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.     

Compaction Behaviour of Musol,A New Direct Compression Vehicle

Abstract

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.     

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.     

Effect of repeated compaction of tablets on tablet properties and work of compaction using an instrumented laboratory tablet press

The repeated compaction of Avicel PH101, dicalcium phosphate dihydrate (DCP) powder, 50:50 DCP/Avicel PH101 and Starch 1500 was studied using an instrumented laboratory tablet press which measures upper punch force, punch displacement and ejection force and operates using a V-shaped compression profile. The measurement of work compaction was demonstrated, and the test materials were ranked in order of compaction behaviour Avicel PH101?>?DCP/Avicel PH101?>?Starch?>?DCP. The behaviour of the DCP/Avicel PH101 mixture was distinctly non-linear compared with the pure components. Repeated compaction and precompression had no effect on the tensile fracture strength of Avicel PH101 tablets, although small effects on friability and disintegration time were seen. Repeated compaction and precompression reduced the tensile strength and the increased disintegration time of the DCP tablets, but improved the strength and friability of Starch 1500 tablets. Based on the data reported, routine laboratory measurement of tablet work of compaction may have potential as a critical quality attribute of a powder blend for compression. The instrumented press was suitable for student use with minimal supervisor input.     

Evaluation of Mujol as a Direct Compression Excipient in Oxytetracycline Hydrochloride Tablet Formulations

Abstract

The physical properties of oxytetracyc1ine hydrochloride tablets compressed with Musol, a new autocompressib1e vehicle obtained by chemical modification of an edible seed polysaccharide were studied, Avice1 PH 101, Fast-f1o lactose and Emcompress were used as basis for comparison.

With the exception of those tablets containing Emcompress, good disintegration and dissolution profiles were obtained in all the batches formulated. The dissolution characteristics of the tablets did not change significantly after storage in the dark at 30°C for 96 weeks.     

Comparison of two Varieties of Microcrystalline Cellulose as Filler-Binders II. Hydrochlorothiazide Tablets

Abstract

In tests of direct-compression hydrochlorothiazide tablets prepared with either of two varieties of microcrystalline cellulose (Avicel PH 101 and Avicel PH 102), PH 102 tablets had better mechanical properties (owing to lower compressibility of mixtures and greater Interparticle bonding), while PH 101 tablets released the active principle faster. These differences are related to observed differences In tablet micropore structure.     

Comparison of two Varieties of Microcrystalline Cellulose as Filler-Binders II. Hydrochlorothiazide Tablets

In tests of direct-compression hydrochlorothiazide tablets prepared with either of two varieties of microcrystalline cellulose (Avicel PH 101 and Avicel PH 102), PH 102 tablets had better mechanical properties (owing to lower compressibility of mixtures and greater Interparticle bonding), while PH 101 tablets released the active principle faster. These differences are related to observed differences In tablet micropore structure.     

Comparison of two varieties of microcrystalline cellulose as filler-binders I. Perdnisone tablets

A comparative study of two varieties of microcrystalline cellulose (Avicel PH 101 and Avicel PH 102) as excipients in direct compression prednisone tablets has been carried out. The effects of compression force, proportion of drug/excipient and variety of cellulose (defined by means of mean particle size) on the structural, mechanical and release properties of the tablets were studied. Differences were observed in the behaviour of the two varieties of cellulose affecting all the properties analyzed. These differences diminished, and disappeared in some cases, when 10% prednisone was present. The different degrees of interparticle association and the relations between the structural, mechanical and drug release properties of the tablets explain the differences observed.     

Comparative Evaluation of Certain Excipients and their Binary Blends for Direct Compression Oxytetracycline Hydrochloride Tablets

Abstract

Five direct compression excipients as well as their binary blends in ratios of 1:1, 1:3 and 3:1 were comparatively evaluated to compress oxytetracycline hydrochloride into tablets. With respect to the mechanical properties of the produced tablets, Avicel PH101, Celutab and STAR-x1500 in this order, were the most suitable single excipients for the production. The results showed that the incorporation of a second excipient in the formulation changes the physical standards of the produced antibiotic tablets. It was found that not only the type of the incorporated excipient is effective but also, its concentration in the formula. The investigation proved that Avicel/STAR-x1500 blends in all different ratios followed by some blends of celutab with Avicel or STAR-x1500 were the best blended excipients to produce satisfactory antibiotic tablets.     

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.     

Influence of process variables on physical properties of the pellets using extruder and spheronizer

Placebo pellets containing lactose and microcrystalline cellulose (Avicel PH101®) ratio 60:40 were prepared by the extrusion-spheronization process. The influence of processing variables, including the spheronizer speed, the spheronization time, the binder type, and the concentration and amount of water content on physical properties of the pellets, were studied. The sphericity of pellets was increased with increasing spheronizer speed during wet mass process. When spheronization time was increased, sphericity, smooth surface, and particle size of pellets were increased. Increasing binder concentration will increase particle size. Pellets using HPC-M® as a binder at high spheronizer speeds showed spherical shape, narrow size distribution, and good flow properties when compared with Methocel E-15LV®, HPC-L®, and Methocel A4M®. In addition, increasing HPC-M concentration had no effect on shape and particle size of pellets. The amount of water content was found to affect shape, flow rate, and density. In summary, suitable conditions consisted of 2% w/w of HPC-M, 40% w/w of water, and 15 min of spheronization time at 951 rpm of spheronizer speed.     

Comparison of Xylan and Some Commercial Materials as Disintegrants in Tablets

Abstract

The disintegrant properties of xylan, a polymerization product of the pentose sugar xylose, were evaluated and these were compared with the properties of four commercial materials used for direct compression of tablets. The reference adjuvants were microcrystalline cellulose, Avicel PH 101, microfine cellulose, Elcema G 250, carboxymethyl starch, Primojel STD, and modified starch, Sta-Rx 1500.     

Comparison of Disintegrant and Binder Activity of Three Corn Starch Products

This study demonstrates the differences obtained when using different corn starch products as both binder and disintegrant in pharmaceutical tablets. Formulations made with Fluftex W, Tablet White and Purity 21 starches were compared. In addition, Avicel PH101 was used in this study as a benchmark component whose properties are well understood.

Four test formulations containing hydrochlorothiazide were prepared by wet granulation. Starch was incorporated in both powder and paste form. All granulations were found to possess similar traits when evaluated based upon geometric mean diameter, particle size distribution, bulk/tap densities, powder flow rate and surface characteristics.

Tablets prepared from these granulations were shown to be similar when evaluated for degree of friability, weight and content uniformity. All starch formulations disintegrated within 30 seconds and produced similar dissolution profiles. Tablets produced with Avicel, however, were found to exhibit significantly longer disintegration times than the starch formulations. In addition, these tablets displayed a dissolution profile that was significantly different than the starch formulations, particularly during the earlier stages of the dissolution process.

When monitoring compression and ejection forces required to produce tablets of the same degree of hardness (≈6kg), Fluftex W and Tablet White granulations were found to use significantly lower forces than the Purity 21 granulation. This may be indicative of Fluftex W and Tablet White's superiority over Purity 21 in terms of binder capacity.     

Comparison of Disintegrant and Binder Activity of Three Corn Starch Products

This study demonstrates the differences obtained when using different corn starch products as both binder and disintegrant in pharmaceutical tablets. Formulations made with Fluftex W, Tablet White and Purity 21 starches were compared. In addition, Avicel PH101 was used in this study as a benchmark component whose properties are well understood.

Four test formulations containing hydrochlorothiazide were prepared by wet granulation. Starch was incorporated in both powder and paste form. All granulations were found to possess similar traits when evaluated based upon geometric mean diameter, particle size distribution, bulk/tap densities, powder flow rate and surface characteristics.

Tablets prepared from these granulations were shown to be similar when evaluated for degree of friability, weight and content uniformity. All starch formulations disintegrated within 30 seconds and produced similar dissolution profiles. Tablets produced with Avicel, however, were found to exhibit significantly longer disintegration times than the starch formulations. In addition, these tablets displayed a dissolution profile than was significantly different than the starch formulations, particularly during the earlier stages of the dissolution process.

When monitoring compression and ejection forces required to produce tablets of the same degree of hardness (≈6kg), Fluftex W and Tablet White granulations were found to use significantly lower forces than the Purity 21 granulation. This may be indicative of Fluftex W and Tablet White's superiority over Purity 21 in terms of binder capacity.     

Comparison of Xylan and Some Commercial Materials as Disintegrants in Tablets

The disintegrant properties of xylan, a polymerization product of the pentose sugar xylose, were evaluated and these were compared with the properties of four commercial materials used for direct compression of tablets. The reference adjuvants were microcrystalline cellulose, Avicel PH 101, microfine cellulose, Elcema G 250, carboxymethyl starch, Primojel STD, and modified starch, Sta-Rx 1500.     

Comparison of Disintegrant and Binder Activity of Three Corn Starch Products

Abstract

This study demonstrates the differences obtained when using different corn starch products as both binder and disintegrant in pharmaceutical tablets. Formulations made with Fluftex W, Tablet White and Purity 21 starches were compared. In addition, Avicel PH101 was used in this study as a benchmark component whose properties are well understood.

Four test formulations containing hydrochlorothiazide were prepared by wet granulation. Starch was incorporated in both powder and paste form. All granulations were found to possess similar traits when evaluated based upon geometric mean diameter, particle size distribution, bulk/tap densities, powder flow rate and surface characteristics.

Tablets prepared from these granulations were shown to be similar when evaluated for degree of friability, weight and content uniformity. All starch formulations disintegrated within 30 seconds and produced similar dissolution profiles. Tablets produced with Avicel, however, were found to exhibit significantly longer disintegration times than the starch formulations. In addition, these tablets displayed a dissolution profile that was significantly different than the starch formulations, particularly during the earlier stages of the dissolution process.

When monitoring compression and ejection forces required to produce tablets of the same degree of hardness (≈6kg), Fluftex W and Tablet White granulations were found to use significantly lower forces than the Purity 21 granulation. This may be indicative of Fluftex W and Tablet White's superiority over Purity 21 in terms of binder capacity.     

Comparison of Disintegrant and Binder Activity of Three Corn Starch Products

Abstract

This study demonstrates the differences obtained when using different corn starch products as both binder and disintegrant in pharmaceutical tablets. Formulations made with Fluftex W, Tablet White and Purity 21 starches were compared. In addition, Avicel PH101 was used in this study as a benchmark component whose properties are well understood.

Four test formulations containing hydrochlorothiazide were prepared by wet granulation. Starch was incorporated in both powder and paste form. All granulations were found to possess similar traits when evaluated based upon geometric mean diameter, particle size distribution, bulk/tap densities, powder flow rate and surface characteristics.

Tablets prepared from these granulations were shown to be similar when evaluated for degree of friability, weight and content uniformity. All starch formulations disintegrated within 30 seconds and produced similar dissolution profiles. Tablets produced with Avicel, however, were found to exhibit significantly longer disintegration times than the starch formulations. In addition, these tablets displayed a dissolution profile than was significantly different than the starch formulations, particularly during the earlier stages of the dissolution process.

When monitoring compression and ejection forces required to produce tablets of the same degree of hardness (≈6kg), Fluftex W and Tablet White granulations were found to use significantly lower forces than the Purity 21 granulation. This may be indicative of Fluftex W and Tablet White's superiority over Purity 21 in terms of binder capacity.     

Evaluation of Tableted Microspheres of Dipyridamole

Microspheres of dipyridamole were prepared by solvent evaporation methods. The effect of additives Avicel PH 101, and beta cyclodextrin on the release rate of tableted microspheres were studied. Incorporating Avicel or beta cyclodextrin increased the dipyridamole release rates in tableted microspheres. Beta cyclodextrin was found to be a good additive for microsphere tablets to increase the drug release rates without causing disintegration.     

Compressional Behaviour of an Agglomerated Cellulose Powder

The ability of an agglomerated cellulose powder to total and plastic deformation was evaluated and compared with those of Avicel PH 101, Emcocel and an experimental depolymerized cellulose powder. The elastic recovely of compressed cellulose tablets was also measured. The effects of deformation of the material during the tableting process and recovery of tablet after maximum compression on the mechanical strength of tablets were also discussed.

The apparent net work done into tablets during compression as well as the yield pressures to total and plastic deformation, determined from the Heckel treatment, showed no great differences between the agglomerated cellulose powder and the other cellulose powders. Thus all the cellulose materials studied had rather similar ability to total, i.e. elastic and plastic, deformation and to permanent, i.e. pure plastic, deformation. The obvious fragmentation of the agglomerated cellulose powder already at low compressional pressure, however, seemed to be advantageous for the formation of strong compacts.     

Comparing the Compressibility of Ludipress with the Other Direct Tableting Agents by Using Acetaminophen as an Active Ingredient

Ludipress is a direct tableting agent which acts as an unique component, is really a multi component. In this study Ludipress compressibility and powder technological properties are compared with the other kind of DC agents (Avicel PH 102, Elcema G 250 and Elcema P 050) which are structurally based on cellulose. Acetaminophen has been chosen as an active ingredient.

The compression properties of powders and three direct tableting agent were investigated using the Heckel and Kawakita equations. Each formulations and compressed tablets which are compacted by hydraulic press with different pressure value were photographed by scanning electron microscope.

As a result Ludipress shows stable flow properties and the dilution potential of Ludipress is lower than the other DC agents.