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7/22/2019 4006Oral Solutions, Syrups, & Elixirs
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Oral Solutions, Syrups, &Elixirs
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Physicochemically:
Solution may be prepared from any combinationof
solid, liquid, & gas.
Pharmaceutically:
Solution are liquidpharmaceuticalformulations thatcontain one or more chemical substances dissolved
in a suitablesolvent or mixtureof mutually miscible
solvents.
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Solutions are classified based on their use:
1. Oral solution;
2. Otic solution;
3. Ophthalmic solution;
4. Topical solution;
5. Injection solution.
Solutions are classified based on their formulation:
1. Syrups;
2. Elixirs;
3. Spirits;
4. Aromatic water;
5. Tincture or fluid extract;
6. Injection solution.
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Oral solution contains:
1. ;
2. ;3. ;
4. (i.e. preservatives,
antioxidants,..etc). In compoundingpharmaceutical solution,
pharmacist must beaware of:
1. of the solute;2. of common pharmaceutical solvents;
3. with regard to all components of
formulation;
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Dissolution & SolubilityI. The Process of Dissolution & Kinetic theoryof Matter:
In solid stateof matter (condensed phase) the thermalmotionsof molecules or atoms are reducedto the
minimum, so that the forces resultin a coherentmasses of molecules (TDorganization).
In gaseous phases the molecules move
within the container, because they
have very weakintermolecular bonds.
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In liquidcondensed systems the thermal motion ofmolecules are>than that of the solidsbut are
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G = HT.S eq. 1G, is the variation in the free energy
H, is the variation in the enthalpy
S, is the variation in the entropy
T, is the thermodynamic temperature of the system. Therefore:
If H is (-), the transformation is called exothermic(spontaneous dissolution).
If H is (+), the transformation is called endothermic(non-spontaneous dissolution).
If H is 0, the transformation isin equilibrium(idealsolution).
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S is usually (+)for any process like dissolution.
In real solutions a change in the enthalpywill thereforeaccompany the dissolution.
From equation 1 we fined that the dissolutionwilloccur if His either negativeor if it ispositivebut
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H = Hcr+ Hsolv eq. 2
Hcris the absorbedheat when the crystalline
moleculewere separatedby an infinitedistanceagainstthe effect of their intermolecularattractive
forces.
Hsolvis the enthalpy of solvation & it is the absorbedheatwhen the solutemolecules are immersedin the
solvent.
Hcris always (+).
Hsolvis always (-).
But in must cases Hcr>Hsolv
So H is usually (+)& the process is endothermic.
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II. Solubility
G is the required energy to perform a work.
G = 0 at equilibrium.
Solution achieved when equilibriumis establishedbetween dissolved& un-dissolvedsolute in a
dissolutionprocess is termed a saturated solution.
Solubility is the maximumamount of solutethat can
be dissolved in certainsolvent at constant
temperature & pressure.
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Types of interactions between molecules & Solubility:
1. Dipole-dipoleinteractions (Van der Walals forces);
2. Ion-dipole& H-bonds.
H-bondsare very important because of smallsize & largeelectrostatic field.
Hydrogen bonds involve strongly electronigativeatoms (i.e. O2,
Cl2, F2,..etc.)
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When solute dissolves:
1. The (attractiveforces) between:
a) the ownmolecules of solute&
b) the ownmolecules of solventare
(attractiveforces) between:molecules of solute& solvents.
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Methods for increasingdrug solubility:
1. Selectionof ;
2. Selectionof of the medicinal agent;
3. ;
4. , of the solvent;
5. :
I2+ KI K+I-3
solubility of I2is 1g/3000mL, while solubility of KI-3 is
2g/100mL
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6. :
Mostmedicinal agents need heatfor dissolution ();
Fewdrugs exhibit a decreasein solubility with a riseintemperature ().
7. Variation of chemical&physicalproperties of both
& such as:Pressure, acidity or basicity of the solution.
The solubilityof apurechemical at given P& Tis constant
but its dissolutionrate depends on factors such as:
Particle size & Aspof the solute & agitation during dissolutionprocess.
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Steps of solubility determination:
1. of the drug at given T & P;
2. Analyzethe amountof drugpresent
in a given amount of solution;3. Calculationof .
Method of expressing solubility when exact solubility is unknown
(USP method):
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Table 1 & 2
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There is no exact ruleforpredictingexactsolubilityof a drug in a
specific solvent.
The mostfrequently used ruleis: Like Dissolve Likeso,Organic compounds (bases & acids) are more soluble in alcohol than in
water.
Pharmaceuticalscientist can estimategeneral solubility of a drugbased
on its chemicalstructure such as:1. in organic compounds (i.e. polar groups increase water
solubility);
2. ;
3. ; OH
OH OH
OH
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General rules of solubility for Inorganic Molecules:
G l l f l bilit f O i M l l
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General rules of solubility for Organic Molecules:1. Moleculeswith functional group are
water-solubleto a total length of ;
2. Branchedchain molecules are thanisomers;
3. decrease solubility;
4. between solvent& drugresults in of
solubility.How pharmacists select pharmaceutical solvent?1. ;
2. ;
3. ;4. with drug& in the
formulation;
5. (i.e. palatability, clarity and smell).
W t i th t d l t i h ti
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Water is the most used solvent in pharmaceutics;
Some solvents for oral preparations:
I. Alcohol, USP(Ethyl Alcohol, Ethanol,CH3CH2OH)
Alcohol, USP, is CH3CH2OH whendetermined at 15.56 C
The above T is the for alcoholdetermination.
II. Dehydrated Alcohol, USP, containsCH3CH2OH.
The above alcohol is used for when
anhydrous conditions are desired.
Alcohol is considered as pharmaceutical
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Alcohol is considered as pharmaceutical
Alcohol has activity which make it an
acceptable preservative.Alcohol is used in combinationwith ,
, & to the amountof alcohol due to its .
The of alcohol its usein OTC.
The FDAregulation for OTCproduct intended forpediatricuse:
1. < 6years [ethanol content ]
2. 612years [ethanol content ]
3. > 12years [ethanol content ]
III Dil t d Al h l NF
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III. Diluted Alcohol, NF
1. Diluted alcohol, NF, is prepared by mixingequalvolumes ofAlcohol, USP, & Purifiedwater,
2. The sumof the two volumesis 3% lessthan the expected.
3. [Alcohol] of 50 mlof alcohol 96 % + 50 mlof water is 49%.
96 alcohol : 100 ml solution
X1 : 50 ml
X1=50 . 96 =47.3 mlof alcohol in 50 mlof solution.100
Thus, mixing 50 ml of alcohol, USP + 50 ml water we will have 97 ml of
final volume with the following exact concentration:
47.3 ml alcohol : 97 ml solution
X2 : 100 ml of solution
X2=47,3 . 100 =49.2 % v/v.
97
Gl i USP (Gl l) CH OHCH(OH)CH OH
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Glycerin, USP (Glycerol), CH2OHCH(OH)CH2OH
1. Glycerin is a with a
2.
& miscible.3. It has capacity comparable with
alcohol.
4.
Its high viscosity () slow its capacity, so, heatwill & dissolvingcapacity of
glycerol.
5. It has capacity.
6. It is usedin many formulations.
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Propylene Glycol, USP, CH3CH(OH)CH2OH
1. & liquid.
2. & miscible .
3. Has properties.
4. Its properties are similarto glycerin.
5. It glycerin in many modern formulations.
W t
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Water:
I. Drinkable or Tap water;
II. Purified water, USP, H2O
Characteristicsof drinkable or tap water:
1. , and liquid;
2. Total is 0.1%w/v;3. ;
4. .
Drinkable water can notbe usedin .because:
Chemical .(i.e. precipitation,
discoloration, & effervescence).
It is usedonly for .& cleaningof
pharmaceutical machinery.
P ifi d t USP H O
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Purified water, USP, H2O:1. Total solidcontent is 0.001%w/v (1mg/100ml).
2. It is used for cosmetic, &pharmaceuticalpreparation
Types of Purified water:I. .water (ion-exchange method);
II. .water;
III. .(RO) water.
Purified water is prepared from water complying with the
federal environmental protection agency with respect to
drinking water.
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I. Demineralized or De-ionized water
This water is obtained .method.
Ion-exchange equipment involves the use of waterinsoluble resins:
1. .or acid exchanger resin:
H-Resin + M++ X-+ H2O M-Resin + H++
X-+ H2O
2. .or base exchanger resin:Resin-NH2+ H
++ X-+ H2O Resin-NH2.HX+ H2O
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II. Reverse Osmosis(RO):
Industrially known as cross-flowor;
Known as Tangential flowmembrane filtration:
A i d t f t i d ll l t
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1. Apressurized streamof water is passed parallel to
the inner side of a filter membrane core;
2. A .of the .water, or
influent, permeatesthe membrane as filtrate;
3. While the balance of the water sweeps tangentially
along the membrane;
4. This last oneexit the system withoutbeing filtered;
5. The filteredportion is called
.(purified);
6. The non-filteredportion is called
.(rejected);
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1. In Reveres Osmosis the flow is from the high concentrated solution to
the less concentrated.
Removing of particles depends on pore size of cross-flow
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Removingof particles depends onpore sizeof cross flowfilter membrane:
1. .removes bacteria (0.12 m);
2. .removes viruses (0.010.1 m);
3. .removes organic compounds MW 3001000 (0.0010.01 m);
4. ROremoves virtually all viruses, bacteria, pyrogens, organic molecules &90-99% of all ions ( 0.001 m).
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III. Distilled water
The first portion of the distilled water (1020%) must be
discharged.
The last 10% of the original water for distillation must be
discharged.
Preparation of Solution
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Preparation of Solution
Most Pharmaceutical solutions are unsaturated.
Thus, the amount of .than the
.of the volume of solvent
employed.
Methods of expressing strength of pharmaceutical
solutions:Table 6-4
Pharmacists may employ the following methods to increase
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Pharmacists may employ the following methods to increase
the dissolutionrate of a drug:
1. .;
2. .;3. Use of .;
4. Rigorous ..
Increase of rate of dissolution is important since most
pharmaceutical solutions are unsaturated.
Heat use must not exceed the .due to:
1. Drug .;
2. Presence of ., or solvents, or additives;
3. .dissolution of certain drugs (i.e. Ca(OH)2)
Water solubility of calcium hydroxide topical solution
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Water solubility of calcium hydroxide topical solution,
USP:
1. 140 mg/100 ml at 25 C;
2. 170 mg/100 ml at 15 C.
The storagetemperature .the [] of
the resultant solution.
Mostoral solutions are prepared by .
.of solutes in the solvent or
solvent mixtures.
Industriallyvery large .are used.
If heatis required, a .controlled
mixerstanks may be utilized.
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Oral Solutions & Preparations for Oral Solution
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Oral Solutions & Preparations for Oral Solution
Oral solution usually contains:
1. Flavorants & Colorants;2. Sweetening agents;
3. Stabilizers for chemical & physical stability (i.e.
antioxidants);4. Preservatives to prevent microbial growth (i.e. mp
& pp);
Compounding pharmacists must be aware of:
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Compoundingpharmacists must be awareof:
Chemical & physical incompatibilities between thevarious componentsof solution.
These .results in drug.& loss of potency.
Estersof parahydroxybenzoic acid (i.e. mp, ep, ppetc.) have the .to
.into certain .oils.
Thispartition theirpreservationefficacy.
Tools for oral solution administrations:
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Tools for oral solution administrations:
1. Tea spoonful = 5 mL;
2.
Table spoonful = 15 mL;3. .;
4. ..
Few solutions have large doses (i.e. Mg citrate oral
solution, USP, with actual dose of 200 mL).
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Dry Mixtures for Solution
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Dry Mixtures for Solution
For drugs (i.e. antibiotics) that have insufficientstability
in water to meet .shelf-lifeperiods.
Manufacturers provide these .in dry
powder or granules readyfor ..
The dry mixture containsall .including
., ., sweeteners, etc.
Once they are reconstituted with addition of solvent/s,
the .is .from 7to 14
daysdepending on drug & storage conditions.
Patientmust be .to .the
remainingpart of formulationafter the patient
completeshis course therapy.
Oral Solutions
http://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DXhttp://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DXhttp://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DXhttp://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DXhttp://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DXhttp://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DXhttp://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DXhttp://images.google.com/imgres?imgurl=http://www.pharmavista.net/images/20/2059115o.jpg&imgrefurl=http://www.pharmavista.net/scripts/api.dll%3Fpgm%3DCDQ32%26cmd%3DC2D17D0%26par0%3DPH%26match0%3D2080256&h=600&w=532&sz=24&hl=en&start=2&tbnid=OjKi1F0eqRFvyM:&tbnh=133&tbnw=117&prev=/images%3Fq%3Daugmentin%2Bsuspension%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DX7/22/2019 4006Oral Solutions, Syrups, & Elixirs
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Oral Solutions
Pharmacist must advise patient on:
1. .;
2. .;
3. .;
4. ..
Pharmacists must know:
Characteristics of solventused in the formulation to:
Advisepatient about mixingformulation with Juice, milk
or otherbeverages.Product label& Packageinsert must contain
.about .used informulation.
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Table 6-8
Oral Rehydration Solutions
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Oral Rehydration Solutions
Diarrheais a normal .body .
against noxiousor toxicsubstance e.g., Rotavirus, E. coli.
Diarrhea is characterized by an frequency of loosewaterystools.
Duringdiarrhea the .in smooth intestinelargely exceedthe capacityof large intestine to reabsorb it.
Diarrhea can leadto dehydration& ultimately death,
particularly inpediatric& elderlyPatients.
Over 5 million children < 4years age diedue to diarrhea each
year worldwide.
Lossof fluid during diarrhea resultsin loss of Na+, K+&
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g ,HCO3 -.
Sever loss in the above ions results in:
1. .shock;2. .;
3. .;
4. ., which if continuous lead to malnutrition.
Treatment approach of diarrhea:
1. Allow diarrhea to .& .itquickly.
2. Replacethe lost fluid& electrolyteswith an oral rehydrationsolution to avoid dehydration.
3. These are OTCproducts effectivein patients with mild volumedepilationof 510% of body weight.
Composition of oral rehydration solution
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Composition of oral rehydration solution
The active absorption of glucose in the smooth intestinepromotes:
Absorption of Na+, whichpromotesanion (X-) absorption,
NaX absorptionpromotesH2O absorption.
Therefore, the composition of oral solution is:1. Glucose: 110 mM 2% w/v.
2. Na+: 60 mEq/L.
3. HCO3- & /or citrate to correct blood acidosis.
A typical oral rehydration solution contains:
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A typical oral rehydration solution contains:
1. 45 mEq Na+,
2. 20 mEq K+,
3. 35 mEq Cl-,
4. 30 mEq citrate,
5. 25 g of dextrose per liter.
These formulations are available il liquid or powder/ packet form
for reconstitution.
Oral Colonic Lavage Solution
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O Co o c v ge So u o
Oral .solution is used to prepare the bowel for
.examinations (i.e. colonoscopy).
The .is a long narrow flexible tube containing a tinylight& camera at one end. The camera carries pictures of your rectum
& colon to a television screen, where they can be viewed by the
doctor & nurse.
http://images.google.com/imgres?imgurl=http://www.med.nyu.edu/virtualcolonoscopy/images/VC1.jpg&imgrefurl=http://www.med.nyu.edu/virtualcolonoscopy/virtualcolon/&h=371&w=656&sz=75&hl=en&start=16&tbnid=52KNNLKcMO3rJM:&tbnh=78&tbnw=138&prev=/images%3Fq%3Dcolonoscopy%2B%26svnum%3D10%26hl%3Den%26lr%3D%26sa%3DG7/22/2019 4006Oral Solutions, Syrups, & Elixirs
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A Typical formulation of oral colonic lavage solutionis:
1. Polyethylene Glycol 3350 236.00 g
2. Sodium sulfate 22.74 g
3. Sodium bicarbonate 6.74 g
4. Sodium Chloride 5.86 g
5. Potassium Chloride 2.97In 4800 mL disposable container
The recommended adult dose of this formulation is:
1. 4 liters of the solution before the GI procedure.2. The solution must be drunk as 240 mL every 10 minutes
until complete consume of the solution.
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Syrups
Syrups are concentrated, aqueous preparations of a
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Syrups are concentrated, aqueous preparations of a
sugaror sugar-substitutewith or without added
flavoring agents & medicinal substances.
There are 3types:
1. ., which is a bout saturated sugar
solution without flavour or medicine.
2. .: is a flavored simple syrup.
3. .: is a syrup containing medicinal
agent.
Syrups are useful alternativeof soliddosage forms forchildren & elderly.
Pharmacists canpreparesyrups in their own
pharmacy.
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Requirements for preparing syrups:
1. .of drug solubility& stability;
2. .must be considered case by case.
Medicated syrups are commercially prepared by:
1. .sucrose & purified water ( simplesyrup is obtained);
2. .& .the therapeutic
agent;
3. .of flavoring & coloring agents;
4. Additionother necessary & desirable ingredient.
Components of commercial syrups:
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Components of commercial syrups:
1. Sugar (sucrose) or sugar-substitutes used to
provide sweetness & viscosity;2. .;
3. .agents;
4. .;
5. .solvents;
6.
.agents;7. Thickeners, or stabilizers.
Advantages of medicated syrups:
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1. .of administration of a liquid form of abadtastingdrug;
2. This .attractivefor youngsters.
3. ., since these dosage forms .;
4. The .& .syrups have a soothingeffect on the irritatedtissue of the throat as they pass over them.
In summary:
1. Any.may be added to flavored syrup.
2. However, caremust be played to .betweenall components of the syrup.
Since thereare acidic,basic& neutralflavored syrups,attentionmust be exercised to the .of theadded drug.
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Table 6-6
Table 6-7
Sucrose & Non-Sucrose Based Syrups
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y p
Characteristics of simple sucrose syrup (85% w/v):
1. .;
2. .;
3. Preservation (hypertonic solution);
4. High density & specific gravity (s.g. =1.313)
Specific gravity =weight of substanceweigh of equal volume water
1.313 =w , thus, weight of 100 mL syrup is 131.3
100131.3g - 85g = 46.3 g or mL of water in the syrup.
Thus, 46.3 g of water are mixed with 85 g of sucrose to
give syrup 65.5% w/w or 85%w/v.
Solubilityof sucrose in water is 1g /0.5 mlof water, thus, 85 gofd 42 5 f t
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sucrose need 42.5 gof water.
Thus, the excessof water in 85%w/v syrup is3.8 mL.
These 3.8 mLof water are freeof sucrose.
This meansthat syrupisNot saturatedbut ..
Ifthe syrup was completely ., any variationof storageconditions (i.e. cooling) might produce sucrose .fromthe syrup.
This would starta chain of .& sucrose..
The syrupwould thenbe very much unsaturated & suitableformicrobialgrowth.
Since many officialsyrups are not saturatedsuitable .in
the formulation.
In special circumstances sucrose may be replaced in
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p y pwhole or in part by:
I. .substances (materials converted to
glucose in the body) such as:1. Other sugars (i.e. dextrose);
2. Non-sugars (i.e. sorbitol, glycerin propylene glycol ..etc.).
II. .substances such as methylcellulose(MC) or hydroxyethylcellulose HEC).
Characteristics of MC & HEC:
1. .& absorbed in the blood stream;
2. .viscosity or vehicle;
3. .& favors results in facsimile of a truesyrups.
4. .patients & child with carries teeth.
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Antihistamine syrup formulation
.. etc
Page 243
Antimicrobial Preservatives
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The amountof required preservative for protectiondepends on:
1. Amountof .for microbial growth;2. Nature& inherentpreservativeactivity of some
formulativematerials (i.e. many flavoring oils);
3. .of thepreservativeitself. Some preservatives & correspondent usual
concentration:
1. Benzoic acid or Sodium benzoate 0.10.2%
2. Combinations of m., e., p., b. parbens total 0.1%
3. Alcohol 1520 %
4. Propylene glycol & Glycerin 1 ml / 1ml.
Methods for Preservation of Syrups
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Methods for Preservation of Syrups
I. Storageat temperature;
II. Additionofpreservativessuch as glycerin, parabens;
alcohol,..etc.
III. Maintenanceof a [] of sucroseas a part of the
formulation.
Example: RxActive drug 5 mL volume occupied
Other drug solids 3 ml volume occupied
Glycerin 15 mL
Sucrose 25 gEthanol 95 % q.s.
Purified water q.s. 100 mL
How much alcohol would be required to preserve this prescription?
Answer:S S (85 % / ) h 1 313 th
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1. S. Syrup (85 %w/v) has s.g = 1.313, thus,
2. 85 g sucrose are in 100 ml 131.3 g of solution. 131.3
3. 131.3g85g = 46.3 g or 46.3 mL of water.
4. 100mL - 46.3 mL = 53.7 mL is the v. of 85 g of sucrose.5. Thus, 85 g of sucrose preserves 46.3 mL of water.
So, 85 g 46.3 mL
25 g X, thus, X = 13.62 mL of water preserved.
V. Of sucrose is:
85g 53.7 mL
25g x
Thus, X = 15.7 mL
6. v. of active drug+ v.of other drugsoccupies 5 + 3 = 8 mL
7. 1 mLof glycerinpreserves1 mL of water & occupy1 mL.So, glycerin preserves: 15 mL + 15 mL = 30 mL total.
8. The volume taken care = 13.62 + 15.7 + 8 +30 = 67.3 mL.
9. 100 ml67.3 mL of water preserved = 32.68 ml of water whichneed preservation.
10. Since it requires about 18% of alcohol to preserve water:
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So, 18 100 mL
x 32.68 mL, x = 5.88 mL of alcohol 100%.
11. But the available alcohol 95%:
So, C1 . V1 = C2 . V2
100 . 5.9 = 95 . V2 V2 = 6.2 ml of alcohol 95%
is required.
So, add 6.2 ml of alcohol to the syrup and complete volume up to 100mL with water.
Flavorants or Flavoring agents
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.flavorants.
.flavorants as volatile oils (e.g. orange oil,
vanilla ..etc.).Flavorants must posses sufficient water solubility.
Alcohol may added to improve solubility of flavors.
Colorant
http://images.google.com/imgres?imgurl=http://www.rarefruit-sa.org.au/images/Pluot%2520-%2520Flavor%2520Rich%25202.jpg&imgrefurl=http://www.rarefruit-sa.org.au/Samples.htm&h=600&w=800&sz=51&hl=en&start=15&tbnid=pT14UELReFPk7M:&tbnh=107&tbnw=143&prev=/images%3Fq%3Dflavor%2B%26svnum%3D10%26hl%3Den%26lr%3D7/22/2019 4006Oral Solutions, Syrups, & Elixirs
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Enhancethe appealof syrup.
Selection of colorant in correlation with
... (i.e. green with mint, brown with
chocolate, etc.).
Colorant must be:
1. ...;
2. ... with other syrup components;
3. Color stableat thepHrange & underthe intensityof lightthat the syrup is likely encountered during
its shelf-life.
Preparation of Syrups
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Preparation of syrup depends on chemical &physical
characteristics of the ingredients involved in
formulation.
There are 4 methodsfor syrup preparation:
1. Solution of the ingredients ...;
2. Solution by agitation ...;
3. Additionof sucroseto a medicated liquidor to a
flavored liquid;
4. ....
Solution with the Aid of Heat
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Advantages of this method:
1. ...method;
2. The heat provide ....
Disadvantages of this method:
1. Problems arise when ...ingredients areused;
2. ...of sucrose known as inversion:
Sucrose glucose (dextrose) + fructose (levolose);3. ...of the sucrose (browning of the
syrup);
Preparation procedure:
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1. Weigh 85 g of sucrose;
2. Place them in 100 ml of volumetric flask;
3. Addhot water & mixtell complete dissolutionof
sucrose;
4.
Addwater upto volume.5. Dissolveor addas dissolvedother components
such as flavor, color, medicine, & preservatives;
6. Fill in bottles then, close bottles after cooling.
S l ti b A it ti ith t th Aid f H t
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Solution by Agitation withoutthe Aidof Heat
Advantages of this method:
1. It is used for ...ingredients;
2. Avoidsugar ...&
.... Disadvantages of this method:
1. ...& ...are
employed for large scale preparation;
2. Needs ...of preparation;
3. ... to preservation.
P ti P d
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Preparation Procedure:
1. Put sugar& other formulativeagentsin large vessel
to permit thorough agitation;2. Mix well tell completedissolutionof sugar & other
solubleingredients;
3. Drugsare ... ... & then,added to syrup;
4. Add water upto volume;
5. ... directlyto syrup because it needslong time to be dissolved.
Addition of sucrose to Medicated liquid or to a Flavored Liquid
It is frequently used when or are
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It is frequently usedwhen ... or ... areemployed as the sourceof medications.
These fluid extracts are .or .. preparations.If the alcoholsolublecomponentsare ..., means of their
... are employed.
If the ...componentsare ... components,
they are generally removed by:1. Mixingthe tincture or fluid extract with ...;
2. Leavethe mixture to stand tell ... of water insolublecompounds;
3.
....4. Add sucrose to the filtrate & complete the procedure.
If fluid extracts (drug/s) are ...add them directly to a...to medicate it.
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Percolation
Types of percolation:
P l ti f t
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I. Percolation of ... to prepare syrup or;
II. Percolation of ... components:
1. Preparation of extract;2. Addsyrupto the ... to achieve the desired
syrup.
Preparation of Ipecac Syrup:
1. Prepare the extractby ...;
2. Add ... & ... to thepercolated ipecac.
The drug ipecacconsists of the dried rhizome& roots ofCephaelis ipecacuanha.
The extracted alkaloidsby ... with...solvent are: emetine, cephaeline, &
psychotrine.
It is an emetic syrup.
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Usual dose is 15ml for ... in childrenwhen stomach evacuation is desired.
Vomitingis achieved within hour in 80% of treatedchildren.
Abuseof this syrup was in young womenin attempt to
....Excessof emetinein tissue due to excess use cause
cardiacmuscle damage.
Toxic symptoms are:
1. ...;
2. ...symptoms;
3. ....
Elixirs
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Elixirs
Elixirs are, sweetened, flavored, hydro-alcoholicl ti i t d d f l
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solutions intended for oral use.
Types of elixirs:
1. Non-medicated elixir employed as vehicle.2. Medicated elixir employed for therapeutic effect
of the drug they contain.
Syrup Elixir... Less sweet
... Less viscose
... Lower sucrose content
Lower dissolving capacity Higher dissolvingcapacity
... Simple manufacturing
... More stable
The amountof alcoholin elixir depends on solubilityofdissolved agents
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dissolved agents.
Elixir with 1012 % alcohol dont need preservatives.
This alcoholic content represents Disadvantagefor:1. ...patients;
2. Adultswho ...consumption;
3.
Also represents another disadvantage for many....
Because of their ...& ...oilscontent, elixirs must be storedin:
1. Tightly ...containers;2. ...containers;
3. In ...place.
Preparation of Elixirs
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1. By simple solution (...);
2. By mixture of 2 liquid ingredients:
Dissolve alcohol soluble ingredients;
Dissolve water soluble ingredients separately;
Add ... solution to the ... one (
dont make the reverse).
Add the desired ... up to volume.
Frequently the final mixture is not clear. What is the reasonbehind this?
What can you do, if the obtained solution is cloudy?
What is the role of Glycerin; Syrup;
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Sorbitol & Propylene glycol in in
Elixir Formulation?1. Contribution ...of the
Hydro-alcoholic solvent;
2. Assist the ...of thesolute;
3. ...of the preparation4. ...of the formulation.
Non-Medicated elixirs in extemporaneouspreparations:
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preparations:1. Addition of a drug ...vehicle;
2. Dilution of an ...( amount of alcoholmust be equal in the two elixirs).
The selection of a vehicle depends on:...& ...of the drug in both
...& ....
The amount of alcohol must be onlyslightly above the amount which is
required to:1. ...
2. ...of the drug.
Flavors, Colors and all components must be
compatible.
Medicated Elixirs
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Usually most elixirs contains only
...single therapeuticagent.
Physician prefer this kind of elixir.
What is the advantage of having asingle drug in the elixir?
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Phenobarbital elixirs
Page 247
Digoxin elixir & figures. Page 251
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