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

R. Saripilli
R. Saripilli
, 
P. Teella
P. Teella
 e 
Kalakonda S. Nataraj
Kalakonda S. Nataraj
   | 07 giu 2024
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Article Category: Original Paper
Pubblicato online: 07 giu 2024
Pagine: -
Ricevuto: 29 dic 2023
Accettato: 04 apr 2024
DOI: https://doi.org/10.2478/afpuc-2024-0005
Parole chiave
© 2024 R. Saripilli et al., published by Sciendo
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Figure 1.

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

Figure 2.

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

Figure 3.

Differential scanning calorimetry thermogram 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.

Figure 4.

X-ray diffraction pattern 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.

Figure 5.

Scanning electron microscope images of (a) Valsartan, (b) Sodium starch glycolate and (c) 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.
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
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 variationa (mg) Hardnessb (Kg) Thicknessc (mm) Friabilityd (%) Drug contente (%) Disintegrationb (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 contenta (%) 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
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