Amorphous solid dispersion method for improving oral bioavailability of poorly water-soluble drugs

Gurunath, Surampalli; Kumar, Sabbani Pradeep; Basavaraj, Nanjwade K.; Patil, P. A.

doi:10.1016/j.jopr.2013.04.008

Cited by 48 publications

(45 citation statements)

References 19 publications

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“…Solid dispersion is defined as “The dispersion of one or more active ingredients in an inert carrier matrix at solid-state’’ 3 . There are many methods to prepare solid dispersions such as the fusion method, ball milling, solvent evaporation, lyophilization, hot melt extrusion (HME) and supercritical fluid methods 4, 5 …”

Section: Introductionmentioning

confidence: 99%

Influence of pressurized carbon dioxide on ketoprofen-incorporated hot-melt extruded low molecular weight hydroxypropylcellulose

Ashour

Kulkarni

Almutairy

et al. 2015

Drug Development and Industrial Pharmacy

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Objectives The aim of the current research project was to investigate the effect of pressurized carbon dioxide (P-CO2) on the physico-mechanical properties of Ketoprofen (KTP)-incorporated hydroxypropylcellulose (HPC) (Klucel™ ELF, EF and LF) produced using hot melt extrusion (HME) techniques and to assess the plasticization effect of P-CO2 on the various polymers tested. Methods The physico-mechanical properties of extrudates with and without injection of P-CO2 were examined and compared to extrudates with the addition of 5% liquid plasticizer of propylene glycol (PG). The extrudates were milled and compressed into tablets. Tablet characteristics of the extrudates with and without injection of P-CO2 were evaluated. Results & conclusion P-CO2 acted as a plasticizer for tested polymers, which allowed for the reduction in extrusion processing temperature. The microscopic morphology of the extrudates were changed to a foam-like structure due to expansion of the CO2 at the extrusion die. The foamy extrudates demonstrated enhanced KTP release compared to the extrudates processed without P-CO2 due to the increase of porosity and surface area of those extrudates. Furthermore, the hardness of the tablets prepared by foamy extrudates was increased and the percent friability was decreased. Thus, the good binding properties and compressibility of the extrudates were positively influenced by utilizing P-CO2 processing.

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Section: Introductionmentioning

confidence: 99%

Influence of pressurized carbon dioxide on ketoprofen-incorporated hot-melt extruded low molecular weight hydroxypropylcellulose

Ashour

Kulkarni

Almutairy

et al. 2015

Drug Development and Industrial Pharmacy

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“…The main disadvantage of the first generation solid dispersions is the high thermodynamic stability of the carrier, which promotes lower dissolution rates compared with amorphous solid dispersions [13,34]. Also, the high melting point of some carriers used in crystalline solid dispersions complicates the preparation of such systems by the melting method [13,14]. Urea, organic acids, and most sugars (mannitol is an exception) are thermally unstable; therefore, they are unsuitable for solid dispersion preparation by the melting method.…”

Section: First-generation Solid Dispersionsmentioning

confidence: 99%

“…The need for effective formulations for BCS-classes II and IV drugs led to the progress of knowledge in the area of drug delivery systems for oral administration, over the years, and to the development of various technological strategies to remedy unsatisfactory biopharmaceutical properties, for example, micronization [8], formation of complexes with cyclodextrins [9], self-emulsifying drug delivery systems (SEDDS) [10], liquisolid systems [11,12] and solid dispersions [13,14].…”

Section: Introductionmentioning

confidence: 99%

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

et al. 2018

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The oral solid dosage forms are extremely relevant to drug therapy and responsible for much of the pharmaceutical industry turnover worldwide. However, the development of medicines in solid form involves significant challenges, including obtaining formulations with appropriate bioavailability for low aqueous solubility drugs (classes II and IV of the Biopharmaceutics Classification System). One of the most effective strategies to overcome poor dissolution rate and low absorption of drugs is the solid dispersion technique, however, although it has been the focus of much research in recent decades, there are relatively few commercially available products based on such technology. This is mainly due to problems related to production scale-up and physicochemical instability and creates opportunities for new studies to explore the full potential of the technology. This review presents an overall approach to the factors affecting the dissolution rate and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology.

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“…In addition, specific intermolecular interactions between API and polymer in ASD aid to inhibit nucleation and crystal growth. These benefits of ASD have been exploited as one of the key approaches of oral bioavailability improvement of poorly water soluble drugs …”

Section: Amorphous Solid Dispersionmentioning

confidence: 99%

“…There are very few analytical techniques that offer spatial capability to probe the miscibility at molecular level in complex ASD . This is one of the key hurdles in identifying, at nanoscopic level, whether API molecules are dispersed at molecular level (glass solution), present as amorphous clusters (amorphous solid suspension) in carrier matrices or present spatial heterogeneity of composition .…”

Section: Amorphous Solid Dispersionmentioning

confidence: 99%

Structural and Dynamic Properties of Amorphous Solid Dispersions: The Role of Solid-State Nuclear Magnetic Resonance Spectroscopy and Relaxometry

Paudel

Geppi

Mooter

2014

Journal of Pharmaceutical Sciences

117

103

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Amorphous solid dispersion method for improving oral bioavailability of poorly water-soluble drugs

Cited by 48 publications

References 19 publications

Influence of pressurized carbon dioxide on ketoprofen-incorporated hot-melt extruded low molecular weight hydroxypropylcellulose

Influence of pressurized carbon dioxide on ketoprofen-incorporated hot-melt extruded low molecular weight hydroxypropylcellulose

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Structural and Dynamic Properties of Amorphous Solid Dispersions: The Role of Solid-State Nuclear Magnetic Resonance Spectroscopy and Relaxometry

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