Development and Characterisation of Valsartan Immediate Release Dosage Form Using Solubility Enhancement Technique

Formulation code	Carriers	Drug to polymer ratio
PM1	β-cyclodextrin	1:3
PM2	β-cyclodextrin	1:4
PM3	β-cyclodextrin	1:5
PM4	PVP K30	1:3
PM5	PVP K30	1:4
PM6	PVP K30	1:5
PM7	Poloxamer 188	1:3
PM8	Poloxamer 188	1:4
PM9	Poloxamer 188	1:5

[i] PM, physical mixtures; PVP K30, polyvinyl pyrrolidone K30.

Table 2.

Formulation of valsartan immediate release tablets (IF1–IF3).^a

Formulation code	VAL physical mixture	SSG (mg)	Lactose (mg)	Magnesium stearate (mg)	Total (mg)
IF1	200	6.9	20.8	2.3	230
IF2	200	9.2	18.5	2.3	230
IF3	200	11.5	16.2	2.3	230

a Each batch contains 60 tablets.

IF, immediate release formulation; SSG, sodium starch glycolate; VAL, valsartan.

(a) Calibration curve of valsartan in a pH 1.2 buffer and (b) The wavelength scan or ultraviolet spectrum of valsartan.

Table 3.

Concentration versus absorbance values of valsartan in 0.1 N Hydrochloric acid.

No.	Valsartan
No.	Concentration (μg/mL)	Absorbance (205 nm)
1	2	0.223±0.29
2	4	0.402±0.24
3	6	0.543±0.20
4	8	0.707±0.16
5	10	0.862±0.11
6	12	1.029±0.09

[i] Note: All values are expressed in mean±SD (n=3).

Fourier transform infrared spectroscopy of (a) Valsartan, (b) Poloxamer 188, (c) Sodium starch glycolate and (d) IF2 optimised formulation. IF, immediate release formulation.

Differential scanning calorimetry thermogram of (a) Valsartan, (b) Poloxamer 188, (c) Sodium starch glycolate and (d) IF2 optimised formulation. IF, immediate release formulation.

X-ray diffraction pattern of (a) Valsartan, (b) Poloxamer 188, (c) Sodium starch glycolate and (d) IF2 optimised formulation. IF, immediate release formulation.

Scanning electron microscope images of (a) Valsartan, (b) Sodium starch glycolate and (c) IF2 optimised formulation. IF, immediate release formulation.

Table 4.

In vitro drug release data of valsartan solid dispersions (PM1–PM9) using different carriers.

Time (min)	PM1	PM2	PM3	PM4	PM5	PM6	PM7	PM8	PM9
5	6.12±0.2	7.42±1.3	10.2±2.4	14.8±0.2	12.9±1.1	12.7±2.1	11.7±1.0	26.4±0.3	34.4±0.2
10	10.3±0.5	11.8±1.4	14.7±2.1	20.0±0.4	25.8±1.3	19.4±1.2	37.3±1.2	51.9±0.5	60.1±2.0
15	12.1±0.7	16.5±1.6	22.1±2.6	25.6±0.2	36±1.4	60.3±1.1	57.3±1.3	70.5±0.6	74.5±2.2
30	22.4±0.9	31.7±1.9	27.0±2.7	43.5±0.1	72.2±1.1	72.9±0.2	68.3±1.5	94.2±0.8	96.8±2.0
45	27.7±1.2	41.8±2.6	46.3±2.8	49.4±0.2	98.7±1.1	79.8±0.2	85.9±1.0	96.9±0.9	99.6±1.0
60	39.8±1.5	44.8±2.1	58.3±2.1	75.7±0.9	100.2±1.6	99. 6±0.1	91.4±0.1	99.9±1.0	99.6±1.1

[i] Note: All values are expressed in mean±SD (n=3).

[ii] PM, physical mixture.

Table 5.

Flow properties of valsartan immediate release formulations (IF1–IF3).

Formulation code	Angle of repose (º)	Bulk density (g/cm³)	Tapped density (g/cm³)	Compressibility index (%)	Hausner’s ratio
VAL	42.54±0.2	542±0.2	522±1.1	27.38±1.1	1.37±2.0
IF1	28.36±0.3	600±0.6	666.6±1.2	9.99±1.2	1.11±1.3
IF2	22.92±0.6	500±0.5	600±1.5	6.66±2.0	1.12±0.6
IF3	28.88±0.5	461.5±30.9	491.8±2.0	6.15±2.5	1.06±3.2

[i] Note: All values are expressed in mean±SD (n=3).

[ii] IF, immediate release formulation; VAL, valsartan.

Table 6.

Postcompression parameters of valsartan immediate release formulations (IF1–IF3).

Formulation code	Weight variation^a (mg)	Hardness^b (Kg)	Thickness^c (mm)	Friability^d (%)	Drug content^e (%)	Disintegration^b (min)
IF1	215.3±2.5	4.75±0.3	2.03±0.5	0.228±0.3	92.66±3.5	5.3±0.2
IF2	212.3±2.5	4.56±0.3	2.12±0.1	0.456±0.9	97.15±1.4	6.2±0.4
IF3	218.3±1.5	4.75±0.3	2.09±0.4	0.227±2.1	100.3±0.8	4.5±2.1

Note: All values are expressed in mean±SD.

a n=20.

b n=3.

c n=30.

d n=10.

e n=6.

IF, immediate release formulation.

In vitro drug release profile of (a) Valsartan Pure drug with immediate release tablets (IF1–IF3) and (b) Valsartan IF2 optimised formulation with marketed product.

Table 7.

Stability studies of valsartan immediate release formulation (IF2).

Storage condition	Duration (months)	Drug content^a (%)	Disintegration (min)^b	Drug release at 1 hr
Initial	0	97.15±1.4	6.2±0.4	99.69±0.01
Accelerated (40±2°C at 75±5% RH)	6	96.99±1.1	6.1±0.2	99.64±0.02
Long term (25±2°C at 60±5% RH)	12	97.11±0.9	6.1±0.5	99.59±0.03

[i] Note: All values are expressed in mean±SD, (Where: a - n=6, b - n=3).

[ii] IF, immediate release formulation, RH - Relative Humidity

References

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Articles in this issue

DOI: https://doi.org/10.2478/afpuc-2024-0005 | Journal eISSN: 2453-6725 (formerly 1338-6786) | Journal ISSN: 0301-2298

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Language: English

Page range: 32 - 42

Submitted on: Dec 29, 2023

Accepted on: Apr 4, 2024

Published on: Jun 7, 2024

Published by: Comenius University in Bratislava, Faculty of Pharmacy

In partnership with: Paradigm Publishing Services

Keywords:

Immediate release tablets,

valsartan,

β-cyclodextrin,

poly vinyl pyrrolidone K30,

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© 2024 R. Saripilli, P. Teella, Kalakonda S. Nataraj, published by Comenius University in Bratislava, Faculty of Pharmacy
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Volume 71 (2024): Issue 1 (August 2024)

Development and Characterisation of Valsartan Immediate Release Dosage Form Using Solubility Enhancement Technique

Figures & Tables

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Table 2.

Figure 1.

Table 3.

Figure 2.

Figure 3.

Figure 4.

Figure 5.

Table 4.

Table 5.

Table 6.

Figure 6.

Table 7.

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