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Boris Golman

Publications and source records attributed to Boris Golman.

5 recordsLinked to original sources

Batch grinding kinetics of Ethenzamide particles by fluidized-bed jet-milling.

Ethenzamide solids as a representative active pharmaceutical ingredient (API) were batch-ground by means of a fluidized-bed jet-mill which is a relatively new equipment and promising for production in the pharmaceutical field. Thus, the characteristic grinding mechanism was investigated. As a result, the variation of the residual ratio with grinding time after milling was expressed simply by a mathematical model using only the first Kapur function, and it was consistent with experimental data satisfactorily. As the shape of the function was much different from that of inorganic compound and peculiar to API, a cubic function with respect to particle diameter was defined newly and well fitted to the experimental data. The function was also found to be affected by the operating parameters as the grinding gas pressure, the charge weight of raw material and the linear velocity at the grinding nozzle. According to the assessments of the breakage and the selection functions derived from the first Kapur function, it was found that the grinding mechanism of Ethenzamide particles was related with particle attrition mainly.

Kinetics↗

Dissolution characteristics of cylindrical particles and tablets.

In this paper, dissolution characteristics of primary-particles and compressed tablets were investigated by experiments using a mathematical model. For the primary-particle, it was found that the dissolution rate increased with a decrease in the particle size. Assuming that primary-particles of size distribution were of cylindrical shape and that the dissolution occurs from the total external surface, an extended Nernst-Noyes-Whitney equation fitted to the experimental data well. As the influences of particle size and shape on thickness of a diffusion-boundary film were found to be quite low, the dissolution rate was considered to be affected by the specific surface area dominantly. Furthermore, the same model was applied to a compressed tablet and fitted to the data well. Though the rate constant obtained were not affected by the properties of primary-particles forming the tablet, it was found to increase with the apparent voidage which occupies the inter-particle volume of tablet diluent among less soluble particles. Consequently, an increase in the apparent voidage is presumed to accelerate penetration of water into the internal voids of the tablet. Thus, the dissolution going, the effective surface area inside the tablet is considered to be extended.

Kinetics↗

Effect of particle shape of active pharmaceutical ingredients prepared by fluidized-bed jet-milling on cohesiveness.

Milling is a common procedure to improve bioavailability of many active pharmaceutical ingredients (APIs), which typically have low solubility in water. But such micronization can yield an increase in the cohesiveness of particles. Although particle cohesiveness is desirable for tablet strength in the subsequent formulation process, increased particle cohesiveness can lead to operational difficulties in a milling equipment due to compaction of particles inside. In this article, the impact of milling via a fluidized-bed jet-mill on the cohesive strength and interparticle force was studied using Ethenzamide as a pharmaceutical model compound. As a result, the particle shape was found to affect both the tensile strength of powder bed and the interparticle cohesive force. A powder bed, having relatively high void fraction by direct tensile test, shows a positive correlation between the cohesive force and the particle sphericity, while powders with low void fraction by diametral compression test show a positive correlation between the cohesive force and the angularity of the particle.

Adhesives↗

Variation in particle shape of active pharmaceutical ingredients prepared by fluidized-bed jet-milling.

In pharmaceutical industries, most active pharmaceutical ingredients are poorly water soluble, and therefore milling processes are important to obtain fine particles that can be easily dissolved in the body. However, the main purpose of milling is micronization of particles. From the viewpoint of fine particle preparation in the formulation process, milling has not been investigated sufficiently. In this paper, ethenzamide was milled under various operating conditions using a fluidized-bed jet-mill. It was found that not only the particle size but also the particle shape varied with the milling conditions. The relationship between particle shape and milling conditions has been obtained experimentally.

Particle Size↗

Controlled release with coating layer of permeable particles.

An enhanced method was proposed for controlled release of core material using a coating layer of fine permeable particles dispersed in an impermeable wax prepared by dry-based process. A mathematical model was constructed to describe in detail the core material release by diffusion through the connected permeable particles inside the coating layer. The effective diffusivity was simulated by a random walk method taking into account the structure of the coating layer. The released characteristics were measured for the urea core particle coated with the layer of the starch permeable particles dispersed in the paraffin wax. The calculated results were in a good quantitative agreement with experimental data in all range of coating conditions. As a result, the low release rate was proven to be obtained with thicker coating layer of lower volume fraction of permeable particles. Moreover, the application of permeable particles instead of soluble ones [J. Chem. Eng. Jpn. 35 (2002) 40] resulted in significant decrease in release rate.

Algorithms↗