INTERNATION CONFERENCE

ADVANCES IN BIO POLYMER DRUG DELIVERY SYSTEM

PHARMA TRANSPIRE -2014

Pharmacokinetic study of Aspirin suppositories and Aspirin nanoparticles loaded

suppositories
V. Ravi Sankar * 1, Y.Dastagiri reddy1
1

Department of Pharmaceutics, C.E.S College of Pharmacy, 51812, Kurnool, India.

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Introduction
An attempt was made to develop a new dosage form nanoparticles loaded suppositories, the mechanism involved in
release nanoparticles form the suppositories was explained in five steps. The mechanism involved was explained in five
steps. 1. Delivery of suppositories to rectal cavity 2. Dissolution of suppositories (release of nanoparticles) by the rectal
fluids 3. The nanoparticles will enter in fenestrated capillaries 4. Diffusion of drug from nanoparticles. 5. Nanoparticles
whose size is restricted to the entry of fenestrated capillaries due to the mucoadhesive character nanoparticles will adhere
to mucosa of rectum for a prolonged period of time and release the drug. The main aim and objective of the present work
was to compare the pharmacokinetic parameters of aspirin suppositories with aspirin nanoparticle loaded suppositories.
Experimental
Aspirin (ASA)-nanoparticles prepared based on ionicgelation mechanism and optimized Fa9 (2mg/ml STPP) formulation
was isolated for incorporation in glycerogelatin base. ASA-suppositories prepared for the selection of suitable base
composition based on evaluation tests (In-vitro drug release, physical and chemical tets) FS2, FS4, FS9, FS11 were
identified as suitable for incorporation. Selected Fa9 formulation was incorporated into the selected based compositions
based on fusion method and evaluated for various evaluation tests. Pharmacokinetic models were designed in fifteen
New Zealand male rabbit model which were divided in five groups. Method developed in high performance liquid
chromatography in rabbit plasma linearity was observed with r 2=0.999 in sodium chlorite buffer pH 2.5, acetonitrile, and
isopropyl alcohol flow rate of 2ml/min, retention time of 5.310 minutes was observed. PK1 and PK2 excel function were
used for calculating pharmacokinetic parameters. The same validate method was used for the determination of various
pharmacokinetic parameters, Area under curve (AUC0-t), Area under zero infinity (AUC0-infinite), Cmax, Tmax, half life,
elimination rate constant, Mean residence time.
Results & Discussions:
The elimination half life and MRT was extended in the aspirin nanoparticles loaded suppositories when compared with
ASA-suppositories from 1.430.56 to 5.110.15h and 1.410.31 to 8.230.06h. Thus aspirin nanoparticle gives a
controlled release of drug after released from the suppositories from the mechanism discussed earlier which will improve
the bioavailability due to the cationic and mucoadhesive character.