ChemInform Abstract: A Promising Novel Approach for Improving the Solubility of Poorly Soluble Drugs

Kushwaha, Anjali

doi:10.1002/chin.201232267

Cited by 2 publications

(8 citation statements)

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“…the liquid initially absorbed in the interior of the particles is captured by its internal structure, and after the saturation of this process, adsorption of the liquid onto the internal and external surfaces of the porous carrier particles occur. Then, the coating material having high adsorptive properties and large specific surface area gives the liquisolid system the desirable flow characteristics 19,23 .…”

Section: Liquisolid Methodmentioning

confidence: 99%

“…Ex. of complexing agents are; chelates-EDTA, EGTA, molecular complexes-polymers, inclusion complexes cyclodextrins 22,23 .…”

Section: Amorphous >Metastable Polymorph >Stable Polymorph (E) Complementioning

confidence: 99%

“…Types of solid dispersions [16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32] a. Simple eutectic mixture: An eutectic mixture of a sparingly water soluble drug and a highly water soluble carrier may be regarded thermodynamically as an intimately blended physical mixture of its two crystalline component.…”

Section: Third Generation Solid Dispersionmentioning

confidence: 99%

“…HME differs from simple extrusion in that, polymer, drug and excipients blends are mixed thoroughly in the molten state in this process, needing no solvents for granulation. The molten polymer serves as the thermal binder 19,23 .…”

Section: Difficulty In Incorporating Into Formulation Of Dosage Formsmentioning

confidence: 99%

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Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability

Pawar

Barhate²

2019

J. Drug Delivery Ther.

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The solubility of a solute is the maximum quantity of solute that can dissolve in a certain quantity of solvent or quantity of solution at a specified temperature. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Solubility is essential for the therapeutic effectiveness of the drug, independent of the route of administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. Poorly soluble drugs are often a challenging task for formulators in the industry Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non-aqueous media. Drug with poor water solubility cause slow dissolution rates, generally show erratic and incomplete absorption leading to low bioavailability when administered orally. Solubilization may be affected by cosolvent water interaction, micellar solubilization, reduction in particle size, inclusion complexes, solid dispersion, and change in polymorph. Some new technologies are also available to increase the solubility like micro emulsion, self-emulsifying drug delivery system and supercritical fluid technology. This present review details about the different approaches used for the enhancement of the solubility of poorly water-soluble drugs include particle size reduction, nanonization, pH adjustment, solid dispersion, complexation, co‐solvency, hydrotropy etc. The purpose of this article is to describe the techniques of solubilization for the attainment of effective absorption and improved bioavailability. Keywords: Solubility, Solubility Enhancement, bioavailability, solid dispersion, Solid Dispersion, Solubilization.

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Section: Liquisolid Methodmentioning

confidence: 99%

“…Ex. of complexing agents are; chelates-EDTA, EGTA, molecular complexes-polymers, inclusion complexes cyclodextrins 22,23 .…”

Section: Amorphous >Metastable Polymorph >Stable Polymorph (E) Complementioning

confidence: 99%

Section: Third Generation Solid Dispersionmentioning

confidence: 99%

Section: Difficulty In Incorporating Into Formulation Of Dosage Formsmentioning

confidence: 99%

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Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability

Pawar

Barhate²

2019

J. Drug Delivery Ther.

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“…Then, the film was further dried for 24 h and then grinds to form a powder. This solid dispersion powder was passed through sieve no 40 [14].…”

Section: Preparation Of Meloxicam Solid Dispersion By Solvent Evaporamentioning

confidence: 99%

Formulation and Evaluation of Mouth Dissolving Tablet of Meloxicam Using Natural Superdisintegrants

Pawar¹,

Mutha²,

Bhise³

et al. 2020

Asian J Pharm Clin Res

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Objective: The objective of the present work was the preparation and evaluation of mouth dissolving tablets (MDTs) of meloxicam using natural superdisintegrants. Methods: Meloxicam is BCS Class II (low soluble, and high permeable) drug increasing the dissolution properties of the poorly water-soluble drug meloxicam using a solid dispersion method (solvent evaporation method). Solvent evaporation method using drug and carrier as polyethylene glycol (PEG)-6000 and PEG-15,000 the ratio of 1:1, 1:2 (drug:carrier), and acetone as solvent. In house prepared banana powder were used as natural superdisintegrant. Manufacturing of MDT was done by the direct compression method. In this MDTs, various excipients were used such as mannitol used as the diluent, sodium saccharin used as a sweetening agent, Avicel pH-102 used as a binding agent, and talc and sodium lauryl sulfate (SLS) used as lubricant and glidant. The best formula of the tablet was selected according to the disintegration time (DT) and friability tests. Results: The results have shown that an increase in the meloxicam solubility was obtained using solid dispersion with the solvent evaporation method using PEG-15000 as a carrier in the ratio of 1:2 (drug:carrier). Taste masking was also done by a solid dispersion method. Tablet prepared with in house prepared banana powder gave less DT (70 s) as compared to tablet prepared with branded banana powder (80 s), but formulation F5 failed in friability testing. Improved strength of tablet obtained using SLS (<1%) also showed an increase in the dissolution performance of the tablet in formulation F6. This F6 formulation having 10% natural super disintegrating agent (in house prepared banana powder) has shown 99% cumulative drug release within 18 min. It also passed the friability test. Conclusion: Accordingly, the solubility of meloxicam was successfully enhanced through solid dispersion with carrier PEG-15,000 and formulated as a MDT to improve its oral absorption. PEG has also been used as a taste masking agent in these formulations. It was concluded that in house banana powder had excellent DT as compared to branded banana powder. Banana powder is “economical” and “easily available” than other commonly used synthetic superdisintegrants. The process of banana powder preparation is eco friendly. The meloxicam MDT formulated with natural superdisintegrant in house prepared banana powder found to pass all pharmacopeial tests.

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ChemInform Abstract: A Promising Novel Approach for Improving the Solubility of Poorly Soluble Drugs

Abstract: Review: 36 refs.

Cited by 2 publications

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Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability

Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability

Formulation and Evaluation of Mouth Dissolving Tablet of Meloxicam Using Natural Superdisintegrants

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