PHT 3101: Liquid and semisolid dosage forms
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Transcript of PHT 3101: Liquid and semisolid dosage forms
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PHT 3101: Liquid and semisolid dosage forms
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Liquid and semisolid dosage forms
What to cover:• Solutions• Emulsions• Suspension • Ophthalmic ,otic and nosal preparations• Ointments ,creams and gels• Suppositories and inserts• QA(QC and cGMP)
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Course aim
• To prepare the students with the relevant knowledge, skills and attitudes, skills and attitudes to competently formulate and manufacture and evaluate liquid and semi-solid dosage forms
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Course outcomes
The students will be able to:• describe the various liquid and semi-solid dosage
forms• formulate liquid and semi-solid preparations• perform QA and QC on liquid and semi-solid dosage
forms according to Pharmacopoeia specifications• apply GMP in liquid and semi-solid dosage form
manufacture:
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Solutions
Definition of solutions and expressions of solubility advantages and disadvantages of using solutionsChoice of solvent Methods of controlling solubilityWhat a vehicle is and selection of appropriate vehiclesImprovement of solubilityNon aqueous solventsFormulative additives(buffers, density modifiers, tonicity modifiers,preservatives,reducing agent and antioxidants, sweetening agents, flavours and perfumes)Stability of solutions,Manufacture of solutions
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Solution contdPrinciples of dispensing:Solutions for oral useDiluentsMouthwashesNasal.oral,and aural solutionsEnemas Use of oral syringes
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Solutions Definition:
Homogenous mixture=two or more components
Dissolved in one or more solutes dissolved in one or more solvents
Usually solids in liquids
solvents mainly aqueous can be oily alcoholic and some other solvent
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Pharmaceutical solutions for oral dosage
Is based on their composition or medical useExamples and what they are:SyrupsElixirsLinctusesMixturesOral drops
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Solutions for other pharmaceutical uses
Examples and their uses or applications:
Mouth washes and garglesNasal solutionsEar dropsenemas
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Expression of concentrationsWays in which strength of pharmaceutical solutions are expressed.Amnt of drug in 5ml teaspoonful/percentage strength %w/v, %w/w,%v/v,%v/w .find out what these expressions mean and derive your own examplesOther ways of concn expression:MolarityMolalityMole fractionsmEq,mMol
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COMMON PHARMACEUTICAL SYRUP
SIMPLE SYRUP BP:Sucrose…..66.7%w/wWater……..33.3%w/w
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Advantages of solutions as an oral dosage form
• Liquids are easier swallow (paed/ geriatrics)• Therapeutic response faster • Are homogenous system and drug uniformly
distributed• Irritation by certain drugs (ASA, Kcl) reduced
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Disadvantages of solutions as an oral dosage form
• Bulky, inconvenient to transport and store• Ingredients in solution unstable, shorter shelf
life• Suitable media for mos growth• Measuring accurate dose difficulty by
individuals• Unpleasant taste more pronounced
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Choice of solvent, non-aqueous solvents;
Aqueous solutions:• Water –most widely used pharmaceutical
vehicleWhy? Advantages and why not used in other
circumstances
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Choice of solvent
• Types of pharmaceutical water.Portable waterPharmacopoeial purified waterWater for injectionsWater for injection free of carbon
dioxide/dissolved air
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Improvement of aqueous solubility
• Water –not possible to completely dissolve all ingredients at normal storage/room temps
• Over wide pH range readily dissolve strongly ionized materilas
• Weak acid and weak bases adequately dissolve at favorable pH
• Note concn of any material not close to limit of solublity
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Methods used to improvement of aqueous solubility
• Cosolvents: vehicles used in combination to increase solubility
Solubility in mixed solvents > individual solvent
Solubility of weak electrolyte or non-polar compound in water –improved by altering polarity of the solvent.
Addition of another solvent both miscible with water and in whc the compound is soluble
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Co solvents contd
Choice of co solvents limited in p’ceuticals:Toxicity and irritancyIdeally suitable cosolvents –dielectric constant btwn
25 and 80.Most widely used with this range-water and EtOHOthers solvents used with water:-Sorbitol,glycerol,propylene glycol, and syrup Read and makes notes on their properties and why
preferred in different circumstances
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Co solvents contd
• Propylene glycol + water with co-trimoxazole in oral solution
• Alcohol +Propylene glycol + syrup with paracetamol elixir
• Water/isoproply alcohol with betamethasone valerate
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Other methods used to improvement of aqueous solubility
• pH control• Solubilization ( addition of surface active agents,
micelles, hydrophilic surfactants’ HLB> 15 are solubilizers and their pharmaceutical applications)
• Complexation• Chemical modification• Particle size control
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Non-aqueous solutions
• Fixed oils of vegetable originNon volatile oils containing mainly fatty acidsesters of glycerol i.e almond oil consits of Glycerides mainly of oleic acid (oil phenol inj,
arachis oil for dimercaprol inj)others : olive oil, sesame oil, maize oil,cotton
seed oil,soya oil,castor oil(find out where applicable)
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Alcohols
• EtoH most widely used solvent in this classesp for external applications(> 15%v/v =
antimicrobial activity)• Industrial methylated spirit has MeOH 5%V/V,
denaturation property • Isopropyl alcohol
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Polyhydric alcohols
• A glycol=an alcohol with 2-OH groups per molecule
• Rarely used internally • Exceptional is propylene glycol used in
combination with water or glycerol as cosolvent• LMW PEGS(polyethylene glycols) or macrogols• Others find out• Glycerol =a tri-OH groups alcohol
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Other non-aqueous
• Dimethylsulfoxide• Ethyl ether• Liquid paraffin
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Miscellaneous solvents
• Isopropyl myristate• Isopropyl palmitate
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Other formulation additives in solutions(excipients)
Excipients include: buffers, density modifiersIsotonicity modifiersViscosity enhancersPreservativesReducing agents and antioxidantsSweetening agentsFlavours and perfumesColours
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Buffers
• Added substances that enable the solution to resist any change in pH shd an acid or an alkali be added
• Choice dependable on pH and buffering capacity required
• P,ceutically acceptable buffering based on:Carbonates,citrates,gluconates,lactates,phosphates
or citrates (and borates for external use)• Solutions of drugs (weak electrolytes)• Many body fluids
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Density modifiers
• Used in formulating spinal anaesthetics• Lower density than CSF tend to rise after
injection• Higher density fall• Ctrl of inj density and position of the operating
table enable control of the site to be anaesthetized
• Terms of expression • Isobaric, hypobaric and hyperbaric• i.e Dextrose
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Isotonicity modifiers
Required in formulating solutions isosmotic with body fluids for solutions for:
• injection• Application to mucous membranes • Ophthalmic use in large-volumes otherwise
irritant and painfulMost used Dextrose and sodium chloride
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Viscosity enhancers• Increase time of contact at site/area of
application as in eyes and skin• Increase palatability• Are non-ionic, ionic • Are used in low concnExamples :• Povidone, • Hydroxyethylcellulose,hydroxypropylcellulose,SCMC, Cellulose, sodium alginate• Carbomers
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Preservatives
• Broad spectrum of activity gram-ve & gram+ve bacteria, yeasts, moulds (for ctrl of microbiological bioburden in formulation)
• Low toxicity for human• Good solubility in water; low oil solubility• Stable ,effective over wide ph range,
compatible with other excipients• Non-volatile,odourless and tasteless
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Others excipients
• Reducing agents,sweetening,flavours and perfumes
Assignment:Stability of solutionsManufacture of solutions
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End