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Topical Agents Definition • Topical : Place the use of these drugs or compounds on the surface • Ex: Antiseptic • Systemic: The drugs are absorbed into circulatory system and distributed to various organs or tissues. Types of inorganic topical agents • The compounds used topically will be divided into broad categories based on their usual action or uses. • There are TWO types: • 1- Protective agents. • 2- Antimicrobial agents. Protective agents • Are substances which may be applied to skin to protect certain areas from irritation. • Properties of protective agents are insoluble in water ( H2O), and chemically inert ( unreactive), in order to prevent interactions between the protective substance and the tissue. • Also, small fine partials(large surface area). Classification of protective agents • 1- Dusting powders. • 2-Suspensions. • 3- Ointments Talc • MgO.4SiO2.H2O • Hydrous magnesium silicate, very fine white powder, smoothly, greasy feeling to the touch( soapstone). • Talc is characterized as fine powder ( 80/100) mesh particle size, odorless, insoluble in water ,dil HCl, bases. Uses of Talc • 1- It is useful in lubricating, protective dusting, • Can be prevent any friction. • 2-Used for wound & surgical incision because can produce sterile abscesses • 3- Used in medical gloves.( plastic disposable) • 4- Used in cosmetic may be perfumed • Medical Talc by mixing boric acid with talc as antimicrobial agents. Zinc Oxide • The chemical formula for Zinc oxide is ZnO • Is a very fine, oderless, amorphous , white or fait yellow powdwer, can heated 400-500 ∙C • Zno is insoluble in water, alcohol, but react with dil HCl • ZnO + HCl --------- ZnCl2 + H2O Uses of Zinc Oxide • 1- Is a mild astringent and weak antimicrobial agents. Used as powder, ointments to protect the skin. • 2- Dusting powder used in the treatment of skin ulceration & other dermatological problems. • Medicated zinc oxide by mixing with boric acid as antimicrobial agents. Calamine • The formula is ZnO.xFe2O3 • Can be synthesized by mixing ZnO with ferric oxide. • It is a fine powder, water insoluble, alcohols ,adhering to the skin. Uses of Calamine • Calamine can be used as topical protective agent. • 1- It is USP product used as dust powder, calamine lotion ( applied to skin )pink color. • Calamine is applied to the skin for its adsorbent, protective properties, used in dermatological problems. • The calamine lotion contain ZnO and ferric oxide equally mixed Bentonite magma in the solution of Calcium hydroxide. • Phenolated calamine lotion( USP ) contains 1% liquid which provide a local anesthetic and anti- itching action. Titanium Dioxide • TiO2 as topical protective agent, it is characterized by off white powder color, tasteless, odorless. A 1 to 10 aqueous suspension of the solution is neutral to litmus paper. • It is insoluble in water , HCl. HNO3, dil H2SO4. • It is soluble in HF, Conc. H2SO4.Also, in H2O2 • TiO2 + H2O2 -------• Tritium dioxide TiO3 Titanium trioxide Uses of TiO2 • TiO2 is a protective agent, topically, used as Sun screen light ( UV light radiation) due to its highly refractive index. • Many pharmaceutical preparation as TiO2 cream, 5, 10, ..25% ointments. • Other organic sun screen agent p- aminobenzoic acid ( PABA). • TiO2 used in cosmetic and paints. Aluminum • Aluminum ( Al ) is a silver- white metal as protective agents , highly affinity to O2 forming Al2O3as protective layer. • It is insoluble in water, alcohols, and uncreative towards HNO3,H2SO4 • It react rapidly with dil HCl • HCl + Al ------ AlCl3. 6H2O • Aluminum, paste ( ZnO with base ) used for prevent irritation. Silicon Polymer • There are inert protective substances occurring in liquid form known as Silicon oils; e.g.dimethyl silicon ( Dimethicon,or Simethicone ) • CH3 CH3 CH3 • CH3 Si-O- ( - Si - O ) ------Si - CH3 • CH3 CH3 CH3 • Very well adhere to skin, but not wound, be avoided contact to the eyes. 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 • below the skin prevents the possibility of deeper in fections-) • 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.