Compaction Behaviour of Musol, A New Direct Compression Vehicle

The compaction characteristics of Musol, a new autocompressible vehicle derived through chemical modification of mucuna gum was investigated. Avicel PH 101, Zeparox and Encompress were used as reference tablet vehicles. Values of the mean yield stress derived from the analysis of Heckel plots indicate that Musol consolidates principally by plastic deformation, The effect of lubrication and recompression on friability, tensile strength and re-working potential of the tablets prepared with the vehicles were determined. While Avicel PH 101 yielded the strongest tablets, Musol showed the highest re-working potential for lubricated and un-lubricated slugs. On the basis of friability, tensile Values of strength and re-working potential, Musol than the grades of Zeparpx or Encompress performed better used in the study.     

Tabletting Properties of Musol; A New Direct Compression Vehicle

A new autocompressible vehicle, Musol, obtained by chemical modification of an edible seed polysaccharide was evaluated for direct compression properties, A Hausner ratio of 1,2 and percent compressibility of 16.7 obtained for Musol indicate that it has very good flow properties. Musol showed superiority over Avicel PH 101, USP Fast-Flo lactose, and Encompress when evaluated in terns of flow rake of powders and moisture sorption by both powders and their slugs, Compacts prepared with Musol were found to disintegrate by erosion and therefore did not perform as well as either alginic acid or Ac-disol in 250 mg Sulphadimidine tablets. However, good drug release was obtained from aspirin tablets containing 5% w/w Musol as a dry binder. The t₅₀, t₉₀ and Dissolution efficiency were as good as the values obtained with 5% w/w Avicel PH 101, A 50/50 blend of Musol and Avicel PH 101 surpassed other blends in performance.     

Tabletting Properties of Musol; A New Direct Compression Vehicle

A new autocompressible vehicle, Musol, obtained by chemical modification of an edible seed polysaccharide was evaluated for direct compression properties, A Hausner ratio of 1,2 and percent compressibility of 16.7 obtained for Musol indicate that it has very good flow properties. Musol showed superiority over Avicel PH 101, USP Fast-Flo lactose, and Encompress when evaluated in terns of flow rake of powders and moisture sorption by both powders and their slugs, Compacts prepared with Musol were found to disintegrate by erosion and therefore did not perform as well as either alginic acid or Ac-disol in 250 mg Sulphadimidine tablets. However, good drug release was obtained from aspirin tablets containing 5% w/w Musol as a dry binder. The t₅₀, t₉₀ and Dissolution efficiency were as good as the values obtained with 5% w/w Avicel PH 101, A 50/50 blend of Musol and Avicel PH 101 surpassed other blends in performance.     

Comparative Evaluation of A New Direct Compression Excipient, SoludexTM 15

Soludex^TM15, a new corn-based maltodextrin, has been evaluated and compared to nine frequently used commercial excipients for direct compression. The properties of the excipients reported are median size, particle size distribution, bulk density, flow rate, repose angle, moisture content, and hardness and compressibility at several compaction pressures. The influence of concentration of lubricant and mixing time with a lubricant on hardness of Soludex 15 compacts were determined. The effect of 1% magnesium stearate on the hardness of compacts was determined for the ten excipients. Model formulations for direct compression tablets using Soludex 15 are presented, and for a batch of these tablets the weight variation, friability, hardness, disintegration and dissolution are reported. Soludex 15 exhibited excellent flow and compressibility, and model tablets using Soludex 15 as the direct compression diluent met USP specifications and provided a rapid dissolution of the active ingredient.     

Direct Compression of Piracetam

It is demonstrated that piracetam undergoes plastic deformation during compression. Incorporation of magnesium stearate dramatically reduces the mechanical strength of the tablets. This effect is much less pronounced when using glyceryl behenate as a lubricating agent.

Silicon dioxide on the contrary increases to a great extent the tensile strength of piracetam tablets. This advantageous impact remains unaffected by addition of magnesium stearte on condition that the drug is mixed with silicon dioxide prior to the addition of the lubricant.     

Evaluation of Xylitab 200, a New Filler/ Binder for Direct Compression, Using Factorial Design

The influence of a number of tablet factors were used to evaluate Xylitab 200®, a new filler/binder for direct compression, following a factorial design. The factors include types of filler/binder, drug, disintegrant, and amount of compression force. In the extended design, two storage conditions were selected. Factors found to have strong influence on tablet qualities from time after manufacturing to storage were drug solubility, amount of compression force, and storage condition. Comparison between tablets manufactured with the new filler/binder and those prepared with a known good filler/binder have shown that the latter is better than the former.     

The use of an Elastic Recovery Index as a Criterion of Compactional Behaviour of Some Direct Compression Bases

Abstract

The effects of compression force and holding time on computer logged strain movements (at constant stress) and elasticviscoelastic expansions (on load release) of compacts made from eight pharmaceutical powders are reported. The feasibility of using an elastic recovery index (the ratio of elastic recovery to viscoelastic strain movements) to predict the quality of a material is also discussed.

All compacts continued to consolidate by viscoelastic and plastic flow when held under constant stress during the holding period. The “compressible” bases Avicel PH-101 and Sta-Rx 1500 exhibited more time dependent movements than powders such as Paracetamol DC, Paracetamol, Emcompress and magnesium stearate. Poorly compressible materials such as magnesium carbonate and paracetamol showed the greatest elastic expansions on load release.

It has been found that the elastic recovery indices of the compressible materials were lower than those of poorly compressible powders.     

The use of an Elastic Recovery Index as a Criterion of Compactional Behaviour of Some Direct Compression Bases

The effects of compression force and holding time on computer logged strain movements (at constant stress) and elasticviscoelastic expansions (on load release) of compacts made from eight pharmaceutical powders are reported. The feasibility of using an elastic recovery index (the ratio of elastic recovery to viscoelastic strain movements) to predict the quality of a material is also discussed.

All compacts continued to consolidate by viscoelastic and plastic flow when held under constant stress during the holding period. The “compressible” bases Avicel PH-101 and Sta-Rx 1500 exhibited more time dependent movements than powders such as Paracetamol DC, Paracetamol, Emcompress and magnesium stearate. Poorly compressible materials such as magnesium carbonate and paracetamol showed the greatest elastic expansions on load release.

It has been found that the elastic recovery indices of the compressible materials were lower than those of poorly compressible powders.     

Comparative Tableting and Microstructural Properties of a New Starch for Direct Compression

A new directly compressible starch for direct compression marketed as Sepistab® St 200 has been studied in relation with the classical variety for direct compression—Sta Rx® 1500. Flowability of Sta Rx was in general higher. Sepistab showed a weight mean diameter two times higher than Sta Rx. Particle size of Sepistab demonstrated a better fitting to normal distribution. No differences of note were observed in the consolidation mechanism on the basis of the tablet-in-die Heckel method. Binding properties and plasticity of Sepistab were higher. Sta Rx showed more interparticulate and die wall friction during compression. Disintegration of the tablets was absolutely different. Sta Rx showed swelling of the tablet with gel formation and longer disintegration times. On the contrary, Sepistab showed almost immediate disintegration. This different behavior can be partially explained on the basis of the content of amylose as effective disintegrating agent. The microstructure of the tablets was measured by mercury porosimetry. The parameters calculated were the total porosity, median size of pore expressed as radius, and surface area of pores, assuming cylindrical pores. The microstructure of tablets of Sepsitab—with higher porosity, surface area of pores, and median pore radius-can also enhance the water penetration and disintegration of the tablet by breaking the hydrogen bonding which is formed during compression and suddenly released in the presence of water.     

Comparative Tableting and Microstructural Properties of a New Starch for Direct Compression

Abstract

A new directly compressible starch for direct compression marketed as Sepistab® St 200 has been studied in relation with the classical variety for direct compression—Sta Rx® 1500. Flowability of Sta Rx was in general higher. Sepistab showed a weight mean diameter two times higher than Sta Rx. Particle size of Sepistab demonstrated a better fitting to normal distribution. No differences of note were observed in the consolidation mechanism on the basis of the tablet-in-die Heckel method. Binding properties and plasticity of Sepistab were higher. Sta Rx showed more interparticulate and die wall friction during compression. Disintegration of the tablets was absolutely different. Sta Rx showed swelling of the tablet with gel formation and longer disintegration times. On the contrary, Sepistab showed almost immediate disintegration. This different behavior can be partially explained on the basis of the content of amylose as effective disintegrating agent. The microstructure of the tablets was measured by mercury porosimetry. The parameters calculated were the total porosity, median size of pore expressed as radius, and surface area of pores, assuming cylindrical pores. The microstructure of tablets of Sepsitab—with higher porosity, surface area of pores, and median pore radius-can also enhance the water penetration and disintegration of the tablet by breaking the hydrogen bonding which is formed during compression and suddenly released in the presence of water.     

Direct Compression Characteristics of Vitamin A-Acetate

A study of the direct compression characteristics of vitamin A-acetate has been made, using a wide range of compression speeds (24-620 mm/s). Relative powder density, mean yield pressure derived from Heckel analyses and radial tensile strengths were used as the basis of the investigation.

The mean yield pressure appeared to be independent of compression speed in the range 24-60 mm/s, whilst an increase was observed at higher speeds of 150-620 mm/s, attributable to the presence of predominantly fragmentation and plastic deformation mechanisms of consolidation respectively. Changes in tablet radial tensile strength and relative powder bed density (Do) appears to correlate with the hypothesis of a mixed mechanism of consolidation for vitamin A-acetate.     

Evaluation of a New Fine Particulate Cellulose as a Direct Compression Tablet Aid

Abstract

A new grade of α-cellulose, composed of a mixture of amorphous and crystalline cellulose was evaluated in this preliminary study for its potential as an inert direct compression tablet vehicle. Though not a micro-crystalline cellulose, this product, identified as EGC, possesses the tabletting characteristics of micro-crystalline cellulose. It is prepared by a physicochemical procedure that does not require severe heat or acid treatment but yields a product which is white, fine granular, free-flowing and highly compressible.     

Evaluation of a New Cellulose Material as Binding Agent for Direct Compression of Tablets

The properties of a new microcrystalline cellulose product Emcocel^R, was compared with those of fine grade of other commercial microcrystalline cellulose, Avicel^R PH 101. The crystal structure of Avicel was noticed to be some more amorphous than that of Emcocel. Both materials were similarly composed of irregularly shaped fibrous cellulose particles. The particle size distribution was clearly larger for Emcocel than for Avicel. Emcocel contained more both very small and very large particles. The loose density was also slightly smaller for Emcocel. There was practically no difference in spesific: surface area, water content and effective density of these materials. The behaviour of both microcrystalline cellulose powders during flow and binding processes was similar. Emcocel and Emcocel were rather cohesive and only fairly flowing materials. Tablets with very advantageous strength/pressure profiles were possible to produce using plain materials and also using tablet masses containing high concentrations of acetaminophenone. According to the results of this evaluation the physical and tableting properties of a new microcrystalline cellulose material, Emcocel, resemble very closely those of Avicel PH 101. Thus neither advantage nor disadvantage is derived using Emcocel instead of Avicel PH 101 as a binding component in tablet masses.     

A Contribution to the Manufacture of Diiodoquin TABLETS by Direct Compression

Abstract

Six direct compression vehicles and their binary blends in ratios of 1:1, 1:3 and 3:1 were investigated to compress diiodoquin directly into tablets. With respect to the mechanical properties of the produced tablets, Avicel, Celutab and 5TAR-x1500 were the suitable single vehicles for the manufacturing. Five vehicles, except STAR-x1500, produced tablets of fairly long disintegration times (120 min), while the other vehicle could not compress diiodoquin. The results shewed that blending of Avicel or Celutab with STAR-x1500 improved the physical standards of the produced tablets. Other than being a powerful disintegrant, STAR-x1500 could recover the disintegrating effect of Avicel. On the other hand, the reduction in disintegration times of the tablets compressed with STAR-/Celutab blends, was due to the incorporation of STAR-x in the formulations.

In such a case of noncompressible drug, a large concentration of a binary blended vehicle was needed to compress tablets of good physical characters. The least concentration needed to compress diiodoquin into tablets was not less than 42.0% w/w.     

A Contribution to the Manufacture of Diiodoquin TABLETS by Direct Compression

Six direct compression vehicles and their binary blends in ratios of 1:1, 1:3 and 3:1 were investigated to compress diiodoquin directly into tablets. With respect to the mechanical properties of the produced tablets, Avicel, Celutab and 5TAR-x1500 were the suitable single vehicles for the manufacturing. Five vehicles, except STAR-x1500, produced tablets of fairly long disintegration times (120 min), while the other vehicle could not compress diiodoquin. The results shewed that blending of Avicel or Celutab with STAR-x1500 improved the physical standards of the produced tablets. Other than being a powerful disintegrant, STAR-x1500 could recover the disintegrating effect of Avicel. On the other hand, the reduction in disintegration times of the tablets compressed with STAR-/Celutab blends, was due to the incorporation of STAR-x in the formulations.

In such a case of noncompressible drug, a large concentration of a binary blended vehicle was needed to compress tablets of good physical characters. The least concentration needed to compress diiodoquin into tablets was not less than 42.0% w/w.     

Optimization of a New Filler/Binder for Direct Compression Using Central Composite Design

Abstract

An experimental design, the Central Composite, was used for the optimization of a new filler/binder (Xylitab 200®) for direct compression, with aspirin as the model drug. The design consists of four independent variables filler/binder, drug, disintegrant, and compression force) in varying amounts, and with crushing strength, friability, weight variation, disintegration time, and dissolution rate as response variables. Multiple regression in the form of a second-order polynomial was used to determine meaningful relationships. In this study, the amounts of compression force and disintegrant played an important role in controlling the response variables.     

Optimization of a New Filler/Binder for Direct Compression Using Central Composite Design

An experimental design, the Central Composite, was used for the optimization of a new filler/binder (Xylitab 200®) for direct compression, with aspirin as the model drug. The design consists of four independent variables filler/binder, drug, disintegrant, and compression force) in varying amounts, and with crushing strength, friability, weight variation, disintegration time, and dissolution rate as response variables. Multiple regression in the form of a second-order polynomial was used to determine meaningful relationships. In this study, the amounts of compression force and disintegrant played an important role in controlling the response variables.     

Experimentally Designed Optimization of Direct Compression Tablets

The work reported here describes the improvement of an industrial production of tablets formed by direct compression. This formulation contained 50% active substance of plant origin as a nonhygroscopic powder. The first step was to evaluate a number of direct compression excipients in preformulation tests and then make up a basic formulation providing tablets with correct characteristics. The second step was the optimization of the initial formulation using a two-level factorial experimental design. This enabled the best formulations to be selected objectively.     

Comparative Evaluation of Several Direct Compression Sugars

Three new and two commercially available sugar matrices were comparatively evaluated for several fundamental properties of direct compression powder systems. These properties included: particle size distribution, powder flow (determined by a recording powder flow meter), bulk density and moisture content. The matrices studied were Dipac, Nutab, and California and Hawaiian (C & H) Products A, B, and C. These matrices were formulated in to chewable ascorbic acid, multivitamin, and antacid tablets, and analyzed for: weight uniformity, thickness, diameter, hardness, disintegration, resistance to impact stress, friability, dissolution and effect due to aging.

The data obtained showed that the new products (C & H products) were comparable, and in some cases, even superior to the commercially available ones.     

Comparative Evaluation of Several Direct Compression Sugars

Abstract

Three new and two commercially available sugar matrices were comparatively evaluated for several fundamental properties of direct compression powder systems. These properties included: particle size distribution, powder flow (determined by a recording powder flow meter), bulk density and moisture content. The matrices studied were Dipac, Nutab, and California and Hawaiian (C & H) Products A, B, and C. These matrices were formulated in to chewable ascorbic acid, multivitamin, and antacid tablets, and analyzed for: weight uniformity, thickness, diameter, hardness, disintegration, resistance to impact stress, friability, dissolution and effect due to aging.

The data obtained showed that the new products (C & H products) were comparable, and in some cases, even superior to the commercially available ones.