Mineral excipients

Transdermal delivery of certain APIs is now common for the treatment of some medical conditions, and there are several excipients that are promoted as transdermal penetration enhancers. One of the earlier materials developed was laurocapram (Azone ). There is a detrimental interaction between laurocapram and mineral oil (liquid paraffin) whereby when both are included in the same formulation, the skin penetration-enhancing properties of laurocapram are lost. Such interactions have implications for extemporaneous mixing of different cream and ointment formulations in the pharmacy. 

Excipients are produced by a diverse group of manufacturers who range from pharmaceutical companies to specialty chemical manufacturers, food producers, and even mineral quarries. These manufacturers are involved in a diverse range of chemical processing and usually produce excipients as a small component of their product mix. 

Mineral product companies also provide excipients to the industry. Such companies may produce these inorganic chemicals by quarrying rock and separating the desired chemical entity such as talc, sodium chloride, or sodium carbonate. Alternatively sometimes the inorganic excipient is produced synthetically. The market for excipient grade minerals is dwarfed by other applications for these products in the industrial market. 

For the purposes of this guidance, natural product refers to materials (e.g., drug substance, excipients) that are derived from plants, animals, or microorganisms. The specific recommendations for natural products are not applicable to inorganic compounds (e.g., salts, minerals). 

Microcrystalline cellulose (Avicel) is purified partially depolymerized cellulose, prepared by treating a-cellulose with mineral acids. In addition to being used as a filler, it is also used as dry binder and disintegrant in tablet formulations. Depending on the preparation conditions, it can be produced with a variety of technical specifications depending on particle size and crystallinity. It is often used as an excipient in direct compression formulations but can also be incorporated as a diluent for tablets prepared by wet granulation, as a filler for capsules and for the production of spheres. 

The areas of pharmacopeial standards most frequently cited at those meetings as in need of harmonization were pharmaceutical excipients and analytical tests and assays. Excipients posed the greatest barrier to commerce as a result of a patchwork of standards in the USP, EP, and JP for a small universe of substances and many natural products of animal, mineral, and vegetable origin that are shared throughout the world. Standards for these common substances reflect cultural, scientific, and temporal differences in how... 

Kumar, A. Aitas, A.T. Hunter, A.G. Beaman, D.C. Sweeteners, dyes and other excipients in vitamin and mineral preparations. Clin. Pediatr. 1996, 35 (9),... 

Esophageal obstruction may occur if methylcellulose is swallowed with an insufficient quantity of liquid. Consumption of large quantities of methylcellulose may additionally interfere with the normal absorption of some minerals. However, this and the other adverse effects discussed above relate mainly to the use of methylcellulose as a bulk laxative and are not significant factors when methylcellulose is used as an excipient in oral preparations. 

Mineral oil is used primarily as an excipient in topical pharmaceutical formulations, where its emollient properties are exploited as an ingredient in ointment bases see Table I. It is additionally used in oil-in-water emulsions,as a solvent, and as a lubricant in capsule and tablet formulations, and to a limited extent as a mold-release agent for cocoa butter suppositories. It has also been used in the preparation of microspheres. " ... 

Mineral oil is used as an excipient in a wide variety of pharmaceutical formulations see Section 16. It is also used in cosmetics and in some food products. 

Excipients are inactive ingredients in drugs and vitamin and mineral preparations. These compounds are considered to be inert, not affecting the intended functioning of the active ingredients. Excipients, which frequently constitute the majority of the mass or volume of oral preparations, have a variety of purposes that include... 

Many excipients have been associated with adverse reactions in those ingesting drugs and vitamin/mineral formulations containing these compoundsJ78 79 Antioxidants (e.g., sodium sulfite, sodium and potassium bisulfites, and metabisulfites), bacterial preservatives (e.g., benzyl alcohol and benzalkonium chloride), artificial sweeteners (e.g., aspartame and saccharine), coloring agents (e.g., FD C yellow 5, blue 2, and red 40), and propylene glycol. A few examples of the toxic effects of these follow. 

Material Fine/medium powder Fly ash, pulverized coal, plastic powders, alumina, granular sugar, pharma excipients Course powder Sand, salt, granules, mineral powders, glass beads Cohesive fine powder Cement, corn starch, tit anium dioxide, carbon-black powder, many pharma actives Granular Plastic pellets, wheat, large glass beads, tablets, course sand, seeds... 

Actions and Uses.—Internally —Cathartic and diuretic, but chiefly employed as an antacid, as an antidote to poisoning by the mineral acids, and in the preparation of clysters. Externally —Stimulant to sprains and contusions also applied to burns and scalds to diminish the irritation and pain by excluding air. Likewise employed as an excipient in making up boluses, liniments, and oint-... 

The bentonite excipient in the aminosalicylic acid granules adsorbs the rifampicin onto its surface so that much less is available for absorption, which results in reduced serum levels. Bentonite is a naturally occurring mineral (montmorillonite) consisting largely of hydrate aluminium silicate, and is similar to kaolin. 

The use of crystalline nanoparticles of cellulose (CNP) allows for paving a new path for the development of nanocosmetics. The CNP for cosmetics application can be produced by hydrolysis of pure cotton cellulose with mineral acids as was described in Section 9.3.1. The paste of CNP for cosmetic application was obtained by evaporation of dilute aqueous dispersion. The powder of CNP was prepared by freeze-drying of the aqueous dispersion. Testing has shown that the obtained powder of CNP meets requirements of the US pharmacopeia 23/NF 18 for inactive medical excipients (Table 9.13). 

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