Development and evaluation of solid dispersion based rapid disintegrating tablets of poorly water-soluble anti-diabetic drug

Sakure, Kalyani; Kumari, Leena; Badwaik, Hemant

doi:10.1016/j.jddst.2020.101942

Cited by 15 publications

(11 citation statements)

References 15 publications

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“…The mixture was stirred continuously for 48 h, maintaining a temperature of 37 ± 0.5 • C with a water bath. Then the sample was filtered and analyzed for the drug concentration after suitable dilutions using a UV-visible spectrophotometer at 265 nm [18][19][20].…”

Section: Determination Of Saturation Solubilitymentioning

confidence: 99%

Development and Characterization of Oral Raft Forming In Situ Gelling System of Neratinib Anticancer Drug Using 32 Factorial Design

et al. 2022

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Neratinib (NTB) is an irreversible inhibitor of pan-human epidermal growth factor receptor (HER-2) tyrosine kinase and is used in the treatment of breast cancer. It is a poorly aqueous soluble drug and exhibits extremely low oral bioavailability at higher pH, leading to a diminishing of the therapeutic effects in the GIT. The main objective of the research was to formulate an oral raft-forming in situ gelling system of NTB to improve gastric retention and drug release in a controlled manner and remain floating in the stomach for a prolonged time. In this study, NTB solubility was enhanced by polyethylene glycol (PEG)-based solid dispersions (SDs), and an in situ gelling system was developed and optimized by a two-factor at three-level (32) factorial design. It was analyzed to study the impact of two independent variables viz sodium alginate [A] and HPMC K4M [B] on the responses, such as floating lag time, percentage (%) water uptake at 2 h, and % drug release at 6 h and 12 h. Among various SDs prepared using PEG 6000, formulation 1:3 showed the highest drug solubility. FT-IR spectra revealed no interactions between the drug and the polymer. The percentage of drug content in NTB SDs ranged from 96.22 ± 1.67% to 97.70 ± 1.89%. The developed in situ gel formulations exhibited a pH value of approximately 7. An in vitro gelation study of the in situ gel formulation showed immediate gelation and was retained for a longer period. From the obtained results of 32 factorial designs, it was observed that all the selected factors had a significant effect on the chosen response, supporting the precision of design employed for optimization. Thus, the developed oral raft-forming in situ gelling system of NTB can be a promising and alternate approach to enhance retention in the stomach and to attain sustained release of drug by floating, thereby augmenting the therapeutic efficacy of NTB.

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Section: Determination Of Saturation Solubilitymentioning

confidence: 99%

Development and Characterization of Oral Raft Forming In Situ Gelling System of Neratinib Anticancer Drug Using 32 Factorial Design

et al. 2022

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“…SDs thus obtained were pulverized in a mortar and pestle and passed through sieve #80. Finally, the dried and pulverized product was preserved in desiccator for further use [23,24,[37][38][39][40]. Composition of the formulations is provided in Table 1.…”

Section: Preparation Of Sdsmentioning

confidence: 99%

“…SD in ternary mixture of SKM-U-CP SDs of ACF in ternary mixture of SKM-U-CP were prepared as before in the ratios of 1:5:0.75:0.25, 1:5:0.75:0.50, 1:5:0.75:0.75, and 1:5:0.75:1 [25,26,[37][38][39][40]. Composition of the formulations is provided in Table 1.…”

Section: Preparation Of Sdsmentioning

confidence: 99%

Formulation Development and in Vitro Characterization of Ternary Hydrotropic Solid Dispersions of Aceclofenac

SARKAR¹,

Majee²

2022

Asian J Pharm Clin Res

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Objective: Among the various strategies employed to enhance solubility, dissolution, and bioavailability of poorly soluble drugs in vivo, formulation of solid dispersion (SD) using hydrophilic and/or water-soluble carriers with varying physicochemical characteristics seems to be a developable, economically viable and easy option. The goal of the present study was to explore the possibilities of skimmed milk (SKM)-urea (U)-crospovidone (CP) as a novel ternary mixture of carrier-hydrotrope-superdisintegrant in SD of poorly water-soluble aceclofenac (ACF). Methods: Compatibility of ACF and ternary mixture of SKM-U-CP was confirmed by FTIR spectroscopic analysis. SDs of ACF-SKM, ACF-SKM-U and ternary hydrotropic SD, and ACF-SKM-U-CP were prepared in varying ratios of 1:1–1: 5 for ACF-SKM; 1:5:0.5, 1:5:0.75, and 1:5:1 for ACF-SKM-U and 1:5:0.75:0.25–1:5:0.75:1 for ACF-SKM-U-CP by solvent evaporation technique and were characterized by their solubility enhancement (compared to pure drug) at 25°C and drug dissolution profiles in double-distilled water and phosphate buffer (pH 6.8). Results: Based on solubility enhancement data (82.10% and 44.06%) and maximum cumulative percentage drug release data (88.45% in 9 min and 76.18% in 60 s) in double-distilled water and phosphate buffer, respectively, ACF-SKM-U(1:5:0.75) was found to the best among ACF-SKM and ACF-SKM-U SDs which were used for studying the effect of adding CP as superdisintigrant. ACF: SKM: U: CP (1: 5: 0.75: 0.50) exhibited maximum solubility enhancement of 83.92% and 49.69% and cumulative percentage release of 98.55 % in 9 min and 85.67 % in 60 s in double-distilled water and buffer, respectively. Conclusion: Therefore, the novel ternary mixture of SKM-U-CP has demonstrated marginal superiority over SKM as carrier for from hydrotropic SDs of ACF.

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“…The effect of crospovidone on disintegration and dissolution has been extensively investigated, mostly on tablets prepared with conventional technologies. Not only did formulation factors have an influence, the effects of crospovidone are also governed by the manufacturing process [53][54][55]. Compression pressure is reported as an important parameter for consideration [56,57].…”

Section: Effect Of Crospovidone On Drug Releasementioning

confidence: 99%

Understanding the Effect of Energy Density and Formulation Factors on the Printability and Characteristics of SLS Irbesartan Tablets—Application of the Decision Tree Model

et al. 2021

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Selective laser sintering (SLS) is a rapid prototyping technique for the production of three-dimensional objects through selectively sintering powder-based layer materials. The aim of the study was to investigate the effect of energy density (ED) and formulation factors on the printability and characteristics of SLS irbesartan tablets. The correlation between formulation factors, ED, and printability was obtained using a decision tree model with an accuracy of 80%. FT-IR results revealed that there was no interaction between irbesartan and the applied excipients. DSC results indicated that irbesartan was present in an amorphous form in printed tablets. ED had a significant influence on tablets’ physical, mechanical, and morphological characteristics. Adding lactose monohydrate enabled faster drug release while reducing the possibility for printing with different laser speeds. However, formulations with crospovidone were printable with a wider range of laser speeds. The adjustment of formulation and process parameters enabled the production of SLS tablets with hydroxypropyl methylcellulose with complete release in less than 30 min. The results suggest that a decision tree could be a useful tool for predicting the printability of pharmaceutical formulations. Tailoring the characteristics of SLS irbesartan tablets by ED is possible; however, it needs to be governed by the composition of the whole formulation.

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Development and evaluation of solid dispersion based rapid disintegrating tablets of poorly water-soluble anti-diabetic drug

Cited by 15 publications

References 15 publications

Development and Characterization of Oral Raft Forming In Situ Gelling System of Neratinib Anticancer Drug Using 32 Factorial Design

Development and Characterization of Oral Raft Forming In Situ Gelling System of Neratinib Anticancer Drug Using 32 Factorial Design

Formulation Development and in Vitro Characterization of Ternary Hydrotropic Solid Dispersions of Aceclofenac

Understanding the Effect of Energy Density and Formulation Factors on the Printability and Characteristics of SLS Irbesartan Tablets—Application of the Decision Tree Model

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