Solid Dispersion: An Alternative Technique for Bioavailability Enhancement of Poorly Soluble Drugs

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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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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Development of an Oral Curcumin Nanocrystal Formulation

Journal of Nanotechnology in Engineering and Medicine ◽

10.1115/1.4023947 ◽

2012 ◽

Vol 3 (4) ◽

Cited By ~ 4

Author(s):

R. Ravichandran

Keyword(s):

The Body ◽

Dissolution Behavior ◽

Poorly Soluble Drugs ◽

Solid Dosage Forms ◽

Bioavailability Enhancement ◽

Solid Dosage ◽

Rapid Dissolution ◽

Poorly Soluble ◽

Drug Nanocrystal ◽

Spray Dried

During the last ten years, the formulation of drugs as nanocrystals has rapidly evolved into a mature drug delivery strategy, with currently five products on the market. The major characteristic of these systems is the rapid dissolution velocity, enabling bioavailability enhancement after oral administration. This study describes the preparation of a solid dosage capsule form of spray-dried curcumin nanocrystal and compares its dissolution behavior with market capsule in different media. The aim was to obtain a stable nanocrystal loaded drug capsule with an increased drug saturation solubility and dissolution velocity. The solubility and dissolution experiments were performed to verify the obvious improvement of the dissolution behavior compared with commercial product. Improved dissolution behavior in drug nanocrystal-loaded solid dosage forms should lead to better bioavailability of poorly soluble drugs in the body.

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