Formulation and Evaluation of 5-Fluorouracil Floating Beads

Nagadeepa Papireddygari*, Venkata Ramana Bachu, Venkata Badarinath Atluri
Dr. K. V. Subba Reddy Institute of Pharmacy, Kurnool, Andhra Pradesh, India – 518218

A B S T R A C T
The novel design of an oral controlled drug delivery system should be primarily aimed   at achieving more predictable and increased bioavailability of drugs. These considerations have led to the development of oral controlled-release dosage forms possessing gastric retention capabilities. Various types of drugs, which can benefit from using gastro retentive devices, are (a) Drugs acting locally and primarily absorbed in the stomach, (b) Drugs that are poorly soluble at an alkaline P^H, (c) Those with a narrow window of absorption, (d) Drugs absorbed rapidly from the GI tract, and (e) Drugs that degrade in the colon. Floating drug delivery system is suitable for 5-Fluorouracil as the absorption and solubility of drugs high at pH<3. 5-Fluorouracil was having extensive first pass metabolism, and relative Elimination half‐life of about 10-20mins. (extended‐release) and associated with frequent dosing of conventional dosage form makes it suitable candidate for sustained release dosage form for patient compliance. Therefore, it is selected as a suitable drug for the design of a gastro retentive floating drug delivery system (GFDDS) with a view to improve its oral bioavailability. In the present work, an attempt has been made to formulate GFDDS of 5-Fluorouracil   using HPMC 100K, Sodium alginate as rate controlling polymer Sodium bicarbonate as floating agent, Sunflower oil also added to study the effect of oil concentration in the formulation, Cacl₂ as cross linking agent in order to prolong the drug release, and to impart floating properties to the 5-Fluorouracil floating alginate beads. Floating alginate beads are subjected to evaluations, it includes Floating lag time, Duration of floating, Percentage of beads floated, Drug entrapment efficiency and Drug loading, Percentage yield, Moisture content, swelling index, Density were determined From this Dissolution data and floating lag time, floating duration of optimized formulations of 5-Fluorouracil floating alginate beads finally concluded by considering two designs of formulations.
Keywords: 5-Fluorouracil, HPMC100 K, Sodium Alginate, Sodium Bicarbonate.