Direct Compression Tablet Formulation Research Articles

Optimization of Tablet Formulations Containing

AbstractAn optimized direct compression tablet formulation of a conventional theophylline tablet was developed using the technique of response surface methodology and successive quadratic programming (SQP). The response surfaces were obtained from fitting data generated from a secondorder uniformprecision rotatable hexagonal experimental design. The tablet formulation was optimized for mean in vitro dissolution time using disintegration time, ejection force, friability and hardness, as constraints within the experimental region by the SQP technique. The response surface model was validated by preparing and evaluating the predicted formulation. The characteristics of the tablet formulation were analyzed by principal component analysis. Sensitivity analysis for the optimal solution was performed for each constraint, while all remaining constraints were held constant. The robustness of the response surface model was evaluated by simulation for error in the compression force values.

The Effect of Aging on Disintegrant Efficiency in Direct Compression Tablets with Varied Solubility and Hygroscopicity, in Terms of Dissolution

AbstractThe effect of tablet aging on the dissolution efficiency of three “super disintegrants”, sodium starch glycolate, crospovidone, and croscarmellose sodium, was investigated utilizing directly compressed tablets. Lactose, dicalcium phosphate dihydrate, and sorbitol, alone or in combination, provided varying degrees of solubility and hygroscopicity to the direct compression tablet formulations. The results indicate that aging did not decrease the effectiveness of the super disintegrants in promoting invitro dissolution. The composite solubility and hygroscopicity of the tablets did not adversely influence the aging characteristics of the super disintegrants. Super disintegrants that complied with the same compendial specifications but were obtained from different sources behaved similarly in promoting tablet dissolution after storage.

Effect of Tablet Solubility and Hygroscopicity on Disintegrant Efficiency in Direct Compression Tablets In Terms of Dissolution

The effect of tablet composite solubility and hygroscopicity on the dissolution efficiency of three “super disintegrants”, sodium starch glycolate, crospovidone, and croscarmellose sodium, was investigated. Lactose, dicalcium phosphate dihydrate, and sorbitol, alone or in combination, provided varying degrees of solubility and hygroscopicity to the direct compression tablet formulations. To monitor in vitro dissolution, 1% p-aminobenzoic acid was added to the formulation as a tracer. The results indicate that hygroscopic ingredients decrease the effectiveness of super disintegrants in promoting in vitro dissolution. The greater the overall hygroscopicity of the tablet formulation, the larger the decrease in the efficiency of the super disintegrant. Composite tablet solubility did not influence the effectiveness of the super disintegrants. Super disintegrants that complied with the same compendial specifications, but were manufactured by different companies, behaved similarly in promoting tablet dissolution.

Studies of the Utility of Cross Linked Polyvinlpolypyrrolidine as a Tablet Disintegrant

Studies of different particle size grades of cross linked polyvinylpolypyrrolidone (Polyplasdone G.A.F. Corporation) In direct compression tablet formulations show that Increase in mean particle size enhances powder flow, disintegration and dissolution although hardness and friability were slightly better for tablets made from the finer grades. The disintegrant exhibits powerful disintegrant action at low concentrations. It should probably be rarely, if ever, necessary to use more than five per cent in a tablet in order to achieve rapid dissolution. It appears that the use of polyvinylpolypyrrolidone (P.V.P.P.) as a tablet disintegrant at high concentrations may be self limiting since certain properties such as powder flow, tablet weight variation, hardness and friability start to reach unacceptable levels at high disintegrant concentrations. Data presented in this paper indicates that tablets con-taining acetylsalicylic acid or multi-vitamins can be very effec-tively formulated using P.V.P.P. as a disintegrant.

Effect of Variation in Compaction Force on Properties of Six Direct Compression Tablet Formulations

The effect of variation in compaction force on six direct compression tablet matrixes was investigated. An instrumented tablet press allowed direct measurement of applied and ejection forces. Hardness, apparent tablet density, and disintegration times also were determined. The disintegration time of spray-dried lactose tablets was essentially independent of compaction force. However, in the other systems investigated, the properties studied showed varying types of dependence on compaction pressure. A direct compression formula was developed and exhibits a decrease in disintegration time as compaction force is increased.

Formulation of Griseofulvin Tablets

AbstractDifficulties in the formulation of griseofulvin tablets are reviewed. A number of griseofulvin direct compression, pre-compression and polyvinylpyrrolidone granulated tablet formulation have been successfully produced and evaluated, in all cases a mixture of dicalcium phosphate dihydrate and calcium phosphato-carbonate complex was used as tablet matrix. Attempts to use other direct compression tablet matrices proved unsuccessful. The tablets produced have been compared with two commercially available products and the data obtained indicated that the formulations developed in this study have potential for further exploitation.