You are hereFORMULATION AND EVALUATION OF ITOPRIDE HCL SUSTAINED RELEASED PELLETS

FORMULATION AND EVALUATION OF ITOPRIDE HCL SUSTAINED RELEASED PELLETS


ABOUT AUTHORS:
Shankar Soni1*, Dr. Puspendra singh Naruka1, Sunil kumar ola2
1B N College Of Pharmacy, Udaipur
2Goenka College Of Pharmacy, Laxmangarh
*slsoni85@gmail.com

ABSTRACT
The present work was aimed at formulation development, evaluation and comparative study of the effects of ethyl cellulose in Itopride HCL CR pellets. The controlled release polymers used for the present study were Ethylcellulose N-14 and Ethylcellulose N-20. The formulated pellets were evaluated for various pellet properties, like hardness, bulk density, tapped density, cars index and dissolution rate. Comparative evaluation of the above-mentioned parameters established the superiority of the pellets formulated with Ethylcellulose those formulated with different grades.
The main objective of this work is to develop and explore formulation as sustained release pellets of Itopride hydrochloride.From the literature it was found that different carriers like ethyl cellulose N-20, Ethyl cellulose N-50 were used to prepare controlled release pellets of water soluble drugs. Hence, in the present investigation it is aimed to test the suitability of using ethyl cellulose in the development of gastric retentive systems and for controlling the drug release from the pellets.

Reference Id: PHARMATUTOR-ART-1977

INTRODUCTION
A peptic ulcer is a hole in the Gut lining of the stomach, duodenum, or esophagus. A peptic ulcer of the stomach is called a gastric ulcer of the duodenum, a duodenal ulcer, and of the esophagus, an esophageal ulcer. An ulcer occurs when the lining of these organs is corroded by the acidic digestive juices which are secreted by the stomach cells.

Peptic ulcer disease is common, affecting millions of Americans yearly Proton pump inhibitors (or "PPI"s) are a group of drugs whose main action is a pronounced and long-lasting reduction of gastric acid production.

These drugs are utilized in the treatment of many conditions such as Dyspepsia, Peptic ulcer disease (PUD), Gastroesophageal reflux disease Laryngopharyngeal Reflux Disease, Barrett's esophagus, prevention of stress gastritis. Gastrinomas and other conditions that cause hypersecretion of acid, Zollinger-Ellison syndrome.

Proton pump inhibitors act by irreversibly blocking the hydrogen/potassium adenosine triphosphatase enzyme system (the H+/K+ ATPas) or more commonly just gastric proton pump) of the gastric parietal cell. The proton pump is the terminal stage in gastric acid secretion, being directly responsible for secreting H+ ions into the gastric lumen, making it an ideal target for inhibiting acid secretion.

1.1. INTRODUCTION OF DRUG DELIVERY SYSTEM:
The aim of any drug delivery system is to provide therapeutic amount of drug and maintain it constant through out the period of treatment from decades an ACUTE OR CHORONIC illness is being clinically treated through the delivery of the drugs to the patient in the form of various dosage forms like Tablets, Capsules, Ointments, Syrups, Suspositories, Aerosols, Pills, Liquids, Gels etc.

New drug delivery systems can be over looked as

  • Delayed Release System
  • Controlled  Release System
  • Sustained  Release System
  • Prolonged Release System
  • Site Specific And Receptor Targeting

1.2. DELAYED RELEASE SYSTEM:
Use repetitive, intermittent dosing of a drug from one or more immediate release units, incorporated into a single dosage form. The two types of delayed release systems are

  1. INTEESTINAL RELEASE SYSTEM
  2. COLONIC PELEASE SYSTEM

a. Intestinal release systems:
A drug may be enteric coated for intestinal release for several known reasons such as to prevent gastric irritation, prevent destabilization in gastric pH etc.

b. Colonic release systems:
Drugs are poorly absorbed through colon but may be delivered   to such a site for two reasons
a) Local action in the treatment of ulcerative colitis and
b) Systemic absorption of protein and peptide drugs

Advantage is taken of the fact that PH sensitive bio degradable polymers like poly methacrylates release the medicament only at the alkaline pH of colon or use of divinylbenzene cross-linked polymers that can be cleaved only by the azo reductase of colonic bacteria to release free drug for local effect or systemic absorption.

eg. Repeat action tablets, enteric-coated tablets.

1.3. CONTROLLED DRUG DELIVERY (PRE PROGRAMED):

  • Controlled drug delivery is delivery of drug at a rate or at a location determined by needs of body or disease state over a specified period of time.
  • Activation modulated
  • Feed back regulated
  • Site targeting
  • Provides constant drug levels with zero order kinetics.

1.3.1. Advantages:
1. Improved patience compliance and convince due to less frequent drug administration
2. Increased safety margin of high potency drugs due to better control of plasma levels.
3. Reduction in health care costs through improved theory, shorter treatment period, less frequency of dosing and reduction in personnel time to dispense Administer and monitor patient.

1.3.2. Disadvantages:
1.  Poor in vitro –in vivo correlations.
2. Possibility of dose dumping due to food, physiologic formulation variables or chewing or grinding of oral formulation by the patient and thus increased risk of toxicity
3. Retrieval of drug is difficult in conc. of toxicity poisoning or hypersensitivity reaction

The oral controlled release systems are classified as follows:
A) Continuous release systems.
B) Delayed transit and continuous release systems.

1.4. SUSTAINED DRUG DELIVERY (PROGRAMED):
The aim of any drug delivery system is to provide therapeutic amount of drug to appropriate site in the body to achieve immediate therapeutic response and to maintain the desired drug concentration.

In the recent years sustained release (SR) dosage forms continue to draw attention in the research for improved patient compliance and decreased incidence of adverse drug reactions.

Sustained release, sustained action, prolonged action, extended action are the terms used to identify drug delivery system that are designed to achieve a prolong therapeutic effect by continuously releasing medication over an extended period of time after administration of a single dose.

1.4.1. Advantages:
1.Improvement of patient compliance because of decreased frequency of dosage.
2. Avoidance of costly interventions such as laboratory services.
3. Allowing patients to receive medications as outpatients.
4. Optimization of duration of action of drug.
5. Controlling the site release.

1.4.2. Disadvantages:
1.Increased   variability among dosage units.
2. Stability problems.
3. Increased cost per unit dose.
4. More rapid development of tolerance.
5. Need of additional patient education and counseling.


Figure 1: Plasma drug concentration profiles for conventional tablet or capsule formulation, a sustained release formulation and a zero order controlled release formulation.

1.5. PROLONGED RELEASE:
Provide extended release, but not necessarily constant drug levels.  May not follow perfect Zero Order.

1.6. SITE SPECIFIC AND RECEPTOR RELEASE:
Targeting drug to the particular organ or tissue of the body. For receptor release   target is particular receptor for a drug within an organ or tissue.

1.7. PELLETIZATION

Pellets:
Pellets can be defined as small, free flowing spherical or semi-spherical solid units, typically from about 0.5 mm to 1.5 mm, and intended usually for oral
Administration, manufactured by the agglomerates of fine powders or granules of   bulk drugs and Excipients using appropriate processing equipment. Pellets can be prepared by many methods, the compaction and drug-layering being the most widely used today.

Regardless of which manufacturing process is used, pellets have to meet the following requirements. They should be near spherical and have a smooth surface both considered optimum characteristics for subsequent film coating. The particle size range should be as narrow as possible. The optimum size of pellets for pharmaceutical use is considered to be between 600 and 1000mm.

The pellets should contain as much as possible of the active ingredient to keep the size of   the final dosage form within reasonable limits. They should be near spherical and have a smooth surface both considered optimum characteristics for subsequent film coating. The particle size range should be as narrow as possible. The optimum size of pellets for pharmaceutical use is considered to be between 600 and 1000mm.

The pellets should contain as much as possible of the active ingredient to keep the size of the final dosage form within reasonable limits. Regardless of which manufacturing process is used, pellets have to meet the following requirements. They should be near spherical and have a smooth surface both considered optimum characteristics for subsequent film coating.

The particle size range should be as narrow as possible. The optimum size of pellets for pharmaceutical use is considered to be between 600 and 1000mm. The pellets should contain as much as possible of the active ingredient to keep the size of the final dosage form within reasonable limits. They should be near spherical and have a smooth surface both considered optimum characteristics for subsequent film coating.

1.8. Significance of Pellets:
Pellets may have varied applications in varied industries. It just requires an innovative bend to use it to derive maximum profitability. The smooth surface & the uniform size of the pellets allow uniform coating not only for each pellet but also from batch to batch. Highlighted below are some of the few instances where smooth surfaced uniform pellets are being successfully used.

1. Pellets ensure improved flow properties, and flexibility in formulation development and manufacture.

2. The coating material may be colored with a dye material so that the beads of different coating thickness will be darker in color and distinguishable from those having fewer coats.

3. The beads or granules of different thickness of coatings are blended in the desired proportions to give the desired effect.

4. The thickness of the coat on the pellets dictates the rate at which the drug contents are released from the coated particles.

5. By selecting the proper formulation, processing conditions and processing equipment it is possible to attain smooth surfaced & uniform pellets.

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