Preservatives Preservatives are used in pharmaceutical chemistry to prevent the growth of bacteria, mold and other microbes.

They are used in the manufacture of pharmaceutical drugs and cosmetics, for their individual antibacterial (destroying and inhibiting the growth of bacteria) and antifungal (destroying and inhibiting the growth of fungus) properties.[1] Classification of preservatives Preservatives are classified into two main classes: antimicrobial preservatives and antioxidants.[2][3] Antimicrobial preservatives Antimicrobial preservatives are included in the preparations to kill or to inhibit the growth of microorganisms inadvertently introduced during manufacture or use. They are used in sterile preparations such as eye drops and multidose injections to maintain sterility during use. They may be also added to aqueous injections that cannot be sterilized in their final containers and have to be prepared using aseptic precautions. Preservatives are also used in cosmetics, foods, and non sterile pharmaceutical products such as oral liquids and creams to prevent microbial spoilage.[4] Antimicrobial preservatives are classified into two main subgroups: anti-fungal preservatives and anti-bacterial preservatives. Anti-fungal preservatives include compounds such as benzoic and ascorbic acids and their salts, and phenolic compounds such as methyl, ethyl, propyl and butyl phydroxybenzoate (parabens). Antibacterial preservatives include compounds such as quaternary ammonium salts, alcohols, phenols, mercurials and biguanidines.[3]

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Table 1: Antimicrobial preservatives.[2] Use of some antimicrobial preservatives Benzoic Acid: Benzoic acid (C7H6O2) is used as a pharmaceutical preservative for its antifungal properties. Benzoic acid and its salts inhibit the growth of bacteria, yeast and mold. It is used in chemically based ointments to treat fungal diseases, such as athlete's foot, ringworm and tinea. A 0.1 percent concentration of benzoic acid is used in pharmaceutical applications. It is used as an antiseptic in mouthwashes and lotions.[1] Ethyl paraben: Ethyl paraben or ethyl para-hydroxybenzoate, is an antimicrobial preservative most commonly used in cosmetics and pharmaceutical formulations. It is an antifungal agent and found as a white crystalline powder. Ethyl paraben is used as a stand-alone agent or in combination with other antimicrobials and parabens. It is ineffective against molds and yeasts.[1] Methyl paraben: Methylparaben, also methyl paraben is a preservative. It is an anti-fungal agent often used in a variety of cosmetics and personal-care products. It is readily absorbed from the gastrointestinal tract or through the skin. It does not accumulate in the body. Acute toxicity studies have shown that methylparaben is practically non-toxic by both oral and parenteral administration in animals. Studies indicate that methylparaben applied on the skin may react with UVB, leading to increased skin aging and DNA damage. [8] Butyl paraben: Butyl paraben combats mold, fungus and bacteria in pharmaceuticals, cosmetics, food and other products. It has been shown to be non-toxic when used as .05 percent of a solution, but if a stronger solution is used it can irritate the skin. Exposure to butyl paraben also adversely affects the male reproductive system as well as the production of testosterone, the principal male sex hormone.[6] Antioxidants Antioxidants are included in the pharmaceutical products to prevent deterioration from oxidation. Antioxidants are classified into 3 groups. The first group is known as true antioxidants, or antioxygen, probably inhibit oxidation by reacting with free radicals blocking the chain reaction. Examples are alkygallates butylated hydroxyanisol, butylated hydroxytoluene, nordihydroguaiaretic acid and the tocopherols. The second group consists of reducing agents; these substances have lower redox potentials than the drug or adjuvant which they are intended to protect, and are therefore, more readily oxidized. Reducing agents may act also by reacting with free radicals. Examples are ascorbic acid, the potassium and sodium salts of sulphurous acid. The third group consists of antioxidant synergists which usually have little antioxidant effect themselves but probably enhance the action of antioxidants in the first group by reacting
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with heavy metal ions which catalyze oxidation. Example of antioxidant synergists are citric acid, editic acid and its salts, lecithin and tartaric acid.[7][8]

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Table 2: Antioxidants.[2] Use of some antioxidants TPGS: D-α-tocopherol acid polyethylene glycol 1000 succinate (TPGS) is a light yellow to yellow waxy solid. The active ingredient, vitamin E succinate, is derived from natural sources, i.e. from edible vegetable oils, and is produced by suitable physical and chemical means. and it is a water-soluble derivative of vitamin E that can directly enhance the bioavailability of poorly soluble drugs. TPGS is commonly used in pharmaceutical formulations including anti-HIV medications and anti-cancer drugs, and is also used in ethical, prescription-free pharmaceutical formulations as well as dietary supplements. [1]
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Monothioglycerol : Monothioglycerol is used as an antioxidant in pharmaceutical formulations, mainly in parenteral preparations. Monothiogly-cerol is reported to have some antimicrobial activity. Therapeutically, monothioglycerol has been used in a 0.02%w/w aqueous solution to stimulate wound healing, and as a 0.1% w/w jelly in atrophic rhinitis. Monothioglycerol is generally regarded as a relatively nontoxic and nonirritant material. It is used in topical and injectable preparations. Undiluted monothioglycerol is considered a poison by the IP and IV routes; it has also been reported to be mutagenic. [9] Ascobyl Palmitate: Ascobyl Palmitate is a fat (oil) soluble form of vitamin C. It is used as an antioxidant and preservative in foods, vitamins, drugs and cosmetics. Ascorbyl palmitate protects fats from peroxidation, and can be stored in the body in small amounts. Ascorbyl palmitate acts synergistically with other antioxidants such as vitamin to boost immunity in our bodies. [9] Butylated hydroxyanisole (BHA): BHA is used as a preservative and antioxidant in pharmaceutical preparations. The US National Institutes of Health report that BHA is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in experimental animals. When examining human population statistics, the usual low intake levels of BHA shows no significant association with an increased risk of cancer.[9] Propyl gallate: Propyl gallate has become widely used as an antioxidant in cosmetics, perfumes, foods, and pharmaceuticals. It is primarily used, in concentrations up to 0.1% w/v, to prevent the rancidity of oils and fats; it may also be used at concentrations of 0.002% w/v to prevent peroxide formation in ether, and at 0.01% w/v to prevent the oxidation of paraldehyde. Synergistic effects with other antioxidants such as butylated hydroxyanisole and butylated. Studies have shown that, when added to powder blends containing ketorolac, propyl gallate significantly increases the drug stability in the preparation.[9]

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Referencing 1. Gilani, N. (2012) „Types of Preservatives in Pharmaceutical Chemistry.‟ eHow 2. Fahelelbom, K. M.S. (2012) „Analysis of preservatives in pharmaceutical products.‟ Pharmainfo.net 3. K. Parfitt, “Martindale: The Complete Drug Reference” 32 nd Ed., Pharmaceutical Press, Massachusts (1999). 4. Hang, H., Y., Lai, Y., C., Chiu, C., W., Yeh, J., M., and Chromatogr, J. 993 , 153 (2003). 5. W. J. Reilly, "Pharmaceutical Necessities", in: "Remington: The Science and Practice of Pharmacy", 20th Ed., Edited by A. R. Gennaro, Mack Publishing Comp., Philadelphia (2000). 6. Chemical Preservatives in Medicines-Chemical Preservatives In Medicines Manufacturer. Accessed at: http://www.alibaba.com/showroom/chemical-preservatives-in-medicines.html 7. D. M. Johnson, and L. C. Gu, "Encyclopedia of Pharmaceutical Technology", edited by J. Swarbick, and J. C. Boylan, Marcel Dekker, Inc., New York , (1988).

8. A. Wade, and P. Willer, “Handbook of Pharmaceutical Excipints”, Am. Pharm. Assoc., Washington. (1994). 9. Rowe, R. C., Sheskey, P., J. and Quinn, M., E. (2006) „Handbook of pharmaceutical excipients‟ 6th edn. Chicago: Pharmaceutical press

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