Lesson 08_AntioxidantsWatersGlasses PDF

PHCH 1102: ANTIOXIDANTS, GLASSES & WATERS Eden P. Cesista, RPh, MSc  OUTLINE I. Antioxidants II. Glasses III.Official Waters PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  OBJECTI...

PHCH 1102: ANTIOXIDANTS, GLASSES & WATERS Eden P. Cesista, RPh, MSc  OUTLINE I. Antioxidants II. Glasses III.Official Waters PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  OBJECTIVES At the end of this session, the student should be able to: 1. Discuss the different antioxidants and their mechanisms 2. Determine the types of glasses and its application 3. Explain the properties of water and its pharmaceutical application PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY ANTIOXIDANTS PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  INTRODUCTION ▶ Reduction-Oxidation (RedOx) Reactions Reduction/Oxidizing Agent: Oxidation/Reducing Agent: PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  INTRODUCTION ▶ Reduction-Oxidation (RedOx) Reactions Reduction/Oxidizing Agent: Oxidation/Reducing Agent: PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY TRY ▶ Reduction-Oxidation (RedOx) Reactions Reduction/Oxidizing Agent: Oxidation/Reducing Agent: PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY INTRODUCTION ANTIOXIDANTS? PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  INTRODUCTION ▶ Free radicals Highly reactive, short-lived organic and inorganic molecules that result from normal physiological metabolism in living systems Unstable; has unpaired electron ▶ Effect of Free radicals? Damage cells ❑ leading to various diseases such as hypertension, atherosclerosis, heart failure, diabetes, neurological diseases, and cancerogenesis PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY INTRODUCTION Free radical – unpaired electron Antioxidants – neutralize free radicals by giving up some of their own electrons PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  INTRODUCTION ▶ Antioxidants any compound that can counteract unstable molecules called free radicals that damage DNA, cell membranes, and other parts of cells. they act as a natural "off" switch for the free radicals. PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  ANTIOXIDANTS Sodium nitrite Hypophosphorus acid Sodium thiosulfate Nitrogen Sodium dioxide Sodium bisulfite Sodium metabisulfite PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM NITRITE ▶Sodium Nitrite Can act both as reducing or oxidizing agent Reducing property: Oxidizing property (in acidic condition and neutral to alkaline condition)) PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM NITRITE ▶Sodium Nitrite Preservative Carcinogenic due to formation of _____________ Antidote PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM NITRITE ▶Cyanide Poisoning Mechanism of Toxicity o binds to cytochrome oxidase o Inhibits electron transport chain (ATP will not be produced) o Decrease utilization of oxygen (hypoxia) PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM NITRITE ▶Sodium Nitrite Antidote for cyanide poisoning 1. Promote the formation of methemoglobin 2. Methemoglobin has high affinity to cyanide (CN-) 3. Formation of cyanmethemoglobin (less toxic) PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM THIOSULFATE Uses: ❑ Act as antioxidant to solutions containing iodides ❑Antidote for cyanide poisoning PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SULFUR DIOXIDE Sulfurous anhydride Has a characteristic of burning sulfur → Suffocating odor In neutral to alkaline condition, it is converted to bisulfite Produces acidic solution: PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SULFUR DIOXIDE Use: ❑ Antioxidant for injectable preparations in single or multiple dose containers PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM BISULFITE ▶ Sodium Hydrogen Sulfite, Sodium Acid Sulfite ▶ Odor of sulfur dioxide (SO2) ▶ Both sulfite and bisulfite are neutralized by the addition of acid: PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM BISULFITE ▶Strong reducing agents In acidic condition, they are oxidized by oxidizing agents such as Permanganate Dichromate Halogens (Equation 4) Hydrogen peroxide (Equation 5) Hypochlorous acid Sodium hypochlorite Ferric salts, etc. PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM BISULFITE ▶Use ▶ Epinephrine hydrochloride injections ▶ Phenylephrine hydrochloride injections ▶ Ascorbic acid injections PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SODIUM METABISULFITE ▶ Disodium pyrosulfite ▶ Odor of SO2 ▶ Source of bisulfite Most of the commercial sodium bisulfite is actually the metabisulfite which upon solution in water is immediately converted to the bisulfite PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  HYPOPHOSPHORUS ACID ▶ Uses: Preservative in Diluted Hydroiodic Acid and Ferric Iodide Syrup It acts to reduce free iodine and ferric ion back to iodide and ferrous ion, respectively. PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  NITROGEN ▶Inert gas ▶Provides an inert atmosphere for oxidation-sensitive pharmaceuticals PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  TEST YOURSELF 1. Enzyme responsible for the conversion of cyanide to thiocyanate. 2. Reducing agent for Vitamin C injections 3. Cyanide antidotes: 4. Reaction of Nitrite with the organic amines present in meat leads to the formation of carcinogenic substance: ________________ PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY GLASS CONTAINERS FOR PHARMACEUTICAL USE PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  GLASS ▶Refers to vitreous material ▶ Composed mainly of _______________ ▶Glass types are determined by the results of TWO USP Tests: 1. ______________________________ 2. ______________________________ PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  GLASSES Additive Description Boron Decrease coefficient of expansion Potassium Amber-colored/ Brown-light resistant glass PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  TYPE I Description: ❑ Highly resistant borosilicate glass Test: ❑ Powdered Glass Use: ❑Suitable for all products, strong acids and alkalis, parenteral and non- parenteral preparation PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  TYPE II Description: ❑ Treated Soda Lime Glass Test: ❑ Water Attack Uses: ❑For alkali-sensitive products, buffered solutions, infusion fluids, blood and plasma, and large-volume containers. PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  TYPE III Description: ❑ Soda Lime-silica Glass Test: ❑ Powdered Glass Use: ❑ Solid dosage forms (__________, ______________) PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  TYPE IV Description: ❑General Purpose Soda Lime Glass Test: ❑ Powdered Glass Use: ❑ Non-parenteral preparations PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY PHARMACEUTICAL GLASSES Types Description Test I Highly resistant borosilicate II Treated soda-lime III Soda-lime-silica IV General purpose soda-lime PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  GLASS ▶Glass used for pharmaceutical containers is either borosilicate glass or soda-lime-silica glass. 1. Borosilicate glass: Boric oxide, Aluminum oxide, alkali/alkaline earth oxide 2. Soda-lime-silica glass: __________, _________ PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY WATER PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  WATER ▶Universal solvent ▶Best expectorant: _______________ ▶Properties: Amphoteric High dielectric constant Auto-protolytic/ self-ionization PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  Types of Water I. Natural/Well/Mineral Water II. Potable Water III. Hard water IV. Official USP Waters V. Heavy Water PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  I. Natural Water ▶Unfit for drinking Water Composition Alkaline Water Na2SO4, MgSO4 Saline/Purgative Water Na2SO4, MgSO4 NaCl Carbonated Water CO2 under pressure Effervescence Chalybeate Water Iron (Fe) in sol/suspension Ferroginous taste PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  I. Natural Water ▶Unfit for drinking Water Composition Lithia Water Li2CO3, LiCl Sulfur Water H2S Siliceous Water Soluble alkali silicates PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  II. Potable Water ▶Fit for drinking ▶Treated by the following USP Methods: ❑Reverse osmosis ❑Ion exchange ❑Distillation PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  III. Hard Water ▶Ions responsible: ▶Two types of Hardness 1. Temporary 2. Permanent PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  III. Hard Water Temporary Permanent Hardness Hardness Ca & Mg: Ca & Mg: Sulfate Cause Bicarbonates Chloride Hydroxides PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY Read: Brown et. al., (2012)  IV. Official USP Waters A. Purified Water B. Water for Injection C. Bacteriostatic Water for Injection D. Sterile Water for Injection E. Sterile Water for Irrigation F. Sterile Water for Inhalation PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  IV. Official USP Waters A. Purified Water ▶ Non-parenteral preparations ▶ Assays and tests PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  IV. Official USP Waters B. Water for Injection ▶ Solvent/Vehicle for Parenteral Preparations PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  IV. Official USP Waters C. Bacteriostatic Water for Injection ▶ Prepared from sterile water for injection to which has been added with one or more suitable antimicrobial preservatives ______________ ▶ It may be packaged in single-dose or multiple dose containers not larger than 30mL With label: “NOT FOR USE IN NEONATES” ▶ Multiple withdrawals PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  IV. Official USP Waters D. Sterile Water for Injection ▶ For extemporaneous compounding of parenteral preparations, including those used in animal assays ▶ No antimicrobial agent added PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  IV. Official USP Waters E. Sterile Water for Irrigation ▶ Irrigating solution ▶ No antimicrobial agent added With label: “For Irrigation only and not for Injection” PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  IV. Official USP Waters F. Sterile Water for Inhalation ▶ For the preparation of inhalational solutions ▶ No antimicrobial agent added With label: “For Irrigation only and not for Injection” PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  V. Heavy Water ▶ composed of isotopes of hydrogen (__________ & ____________) PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  SUMMARY I. Natural/Well/Mineral Water II. Potable Water III. Hard water IV. Official USP Waters V. Heavy Water PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY  REFERENCES Block, J.H., Roche, E. B., Soine, T. O., & Wilson, C. O. (1974). Inorganic Medicinal and Pharmaceutical Chemistry. London, Great Britain: Henry Kimpton Publishers. Brown T., Lemay H.E., Bursten, B., Murphy, C., Woodward, P. (2012). Chemistry: the Central Science (12th edition). United States of America, Pearson Prentice Hall Chang, R. (2010). Chemistry (10th ed.). New York: The McGraw-Hill Companies, Inc. United States Pharmacopeia (nd). Water for Pharmaceutical Purposes. Retrieved October 27, 2024 from http://www.uspbpep.com/usp29/v29240/usp29nf24s0_c1231.html United States Pharmacopeia (nd). Containers-Glass. Retrieved October 27, 2024 from http://www.uspbpep.com/usp31/v31261/usp31nf26s1_c660.asp US Department of Health and Human Services (2024). Sodium Nitrite – Medical Countermeasures Database. Retrieved October 27, 2024 from https://chemm.hhs.gov/countermeasure_sodium-nitrite.htm PHARM CHEM 1102 PHARMACEUTICAL INORGANIC CHEMISTRY