poster presentation in international conference 2022 topic: Significance of Drug excipient interaction...

1. A Review: Significance of Drug-Excipients Interaction
*Shiva Kant Thakur, Rahul Pal, Arsh Chanana, Himmat Singh Chawad ,Ravinder Pal Singh
NIMS Institute of Pharmacy; NIMS University Jaipur 303121, Rajasthan, India.
*shivakant18051999@gmail.com
ABSTRACT METHOD OF ANALYSIS
INTRODUCTION
REFERENCES
TYPES OF DRUG EXCIPIENT INTERACTION
MECHANISM OF DRUG EXCIPIENT INTERACTION
RECENT ADVANCEMENT
 High sensitivity DSC/ HS-DS
 High-sensitivity differential scanning calorimetry is a modern powerful method of evaluation
 protein
 Energetic
 structure and interactions.
 This technique has been developed in the Former Soviet Union to study co-operative
conformational transitions of biopolymers in extremely dilute solutions.
 More sensitivity and precision exceeding most other commercial scanning calorimeters.
 A specific property of these instruments is uses of built-in calorimetric cells and relatively high
heating rates (1-2 K/min).
 A further benefit of HS-DSC is rather short measurement time and modest sample
consumption.
It has considerable benefit whereby even gross incompatibilities could be detected in a matter
of hours rather than weeks.
Excipients are the fundamental requirements to these modifications allowing
formulation scientists to achieve their objectives.
Excipients in brief can be defined as “The components of a formulation other than
the active ingredient”.
Excipients play a very important role in the design of dosage forms, as drugs cannot
be administered in pure form.
Enhance any other attribute of the overall safety and effectiveness of the drug
product during storage or use.
Although excipients are the non-active ingredients, they are essential in the successful
production of acceptable dosage forms such as tablets, powders, parenterals, semi
solids and liquid orals.
The following criteria are essential for excipients selection and use :
a) Physiological inertness.
b) Physical and chemical stability.
c) No influence on drug bioavailability.
d) Cost effectiveness.
 Important of drug excipients interaction :
In the designing and development of drug products from active drug(s), some of the important non-therapeutic substances are
essentially included. These non-therapeutic substances are broadly termed as excipients. The pharmaceutical drug-excipients
and their different techniques reviewed in detail in this article. Excipients are generally considered inert additives included in
drug formulation to help in the manufacturing, administration or absorption. The main classes namely, chemical, physical, and
biopharmaceutical will be defined and drug excipients incompatibility. Physical interactions occur mainly in three forms:
complexation, adsorption, or solid dispersions. Chemical interactions occur mainly as hydrolysis, oxidation, Maillard reaction,
Isomerization, or polymerization. Biopharmaceutical interactions occur after drug administration and mainly affect the
pharmacokinetics of the drugs. Various advanced analytical techniques like thermal methods (TG, DTA, DSC, Thermo
microscopy, Isothermal microcalorimetry, Isothermal Titration Calorimetry, High sensitivity DSC), Isothermal stress testing,
Optical microscopy, XRD, IR, NMR and chromatography can detect potential drug excipient incompatibilities.
This review emphasizes the essential criteria of excipients, different kinds of existing excipients, new grades of novel
excipients, combinations of different excipients and some of the new applications of existing excipients.
Keywords: Pharmaceutical excipients, Drug excipient Interaction, Drug- excipient incompatibility.
 Thermal analysis :
i. Thermogravimetry (TG): A technique in which a
change in the weight of a substance is recorded as
function of temperature or time.
i. Differential Thermal Analysis (DTA): a technique in which the temperature
difference between a substance and reference material is measured as a
function of temperature while the substance and reference are subjected to
a controlled temperature Programme.
ii. Differential Scanning Calorimetry (DSC): A technique in which the
difference in energy inputs into a substance and reference material is
measured as function of temperature Programme.
 X-ray powder diffraction : used for phase analysis and polymorph screening,
crystallinity determination, crystallography and crystal structure determination,
compatibility studies, manufacturing and production, stability studies, process control
and for control of ingredients.
 Spectroscopy method :
i. Vibrational spectroscopy
ii. Simultaneous DSC–FTIR microspectroscopic technique
iii. FT-Raman spectroscopy
iv. Diffuse Reflectance Spectroscopy (DRS)
v. Nuclear Magnetic Resonance (NMR)
 Chromatography
i. Thin Layer Chromatography (TLC)
ii. High Pressure Liquid Chromatography (HPLC)
1. Baldrick P. Pharmaceutical excipient development: the
need for clinical guidance, Regul Toxicol Pharmacol, 2000; 32: 210
2. Shireesh P Apte, Sydney O Ugwu. A review and classification of emerging excipients in
paranteral medications. Pharm Tech. 2003; 46-60.
3. Giorgio P. Patrizia R. The safety of pharmaceutical excipients, IL Farmaco, 2003; 58: 541-550. fig
https://www.researchgate.net/profile/Roger_Rowell/publication/268372341/figure/fig4/AS:66
8300954587141@1536346772724/Schematic-diagram-of-a-simple-thermogravimetric-analysis-
system.png:https://www.researchgate.net/profile/Roger_Rowell/publication/268372341/
Presented at the “International Conference on Fostering High Quality Clinical Research for A Healthier World” held at NIMS University, Jaipur
on 26th November 2022.
Important
Stability of dosage form
Bridge between discovery
and development .
In IND submission
Avoid surprise problem during
formulation process.
Drug –Excipient
intreaction
Drug –Drug intreaction
Drug – packing
intreraction
Types
1. Physical Interactions
a. Complexation
b. Adsorption
c. Solid Dispersion
2. Chemical interaction
a. Hydrolysis
b. Oxidation
figure/fig4/AS:668300954587141@1536346772724/Schematic-diagram-of-a-simple-thermogravimetric-analysis-system.png