Granule formulations

Product bioavailability is mentioned, especially where it is low. Where there are differences between the formulations tested for bioavailability during the development process and the formulation to be marketed, there is considerable discussion of the data provided on the bioequivalence of the different products and/or formulations. This is particularly so where, for example, early clinical studies were undertaken with capsules but the marketed dosage form is to be a tablet. Bioequivalence data and pharmacokinetic data (e.g., in crossover studies) and comparative dissolution studies are usually reported. This is particularly significant where the different strengths of the final products are not achieved by using different quantities of the same granulate formulation. Process optimization may also be addressed in such cases. 

Water-dispersible granule formulation is considered to be the first commercial formulation enabling storage of S. carpocapsae for 6 months at 25°C at a concentration of over 300,000 infective juveniles per gram (Grewal 2000). When stored at... 

The samples from the plot receiving the granulated formulation (Table I) revealed a different situation. The overall variability was much larger with a coefficient of variation of 395, with increased variability both between and within the five samples. Analysis of variance gave components of 140 between field samples, and 264 between laboratory subsamples. Since the analytical procedures were identical with those used in the EC plot samples, where reproducibility was good, these results clearly indicate a much greater irregularity of the distribution of the herbicide in... 

With dosage form design, it is often necessary to compare the performance of two different granule formulations. These two formulations differ in composition and, as a consequence, vary also in the amount of granulating liquid required. 

In Figure 4, data from a low dose wet granulation formulation produced in production on a Courtoy R100/36 is compared to the Presster tablet hardness data. The force-hardness data from the two machines was comparable. 

For the wet granulation formulation, 2.12% Glucidex 2B (Roquette) was added as binder. 

Boydston, R.A. (1992). Controlled release starch granule formulations reduce herbicide leaching in soil columns. Weed Technol., 6 317-321. 

This chapter focuses on the use of fluidized bed granulation process in the development and preparation of low-dose granule formulations for further conversion to immediate release tablets for personal administration. As a reference document, the chapter does not cover some very common subjects such as process safety, material characterization techniques and basic process and instrumentation technologies. Because the authors intention is to relate their experience in this specialized area, these areas are not discussed in any depth however their omission does not reduce their importance. 

Through appropriate formulation and manufacturing selection, Drugs A and B were designed into dry granulated formulations that achieved chemical and physical stability. The formulations were designed as stable, commercially viable drug products, and therefore did not require additional external controls. 

TABLE 6.6 Physical and Mechanical Properties of the Drug and Diluents Used in the Low-Dose Dry Granulation Formulations... 

Figure 12.1 Characterization of changes occurring during drying of a wet granulated formulation. The top trace is of lactose monohydrate. The middle three are of the formulation composed of a mixture of hydrated and anhydrous lactose, as well as the drug at 15, 60, and 120 min (top to bottom). The lower trace shows a diffraction pattern of anhydrous lactose.

Van der Merwe, Verhoef, J.C., Kotze, A.F. and Junginger, H.E. (2004b) A-Trimethyl chitosan chloride as absorption enhancer in oral peptide drug delivery. Development and characterization of minitablet and granule formulations. Eur. J. Pharm. Biopharm. 57 85-91. 

This spring Elanco Products Company (a Division of Eli Lilly and Company) introduced a 60 /o dry flowable (or water dispersible granule) formulation of BALAN. BALAN is a preemergence, dinitroaniline herbicide used on peanuts and lettuce. BALAN Dry Flowable is an addition to formulations of BALAN which are produced and sold by Elanco. BALAN LC, a 1.5 Ib/gal emulsifiable concentrate which has been on the market for several years, is often tank mixed with several other agrichemicals. Therefore, it was critical to evaluate this new product form for tank mix performance with all agrichemicals with which it could be tank mixed. 

A water-dispersible granule formulation contains typically a toxicant (50%-95%, w/w), dispersant, binder, and diluent. This formulation, also known as dry flowable, is intended for application after disintegration and dispersion in water by conventional spraying equipment. WGs are easier to use than WPs, because they have low-dust properties (due to larger particles) and exhibit good flowability. 

The amount of exposure for a body part is a PHED-based distribution depending on the body part and the type of user, as well as the type of herbicide formulation used. The latter can be granule formulations (used only by home-owners using atrazine for residential lawn care), flowable formulations (FFs) (which are among the formulations classified as emulsifiable concentrates (ECs) in PHED) and water-dispersible granules (WDGs). 

Figure 8.6 Distributions of the margins of exposure for atrazine from herbicide handhng with water-dispersible-granule formulations for different-use populations in the USA...

Fignres 8.9 and 8.10 indicate the distributions of the MOEs in the atrazine handling population involved in com production and each of its subpopulations for the flowable and water-dispersible-granule formulations, respectively. 

Table 8.1 Margin-of-exposure assessment for US herbicide handlers using flowable or water-dispersible-granule formulations of atrazine or simazine and including drinking water and dietary exposures to atrazine and simazine combined ...

With diquat Actor, Preeglone, Preglone, Priglone, Weedol (a 2.5% soluble granule formulation). 

Endothermic Fusion Vaporization Sublimation Desorption Desolvation Melting of drug substances purity evaluations Evaporation of liquid or semisolid excipients Removal of frozen water during lyophilization Drying of wet granulated formulations Removal of stoichiometric water from crystalline hydrates... 

Fig. 7 Influence of drug loading levels on theophylline release properties of the tablets containing hot-melt extruded granules (n — 3). Tablets 20%, 300-425 pm extruded granules (Formule 1-4 theophylline, 2% PEG and PVAc qs to 100%), 79.5% Avicel PH 200, and 0.5% magnesium stearate. (4) 5% loading ( ) 15% loading (a) 25% loading (O) 50% loading. (Prom Ref l)...

Citric acid is used in effervescing mixtures and granules. Formulations that contain citric acid are used in the management of dry mouth and to dissolve renal calculi, alkalinize the urine, and prevent encrustation of urinary catheters. Citric acid is also an ingredient of citrated anticoagulant solutions. 

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