topical agents inorganic chemistry b. ph sem 1

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TOPICAL AGENTS Dr. Nihar Shah Assistant Professor Dept. of Pharmaceutical Technology L. J Institute of Pharmacy Email add.: [email protected] M. No.: 9998691597

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Page 1: Topical agents   inorganic chemistry b. ph sem 1

TOPICAL AGENTS

Dr. Nihar ShahAssistant ProfessorDept. of Pharmaceutical TechnologyL. J Institute of PharmacyEmail add.: [email protected]. No.: 9998691597

Page 2: Topical agents   inorganic chemistry b. ph sem 1

PROTECTIVE AND ADSORBENTS ACTIVATED CHARCOAL

Test for Purity Acidity or alkalinity Acid- soluble substances Ethanol-soluble substances Alkali-soluble colored matter Chloride Sulphate Sulphide Uncarbonised constituents Copper Lead Zinc Sulphated ash Loss on drying Adsorbing power

Page 3: Topical agents   inorganic chemistry b. ph sem 1

ACTIVATED CHARCOAL

Storage: Store in well closed containers. Medicinal and Pharmaceutical Uses: Adsorbent. Charcoal is of great value in the

purification of chemicals and the adsorption of gases.

Page 4: Topical agents   inorganic chemistry b. ph sem 1

TALC (TALCUM, FRENCH CHALK, PURIFIED TALC) 3MgO, 4SiO2, H2O Test for Purity Acidity or alkalinity Water-Soluble substances Acid-Soluble substances Iron Carbonates Loss on drying Organic compounds Chloride

Page 5: Topical agents   inorganic chemistry b. ph sem 1

TALC (TALCUM, FRENCH CHALK, PURIFIED TALC) Storage: Talc is an inert substance not affected by acids or bases

or other chemicals. So store in a well closed container. Medicinal and pharmaceutical Uses: Pharmaceutical aid (dusting powder). It is used as a

filtering and distributing medium in the preparation of aromatic waters etc. it is the main ingredient in talcum powders and dusting powders

Page 6: Topical agents   inorganic chemistry b. ph sem 1

ZINC OXIDE,ZNO Preparation Zinc oxide is prepared on a large scale by burning

zinc metal in a current of air. Zn + O2 = 2ZnO

In this method, Zinc carbonate is prepared first by reacting zinc sulphate with a boiling solution of sodium carbonate. The precipitated basic carbonate of zinc is collected, washed to remove sulphate, dried and finally gently ignited. It loses carbon dioxide and water, leaving zinc oxide as the residue 2ZnCO3,2Zn(OH)2= 4ZnO + 2CO2 + 2H2O Basic Zinc carbonate.

Page 7: Topical agents   inorganic chemistry b. ph sem 1

ZINC OXIDE,ZNO Assay: The sample is dissolved in 2M acetic acid and diluted with water.

Xylenol orange titrurate and sufficient hexamine to produce violet pink colour are added. A further quantity of hexamine is added and titrated with 0.1M disodium edetate until the solution becomes yellow.

In this complexometric titration hexamine is added to raise the pH to the alkaline side and the zinc oxide converted to zinc acetate by dissolving in acetic acid and titrated with 0.1M disodium edetate using xylenol orange as indicator. Zinc is complexed by the disodium edetate and the indicator changes colour from violet-pink to yellow at the end point.

Page 8: Topical agents   inorganic chemistry b. ph sem 1

ZINC OXIDE,ZNO Test for Purity Alkalinity Carbonates and substances insoluble in acids. Arsenic Iron Lead Loss or ignition Storage: Since it absorbs carbon dioxide from the air, store it in a well closed

container. Medicinal Use: Astrigent and topical protective. Zonic oxide is a mild antiseptic and

astringent. In the form of zinc oxide ointment or dusting powder, it is used in the treatment of eczema, ringworm, pruritus and psoriasis. It is also widely used in the manufacture of plasters.

Page 9: Topical agents   inorganic chemistry b. ph sem 1

ZINC OXIDE,ZNO Zinc Oxide Paste Zinc Oxide: 250 gm Starch: 250 gm White Soft Paraffin: 500 gm

Zinc Oxide Ointment Zinc Gelaitn

Page 10: Topical agents   inorganic chemistry b. ph sem 1

ZINC STEARATE, (C17H35COO)2ZN Zinc stearate is mixture of Zinc salts obtained from commercial stearic acid

which itself is prepared from the hydrolysis of fats. It consists mainly of variable proportions of Zinc stearate and Zinc palmitate.

Test for Purity Acidity or alkalinity Alkalis and alkaline earths Chloride Arsenic Heavy metals Sulphate Storage: Store in well closed containers. Medicinal and Pharmaceutical Uses: Dusting powder. Since zinc stearate is a mild antiseptic and astringent, it is

used in the form of dusting powder or ointment in several skin conditions. Sometimes it is used as solid diluents.

Page 11: Topical agents   inorganic chemistry b. ph sem 1

CALAMINE According to B.P. calamine is basic Zinc carbonate

suitably coloured with ferric oxide. According to the I.P. Calamine is Zinc oxide coloured with Ferric oxide. It is an amorphous , reddish brown powder and the colour depends on the variety and amount of ferric oxide present and the method by which it is incorporated. It is practically insoluble in water and completely soluble in mineral acids. Since there is a possibility of adulteration with dyes, there are tests for water soluble dyes and alcohol soluble dyes.

Page 12: Topical agents   inorganic chemistry b. ph sem 1

CALAMINE Test for Purity Acid-insoluble substances Alkaline substances Arsenic Calcium Lead Water-soluble dyes Alcohol-soluble dyes Loss on ignition

Storage: Store in well closed containers. Medicinal and Pharmaceutical Uses: Topical protective. Widely used in lotions, ointments and dusting powders as

asoothing agent. It is used in sunburns, eczema and urticaria and some other skin conditions. Calamine lotion (Lotio Calaminae) is very popular.

Page 13: Topical agents   inorganic chemistry b. ph sem 1

CALAMINE Calamine Lotion Calamine: 150 gm Zinc Oxide: 50 gm Bentonite: 30 gm Sodium Citrate: 5 gm Liquefied Phenol: 5 ml Glycerine: 50 ml Rose Water: 1000 ml Calamie Cream Calamine Ointment

Page 14: Topical agents   inorganic chemistry b. ph sem 1

TITANIUM DIOXIDE, TIO2 Titanium dioxide occurs in nature in the mineral rutile, brookite

and ilmenite. Magnetic iron ores usually contain titanium. Preparation: Titanium dioxide is prepared by heating

ilmenite FeTiO3 with hydrogen chloride and chlorine. 2FeTiO3 + 4HCl + Cl2 = 2FeCl3 + 2TiO2 +2H2O. Test for Purity Clarity and colour of solution Acidity or alkalinity Water-soluble substances Arsenic Barium Heavy metals Iron

Page 15: Topical agents   inorganic chemistry b. ph sem 1

TITANIUM DIOXIDE, TIO2 Storage: Store in well closed containers made of glass or any

metal other than aluminium.

Medicinal and Pharmaceutical Uses: Pharmaceutical Aid and Topical Protective. Since it

spreads well, it is used as a white pigment in paints. Because of its high refractive index it is used in sun-tan preparations.

Page 16: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS AND ASTRINGENTS These are the chemicals and their preparations used in

reducing or preventing infection due to microorganisms.

Antiseptic: Inhibit the growth of MO Disinfectant: Destroy the Pathogenic MO Germicides: Kill Bacteria, Fungi, Viruses, Spores Bacteriostatics: Primarily inhibit the Bacteria – Only

arrest their growth not to kill Sanitizers: For maintaining the health for Sanitization

purpose

Page 17: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS AND ASTRINGENTS Uses: 1% solution used for installation into theeyes of

newborn babies, as prophylacticmeasure against opthalmia neonaturum.

Effective against gonoccocal organisms. 0.5% aqueous solution in the form of wetdressing

applied to third degree burn. Packaging and storage: Preserve in tight,light-

resistant containers.

Page 18: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS AND ASTRINGENTS CLASSIFICATION OF DISINFECTANTS AND ANTISEPTICS

1. Halogens (chlorinated lime, chloramine B, chlorhexidine, iodinole, iodovidone)

2. Oxidizing agents (hydrogen peroxide, potassium permanganate)

3. Acids (salicylic acid, boric acid)

4. Phenol derivatives (phenol, cresol, resorcinol, vagotil)

5. Aldehydes and alcohols (formaldehyde, glutaraldehyde, ethanol, isopropanol)

6. Metallic salts (silver nitrate, zinc sulfate, and copper sulfate)

7. Dyes or tints (brilliant green, rivanol, methylene blue)

8. Detergents (roccal, aethonium, cerigelum, decamethoxinum, soaps)

9. Derivatives of different chemical groups (furacilinum)

10. Agents from plant source (novoimaninum, chlorophylliptum, and lysocim)

Page 19: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS AND ASTRINGENTS MOA 1: Oxidation 2: Halogenation 3: Protein Precipitation

Page 20: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS HYDROGEN PEROXIDE, H2O2 Laboratory method: Na2O2 + H2SO4 → Na2SO4 + H2O2 BaO2.8H2O + H2SO4 → BaSO4 ↓+

H2O2 + 8H2O Industrial method: 2H2SO4 ——————→ H2S2O8 (aq.) +

H2 H2S2O8 + 2H2O ——→ 2H2SO4 + H2O2 By redox process:

Page 21: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTSBy redox process: Industrially H2O2 is prepared by the auto-oxidation of 2-alkylanthraquinols. The process involves a cycle of reactions. The net reaction is the catalytic union of and to give

The H2O2 formed (about 1%) is extracted with water and concentrated.

Page 22: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS HYDROGEN PEROXIDE, H2O2 Test for purity: Acidity Organic stabilizers Non-volatile matter Storage: H2O2 is not stored in glass bottles since the

alkali metal oxides present in glass catalyse its decomposition. It is, therefore, stored in paraffin wax coated glass, plastic or teflon bottles. Small amounts of acid, glycerol, alcohol, acetanilide and H3PO4are often used as stablizers to check its decomposition.

Page 23: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS Uses: (i) For bleaching delicate articles like wool, hair, feather, ivory, etc. (ii) For restoring colour of old lead paintings whose white lead has

blackened due to formation of PbS by H2S of atmosphere. Hydrogen peroxide converts the black lead sulphide to white lead sulphate

(iii) As an aerating agent in production of spong rubber. (iv) As an antiseptic and germicide for washing wounds, teeth and

ears, under the name of perhydrol. (v) In the manufacture of sodium perborate, sodium percarbonate.

These are used in high quality detergents. (vi) As an antichlor. (vii) As an oxidant for rocket fuel. (viii) In the detection of Ti, V and Cr ions with which it forms

peroxides of characteristics colours. (ix) In the production of epoxides, propylene oxide and

polyurethanes. (x) In the synthesis of hydroquinone, pharmaceuticals

(cephalosoporin) and food products like tartaric acid.

Page 24: Topical agents   inorganic chemistry b. ph sem 1

ANTIMICROBIAL AGENTS BORIC ACID, H3BO3 Boric acid, also called hydrogen borate,

boracic acid, orthoboric acid and acidum boricum, is a weak acid of boron often used as an antiseptic, insecticide, flame retardant,neutron absorber, or precursor to other chemical compounds. It has the chemical formulaH3BO3 (sometimes written B(OH)3), and exists in the form of colorless crystals or a white powder that dissolves in water. When occurring as a mineral, it is called sassolite.

Page 25: Topical agents   inorganic chemistry b. ph sem 1

BORIC ACID, H3BO3

Preparation: Boric acid may be prepared by reacting

borax (sodium tetraborate decahydrate) with a mineral acid, such as hydrochloric acid:

Na2B4O7·10H2O + 2 HCl → 4 B(OH)3 [or H3BO3] + 2 NaCl + 5 H2O

It is also formed as a by product of hydrolysis of boron trihalides and diborane:

B2H6 + 6 H2O → 2 B(OH)3 + 6 H2 BX3 + 3 H2O → B(OH)3 + 3 HX (X = Cl,

Br, I)

Page 26: Topical agents   inorganic chemistry b. ph sem 1

BORIC ACID, H3BO3 Assay: Assayed by acid-base titration. Sample + water + glycerol titrate against

standard sodium hydroxide using phenolphthalein as indicator. Test for Purity: clarity and colour of the solution sulphate . solubility in ethanol . arsenic . heavy metals . loss on drying

Storage: The substance is quite stable in air. Store in well closed containers. Uses: Boric acid can be used as an antiseptic for minor burns or cuts and is

sometimes used in dressings or salves. Boric acid is applied in a very dilute solution as an eye wash. Dilute boric acid can be used as a vaginal douche to treat bacterial vaginosis due to excessive alkalinity.[14] As an anti-bacterial compound, boric acid can also be used as an acne treatment. It is also used as prevention of athlete's foot, by inserting powder in the socks or stockings,

Page 27: Topical agents   inorganic chemistry b. ph sem 1

POTASSIUM PERMANGANTE, KMNO4 Potassium permanganate is an inorganic chemical compound with the formula

KMnO4. It is a salt consisting of K+ and MnO4− ions. Formerly known as permanganate of potash or Condy's crystals, it is a strong oxidizing agent.

Test for Purity: Chloride and sulphate Water-insoluble matter Colour of the solution

Storage: Solid KMnO4 is a strong oxidizer and thus should be kept separated from

oxidizable substances. Store in well-closed containers. Uses: As an oxidant, potassium permanganate can act as an antiseptic Permanganate washes were once used to treat gonorrhea[25] and are still

used to treat candidiasis.[26] It can also be used to inactivate the poison strychnine.

Potassium permanganate is one of the principal chemicals used in the film and television industries to "age" props and set dressings. Its oxidising effects create "hundred year old" or "ancient" looks on hessian cloth, ropes, timber and glass.

Page 28: Topical agents   inorganic chemistry b. ph sem 1

IODINE, I2 Iodine, I, is a dark violet (Greek, ioeides,

violet) non-metallic halogen element belonging to Group VIIb (i.e. the Halogen Gro

Preparation: Iodine can be prepared in the laboratory

by heating potassium Iodide or sodium iodide with dilute sulphuric acid and manganese dioxide.

2 KI + MnO2 + 3 H2SO4 ==> I2 + 2 KHSO4 + MnSO4 +2 H2O up of elements) of the periodic table.

Page 29: Topical agents   inorganic chemistry b. ph sem 1

IODINE, I2 Test for Purity: Bromides and chlorides Non-volatile matter

Storage: It is volatile in nature. Iodine topical solution should be stored

in light-resistant containers at a temperature not exceeding 35 °C and iodine tincture should be stored in air-tight containers.

Uses: Iodine is used n medicine, where its solution in alcohol, called "tincture of

iodine", is used as a disinfectant, n the manufacture of compounds used in photography (e.g.

silver iodide which is a light sensitive material used in film), n the manufacture of dyestuffs and drugs, and s a reagent in analytical chemistry.

Page 30: Topical agents   inorganic chemistry b. ph sem 1

SILVER NITRATE, AGNO3 Silver nitrate is an inorganic compound with chemical formula

AgNO3. Test for Purity: clarity and colour of the solution acidity and alkalinity foreign salts aluminium, bismuth, copper and lead

Storage: Affected by light, store in tightly closed light resistant containers. Uses: Silver salts have antiseptic properties. Until the development and

widespread adoption of antibiotics, dilute solutions of AgNO3 used to be dropped into newborn babies' eyes at birth to prevent contraction of gonorrhea from the mother. Eye infections and blindness of newborns was reduced by this method; incorrect dosage, however, could cause blindness in extreme cases.

Page 31: Topical agents   inorganic chemistry b. ph sem 1

POVIDONE-IODINE Povidone-iodine (PVP-I) is a stable chemical complex

ofpolyvinylpyrrolidone (povidone, PVP) and elemental iodine. It contains from 9.0% to 12.0% available iodine, calculated on a dry basis.

Test for Purity: heavy metals nitrogen iodide sulphated ash loss on drying

Storage: Since it slightly hygroscopic in nature, store in a well closed , light

resistant containers. Uses: It is used as a disinfectant. Povidone-iodine is a broad spectrum

antiseptic for topical application in the treatment and prevention of infection in wounds.

Page 32: Topical agents   inorganic chemistry b. ph sem 1

SELENIUM SULPHIDE,SES2 Selenium disulfide is an inorganic compound with

the approximate formula SeS2. Both sulfur and selenium catenate (form chains and rings) readily, and mixtures of selenium and sulfur likewise give rise to numerous "alloys".[1] This compound is not an analogue of sulfur dioxide.

Test for Purity: soluble selenium compounds

Storage: Store in well closed containers. Uses: In the treatment of dandruff. Available as Selsun

cream and suspension.

Page 33: Topical agents   inorganic chemistry b. ph sem 1

ASTRINGENT Astringents are protein precipitant with limited penetration

power It coagulates the protein on the surface of the cell and brings

out hardening effet. It constricts the tissue: Small Blood vessels These are mild Antimicrobial Agents USES: Styptic to arrest minor blleding by coagaulation of blood Anti perspirant to reduce perspiration by constricting pores of

skin Anti Inflammatory action At high concentration to remove unwanted tissue growth Internally they can use in diarrhoea As cosmetic as skin tone and bring out the hardening effect In dental products it can promotes hardening the gums It reduces the cell permeability

Page 34: Topical agents   inorganic chemistry b. ph sem 1

ASTRINGENT Aluminum Compound 1: Alum: Potash Alum:[AlK(SO4)2, 123H2O] Ammonia Alum:[NH4Al(SO4)2,12H2O] Formula: AlK(SO4)2,12H2O Synonums: Aluminium Potassium Sulphate, Potash Alum,

Potassium Alum Uses: Large dose gives irritation and gives Gum

Necrosis, GI Haemorrhage Alum precipitate proteins Used as mordant in dyeing industry.

Page 35: Topical agents   inorganic chemistry b. ph sem 1

ZINC SULPHATE Three forms are official – heptahydrate, hexahydrate,

monohydrate Formula: ZnSO4.7H2O Mol. Wt: 287.54 Preparatio: Zns + 2O2-------ZnSO4 Zn + H2SO4 -------- ZnSO4 + H2 Properties: Colorless, Transparent crystals, Odourless Very solublein water; practically insoluble in ethanol USES: When taken internally: Causes abdominal pain, dyspepsia,

nausea, vomiting, diarrhoea, gastic irritation I High dose - Anemia, Neutropenia Water soluble Zinc is used as supplements for Zinc deficiency In Verity of Skin condition