Enteric and hydrophilic polymers enhance dissolution and absorption of poorly soluble acidic drugs based on micro-environmental pH-modifying solid dispersion

Objective: The aims of the study to enhance solubility and dissolution of famotidine using natural polymer. Solubility study of a drug is one of the contributing factors of its oral bioavailability. The formulation of poorly soluble drugs for oral delivery presents a challenge to the formulation technologists. Methods: The present study has shown that it is possible to raise the solubility for poorly soluble drugs like famotidine, by preparing solid dispersion using natural water-soluble polymer (xyloglucan and hyaluronic acid) as solubilizer through solvent evaporation method. Physical mixture and solid dispersion of famotidine with xyloglucan (XG) or hyaluronic acid in a ratio of 1:1, 1:2, 1:3 were prepared. Solubility study, drug content, dissolution profile and compatibility study were performed for famotidine in solid dispersions XS1, XS2, XS3, HS4, HS5, HS6 as well as in physical mixtures at a ratio 1:1 for both polymer (XG and hyaluronic acid). Results: It was observed that solid dispersions of each drugs showed an increase in dissolution rate in comparison with its pure drug in the ratio of 1:1 (Drug: carrier). It can be concluded that with the care and proper use of xyloglucan, the solubility of drugs poorly soluble can be improved. The prepared solid dispersion showed improvement of drug solubility in all prepared formulas. The best result was obtained with formula XS1 (famotidine: xyloglucan at ratio 1:1) that showed 26 fold increase in solubility compared to the solubility of pure drug. Conclusion: The natural solid dispersion, increased wettability and reduced crystallinity of the drug which leads to improving solubility and dissolution.

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Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) ◽

10.31351/vol28iss2pp105-114 ◽

2019 ◽

Vol 28 (2) ◽

pp. 105-114

Author(s):

Samer K. Ali ◽

Eman B. H. Al-Khedairy

Keyword(s):

Polyethylene Glycol ◽

Solid Dispersion ◽

Water Solubility ◽

Drug Carrier ◽

Solid Dispersions ◽

Poloxamer 407 ◽

Dissolution Enhancement ◽

Drug Solubility ◽

Scanning Calorimetry ◽

Poorly Soluble

Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .

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RECENT APPROACHES OF SOLID DISPERSION: A NEW CONCEPT TOWARD ORAL BIOAVAILABILITY SABITRI BINDHANI* , SNEHAMAYEE MOHAPATRA

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i2.23161 ◽

2018 ◽

Vol 11 (2) ◽

pp. 72 ◽

Cited By ~ 2

Author(s):

Sabitri Bindhani ◽

Snehamayee Mohapatra

Keyword(s):

Solid Dispersion ◽

Relative Bioavailability ◽

Review Article ◽

Water Soluble ◽

Advanced Technology ◽

Minimum Level ◽

Bioavailability Enhancement ◽

The Past ◽

Poorly Soluble

Solid dispersion (SD) has been a major advanced technology in overcoming dissolution and bioavailability problem of poorly soluble compounds. Formulation of SD in water-soluble carrier has becoming more researched over the past four decades for solubility and relative bioavailability enhancement. By reduction of the size of the drug particle to the minimum level which will enhance drug wettability and ultimately bioavailability will be definitely improved. This review article elaborates recent advanced technology and characterization of SDs and also discusses the problems and their solution for the development of better formulations.

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Solid dispersion technology as a strategy to improve the bioavailability of poorly soluble drugs

Therapeutic Delivery ◽

10.4155/tde-2019-0007 ◽

2019 ◽

Vol 10 (6) ◽

pp. 363-382 ◽

Cited By ~ 9

Author(s):

Alicia Graciela Cid ◽

Analía Simonazzi ◽

Santiago Daniel Palma ◽

José María Bermúdez

Keyword(s):

Solid Dispersion ◽

Poorly Soluble Drugs ◽

Poorly Soluble

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Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502016000100002 ◽

2016 ◽

Vol 52 (1) ◽

pp. 1-13 ◽

Cited By ~ 6

Author(s):

Ehsan Adeli

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Water Soluble ◽

Polyethylene Glycols ◽

X Ray Diffraction ◽

Drug Release Profile ◽

Scanning Calorimetry ◽

Peg 4000 ◽

Poorly Soluble

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

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