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TEKNOLOGI
LIKUIDA
Dr. Rendra Pranadipa Tofani, Apt.
2017
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• Jam Kuliah Panjang Ngantuk?
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OUTLINE
1. Introduction to Dosage Forms & Liquids
2. Pharmaceutical Solutions:
1. Aqueous
2. Non-Aqueous & Viscid
3. Disperse Systems:
1. Suspension
2. Emulsion
3. Colloidal
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FORMULASI dan TEKNOLOGI LIKUIDA
Kuliah 1A:
INTRODUCTION to
DOSAGE FORMS
Dr. Rendra Pranadipa Tofani, Apt.
2017
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Objectives of the Lecture
Pada akhir kuliah, anda akan bisa menjelaskan:
• Why drugs are not used as such?
• What are excipients?
• What are dosage forms (bentuk sediaan)?
• Why formulation is necessary?
• Pharmaceutical Dosage Form vs. Pharmaceutical
Preparation (Bentuk Sediaan vs. Sediaan Jadi)
• Types of dosage forms available
• Consideration factors before formulating
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Active Pharmaceutical Ingredients (API) / Drug
Active drug substance (active pharmaceutical
ingredient - API)
• chemical compound with pharmacological (or
other direct effect ) intended for used in
diagnosis, treatment or prevention of diseases
• International nonproprietary names (INN,
„generic“ names)
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Why needs DOSAGE FORMs ?
1. safe and convenient delivery of accurate dosage
Examples: Tablets, Capsules, syrups
• Therapeutic Considerations
– Nature of the disease
– Age of Patients, or other limitations of administration
• Biopharmaceutics Considerations
– Biopharmaceutics
– Bioavailability
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Any Questions ??
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FORMULASI dan TEKNOLOGI LIKUIDA
Overview of
SOLUTION / LARUTAN
Dr. Rendra Pranadipa Tofani, Apt.
2017
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TYPES of LIQUID Dosage Forms
Active/s DISSOLVED in
a vehicle: CLEAR, Preparation with 2 or
HOMOGENOUS more PHASES
Fine PARTICLES
SUSPENDED in Liquid
Aqueous Solutions Colloids
Active/s dissolved in
NON-AQUEOUS LIQUID Active/s or
Solvent/s system/s DISPERSED
in Liquid
Non-Aqueous Solutions Emulsion
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Definition of SOLUTION (LARUTAN)
• Homogenous
• One-Phase
• Transparent
• Consists of 2 or more components
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SOLUBILITY (KELARUTAN)
MAX amount of a Solute (weight) that can be
dissolved in an amount of Solvent (volume), under
specific Temperature and Pressure.
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Factors affecting Solubility
• Electrostatic forces between water and solid
ion/molecules
• Pressure (in gases)
• Size of solute: molecule / particle / agregates
– Molecular size: larger particle generally LESS soluble.
– “branching” organic compounds ↑ solubility
reduce size of the molecule easier for solvation
– Solubility of a substance is CONSTANT, BUT the RATE
of solution depends on size.
• External physical forces: agitation
• Temperature: heat provides energy to break
bonds in the solid (generally)
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• pH of solution: Many important organic medicinal
agents are either weak bases or weak acids and their
solubility depends on the pH of the solvent. These
drugs react either with strong acids or strong bases
to form water-soluble salts.
• Weak bases NOT very soluble in water, BUT soluble in
dilute solutions of acids.
– Alkaloids (atropine), local anesthetics (cocaine, procaine),
etc.
• Weak acids form water-soluble salts in basic solution.
– Barbiturates (phenobarbital), sulfonamides (sulfadiazine),
etc.
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WHY Liquid Dosage Forms ??
• Route of administration for patients UNABLE to
swallow solid DF
• Children
• Elderly
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Classification of Solutions: Based on ROUTEs of ADM
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Methods of Preparations
3. Solution by Extraction
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1. SIMPLE SOLUTION
• Dissolving solute/s in a suitable solvent:
By Stirring and/or Heating
• Examples: Calcium hydroxide solution USP (lime
water)
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3. Solution by Extraction
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EXCIPIENTS in Solutions
1. Preservatives
2. Antioxidants
3. Sweetening Agents
4. Bufferss
5. Isotonicity modifiers
6. Viscosity enhancers
7. Flavours or fragrances
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Excipients: 1. PRESERVATIVES
Contamination may be resulted from:
• Raw materials are excellent growth media for
bacteria gums, dispersing agents, sugars, flavours.
• During manufacture: personnel, instruments,
environment
• Incorrect usage of the product by consumers.
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Esters of p-hydroxybenzoic acid (parabens)
• R: methyl, ethyl, propyl, butyl
• Usage: =< 0.2%
• Effective at pH 4 – 8
• Examples of antioxidants:
– Propyl & octyl esters of gallic acid
– Ascorbic acid (vitamin C)
– Sodium sulfite, sodium metabisulfite
– Oil-soluble: Tocopherols (vitamin E), BHT
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Excipients: 3. SWEETENING AGENTS
• Most widely used: SUCROSE
Colourless, highly water-soluble, increase viscosity,
Stable in wide pH (4-8), masks salty & bitter taste,
Soothing sensation on throat.
• Polyhidric alcohols:
– Sorbitol, mannitol, glycerol
– Lower Glycemic Index for diabetic preparations
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Excipients: 4. BUFFERS
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Excipients: 5. ISOTONICITY MODIFIERS
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Excipients: 6. VISCOSITY ENHANCEMENT
• Commonly used in TOPICAL solution formulations
• Low viscosity of aqueous-based solution very
short CONTACT TIME with the skin
• Need to SLIGHTLY increase Viscosity
• Examples: Acacia Gum, Xanthan Gum, Na-CMC,
Bentonite, etc.
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Excipients: 7. FLAVOURs and FRAGRANCEs
• To mask unpleasant taste and odour
• Artificial fragrances:
– Cheaper
– Better stability
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STABILITY of Solutions
• PHYSICAL stability:
– Clarity
– Viscosity
• CHEMICAL stability:
– Colour
– Odour
– Taste
– Active content
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Any Questions ??
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