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MONOPHASIC LIQUID DOSAGE FORMS

MONOPHASIC LIQUID DOSAGE FORMS. SOLUTION:. “A solution is a liquid-preparation that contains one or more soluble chemical substances dissolved in a specified solvent.” Advantages Immediately available for absorption

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MONOPHASIC LIQUID DOSAGE FORMS

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  1. MONOPHASIC LIQUID DOSAGE FORMS

  2. SOLUTION: • “A solution is a liquid-preparation that contains one or more soluble chemical substances dissolved in a specified solvent.” • Advantages Immediately available for absorption Useful for hygroscopic drugs which must be administered as a solution • Disadvantages Less stable Incompatibility is faster Bacterial contamination

  3. A. Aqueous liquids: Water Purified Water Water for injection Sterile water for injection Bacteriostatic water for injection B. Oils &oily materials: Animals source…pig fat Vegetable Source…corn,cotton Mineral Source…liquid paraffin Synthetics….ethyl oleate C. Hydroxylated Compounds: Ethanol Propylene Glycol D. Hydro-alcoholic Mixtures E. Modern Vehicles: Dioxalanes Solvent for aerosol sprays Dimethylecetamide Solvents used

  4. -Vehicle for the internal Use 1. Purified Water 2.Aromatic Water a. Chloroform Water b. Peppermint Water c. Cinnamon Water d. Dill Water - vehicles for external use Isopropyl myristate Liquid Paraffin -vehicles for extraction Isopropyl Alcohol Acetone

  5. Formulation Consideration • 1) Solubility a) pH  b) Cosolvency  c) Solubilization  d) Complexation  e) Hydrotrophy  f) Chemical modification of the drug molecule 2) Preservation a) Preservatives  b) Antioxidants  c) Reducing agents  d) Synergists 3) Organoleptic consideration a) Sweetening agents  b) Flavoring agents  c) Coloring agents  d) Viscosity control  e) Overall appearance 4) Stability a) Chemical stability  b) Physical stability 

  6. 1.SOLUBILITY • Expression of solubility According to Indian Pharmacopoeia Descriptive Phrase - Approximate quantities(ml) of solvent by volume for 1 part (1 gm) of solute by weight Very soluble - less than 1 part Freely soluble - from 1 to 10 parts Soluble - from 10 to 30 parts Sparingly soluble - from 30 to 100 parts Slightly soluble - from 100 to 1000 parts Very slightly soluble - from 1000 to 10,000 parts Practically insoluble - more than 10,000 parts

  7. a. pH A large number of drugs are either weak acids or weak bases. The solubility of these agents can be markedly influenced by the pH of the environment • Weak Acid pH = pKa + log (ionised ) /(un ionised) pH = pKa + log (base) / (acid) Weak Base pH=pKa +log (unionised) / (ionised) pH = pKa+ log( base )/(acid) b. COSOLVENCY  Weak electrolytes and nonpolar molecules frequently have poor water solubility. These types of solutes are more soluble in a mixture of solvents than in one solvent alone. This phenomenon is known as cosolvency.

  8. c. DIELECTRIC CONSTANT One property of a solvent system is its dielectric constant. The dielectric constant of a solvent can be defined as the ratio of the capacitances of a capacitor filled with the solvent and air respectively.  d. SOLUBILIZATION spontaneous increase of solubility of a poorly water-soluble solute molecules into an aqueous solution of surface active agents (or surfactants) in which a thermodynamically stable solution is formed.

  9. e. COMPLEXATION Solubility of a compound may be increased by complexing with a complexing agent. e.g. solubility of para amino benzoic acid (PABA) may be increased by complexing with caffeine f. HYDROTROPHY The term hydrotrophy has been used to designate the increase in solubility in water of various substances due to the presence of large amounts of additives.  g. CHEMICAL MODIFICATION OF DRUG Poorly soluble drugs are chemically modified into water soluble derivatives.

  10. 2.PRESERVATION a.Preservatives Some pharmaceutically useful preservative Class -------Preservative ------Usual concentration (%) -Acidic Phenol - 0.2 - 0.5 Chlorocresol - 0.05 - 0.1   -Neutral Chlorbutanol - 0.5 Benzyl alcohol - 1.0 -Mercurial Thiomersal - 0.001 - 0.1 Nitromersol - 0.001 - 0.1 -Quarternary ammonium compoundsBenzalkonium chloride - 0.004 - 0.02 Cetylpyridinium - 0.01 - 0.02 

  11. b. Antioxidants An antioxidant is a molecule that inhibits the oxidation of other molecules c. Reducing agent A reducing agent (also called a reductant or reducer) is the element or compound in a reduction-oxidation reaction that donates an electron to another species however, since the reducer loses an electron we say it is "oxidized". This means that there must be an "oxidizer"; because if any chemical is an electron donor (reducer), another must be an electron recipient (oxidant).

  12. 3.ORGANOLEPTIC ADDITIVESa. Colouring Agents • Colouring Agents generally used in case of cosmetic preparations. • The second reasons is to distinguish one product from the products. A third reason is to distinguish the preparation being administered • Classification- 1.natural colouring agents-plant -animal -minerals 2.syntetic -coal tar

  13. 1. Natural Colouring Agents:  • Plants: • Many plants contain colouring agents which may be extracted. and used as colorant. • Some Examples are: a. Chlorophyll-green b. Annatto seeds-yellow to orange

  14. Animal:- Cochineal: It is an alkaline solution of the soluble Colouring principles caraminic acid of cochineal insects preserved by the addition of.It is very dark purplish red liquid.Minerals: -Mineral colours are termed pigments. -They are used to colour lotions, cosmetics and other preparation for external application. -As they are toxic, their use for internal preparation is forbidden. Ex: Red ferric oxide Yellow Ferric Dioxide

  15. 2. Synthetic colouring agents • The synthetic colours are coal tar dyes, because many of them are produced from substance obtained from coal-tar. • The certified colours are classified into three groups: • Group I- F.D. and C. Colours used in foods, drugs and cosmetics. • Groups II- The D. and C. Colour used in drug and Cosmetics. • Group III- The External D. and C. Colour.

  16. b. Flavouring agents • The use of flavour is actually a composite sensation of taste, touch, smell, sound and heat. • There are simply four types of tastes - Sweet - Sour - Salty - Bitter . Similarly there are seven basic odours like - Ethereal , camphoraceous ,Musky, Floral ,Pepperminty ,Pungent ,Putrid

  17. Classification of flavouring agents Two Types: 1. Natural and 2. Synthetic 1. Natural a. Fruits (Sweet, Sur and Astringent) Citrus Fruits (Orange, Lemon) b . Seeds (Vanilla, Anise, Nutmeg) 2.synthetics Benzaldehyde - Bitter Almond, Cherry pits Decyl Aldehyde - Citrus Flavours (Orange) Cinnamic aldehyde - Cinnamon type

  18. c. Sweetening agents • Sucrose • Sorbitol (Half Sweet than Sucrose) • Glycerin • Honey • Saccharin Sodium (300-550 times) • Cyclametaes (30 times sweeter than sucrose) • Aspartame

  19. d.Viscosity control Used to increase palatability and pourability Examples of viscosity controlling agents are -PVP -cellulose derivatives e.General apperance depends on colour and clarity

  20. 4.STABILITY a. Chemical stability Ex- effect of amino acids on stability of aspirin in propylene glycol solutions. b. Physical stability Oral liquids are stable if it retains viscosity,colour,taste and odour throughout its shelf life

  21. liquid dosage forms Monophasic (homogeneous solutions in which solute and solvent cannot be differentiated) Biphasic Emulsions suspensions External Internal Draughts Drops Linctus Syrups Elixirs mixtures Liquids for oral cavities Liquids appiled on body cavities Liquids appilied on skin Douches Enemas Ear drops Nasal drops Inhalants and eye drops Gargles Mouthwashes Throat paints Glycerites Throat spray Liniments Lotions collidions

  22. ORAL MONOPHASIC DOSAGE FORM • ORAL MONOPHASIC DOSAGE FORM Draughts Drops Linctuses Syrups Elixirs Mixtures

  23. A. Draughts • It is simple solution (mixture) which contains a single dose. • Each dose is sent in separate bottle.Total volume is 50 ml. • It is essential to be labelled with storage conditions on draughts. • It is given very early expiry date (48 hours). Examples: 1.Ipecacuanha emetic draughts-BPC (Treatment of poison) 2. Paraldehyde draughts- Oxidized to acetic acid and cause death Do not use, if the solution is discolored.

  24. Classification of mixtures • Mixtures containing soluble substances Eg: Carminative mixtures • Mixtures containing diffusible solids Eg: Bismuth, magnesium carbonate • Mixtures containing in diffusible solids Eg: Salicylic acid, quinine salicylate • Mixtures containing precipitates forming liquid Eg: potassium iodide

  25. D . SYRUPS: • “It is concentrated aqueous solution of sucrose mixed with solution of medicaments and others additives.” • Generally syrup is prepared by sucrose but is partly replaced by dextrose or other polyhydric alcohols to reduce crystallisation of sucrose or to increase solubility of medicaments and other additives. • Consists of 85% sugars • 2 types of syrups Non medicated syrup Medicated syrup

  26. FORMULATION OF SYRUP • Sugar-85% • Anti microbial preservatives(0.1-0.2%) benzoic acid ,sodium benzoate • Flavorant • colorant Example- Active drug – 5ml Other drug solids -3ml Glycerin - 15ml Sucrose -25g Ethanol - 95%qs Purified water - 100ml

  27. Function of Syrups • Sweetening agent • Good antioxidant • Preservatives • Demulcents and • soothing agent • EXAMPLES OF SYRUPS: Codeine phosphate syrup Squill syrup

  28. Syrups are used for formulating   Antibiotics Antitussives Antihistamines Vitamins Analgesic/antipyretic PREPARATION OF SYRUP – 1.Solution with heat: For non-volatile, thermostable drugs 2.Agitation without heat: For volatile, thermolabile drugs 3.Addition of medicating liquid to syrup: For liquid medicaments such as extracts, tinctures 4.Percolation:

  29. E. ELIXIRS Elixirs are clear, pleasantly-flavoures, sweetened Hydro alcoholic liquid intended for oral use. 2 types of elixirs • Medicated elixir • Non medicated elixir

  30. ADDITIVES 1.Chemical Stabilizers: pH Adjustment Sequestering agents- like EDTA 2.Colouring Agents: Amaranth Compound Tartrazine 3.Flavouring Agents: Lemon spirit ,Compound orange spirit 4.Sweetening Agents: Invert Syrup, Sodium Sachharin 5. preservatives: 20% Alcohol as vehicle Propylene glycol

  31. Formulation of phenobarbital elixir phenobarbital - 4g orange oil - 0.25ml propylene glycol - 100ml alcohol - 200ml sorbitol solution - 600ml colour - qs purified water - 1000ml EXAMPLES- Chloral Elixir pediatric Paracetamol Elixir Ephedrine Elixir Phenobarbitone Elixir

  32. FORMULATION OF LINCTUSES • 1. Vehicle 2. Additives • 1. Vehicles: a. Syrup b. Tolu Syrup • It also provides aromatic odour and flavour, it has also mild expectorant action. • Due to high content (68%) of sucrose, solution tends to crystallise, so stored at constant temperature. • Due to high solid and low water content, dissolution of medicament is slow. Sometime glycerol is used as Auxiliary Vehicle.

  33. 2. Additives A. Chemical Stabilizers : Linctuses are self stabilized due to syrup, so no need of any other stabilizer. B. Colouring Agent: Coal-tar dyes Ex: Compound Tartrazine solution C. Flavouring Agent: Syrup itself act as masking agent. Some fruit flavours used are; Lemon and Black current D. Preservatives: Syrup has preservative action due to high osmotic pressure. Tolu syrup contain Benzoic acid and cinnamic acid.Some other preservatives are -Chloroform spirit -Benzoic acid spirit solution

  34. Liquids for Special Use (Oral Cavity) • Gargles • Mouth-washes • Throat paints • Glycerites • Throat Spray

  35. A. Gargles: -Gargles are aqueous clear solutions intended to be used in the mouth and throat.. Gargles are pleasantly flavoured and 5-9.5 pH appear to be safe. -Some therapeutic agents used in gargles are antibiotics, antiseptics , local anesthetics,Analgesic, Deodorants and Astringents. Label : “For external use only” Examples: Phenol gargles Potassium chlorate and phenol gargles Thymol glycerin compound

  36. B. Mouth Washes - Mouth washes are aqueous solution used to cleanse and deodorise the buccal cavity. - used for its deodorants, refreshing or antiseptic property. Mouth washes generally contain antibiotic agents or astringent ,alcohol, glycerin, sweeteners and surfactants, flavouring and coloring agents. Label : “For external use only” Examples: - Alkaline phenol mouth wash Hydrogen peroxide mouth wash Buffer sodium perborate mouth wash Compound sod. Chloride mouth wash

  37. C. Throat Paints • Throat paints are viscous liquid preparations applied to mucous surfaces. • They may be aqueous or alcoholic solution more viscous due to high content of glycerin and prolong the action of medicaments. • Throat paints are used for the mouth and throat infection. • contains – antiseptic, astringent and analgesic. CONTAINERS: Dispensed in airtight colored bottle in order to distinguish from preparation meant for internal use. EXAMPLES: Compound iodine paints Crystal violet paint

  38. D. Throat Spray • Spray solutions are aqueous alcoholic or glycerin solution intended for throat or nose by means of atomizer or nebulizer. • The spray device should produce coarse droplets for upper respiratory tract, while fine droplets for lungs (produced by nebulizer). • Spray solution contain antibiotics, antihistaminic, vasoconstrictors, alcohol and suitable solubilizing and wetting agents. Spray solution contain chlorbutol as an antibacterial and antifungal agent. • EXAMPLES: Adrenaline and Atropine spray compound-BPC.

  39. LIQUIDS FOR SPECIAL USE (OTHER THAN ORAL CAVITY):  • DOUCHES • ENEMAS • EAR-DROPS • NASAL DROPS • INHALANTS/SPRAY/AEROSOLS • Eye drops

  40. A. Douches • Douches is medicated aqueous solution for rinsing body cavity applied at lower pressure like • Eye douches • Pharyngeal douches • Nasal douches • Vaginal douches • Bladder douches • Rectum douches • Generally three cavities are widely used ; For vaginal purpose termed as Douches For bladder purpose termed as Irrigation For rectum purpose termed as Enemas.

  41. -Douches are restricted to vaginal solution have cleansing or antiseptic action. -Promote healing or as an astringent. -Vaginal douches must be sterile if used after child birth or surgery. -Bladder irrigation must always be sterile as bladder is a sterile organ. -Douches dispensed as concentrated forms and directions for dilution with warm water.

  42. Category Ingredients 1. Cleansing -Isotonic sodium chloride solution -Boric acid (2%) -Sodabicarb (1-2%) - Saponated cresol (0.2-.05%) 2. Antiseptic Chlorhexidine (0.02%) Chlorxylenol (5-10%) Lactic acid (0.5-2%) Mercuric chloride (0.001%)KMnO 4 (0.001-1%) 3. Astringent - Alum (1%) Tannic acid Zinc sulphate

  43. B. ENEMAS • “Enemas are aqueous or oily solution or suspension or oil in water emulsion introduced into rectum or colon for cleansing , therapeutic or diagnostic purpose. • Types of Enemas: 1.Cleansing enemas 2.Therapeutic enemas. 3.Diagnostic enemas

  44. 1.CLEANSING ENEMAS: Cleansing enemas used to evacuate feaces in constipation or before an operation. Two types: A. By stimulating of peristalsis i . Large volume: Plain water Soft soap Turpentine enemasii. Small volume (Osmotic retention) Sodium phosphate enema Magnesium sulphate enema Sorbitol Sodium chloride SodabicarbB. By lubricating impacted feaces: Olive oil enemas Araches oil Enemas Glycerin enemas

  45. 2.THERAPEUTICS ENEMAS: Category Ingredient a. Sedative Chloral hydrate Paraldehyde b. AnthelminticsQuassia c. anti-inflammatory Corticosteroids d. nutrients3.Diagnostic enemas: It is used for X- Ray Examination of lower bowel. Ex: Barium sulphate enemas.

  46. C. Ear Drops:Ear drops are solutions or suspension of drugs that are used into the ear. VEHICLES: - Water ,Propylene glycol,glycerin , PEG-4000 ,Dil. Alcohol ,Haxylene glycol uses category 1. For mild infection Antibiotics, anti bacterial 2. For softening wax Hydrogen peroxide, sodabicarb 3. For cleansing Spirit 4. Drying weeping surface Astringent, ammonium acetate 5. antiseptic- anaesthesic phenol

  47. CONTAINERS: Coloured fluted glass bottle with dropper LABELLED: - not to be taken orally Store in a cool place Not to be diluted List of official ear drops: Chloramphenicol ear drops Hydrocortisone. Hydrogen peroxide E.D. Phenol E.D. Sodium Bicarbonate E.D.

  48. D.NASAL DROPS “Nasal drops are liquid preparation and may be aqueous or oily for instillation into nostrils.” The following category can be formulated for nasal drops: - sympathomimetics ------- vasoconstrictor (ephedrine) Anti niflammatory ------ corticosteroids Anti bacterial Anti histamine Local anaesthetics

  49. Nasal Vehicles: they should possess following properties:- pH range of 5.5-7.5. - Have mild buffer capacity. - Tonicity equivalent to normal saline.- The viscosity should not exceed the normal viscosity of nasal mucus. Contain antimicrobial agents Containers : - Fluted color glass bottle with plastic screw cap and dropper.Label: -FOR EXTERNAL USE ONLY - STORE IN A COOL PLACE

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