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

Saripilli, R.; Teella, P.; Nataraj, Kalakonda S.

doi:10.2478/afpuc-2024-0005

Figures & Tables

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

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.

Figure 6.

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.

Formulation of solid dispersions of valsartan using different carriers_

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

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

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

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

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

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

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

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

Figures & Tables

Figure 1.

Figure 2.

Figure 3.

Figure 4.

Figure 5.

Figure 6.

Formulation of solid dispersions of valsartan using different carriers_

Concentration versus absorbance values of valsartan in 0_1 N Hydrochloric acid_

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

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

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

Stability studies of valsartan immediate release formulation (IF2)_

Formulation of valsartan immediate release tablets (IF1–IF3)_a

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