• YAKHAK HOEJI
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• v.36 no.6
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• pp.513-517
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• 1992

The effect of solubility and hygroscopicity of some tablet diluents on the disintegration of enzyme tablets was investigated. Tablets were prepared by direct compression method using sodium starch glycolate, crospovidone, croscarmellose sodium and low-substituted hydroxypropyl cellulose as super disintegrants. Lactose, dextrose, sucrose, sorbitol and calcium phosphate dibasic were selected as typical diluents in this study. They were different in solubility (sucrose, sorbitol>dextrose>dextrose>lactose>calcium phosphate dibasic) and hygroscopicity (sorbitol>sucrose>dextrose>caicium phosphate dibasic, lactose). The disintegrants accelerated differently the disintegration of the tablets prepared with different diluents in the decreasing order of calcium phosphate dibasic>lactose>dextrose>sucrose and sorbitol. These results indicate highly soluble and/or hygroscopic diluents decrease the efficiencies of super disintegrants in the enzyme tablets.

• Journal of Pharmaceutical Investigation
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• v.20 no.1
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• pp.7-12
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• 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
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• v.22 no.1
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• pp.41-48
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• 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.

• Journal of Pharmaceutical Investigation
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• v.33 no.1
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• pp.67-71
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• 2003

Drug excipients are material used in the formulation of pharmacologically active drugs. They have a variety of roles including dilutents/fillers/bulking agents, binders/adhesives, propellant, disintegrants, lubricants/dlidants, colors, flavors, coating agents, polising agents, fragrance, sweeteening agent, polymers and waxes. Excipient should be inert or inactive and does not interfere with the test. Nowadays within industry there has been a recent surge of interest in novel excipient for novel dosage forms. The purpose of the review is to introduce the administration systems of drug excipient about kinds, matters to be attended to change of excipients.

• Journal of Pharmaceutical Investigation
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• v.38 no.1
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• pp.51-55
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• 2008

To develop a novel metformin HCl-loaded GR type tablet, various tablets were compressed with poly acrylic acid (PAA) and hydroxypropylmethyl cellulose (HPMC) using a wet granulation, and their physical properties such as swelling rate, hardness and dissolution were then investigated. Among the formulae tested in this study, the tablet prepared with PAA 971 and 974 as disintegrants showed fastest dissolution rate and swelling rate. Furthermore, the tablets prepared with PAA and HPMC improved the swelling rate, hardness and dissolution compared to those prepared with only HPMC. Our results suggested that the tablets prepared with PAA 971, 974 and HPMC might be a potential candidate for gastric retention type tablets.

• Journal of Pharmaceutical Investigation
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• v.37 no.5
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• pp.275-280
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• 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.

• Journal of Pharmaceutical Investigation
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• v.23 no.1
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• pp.51-53
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• 1993

Mucoadhesive tablets containing hydroxypropylcellulose-H (HPC) and carbopol 934 (CP) were prepared from direct compression. Their adhesive forces and water absorptions were investigated by using mouse peritoneal membrane and 1.5% agar plate, respectively. Adhesive force was significantly improved with increasing CP concentration, but was not affected by compression force and addition of disintegrants. And adhesive force to mouse peritioneal membrane was increased as fixing time increased. In conclusion, adequate adhesive force can be obtained by control of CP/HPC ratio and fixing time.

• Advances in Traditional Medicine
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• v.5 no.1
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• pp.29-36
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• 2005

Polysaccharide hydrogels constitute a structurally diverse class of biological macromolecules with a wide range of physicochemical properties. They also constitute important members of the family of industrial water-soluble polymers. They find application in Pharmacy as binders, disintegrants, suspending, emulsifying and sustaining agents. According to the International Pharmaceutical Excipients Council (IPEC), an excipient must have an established safety profile. Hence, in the present study, in vitro cytotoxicity on Vero and HEp-2 cell lines, and in vivo acute toxicity in rats were carried out to establish the safety of polysaccharide hydrogels from the seeds of Plantago ovata and Ocimum basilicum. The in vitro cytotoxicity was determined by MTT and SRB assays. In the in vivo acute toxicity, the effects of three different doses of hydrogels (100, 200 and 400 mg/kg body weight) on food and water intake, body weight, biochemical and hematological parameters were studied. The results of in vitro did not show any cytotoxicity on both the cell lines used. In the in vivo acute toxicity, the hydrogels did not show any toxic symptoms in all three dose levels. This establishes the safety of the selected hydrogels. Hence, they can be used as excipients in pharmaceutical dosage forms.

• Journal of Pharmaceutical Investigation
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• v.27 no.2
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• pp.133-137
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• 1997

Buccal absorption test of omeprazole in human was performed to determine the permeability of the drug molecule through oral mucous membrane. Oral mucosal adhesive tablets of omeprazole were prepared by compressing the omeprazole with a mixture of sodium alginate and hydroxypropylmethyl cellulose (HPMC) as bioadhesive polymers, magnesium oxide (MgO) as a stabilizer and sodium carboxymethyl cellulose (Na CMC) or cros-carmellose sodium (Ac-Di-Sol) as disintegrants. The bioadhesive force, stability in saliva and release characteristics of the tablets were evaluated. Omeprazole was absorbed about 23% in 15 min through human buccal mucous membrane. Furthermore, omeprazole was stable in saliva for more than 8 hrs when MgO was added to the tablet as the amount of 2.5 fold of omeprazole. The release rate of omeprazole was increased with increasing the amount of sodium alginate in the tablet. From these results, it is suggested that tablets composed of [omeprazole/HPMC/sodium alginate/MgO/Ac-Di-Sol and/or Na CMC (20/6/24/50/10) (mg/tablet)] are potential candidate for buccal drug delivery system.

• Journal of Pharmacopuncture
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• v.25 no.4
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• pp.317-325
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• 2022

Polymers are the major constructive material of pharmaceutical formulations that play a prime role in designing effective drug-delivery systems and releasing drugs at their sites of application. Polymers are composed of multiple repeating units of high molecular mass components with attendant properties. Most synthetic polymers are non-biocompatible, expensive, and extremely inclined to deliver adverse impacts. Meanwhile, edible polymers obtained from natural sources have gained remarkable recognition for their promising use in modern medicine. Moreover, polymers derived from natural sources are generally preferred due to certain of their unique features such as abundant availability, biocompatibility, nontoxicity, economical, safe, and effective functions that fit the purpose. Polysaccharides including starch, cellulose, hemicellulose, pectin, and mucilage are identified as a major class of naturally obtained molecules that have a substantial role as functional polymers. This review summarizes the potential role of polysaccharides derived from vegetable sources such as adhesives, anticaking agents, binders, disintegrants, emulsifiers, film-framing agents, and thickeners. This is simply an opportunity to abandon synthetic excipients that hurt our bodies and think back to nature from where we originate.