MT dose, ratio of immediate and controlled release MT, and pharmacokinetic parameters selected are adjusted to mimic endogenous MT concentration-time curve. In another study, 0.2 mg MT having 10% of immediate release portion and 80% controlled release portion produced plasma MT concentration-time curve which is more similar to endogenous profiles. A low bioavailability (<20%) may result from extensive first pass metabolism and remaining amounts of MT from controlled beads. A good correlation between plasma MT concentration and urinary excretion rate of 6-sulphatoxymelatonin (6-STMT), a major metabolite of MT was observed. As plasma MT concentration increased, urinary excretion rate of 6-STMT increased concomitantly. The linear relation between plasma MT and urinary excretion rate of 6-STMT was statistically significant. This result suggests that urinary 6-STMT may be used as an index of circadian rhythms of MT in humans.

• 약학회지
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• 제41권3호
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• pp.305-311
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• 1997

Sustained release-microspheres and immediate release-pellets were prepared to develop a controlled release multiparticulate system containing both water soluble and insoluble dr ug. Pseudoephedrin.HCl (EPD) and terfenadine (TRF) were used as model drugs, respectively. Sustained release-EPD microspheres were prepared by solvent evaporation method using Eudragit RL or RS as a matrix combined with pH-insensitive film coating. Smaller EPD microspheres were obtained when smaller amount of Eudragit as a matrix material or larger amount of magnesium stearate as a dispersing agent was used. However the obtained microspheres did not show syfficient sustained release characteristics. About 97% of EPD was released after 1 hr irrespective of matrix material used. Subsequent coating of the microspheres with pH-insensitive polymer such as Eudragit RS or ethylcelulose (EC) resulted good sustained in 37.5, 73.3 and 92.0% release of encapsulated EPD in distilled water after 1, 3 abd 7 hr, respectively. It corresponds to mean dissolution time (MDT) of 2.3 hr, which is much larger than that of un-coated EPD microspheres (0.0048 hr). Immediate release TRF pellets were prepared by spherically agglomerated crystallization using Eudragit E as an inert matrix and methylene chloride as a liquid binder. Using Eudragit E alone as a matrix resulted in satisfactory physical properties of the pellets such as sphericity, surface texture and flowability, but led to slower release of TRF from pellets than un-modified TRF powder (MDT of 1.70 vs 1.43 hr in pH 1.2 dissolution medium). Introducing propylene glycol or sodium lauryl sulfate as an emulsifier brought about faster release of TRF from pellets (MDT of 1.14 and 0.95 hr, respectively). In conclusion, microencapsulation by solvent evaporation combined with film coating and spherically agglomerated crystallization were successfully utilized to prepare controlled release multiparticulate system composed of sustained release EPD-microspheres and immediate release TRF pellets.

• Journal of Pharmaceutical Investigation
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• 제34권1호
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• pp.57-71
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• 2004

The objective of this study was to provide a better understanding of SUPAC-IR and its application in handling postapproval changes to immediate release solid oral dosage forms. Originally, SUPAC-IR was aimed at reducing the regulator burdern of the industry when they were making postapproval changes, but still at maintaining the formulation quality and performance of a drug product. The postapproval changes that were covered under SUPAC-IR included variations in the components ad composition of formulation, the site of manufacturing, batch size, manufacturing equipment, and manufacturing process. The guidance defined levels of changes, based on the likelihood of risk ocurrence and potential impact of postapproval changes upon the safety and efficacy of a drug product I suggested what a type of fing report should be submitted to the FDA for each level of change. Chemist, manufacturing, and control tests to be executed were also recommended for each change level The important tests specified in the guidance included batch release, stability, in vitro dissolution, and in vivo bioequivalence tests. However, there have been strong demands on revising the current SUPAC-IR in order to resolve some issues and to improve its usefulness in evaluating postapproval changes to immediate release solid oral dosage forms. In particular, the rigorous requirement of case C dissolution test and the definition of batch size were challenged by both academia and the industry. A revision work was in progress to reflect these inputs and to expand the utility of SUPAC-IR. As a result of these concerted efforts, an updated 2nd version of SPAC-IR would be likely to be issued ver soon to the public.

• 국제물리치료학회지
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• 제10권1호
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• pp.1739-1745
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• 2019

Background: There have been many studies on self-myofascial release (SMR) stretching, but there are few comparative studies on the effects of massages using a release ball, which is a type of the SMR method. Objective: To investigate the immediate effects of release ball massage and self-stretching on proprioceptive sensory, hamstring's temperature, range of motion (ROM) muscle strength,. Design: Crossover study. Methods: Thirty women in 20's at S University in Busan voluntarily participated in the study. Participants were random to release ball group (n=15) or self-stretching group (n=15). Both groups performed 3 sets of exercises, stretching for 30 seconds and resting for 15 seconds in each position. The proprioceptive sensory, temperature of the hamstring muscle, ROM, and strength were measured before exercise, 5 minutes after exercise, and 30 minutes after exercise. Results: Release ball group showed significant differences in muscle length and temperature over time (p<.05). The comparison between two group over time showed significant differences in muscle length, temperature, and muscle strength (p<.05). Conclusions: These results demonstrate that release ball massage and self-stretching are beneficial for improving hamstring's temperature, ROM and muscle strength.

• Bulletin of the Korean Chemical Society
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• 제35권2호
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• pp.557-561
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• 2014

The aim of the present study was to improve dosing of lacosamide, a functionalized amino acid used as an antiepileptic agent, from twice daily to once daily for the convenience of patients. A sustained-release lacosamide tablet was developed and dissolution testing was employed to determine in vitro release behavior using water or buffer solutions at pH 1.2, 4.0, or 6.8. Lacosamide was released for 12 h from the sustainedrelease (SR) tablet, as compared to complete release within 1 h from an immediate-release $Vimpat^{(R)}$ tablet. Each formulation (100 mg) was orally administered to six beagle dogs and six mini-pigs under fasted conditions, and pharmacokinetic parameters such as the area under the concentration time curve ($AUC_t$), the maximum plasma concentration ($C_{max}$), and the time at which this occurred ($T_{max}$) were calculated. These results showed similar values for $AUC_t$, $C_{max}$, and $T_{max}$ following oral administration of immediate-release ($Vimpat^{(R)}$) and SR lacosamide tablets.

• 약학회지
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• 제40권6호
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• pp.679-683
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• 1996

The current study evaluates the capacity of eugenol to regulate immediate allergic reaction by control of histamine release. Administrations of eugenol (1M/kg, i.p.) at 60 min b efore and 5, 10 min after the compound 48/80 treatment (8mg/kg, i.p.) were shown the mortality rates as 0, 44.4, and 77.8%, respectively. A 60 min before administered group revealed a significant inhibition of serum histamine release compared with those of 5 and 10 min after the compound 48/80 injection. Eugenol (6-48mM) was also showed a dose-dependent activity on the compound 48/80-induced histamine release from the highly purified population of Alcian Blue-positive peritonea] mast cells. These results indicate that in vitro treatment with exogenous eugenol inhibited the active response of mast cell populations and modulated its characteristics.

• The Journal of Korean Physical Therapy
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• 제28권3호
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• pp.201-204
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• 2016

Purpose: The purpose of this study was to compare the immediate effects of alternative treatment methods in lowering the blood pressure and pulse of prehypertensive patients. Methods: A total of 48 prehypertensive patients were randomly divided into 4 groups of 12 patients and each group received a different intervention. The control group was made to rest, the heat pack (HP) group received heat pack treatment, the ultrasound (US) group received an ultrasound massage, and the myofascial release (MFR) group received myofascial release. The blood pressure and pulse rate were measured before and after intervention. Results: Following intervention, the patients of the MFR group showed a decrease in systolic pressure, diastolic pressure, and pulse rate. Although blood pressure was similar in all groups, a significant decrease in pulse rate was seen in the MFR group compared to others. Conclusion: The application of MFR was shown to be an effective method for lowering the blood pressure and pulse rate in prehypertensive patients.

• Physical Therapy Rehabilitation Science
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• 제13권1호
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• pp.124-133
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• 2024

Objective: This study aims to investigate the immediate effects of myofascial release and Duoball assisted self-relaxation (DASR) techniques on pain and muscle tension in patients experiencing chronic cervical pain. Design: A randomized controlled trial. Methods: This study is a randomized controlled experimental study. Eighteen patients with chronic neck pain who met the selection criteria were randomly assigned to myofascial release group and myofascial release group using Duoball. Results: The frequency results for assessment muscle tension showed a decrease of about 10% in the suboccipital muscle, SCM, Pect m, UT, and LS in both the MFR and DASR groups, and the stiffness results showed a decrease in all muscles except the upper trapezius in the MFR group and the DASR group. All were found to decrease by about 10% in the suboccipital muscle, SCM, Pect m, UT, and LS, and the decrement results showed an increase of about 15% in the suboccipital muscle, SCM, Pect m, UT, and LS in both the MFR and DASR groups(p<0.05). Conclusions: In patients experiencing chronic neck pain, application of MFR and duoball assisted self relaxion was shown to be effective on pain and muscle tension. MFR is a non-pharmacological intervention method with few potential side effects and is considered a universal and easily applicable treatment method.