• Journal of Pharmaceutical Investigation
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• v.40 no.5
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• pp.313-319
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• 2010

The objectives of this study were to evaluate the effect of formulation ingredients on the drug release and to optimize the novel sustained release matrix tablet formulations of bupropion hydrochloride. A three factor, three-level Box-Behnken design was used for the optimization procedure, with the amounts of PEO ($X_1$), citric acid ($X_2$) and Compritol 888 ATO ($X_3$) as the independent variables. The selected dependent variables were the cumulative percentage values of bupropion hydrochloride that had dissolved after 1, 4 and 8 hr. Various dissolution profiles of the drug from sustained release matrix tablets were obtained. Optimization was performed for $X_1$, $X_2$ and $X_3$ using the following target ranges; $30%{\leq}Y_1{\leq}45%$; $70{\leq}Y_2{\leq}85%$; $85%{\leq}Y_3{\leq}100%$. The optimized formulation for bupropion hydrochloride was achieved with 12.5% PEO ($X_1$), 2.5% citric acid ($X_2$) and 10% Compritol 888 ATO ($X_3$). The sustained release matrix tablets with the optimized formulation provided a release profile that was close to predicted values. In addition, the dissolution profiles of the sustained release matrix tablet with the optimized formulation were similar to those of the commercial product Wellbutrin$^{(R)}$ SR tablets ($f_2$=79.83).

• 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.

• Korean Journal of Plant Resources
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• v.21 no.1
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• pp.103-109
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• 2008

Nelumbo nucifera root(NNR) is used to clear summerheat(暑熱), bear Yang(陽) upwards and stop bleeding as mentioned in traditional Korean medicine. Also, it has been known that NNR is effective for lowering blood pressure and hyperlipidemia. The rhizome is considered to be nutritive, demulcent, diuretic and cholagogue and is used to treat piles, dyspepsia and diarrhea. An increasingly growing market for nutraceuticals and functional foods has triggered the study on natural sources for nutraceuticals, health foods and functional foods. But rhizome was inconvenient to formulate liquid dosage form(extract) by way of hot water because of its limited storage. Also the majority of the consumers have a complaint against the dosage. The purpose of this study was to develop the functional materials from NNR without side effects. We formulated the solid dosage form viz tablet and granule from the lotus root. Sensory evaluation was performed in terms of smell, taste, color and overall of lotus root and all colored forms(brown, dark brown, light green and yellow) of tablet and granule to evaluate the acceptability of the formulated tablets and granules. In sensory evaluation, among the formulated tablets and granules, light green granules obtained best score overall and yellow tablets showed the overall improved acceptability. In conclusion, lotus rhizome could be recommended as functional food. Further studies to clarify bioactive functions of Nelumbo nucifera in experimental animal model on atopic dermatitis are in progress.

• Journal of Pharmaceutical Investigation
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• v.27 no.3
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• pp.213-217
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• 1997

The present sustained-release terfenadine-pseudoephedrine HCl dosage form was the core tablet composed of outer (fast-release) layer containing 60 mg of terfenadine and l0mg of pseudoephedrine HCl, and inner (sustained-release) layer containing 110 mg of pseudoephedrine HCl. The purpose of this study was to investigate the possibility of formulating the terfenadine-pseudoephedrine HCl double-layered tablet which was bioequivalent to the core tablet. Its sustained-release and fast-release layer were formulated with disintegrating agents and polymers, respectively, varying with their kinds and amounts. The comparative dissolution test of double-layered and core tablet was carried out at pH 1.2, 4.0 and 6.8, leading to select composite of double-layered tablet whose dissolution pattern was similar to that of core tablet. It was composed of fast-release layer containing 60mg of terfenadine. 10 mg of pseudoephedrine HCl, sodium bicarbonate, microcrystalline cellulose and sodium starch glycolate, and sustained-release layer containing 110 mg of pseudoephedrine HCl and ethylcellulose/hydroxypropyl methylcellulose) (110/30 mg/tablet).

• Journal of Pharmaceutical Investigation
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• v.25 no.1
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• pp.19-29
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• 1995

The study was carried out to develop useful formulation for omeprazole(OMP) through OMP-ethylendiamine complex(OMPED), and the pharmaceutical properties of formula were tested to find out the difference in vivo behaviors of formulations between the free and complexed OMP. Oral and suppository dosage forms were also formulated and the dissolution profiles and pharmacokinetic parameters were measured to observe the difference in bioavailability between the free and complex form, and the correlation between dissolution rate and bioavailability was evaluated. The results are summarized as follows; In the case of formulation for oral administration, the release of OMP from enteric OMPED pellets was found satisfactory to the requirement standard and no decomposition of OMP in the pellets was found in acidic solution. Therefore the enteric OMPED pellets are anticipated to be a stable formulation. The release of OMP from OMPED tablet with chitosan as excipient and coated with cellulose acetate phthalate was found to be significantly retarded. The results of bioavailability test for OMP and OMPED tablets with lactose-excipient showed that the AUC value of OMP tablet was $116.89\;{\mu}g\;{\cdot}\;min/ml$, that of OMPED tablet was $161.10\;{\mu}g\;{\cdot}\;min/ml$, respectively. The reason why was thought that OMP decomposes more readily in body than OMPED, and the AUC of the tablet with chitosan-excipient and coated with cellulose acetate phthalate was most enhanced. In the case of bioavailability for suppositories with OMP, $OMP-{\beta}\;-cyclodextrin$ complex and OMPED, the AUC of OMPED suppository was most increased. From the above results, it is thought that the more stable and bioavailable oral or rectal dosage forms could be developed by using the OMPED as a potential OMP complex.

• Journal of Pharmaceutical Investigation
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• v.39 no.4
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• pp.269-273
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• 2009

The objective of this investigation was to develop a gastro-retentive(GR) dosage form of gabapentin and was to evaluate of its dissolution characteristics. GR tablet consists of expandable core tablet matrix and semi-permeable membrane coating. Poloxamer 407 and sodium bicarbonate were used to prepare the core matrix. Polyvinly acetate dispersion (Kollicoat $SR30D^{(R)}$) and polyvinyl alcohol-polyethylene glycol copolymer ((Kollicoat $IR^{(R)}$)) were employed to form the semi-permeable membrane. The GR tablets significantly expanded up to fivefold in simulated gastrointestinal fluids with no apparent damage of the coating membrane over 12 hours. Also, the swelling rate was controllable with the amount of sodium bicarbonate. The drug release was observed to be substantially sustained based on coating level. The release rate of gabapentin from the GR tablet was gradually slowed down as the coasting amount was increased. The gabapentin GR tablet with 8% coating level showed a pseudo-zero order release kinetics over 12 hours. These results suggest that this swellable GR tablet system having semi-permeable membrane coating can be applicable for hydrophilic drug substances like gabapentin.

• YAKHAK HOEJI
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• v.18 no.1
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• pp.49-58
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• 1974

Tablet product design problem was structured as constrained optimization problem and subsequently solved by multiple regression analysis and Lagrangian method of optimization. Aluminum flufenamate was the drug chosen and microcrystalline cellulose nad starch were the binder and disintegrant, respectivley. The effect of the binder and disintegrant concentration on tablet hardness, friability, volume, in vitro release rate, and urinary excretion rate of drug in human subjects was recorded. Since a reasonably rapid release rate of drug is generally an important objective in the design of solid dosage form, optimization of this parameter was employed in studying the applicability of constrained optimization to a pharmaceutical product design problem. In addition to finding optimal sitivity analysis studies to such problems was also illustratd. It would appear that prediction of the in vivo t$_{50%}$ response from a knowledge of the incitro t$_{50%}$ response can be made fairly accurately for the tablet system used in this study.

• Journal of Powder Materials
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• v.26 no.3
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• pp.225-230
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• 2019

To develop Taraxacum platycarpum extract (TP)-loaded particles for tablet dosage form, various TP-loaded particles composed of TP, dextrin, microcrystalline cellulose (MCC), silicon dioxide, ethanol, and water are prepared using a spray-drying method and fluid-bed-drying method. Their physical properties are evaluated using angle of repose, Hausner ratio, Carr's index, hardness, disintegrant time, and scanning electron microscopy. Optimal TP-loaded particles improve flowability and compressibility. Furthermore, 2% silicon dioxide gives increased flowability and compressibility. The formula of TP-loaded fluid-bed-drying particles at a TP/MCC/silicon-dioxide amount of 5/5/0.2 improves the angle of repose, Hausner ratio, Carr's index, hardness, and disintegrant time as compared with the TP-loaded spray-drying particles. The TP-loaded fluid-bed-drying particles considerably improve flowability and compressibility ($35.10^{\circ}$ vs. $40.3^{\circ}$, 0.97 vs. 1.17, and 18.97% vs. 28.97% for the angle of repose, Hausner ratio, and Carr's index, respectively), hardness (11.34 vs. 4.7 KP), and disintegrant time (7.4 vs. 10.4 min) as compared with the TP-loaded spray-drying particles. Thus, the results suggest that these fluid-bed-drying particles with MCC and silicon dioxide can be used as powerful particles to improve the flowability and compressibility of the TP.

• Journal of Powder Materials
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• v.28 no.3
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• pp.227-232
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• 2021

The purpose of this study is to optimize the powder formulation and manufacturing conditions for the solidification of an extract of the herb Bangpungtongseong-san (BPTS). To develop BPTS-loaded particles for the tablet dosage form, various BPTS-loaded particles composed of BPTS, dextrin, microcrystalline cellulose (MCC), silicon dioxide, ethanol, and water are prepared using spray-drying and high shear granulation (high-speed mixing). Their physical properties are evaluated using scanning electron microscopy and measurements of the angle of repose, Hausner ratio, Carr's index, hardness, and disintegration time. The optimal BPTS-loaded particles exhibit improved flowability and compressibility. In particular, the BPTS-loaded particles containing silicon dioxide show significantly improved flowability and compressibility (the angle of repose, Hausner ratio, and Carr's index are 35.27 ± 0.58°, 1.18 ± 0.06, and 15.67 ± 1.68%, respectively), hardness (18.97 ± 1.00 KP), and disintegration time (17.60 ± 1.50 min) compared to those without silicon dioxide. Therefore, this study suggests that particles prepared by high-speed mixing can be used to greatly improve the flowability and compressibility of BPTS using MCC and silicon dioxide.

• Journal of Pharmaceutical Investigation
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• v.19 no.4
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• pp.191-194
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• 1989

Bioequivalence test of $Asthcontin^{\circledR}$ tablet, a commercial slow-release theophylline (TP) dosage form, was performed using $Slo-bid^{\circledR}$ capsule as the reference. Since it has been confirmed that the saliva concentration of TP is closely correlated with the plasma concentration in man, the area under the saliva concentration-time curve was used as a bioavailability parameter. The statistical analysis showed that the two dosage forms are equivalent in bioavailability estimating from the saliva concentration. The results supported that the use of soliva as a test sample provides simple and easy techniques for bioequivalence tests of TP-containing dosage forms.