Characterization of Ibuprofen as a Nontraditional Plasticizer of Ethyl Cellulose

Brabander, C De; Mooter, Guy Van den; Vervaet, Chris; Remon, Jean Paul

doi:10.1002/jps.10159

Cited by 109 publications

(50 citation statements)

References 19 publications

(16 reference statements)

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“…Wafers with larger pores allow a more rapid ingress of water during dissolution which is expected to increase drug release rates. Figure 4a shows that addition of IBU increased the work of compression (WOC) [17] while PM decreased it to approximately half that of IBU loaded wafers, and also lower than the blank (non drug loaded wafer). These results combined with SEM observations showed that addition of PM decreased mechanical strength due possibly to the reduced availability of free polymer as a result of the higher amounts of PM distributed throughout the matrix.…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Lyophilized wafers comprising carrageenan and pluronic acid for buccal drug delivery using model soluble and insoluble drugs

Kianfar

Antonijević

Chowdhry

et al. 2013

Colloids and Surfaces B: Biointerfaces

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Lyophilized muco-adhesive wafers with optimum drug loading for potential buccal delivery have been developed. A freeze-annealing cycle was used to obtain optimized wafers from aqueous gels containing 2% κ-carrageenan (CAR 911), 4% pluronic acid (F127), 4.4% w/w polyethylene glycol with 1.8% w/w paracetamol or 0.8% w/w ibuprofen. Thermogravimetric analysis showed acceptable water content between 0.9 -1.5%. Differential scanning calorimetry and X-ray diffraction showed amorphous conversion for both drugs. Texture analysis showed ideal mechanical and mucoadhesion characteristics whilst both drugs remained stable over six months and drug dissolution at a salivary pH showed gradual release within two hours. The results show the potential of CAR 911 and F127 based wafers for buccal mucosa drug delivery.Keywords: Amorphous, Buccal drug delivery system, Carrageenan, Dissolution characteristics, Lyophilized wafer, (Muco)-adhesion, 3 IntroductionMucosal drug delivery systems have many advantages such as bypassing first pass liver metabolism and avoiding GI enzymatic degradation. Drug absorption via the buccal mucosa surface and into the systemic circulation is relatively fast (compared to the skin) owing to the highly vascularized structure underneath the mucosal tissues [1,2].Lyophilisation has been used in pharmaceutical industries to improve the stability of formulations. The investigation of fundamental physical phenomena occurring during each step of freeze drying has enabled formulators to produce stable and well-designed freezedried pharmaceutical dosage forms [3]. Freeze dried products do not necessarily need to be refrigerated and can be stored at ambient temperatures. This will be favourable for labile drugs including vaccines and proteins [4].Lyophilisation comprises a freezing step where ice crystals form and the solute becomes extremely concentrated. As the temperature falls below the glass transition temperature (T g ), the system is changed into a viscous glass. Incomplete crystallization may, however, lead to sample collapse or formation of mixtures of different polymorphic forms that causes problems in characterization and manufacturing reproducibility. Frozen products can be categorized as either crystalline or amorphous glass in structure. Crystalline products have a distinct "eutectic" freezing/melting point which is referred to as the collapse temperature. Amorphous products have a corresponding "glass transition" temperature and they are much more difficult to freeze-dry. Even though most materials that are freeze dried are actually amorphous, the term "eutectic" is often used to define the freezing/melting point of sample [4].To optimise the process of solute crystallization during freezing, thermal treatment, or "annealing", will be advantageous. Annealing is the process of heating a sample above its 4 glass transition temperature (but below the eutectic and/or ice melting temperature) and allowing the glass to relax and crystallize. Metastable glass formation is possible depending on the f...

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Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Lyophilized wafers comprising carrageenan and pluronic acid for buccal drug delivery using model soluble and insoluble drugs

Kianfar

Antonijević

Chowdhry

et al. 2013

Colloids and Surfaces B: Biointerfaces

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“…The HME process was conducted at 140°C, to produce smooth extrudates at two different IBU loading levels of 25 and 40%. Eudragit® E PO was selected as the primary matrix-forming polymer, and plasticizers were not used in this formulation because IBU has been shown to possess plasticizing effects comparable to traditional plasticizers (52). The extrudates were analyzed using XRD to examine the IBU crystallinity, and the results showed that even at the high drug loading (40%) level, IBU remained in an amorphous state.…”

Section: Taste Maskingmentioning

confidence: 99%

“…The most commonly used traditional plasticizers are triacetin (48), citrate ester (41,49), vitamin E D-alpha tocopheryl PEG 1000 succinate (TPGS) (50), surfactants (51), and lowmolecular-weight polyethylene glycols (31). Non-traditional plasticizers are included in formulations to serve other critical functions and are often low-molecular-weight materials such as the active substance itself (52)(53)(54)(55). Special plasticizers are low-molecular-weight materials, which also act as plasticizers for polymeric carriers depending on their physical state.…”

Section: Plasticizersmentioning

confidence: 99%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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Abstract. Hot-melt extrusion (HME) is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. In drug discovery and development, industry estimates that more than 50% of active pharmaceutical ingredients currently used belong to the biopharmaceutical classification system II (BCS class II), which are characterized as poorly water-soluble compounds and result in formulations with low bioavailability. Therefore, there is a critical need for the pharmaceutical industry to develop formulations that will enhance the solubility and ultimately the bioavailability of these compounds. HME technology also offers an opportunity to earn intellectual property, which is evident from an increasing number of patents and publications that have included it as a novel pharmaceutical formulation technology over the past decades. This review had a threefold objective. First, it sought to provide an overview of HME principles and present detailed engineered extrusion equipment designs. Second, it included a number of published reports on the application of HME techniques that covered the fields of solid dispersions, microencapsulation, taste masking, targeted drug delivery systems, sustained release, films, nanotechnology, floating drug delivery systems, implants, and continuous manufacturing using the wet granulation process. Lastly, this review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology.

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“…The plasticizing effect can be attributed to the increase of free volume, the decrease of friction between polymer chains and the consequent improvement of chain mobility of polymer, resulting in reducing the drug and polymeric carrier degradation and improve the stability profile of the active compound (Aharoni, 1998). IBU, a low melting point drug (78 °C), with a known plasticizing effect, and higher IBU loading led to subsequent increase in its plasticizing effect as reported previously with different polymers such as Kollidon ® SR (De Brabander et al, 2002;Kidokoro et al, 2001;Özgüney et al, 2009). Therefore, IBU is considered a good candidate for HME technologies.…”

Section: Introductionmentioning

confidence: 59%

Hot melt extrusion method for preparation of ibuprofen/sucroester WE15 solid dispersions: evaluation and stability assessment

2017

J App Pharm Sci

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Low melting points Sucroesters (SEs) are used in hot-melt extrusion technology (HME). However, there are few literatures studying the effect of SEs on drug release and their storage stability. In this study, SE  WE15 was proposed to prepare sustained-release solid dispersions with Iburpofen (IBU), containing 60 & 30% w/w, by HME, fusion method and compared to physical mixtures. The fresh and stored samples were evaluated by a well-established release rate study (USP Apparatus IV), DSC and XRD. Results revealed that HME technique succeeded to produce sustained-release patterns for IBU. Stored samples (6 months at 40C / 75 % RH) were unstable and showed gradual decrease in IBU release rate for both IBU loadings. HME formula (60% w/w IBU) showed an increase in the amount of drug released. Long term stability, one year at room temperature, showed a marked increase in IBU release rate for both drug loadings. Only HME containing 30% w/w IBU gave stable form among others. DSC and XRD suggested that increase of SE content led to almost complete IBU dissolved in this carrier, and considerable decrease in IBU release rate. This has been proven by DSC and XRD data analysis for IBU and SE (enthalpy and counts).

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Characterization of Ibuprofen as a Nontraditional Plasticizer of Ethyl Cellulose

Cited by 109 publications

References 19 publications

Lyophilized wafers comprising carrageenan and pluronic acid for buccal drug delivery using model soluble and insoluble drugs

Lyophilized wafers comprising carrageenan and pluronic acid for buccal drug delivery using model soluble and insoluble drugs

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

Hot melt extrusion method for preparation of ibuprofen/sucroester WE15 solid dispersions: evaluation and stability assessment

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