Floating drug delivery systems (FDDS).pptx

Floating drug delivery systems (FDDS) evaluation process and pharmacokinetic parameters

1. FDDS Floating drug delivery systems (FDDS) are invented to retain the drug in the stomach and applicable for drugs with poor solubility and low stability in intestinal fluids. FDDS are hydro-dynamically controlled low-density systems with sufficient buoyancy to float over the gastric contents and remain buoyant in the stomach without affecting the gastric emptying rate for a prolonged period. The residual system is emptied from the stomach with the release of the drug. This results in enhanced gastric residence time and good control over plasma drug concentration fluctuations. The principle of buoyant preparation offers a simple and practical approach to achieve increased gastric residence time for the dosage form and sustained drug release INTRODUCTION 1

2. Advantages Floating dosage forms such as tablets or capsule will remains in the solution for prolonged time even at the alkaline pH of the intestine. FDDS are advantageous for drugs meant for local action in the stomach e.g.: Antacids FDDS dosage forms are advantageous in case of vigorous intestinal movement and in diarrhoea to keep the drug in floating condition in stomach to get a relatively better response. Acidic substance like aspirin causes irritation on the stomach wall when meet it hence; HBS/FDDS formulations may be useful for the administration of aspirin and other similar drugs. The FDDS are advantageous for drugs absorbed through the stomach eg : Ferrous salts, Antacids INTRODUCTION 2

3. Disadvantages Floating systems are not feasible for those drugs that have solubility or stability problems in gastric fluids. Drugs such as Nifedipine, which is well absorbed along the entire GI tract and which undergo significant first-pass metabolism, may not be suitable candidates for FDDS since the slow gastric emptying may lead to reduced systemic bioavailability. there are limitations to the applicability of FDDS for drugs that are irritant to gastric mucosa. One of the disadvantages of floating that they require a sufficiently high level of fluids in the stomach, so that the drug dosages form float therein and work efficiently INTRODUCTION 3

4. Criteria selection of drug candidate for the floating drug delivery system Readily absorption via upper gastrointestinal tract. Drugs with low pKa , that does exhibit unionized characters Drugs are possessing lower solubility at higher pH. Effect of local action of drugs e. g. treating Helicobacter pylori in treatment of ulcerative conditions. Drugs which get degraded in alkaline pH conditions; bioavailability of those can be enhanced by fabricating into gastro-retentive forms. Minimizing gastric irritation as it may result in the increase of drug concentration level in the stomach. INTRODUCTION 4

5. The mechanism associated with FDDS system is selective for the drugs with an absorption window in the stomach or in the upper small intestine This has a less density then gastric fluids and hence remain buoyant in the stomach without affecting gastric emptying rate for a prolonged period, and the drug is released slowly as a desired rate from the system. After the release of the drug, the residual system is expelled from the stomach. This results in an increased gastric retention time and better control on the fluctuation in plasma drug concentration INTRODUCTION 5

6. Single Unit Floating Dosage Systems Effervescent Systems (Gas-generating Systems) Non-effervescent Systems Multiple Unit Floating Dosage System Effervescent Systems (Gas-generating Systems) Non-effervescent Systems Hollow Microspheres Raft Forming System CLASSIFICATION OF FLOATING DRUG DELIVERY SYSTEM 6

7. Enhanced bioavailability Enhanced first-pass biotransformation Improved bioavailability due to reduced P-glycoprotein (P- gp ) activity in the duodenum Reduced frequency of dosing Targeted therapy for local ailments in the upper GIT Reduced fluctuations of drug concentration Improved selectivity in receptor activation Reduced counter-activity of the body Minimized adverse activity at the colon Pharmacokinetic and pharmacodynamic aspects of FDDS 7

8. Bilayer tablet remains a novel epoch designed for the effective advance of controlled delivery design laterally through numerous sorts to deliver an approach of efficacious drug transport system. Bi-layer tablet remain seemly intended for ensuing discharge of two medications in combination, discrete two discordant constituents then similarly designed for sustained discharge tablet in that single layer is immediate release as initial dose and the subsequent layer is the maintenance dose. Bilayer tablet remains enhanced favourable knowledge to overwhelmed the inadequacy of the single-layered tablet Bilayered Tablet Formulation 8

9. The aim of the present study is to carry out formulation and evaluation of floating bilayer tablet. The developed formulation could be an aid to enhance bioavailability of the drugs. Aim and Objective 9

10. Literature survey Selection of drug and excipient Pre-formulation studies Raw material analysis of drug Drug-Excipient compatibility study Physical observation Construction of calibration curve by UV spectrophotometer FTIR study ● Formulation of bilayer tablet ● Evaluation of formulation Shape of tablets Hardness of Tablet Tablet dimensions Weight variation Thickness of tablet Measurement of floating capacity Measurement of the density of the formulation Determination of drug content in tablets In vitro dissolution study Buoyancy/Floating test Swelling study Plan of Work 10

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