Pre-Thesis Presentation

 SHRI VENKATESHWARA UNIVERSITY,

(UTTAR PRADESH)
Topic-Design and evaluation of
floating tablets using selected drugs
 INTRODUCTION

 Preference towards oral drug delivery

 Approach towards prolong gastric retention
 Benefits of prolong gastric retention
 Gastrotretentive drug delivery system
 Factors affecting gastric residence time
 Suitable drugs for gastroretentive drug

delivery
 Advantages and disadvantages
Anatomical and physiological considerations of gastrointestinal tract
 Gastric emptying

 Migrating myoelectric cycle (MMC) is divided into four phases as

described by Wilson and Washington
 1.Phase I (Basal phase) have contractions which last from 30 to 60

minutes with some shrinkage.

 2.Phase II (Preburst phase) the frequency increase gradually with

irregular spasmodic action potential and reduction in size as the

process advances which lasts for 20 to 40 minutes.
 3.Phase III (Burst phase) all the undigested material is transferred to

the small intestine in this wave which lasts for 10 to 20 minutes. It

includes regular and intense contractions for diminished period.
 4.Phase IV It happens between phases III and I of 2consecutive

cycles and is persistent for 0 to 5 minutes.

  
Advancements to prolong the gastric residence
time (grt) of drug delivery system
 REVIEW OF LITERATURE
 Bahri-Najafi R.et.al.,2017,27studied floating dosage form containing acyclovir was developed to
increase its oral bioavailability. Optimized formulation showed good floating properties and  in
vitro drug release characteristics with mean dissolution time and dissolution efficacy of about
4.76 h and 54.33%, respectively.

 Kai Chen.et.al.,2017,28designed floating tablets by the dry-coated method of dipyridamole. The

effect of agents with nonidentical viscosities, hydroxypropylmethylcellulose (HPMC) and
polyvinylpyrollidon K30 (PVP K30)

 Rahim Bahri-Najafi.et.al.,2017,29studiedEffervescent floating tablets containing 200 mg Acyclovir

were produced by direct compression method with three different rate controlling polymers
including Hydroxypropyl methylcellulose K4M, Carbapol 934, and Polyvinylpyrrolidone.

 RamuB.et.al.,2017,30designed and evaluated gastroretentive floating bioadhesive tablets of

hydrochlorothiazide whichwere formulated by direct compression technique using polymers
xanthan gum, carbopol 974 P, HPMC K15M, HPMC K100M.

 Gaurav Singh Gurjar.et.al.,2017,31 formulated a gastroretentive system for sustained release of

therapeutically active agent having an absorption mechanism through the mucosa with limited
capacity using Cefuroxime axetil.

 Mohammed Gulzar Ahmed.et.al.,201632, designed a Gastro retentive floating tablets (GRFT) of

Rosvastatin which was developed by direct compression method, by using drug with different
polymersratio like HPMC E50, HPMC K15M and HPMC 5cps. By studying the release kinetics, all
the tablets fitted best in the Higuchi, first-order model and non-Fickian as the mechanism of
drug release.
List of formulations available in
market
Objective, scope and Limitation
 The aim of the associated study was to design and evaluate the Gastro
retentive floating tablets of selected drugs with the following objectives.
 Quinapril is a prodrug which transforms to its active metabolite
quinaprilat in the liver. It inhibits angiotensin converting enzyme which
catalyses the formation of angiotensin II from its precursor angiotensin I.
  Nimodipine has been developed for the treatment of hypertension asit
is a calcium channel blocker.
 Ivabradine HCL is used for the treatment of high blood pressure.
Ivabradine HCLis a dihydropyridine calcium channel blocker.
  Objectives and scope:
 To estimate the consequence of concentration of polymers on the
floating and dissolution from floating tablets.
 Upgrade the bioavailability of the drug through floatation.
 To increase the effectiveness in therapy.
 Reduction of dosing frequency.
 To retain the plasma concentration of drug in therapeutic range for
longer time by enhancing GRT.
 To improve patient compliance.
Research Methodology
1. Procurement of the identical drugs and the required polymer and the other
formulation ingredients.
2. Preformulation studies, to inspect the compatibility between the drug and the
excipients
3. Formulation of gastro retentive floating tablets using different natural and synthetic
polymers to retard the drug release and to maintain the drug in gastric medium for
more time.
4. Evaluation of pre-compression parameters such as Angle of repose
 Bulk density
 Tapped density

 Compressibility index

 Hausners ratio

5. Evaluation of post compression parameters like

 Thickness
 Hardness
 Friability

 Diameter
 Swelling Index

 Drug content

 Floating lag time

 Total floating time

 In vitro dissolution
 In-vitro drug release kinetics studies and stability studies
 Preformulation studies
 Solubility studies

 Determination of melting point

 Analytical method Development

 Compatibility Studies
Preparation of floating tablets by direct
compression method (Quinapril HCL floating tablets by Effervescent
technique):
Composition of Quinapril HCL floating tablets
by non-effervescent technique
Composition of Nimodipinefloatingtablets by effervescent technique:
 
Composition of Nimodipine floating tablets by
non-effervescent technique
Composition of Ivabradine HCL floating
tablets by Effervescent technique:
Composition of Ivabradine HCL floating
tablets by Non - Effervescent technique