Improved Dissolution Time and Oral Bioavailability of Pioglitazone Using Liquisolid Tablets: Formulation, <i>In Vitro</i> Characterization, and <i>In Vivo</i> Pharmacokinetics in Rabbits

In the current study, it was intended to prepare liquisolid tablets of pioglitazone HCl to improve the bioavailability and dissolution time of the drug, as it has low solubility in water. Mathematical formulas were adopted, and the quantities of the carrier (MCC), coating material (colloidal silicon dioxides), and nonvolatile liquid vehicle (Tween 80) were taken. Various ratios of the drug to liquid and carrier to coating had been used in the formulation of liquisolid compacts. The evaluation of the formulated liquisolid compacts was done by performing FTIR, DSC, XRD, and SEM studies. Postcompression parameters, dissolution, stability, and bioavailability were accessed for the optimized formulation. FTIR and DSC studies showed the compatibility of the drugs and excipients. XRD revealed the transition to the amorphous state. It was found that the properties of the newly manufactured liquisolid tablets were within the parameters of what is considered acceptable. The optimized formulation of LST10 showed 99.87 ± 0.19% (<i>p</i> < 0.05) pioglitazone released within 60 min of dissolution. Dissolution data treatments (<i>Q</i> <sub>15</sub>, IDR, RDR, %DE, MDT, <i>f</i> <sub>1</sub>, and <i>f</i> <sub>2</sub>) resulted in better drug release than other drugs studied and marketed tablet formulations. The optimized formulation produced had been proven stable when it was subjected to accelerated stability testing. This suggested that the bioavailability of pioglitazone was enhanced, as indicated by the substantial increase in AUC<sub>0-<i>t</i></sub> (3.06-fold) and <i>C</i> <sub>max</sub> (4.18-fold). According to the findings, the selected combination and method significantly increased the dissolution time and bioavailability of pioglitazone. Moreover, this developed method can be used for other drugs with low water solubility.

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Publication Details

Journal
ACS Omega
Published
2024-10-08
DOI
https://doi.org/10.1021/acsomega.3c09145
Citations
4
Primary Topic
Drug Solubulity and Delivery Systems
Type
article
Field-Weighted Citation Impact
0.83
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article

Improved Dissolution Time and Oral Bioavailability of Pioglitazone Using Liquisolid Tablets: Formulation, In Vitro Characterization, and In Vivo Pharmacokinetics in Rabbits

Abhishek Bhattacharjee, Ranjit Prasad Swain, Jiyauddin Khan, Ram Kumar Sahu et al.
4 citations
ACS Omega
Drug Solubulity and Delivery Systems
0.83
article

Improved Dissolution Time and Oral Bioavailability of Pioglitazone Using Liquisolid Tablets: Formulation, In Vitro Characterization, and In Vivo Pharmacokinetics in Rabbits

Abhishek Bhattacharjee, Ranjit Prasad Swain, Jiyauddin Khan, Ram Kumar Sahu, Gamal Osman Elhassan
article en
4 citations

Abstract

In the current study, it was intended to prepare liquisolid tablets of pioglitazone HCl to improve the bioavailability and dissolution time of the drug, as it has low solubility in water. Mathematical formulas were adopted, and the quantities of the carrier (MCC), coating material (colloidal silicon dioxides), and nonvolatile liquid vehicle (Tween 80) were taken. Various ratios of the drug to liquid and carrier to coating had been used in the formulation of liquisolid compacts. The evaluation of the formulated liquisolid compacts was done by performing FTIR, DSC, XRD, and SEM studies. Postcompression parameters, dissolution, stability, and bioavailability were accessed for the optimized formulation. FTIR and DSC studies showed the compatibility of the drugs and excipients. XRD revealed the transition to the amorphous state. It was found that the properties of the newly manufactured liquisolid tablets were within the parameters of what is considered acceptable. The optimized formulation of LST10 showed 99.87 ± 0.19% (<i>p</i> < 0.05) pioglitazone released within 60 min of dissolution. Dissolution data treatments (<i>Q</i> <sub>15</sub>, IDR, RDR, %DE, MDT, <i>f</i> <sub>1</sub>, and <i>f</i> <sub>2</sub>) resulted in better drug release than other drugs studied and marketed tablet formulations. The optimized formulation produced had been proven stable when it was subjected to accelerated stability testing. This suggested that the bioavailability of pioglitazone was enhanced, as indicated by the substantial increase in AUC<sub>0-<i>t</i></sub> (3.06-fold) and <i>C</i> <sub>max</sub> (4.18-fold). According to the findings, the selected combination and method significantly increased the dissolution time and bioavailability of pioglitazone. Moreover, this developed method can be used for other drugs with low water solubility.

ACS OmegaVol. 9(42)
Management and Science University (MY), Qassim University (SA), Hemwati Nandan Bahuguna Garhwal University (IN), Siksha O Anusandhan University (IN), Assam University (IN), GITAM University (IN)
Clean water and sanitation
Openalex Percentile: Top 31%
Drug Solubulity and Delivery Systems
0.83
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