• Journal of the Korea Academia-Industrial cooperation Society
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• v.16 no.11
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• pp.7549-7554
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• 2015

The aim of this study was to develop gastric retentive bi-layered tablet using floating drug delivery technique. Metformin was selected as a model drug due to its narrow absorption window as well as very highly water solubility. These properties of metformin led to be difficult controlling the drug release. The bi-layered tablet was prepared with bi-layered compression machine to minimize interference between floating part and controlling part. The tablet weight, appearance and hardness were evaluated after compression process. The times of 'time to floating' and 'Floating duration' were tested for floating ability and drug release study was also carried out to understand drug release behavior. Furthermore, the drug release of bi-layered tablet was compared with marketed metformin tablet with sustained release pattern (Glucopharge XR$^{(R)}$).The floating ability and drug release behaviors were well controlled by changing amounts of $NaHCO_3$ (floating substance) and hydroxypropyl methylcellulose (HPMC; release control material). Bi-layered tablet had 13s of time to float, over 10h of floating duration and very similar drug release behavior compared with Glucopharge XR$^{(R)}$($f_2$: 89.6). Consequently, the bi-layered tablet with floating ability was successfully prepared and these properties can maximize the efficacy of metformin.

• Journal of Pharmaceutical Investigation
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• v.35 no.3
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• pp.151-155
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• 2005

A drug delivery system(DDS) for practically insoluble meloxicam was developed and evaluated by dissolution study. A novel DDS is two layered system, where the first layer is consisted of gas-forming agent for an immediate release and the second layer is composed of metolose SR(HPMC) for sustained release. This bilayered tablets were manufactured by using manual single punch machine. The results of dissolution study showed an initial burst release followed by sustained release for the experimental period time. From a pharmaceutical point of view, the designed DDS for meloxicam would be informative system in terms of poorly soluble analgesic medicines.

• Polymer(Korea)
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• v.36 no.3
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• pp.332-337
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• 2012

The primary objective of this work is to find the properties of sustained release dissolution pattern depending on solubility of drugs, so venlafaxine HCl and carbamazepine tablets were made by using polymer wich various particle size. Hydroxy propyl methyl cellulose (HPMC) has been utilized in this study as an excipient that is one of the most widely used polymers for an oral sustained release formulation, and drug release pattern was strongly influenced by swelling rate depending on particle size of HPMC. Scanning electron microscope (SEM) was employed to investigate the surface of tablets with various HPMC particle size, and differential scanning calorimeter (DSC) was employed to investigate the crystallization of drugs in tablets. The release model equation was applied to analyze the main mechanism of drug release pattern. The results demonstrate that drug release pattern is controlled by the drug solubility and HPMC particle size.

• Review of Korea Contents Association
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• v.10 no.2
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• pp.17-24
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• 2012

• Journal of the Korea Academia-Industrial cooperation Society
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• v.11 no.7
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• pp.2451-2458
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• 2010

We prepared sustained release matrix system which contains carvedilol with Compritol 888 ATO used as lipophilic sustained release excipient and hydroxypropyl methyl cellulose (HPMC) or polyethylene oxide (PEO) used as hydrophilic sustained release polymer. Wet granulation compressed method was used for preparing carvedilol sustained release matrix tablets. When carvedilol sustained release matrix tablets were prepared, we evaluated the drug release kinetics which is affected by Compritol 888 ATO ratio, a kind of hydrophilic polymer (HPMC, PEO) and hot melt coating coagglutination (HMCC) process was done. The drug release kinetics was measured for 24 hours in pH 1.2 simulated gastric fluid and pH 6.8 simulated intestinal fluid, using a dissolution tester at $37.5^{\circ}C$ in 50 rpm. Dissolution rate of controlled release matrix tablets of carvedilol was evaluated by paddle method. We confirmed that HMCC process was very effective to controlled release of drugs. The rate of Compritol 888 ATO, as a lipidic material, can control the drug release pattern about the elution rate of 95% and 24 hours delay than that of the normal tablet.

• Journal of Pharmaceutical Investigation
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• v.37 no.2
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• pp.119-126
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• 2007

Tablet splitting is used in pharmacy practice to adjust the dose to be administered. However, it also causes several problems such as undesirable effect for sustained release or enteric-coated dosage form, inaccuracy of dose, and pharmacist's safety by splitting hazardous drugs. This study investigated the current status of oral dosage form splitting for patients older than 19 years by analyzing Korea National Health Insurance Claims Database. Out of oral solid drugs prescribed (N=1,486,584) 9.8% of them included tablets (or capsules) split. There were some splitting cases even in sustained release (4.9%), enteric-coated forms (1.3%) and hazardous drugs (2.7%) that were selected by NIOSH (The National Institute for Occupational Safety and Health). The most frequently split drugs were antihistamines, neuropsychotics and steroids. In case of digoxin and warfarin, unit doses in a domestic market were not diverse compared to foreign markets. Guidelines for splitting oral solid dosage forms, approval of diverse doses and conducting dose-response studies for the commonly splitting ingredients on Korean people are needed for the saff and effective use of oral solid drugs.

• YAKHAK HOEJI
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• v.36 no.3
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• pp.212-219
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• 1992

Although oral route is the most convenient route for drug administration, the short and variable transit of drug through GI tract restricts the sustained drug absorption after oral administration. Thus, for sustained absorption of drugs, it is desirable to prolong the GI transit time by retaining the dosage forms in the stomach. In this study, the enzyme-digestible swelling hydrogel was synthesized by heating the mixed solution of N-vinyl-2-pyrrolidone[monomer], acrylated albumin[crosslinking agent] and proxyphylline[drug] at $65^{\circ}C$ for 10 hours in the cylindrical test tube. The resultant hydrogel tablet (diameter; 0.77 cm, thickness; 0.47 cm) was designed to swell in the gastric fluid after oral administration to such a size that passing through the pylorus could be inhibited during the drug release. After releasing drug, the hydrogel was expected to be degraded by pepsin, an enzyme in the stomach, and eventually solubilized. Actually, the hydrogel synthesized in the study swelled to a size larger than the diameter of the pylorus ($1.3{\pm}0.7$ cm) and slowly digested in the presence of pepsin. Drug release from the hydrogel was prolonged up to about 12 hours. The swelling kinetics was dependent on albumin acrylation time, drug content and gel thickness. Particularly the gel thickness was the most important factor that influences on drug release. By adjusting these factors, the albumin-crosslinked hydrogel was expected to be retained in the stomach for up to 60 hours and used as a potential platform of drugs for long-term GI absorption.

• Journal of Pharmaceutical Investigation
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• v.36 no.4
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• pp.271-276
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• 2006

Felodipine, a calcium-antagonist of dihydropyridine type, is a poorly water soluble drug and has very low bioavailability. As preceding studies, use of solid dispersion systems and surfactants(solubilizers) has been suggested to increase dissolution and to improve bioavailability of felodipine. But in case of solid dispersion systems, large amount of toxic organic solvents should be used and manufacturing process time become longer than conventional process. In case of using surfactants, as time elapsed, decreasing of dissolution rate of felodipine due to crystallization has been reported. In this study, Copovidon as a hydrophilic polymer and $Transcutol^{\circledR}$ as a surfactant were combined to formulations if order to increase dissolution of felodipine and conventional wet granulation process were applied to manufacturing of formulations. The effect of Copovidon and $Transcutol^{\circledR}$ on the dissolution oi felodipine was investigated in-vitro. When Copovidon and $Transcutol^{\circledR}$ used simultaneously, the dissolution rate of felodipine was prominently increased compared with when used separately and the maximum increase in the dissolution of felodipine was 5.8 fold compared to control. This is most probably due to synergy effect by combination of Copovidon and $Transcutol^{\circledR}$. Felodipine sustained release tablets were successfully formulated using several grades of HPMC as a release retarding agent. The stability of felodipine sustained release tablet was evaluated after storage at accelerated condition($40^{\circ}C/75%\;RH$) for 6months in HDPE(High density polyethylene) bottle. Neither significant degradation nor change of dissolution rate for felodipine was observed after 6months. In conclusion, felodipine sustained release tablet was successfully formulated and dissolution of felodipine, poorly water soluble drug, was prominently increased and also stability was guaranteed by using combination system of hydrophilic polymer and surfactant.

• Korean Journal of Food Science and Technology
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• v.44 no.3
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• pp.274-279
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• 2012

The objective of this study was to develop oral matrix tablets for the sustained release of vitamin C. In this study hydroxypropyl methylcellulose (HPMC) has been utilized as an excipient, as it is one of the most widely used polymers, for use during long periods of time in formations. The vitamin C tablet formulation depends on the molecular weight and concentration of sustained-delivery in HPMC. Anti-oxidants have been added as a dissolution medium in order to prevent vitamin C degradation in water. The dissolution test was carried out in a distilled water medium, and the release model equation was applied to analyze the vitamin C release pattern. The results demonstrated that the release and lasting power of vitamin C tablets, containing HPMC, lasted for more than 12 h.

• Journal of Pharmaceutical Investigation
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• v.30 no.3
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• pp.179-189
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• 2000

Clebopride malate(Cm) is a new benzamide drug which has a potent central antidopaminergic activity possessing antiemetic and anxiolytic properties. A purpose of this study was to assess the feasibility of formulating sustained release preparation by dispersing a drug in hydrophilic polymeric matrices and double layered tablets(DLT), using HPMC, carbopol, PEO, PVP/VA and other polymers as a rate controlling barrier. The matrix and DLT showed optimum dissolution pattern up to 8 hours and the contents of polymer were optimized at 30% level in this preparation. After an oral administration in beagle dog, Cm concentration was determined by use of GC-ECD and pharmacokinetic parameters were calculated by Vallner's method. The AUC of DLT showed similar results and the duration of action was increased 55% compared to that of regular release dosage form. The calculated absorption rate effectiveness(ARE) and controlled release effectiveness(CRE) for DLT increased 50% compared to that of matrix, the overall effectiveness(E) of this product appears to be about 70%. in vivo effectiveness test, DLT showed significant differences from control on antiemetic action of Cm. In consequence, it was possible to conclude that double layered tablet might be a good candidate for the sustained release dosage forms.