Controlled-release of diclofenac sodium from wax matrix granule

Miyagawa, Yasuhiko; Okabe, Toshio; Yamaguchi, Y.; Miyajima, Masaharu; Satō, Hiroshi; Sunada, Hisakazu

doi:10.1016/0378-5173(96)04547-4

Cited by 59 publications

(25 citation statements)

References 7 publications

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“…The carriers that have been used include water-insoluble polymers and waxes such as ethyl cellulose or carnauba wax from which the rate of drug release is diffusion controlled. Granules containing diclofenac sodium using carnauba wax have been reported (33). The use of waxes and other wax-based materials has the potential advantage that these materials are relatively inert.…”

Section: Materials Used In Hmementioning

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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Section: Materials Used In Hmementioning

confidence: 99%

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

2015

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“…Major advantages of this method are absence of the risk of residual solvents unlike other solid dispersion techniques involving use of solvents, easy processing in terms of drying, and improved miscibility of drug and polymer at relatively low temperatures (13). In addition to enhancement of solubility, fusion method has also been employed for controlled and modified release application using hydrophobic polymers like glyceryl behenate (14), stearic acid (15), carnauba wax (16), etc. Scope of the current study was to prepare and evaluate the potential of Poloxamer 407 (Lutrol® F127 NF Prill) in improving the solubility and dissolution rate of model BCS class II drug ibuprofen.…”

Section: Introductionmentioning

confidence: 99%

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

2016

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ABSTRACT. Aim of current research was to prepare ibuprofen-poloxamer 407 binary mixtures using fusion method and characterize them for their physicochemical and performance properties. Binary mixtures of ibuprofen and poloxamer were prepared in three different ratios (1:0.25, 1:0.5, and 1:0.75, respectively) using a water-jacketed high shear mixer. In vitro dissolution and saturation solubility studies were carried out for the drug, physical mixtures, and formulations for all ratios in de-ionized water, 0.1 N HCl (pH = 1.2), and phosphate buffer (pH = 7.2). Thermal and physical characterization of samples was done using modulated differential scanning calorimetry (mDSC), X-ray powder diffraction (XRD), and infrared spectroscopy (FTIR). Flow properties were evaluated using a powder rheometer. Maximum solubility enhancement was seen in acidic media for fused formulations where the ratio 1:0.75 had 18-fold increase. In vitro dissolution studies showed dissolution rate enhancement for physical mixtures and the formulations in all three media. The most pronounced effect was seen for formulation (1:0.75) in acidic media where the cumulative drug release was 58.27% while for drug, it was 3.67%. Model independent statistical methods and ANOVA based methods were used to check the significance of difference in the dissolution profiles. Thermograms from mDSC showed a characteristic peak for all formulations with T peak of around 45°C which suggested formation of a eutectic mixture. XRD data displayed that crystalline nature of ibuprofen was intact in the formulations. This work shows the effect of eutectic formation and micellar solubilization between ibuprofen and poloxamer at the given ratios on its solubility and dissolution rate enhancement.

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“…Recently, lipids are considered as alternative to polymers in the design of sustained drug delivery systems [16] due to their chemical inertness [17], cost-effectiveness, regulatory acceptance, and above all flexibility to achieve the desired drug release profile [18]. Wide arrays of wax-lipid based hydrophobic materials are available for sustaining drug action as Compritol® 888 ATO (glyceryl behenate) [19][20][21], Precirol® ATO 5 (glyceryl palmito-stearate) [22][23][24], stearic acid [23][24][25], and tristearin [26].…”

Section: Introductionmentioning

confidence: 99%

Formulation and In Vitro and In Vivo Evaluation of Lipid-Based Terbutaline Sulphate Bi-layer Tablets for Once-Daily Administration

et al. 2015

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Abstract. The objective of this study was to prepare and evaluate terbutaline sulphate (TBS) bi-layer tablets for once-daily administration. The bi-layer tablets consisted of an immediate-release layer and a sustained-release layer containing 5 and 10 mg TBS, respectively. The sustained-release layer was developed by using Compritol®888 ATO, Precirol® ATO 5, stearic acid, and tristearin, separately, as slowly eroding lipid matrices. A full 4×2 2 factorial design was employed for optimization of the sustainedrelease layer and to explore the effect of lipid type (X 1 ), drug-lipid ratio (X 2 ), and filler type (X 3 ) on the percentage drug released at 8, 12, and 24 h (Y 1 , Y 2 , and Y 3 ) as dependent variables. Sixteen TBS sustained-release matrices (F1-F16) were prepared by melt solid dispersion method. None of the prepared matrices achieved the targeted release profile. However, F2 that showed a relatively promising drug release was subjected to trial and error optimization for the filler composition to develop two optimized matrices (F17 and F18). F18 which consisted of drug-Compritol®888 ATO at ratio (1:6 w/w) and Avicel PH 101/dibasic calcium phosphate mixture of 2:1 (w/w) was selected as sustained-release layer. TBS bilayer tablets were evaluated for their physical properties, in vitro drug release, effect of storage on drug content, and in vivo performance in rabbits. The bi-layer tablets showed acceptable physical properties and release characteristics. In vivo absorption in rabbits revealed initial high TBS plasma levels followed by sustained levels over 24 h compared to immediate-release tablets.

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Controlled-release of diclofenac sodium from wax matrix granule

Cited by 59 publications

References 7 publications

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

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

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

Formulation and In Vitro and In Vivo Evaluation of Lipid-Based Terbutaline Sulphate Bi-layer Tablets for Once-Daily Administration

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