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Physicochemical properties of powdered medicine substances

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СATALOGUE / TECHNOLOGIES AND EQUIPMENT FOR THE PRODUCTION OF POWDERS / Physicochemical properties of powdered medicine substances

Physicochemical properties of powdered medicine substances

Particle shape and size. Pharmaceutical substances are polydisperse powders, have a complex shape and usually have a significant roughness. Powdered medicine substances (substances) are systems that have particles of various shapes and sizes. In many medicine substances, the particles are anisodiametric (asymmetric, different axes). They may be elongated (sticks, needles) or lamellar (laminae, scales, leaflets). The smaller part of powdery substances has particles isodiametric (symmetric, equiaxed) – these are spherical formations. For example, in JSC “Chemical-Pharmaceutical Combine “AKRIHIN” studies of substance samples were conducted, which showed that the whole variety of their crystals’ shapes in plane projection can be reduced to several geometrical figures, such as spheres, flat plates (practically having no thickness), volume plates, sticks, needles and prisms.
It should be noted that some powders may contain crystals of different shapes and their fragments: for example, acyclovir substance along with plate-shaped particles has fractions in the form of sticks and prisms, a nq-powder of loratadine contains particles in the form of sticks, plates and polyhedrons of rounded shape. All studied powders were divided into six groups according to the shape of particles of the main fraction. It is accepted that the dominant fractions have the greatest influence on the technological properties of powders, so a strict characterization of linear size and shape is necessary for these fractions.

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  • Information updated : 09 / 07 / 2024
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  • Manufacturer : 1 year for Physicochemical properties of powdered medicine substances

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Visually, the tendency of the surface of powders to wet with water is manifested by: full wetting, in which water completely spreads over the surface of the powder; partial wetting, in which water partially spreads over the surface; full non-wetting, in which a drop of water does not spread, maintaining a shape close to spherical. Hydrophobic (non-wettable by water) substances can be well wetted by other liquids, such as organic solvents. Wettability of medicine substances is important in predicting tablet disintegration. Tablets obtained by pressing well-wetted substances with water easily penetrate water, which accelerates tablet disintegration.
Hygroscopicity is the property of some substances to absorb water vapor from the air. If a powdered mass prepared for tabletting is hygroscopic, it will begin to absorb vapors from the air and dissolve in the absorbed water. If the substance is highly hygroscopic, it predetermines the use of auxiliary substances – moisture stimulants.
Crystallization water – water involved in salt composition during its crystallization (water contained in crystals, being in connection with molecules of substance in strictly defined quantities). Crystallization water molecules determine mechanical (strength, plasticity) and thermal (relation to the temperature of the medium) properties of the crystal and have a significant influence on the behavior of the crystal under pressure. The phenomenon of “cementation” is also closely related to the presence of crystallization water in tableted substances.

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Technical specifications

The size of substance particles determines the choice of tablet production technology, the method and equipment for granulation, the strength and density of the obtained granules and, accordingly, the mechanical properties of the tablets themselves, their disintegration and dissolution. For example, in JSC “Chemical-Pharmaceutical Combine “AKRIHIN” as a result of research of a large number of preparations the practical material confirming the influence of the shape and size of crystals of substances on the parameters of the technological process of obtaining tablet masses and modes of their pressing was obtained. For example, for production of aminalon core tablets only fine crystalline substance is necessary, and aminalon crystals of 500-1000 microns in size give unstable, loose tablets. Tablet dosage form of carbamazepine of proper quality by fluidized bed granulation method can be obtained from micronized substance (up to 20 μm), and by conventional wet granulation method – only from powder with particle size from 50 to 300 μm. To obtain acyclovir tablets with a high dissolution index, the particle size of the substance is standardized – not more than 50 microns. It was also found that glibenclamide tablets have good dissolution indexes only when micronized powder is used.
Especially noticeable is the influence of the shape and particle size of substances on the technological characteristics of tablet mass intended for direct pressing.
It is known that only substances belonging to the cubic system are pressed into tablets directly, i.e. by direct pressing, without granulation and auxiliary substances.

Additional information

The more complex the powder surface, the greater the adhesion and lesser the friability, and vice versa. Since direct pressing is increasingly being introduced into pharmaceutical production due to its clear economic advantages and the emergence of modern high-speed tablet presses with high pressing forces, research aimed at studying and normalizing the technological and rheological parameters of tablet mixtures, as well as their constituents, i.e. active and excipients, is particularly relevant. These studies are especially in demand nowadays, when the number of firms-suppliers of medicine substances has increased dramatically, which often differ significantly from series to series in their physicochemical and technological parameters. Specific surface area is the surface area of a solid substance (powder) referred to the unit of mass or volume. If the substance has a porous structure, the total area of all its pores is taken into account.
Contact surface – surface formed when powder particles come into contact with each other. True density is the limit of the medicine mass to volume ratio at zero powder porosity. Wettability is the ability of powdered medicine substances to interact with various liquids (lyophilicity), and above all with water (hydrophilicity). The surface of solid particles of medicine substances contains a certain number of hydrophilic groups (OH, -SON, etc.) or oxygen atoms, which are structural elements of their crystal lattice, so the wettability of the surface of powders has a different value depending on the intensity of interaction of intermolecular forces.

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