Quality-by-Design based development and characterization of pioglitazone loaded liquisolid compact tablets with improved biopharmaceutical attributes

Bonthagarala, Brahmaiah; Dasari, Varun; Kotra, Vijay; Swain, Sanjit Kumar; Beg, Sarwar

doi:10.1016/j.jddst.2019.03.033

Cited by 22 publications

(12 citation statements)

References 24 publications

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“…Scanning Electron Microscope (SEM) is used to determine the surface structure or morphology of a sample to produce a different form between the active material and the modified result. The results of the SEM in the liquisolid formula showed a change in the pure active ingredients with the results of the liquisolid formula, the results of the liquisolid formula of surface morphology were not found in crystalline form but rather in the form of amorphous (25).…”

Section: Scanning Electron Microscope (Sem)mentioning

confidence: 64%

Enhancement of Solubility BCS Class II and IV Pharmaceuticals by Liqusolid Technique: A review

2020

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Many techniques can be used to improve drug solubility, which is the development of the liquisolid technique. This technique has a mechanism for increasing the surface area of the drug as well as wetting from the addition of non-volatile solvents resulting in a lower surface tension and contact angle, so the solubility and drug release very increases. Liquisolid tablets show a lower contact angle compared to the conventional tablets. The liquisolid technique approach is also promising because the process is simple in making low production costs and allows the manufacturing industry, including non-volatile solvents, fillers, dryers, and disintegrants. Liquisolid characterized by specific instruments such as powder x-ray diffraction (PXRD), Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscope (SEM). Several liquisolid techniques are described in this review. The liquisolid technique is proven and able to change the physicochemical properties of active pharmaceutical ingredients, especially the solubility, drug release, and stability of the formula so that this technique can be a solution for class II and IV BCS pharmaceutical active drug classes.Keywords: Active Pharmaceutical Ingredients, Contact Angle, Solubility, Drug Release, Stability, Liquisolid Technique

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Section: Scanning Electron Microscope (Sem)mentioning

confidence: 64%

Enhancement of Solubility BCS Class II and IV Pharmaceuticals by Liqusolid Technique: A review

2020

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“…However, this technology has gained increased research interest more recently, and during the last decade enhanced dissolution from LS systems has been reported for various poorly soluble drugs (3)(4)(5)(6)(7)(8). Furthermore, recently reported in vivo studies showed improved bioavailability in the case of LS systems with different poorly soluble drugs (9)(10)(11)(12)(13)(14)(15).…”

Section: Introductionmentioning

confidence: 99%

Liquisolid systems: Evaluation of the influence of formulation variables on the optimum liquid load

Aleksić¹,

Glišić²,

Cvijić³

et al. 2022

Arhiv za farmaciju

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Liquisolid systems represent an emerging approach in the preparation of solid dosage forms with liquid lipophilic drug or poorly water-soluble drug solution/suspension in suitable liquid vehicle. This study addresses the lack of data regarding the compaction behavior of liquisolid systems, with the aim to investigate the influence of liquid load, carrier to coating ratio, carrier type (microcrystalline cellulose vs. spray dried calcium hydrogen phosphate, anhydrous (Fujicalin®)) on flowability and compaction properties of liquisolid systems and to determine the optimum liquid loads. Liquisolid admixtures with Fujicalin® showed notably better flowability than those with microcrystalline cellulose. An increase in carrier to coating ratio led to enhanced flowability of the admixtures. Compacts with Fujicalin® had good mechanical properties up to 24.7% liquid, while those with microcrystalline cellulose had acceptable mechanical strength up to 16.2% liquid. Liquisolid systems with Fujicalin® showed similar tabletability profiles as those with microcrystalline cellulose, despite having higher liquid content. The ejection stress values indicated that the addition of lubricant might be needed in the case of liquisolid systems with Fujicalin®. Superior properties of Fujicalin® as a carrier for liquisolid tablets were revealed, and dynamic compaction analysis was found to be a valuable tool for the assessment of compaction behavior of liquisolid systems.

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“…[4] Due to low aqueous solubility and restricted intestinal permeability, around 40% of newly discovered drug encounters significant biopharmaceutical difficulties, resulting in poor drug absorption and minimal ORIGINAL ARTICLE therapeutic benefits. [5] Various methods have been employed to increase the dissolution rate of rosuvastatin calcium which involves SNEDDS, [6] nanoparticles, [7] SEDDS, [8] and niosomes. [9] The liquisolid compact technique aims to improve the dissolution rate of the poorly water-soluble drug belongs to BCS Class II and IV by employing the cosolvency approach which is a low cost-effective technique compared to other methods.…”

Section: Introductionmentioning

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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Quality-by-Design based development and characterization of pioglitazone loaded liquisolid compact tablets with improved biopharmaceutical attributes

Cited by 22 publications

References 24 publications

Enhancement of Solubility BCS Class II and IV Pharmaceuticals by Liqusolid Technique: A review

Enhancement of Solubility BCS Class II and IV Pharmaceuticals by Liqusolid Technique: A review

Liquisolid systems: Evaluation of the influence of formulation variables on the optimum liquid load

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