Elixir 1111111111111111111111111111.pptx

Elixir

1. LIQUID DOSAGE FORMS (ELIXIRS) Binamra Rai M. Pharm. (Industrial Pharmacy) Kathmandu University

2. INTRODUCTION Clear, sweetened, flavoured hydro-alcoholic solutions. Intended for oral use. Either used as vehicles or as the dosage form. Usually flavoured to enhance palatability. Alcohol content from 10 to 20%. Can be as high as 40% . Primary solvents- water and alcohol Additional solvents- sorbitol, glycerin, syrup As sweetening agents.

3. NEED FOR ELIXIR Some drugs are insoluble in water. Hence syrups and suspensions cannot be formulated. When we need to make a dosage form which could dissolve non-polar compounds. When we need to mask unpleasant taste of the API.

4. FORMULATION Components of elixir Alcohol Water Sweetener Flavoring agent Propylene glycol Preservatives Each elixir requires a specific blend of water and alcohol . Poor water-soluble compounds- High alcohol ratio Good water-soluble compounds- Low alcohol ratio

5. FORMULATION Sweetener Most elixirs are sweetened with sucrose or sucrose syrup. Some use: Sorbitol Glycerin Artificial sweeteners High alcoholic content elixirs use artificial sweeteners. E.g., saccharine. Required in small amounts unlike sucrose. Sucrose is poorly soluble in alcohol.

6. FORMULATION Propylene glycol Propylene glycol is used as a solvent. Also inhibits the growth of fungi and micro-organisms. Preservatives Parabens and benzoates are used. Paraben- Methyl, propyl Benzoate- Potassium, sodium Elixirs with alcohol content of more than 10 to 12% are self-preserving . Do not require additional antimicrobials.

7. FORMULATION Incompatibility Contain alcohol, thus incompatible with tragacanth , acacia, and agar. Precipitates the components. Should be avoided or used in concentrations that avoid precipitation. Alcohol also increases saline taste of bromides. Remedy- Use another solvent. When aqueous solution is added, partial precipitation may occur. Due to reduced alcoholic content.

8. METHOD OF PREPARATION Dissolve water-soluble components in a fraction of water. Then add sucrose to it. Sucrose reduces solubility of water. So should be added later. Dissolve alcohol-soluble components in alcohol. Alcohol content should be between 5-40%. Aqueous solution is added to the alcoholic solution with constant stirring. This is done to maintain high alcoholic concentration at any given time. Mark up the volume with the specified solvent/vehicle. Filtration should be done since elixirs should be clear.

9. METHOD OF PREPARATION Alcohol soluble and water-soluble components are generally dissolved separately. Aqueous solution is added to the alcoholic solution to ensure minimal separation of alcohol soluble components. Mixture is made up to volume with the specific solvent or vehicle. Talc is used to remove excess amount of oil. Preparation is filtered.

10. TYPES OF ELIXIR Non-medicated These are simple elixirs that do not contain API. Contain: Alcohol Sweetening agent Colouring agent Medicated These are solutions with API dissolved in water and alcohol. Contains other excipients.

11. TYPES OF ELIXIR Non-medicated These are simple elixirs that do not contain medicated agents. Contain: Alcohol Sweetening agent Colouring agent Medicated These are solutions with API dissolved in water and alcohol. Contains other excipients. Elixir might mean two things: Vehicle to add to a formulation. Dosage form with API.

12. TYPES OF ELIXIR Non-medicated Does not require preservative Self preserving Uses of non-medicated elixir: Used as diluting agents. Solvents for drugs. Same alcohol conc. is required to dilute medicated elixir. Common examples: Aromatic elixir Compound benzaldehyde elixir Iso-alcoholic elixir Medicated These are solutions with API dissolved in water and alcohol. Contains other excipients.

13. TYPES OF ELIXIR Medicated These are solutions with API dissolved in water and alcohol. Contains other excipients. Non-medicated Does not require preservative Self preserving Uses of non-medicated elixir: Used as diluting agents. Solvents for drugs. Same alcohol conc. is required to dilute medicated elixir. Common examples: Aromatic elixir Compound benzaldehyde elixir Iso-alcoholic elixir

14. TYPES OF ELIXIR Medicated Medicated elixirs are solutions with API. Dissolved in alcohol and water. Contains other components such as preservatives. Various concentrations of alcohol required. Non-medicated Does not require preservative Self preserving Uses of non-medicated elixir: Used as diluting agents. Solvents for drugs. Same alcohol conc. is required to dilute medicated elixir. Common examples: Aromatic elixir Compound benzaldehyde elixir Iso-alcoholic elixir

15. TYPES OF ELIXIR Medicated Medicated elixirs are solutions with API. Dissolved in alcohol and water. Contains other components such as preservatives. Various concentrations of alcohol required. Non-medicated Does not require preservative Self preserving Uses of non-medicated elixir: Used as diluting agents. Solvents for drugs. Same alcohol conc. is required to dilute medicated elixir. Common examples: Aromatic elixir Compound benzaldehyde elixir Iso-alcoholic elixir ALCOHOL CONC. (%) TYPE ~ 25 Simple 8-10 Iso-alcoholic 75-78 High alcoholic

16. TYPES OF ELIXIR Medicated Most medicated elixirs contain a single API. Dose can be adjusted by adjusting amount of elixir consumed. Medicated elixir examples: Antihistamine- Diphenhydramine HCl Analgesic- Acetaminophen Cardiotonic- Digoxin Antispasmodic- Hyoscine Sulfate Sedative- Phenobarbital

17. TYPES OF ELIXIR Dry elixir Novel dosage form. Very poorly water-soluble drugs microencapsulated . Dextrin used. Dextrin is water-soluble. Made from starch. Drug dissolved in ethanol-water co-solvent system. Spray dried. Ethanolic drug solution is contained in dextrin shell.

18. MERITS AND DEMERITS Merits Elixirs with alcohol content > 10-12% are self-preserving. Able to maintain both water-soluble and alcohol-soluble components. Easy to prepare. Relatively stable dosage form. Easy to administer. Can serve as a vehicle. Can be used to dilute medicated elixirs.

19. MERITS AND DEMERITS Demerits Alcohol content makes it unsuitable for children and teetotalers. Volatile ingredients requires special storage measures and precautions. Requires air-tight screw-top jar. Less effective than syrup in taste-masking. Required to keep away from flammable sources due to the presence of alcohol in the formulations. Liver sclerosis. Large amounts of alcohol can cause burning sensation on tongue.

20. SYRUP AND ELIXIR COMPARISON SYRUPS ELIXIRS Alcohol is not a compulsory component. Alcohol is compulsory. Sweeter than elixir. Less sweet than syrup. More viscous. Less viscous. Higher sugar concentration. Lower sugar concentration. Less stable. More stable. Relatively harder to formulate. Relatively easier to formulate. More effective taste-masking. Less effective taste-masking. Not clear, and usually opaque and coloured . Elixirs are clear and have to be so. Sucrose-containing syrups not used for diabetics. Can be used for diabetics.

21. QUALITY CONTROL OF ELIXIR Determination of alcohol concentration Elixirs need to be crystal clear . In cases where colourants are added, coloured but clear. Cloudy extracts can be clarified. Using talc or calcium carbonate. Followed by filtration. Alcohol content should be between 5-40% . Alcohol content should be determined if not specified in individual monograph. Via distillation. Loss of alcohol due to evaporation must be minimized.

22. QUALITY CONTROL OF ELIXIR Viscosity measurement Important test. Types of viscosity: Absolute It is a fluid’s internal flow resistance. When all specs and parameters are defined. Aka dynamic viscosity. Resistance to flow when one layer or plane attempts to move over another identical layer or plane at a given speed.

23. QUALITY CONTROL OF ELIXIR Relative When measured against a standard. Kinematic Absolute viscosity of a liquid divided by its density at the same temperature. Ratio of absolute/dynamic viscosity to density. v= μ/ ρ v- Kinematic viscosity μ - Absolute/dynamic viscosity ρ - Density

24. QUALITY CONTROL OF ELIXIR Methods used: U-tube viscometer Capillary tube viscometer Rotational viscometer Concentric cylinder viscometer Cone-plate viscometer Spindle viscometer Most used- Brookfield viscometer.

25. PARAMETERS Automated process. Maintain temperature. Various spindles. Small adapter To measure small quantities with low viscosity. Helipad adapter 6 types of spindles. For semi-solids. Vane Measures viscosity of pastes/slurries.

26. PARAMETERS US/UY adapter For low viscosity samples. RV spindle set- contains 6 spindles. For medium viscosity samples. Works on rotational viscometer principle. Fixed rpm- 0.5 to 100. Selection of type of tool based on type of sample. External or stand-alone mode. Speed- Between 10 to 100%.

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