01 Pharmaceutics II

50
‫هذا العمل ال يغين عن حضور المحارضة‬
5 ‫جـ‬## ‫ وجــــه‬:‫السعر‬
Pharmaceutical solutions ‫جـ‬## ‫ وجهني‬:‫السعر‬

Pharmaceutical solutions
• Solutions: are dosage forms prepared by dissolving the active ingredient(s) in an aqueous or non aqueous
solvent.

non aqueous ‫أو‬aqueous ‫ عبارة عه محلول كل المواد ايل فيه بتكون دايبه سواء كاىت يف مزيب‬solution ‫ ال‬

• Solutions can be formulated for different routes of administration:-

-:‫ ليها ا كتر مه طريقه تتاخذ بيها‬solutions ‫ال‬

 Orally: Syrups, elixirs, drops )‫(بيكون يف ػورة دواء طرب أو قطرات‬

 In mouth and throat: mouth washes, gargles, throat sprays.
local effect ‫بيكون يف ػورة مؾمؾه للفم أو للحلق ويف الحاله دي بيكون له‬ 
 In body cavities: douches, enemas, ear drops, nasal sprays.
)‫(بيتاخذ يف تجاويف الجسم زي الحقوة الضرجية و قطرات األىف واالرن‬ 
 On body surfaces: collodions, lotions.
‫بتتذهه علي سطح الجلذ زي اللوطه‬ 
 Oral route give systemic effect due to drug absorption from GIT.
 Solubility is of great importance in solution preparations

‫الن الزو كم انمواد اني فيه تكون دايبه‬solution ‫مهمه في حانه ال‬solubility ‫ ال‬

Advantages of solution Disadvantages of solution

1) Easier to swallow therefore easier for : 1) Bulky therefore difficult to transport and
 children(pediatric) store.
 old age(geriatric) ‫ بتكون حجمها كبير ػعب ىاخذها معاىا يف اي مكان‬

2) More quickly effective than tablets and

capsules
‫بيمتع بسهوله اسرع مه التابلت والكابسول الن اوريذي كل‬ 
‫المواد ايل فيه بتكون دايبه ف هتمتع علطول مص لسه‬
‫هتتكسر زي التابلت وكذا‬
3) Homogenous (one phase system) therefore
give uniform dose (don’t need shaking).
‫ مص بوحتاج ىرجه قبل االستخذام الن كذا كذا دايب‬
4) Dilute irritant action of some drugs (aspirin,
Kl, KBr) minimize adverse effects in the GIT
like KCl
aspirin , kl, ‫ زي‬GIT ‫ يف ال‬irritation ‫لو عوذي مواد بتعمل‬
‫علضان تخفف االلتهابات ايل بتعملها‬solution ‫بحؾرها يف ػورة‬kBr
‫ دا حغله حاجه عه طريق اين‬solution ‫ بستدل عهي ان ال‬
2) Unpleasant taste or odors are difficult to
mask.
‫بس ببقا واخذ‬syrup ‫ ساعات بيكون ليها طعم مر ف بحط معاها‬
‫بايل اىه بوسب معيوة مص بحط كذا وخالظ ف ممكه يفؾل يف‬
‫طعم مر بردو‬
3) Needs an accurate spoon to measure the
dose.
4) Less stable than solid dosage forms.
‫بتكون اقل ثباتيه مه التابلت مثال ألىها بتكون معرؿه ان يحغلها‬ 
‫او ممكه يحغل للسكر ايل فيه‬hydrolysis ‫أو‬oxidation
‫علي فوهه السجاجة‬crystallization
 major signs of instability : color change,
precipitation, microbial growth, chemical gas
formation
‫بالحع تغيير يف اللون أو ترسيب أو تكون غازات‬

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 Pharmaceutics II solutions 01

Solubility of inorganic molecules:

 Both cation and anion that are monovalent are very water soluble e.g. NaCl , LiBr , KI
 Only one of the two ions is monovalent: water solublee.g. BaCl2, MgI2, Na2So4
 Both ions are multivalent: poor water solubility e.g. CaSo4, BaSo4, except ZnSo4 and FeSo4
‫ مص بتذوب‬multivalent ions ‫ بتذوب اما ال‬monovalent ions ‫ال‬ 
 Common salts of alkali metals (Na, K, Li) are water soluble except Li2Co3
 Ammonium and QAS are water soluble
 Nitrate, nitrite, acetate, chlorate, and lactate are water soluble except silver and mercury acetate
 Sulfate, sulfite, thiosulfate are water soluble except calcium and barium salts
 Hydroxides and oxides are water insoluble except alkali and ammonium salts
 Sulfides are water insoluble except alkali metal salts
 Phosphates, carbonates, silicates, borates and hypochlorites are water insoluble except their alkali
metal salts and ammonium salts

Solubility of organic molecules:

 Molecules have one polar gp are water soluble (up to 5 carbon chain length)
 Branched chains are more soluble than straight one
‫مع‬contact ‫ علي بعؾه وبالتايل بتسود ال‬compact ‫ ألىها بتموع ان المركب يكون‬straight ‫ مه ال‬solubility ‫ بتكون ا كتر‬branched chain ‫ال‬ 
solvent ‫ال‬
 Water solubility decrease with increasing molecular weight
 Solubility increase with increasing structural similarity between solvent and solute
solubility ‫ وهيسود ال‬interaction ‫ طبهه بعؽ يف التركيب دا هيخلي يف بيوهم‬solute ‫ و‬solvent ‫لو ال‬ 
 Other solvent properties required for solution preparation include: clarity, low viscosity, compatibility
with other formulative ingredients(additives), chemical inertness, palatability(good taste), odor, color and
economy.
‫و يكون له طعم مقبول‬additives ‫ و اللسوجه بتاعته قليله ويكون بيذوب المواد ايل بتوؾاف عليه زي ال‬clear ‫اىه يكون‬solvent ‫خغائع ال‬ 
‫ورائحة ولون كويسيه و يكون رخيع‬
 Water possess all these properties
‫فيها كل الخغائع دي‬solvent ‫الماء ك‬ 

Alcohol, glycerin and propylene glycol are the most commonly used auxiliary solvent (same properties and
increased stability)
Acetone, ethyl oxide and isopropyl alcohol are toxic so avoided in solution preparation
‫بيكون‬toxic ‫في حانه نو‬oral ‫نكه ممكه عادي يكون‬topical ‫زي‬isopropyl alcohol
Fixed oils as corn oil, cottonseed oil, peanut oil and sesame oil are used as solvent for oleaginous injection
for prolonged action
‫يف الوريذ ) علضان بتطلع‬oil ‫الن ميوفعص احقه‬intramuscular ‫ وغالبا يف الحقه (خغوػا يف ال‬non aqueous vehicle ‫ك‬fixed oil ‫يستخذم ال‬
‫الذواء ببطء وبالتايل تأثيرها بيفؾل مذة اطول‬

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 Pharmaceutics II
Pharmaceutical solvents
1) Alcohol (ethyl alcohol) (ethanol)
 Together with water (hydro-alcoholic mixture)
used as solvent for both alcohol-soluble and
water-soluble substances
‫ممكه ىستخذم كحول مع ماء ويف الحاله دي علضان ادوب المواد‬
‫ايل بتذوب يف الكحول أو الماء‬
‫ بيحسه الزوبان للمواد ايل‬cosolvent ‫وبوستخذم الكحول بردو ك‬
‫مص بتذوب يف الماء‬
 Alcohol USP is 94.9- 96%
 Dehydrated alcohol is 99.5%
 Due to its miscibility with water used to
dissolve many water-insoluble ingredients
including drug substances, flavorants,
antimicrobial and preservatives.
 Used as antimicrobial or combined with other
as parabens, benzoate and sorbates
 Potential toxicity of alcohol restrict its use :
product used for children under 6 year with
alcohol limit of 0.5%, children 6-12 years age
alcohol limit is 5% and older ages 7 and adults
alcohol limit is 10%
‫ لالطفال‬%5.0 : ‫ ف بيتاخذ بوسب معيوه‬toxic ‫ الكحول ممكه يبقا‬
‫ لالطفال‬%٢١ ، ‫ سوة‬٢١ ‫ ايل‬٦ ‫ لالطفال مه‬%٥ ، ‫ سووات‬٦ ‫تحت‬
‫ سويه أو البالغيه‬٧ ‫ا كتر مه‬ ‫يعوي كحول ؿيفوا عليه حاجة‬Denaturated Alchol
2) Diluted alcohol:
 Mixture of water and alcohol 1:1 (the resulting
volume not Equal the sum of two due to
contraction of the liquid upon Mixing) give
solution volume of 3% less
 Used for hydroalcoholic preparations
‫بيه كحول وماية بوسبة واحذ ايل واحذ بيبان معاىا ان‬mix ‫ بوعمل‬  Clear syrupy solution with sweet taste, used as
liquid‫يف ال‬contraction ‫الوسبة مص كذة ىتيجة ان حغل‬
5) Isopropyl rubbing alcohol:
 70% concentration, water, with or without color 
Additives, stabilizer, perfumes  Solvent used as a substitute for glycerin due to its
 Used external as rubefacient, disinfectant for
Hypodermic needle in diabetic patients
solutions 01
3) Alcohol rubbing:
 It is prepared from a special denatured alcohol
solution and contains approximately 70% by
volume of pure, Concentrated ethanol or
 isopropyl alcohol.
‫ كحول والبايق ماية‬%٧١ 
  Rubbing alcohol has cooling, soothing application
for bedridden patients and athletes.
‫بوستخذمه كملطف للواس طريحي الفراش‬ 
 It is used for cleansing surgeons’ hands and
instruments and for the disinfection of skin prior
to penetration by a Hypodermic needle and as an
antiseptic.
rubefacient ‫كمان بوستخذمه كمطهر قبل الحقه وبوستخذمه ك‬ 
‫عه‬mild irritation in the skin and cause ridness ‫يعوي بيعمل‬
‫هيحسه‬ ‫وبالتايل‬dilation in capillers ‫حغل‬ ‫ان‬ ‫طريق‬
skeletal pain‫لل‬relive ‫ودة هيعمل‬circulation ‫ال‬
Rubbing alcohol used as rubefacient because it
evaporates Quickly and is used to cool and soothe
skin.
 Denatured alcohol or methylated spirits is ethanol
that has Additives to make it undrinkable (it may
be dyed).

oral ‫فمبقاش يوفع استخذمه يف حاجة‬
 Methanol is commonly used to make it difficult to
use Distillation or other simple processes to
reverse the denaturation (its boiling point is close
to that of ethanol and it is toxic).
4) Glycerin:
 Used in many internal and external preparation
stabilizer
 Miscible with water and alcohol
 Solvent as alcohol but due to its viscosity solute
dissolve in it Slowly (otherwise heated
‫لو سخوا الجلسيريه اللسوجة هتقل طوية فهيسرع عمليه الزوبان‬
6) Propylene Glycol:
Miscible with water and alcohol
Viscosity
viscosity‫ قريب اوي للجليسرول بس بيبقي اقل يف ال‬
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 Pharmaceutics II solutions 01

Waters
 Water is used both as vehicle and as a solvent for the desired Flavoring or medicinal ingredients.
Advantages: tasteless, odorless, lack of pharmacological activity, neutral (or slightly acid or alkaline) and
very cheap
‫الماية هي اهم وا كثر طيوعا مه اللي فاتوا‬ 

1) Tap Water: 3) Water for injection

 Contains less than 0.1% (100 mg) of total
solids (evaporate 100 ml and weight)
 It is not permitted to use tap water for the
dispensing of Pharmaceutical dosage forms or
for extemporaneous Compounding due to its
possible bacterial contamination and The
presence of dissolved salts that destroy the
active Ingredients or enhance their
decomposition (precipitation, Discoloration,
effervescence).
 It is used in washing, extraction of crude
vegetable drugs and in certain product for
external use
 Must be used for the formulation of parentral
solutions.
‫وبوستخذمها‬purified water ‫ دي بتبقي اىقي ا كتر كمان مه ال‬
pyrogen free ‫غالبا يف الحقه والزم تبقي‬
 It is obtained by sterilizing pyrogen-free distilled
water.
 Note
 Hard” waters are those that contain the Ca and
Mg

‫يف‬ ‫استخذمها‬ ‫ميوفعص‬ ‫الحوفية‬ ‫ماية‬Tap water  soft ‫و‬Hard ‫يف ىوعيه مه الماية‬ 

‫الىها اػال مص مواسبة‬pharmaceutical dosage form ‫ال‬ ‫لو جيت تغسل ايذك بيها‬metals ‫دة بيحتوي علي‬Hard water 

‫العادي كمان اػالوفيها امالح ومواد تاىية ممكه تذمر المواد‬ ‫دي وال‬metals ‫مص هترغي عضان بيحغل تفاعل بيه ال‬

‫ممكه بقي‬instability ‫الفعالة وتعملها اي طكل مه اطكال ال‬ metals ‫دة مفهوش ال‬soft water‫لكه ال‬surface active agent

purification ‫ىستخذمها لو هوعملها‬ ‫دي فذة اللي بوستخذمه عادي‬

Freshly Boiled and Cooled Water: ‫ماية غليتها‬

‫وبردتها لكه مص هقذر استخذمها برؿو يف التحؾيرات الذاوئية‬  Alkaline waters are those that contain
bicarbonates as The major impurity.
 Boiling is used to destroy vegetative bacteria.
But, on Storage for long time spores may yield
 Ultraviolet energy, heat or filtration
vegetative Microorganism
(Milliporefiltration) Can be used to remove or
kill the microorganisms present in the water
2) Purified Water
 Must be used for most pharmaceutical
operations and in All the tests and assays.
‫دي اللي بوستخذمها عادي يف التحؾيرات لكه لو هتتاخذ‬ 
‫الزم يكون فيها معالجة ا كتر وادق‬parental
 Such water is prepared by distillation,
deionization or reverse osmosis.
‫ فوضيل الضوائب او‬distillation‫بوحؾرها عه طريق ال‬ 
Reverse osmosis ‫ىضيل اي ايوىس موجودة او‬deionization
 Free of solid impurities (contain not more than
0.001 % Salts i.e. 1 mg when evaporated)
 Purified water is 100 times more free of
dissolved solids Than is water

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 Pharmaceutics II
Preparation of purified water:
Prepared by:
1- Distillation. 2- Ion-exchange method.
1)Distillation method
1. Prepared using stills of varying capacities (0.5
– 100 gallons/h).
2. The first portion to be discarded as it
contains many foreign volatile substances.
3. The last portion also must be discarded as it
contains decomposed solid impurities that
would contaminate the previously collected
portion of distillate.
 Distillation method is one of the most
common, cheap and available method to be
used at water purification ‫لكوها أقل جودة مه‬
‫الطريقتيه اللي هوتكلم عوهم كمان طويه‬
2)Ion - exchange method
 Have the advantages of:
1. No requirement of heat, less maintenance cost,
eases operation and simpler equipment.
2. Involve the passage of water through a
column of cation or anion exchangers that
consisting of water insoluble, synthetic,
polymerized phenolic, carboxylic, amino or
sulfonated resins of high molecular weight
3. This process is known as softening of water
with high mineral content.
4. The two processes are successively or
simultaneously employed to remove both
anions and cations from water
5. Water obtained is referred as deionized or
demineralized water
solutions 01
3- Reverse Osmosis
‫ احوا بوذخل المياه ىف جهاز‬،‫ىبزة بسيطة كذا عه عملية التقطير‬ 
‫ بعذيه بتتكثف واخر حاجه‬، ‫ بوغليها فطبيعي تبتذى تتبخر‬، ‫التقطير‬
‫بتتحول لمياه تاين بس المرادي المياه بقا بتكون مقطرة متوقعة مه‬
boiling point ‫أي محتوى كان فيها عه طريقة االختالف يف ال‬
‫ لتر‬8.3 ‫ يكاًف‬gallon ‫ال‬ 
‫ احوا‬،‫ىاخذ بالوا أن أول جسء وآخر جسء بيطلع مه عملية التقطير‬ 
.‫بوتخلع موه مص بوكون محتاجيه ليه‬
‫ بيبقي معايا جهاز بسيط بوقي وبقطر‬distillation ‫يف طريقة ال‬ 
‫ لما ا كون عاوز اعمل توقيه أ كثر بذخله علي أجهسة‬،‫موه المياه‬
‫ برده صيادة‬filtration ‫ بيعمل‬HLBC ‫ ا كتر زي ال‬sensitive
‫فالتوقية بتشيذ ا كثر‬
Deionization ‫ بال‬Ion exchange method ‫بوسمي ال‬ 
Demineralization method ‫او‬method
: ‫ ودي عبارة عه‬Ion exchange resin ‫الطريقة دي بتعتمذ علي ال‬ 
 Ion exchange resin: cross linked organic polymers,
microporous in nature, carrying exchange ions.
‫ الغير مرغوب فيه مه المياه وبتوقي المياه موها‬ions ‫يعوي بتاخذ ال‬ 
.‫ تاىية‬ions ‫وبتبذلها ب‬
‫ بيحتوي على مواد‬hard water ‫احوا مه طوية كوا واخذيه ان ال‬ 
‫ فحوا بقا بوستخذم‬Mg ‫ وال‬Ca ‫معذىية بضكل كبير زي مثال ال‬
‫ ىضيل االيوىات دي وتتحول‬، Ion exchange method ‫معاهم ال‬
soft water ‫المياه بقا ل‬
deionized or ‫ دي بسميها بال‬method ‫المياه المتوقية بقا مه ال‬ 
‫ باعتبار ان طيلت االيوىات اللي مص‬demineralized water
.‫عايسها وبذلتها بايوىات تاىية‬
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 Pharmaceutics II solutions 01

‫ عمود بيحغل‬، ‫فكرة الغورة بكل بساطة اىه بيكون عوذي عموديه‬ 
anion ‫ اللي بتحمل طحوات سالبة بسميه بال‬anions ‫فيه تبادل لل‬
‫ اللي يهموي فيه تواجذ مجموعة الهيذروكسيل‬، exchange column
.OH
‫ اللي بتحمل‬cations ‫وعوذي عمود تاين بيحغل فيه تبادل لل‬ 
‫ اللي‬cation exchange column ‫طحوات موجبة بسميه بال‬
. H ‫يهموي فيه تواجذ مجموعة الهيذروجيه‬
Ion ‫ بقا هم دول اللي بيعملوا ال‬OH ‫ وال‬H ‫مجموعات ال‬ 
‫ التاىيه اللي بكون عاوز اتخلع موها وافلتر‬ions ‫ مع ال‬exchange
. ‫المياه موها‬

H ‫ اللي بيكون موجود فيها مجموعات ال‬cation exchange column ‫ دخلت علي ال‬Raw water ‫ عوذىا ال‬، ‫دلوقت بقا يف المثال اللي موجود‬ 
،‫ يكملوا عادي‬Cl ‫ وال‬SO4 ‫ وتسيب بقا ال‬، Ca ‫ وال‬Na ‫ هتبتذي تاخذ االيوىات اللي عليها ىفس الضحوة الموجبة اللي هم ال‬، ‫الموجبة‬
‫ و تتحذ مع‬، ‫ اللي فيه مجموعات الهيذروكسيل السالبة تبتذي تاخذهم بقا‬anion exchange column ‫ رايحيه علي ال‬Cl ‫ وال‬SO4 ‫يقوموا بقا ال‬ 
.‫ كاىت داخله يف االول‬minerals ‫ او‬ions ‫ مياه متوقية مه اي‬،H2O ‫ اللي كان معذي عليها ويطلعلي‬H+ ‫ال‬
. Ion exchange resin ‫ بيعتمذ علي تواجذ ال‬Ion exchange method ‫ىفتكر مع بعؽ ان احوا قولوا ان ال‬ 
،cation exchange column ‫ يف ال‬cation exchange resin ‫ وعوذىا‬، anion exchange column ‫ يف ال‬anion exchange resin ‫فاحوا بقا عوذىا‬ 
، ‫ اللي اخذهم مه المياه عضان يطلع مياه متوقية‬ions ‫ وال‬minerals ‫ دا يبتذي يتضبع بال‬columns ‫ اللي موجود يف االتويه‬resin ‫المهم بقا لما ال‬ 
‫ فيبتذي بقا كفاءة ال‬، dil HCl ‫ ب‬cation column ‫ و بوقي ال‬dil NaOH‫ ب‬anion column ‫ فعضان كذا بوقي ال‬،‫كفاءة طغل الجهاز بتقل‬
.‫ ترجع تشيذ تاين وارجع استخذمها يف مرة تاىيه لتوقية المياه‬method

3)Reverse osmosis
‫الطريقة دي مه أ كثر الطرق كفاءة يف توقية المياه بضكل عايل‬ 

1. RO is a membrane technology filtration method that removes many types of large molecules and ions
from solutions by applying pressure to the solution when it is on one side of a selective membrane (semi
permeable membrane).
2. The result is that the solute is retained on the pressurized side of the membrane and the pure solvent is
allowed to pass to the other side.
3. To be "selective," this membrane should not allow large molecules or ions through the pores (holes) but
should allow smaller components of the solution (such as the solvent) to pass freely.
4. RO removes all virus, bacteria, pyrogens, organic molecules and 90 – 99% of all ions

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 Pharmaceutics II solutions 01

Osmosis: Reverse osmosis:

‫ اىه بيبقي عوذي اتويه‬osmosis ‫اللي بيحغل يف ال‬
، ‫واحذ بيكون محلول مخفف والتاين محلول مركس‬solutions
semi permeable ‫بيكون بيوهم غضاء طبه موفز اللي هو ال‬
‫ ومص بيعذي ال‬pure solvent ‫ دا بيعذي ال‬،membrane
‫ معيه علي حسب ال‬range ‫ كل دا تبع‬، ‫الكبيرة‬molecules
. ‫بتاعت الغضاء‬pores size
‫فاللي بيحغل بقا ان المياه بتتحرك مه تركيسها العايل (اللي‬
)‫فيها أمالح قليله) لتركيسها القليل اللي( فيها امالح اعلي‬
water flow ‫وىاخذ بالوا مه اتجاه ال‬
 ‫ بقا مه اسمها هي عكس طريقة ال‬reverse osmosis ‫يف ال‬ 
‫ يف جسء‬pressure ‫ ل‬apply ‫ اللي بيحغل اين بعمل‬،osmosis
‫ اللي هو بيبقي عوذه امالح‬concentrated solution ‫ال‬
، ‫ فكوتيجة مه تطبيق الؾغط دا‬، ‫وجشيئات ا كتر ومياه اقل‬
، osmosis‫ عه اتجاهه يف ال‬water flow ‫هيوعكس اتجاه ال‬
‫ سايبه فيه‬concentrated solution ‫فتتحرك المياه بقا مه ال‬ 
 ، ‫اي جشيئات او ايوىات او امالح او خالفه وتروح للجهة التاىية بقا‬
‫ بس‬pure water ‫بحيث تكون محتوية علي‬


Additives:
 To resist any change in pH.
Buffers stability ‫ عضان ىحافع علي ال‬، ‫ ثابتة متتغيرش‬ph ‫بتحافع علي ال‬ 
1. Solutions for injection
2. Application to mucous membrane
3. Large-volume solutions for ophthalmic application
4. Most widely used isotonicity modifiers are: dextrose with 5% conc. and NaCl
Isotonicity modifiers: with 0.9% w/v conc.
hypo ‫ ولو هي‬، )‫ (اىكماش‬shrinkage ‫ معواه ان الخلية بيحغلها‬hypertonic ‫ىفتكر مع بعؽ ان‬ 
. ‫ واىتفاخ للخلية‬swelling ‫ بيحغل‬tonic

 It is difficult for aqueous-based topical solutions to remain on the skin or in

the eye,
Viscosity enhancement:
Therefore low concentrations of jelling agents are added to increase the
viscosity of the product.

Preservatives
 Solution may become contaminated for a number of reasons:-
‫اللي بوحؾرها دي ممكه تبوظ وتبقي غير ػالحه الستخذام طيب ده لعذه أسباب اول حاجه‬sol‫ال‬ 
1. Raw materials used in the manufacture of solutions are excellent media for bacterial growth (such as
gums ,dispersing agents, sugars and flavors(
‫اللي بحطه علضان احسه الطعم وغيرها مه المواد واللي‬flavor‫وال‬gum‫زي ال‬sol ‫دي وهي المواد اللي احوا بوستخذمها واحوا بوحؾر ال‬row‫ال‬ 
‫هيبقي غير ػالح لالستخذام‬sol ‫بتبقي وسط مواسب للومو البكتريا ف بالتايل ال‬
2. Equipment, environment and personnel contribute to product Contamination
‫تاين حاجه بقي وهي ال االدوات اللي اىا بستخذمها واىا بحؾر والبيئات اللي حواليا‬ 
3. Consumer use may results in the introduction of Microorganisms
‫تالت حاجه بقي وهي استهالك المريؽ رات ىفسه تكرار الفتح والقفل اعرؼ المحلول للؾوء الحاجات دي ممكه تأثر يحغل ا كسذه المحلول ف‬ 
.preservatives‫بكذه مص هقذر استخذمه وعلضان األسباب دي اىا يستخذم ال‬
 Preservative used should be :
effective against a wide spectrum of microorganisms, stable for its shelf life, non toxic, non sensitizing,
compatible with the ingredients in the dosage form, has no taste and odor.
-: ‫دي زي اي‬preservatives ‫طيب ال‬

7
 Pharmaceutics II solutions 01

Alcohols Esters
 Ethanol is useful as a preservative when it is used  Parabens are esters (methyl, ethyl, propyl and
as a solvent. it needs a relatively high concentration butyl) of p- phydroxybenzoic acid .
(> 10%) to be effective  They are widely used in pharmaceutical
products, they are effective and stable over a
‫وده اقذر استخذمه ك مزيب وف‬ethanol‫اول ىوع عوذىا ال كحول زي ال‬ pH range of 4 to 8 .
‫الزم تركيسه يبقي ا كتر مه عضره‬preservative ‫ىفس الوقت‬ ‫ ده يبقي استر وده ليه حاالت كتير‬preservative ‫ممكه كمان ال‬ 
٤ ‫ايل‬٨ ‫مه‬ph ‫استخذمه فيها بيبقي فعال ا كتر ف‬
 They are employed at concentrations up to
 Propylene glycol also used as a solvent in oral about 0.2%
solutions and topical preparations. it can function as ‫مه عضره‬١ ‫ بوستخذمه بتركيس قليل حوايل‬
a preservative in the range of 15 to 30%. it is not  frequently 2 esters are used in combination:-
volatile like ethanol 1. To achieve a higher total concentration
2. To be active against a wider range of
microorganisms
‫يف ىفس‬preservative ‫ استر مع بعؽ ك‬١ ‫احوا ممكه ىستخذم‬ 
‫ف حاله اين احؾر حاجه‬preservative ‫وده بردوا الكحول بستخذمه ك‬ ‫التحؾيره طيب هوعمل كذه ليه‬
‫علي الجلذ الىها مص بتطاير زي‬application ‫يعوي حاجه ىعملها‬topical ‫اول حاجه عضان تسود تركيسه ف المحلول اللي عوذي تاين حاجه‬ 
‫االيثااىول‬ ‫عضان اققذر اخليه فعال ع البكتريا ف ىطاق واسع‬

Acids QuaternaryAmmonium Compounds

 Benzoic acid and sorbic acid have low solubility in 
water
 They are used in a concentration range from 0.1% 
to 0.5%.
 Only the non-ionized form is effective and therefore
its use is restricted to preparations with a pH below 
4.5
‫ممكه كمان يبقي طبيعته حمؽ زي البوسويك والسكوربك بس‬
‫دوابوهم قليل ف المياه بوستخذمه بتركيس قليل جذا بوستخذمه ف‬
‫وىع‬٤ ‫فيها اقلل مه‬ph ‫التحؾيرات ال‬
Benzalkonium chloride is used at a relatively
low concentration 0.002 to 0.02% .
This class of compounds has an optimal
activity over the pH range of 4 to 10 and is
quite stable at most temperatures .
Because of the cationic nature of this type of
preservative it is incompatible with many
 anionic compound
‫ده اخر ىوع معاىا مه ال‬preservative ‫بوستخذمها بتركيس قليل جذا‬
‫بتبقي مواسبه ف معغم درجات الحراره‬

Antioxidants
 Vitamins, essential oils & almost all fats and oils
can be oxidized .
 Oxidation reaction can be initiated by :
1. Heat: maintain oxidizable drugs in a cool place
2. Light: use of light- resistant container
3. Heavy metals (e.g. Fe, Cu): effect of trace metals
can be minimized by using citric acid or
ethylenediamine tetraacetic acid(EDTA) i.e.
suspending agent.
‫الفيتاميوات والشيوت والذهون كل دي حاجات ممكه يحغلها‬ 
‫ا كسذه ومه الحاجات اللي بتسببلي ان يحغل ا كسذه دي‬
‫الحراره مثال وىتجوبها باىوا ىحط المحلول يف مكان بارد‬
‫تاين حاجه تسبب ا كسذه هي الؾوء ف ىحط المحلول يف زجاج‬ 
‫عازل للؾوء‬
‫تالت حاجه ممكه تسبب ا كسذه المعادن زي الحذيذ و الوحاس‬ 
‫علضان تمسك ف‬edta ‫ف بموع ده باين احط سيترك اسيذ او‬
‫المعادن دي وتعمل كومبلكس معاها ف متأكسذليص المحلول‬

 Antioxidants as propyl & octyl esters of gallic ‫اللي ف المحلول او‬metal ‫ اخر حاجه علضان اعمل عسل لل‬
acid, tocopherols or vitamin E, sodium sulfite, edta ‫اقللها استخذم السيترك اسيذ او ال‬
ascorbic acid (vit. C)
 Advantages: Colorless, highly water soluble,
stable over a wide pH

8
 Pharmaceutics II solutions 01

Sweeting agent Flavours and perfumes

 Sucrose is the most widely used  Mask unpleasant taste or odor

sweetening agent .
 Advantages: Colorless, highly water  Enable the easy identification of the
soluble, stable over a wide pH range (4-8), product .
increase the viscosity, masks both salty and
bitter taste ,has soothing effect on throat  Natural products: fruit juices,
‫دي المواد اللي احوا بوؾيفها علي التحؾيره علضان تخفي اي طعم‬ aromatic oil ) peppermint, lemon(
‫مر ويبقي طعمها مقبول وخغوػا لألطفال مه ؿموها ال سكروز‬
‫وده ا كتر واحذ بيستخذم الن مه مميساته اىه طفاف بيذوب ف المياه‬
‫ بيكون اللسوجه وبيخفي طعم الذوا المر‬٨ ‫ايل‬4 ‫مه‬pH ‫مستقر ف‬
 Artificial perfumes are cheaper, more
readily available and more stable than
‫وبيبقي ليه تأثير على الحلق‬
natural product
 Polyhydric alcohols (sorbitol, mannitol
and glycerol) possess sweetening power ‫مه اسمها كذه هتعرف ان هي بتخفي اي طعم او ريحه مص‬
and can be used for diabetic preparation
‫مستغاغه ىف المحلول بتاعي وممكه تكون حاجه طبيعيه اجبها‬
‫وخاػه ف‬sweeting agent ‫المواد دي بوستخذمها برده ك‬
‫مه الفاكهة مثال او الشيوت الطبيعيه اللي ليها روائح وممكه‬
‫تحؾيرات مرؿي السكر‬
‫تكون حاجه مغوعه زي العطور ودي بتبقي متاحه ا كتر مه‬
‫المواد الطبيعيه واقتغاديه عوها كمان‬

Classification of solutions
Aqueous solutions
 Homogeneous mixtures that are prepared by dissolving a solid, liquid or gas in an aqueous medium
(vehicle)
 Vehicle: This may be water, aromatic water or extract
‫يعوي اي يعوي ابقي جايب حاجه بودر او سائل او غاز وادوبها ف المياه او ممكه الحاجه‬aqueous ‫ده ممكه يكون‬sol‫ طيب ال‬
aromatic water ‫تبقي مستخلع او‬vehicle‫اللي اىا هذوب فيها اللي هي ال‬

Non-aqueous solutions
 Used for water insoluble and poorly soluble materials.
 Used for materials that are unstable in aqueous media
‫ وده ف حاله ان المواد اللي اىا هذوبها دي مص بذوب ف المياه او غير مستقرة فيها‬non aq‫ ممكه بردو المحلول ده يبقي ىوعه‬
non-aqueous ‫علضان كذه بزوبها ف حاجه غير المياه وعلضان كذه سميتها‬
‫ولو حاجه غيرها‬aqueous ‫ لو مياه يبقي‬vehicle‫وده علي حسب ىوع ال‬nonaqueous ‫و‬aqueous‫ل‬solution‫ ىعرف ان بقسم ال‬
non aqueous ‫يبقي‬

9
 Pharmaceutics II solutions 01

Aromatic waters
 Aromatic waters (medicated waters) are clear, saturated aqueous solution of volatile oils or other volatile
substances.
 They are used principally as flavored or perfumed vehicles.
 Volatile oils solutions represent an incompatibility problem of salting out (this occurs after the
incorporation of a very soluble salt in their solution).
very water ‫ ف اجي اؿيف‬aquas solution ‫ ببقي مذوبه بالعافيه بمساعذه الكحول مثال يف المياه الىها‬volatile oil ‫اىا عوذي ال‬ 
soluton ‫ (تعكير ) لل‬turbidity ‫ ويطردها ويعمل‬solding out ‫ هيعملها‬soluble salt
 Aromatic water will deteriorate with time therefore: -

 Should be made in small

‫ كبيره وعضان استخذمها واخلغها بسرعه قبل ميحغلها حاجه‬oil ‫ اعملها بكميات ػغيره عضان متبقاش كميه ال‬
 Protected from intense light and excessive heat by storing in air tight, light resistant containers.
 If they become cloudy or otherwise deteriorate, they should be discarded (deterioration may be due to
volatilization, decomposition or mould growth).
‫ مذة كبيرة المواد المتطايرة موها بتتبخر ف ساعتها بيتم التخلع موها عضان معادتص توفع خالظ‬aromatic water ‫ لما بتسيب ال‬

 There are 2 official methods of preparation:

(a)Distillation process (Stronger Rose Water NF)

 Most satisfactory method but slow and expensive
 The drug should be coarsely ground and mixed with sufficient quantity of purified water in the distillation
unit.
 If the volatile principle in the water are present in small quantities the distillate is returned several times to
the still with fresh portions of drug.

‫العملية ديه بتتم ب اىوا بوطحه الذواء وىحط عليه المياه المقطرة وبعذ كذا بومرر عليها المواد المتطايرة ديه اللى هي الشيوت الطيارة‬
‫والروائح وكذا ف تقوم ماسكة فيها حتى لو بوسبة قليلة وبوفؾل ىكرر التمرير دا لحذ ما ىسبة المواد الطيارة تتواسب مع ىسبة المياه‬

(b) Solution process (Peppermint water)

 Aromatic water may be prepared by shaking volatile substance with purified water. the mixture is set aside
for 12 hours & filtered.
 Talc (inert) may be used to increase the surface of the volatile substance, insure more rapid saturation of
the water and act as a filter aid
‫يف الطريقه دي بحؾر عه طريق رج الماده المتطايره بالماء الوقي وممكه استخذم عامل مساعذ زي التلك الخامل دا بيؾمه ان‬ 
‫التضبع يبقي سريع وكمساعذ للتغفيه‬

10
 Pharmaceutics II solutions 01

Methods of preparation of solutions

a )Simple solution b)Solution by chemical reaction c)Solution by extraction

(A)Simple solution :-
stirring, heating , complexing agent ‫ممكه احؾره بتلت طرق‬

 Solutions of this type are prepared by dissolving the solute in a suitable solvent (by stirring or heating).

 The solvent may contain other ingredients which stabilize or solubilize the active ingredient e.g. solubility
of iodine is 1: 2950 in water however, it dissolves in presence of KI due the formation of more soluble
polyiodides (KI.I2 KI.2I2 KI3.I3 KI.4I4).
[strong iodine solution USP (Lugol’s solution)].

‫ بتاعته قليله طب ادوبه ازاي بحوله ل كومبلكس ب‬solubility ‫ ومثال علي كذا االيوديه ودا ال‬complex agent ‫ فيه استخذام ال‬
Lugol’s solution ‫ فيذيوي‬KI ‫اؿافه‬
 In addition to heating , reduction of the particle size of the solute will increase the surface area of
substance exposed to the solvent
 For substances that undergo exothermic reaction as they dissolve the use of heat would discourage the
formation of solution such as calcium hydroxide solution (solute is soluble in water to the extent of 140
mg/100ml at 25 oC and 170 mg/100ml at 15 oC) so the temperature of preparation and storage will affect
the concentration of the resultant solution.
‫ دا يعوي طارد للحراره ف التسخيه هيبقي ؿذه والمثال مجرد ىعرفه بذون دخول يف تفاػيل‬exothermic reaction ‫ ال‬

(B) Solution by chemical reaction

 These solutions are prepared by reacting two or more solutes with each other in a suitable solvent e.g.
calcium carbonate and lactic acid used to prepare calcium lactate mixture.
‫ مثال‬salt‫ يذوين‬base ‫ مع‬acid ‫ ماده مع ماده يكوىو ماده ثالثه بتذوب يف المياه زي تفاعل‬

(C) Solution by extraction

 Plant or animal products are prepared by suitable extraction process.

 Preparations of this type may be classified as solutions but more often, are classified as extractives.
active ‫ لل‬extraction ‫ زي مثال اىك تحط الضاي يف مياه مغليه بتاليق لوىه اتغير وطعمه بقي طاي ليه بقا ؟؟ الن حغل‬
tea leaf ‫ ال موجوده يف الضاي ف الحاجات ال بتذوب دابت يف المياه وسابت الحاجات ال مص بتذوب ال هي‬constituents

Pharmaceutical solutions
 Aqueous: Douches, Enemas, Gargles, Mouthwashes, Nasal washes, Juices, Sprays, Otic solutions, and
Inhalations.
 Sweet &/or Viscid: Syrups, Honeys, Mucilages, and Jellies
 Nonaqueous: Elixirs, Spirits, Collodions, Glycerins, Liniments, and Oleo Vitamin

11
 Pharmaceutics II solutions 01

Questions
True & false
1) Solid dosage forms are more stable than solution( )
2) Tablets and capsules are more quickly effective than solution ( )
3) Purified water can be used for injection( )
4) Glecrin can be used as a rubifacent( )
5) We can use isoprpyl alchol as a substitute for glycerin( )
6) Mixture of water and alcohol 2:1 in diluted alchol ( )
7) Ion exchange method is more efficient than the reverse osmosis method at water purification. ( )
8) To purify water by ion exchange method, we distract the first and last portion of water as they contain
impurities( )
9) Distillation method is the most cheap, available method to purify water. ( )
10) At ion exchange method, when the anion exchange resin gets saturated with ions and minerals,we purify it
using dil Hcl. ( )
11) Water obtained from ion exchange method is called demineralized water. ( )
12) To purify water by reverse osmosis, when we apply the pressure, the solvent is moved from high ( )
concentration of water to low concentration of water. ( )
13) Dextrose is considered one of isotonicity modifiers. ( )
14) Benzoic acid has a low solubility in water ( )
15) We can use 2ester in combined as a preservative ( )
16) We can protect solution from oxidation by heating ( )
17) Aromatic oil is artificial perfumes( )
18) Solution by extraction are prepared by reacting two or more solutes with each other in a suitable
solvent()
19) Aromatic waters (medicated waters) are unsaturated aqueous solution of volatile oils or other volatile
substances. ( )
20) heating , reduction of the particle size of the solute will increase the surface area of substance exposed to
the solvent( )
21) We use talc in Distillation process method ( )
22) In Solution process the drug should be coarsely ground and mixed with sufficient quantity of purified
water in the distillation unit( )

Choose:

23) Monovalent ions are water(soluble - insoluble) but multivalent ions are (soluble - insoluble)
24) …..... is considered additives. (Buffers - Isotonicity modifiers - Viscosity enhancement – all of this)
25) Using preservatives protect solution from ( contamination- oxidation )

12