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Topical Agents 3rd Year Pharmacy 2016 - 2017 Outline Classification a- protective b- antimicrobial • agents A- protective products • Talc , Zinc oxide ZnO, Calamine, Titinum oxide • TiO2, Al products& silicon polymer Antimicrobials • Mechanism 1-oxidation H2O2,ZnO,KMnO4, Iodine • 2- Halogenations NaOCl • 3- protein ppt AgNO3. • Protective Agents Protective • Any agent that isolates the exposed • surface from harmful or annoying stimuli Properties of protective agents: • Insoluble in water • Chemical Inertness Adsorbent Deeper penetration of topical agents are also • seen in many cases which are beneficial. (Penetration of antiseptics into the tissue deeper of possibility the prevents skin the below • -)infections • Protective Agents Talc Talc (Mg3Si4O10(OH)2 • protective: native hydrous magnesium silicate, • common name and chemical formula. Soapstone can be grinding in 80/100 mesh • particle size. As grease touch., insoluble in water, • Uses as protective agents , as lubricants and • in pharmaceuticals, as cosmetics, ceramics, for plastic cloves, Zinc Oxide ( ZnO ) White or fait yellow color powder, insoluble in • water. Other formulation as Zinc Oxide ointment for adult, & Zinc Oxide in Glycerin for children. Dusting powder, used astringent and protective • topical agent, mild antiseptic, used in the acne preparation, eczema,& psoriasis It is usually used in the manufacture of • plasters. Calamine ZnO and Fe2O3 It used as dusting powder, lotions, • ointments, as smoothing agents, for sunburn, eczema, urticaria. Calamine lotion is very popular. Boric Acid H3BO3 Is a weak acid, used as antiseptic, and as • chemical precursor for many reactions. Uses: • 1- Antiseptic • 2- dilute solution for eye wash • 3-Acne • 4- Vaginal douche against bacteria. • 5-It used as protective against athlete foot. • Titanium dioxide TiO2 Topical protective agents as cream is • used against sunscreen to protect the skin aganist ultra-violet light ( U.V.). The organic topical protective agents is • P-aminobenzoic acid ( PABA) . • Antimicrobial Agents Antiseptic: • Any agent which kills or inhibits the growth of • microorganisms found in living tissue. Disinfectant: • Any agent which kills or inhibits the growth of • microorganisms found in inanimate objects. Germicide: • General term for fungicide, bactericide, • amoebicide Mechanisms of action of antimicrobials There are THREE proposal mechanisms: • 1-Oxidation • 2-Halogenation Protein Precipitation3- Oxidation cell membrane of bacteria SH SH S---S • Halogenation the protein of the cell membrain H2N CHR CO NH CHR1--- • (HOCl) NaOCl H2NCHRCONCl CHR!... Protein pption that kill the microbe H2NCHR1CONHCHR2---- • AgNO3 • H2NCHR1CONHCHR2--- • • Ag • Hydrogen Peroxide H2O2 liquid not store in glass bottles because it • decompose ,it store in white plastic container, keep in cold dark place to prevent decomposition. There are many uses : • 1- Antiseptic for wash wound , teeth and • ear 2-Bleaching color ( hair ). • 3- Laundry for cloths. • Sodium Perborate • :Antimicrobial • Composite of H2O2, NaBO2 and NaOH Used as bleaching agent in non-chlorine laundry bleaches Potassium Permanganate KMnO4 Chemically is a strong oxidizing agent, • solid purple crystalline , odorless. Store in well closed container. • Uses: • 1- Oxidizing agent for skin disease in • different concentrations 1: 5000, 1:15000 2- used in swimming pool for athlete foot. • 3- Strong oxidizing for many organic • reactions. Iodine I2 It is dark violet ,insoluble in water , but the • I2 + KI = I3 – Complex soluble in water as iodine solution, • soluble in alcohol known as tincture iodine Iodine solution weak solution ( 25g I2 + 25g KI ) in 100ml • And strong solution ( 50g I2 + 50g KI ) in 100 ml. • Iodine preparations and compounds • Antimicrobial property due to oxidation and Iodination disinfectants A chemical reagents in analytical reagent. • In drug synthesis. • In Povidin iodine as new product. • • Povidone Iodine ( PVP – I) is a stable chemical complex of poly vinyl • pyrrolidine iodide. It is broad spectrum antiseptic for wounds. It is used disinfectant . 2- Halogenation Dakin's Solution • Sodium hypochlorite solution, (usp) • Contains 4-6% of NaOCl, It is made from bleach that has been • diluted and treated to decrease irritation. Chlorine, the active ingredient in Dakin's solution, is a strong antiseptic that kills .most forms of bacteria and viruses. 3- Protein ppt (Silver Nitrate AgNO3) Prepare as 1% AgNO3 , protective from • light due to oxidation. Effective against gonococcal organism. Antimicrobial activity of these compounds • is due to protein precipitant action. 1% used eye newborn babies. •