An excipient is generally a pharmacologically inactive substance used as a carrier for the active ingredients of a medication EXCIPIENTS USED IN LIQUID DOSAGE FORMS: Solvents/co-solvents ,  Buffering agents, Preservatives, Anti-oxidants,  Humectants, Wetting agents, Anti-foaming agents,  Thickening agents,  Sweetening agents, Flavouring agents, EXCIPIENTS USED IN TABLETS: Binders Coatings Disintegrants Fillers Flavours Colours Lubricants Glidants Preservatives Sweeteners

1. Pharmaceutical Technology
(PD-705)
Pharmaceutical Excipients
Course Teacher : Dr. Sana Ghayas
1

2. Introduction
By Zara Navaid
Roll no 27
2

3. DEFINITION:
An excipient is generally a pharmacologically inactive substance used as
a carrier for the active ingredients of a medication
3

4. A/c to USP:
“An excipient displays either no pharmacological activity or
very limited and directed activity.”
A/c to BP:
“Any substance added in preparing an official preparation shall
not interfere with the assays and tests of the pharmacopoeia.”
4

5. A/c to Handbook of Pharmaceutical Excipients:
“No longer can excipients be regarded simply as inert or inactive
ingredients and a detailed knowledge not only of the physical and
chemical properties but also of the safety, handling and regulatory
status of these materials is essential for formulators.”
5

6. Why use excipients?
• Excipients are added to aid the formulation and manufacture of the
subsequent dosage form for administration to patients.
• The properties of final dosage form are highly dependent on the
excipients chosen, their concentration and interaction with both
active compound and each other.
6

7. • to bulk up formulations that contain very potent active ingredients
• to allow for convenient and accurate dosage
• to aid in the handling of the active substance
• to aid the manufacturing process
• to protect, support or enhance stability
• for bioavailability or patient acceptability.
• to enhance the overall safety or function of the product during
storage or use.
7

8. EXCIPIENTS USED IN LIQUID DOSAGE FORMS:
❖Solvents/co-solvents ,
❖Buffering agents,
❖Preservatives,
❖Anti-oxidants,
❖Humectants
❖Wetting agents,
❖Anti-foaming agents,
❖Thickening agents,
❖Sweetening agents,
❖Flavouring agents,
8

9. EXCIPIENTS USED IN TABLETS:
❖Binders
❖Coatings
❖Disintegrants
❖Fillers
❖Flavours
❖Colours
❖Lubricants
❖Glidants
❖Preservatives
❖Sweeteners
9

10. Disintegrating Agents
Role In Pharmaceutical Formulation
Development Process
By MUZAMMIL
Roll no. 11
10

11. What are Disintegrating agents?
• Disintegrants or disintegrating agents, which promote breakup of the
tablets after administration to smaller particles for ready drug
• availability
11

12. Role In Pharmaceutical
Formulation Development
Process
12

13. Mechanism of Disintegrating agents
• Capillary action and wicking
• Swelling or distension
• As the result of expansion caused by heating entrapped air
• Disintegrating forces
• Deformation of the tablet
• The release of gaseous materials
• Being triggered by enzymatic action
13

14. Swelling
14

15. Porosity and Capillary Action
15

16. Deformation
16

17. List of Disintegrants
17

18. Super Disintegrates
18

19. Reference
• https://www.lfatabletpresses.com/articles/overview-of-disintegrants
• https://www.sciencedirect.com/topics/pharmacology-toxicology-and-
pharmaceutical-science/disintegrating-agent
19

20. Surfactants And Their Role In
Pharmaceutical Formulation
Development Process
By
Zeeshan Ali Rizvi and Bilal Mazhar Ali
20

21. What are surfactants?
Surfactants are termed as
• Surface-active agents also
• Wetting agents,
• Emulsifying agents or
• Solubilizing agents depending on its properties and use.
21

22. Surface-active agents are substances which, at low concentrations,
adsorb onto the surfaces or interfaces of a system and alter the surface
or interfacial free energy and the surface or interfacial tension.
They are also called amphiphilic molecule because of both hydro-
phillic and –Phobic Nature.
22

23. 23

24. Surface tension
vs
Interfacial tension ??..
24

25. 25

26. HLB System
Griffin devised an arbitrary scale of values to serve as a measure of the
Hydrophilic - Lipophilic Balance (HLB) of surface active agents. HLB is
the ratio of oil soluble and water-soluble portions of a molecule.
26

27. 27

28. Classification
Anionic Oleic acid
FDA approved for inhalation, oral, nasal,
topical,
and transdermal preparations
Cationic
Cetyl pyridinium
chloride
FDA approved for oral, inhalation,
iontophoresis,
and transdermal prepamtions.
Nonionic
Lanolin (wool wax) FDA approved for ophthalmic, topical, vaginal,
and transdermal preparations
Zwitterionic
lecithin (soy bean or egg
yolk)
FDA approved for inhalation, intravenous,
intramuscular, oral, otic, rectal, topical, vaginal,
and transdermal preparations.
28

29. How Surfactants are useful in
pharmaceutical formulation development
process ??
29

30. Lecithin
• Lecithins are also used in suppository bases, to reduce the brittleness
of suppositories.
• Have been investigated for their absorption-enhancing properties in
an intranasal insulin formulation.
• Choline is a required component of fda-approved infant formulas.
Other studies have indicated that lecithin can protect against alcohol
cirrhosis of the liver, lower serum cholesterol levels, and improve
mental and physical performance.
30

31. Oleic acid
• Oleic acid can act as a percutaneous absorption enhancer of several
drugs, as it induces the disruption of the lipid structure of the stratum
corneum, allowing drug permeation.
• This organic acid is able to increase the bioavailability of the corticoids
betamethasone , ketorolac, metronidazole, estradiol.
31

32. Microemulsion – A novel drug delivery system
• the aim of this reported work was to develop and characterize a soy
lecithin-based self micro emulsifying drug delivery system (SMEDDS)
of resveratrol to enhance its oral delivery.
• Use of co-surfactants, electrolytes for microemulsion based drug
delivery system.
32

33. Examples of microemulsion based products
33

34. Reference
• Handbook of pharmaceuticals exepients
• https://www.pharmatutor.org/articles/surfactants-and-its-
applications-in-pharmaceuticals-overview?page=5%2C5
• https://knowledge.ulprospector.com/3106/pc-surface-active-agents-
surfactants/
34

35. COLORING AGENTS
TUBA ALIM
5th Prof, Sem IX, Roll # 28
Course: Pharmaceutical Technology,
Dow College of Pharmacy (DUHS)
35

36. INTRODUCTION:
Coloring agents are used in pharmaceutical preparations for esthetics.
36

37. Why colors are use in Drug Development :
❖Tool for identification
❖For patient acceptability
❖To eliminate errors
❖To increase uniformity
❖Contribute to stability
(Example; iron oxide , titanium dioxide)
37

38. IDEAL PROPERTIES:
• Must not interfere with therapeutic efficacy
• Must not interfere with the prescribed assay procedure for the
preparation
• Must be reproducible
• Stable
• Safe
• compatible
38

39. SELECTION CRITERIA:
❖on the basis of their physical and chemical properties
❖solubility of a perspective dye in the vehicle
❖pH & pH stability of the preparation to be colored
❖must be stable in the presence of other formulative ingredients
❖dyes must be photo-stable
39

40. According to FDA certified color additives are
classified according to their approval use:
❖FD&C Color Additives: may be used in food , drugs and cosmetics
❖D&C Color Additives: some of which are approved for use in drugs,
some in cosmetics, and some in medical devices.
❖External D&C Color Additives: their use are restricted to external
part of the body surface.
40

41. Colors may be classified into:
❖colors soluble in water (dyes): suitable for clear liquid preparations
❖colors insoluble in water (pigments): for surface coloration , due to
their lack of color migration, greater opacity and enhanced color
stability.
41

42. • Beta-carotene
• Indigo carmine
• Sunset yellow FCF
• Tartrazine
42

43. 43

44. Due to safety concern FDA take some steps:
❖FD&C Red No 2 (amaranth) cause cancer in rats so its use has been
stopped.
❖FDA terminated the approval for the use of FD&C Red No 4 in
ingested drugs because of unresolved safety question(use only
externally)
❖FD&C Yellow No 5 (tartazine) cause allergic reactions , most likely in
people who are allergic to aspirin. So, FDA requires listing of this dye
by name on the labels of food and ingested drugs containing it.
44

45. SOLUBILIZING AGENTS
By Ayesha Mahmood
Roll no. 84
45

46. Solubilizing agent:
solubilizing agent helps to improve the solubility of
poorly water soluble drugs often resulting in an
alteration of intestinal membrane barrier function and
intestinal membrane damage.
46

47. Most common solubilizing agents:
• Benzethonium chloride
• Benzyl benzoate
• Cyclodextrin
• Glyceryl monostearate
• Lecithin
• Phospholipids
47

48. Cyclodextrin
Nonproprietary Name: Alfadex Betadex
Chemical name & Molecular Weight:
a-Cyclodextrin 972
b-Cyclodextrin 1135
g-Cyclodextrin 1297
48

49. Description:
Cyclodextrins are ‘bucketlike’ or ‘conelike’ toroid molecules,
with a rigid structure and a central cavity, the size of which varies
according to the cyclodextrin type. The internal
surface of the cavity is hydrophobic and the outside of the torus is
hydrophilic; this is due to the arrangement of hydroxyl groups
within the molecule. This arrangement permits the cyclodextrin to
accommodate a guest molecule within the cavity, forming an
inclusion complex.
49

50. Applications in Pharmaceutical formulation:
Cyclodextrins may be used to form inclusion complexes with a
variety of drug molecules, resulting primarily in improvements to
dissolution and bioavailability owing to enhanced solubility and
improved chemical and physical stability.
Cyclodextrin inclusion complexes have also been used to mask
the unpleasant taste of active materials and to convert a liquid
substance into a solid material.
50

51. Cont…
b-Cyclodextrin is the most commonly used cyclodextrin,
although it is the least soluble. It is the least
expensive cyclodextrin; is commercially available from a number of
sources; and is able to form inclusion complexes with a number of
molecules of pharmaceutical interest. However, b-cyclodextrin is
nephrotoxic and should not be used in parenteral formulations;
b-Cyclodextrin is primarily used in tablet and capsule
formulations.
51

52. Cont…
In eye drop formulations, cyclodextrins form water-soluble
complexes with lipophilic drugs such as corticosteroids. They have
been shown to increase the water solubility of the drug; to enhance
drug absorption into the eye; to improve aqueous stability; and to
reduce local irritation.
Cyclodextrins have also been used in the formulation of
solutions, suppositories, and cosmetics.
52

53. Applications in Pharmaceutical Technology
In oral tablet formulations, b-cyclodextrin may be used in both
wet-granulation and direct-compression processes. The physical
properties of b-cyclodextrin vary depending on the manufacturer.
However, b-cyclodextrin tends to possess poor flow properties and
requires a lubricant, such as 0.1% w/w magnesium stearate, when it
is directly compressed.
53

54. Cont…
In parenteral formulations, cyclodextrins have been used to produce
stable and soluble preparations of drugs that would otherwise have
been formulated using a nonaqueous solvent.
54

55. Safety
❖a-Cyclodextrin
❖LD50 (rat, IP): 1.0 g/kg(15)
❖LD50 (rat, IV): 0.79 g/kg
❖b-Cyclodextrin
❖LD50 (mouse, IP): 0.33 g/kg(16)
❖LD50 (mouse, SC): 0.41 g/kg
❖LD50 (rat, IP): 0.36 g/kg
❖LD50 (rat, IV): 1.0 g/kg
❖LD50 (rat, oral): 18.8 g/kg
❖LD50 (rat, SC): 3.7 g/kg
❖g-Cyclodextrin
❖LD50 (rat, IP): 4.6 g/kg(15)
❖LD50 (rat ,IV): 4.0 g/kg
❖LD50 (rat, oral): 8.0 g/kg
55

56. Glyceryl Monostearate
Chemical Name:
Octadecanoic acid
Empirical Formula and Molecular Weight
C21H42O4 358.6
56

57. Applications in Pharmaceutical Formulation
It acts as an effective stabilizer, that is, as a mutual solvent for polar
and nonpolar compounds that may form water-in-oil or oil-in-water
emulsions. These properties also make it useful as a dispersing agent
for pigments in oils or solids in fats, or as a solvent for phospholipids,
such as lecithin.
57

58. Application in Pharmaceutical Technology
Glyceryl monostearate has also been used in a novel fluidized
hot-melt granulation technique for the production of granules and
Tablet. Glyceryl monostearate is a lubricant for tablet manufacturing
and may be used to form sustained-release matrices for solid dosage
forms.
58

59. Cont…
Sustained-release applications include the formulation of pellets for
tablets or suppositories, and the preparation of a veterinary bolus.
Glyceryl monostearate has also been used as a biodegradable,
implantable, controlled- release dosage form.
59

60. Cont…
When using glyceryl monostearate in a formulation, the possibility of
polymorph formation should be considered. The a- form is dispersible
and foamy, useful as an emulsifying agent or preservative. The denser,
more stable, b-form is suitable for wax matrices. This application has
been used to mask the flavor of clarithromycin in a pediatric
formulation.
60

61. Safety:
LD50 (mouse, IP): 0.2 g/kg
61

62. Lecithin Applications in Pharmaceutical
formulation:
Lecithins are used in a wide variety of pharmaceutical applications.
They are also used in cosmetics and food products. Lecithins are
mainly used in pharmaceutical products as dispersing, emulsifying,
and stabilizing agents, and are included in intramuscular and
intravenous injections, parenteral nutrition formulations, and topical
products such as creams and ointments.
62

63. Application in Pharmaceutical Technology
Lecithins are also used in suppository bases,(3) to reduce the
brittleness of suppositories, and have been investigated for their
absorption-enhancing properties in an intranasal insulin
formulation.(4) Lecithins are also commonly used as a component of
enteral and parenteral nutrition formulations. There is evidence that
phosphatidylcholine (a major component of lecithin) is important as a
nutritional supplement to fetal and infant development.
63

64. Cont…
Furthermore, choline is a required component of FDA-approved
infant formulas. Other studies have indicated that lecithin can protect
against alcohol cirrhosis of the liver, lower serum cholesterol levels,
and improve mental and physical performance. Liposomes in which
lecithin is included as a component of the bilayer have been used to
encapsulate drug substances; their potential as novel delivery systems
has been investigated. This application generally requires purified
lecithins combined in specific proportions. Therapeutically, lecithin
and derivatives have been used as a pulmonary surfactant in the
treatment of neonatal respiratory distress syndrome.
64

65. Safety
oral doses of up to 80 g daily have been used therapeutically in the
treatment of tardive dyskinesia.
65

66. Phospholipids Description:
Phospholipids are amphiphilic molecules and are the major component
of most cell membranes. They are able to self- associate and form a
variety of structures, including micelles and liposomes.
66

67. Applications in Pharmaceutical
formulation:
Numerous pharmaceutical formulations use phospholipids to form
various types of liposomes, including unilamellar (one bilayer
membrane surrounding an aqueous chamber), multilamellar (two or
more concentric membranes, each surrounding an aqueous
chamber), and multivesicular (numerous aqueous chambers joined in
a honeycomb-like arrangement) liposomes.(4) Modified
phospholipids have been used to enhance the properties of the
resulting liposomes. The covalent attachment of polyethylene glycol
(PEG) to the phospholipid, or PEGylation, provides steric hindrance to
the surface of the liposomes, resulting in decreased uptake by the
reticuloendothelial system (RES), also known as the mononuclear
phagocyte system, and a prolonged circulation half-life following
intravenous administration; the so-called ‘stealth liposomes.’ 67

68. Application in Pharmaceutical Technology
Conjugation with antibodies produces immunoliposomes, which are
able to target specific cell types and deliver a payload of encapsulated
drug. Phospholipids can be anionic, cationic, or neutral in charge.
Because of their amphiphilic nature, phospholipids will associate at
hydrophobic/hydrophilic interfaces. The charged lipids can be used to
provide electrostatic repulsion and physical stability to suspended
particles. Thus, they have been used to physically stabilize emulsions
and suspensions. Phospholipids have also been used in formulations
administered as lung surfactants, in intravenous fat emulsions, and in
oral solutions (e.g. Rapamune).
68

69. Safety:
LD50 (IV) of 1.1 g/kg and 7.5 g/kg with and without stearylamine
69

70. Preservative
By Sehrish Ayaz
Roll no 52
70

71. Preservative
Preservatives are substances that are commonly added to various
foods and pharmaceutical products in order to prolong their shelf life.
71

72. 72

73. FIRST PRESERVATIVE
The first preservatives to be used were vinegar, salt and sugar.
73

74. Ideal Properties of Preservatives
1. It should not be irritant.
2. It should not be toxic.
3. It should be physically and chemically stable.
4. Preservative should be compatible with other ingredients used in
formulation.
5. It should be act as good antimicrobial agent and should exert wide
spectrum of activity.
6. It should act as preservative in small concentration i.e. it must be
potent.
7. It should maintain activity throughout product manufacturing, shelf
life and usage
74

75. CLASSIFICATION BASED ON
MECHANISM OF ACTION
1. Antioxidants:
• Vitamin E
• Vitamin C
• Butylatedhydroxyanisole ( BHA).
• Butylatedhydroxytoluene (BHT).
2. Antimicrobial agents:
• Benzoates
• Ethanol
• Sodium benzoate
• Sorbates
3. Chelating agents:
• Disodium
ethylenediaminetetraacetic acid
(EDTA)
• Polyphosphates
• Citric acid
75

76. Ethyl Alcohol
• Functional Category: Antimicrobial preservative; disinfectant; skin
penetrant; solvent
76

77. Applications in Pharmaceutical
Formulation or Technology????
• Used as solvent
• Anti microbial preservative
• Penetration enhancer
77

78. Typical Properties:
• Antimicrobial activity Ethanol is bactericidal in aqueous mixtures at
concentrations between 60% and 95% v/v; the optimum
concentration is generally considered to be 70% v/v.
• Antimicrobial activity is enhanced in the presence of eidetic acid or
edentate salts.
• Ethanol is inactivated in the presence of nonionic surfactants and is
ineffective against bacterial spores.
78

79. Benzyl Alcohol
Functional category : anti microbial preservative; disinfectant and
solvent
79

80. • Benzyl Alcohol is an anti microbial preservative used in cosmetics,
foods and a wide range of pharmaceutical formulation. Including oral
and parenteral preparations.
• At concentration up to 2 % v/v
• Concentration up to 3% v/v may be used as preservatives in cosmetics
80

81. Applications in Pharmaceutical
Formulation or Technology?
• Benzyl Alcohol 10% v/v also have some local anesthetic properties
which are exploited in some Parenterals, cough products , ophthalmic
solutions, ointments and dermatological aerosol sprays.
• Although widely used as an anti microbial preservative, benzoyl
alcohol has been associated with some adverse fatal reaction when
administered to neonates.
81

82. Neonatal Deaths Associated With Use Of
Benzyl Alcohol -- United States
82

83. THICKENING AGENT AND SUSPENDING
AGENT
Safia Ahmed
Roll no 23
83

84. DEFINIITON:
“These are the viscosity enhancing agent which is used to reduce the
sedimentation rate of particle In the vehicle .”
They are the hydrophilic colloidal compounds that form colloidal dispersion
with water because of the affinity between the dispersed particle and
dispersion medium.
EXAMPLE:
• Acacia
• Tragacanth
• Bentonite
• Carboxy methylcellulose
84

85. IMPORTANCE: / WHY DOSAGE FORMS
REQUIREDTHICKENING AGENT AND SUSPENDING AGENT
❖It helps to prevent cake formation in suspension .
❖It helps in the formation of stabilized system of deflocculated
system. Used for easy redistribution.
❖Reduce the rate of sedimentation of particles .
❖Uniform dispersion system formation.
85

86. THICKENING AGENT AND SUSPENDING AGENT
TYPES:
• Polysaccharide
• Inorganic salts
• Synthetic
86

87. example of suspending agents in formulation :
The aim of this study was to extend the application of gum extracted from Abelmuscus esculentus
pods (AEG), ripped Chrysophyllum albidium fruit (RCAG) and unripped C. albidium fruit (UCAG) to
pharmaceutical suspensions. The extracted gums, gelatin and compound tragacanth were used to
formulate Paracetamol suspension in concentrations of 0.5 to 4.0% w/v. The sedimentation rates,
sedimentation volume, ease of re-dispersibility and viscosity of the suspension were studied as
assessment parameters. The rank order of the suspending ability of the suspendants as evaluated by
the sedimentation volume was AEG > gelatin > compound tragacanth > RCAG. Suspensions
formulated with RCAG has comparative viscosity with those containing gelatin and compound
tragacanth; however, Paracetamol suspensions having AEG has significantly higher viscosity (p<0.05)
when compared with those containing RCAG, gelatin and compound tragacanth. The flow rate
decreases with increase in the concentration of the suspending agent and increase in the viscosity.
Paracetamol suspensions containing RCAG were easily redispersible with minimum agitation and are
stable enough for adequate dose withdrawal. The viscosity of formulations containing AEG decreases
with increased speed of agitation. On the basis of these findings, pharmaceutical suspension
containing A. esculentus and C. albidium gums as suspending agents may be applied as liquid drug
delivery system for pediatric and geriatric patients
87

88. Gelatin :
• is a glutinous substance made from the bones, connective tissues, and
skins of animals. The calcium is removed and the remaining substance is
soaked in cold water. Then it is heated to 40°C to 60°C (105°F 140°F). The
partially evaporated liquid is defatted and coagulated on glass plates and
then poured into moulds. When solid, the blocks of gelatin are cut into thin
layers and dried on wire netting.
• Gelatin is available in sheets of leaf gelatin, powders, granules, or flakes.
Use it at a 1% ratio. Like some of the other gelling agents, acidity adversely
affects its gelling capacity.
• The quality of gelatin often varies because of different methods of
processing and manufacturing. For this reason, many bakers prefer leaf
gelatin because of its reliable strength.
88

89. Gum Arabic or Acacin
• This gum is obtained from various kinds of trees and is soluble in hot
or cold water. Solutions of gum Arabic are used in the bakery for
glazing various kinds of goods, particularly marzipan fruits.
Gum Tragacanth
• This gum is obtained from several species of Astragalus, low-growing
shrubs found in Western Asia. It can be purchased in flakes or
powdered form. Gum tragacanth was once used to make gum paste
and gum paste wedding ornaments, but due to high labor costs and a
prohibitive price for the product, its use nowadays is uncommon
89

90. Pectin
• Pectin is a mucilaginous substance (gummy substance extracted from
plants), occurring naturally in pears, apples, quince, oranges, and
other citrus fruits. It is used as the gelling agent in traditional jams
and jellies.
90

91. DOSAGE FORM SUSPENDING/
THICKENING AGENT
1 ORAL DOSAGE FORM Acacia, colloidal silicon
dioxide
2 PARENTERAL Colloidal silica ( amphillin )
3 TOPICAL bentonite magma (
calamine )
4 OPTHALMIC PREPARTIONS Polyvinyl alcohol, carboxy
methylcellulose
91

92. PROPERTIES :
• Easily filtered
• Easily sterilized
• Have a requisite refractive index and clarity level
92

93. References
❖https://www.ncbi.nlm.nih.gov/pubmed/23985820
❖https://www.athlone-
laboratories.com/downloads/ampicillin125mg5mloralsuspensionspc.
pdf
❖https://www.researchgate.net/publication/290481755_Suspending_
properties_of_natural_gums_extracted_from_Abelmuscus_esculentu
s_pod_and_Chrysophyllum_albidium
❖https://www.slideshare.net/SilviSingh1/suspending-agents
93

94. LUBRICANTS
Prepared By Amna Khan
Roll no : 65
94

95. WHAT ARE LUBRICANTS?
• Improves Flow ability Of
Blends and Unit Dose
Operations.
• Lubrication plays a key role
in successful manufacturing
of pharmaceutical solid
dosage forms
• reduces friction
• Added in small quantity
(usually 0.25%–5.0%, w/w)
95

96. Magnesium Stearate
Uses:
➢ In cosmetics , foods and pharmaceutical
formulations.
➢ In capsules and tablets.
➢ Also in Barrier creams
Incompatibilities:
➢ With acids , alkalies and Iron salts.
➢ Cannot be used with Aspirin , vitamins and
alkaloidal salt products.
96

97. Other Examples Include :
• Boric acid
• Sodium Oleate
• Sodium Benzoate
• Stearic Acid
• Talc
97

98. Fats And Oils
98

99. CHARACTERISTICS :
❖Fats and oils are a broad group of naturally occurring and
semisynthetic molecules.
❖Fats and oils used in pharmaceutical industries exhibit unique
physical and chemical properties
❖Used as excipients in cosmetics and medicines
❖These oils are classified as an oleaginous vehicle and is present
in some topical pharmaceuticals and intramuscular injectables
99

100. Examples :
100

101. Sunflower Oil
In cosmetics Parenteral Preparations
Peanut Oil
Sustained Release IM Injections In Emulsions and enemas
Almond Oil
As an Emollient Vehicle in Parenteral Preparations
101

102. Castor Oil
Oral and Topical
Formulations
Sustained release tablets
Coconut Oil
In Lotions
Antifungal Properties against
candidia species
102

103. Pharmaceutical Excipients
Sub-topic “solvents”
By SAIM IKHLAQUE SOLEJA
ROLL NO. 29
103

104. Solvents
• Used to dissolve another substance in preparation of a solution; may be
aqueous or not (e.g., oleaginous).
• Cosolvents, such as water and alcohol (hydroalcoholic) and water and
glycerin, may be used when needed.
• Sterile solvents are used in certain preparations (e.g., injections)
Reference: page no.153, Ansels Pharmaceutical Dosage Forms and
Drug Delivery Systems
104

105. List of Solvents
• Albumin,
• Alcohol,
• Almond oil,
• Benzyl alcohol,
• Benzyl benzoate,
• Butylene glycol,
• Carbon dioxide,
• Castor oil,
• Corn oil (maize),
• Cottonseed oil,
• Dibutyl phthalate,
• Diethyl phthalate,
• Dimethyl ether,
• Dimethyl phthalate,
• Dimethyl sulfoxide,
• Dimethylacetamide,
• Ethyl acetate,
• Ethyl lactate,
• Ethyl oleate,
• Glycerin,
• Glycofurol,
• Isopropyl
alcohol,
• Isopropyl myristate,
• Isopropyl palmitate,
• Light mineral oil,
• Medium-chain
triglycerides,
• Methyl lactate,
• Mineral oil,
• Monoethanolamine,
• Octyldodecanol,
• Olive oil,
• Peanut oil,
• Polyethylene glycol,
• Polyoxyl 35 castor
oil,
• Propylene
carbonate,
• Propylene glycol,
• Pyrrolidone,
• Safflower oil,
• Sesame oil,
• Soybean oil,
• Sunflower oil,
• Triacetin,
• Tricaprylin,
• Triethanolamine,
• Triethyl citrate,
• Triolein,
• Water,
105

106. Isopropyl Alcohol
106

107. Isopropyl Alcohol
• Nonproprietary Names
• BP: Isopropyl Alcohol
• JP: Isopropanol
• Ph Eur: Isopropyl Alcohol
• USP: Isopropyl Alcohol
• Chemical Name:
• Propan-2-ol
• Empirical Formula and Molecular
Weight
• C3H8O and 60.1
• Structural Formula:
• Functional Category:
Disinfectant; solvent.
107

108. Applications in Pharmaceutical Formulation and
technology
• Isopropyl alcohol (propan-2-ol) is used in cosmetics and
pharmaceutical formulations, primarily as a solvent in topical
formulations. It is not recommended for oral use owing to its
toxicity;
• Although it is used in lotions, the marked degreasing properties of
isopropyl alcohol may limit its usefulness in preparations used
repeatedly.
108

109. Applications in Pharmaceutical Formulation and
technology…… conti
• Isopropyl alcohol is also used as a solvent both for tablet film-coating
and for tablet granulation, where the isopropyl alcohol is
subsequently removed by evaporation.
• It has also been shown to significantly increase the skin permeability
of nimesulide from carbomer 934.
• Isopropyl alcohol has some antimicrobial activity and a 70% v/v
aqueous solution is used as a topical disinfectant.
• Therapeutically, isopropyl alcohol has been investigated for the
treatment of postoperative nausea or vomiting.
109

110. Description
• Isopropyl alcohol is a clear, colorless, mobile, volatile, flammable
liquid with a characteristic, spirituous odor resembling that of a
mixture of ethanol and acetone;
• it has a slightly bitter taste.
Stability and Storage Conditions
• Isopropyl alcohol should be stored in an airtight container in a cool,
dry place.
110

111. Incompatibilities
• Incompatible with oxidizing agents such as hydrogen peroxide and
nitric acid, which cause decomposition.
• Isopropyl alcohol may be salted out from aqueous mixtures by the
addition of sodium chloride, sodium sulfate, and other salts, or by
the addition of sodium hydroxide.
Method of Manufacture
• Isopropyl alcohol may be prepared from propylene;
• by the catalytic reduction of acetone, or
• by fermentation of certain carbohydrates.
111

112. Safety
• Isopropyl alcohol is widely used in cosmetics and topical pharmaceutical
formulations.
• It is readily absorbed from the gastrointestinal tract and may be slowly
absorbed through intact skin.
• Prolonged direct exposure of isopropyl alcohol to the skin may result in
cardiac and neurological deficits.
• Isopropyl alcohol is metabolized more slowly than ethanol, primarily to
acetone. Metabolites and unchanged isopropyl alcohol are mainly excreted
in the urine.
• Isopropyl alcohol is about twice as toxic as ethanol and should therefore
not be administered orally; isopropyl alcohol also has an unpleasant taste.
112

113. Safety……… conti
• The lethal oral dose is estimated to be about 120–250 mL although
toxic symptoms may be produced by 20 mL.
• Although inhalation can cause irritation and coma, the inhalation of
isopropyl alcohol has been investigated in therapeutic applications.
• Isopropyl alcohol is most frequently used in topical pharmaceutical
formulations where it may act as a local irritant.
• When applied to the eye it can cause corneal burns and eye damage.
113

114. LD50 doses reported in different animals via
different routes
❖LD50 (dog, oral): 4.80 g/kg
❖LD50 (mouse, oral): 3.6 g/kg
❖LD50 (mouse, IP): 4.48 g/kg
❖LD50 (mouse, IV): 1.51 g/kg
❖LD50 (rabbit, oral): 6.41 g/kg
❖LD50 (rabbit, skin): 12.8 g/kg
❖LD50 (rat, IP): 2.74 g/kg
❖LD50 (rat, IV): 1.09 g/kg
❖LD50 (rat, oral): 5.05 g/kg
114

115. Handling Precautions
• Isopropyl alcohol may be irritant to the skin, eyes, and mucous
membranes upon inhalation.
• Eye protection and gloves are recommended.
• Isopropyl alcohol should be handled in a well-ventilated environment.
• In the UK, the long-term (8-hour TWA) workplace exposure limit for
isopropyl alcohol is 999 mg/m3 (400 ppm); the short-term (15-minute)
workplace exposure limit is 1250 mg/m3 (500 ppm).
• OSHA standards state that IPA 8-hour time weighted average airborne
level in the workplace cannot exceed 400 ppm.
• Isopropyl alcohol is flammable and produces toxic fumes on
combustion.
115

116. Peanut Oil
116

117. Peanut Oil
• Nonproprietary Names:
• BP: Arachis Oil
• JP: Peanut Oil
• PhEur: Arachis Oil, Refined
• USP-NF: Peanut Oil
• Synonyms
• Aextreff CT;
• arachidis oleum raffinatum;
• earthnut oil;
• groundnut oil;
• katchung oil;
• nut oil.
• Chemical Name:
• Peanut oil
• Empirical Formula and Molecular
Weight
A typical analysis of refined peanut oil
indicates the composition of the acids
present as glycerides to be:
• arachidic acid 2.4%;
• behenic acid 3.1%;
• palmitic acid 8.3%;
• stearic ac ;
• lignoceric acid 1.1%;
• linoleic acid 26.0%, and oleic acid %.
• Functional Category
• Oleaginous vehicle; solvent.
117

118. Application Pharmaceutical Formulation or
Technology
• Peanut oil is used as an excipient in pharmaceutical formulations primarily
as a solvent for sustained-release intramuscular injections.
• It is also used as a vehicle for topical preparations and as a solvent for
vitamins and hormones. In addition, it has been part of sustained-release
bead formulations, nasal drug delivery systems, and controlled-release
injectables.
• Therapeutically, emulsions containing peanut oil have been used in
nutrition regimens, in enemas as a fecal softener, and in otic drops to
soften ear wax. It is also administered orally, usually with sorbitol, as a gall
bladder evacuant prior to cholecystography.
• Peanut oil is also widely used as an edible oil.
118

119. Description
• Peanut oil is a colorless or pale yellow-colored liquid that has a faint
nutty odor and a bland, nutty taste. At about 38 C it becomes cloudy,
and at lower temperatures it partially solidifies.
119

120. Typical Properties
• Autoignition temperature: 443 C
• Density: 0.915 g/cm3 at 25 C
• Flash point: 283 C
• Freezing point: 5 C
• Hydroxyl value: 2.5–9.5
• Interfacial tension: 19.9mN/m at 25
C
• Refractive index: n
D
25 = 1.466–1.470
• Viscosity (dynamic): 35.2 mPa s
(35.2 cP) at 37 C(5):
• Viscosity (kinematic) 39.0mm2/s
(39.0 cSt) at 37 C(5)
• Solubility: Very slightly soluble in
ethanol (95%); soluble in benzene,
carbon tetrachloride, and oils;
miscible with carbon disulfide,
chloroform, ether, and hexane.
• Surface tension: 37.5mN/m at 25 C
120

121. Stability and Storage Conditions
• Peanut on exposure to air it can slowly thicken and may become
rancid.
• Solidified peanut oil should be completely melted and mixed before
use.
• Peanut oil may be sterilized by aseptic filtration or by dry heat, for
example, by maintaining it at 150 C for 1 hour.
• Peanut oil should be stored in a well-filled, airtight, light- resistant
container, at a temperature not exceeding 40 C.
• Material intended for use in parenteral dosage forms should be
stored in a glass container.
121

122. Incompatibilities
• Peanut oil may be saponified by alkali hydroxides.
Method of Manufacture
• Refined peanut oil is obtained from the seeds of Arachis hypogaea
Linne´ (Fam. Leguminosae).
• The seeds are separated from the peanut shells and are expressed in
a powerful hydraulic press.
• The crude oil has a light yellow to light brown color, and is then
purified to make it suitable for food or pharmaceutical purposes.
• A suitable antioxidant may be added.
122

123. Safety
• Peanut oil is mildly laxative at a dosage of 15–60 mL orally or of 100–
500mL rectally as an enema.
• Adverse reactions to peanut oil in foods and pharmaceutical
formulations have been reported extensively. These include severe
allergic skin rashes and anaphylactic shock following consumption of
peanut butter.
• Peanut oil is harmful if administered intravenously and it should not
be used in such formulations.
123

124. 124

125. Reference
• Handbook of Pharmaceutical Excipients 6th Ed.(2009)
• Ansels Pharmaceutical Dosage Forms and Drug Delivery Systems
125

126. 126