Controlling atorvastatin release from liquisolid systems

Saeedi, Majid; Âkbari, Jafar; Morteza‐Semnani, Katayoun; Hashemi, Seyyed Mohammad Hassan; Ghasemi, Shaghayegh; Tahmasbi, Nima; Azizpoor, Elham; Faghani, Nafiseh; Rostamkalaei, Seyyed Sohrab; Nokhodchi, Ali

doi:10.1080/01932691.2020.1842211

Cited by 6 publications

(1 citation statement)

References 19 publications

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“…From the inference of Korsmeyer-Peppas "n-value," the drug release mechanism can be identified for the liquisolid formulation (F2). [22]…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

Untitled

2021

IJGP

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Aim:The main aim of the investigation was to enhance the dissolution rate of rosuvastatin calcium by formulating it as a liquisolid tablet and compare with a marketed formulation. Materials and Methods: Rosuvastatin calcium liquisolid tablets were formulated using propylene glycol and PEG 400 as a non-volatile liquid vehicle, Avicel pH 102, and Aerosil 200 as carrier and coating material, sodium starch glycolate as superdisintegrant. The formulated rosuvastatin calcium liquisolid tablet was evaluated for pre-compression parameters to increase the flow property of the drug and post-compression parameters. The in vitro drug release characteristics of rosuvastatin calcium liquisolid formulation were performed using pH 6.8 phosphate buffer as dissolution media and compared with the marketed formulation and direct compressible tablet. The analytical study of drug excipient interaction of rosuvastatin calcium was characterized by Fourier transform infrared (FT-IR) and DSC analysis. Results and Discussion:The solubility profile of rosuvastatin calcium in propylene glycol and PEG 400 was found to be higher than the other non-volatile liquid vehicle. The formulated rosuvastatin calcium liquisolid tablet (F1, F2, F3, F5, and F6) has accepted flow properties. The post-compression evaluation data of thickness, weight variation, hardness, friability, disintegration, drug content comply with the Indian Pharmacopoeia limits. Among the eight liquisolid formulations (F2) showed the highest percentage of drug release 99% at 60 min, whereas, marketed formulation showed 86.2% of drug release at 60 min. The FT-IR analysis revealed that there is no interaction between drug and excipient. DSC analysis of liquisolid formulation (F2) confirmed the conversion of crystalline state to amorphous form. A significant difference (P = 0.002 < 0.05) was found in the dissolution rate of the best formulation (F2) when compared with the marketed formulation. Conclusion: It can be concluded from the research work that liquisolid compact technique is a promising method of approach for the dissolution rate enhancement of rosuvastatin calcium due to increased wetting property and more drug surface exposed to the dissolution medium.

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“…From the inference of Korsmeyer-Peppas "n-value," the drug release mechanism can be identified for the liquisolid formulation (F2). [22]…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

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2021

IJGP

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Applying liquisolid technique to enhance curcumin solubility: a central composite design study

Aghajanpour,

Yousefi Jordehi,

Farmoudeh

et al. 2024

Chem. Pap.

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Turmeric, specifically its curcuminoids such as curcumin (C21H20O6), possesses extensive therapeutic benefits including anti-inflammatory, anticancer, and anti-aging properties. However, curcumin’s clinical effectiveness is significantly limited by its hydrophobic nature, leading to poor bioavailability. This study aims to enhance the solubility and bioavailability of curcumin through the development of liquisolid compact dispersion formulations. To address curcumin’s limited water solubility (3.12 mg/l at 25 °C) and high oil–water partition coefficient ($$\text{log}Kow=3.29$$ log K o w = 3.29 ), we employed a central composite design (CCD) to optimize liquisolid compact dispersion formulations. The optimization focused on the tablet’s physical properties, such as hardness, disintegration time, and dissolution rate at 30 min. Critical formulation components included Tween 80 as the liquid vehicle and Aerosil 200 as the coating material, serving as independent variables in the optimization process. The optimized formulation, containing 30 mg of Tween 80 and 75 mg of Aerosil 200, significantly improved curcumin’s dissolution rate. Experimental results confirmed the formulation’s effectiveness, with a marked reduction in the time to dissolve 63.2% of the drug to 165 min, compared to 300 min for conventional formulations. Differential scanning calorimetry and Fourier-transform infrared spectra indicated a transformation of curcumin into a non-crystalline state and the formation of hydrogen bonds with Tween 80, contributing to enhanced solubility. This study successfully demonstrates a viable strategy to enhance the bioavailability of curcumin through liquisolid compact dispersion formulations. By addressing the solubility challenges of curcumin, this technique presents a significant advancement in improving the clinical applicability of BCS class II and IV drugs, potentially benefiting a wide range of therapeutic applications. Graphical abstract

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

Swain,

Elhassan,

Bhattacharjee

et al. 2024

ACS Omega

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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% (p < 0.05) pioglitazone released within 60 min of dissolution. Dissolution data treatments (Q 15 , IDR, RDR, %DE, MDT, f 1 , and f 2 ) 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 0−t (3.06-fold) and C max (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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Controlling atorvastatin release from liquisolid systems

Cited by 6 publications

References 19 publications

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Applying liquisolid technique to enhance curcumin solubility: a central composite design study

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

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