• Journal of Pharmaceutical Investigation
• /
• 제37권5호
• /
• pp.275-280
• /
• 2007

A rapidly disintegration famotidine tablet formulation in the oral cavity was developed using microcrystalline cellulose (MCC) and low-substituted hydroxypropyl cellulose (L-HPC), or additionally cropovidone as an internal disintegrant. Effects of disintegrants on the disintegration time in vitro and hardness were evaluated. Average wetting time of the tablets prepared in scale-up manufacturing process was less than 15 sec. Among the formulations tested, the tablet prepared with crospovidone as an internal disintegrant and Emcocel $90M^{(R)}$ as an external disintegrant showed fastest disintegration. These results may suggest that crospovidone and Emcocel $90M^{(R)}$ possessed excellent wetting nature, which result in the rapid disintegration of tablet.

• 한국분말재료학회지
• /
• 제26권3호
• /
• pp.225-230
• /
• 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.

• 약학회지
• /
• 제18권1호
• /
• pp.49-58
• /
• 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 Pharmaceutical Investigation
• /
• 제6권2호
• /
• pp.69-82
• /
• 1976

Tablet product design problem was structured as constrained optimization problem and subsequently solved by multiple regression analysis and Lagrangian method of optimization. We used Lagrangian method for the purpose of finding the reason of the previous results. Biodiastase and cellulase were the enzymes, chosen, $Avicel{\circledR}$ and corn starch or calcium carboxy methyl cellulose were the binder and disintegrant, respectively. The effect of the dry binder and disintegrant concentration on tablet hardness, friability, volume, disintegration time was recorded. Optimization of this parameter was studied by using the constrained optimization method. In addition to finding a optimal condition of the enzyme tablets, the application of sensitivity analysis studies to such problems was also illustrated. In order to get a stable preparations of the enzyme tablets, accelerated test of coating tablets was carried out in this study. the results are as follows. 1) The minimum disintegration time, such that the average tablet volume did not exceed 0.0154 cubic inch and the average friability value did not exceed 0.62%, was 6.6 minutes and then $Avicel{\circledR}$ and corn starch were 15.4% and 17.2%, respectively. 2) The multiple-correlation coefficients for the regression models of tablet hardness, friability, disintegration time and volume were with in the 95% confidence range. 3) According to the test results, calcium carboxymethyl cellulose can be used as a disintegrant instead of corn starch.

• 대한의생명과학회지
• /
• 제22권4호
• /
• pp.184-188
• /
• 2016

The objective of this study was to develop a pH dependent oral matrix tablet containing probiotics. In this study, hydroxyl-propyl-methyl-cellulose (HPMC) and polyvinyl pyrrolidone K30 (PVP K-30) was utilized as a binder, sodium starch glycolate (SSG) was used as a disintegrant material for the tablet formulation. The disintegration test, hardness test, angle of response were performed to examine the characteristics of prepared tablet. Lactobacillus vitality test was applied to analyze the total Lactobacillus viable count. The results demonstrated that the pH dependent matrix tablet was prepared successfully and can thus be industrialized instead of the current methodologies used for preparation of conventional probiotics.

• Journal of Pharmaceutical Investigation
• /
• 제20권1호
• /
• pp.7-12
• /
• 1990

In case of the slowly disintegrating tablets such as enzyme preparations, disintegration time (DT) may be the important factor in formulating those preparations. The effects of tablet hardness, lubricants and disintegrants on DT were investigated in this approach. Disintegration time was significantly affected by disintegrants, moderately by lubricants, but not by tablet hardness. The effect was in the order of magnesium stearate >talc, PEG, sodium benzoate in case of lubricants, and of Ac-Di-Sol>LHPC>Primogel >Kollidon in case of disintegrants. Because lubricants and disintegrants influenced the tablet hardness and DT profile showed complicated pattern, it should be remembered that all factors mentioned above should be simultaneously considered in the formulation of enzyme tablets.

• Journal of Pharmaceutical Investigation
• /
• 제40권5호
• /
• pp.297-304
• /
• 2010

The present work focuses on preparation of olanzapine, orally dispersing tablets by direct compression method. Effect of super disintegrant crospovidone, disintegration time, drug content on in vitro release has been studied. A factorial design was employed in formulating a prompt dispersible tablet. The selected independent variables crospovidone and fmelt showed significant effect on dependent variables i.e. disintegration time and percent drug dissolved. Disintegration time and percent drug dissolved decreased with increase in the level of crospovidone. The similarity factor $f_2$ was found to be 97.48 for the developed formulation indicating the release was similar to that of the marketed formulation. Pharmacokinetics of olanzapine after single-dose oral administration of orally disintegrating tablet in normal volunteers were evaluated and the results showed that PK parameters (Cmax, Tmax, AUC) of the designed ODT matrix were similar to those of commercial product, Zyprexa Zydis$^{(R)}$ as a reference.

• Journal of Pharmaceutical Investigation
• /
• 제22권1호
• /
• pp.41-48
• /
• 1992

Six common tablet disintegrants (corn starch, Avicel PH102, calcium carboxymethylcellulose, Primojel, Kollidon CL and Ac-Di-Sol) were used at the concentration of 0, 2, 4 and 6% (w/w) in salicylamide tablets made with wet granulation method. Certain physical parameters of the disintegrants (moisture sorption, hydration capacity and bulk density) were determined to evaluate their relative efficiency. The disintegration time and dissolution rate of the tablets were correlated well with the ranks of initial rate of moisture sorption for each disintegrant as follows; Ac-Di-Sol, Kollidon CL, primojel, calcium CMC, corn starch and Avicel PH102. The initial rate of moisture sorption was important for the disintegration capacity as well as hydration capacity. The effect of storage at different temperatures and relative humidity upon the tablets containing various disintegrants was evaluated in terms of tablet hardness and disintegration time. Storage at high temperature reduced the hardness substantially and retarded the disintegration of the all tablets studied. Especially, the hardness of tablets containing Kollidon CL was significantly reduced. Although the tablet hardness was decreased and the disintegration time was increased under a moderate humid condition, both of them were decreased under the severely high humid condition of 80 or 90% RH, which was due to the breakrupture of tablet matrix bonds by the excessive uptake of moisture. Therefore, the stability caused by moisture sorption should be considered, when disintegrants having high moisture sorption such as Kollidon CL, Ac-Di-Sol and Primojel were employed in the tablets containing water-labile or hygroscopic drugs.

• Archives of Pharmacal Research
• /
• 제23권5호
• /
• pp.507-512
• /
• 2000

This study set out to improve the physical and pharmaceutical characteristics of the present formulation using an appropriate experimental design. The work described here concerns the formulation of the dispersible tablet applying direct compression method containing roxithromycin in the form of coated granules. In this study $2^3$ factorial design was used as screening test model and Central Composite Design (CCC) associated with response surface methodology was used as optimization study model to develop and to optimize the proper formulation of roxithromycin dispersible tablet. The three independent variables investigated were functional excipients like binder (X1), disintegrant (X2) and lubricant (X3). The effects of these variables were investigated on the following responses: hardness (Y1), friability (Y2) and disintegration time (Y3) of tablet. Three replicates at the center levels of the each design were used to independently calculate the experimental error and to detect any curvature in the response surface. This enabled the best formulations to be selected objectively. The effect order of each term to all response variable was X3> X2> Xl> X1＊X2> X2＊X2> X2＊X3> X3＊X3> Xl＊X3> Xl＊Xl and model equations on each response variables were generated. Optimized compositions of formula were accordingly computed using those model equations and confirmed by following demonstration study. As a result, this study has demonstrated the efficiency and effectiveness of using a systematic formulation optimization process to develop the tablet formulation of roxithromycin dispersible tablet with limited experiment.