INTRODUCTION

 The Beads are Targeted drug delivery systems have been

designed on the concept of magic bullets given by “Dr. Paul
Ehrlich”.
 This concept is associated with the development of such systems
which when introduced in the body, direct the drug only to its
site of action there by providing maximum therapeutic response
accompanied with reduced toxic effects due to decreased
distribution of drug to other body tissues1.
 Targeted drug delivery systems are those in which maximum
drug concentrations is achieved at the specific site of drug action
either by using inert forms of active dug or by utilizing specially
designed polymers.
 Targeted drug delivery systems which employ a biologically inert
polymer as a carrier to carry the drug to its site of action are
referred to as drug carrier delivery systems 2.
 In these the drug can be either entrapped within the carrier or
covalently bonded to it.
 Several promising drug-carrier systems have been developed, which
utilize beads, microspheres, veicular grafts etc., as carrier molecules.
 The philosophy behind the development of “New drug delivery
system” is to make a therapeutic agent do its best when administered
into the body. This means a high therapeutic efficacy with minimal
toxicity.
 Drugs administered normally distribute throughout the body
interacting not only with the target cells but also with the normal
healthy cells which often results in toxic effects.
 Conventional therapy required frequent administration of the
therapeutic agent to the patient compliance3.
 Systemic administration of the drug often requires high concentration
to maintain a therapeutic effect because of the dilution effect and the
difficulty of drug placement in the target site.
 To obtain maximum therapeutic efficacy, it becomes necessary to
deliver the agent the target tissue in the optimal amount for the right
period of time there by causing little toxicity and minimal side effect.
 A well designed New drug delivery system can overcome some of the
problems of conventional therapy and enhance the therapeutically
efficacy of a given drug.
Ideal Properties of Beads6
 The beads should possess the following characteristics.
 They should enhance the drug action by prolonging its
systemic circulation
 It should increase the drug concentration at its site of
action.
 It should decrease or prevent tissue toxicity
 It should prevent the drug from undergoing metabolic
degradation by providing adequate protection.
 It should confine the drug within the desired body tissues.
 It should carry the drug during the transit and release it
only at the site of action at an appropriate rate.
Preparation Techniques of Beads
 The selection of the appropriate method for the preparation
of beads depends on the physicochemical characteristics of
the polymer and the drug to be loaded.
 On the contrary the preparation techniques largely
determine the inner structure in vitro release profile and the
biological fate of these polymeric delivery systems.
 Two types of systems with different inner structures are
apparently possible
1.A Matrix type system consisting of an entanglement of
oligomer or polymer units.
2.A Reservoir type of system comprised of an oily core
surrounded by an embryonic polymeric shell (Beads)
 One of the most feasible approaches for achieving a
prolonged and predictable drug delivery profile in the GI
tract is to control the gastric residence time.
That is locally active in stomach.
That have absorption window in stomach or in upper
small intestine.
That is unstable in intestinal or colonic environment.
Have low solubility at high pH value.
 AIM AND OBJECTIVES
Need for the study
 The present thesis entitled on “Formulation and
Evaluation of Famotidine Floating Micro Beads” are the
most innovated type of dosage forms that offer highest
attention in the area of novel drug delivery. Such systems
offer numerous advantages compared to solid dosage
forms such as
 To improve therapeutic efficiency
 To reduce adverse side effects and to improve its
tolerability
 To improve patient compliance and
 Reduction in health care cost
Aim and objectives of the study
 The aim and objectives of the study are:
 Preparation of standard calibration curve of Famotidine
 Development of Famotidine Floating Micro Beads by using
polymers like Carbopol, Hydroxy propyl cellulose and Sodium
alginate different ratio by Ionotropic gelation technique
method.
To perform evaluation parameters like
 Preformulation Studies:
 Determination of Melting point of Famotidine
 Drug-Polymer compatibility studies
 FT-IR (Fourier transform Infrared)
 Preparation of Calibration Curve of Famotidine
 Method of preparation of Famotidine Floating Micro Beads
 Characterization Of Floating Micro Beads (Or) Micromeritic
Properties of the Beads
 Angle of repose.
 Bulk density
 Carr’s index
 Hausner’s Ratio
 Morphology of the Particles:
 SEM (Scanning Electron Microscope)

 Evaluation test for floating micro beads

 Entrapment Efficiency

 Swelling index.

 Percentage Yield

 Buoyancy testing

 In vitro Dissolution studies

 Basket type dissolution studies
 MATERIALS AND EQUIPMENTS
 The materials used were either AR/LR grade or the best
possible Pharma grades available and are used as supplied by
the manufacturer.
MATERIALS USED
EQUIPMENTS USED:
 METHODOLOGY
 Pre formulation Studies:
 Pre formulation testing is the first step in rational
development of dosage forms of a drug substance.
 Pre formulation study is the process of optimizing the
delivery of drug through determination of physicochemical
properties of the new compound that could affect drug
performance and development of an efficacious, stable and
safe dosage form.
 It gives the information needed to define the nature of the
drug substance and provide a framework for the drug
combination with pharmaceutical excipients in the dosage
form.
 Hence, pre formulation studies were performed for the
obtained sample of drug for identification and
compatibility studies 38.
 The following pre formulation studies were performed for
Famotidine and polymers.
 Determination of melting point of Famotidine
 Drug - polymer compatibility studies
 Determination of melting point: Melting point was
determined by taking small amount of Famotidine in a
capillary tube closed at one end. The capillary tube
containing drug is placed inside and kept in melting
point apparatus and the temperature at which the drug
melts was recorded 39. This was performed thrice and
average value was calculated.
 Drug Polymer Compatability studies
 FT-IR Spectra: Prior to the development of the dosage
forms, infrared spectra of the physical mixture of the
Famotidine, polymers individually and the mixture of
drug and polymer were taken. The drug-Polymer
Interaction were studied by FTIR spectrometer, shimadzu
8400S 2% w/w of the sample with respect to a potassium
Bromide was mixed with drug KBr. The mixture was
mixed into a fine powder using mortar and then
compressed into a KBr discs in a hydraulic press at a
pressure of 10000 PSI. Each KBr disc was scanned for 10
times at a resolution of 2cm-1 using Happ-Genzel
apodization. The characteristic peaks were recorded.
 Preparation of standard calibration curve of
Famotidine:
 Preparation of standard solution
 Standard stock solution was prepared by dissolving
accurately weighed 100 mg of Famotidine in 0.1N
hydrochloric acid and the volume was made up to 100
ml with 0.1N hydrochloric acid. (Stock solution-I, 1000
mcg/ml). 10 ml of stock solution-I was diluted to 100 ml
with distilled water. (Stock solution-II, 100 mcg/ml). 1
ml of stock solution- II was diluted to 10 ml with
distilled water, so that to produce the concentration 10
mcg/ml. The absorbance of resulting solution was
measured against respective blank solution in the UV
region of 200-400 nm, which shows maximum
absorbance at 360 nm.
 Preparation of sample solutions
 Powder equivalent to 25 mg of Famotidine was weighed
accurately and transferred into a 25 ml standard volumetric
flask. The contents were dissolved in 0.1N hydrochloric acid
and sonicated for five minutes. This solution was filtered
through 0.45 μm whatsmann filter paper. 5 ml of the filtrate
was diluted to 50 ml with distilled water to get the solution
of 100 mcg/ml. An aliquot of 1 ml of test solution was
diluted to 10 ml with distilled water so that to produce the
concentration 10 mcg/ml.
PROCEDURE 42:
 Aliquots of standard solution of Famotidine ranging
from 0.5-2.5 ml (1 ml = 100 mcg) were transferred into a
series of 10 ml volumetric flasks. The volume in each
flask was made up to 10 ml with distilled water and the
absorbance was measured at 360 nm against solvent
blank. The obtained absorbance values when plotted
against the concentration of Famotidine give the
calibration graph.
 FORMULATION DESIGN
 The technique involved in the preparation of Famotidine
Floating Micro beads was Ionotropic gelation technique.
Weigh the required quantity of Famotidine with polymers
such as sodium alginate and carbopol in ethanol solution.
Homogenously mix the above solution for proper dissolving
of drug. With the help of hypodermic syringe drop wise
drop add into the beaker containing 1% CaCl2 (calcium
chloride solution). Finally, beads are dried in a tray dryer at
room temperature 40oC for 5 minutes. The time of drying
was optimized by weighing the beads repeat it until, to
obtain their constant weight.
