RESEARCH ARTICLE T.Vijay et.al / IJIPSR / 2 (8), 2014, 1708-1728

Department of Pharmaceutics ISSN (online) 2347-2154

Available online: www.ijipsr.com August Issue 1708

FORMULATION AND EVALUATION OF ENTERIC COATED

TABLETS OF ILAPRAZOLE

1D.Adukondalu,

2T.Vijay

*,

3K.Ranjith,

4A.Murali,

5Upender,

6L.Purna Chander

1Faculty Department of Pharmaceutics Vaagdevi College of Pharmacy, Ramnagar Hanamkonda

Warangal Telangana State, INDIA

2,3,4,5,6 Department of Pharmaceutics Vaagdevi College of Pharmacy, Ramnagar Hanamkonda

Warangal Telangana State, INDIA

Corresponding author

D.Adukondalu

Department of Pharmaceutics

Vaagdevi College of Pharmacy,

Hanamkonda, Warangal, Telangana State, INDIA

Email: vijjuthallapally@gmail.com

Phone: +91-9966390949

International Journal of Innovative

Pharmaceutical Sciences and Research www.ijipsr.com

Abstract

The present study is an attempt to formulate and evaluate delayed release enteric coated tablets of Ilaprazole using

different enteric coated polymers like Kollicoat MAE 30DP, AQOAT AS-MF and Cellulose acetate pthalate. Core

tablets were prepared by Direct compression method. Core tablets were sub-coated using hydroxy propyl methyl

cellulose and enteric coating with either of polymers. The disintegration of enteric coated tablets i.e. formulations

with 6% weight buildup (F2a to F2c) in 0.1N HCl could not pass the test. However, formulations with 8% and

10% weight buildup (F2d to F2i) showed no disintegration in acid stage. Among the polymers tested, Kollicoat

MAE 30DPwith 8% (F2f) weight buildup showed minimum release in 0.1N HCl and the complete release in pH

6.8 phosphate buffer. Further, the plasticizer effect on Kollicoat MAE 30DP was also studied and found, with

increase in concentration of plasticizer there is decreased drug release in 6.8 pH phosphate buffer. Based on the

tablets evaluation results, the formulation F2f was selected as the optimized formulation.

Keywords: Ilaprazole, sub-coating, enteric coating, Kollicoat MAE 30DP, AQOAT

mailto:email.%3Avijjuthallapally@gmail.comtel:9966390949

RESEARCH ARTICLE T.Vijay et.al / IJIPSR / 2 (8), 2014, 1708-1728

Department of Pharmaceutics ISSN (online) 2347-2154

Available online: www.ijipsr.com August Issue 1709

INTRODUCTION

Tablets are pharmaceutical solid dosage form, comprising a mixture of active substances and

excipients, usually in powder form, pressed or compacted into a solid. Tablets Dosage form is

one of the most preferred dosage form all over the world. Almost all drug molecules can be

formulated in a tablet and process of manufacturing of tablets is very simple and is very flexible

[1]. Tablet dosage forms are preferred due to their accurate dose, good physical & chemical

stability, competitive unit production costs and an elegant distinctive appearance resulting in a

high level of patient acceptability. [2]

Modified Release Dosage Forms

Drug products designed to reduce the frequency of dosing by modifying the rate of drug

absorption have been available for many years. Advances in technology have resulted in novel

modified release dosage form. The United States Pharmacopoeia (USP) defines the modified-

release (MR) dosage form as "the one for which the drug release characteristics of time course

and/or location are chosen to accomplish therapeutic or convenience objectives not offered by

conventional dosage forms such as solutions, ointments, or promptly dissolving dosage forms.

[3]

. Classification

Modified release dosage form may be classified as

A. Delayed release

B. Extended release

1. Sustained release

2. Controlled release

C. Site- specific and receptor targeting.

A. Delayed release dosage forms

Delayed release dosage forms are defined as those that release a drug at anytime other than

promptly after administration. The delay may be time based or based on the influence of

environmental conditions like GIT pH. Enteric coated products are an example of such dosage

form. Delayed release dosage form is the best formulations which are used for drugs that are

destroyed in gastric fluids, or cause gastric irritation or absorbed preferentially in the intestine.

Such preparations contain an alkaline core material comprising the active substance, a separating

layer and enteric coating layer [3].

RESEARCH ARTICLE T.Vijay et.al / IJIPSR / 2 (8), 2014, 1708-1728

Department of Pharmaceutics ISSN (online) 2347-2154

Available online: www.ijipsr.com August Issue 1710

Enteric coating

The technique involved in enteric coating is protection of the tablet core from disintegration in

the acidic environment of the stomach by employing pH sensitive polymer, which swell or

solubilize in response to an increase in pH to release the drug. Enteric coatings are those which

remain intact in the stomach, but will dissolve and release the contents once it reaches the small

intestine. Their prime intension is to delay the release of drugs which are inactivated by the

stomach contents or may cause nausea or bleeding by irritation of gastric mucosa.

MATERIALS

Ilaprazole is .Gift sample from RA Chemicals, Hyderabad, Crosspovidone, Croscarmellose

sodium and Pre-gelatinized starch were gift samples from Himedia chemicals, Triethyl citrate

obtained as gift sample from Merck schuchardt, Kollicoat MAE 30DP is gift sample from BASF

chemicals, Aqoat AS-MF is received as gift sample from Shin-etsu chemicals. Other materials

used were of analytical grade are from commercial source.

METHOD

METHOD OF PREPARATION [31,32,33,34]

Ilaprazole enteric coated tablets were prepared by wet granulation method and enteric coated

with different types of polymers. The compression process was performed by using sixteen

station rotary compression machines.

Preparation of core tablets

Ilaprazole core tablets were prepared by using direct compression technique. It is a convenient

method but the excipients used in this method are costlier when compared to the excipients

used in the wet granulation technique.Different formulations of Ilaprazole were designed to be

prepared by direct compression method using three super disintegrates (sodium starch

glycolate, crospovidone, croscarmellose sodium, Pregelatinized starch) keeping all other

ingredients constant.

Preparation of seal coating solution:

1. Weighed the required amount of HPMC 5cps (seal coating material).

2. Required quantity of water was taken in a mixing vessel.

3. Stirred the water with the help of a propeller in the center and as close to the

RESEARCH ARTICLE T.Vijay et.al / IJIPSR / 2 (8), 2014, 1708-1728

Department of Pharmaceutics ISSN (online) 2347-2154

Available online: www.ijipsr.com August Issue 1711

bottom of the vessel, so that a vortex formed without drawing any air.

4. Now, HPMC was added to the vortex slowly so that powder floatation on the

vortex can be avoided. Increased the speed to maintain the vortex.

5. After completion of adding all the HPMC, reduced the mixer speed to eliminate

the vortex.

6. Then, it was stirred under low agitation for about 45 min.

7. Coating was carried out in conventional coating pan.

Preparation of enteric coating solution:

1. Usually the solvents, water for Kollicoat MAE 30 DP and Aqoat was taken in a

mixing vessel.

2. The required quantity of enteric polymers were weighed and added to the above

beakers containing water.

3. Then specified amount of Tri ethyl citrate was added and stirred for 30 min to get

uniform dispersion of coating material.

4. At last, the sub-coated tablets were coated using above prepared solutions in

conventional coating pan.

5. The coating suspension was applied at the same day as it was prepared.

Table 1: Coating conditions

SL. NO PARAMETERS LIMITS

1 Pan speed 25-27 rpm

2 Inlet air temperature 50-70 C 3 Exhaust air temperature 30 C 4 Gun to bed distance 8cm

5 Atomizing air pressure 1-2 kg/cm

6 Spray gun nozzle diameter 1mm

7 Spray rate 1.0 - 2.0 mL/min

Table 2: Core tablet formulations

Sl. No INGREDIENTS FORMULATIONS qty./ tab (mg)

F1 F2 F3 F4

1 Ilaprazole 10 10 10 10

2 MCC pH102 90 90 90 90

3 Mannitol 86 86 86 86

4 Crosspovidone 8 - - -