Evaluation of Anti-GERD Activity of Gastro Retentive Drug Delivery System of Itopride Hydrochloride

Figures & data

Figure 1. Plot of particle size distribution.

Figure 2. Scanning electron micrographs of floating sodium alginate microspheres of itopride hydrochloride.

Table 1. Drug content analysis of sodium alginate microspheres of itopride (10% & 20% drug loaded)

Sr. No.	Theoretical drug content per 100 ml (mg)	Practical drug content per 100 ml (mg)	Percentage drug content (%)
10% Drug load
1.	2	1.12	56.0
2.	2	1.04	52.0
3.	2	1.08	54.0
20% Drug load
1.	4	2.45	61.25
2.	4	2.25	56.25
3.	4	2.10	52.5

Table 2. In vitro release studies of microspheres of itopride (10%) & (20%) loaded in sodium alginate

	Time Interval in Hours	Cum. Drug Release	% Cum. Drug Release	Time Interval in Hours	Cum. Drug Release	% Cum. Drug Release
Sr. No	10%			20%
1	0.5	02.70	05.40	0.5	03.600	07.20
2	1	04.50	09.00	1	05.410	10.82
3	2	08.10	16.20	2	08.770	17.54
4	3	11.70	23.40	3	12.375	24.75
5	4	15.30	30.60	4	17.110	34.22
6	5	18.90	37.80	5	22.050	44.10
7	6	22.95	45.90	6	26.550	53.10
8	12	46.19	92.38	12	49.210	98.42

Table 3. Results of anti-ulcer activity of different itopride formulations in pylorus ligated rat model

		Ulcer Index
		30 min. after drug administration		6 hrs. after drug administration
Sl. No.	Group	Stomach	Esophagus	Stomach	Esophagus
1.	Control	10.42±0.2386	3.167±0.1667	10.42±0.2386	3.167±0.1667
2.	Marketed Preparation	4.583**±0.2386	1.833**±0.1667	3.750**±0.1118	1.417**±0.1537
3.	Sodium Alginate Microspheres.	5.667**±0.2108	2.250**±0.2141	3.000**±0.1826	1.000**±0.1291

One Way ANOVA – ***P<0.0001

Dunnet's “t” Test: **P<0.01

Table 4. Results of antacid activity of different itopride formulations in pylorus ligated model (after 6 hrs. of drug administration) in rats

		Antacid activity (Pylorus ligation 6 hrs. after drug administration)
Sl. No.	Group	Total gastric volume (in ml.)	pH	Free Acidity (Meq/Lit./100gm)	Total Acidity (Meq/Lit./100gm)
1.	Control	6.050±0.1147	1.667±0.08819	39.33±1.563	80.00±3.141
2.	Marketed Preparation	4.867**±0.1333	2.300**±0.1880	37.33NS±0.9189	73.17NS± 1.740
3.	Sodium Alginate Microspheres	3.950**±0.1057	3.467**±0.08819	28.50**±1.544	59.67**± 1.453

One Way ANOVA – ***P<0.0001

Dunnet's “t” Test: **P<0.01

NS – Non-Significant

Table 5. Effects of different itopride formulations on gastrointestinal motility in rat model

		Gastrointestinal motility (in cm.) length of charcoal meal travelled
Sl. No.	Group	30 min. after drug administration	6 hrs. after drug administration
1.	Control	31.98±1.258	31.98±1.258
2.	Marketed Preparation	73.63**±0.9982	88.90** ±0.7659
3.	Sodium Alginate Microspheres	43.30**±1.013	99.00** ±0.2582

One Way ANOVA – ***P<0.0001

Dunnet's “t“ Test: **P<0.01

Figure 3. Measurement of length of intestine traveled by charcoal.