Experiment – 1
To perform preformulation studies of Aspirin
Submitted by Mohammad Faizan
Aim-
To perform Preformulation studies of aspirin
Abstract-
Before developing a pharmaceutical formulation, it’s essential to understand
the intrinsic chemical and physical properties of the drug. These properties
guide how the drug will interact with other ingredients when creating the
final dosage form. The main goal of preformulation studies is to design a
dosage form that is stable, effective, and safe. This involves:
1. Establishing the Drug’s Kinetic Rate Profile: Understanding how
the drug degrades over time helps determine its shelf life and ensures
it remains effective throughout its use.
2. Assessing Compatibility with Other Ingredients: Ensuring the
drug works well with other ingredients in the formulation to avoid any
negative interactions that could impact its stability or efficacy.
3. Determining Physico-Chemical Parameters: Identifying key
properties such as solubility, pH, and melting point to ensure the drug
can be formulated into a reliable and safe dosage form.
By carefully studying these factors, scientists can develop pharmaceutical
products that are not only effective but also safe and stable for patient use.
Preformation studies of aspirin play a crucial role in understanding its
properties to improve how it's formulated and how effectively it works. These
studies look at various factors like how well aspirin dissolves, its different
crystalline forms, particle size, and stability. Such research helps ensure that
aspirin is consistent in its effects and safe for use. By examining these
aspects, scientists can select the best ingredients and methods to make
aspirin more effective and longer-lasting. This abstract reviews recent
advancements in preformation studies, emphasizing how they contribute to
making aspirin safer and more effective for patients.
Introduction on Preformulation Studies-
Aspirin, also known as acetylsalicylic acid, is one of the most widely used
medications worldwide, renowned for its analgesic, antipyretic, and anti-
inflammatory properties.
Preformulation studies plays an important role in this process of formulation
development, providing essential data on the physicochemical properties of
aspirin that influence its formulation, stability, and bioavailability. These
studies are the foundation upon which successful drug development is built,
ensuring that the final product is both effective and safe for patient use.
These studies involve a series of investigations that characterize the
physical, chemical, and mechanical properties of a drug substance. For
aspirin, these studies are particularly important due to its susceptibility to
hydrolysis and degradation under various conditions. Preformulation is
defined as the steps to be undertaken before the formulation. These studies
focus on the physicochemical properties of the new compound that could
affect the drug action. It gives some guidelines to suitability of potential
equipment’s to be used in formulation. The preformulation investigations
confirm that there are no significant barriers to the compound’s development
as a marketed drug. The formulation scientist uses this information to
develop dosage forms. Various parameters studied during preformulation
studies include Colour, Odour, Particle size, Shape, Bulk characterization etc.
Preformulation Studies of Aspirin
1. API Profile
• Name of API: Aspirin
• Chemical Name: Acetyl-salicylic Acid
• Molecular Formula: C9H8O4
• Appearance: White Powder
• Category: NSAID
• Dose: 500 mg
• Storage: Away from Light & Moisture • Structure:
Aspirin
2. Micrometric Analysis
A. Bulk Density of API
[ B.D= mass / Bulk Volume]
• Weight of sample: 20g
• Volume of sample: 45ml
• Bulk Density: 0.44
B. Tapped Density of API
[ T.D= Tapped mass / Bulk Volume]
• Weight of sample: 20g
• Volume of sample: 36ml
• Bulk Density: 0.55
C. Carr’s index of API
[ C%= TD-BD/TD x 100 ] S.No. Carrs % Type
1 5-15 Excellent
• Tapped Density: 0.55 2 12- Good
• Bulk Density: 0.44 16
• Carr’s Index: 20 3 18- Fai
21 r
• Report: Fair 4 23- Poor
35
5 33- Very Poor
38
6 >40 Extremely Poor
D. Hausener’s Ratio
[ HR= TD/BD ]
• Tapped Density: 0.55
• Bulk Density: 0.44
• Hausener’s Ratio: 1.25
Aspirin
Tablet (B.P) API+Excipients Excipients
Bulk Density 0.5 0.62
Tapped Density 0.58 0.76
Carr’s Index 13.79 18.42
Hausener’s RatioTYPE
INGREDIENT 0.29 % 1.22
Quantity
AspirinAngle of API
Repose 42.7 37.5 36.02
300 mg
Lactose Diluent 46.8 375 mg
Starch Binder/Disintegrant 6 48 mg
Talc Glidant 5 40 mg
Mg/St Lubricant 1.5 12 mg
Angle of Repose (API+EXCIPIENTS)
5% 39.904 Fair
API+Binder 10% 45Angle
Very PoorType
0.50% 37.02<25Fair Excellent
API+Lubricant 2% 41.3425-30 Good
Very Poor
30% 50.1930-40 Fair
Very Poor
>40 Very Poor
API+Diluent 70% 50.19 Very Poor
INGREDIENT TYPE % Quantity
Aspirin API 37.5 300 mg
Lactose Diluent 46.8 375 mg
Starch Binder/Disintegrant 6 48 mg
Talc Glidant 5 40 mg
Mg/St Lubricant 1.5 12 mg
