To enhance dissolution rate of poorly water-soluble drugs: Glucosamine hydrochloride as a potential carrier in solid dispersion formulations

Al-Hamidi, Hiba; Edwards, Alison A.; Mohammad, Mohammad Amin; Nokhodchi, Ali

doi:10.1016/j.colsurfb.2009.10.030

Cited by 94 publications

(50 citation statements)

References 23 publications

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“…PXM is a drug administered via the oral route and it will have to pass through the first pass metabolic pathway, which further lowers its bioavailability. In order to achieve the desired therapeutic effect a high dose of the drug will have to be administered [22]. The poor dissolution characteristics of PXM may be due to poor wettability, where the dissolution media is unable to spread efficiently over the solid surfaces to bring about dissolution [29].…”

Section: Resultsmentioning

confidence: 99%

“…Several authors have classed the solid dispersion approach as one of the most effective method of improving dissolution of drugs [5,8,22]. It involves the dispersion of one or more active ingredients in an inert excipient or carrier, where the active ingredients could exist in a finely crystalline, solubilised or amorphous state [23,24].…”

Section: Introductionmentioning

confidence: 99%

“…Solid dispersion also enhances the absorption and efficacy of drugs in a dosage form, despite limitations such as cost, scale up and physicochemical instabilities of the dispersions under normal storage conditions [25][26][27]. Al-Hamidi and co-workers have studied the rate of carbamazepine (CBZ), ibuprofen (IBU) and PXM (PXM) in solvent evaporated and co-ground solid dispersions [3,22,28,29]. Asare-Addo et al [8], also studied the effect of GLU on indomethacin (IND) dissolution and charging properties using a solvent evaporation process.…”

Section: Introductionmentioning

confidence: 99%

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Adebisi

Kaialy

Hussain

et al. 2016

Colloids and Surfaces B: Biointerfaces

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions, Colloids and Surfaces B: Biointerfaces http://dx.doi.org/10. 1016/j.colsurfb.2016.07.032 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 4. GLU improved the handling of PXM as it significantly reduced its charge in all the spray dried formulations. Technique could be used to determine appropriate formulations that improve handling AbstractThis work explores the use of both spray drying and D-glucosamine HCl (GLU) as a hydrophilic carrier to improve the dissolution rate of piroxicam (PXM) whilst investigating the electrostatic charges associated with the spray drying process. Spray dried PXM:GLU solid dispersions were prepared and characterised (XRPD, DSC, SEM). Dissolution and triboelectric charging was also conducted. The results showed that the spray dried PXM alone, without GLU produced some PXM form II (DSC results) with no enhancement in solubility relative to that of the parent PXM.XRPD results also showed the spray drying process to decrease the crystallinity of GLU and solid dispersions produced. The presence of GLU improved the dissolution rate of PXM. Spray dried PXM: GLU at a ratio of 2:1 had the most improved dissolution. The spray drying process generally yielded PXM-GLU spherical particles of around 2.5 µm which may have contributed to the improved dissolution. PXM showed a higher tendency for charging in comparison to the carrier GLU (-3.8 versus 0.5 nC/g for untreated material and -7.5 versus 3.1 nC/g for spray dried materials). Spray dried PXM and spray dried GLU demonstrated higher charge densities than untreated PXM and untreated GLU, respectively. Regardless of PXM:GLU ratio, all spray dried PXM:GLU solid dispersions showed a negligible charge density (net-CMR: 0.1 -0.3 3 nC/g). Spray drying of PXM:GLU solid dispersions can be used to produce formulation powders with practically no charge and thereby improving handling as well as dissolution behaviour of PXM.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Adebisi

Kaialy

Hussain

et al. 2016

Colloids and Surfaces B: Biointerfaces

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“…Dissolution efficiency (DE) is defined as the area under dissolution curve (y) up to certain time t, express as a percentage of the area of rectangle describe by 100% dissolution in the same time [27].…”

Section: Parameters For Dissolution Studymentioning

confidence: 99%

A Design of Experiment Approach for Optimization and Characterization of Etodolac Ternary System Using Spray Drying

Shaikh

Chaudhari²,

Holkar

2017

Int J Pharm Pharm Sci

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Objective: The objective of the present investigation was to prepare and characterize Etodolac (ETO), Polyvinyl pyrrolidone K30 (PVP K30) and Hydroxypropyl β-cyclodextrin (HPB) ternary system in order to study the effect of complexation on solubility of ETO.Methods: Physical mixtures of a drug and polymers in different weight ratios (1:1, 1:2, 1:4) were prepared to study the effect of individual polymers on solubility of ETO. Spray drying method was used to investigate the combined effect of PVP K30 and HPB on saturation solubility (SS), Dissolution efficiency (DE) and mean dissolution time (MDT) of ETO. Design of experiment (DoE) was used for preparation and optimization of ternary system. Drug polymer interactions were analyzed with Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), Xray diffraction (XRD) and particle size analysis. Results:Results of solubility study suggested that there was significant increase in solubility of ETO with increase in the concentration of PVP K30, Polyvinyl pyrrolidone K 90 (PVP K90) and HPB (*p<0.05). This might be due to the solubilizing effect of PVP K30, PVPK90 and complex formation of ETO with HPB. Various combinations of PVP K30 and HPB prepared using DoE approach by spray drying method showed greater solubility of ETO than its physical mixtures (*p<0.05). Results of FTIR, DSC, SEM, XRD and particle size analysis revealed the interaction between ETO, PVP K30 and HPB. This suggested formation of amorphous ternary system with mean particle diameter in the range of 763±1.35 nm. Conclusion:Combine use of PVP K30 and HPB with DoE approach was an effective tool for formulating ternary system of ETO.

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“…Due to the instability of glucosamine, its salts (either hydrochloride or sulphate) are used in therapy 19 but glucosamine HCl is more stable than glucosamine sulphate. 20 Our previous results showed the ability of glucosamine as a hydrophilic carrier to enhance the dissolution of CBZ in solid dispersion formulations 21 and ground formulations containing piroxicam. 22 Ibuprofen has a low melting point (around also studied to investigate any interaction between drug and glucosamine HCl.…”

Section: Introductionmentioning

confidence: 97%

The dissolution and solid-state behaviours of coground ibuprofen–glucosamine HCl

Al-Hamidi

Asare-Addo

Desai

et al. 2014

Drug Development and Industrial Pharmacy

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The cogrinding technique is one of most effective methods for improving the dissolution of poorly water soluble drugs and it is superior to other approaches from an economical as well as an environmental stand point, as the technique does not require any toxic organic solvents.Present work explores the role of D-glucosamine HCl (GL) as a potential excipient to improve dissolution of a low melting point drug, ibuprofen (Ibu), using physical mixtures and coground formulations. The dissolution of the poorly soluble drug has been improved by changing the ratio of Ibu:GL and also grinding time. The results also showed that although GL can enhance the solubility of Ibu, it also reduces pH around the Ibu particles which led to poor dissolution performance when the concentration of GL is high. The effect of GL on the solubility of Ibu could be misleading if the pH of the final solution was not measured.Grinding reduced the particle size of GL significantly but in case of Ibu it was less effective.Solid state analysis (XRPD, DSC and FT-IR) showed that ibuprofen is stable under grinding conditions, but the presence of high concentration of GL in samples subjected to high grinding times caused changes in FT-IR spectrum of Ibu which could be due to intermolecular hydrogen bond or esterification between the carboxylic acid group in the ibuprofen and hydroxyl group in the GL.

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To enhance dissolution rate of poorly water-soluble drugs: Glucosamine hydrochloride as a potential carrier in solid dispersion formulations

Cited by 94 publications

References 23 publications

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

A Design of Experiment Approach for Optimization and Characterization of Etodolac Ternary System Using Spray Drying

The dissolution and solid-state behaviours of coground ibuprofen–glucosamine HCl

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