Substantiation of the choice of excipients when developing the composition of “Apised” capsules

O. S. Shpychak, O. I. Tikhonov

Abstract


The aim of this work is to substantiate the qualitative composition and quantitative content of excipients; it will allow to provide optimal properties of the mass for capsulation when producing “Apised” capsules – a new original medicine developed on the basis of the standardized substance of natural powder-like honey and the medicinal plant raw material (the herb of garden balm, the cones of hop, the inflorescences of spike lavender). The results of the study of pharmaceutical and technological properties of active substances and their mixture have shown that it is impossible to obtain the mass for capsulation with satisfactory values of flowability and ability to settle without additional introduction of excipients. Antifriction substances were added to the mixture of active substances to improve these parameters. It has been found that addition of aerosil or its mixture with calcium stearate (3:1) in the amount of 2% is the most expedient for improvement of flowability of the mixture of active substances. To reduce ability to settle and prevent stratification of the mixture we have suggested to carry out pre-granulation of the mixture of active substances. Starch (in the form of 5% solution) and polyvinylpyrrolidone, Plasdone K29/32 and Plasdone S629 in different amounts were used as wetting agents. The best values of flowability have been obtained when using Plasdone K29/32 in the amount of 5%; at the same time ability to settle achieve acceptable values and the disintegration time of granules does not exceed acceptable limits. The optimal procedure of preparation of the mass for capsulation has been grounded: 5% Plasdone K29/32 solution is added to the mixture of the medicinal plant raw material, and granulation is carried out, then natural powder-like honey (NPH) and antiantifriction substances (aerosil or its mixture with calcium stearate (3:1)) are added to the granulate obtained. It is recommended to use in future when developing the technology of “Apised” capsules. The absence of necessity of adding humidity regulators into the composition of the mass for capsulation has been shown. The complex of the pharmaceutical and technological research conducted has allowed to substantiate the qualitative composition and quantitative content of excipients in the composition of the mass for capsulation under the conditions of pharmacy and industrial production of “Apised” capsules developed, as well as the procedure of obtaining the mass for capsulation.


Keywords


hard gelatin capsules; excipients; natural powder-like honey; medicinal plant raw material; pharmaceutical and technological properties

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DOI: https://doi.org/10.24959/88954

Abbreviated key title: Vìsn. farm.

ISSN 2415-8844 (Online), ISSN 1562-7241 (Print)