Formulation, development and evaluation of solid dispersions for enhancement of solubility and dissolution rate of clopidogrel bisulfate

Patel, Anil Kumar; Budholiya, Prabhakar; Tyagi, Charu

doi:10.38164/ajper/9.4.2020.76-86

Cited by 3 publications

(3 citation statements)

References 7 publications

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“…The factors like Water concentration (X1), Oil (Krill oil) concentration (X2) and surfactant (Tween 80: Span 80): co-surfactant (Transcutol HP:Ethanol) (Smix) concentration (X3) which were found to have signi cant effect on globule size (Y1) during preliminary study were selected as independent variables (Table 1). Simplex lattice design using design of experiment software (Version 11.0, M/s Stat-Ease, Minneapolis, USA) [27] was used to nd optimum concentration of water, oil and Smix in order to achieve globule size less than 70nm. Globule size was measured by using Malvern zetasizer (Nano ZS, Malvern instruments, UK) which is based on dynamic light scattering principle [28].…”

Section: Development Of Pseudoternary Phase Diagrammentioning

confidence: 99%

Development and evaluation of novel krill oil-based clomiphene microemulsion as a therapeutic strategy for PCOS treatment

Panchal

Pandya

Kevlani

et al. 2023

Drug Deliv. and Transl. Res.

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Polycystic ovary syndrome (PCOS) is frequently diagnosed hormonal disorder with reproductive and metabolic complications. The most common symptoms include cyst in ovaries, anovulation, insulin resistance, and obesity. Clomiphene citrate, an ovulating agent, is the rst-line drug used to treat PCOS. We hypothesized that clomiphene citrate, by stimulating ovarian function, with krill oil used as an oil phase to improve solubility, by addressing PCOSassociated symptoms might be effective in PCOS. Hence, our goal was to target hormonal imbalance along with PCOS-associated symptoms using single formulation. The concentration of water (X1), oil (X2) and Smix(surfactantcosurfactant mixture) (X3) were selected as independent variables, in a simplex lattice design, from microemulsion area derived from pseuodoternary phase diagram while the globule size (Y1) was selected as dependent parameter. The optimized microemulsion showed good sphericity having 41 nm globule size, 0.32 Poly dispersibility index and + 31mV zeta potential. The optimized microemulsion was further evaluated in-vivo using letrozole induced PCOS rats. Formulation treated group reversed the effect of letrozole on body weight and oestrus cycle in comparison to disease control group (p < 0.001). The formulation was also effective in reducing insulin resistance, cholesterol and serum testosterone level (p < 0.001). The in-vivo results were supported by histopathological studies where formulation treated group showed a marked decrease in the number of cystic follicles and a remarkable increase in the number of growing follicles at variable stages, similar to the normal control group. Thus, the results con rmed that novel krill oil based clomiphene microemulsion may become promising therapeutic choice for treatment of PCOS.

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Section: Development Of Pseudoternary Phase Diagrammentioning

confidence: 99%

Development and evaluation of novel krill oil-based clomiphene microemulsion as a therapeutic strategy for PCOS treatment

Panchal

Pandya

Kevlani

et al. 2023

Drug Deliv. and Transl. Res.

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“…After 100 taps in a graded measuring cylinder, the volume remained steady., and the following equation was used to compute it. 18 Dt = (Powder Mass)/(powder Tapped volume) -----Equation 4• Carr's index (compressibility index) and Hausner's ratio calculation 19 The powder sample was placed into a measuring glass cylinder, and the volume of untapped material was measured, then the volume of tapped material was measured after each tap cycle until the volume remained constant, and the Carr's index was determined using the equation: Carr's index= (Tapped density -Bulk density) ÷ (Tapped density) ×100 -----Equation 5• Hausner's Ratio The Hausner's ratio displays the powder material's flow characteristic. It's the ratio of the powder's tapped density to its bulk density, and it's calculated using the equation below: Hausner's ratio= Tapped density ÷ Bulk density = Dt/Db ---------------Equation 6Evaluation of the Prepared Bilayer Tablets (Post Compression Parameter)…”

Section: Angle Of Reposementioning

confidence: 99%

Formulation and In-vitro Evaluation of Two Layers Tablet for Dual Release of a Model Drug

Mohammed¹,

Ali²

2023

IJDDT

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Objective: Glimepiride is a third-generation sulfonylurea medication that has been used to treat type 2 diabetes (T2D) mellitus. It is class II drug according to the biopharmaceutical classifi cation system (BCS) characterized with its low solubility and high permeability. Due to the drug’s weak water solubility, its bioavailability is restricted by its dissolving rate. This study aimed to develop a bilayer tablet of glimepiride with one layer for immediate release (IR), a dose of 2 mg, a second layer for sustained release (SR), and a 4 mg dose Immediate release layer included solid dispersion of glimepiride . Methods: Glimepiride solid dispersions were prepared utilizing four water-soluble carriers (poloxamer 188, polyethylene glycol (PEG6000), Kollicoat IR and soluplus) by solvent evaporation and fusion techniques at 1:1, 1:2, and 1:4 ratios and evaluated in 0.1 N of HCL buff er pH 1.2 with 1% of sodium lauryl sulphate (SLS) for 2 hours. utilizing a USP-II paddle-type dissolution apparatus containing 900 mL dissolution medium kept at 37 ± 0.5℃ and 50 rpm. The sustained release layer of glimepiride bilayer tablet was prepared using various polymers, including HPMC K15, HPMC K4, xanthan gum, carbopol 934 and ethyl cellulose at 1:1, 1:2,1:3 ratios and combination of polymers in phosphate buff er pH 6.8 for 12 hours. The prepared solid dispersion of immediate release were evaluated by X-ray powder diff raction (PXRD), and fourier transform infrared spectroscopy for selected SD9. The FTIR spectroscopy analysis for selected formula (F24) of sustained layer, angle of repose, Hausner’s ratio and Carr’s Index were used to evaluate the fl owability and compressibility of the formulation powders during the pre-compression investigations, while, thickness, hardness, weight variation, friability, drug content, for prepared tablets. Results: The results revealed that SD9 at ratio (1:4 glimepiride: soluplus) was the optimal formula since 94% of drug released at 2 hours for immediate layer formula 24, which included ethylcellulose polymer in a 1:1 ratio in the sustained layer of the tablet, was chosen as the optimal formula out of another formula (F1–F28), This formula demonstrated acceptable sustained properties of the glimepiride over the course of 12 hours. and approximately 96% of the medication was released. Conclusion: This study succussed in designing bilayer tablets containing glimepiride solid dispersion formulation in the fi rst immediate release layer and untreated pure drug formulation in the second layer for sustaining the release of the drug for a specifi c period of time to be used as the eff ective treatment of type II diabetes mellitus.

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“…17 The most generally been used carriers includes PVP, Tween 80, Gelucire, PEG, etc. 18,19 Deferasirox (DFX) belongs to Biopharmaceutical Classification System (BCS) class Π compound showing low solubility and high permeability. The critical parameter for deferasirox bioavailability is mainly its solubility.…”

Section: Introductionmentioning

confidence: 99%

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

Talla,

Wadher,

Umekar

et al. 2024

J. Drug Delivery Ther.

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Deferasirox, an oral iron-chelating agent, is a poorly soluble drug (Biopharmaceutical Classification System class II) having insufficient solubility in physiological fluids resulting in low bioavailability of the drug. The idea behind the present study was to explore the prospects of solid dispersion as a prolific method to enhance the dissolution rate of drug using a water soluble polymer. The solid dispersion was prepared by the solvent evaporation technique using Polyvinyl pyrrolidone with different drug to carrier and solvent ratio. Formulations were characterized through attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), Powder X-ray diffraction (XRD), and in vitro release studies. A 32 factorial design was implemented to obtain optimum solubility, % yield, and optimization of solid dispersion (SD) also quantitates the influence of PVP on the solubility and dissolution profile. Thedrug-to-carrier and solvent ratio was chosen as independent variable, while %yield, drug content, and saturation solubility were chosen as dependent variables. The results showed that the optimized formulation of SD-DFX was able to significantly enhance its solubility. The SD containing a dispersion of Deferasirox with PVP show an exceptional rise in the solubility. This study describes the development of solid dispersion that significantly improved the solubility and bioavailability of DFX. The FTIR studies indicate the interaction between the drug and polymer. The DSC and XRD analysis indicated that the drug was in an amorphous state when dispersed in the polymer. It is resolved that the SD method significantly improves the solubility and dissolution rate, which could also be exploit for other poorly water soluble drug candidates. Keywords: Deferasirox , Polyvinyl pyrrolidone, solid dispersion, Factorial design, Solubility

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Formulation, development and evaluation of solid dispersions for enhancement of solubility and dissolution rate of clopidogrel bisulfate

Cited by 3 publications

References 7 publications

Development and evaluation of novel krill oil-based clomiphene microemulsion as a therapeutic strategy for PCOS treatment

Development and evaluation of novel krill oil-based clomiphene microemulsion as a therapeutic strategy for PCOS treatment

Formulation and In-vitro Evaluation of Two Layers Tablet for Dual Release of a Model Drug

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

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