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FORMULATION AND EVALUATION OF TASTE MASKED ORODISPERSIBLE TABLETS BY ION – EXCHANGE RESINS


2. FORMULATION OF TASTE MASKED ORO-DISPERSIBLE TABLETS OF ONDANSETRON HYDROCHLORIDE-(28)
INTRODUCTION-
Ondansetron hydrochlorideis commonly used as anti emetic. But it is a very bitter drug and slightly soluble in water. So in the work under taken an attempt was made to mask the taste and to formulate into a dispersible tablet by complexation with ion exchange resins, which also acts as super disintegrating agents. Since, these tablets can be swallowed in the form of dispersion; it is suitable dosage form for pediatric and geriatric patients. Cationic exchange resins like Indion-204, Indion-234 and Tulsion-335 were utilized for the sorption of drug.

PREPARATION OF DRUG-RESINATE COMPLEX-
Ion exchange resins like Indion- 204 Tulsion-335, Indion-234 were pretreated with 1N HCl and1N NaOH in order to remove impurities. Drug and resins were mixed in various ratios 1:1 to 1:6 on weight basis and stirred at magnetic stirrer for a period of 4 to 8 hours using deionised water. The resinate obtained was separated by filtration and dried. Non bitter complex was yielded at 1:6,1:5 and 1:6 drug to resin ratio using deionised water of pH 7 and also maximum percentage drug loading( 96.5, 99.1 & 98.8 %) was determined at the same ratio.

FORMULATION OF ORO-DISPERSIBLE TABLETS-

Formulation of tablets formulated with resins Indion-204 (F1), Indion-234 (F2) & Tulsion-335(F3)

EVALUATION OF TABLETS-

All the tablets passed weight variation test, as percentage weight variation was within the pharmacopoeial limits i.e.±7.5%. To be complied with the pharmacopoeial standards, dispersible tablets must disintegrate within 3 minutes. But formulated products have exhibited very less disintegrating time (i.e.14, 21 and 20 seconds), indicating that all three formulations were suitable for oro-dispersible tablets.

3.FORMULATION OF TASTE MASKED ORO-DISPERSIBLE TABLET OF METOCLOPRAMIDE HYDROCHLORIDE-(29)
INTRODUCTION-
Metoclopramide hydrochloride a derivative of paraaminobenzoic acid is a commonly prescribed drug used for the management of gastrointestinal disorders such as gastric stasis, gastro esophageal reflux and for the prevention of cancer chemotherapy- induced emesis. In general, emesis is preceded with nausea and in such condition it is difficult to administer drug with a glass of water; hence it is beneficial to administer such drugs as ODTs. Metoclopramide HCl is an intensely bitter drug; hence, if it is incorporated directly into an ODT the main objective behind formulation of such a dosage form will definitely get futile.
Here we formulate oro-dispersible tablet by taste masking with Indion234.

PREPARATION OF DRUG RESIN COMPLEX-
Metoclopramide Hydrochloride resinate was prepared using a batch process. For preliminary study, we optimized the ratio of resin to drug at 1:3. Resin (3 g) was placed in an Erlenmeyer flask and then 250 ml of distilled water was added. The mixture was shaken in the water bath at 370C. The supernatant was collected and assayed spectrophotometrically at a wavelength of 273 nm (Techcomp, UV 2300, and Shanghai, Japan) to determine the drug-loading equilibrium time. Then, the Metoclopramide Hydrochloride resinates were separated from the filtrates by filtration, washed several times with distilled water, dried overnight at 500C and kept in a desiccators.

FORMULATION OF ORO-DISPERSIBLE TABLET-

Sr. No.  

Tablet Ingredient per Tablet (mg)    

F1

F2

F3

F4 

F5

F6

F7

1

DRC

43.3

43.3

43.3

43.3

43.3

43.3

43.3

2

Mannitol

96

-

48

64

72

32

24

3

MCC

-

96

48

32

24

64

72

4

Crosspovidone

7

7

7

7

7

7

7

5

Aspartame

1

1

1

1

1

1

1

6

Magnesium Stearate

2

2

2

2

2

2

2

7

Flavor

0.7

0.7

0.7

0.7

0.7

0.7

0.7

*-Drug resin complex (DRC) equivalent to 10 mg of Metoclopramide HCl.

EVALUATION OF TABLET-

BATCH NO.

FRIAB
ILITY

*

HARDNESS

KG/CM2

**

THICK
NESS

**

% WEIGHT
VARIATION

#

DISINTEGRA
TION TIME

SEC*

WETTING TIME

(SEC)@

%WATER ABSORPTION RATIO @

F1

0.78± 0.12

4.13±0.24      

2.40
± 0.05

 148.44±
1.50            

57.52±0.41       

10.04± 1.44        

84.64 ± 0.34

F2

0.75± 0.34

4.23±0.30

2.49 ± 0.02

150.71± 1.85

37.50 ± 1.04

10.91± 0.90

82.64 ± 0.21

F3

0.73± 0.36

4.19±0.29

2.50 ± 0.08

150.64± 1.66

25.55 ± 1.32

10.95± 1.31

88.80 ± 0.15

F4

0.76± 0.22

4.14±0.21

2.42 ± 0.09

151.70± 1.33

30.37 ± 0.66

11.09± 0.61

83.75 ± 0.20

F5

0.75± 0.44

4.25±0.26

2.45 ± 0.04

149.12± 2.23

45.24 ± 0.75

11.60± 1.23

78.8 ± 0.35

F6

0.71± 0.24

4.10±0.27

2.47 ± 0.03

150.57± 1.79

49.94 ± 1.34

11.68± 0.40

79.50 ± 0.32

F7

0.72± 0.59

4.45±0.12

2.52 ± 0.07

150.94± 1.45

57.09 ± 0.76

13.34± 1.10

75.43 ± 0.60

*n=3, ** n=6, # n=20, @n=3

Among seven batches, batch F3 which contain MCC and Mannitol in 1:1 ratio along with 7 mg of Crosspovidone was selected as optimized batch because of its lowest disintegration time and highest drug release.

4. FORMULATION OF TASTE MASKED ORODISPERSIBLE TABLETS OF TRAMADOL –(30)
INTRODUCTION-

Tramadol is a centrally acting opioid analgesic structurally related to codeine and morphine used in the treatment of moderate to severe pain in diverse conditions. Combined with low dependence/abuse potential, it has proven to be of significant advantage over other agents, especially in the elderly.

Here bitter taste of Tramadol is masked by forming complex with Tulsion 335.
PREPARATION OF DRC-

Batch method was used to prepare drug–resin complex (DRC). Five grams of Tulsion 335 was allowed to swell for 90 min in a beaker containing 200 ml of deionized water of conductivity less than 2. Then, 5 g of Tramadol HCl was added to it and stirred for 300 min. The mixture was filtered through Whatman filter paper no. 41. The residue was washed with 100 ml of deionized water and dried.

FORMULATION OF ORO-DISPERSIBLE TABLET-

EVALUATION OF TABLETS-


The outcomes of various evaluation parameters are shown in Tables. The dissolution studies indicated 100% drug release within 20 min from all batches. All batches showed DT less than a minute and friability less than 1.02%.

5. FORMULATION OF ORO-DISPERSIBLE TABLET OF AMBROXOL HYDROCHLORIDE-(31)

INTRODUCTION-
Ambroxol hydrochloride (HCL) is a potent mucolytic capable of inducing bronchial secretion. It is used in the treatment of asthma, bronchitis, and cough. But it is a very bitter drug and slightly soluble in water. Thus, in the work under taken, an attempt was made to mask the taste and to formulate into a oro-dispersible tablet by complexation with ion exchange resins (Indion-204 and Indion-234), which also acts as super disintegrating agents.

PREPARATION OF DRC-
Ion exchange resins like Indion 204 and Indion 234 were pretreated with 1N HCl and 1N NaOH in order to remove impurities. Drug and resins were mixed in various ratios 1:1 to 1:6 on weight basis and stirred at magnetic stirrer for a period of 4 to 8 h using deionized water. The resinate obtained was separated by filtration and dried. Non bitter complex was yielded at 1:5 and 1:6 drug to resin ratio using deionized water of pH 7 and also maximum percentage drug loading (96.5 and 98.8 percent) was determined at the same ratio.

FORMULATION OF ORO-DISPERSIBLE TABLET-

DRUG RELEASE PROFILES-


M  stands for Marketed preparation
All the tablets passed weight variation test, as % weight variation was within the pharmacopoeial limits i.e., ±7.5%. To be compliance with the pharmacopoeial standards, dispersible tablets must disintegrate within 3 min. But, formulated products have exhibited very low disintegrating time (i.e., 14 and 21 seconds), indicating that both formulations were suitable for oro-dispersible tablets. In the in- vivo disintegration time, wetting time was observed to be very fast in F 1 formulation when compared to F 2 and marketed product.

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