This document discusses the development of a controlled release transdermal patch containing paracetamol. It first defines transdermal drug delivery and the basic components of transdermal patches. It then discusses the advantages and disadvantages of transdermal patches. The document goes on to describe the selection of paracetamol as the drug, formulation of three patches containing different polymers, and evaluation of the patches. Formulation C containing PVP showed the best results with good consistency, spreadability, and pH between 5-7. The conclusion is that a PVP-containing paracetamol patch can overcome oral administration issues and provide controlled release of the drug.
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Understanding the controlled release behavior of transdermal patch of paracetamol
1. UNDERSTANDING THE CONTROLLED
RELEASE BEHAVIOUR OF
TRANSDERMAL PATCH OF
PARACETAMOL
BY
AMRITA RANI
Reg. 19109161047
UNDER THE GUIDANCE OF
MD. SOHRAB ALAM
M.PHARMA
2. DEFINITION :
Transdermal drug delivery is defined as a self contained discrete dosage
form which when applied to the intact skin , will deliver the drug at a
Controlled rate to the systemic circulation.
Basic components of transdermal patches, Polymer matrix / Drug reservoir,
Drug , Permeation enhancers, Pressure sensitive adhesive (PSA) , Backing
laminates, Release liner and other excipients like plasticizers and solvents.
ADVANTAGES:
• Patches are easy to apply, non-invasive and painless.
• Drug can be delivered over a long period of time.
• Reduces dosing frequency as a single patch continuously delivers the
drug for prolonged period of time.
• No interaction of drug with food, enzymes, drink and other GI flora.
• Suitable for old age peoples who cannot take medicines orally.
• Self-administration is possible.
DISADVANTAGES:
• Difficult to administer large dose i.e. more than 10 mg/ day.
3. • Ionic drugs create problems.
• Drugs in high concentration may cause skin irritation.
• Difficult to achieve high plasma drug concentration.
DISEASE
Antipyretic , low analgesic
OBJECTIVE:
To develop an effective, safe and patient compliant controlled release transdermal gel
formulation of Paracetamol for Fever.
SELECTION OF DRUG
• Molecular size of the drug is less than 500 Daltons.
• The drug should not stimulate an immune reaction in the skin.
• The drug should not be irreversibly bound in the subcutaneous tissue.
• Nonirritant and nontoxic to the skin.
• It is low melting point and suitable for skin body temperature .
• The drug have pH between 5-9 and ideal for skin condition .
• The drug undergoes extensive hepatic first pass metabolism is particularly good
candidate for transdermal delivery.
5. METHOD
Polymers were weighed accurately and dissolved in 10ml of methanol &water (1:1)
kept aside to form clear solution. 500mg of drug added to the all
formulation.PEG600 (20% w/w of total polymer), PVP (10% w/w of total polymer),
PVA (30% w/w of total polymer) used as penetration enhancers. The solution was
poured on the Petridis which is lubricated with glycerin & dried at room
temperature for 24 hours. An inverted funnel places over the Petridis to prevent
evaporation of the solvent. Patches are stored in decicator.
EAVALUATION
The transdermal patch evaluated and the no irritation was found speadibility was
good and was found to be pH 5-7.
RESULT
Parameters Formulation A Formulation B Formulation C
Color White White White
Consistency Good Good Very Good
Irritation No No No
Spread ability Fair Good Very good
Extrudability Fair Good Good
pH 5-7 5-7 5-7
6. CONCLUSION
A comparison of PVP, PEG600 and PVA as penetration enhances for Paracetamol
transdermal were prepared. All formulation also showed good physicochemical
properties like thickness, drug content, and folding endurance. The in-vitro
release data showed that drug release from the patch formulation have been
affected by different penetration enhancers and polymer. Effect of penetration
enhancer like PVP, PEG600, and PVA have been checked on in-vitro permeation
of drug. These studies indicated that as the different penetration enhancers
increased drug permeation. From the results paracetamol with PVP shows good
penetration than PEG600 and PVA. The finding of this result revealed that the
problems of Paracetamol on oral administration like dissolution rate limited
absorption and gastric side effects can be overcome by applying Paracetamol
topically in the form of transdermal patch.
7. REFRENCE
• Michael N Pastore, Yogeshvar N Kalia, Michael Horstmann, Michael S Roberts(2015) Transdermal
patches: history, development and pharmacology, British Journal of Pharmacology,1-30.
• Md. Intakhab Alam1 , Nawazish Alam*2 , Vikramjit Singh2 , Md. Sarfaraz Alam1 , Md. Sajid Ali1 ,
Tarique Anwer1 , Mohammed M. Safhi1(2013) type, preparation and evaluation of transdermal patch:
a review, volume 2, 2199-2233.
• Priyanka Yadav*, Pallavi Tiwari, Ankit Singh,(2020) transdermal patch ˸ a recent review to
transdermal drug delivery system, JETIR, 703-719.
• Https://www.apollo247.com/blog/article/different-types-of-fever-in-india-vc007 Accessed on 15-08-
2023.
• Mark D Tarn,Damien Robert,Sally A. Peyman,Alexander Iles(2009) Temperature-based tuning of
magnetic particle separation by on-chip free-flow magnetophoresis.
• Mallesh Kurakulaa,∗ and G.S.N. Koteswara Rao(2020) Pharmaceutical assessment of
polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a
spotlight on COVID-19 inhibition.
