Release performance of a poorly soluble drug from a novel, Eudragit®-based multi-unit erosion matrix

Mehta, Ketan A.; Kislalioglu, M. Serpil; Phuapradit, Wantanee; Malick, A. Waseem; Shah, Navnit

doi:10.1016/s0378-5173(00)00594-9

Cited by 57 publications

(25 citation statements)

References 5 publications

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“…Because of the nature of the polymers used in the tablet formulations and the high water solubility of SRID, diffusion may be the main mechanism of drug release from the formulations (34,35). When the dissolution data were plotted following Higuchi's model, all the formulations fitted well with the model, as indicated by the correlation coefficient values (R 2 ); this pattern confirms the suggestion that diffusion is the mechanism of drug release (36)(37)(38).…”

Section: Dissolution Profilesupporting

confidence: 72%

Influence of Formulation Factors on Tablet Formulations with Liquid Permeation Enhancer Using Factorial Design

2009

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Abstract. For a drug with low bioavailability, a matrix tablet with liquid permeation enhancer (Labrasol®) was formulated. Factorial design was used to evaluate the effect of three formulation factors: drug percentage, polymer type (Methocel® K100M or Eudragit® L 100-55), and tablet binder percentage (Plasdone® S-630) on tablet characteristics. Tablets were prepared by direct compression and characterized. Compressibility index values ranged between 15.90% and 29.87% and tablet hardness values from 7.8 to 29.78 Kp. Eudragit®-containing formulations had better compressibility index values with higher tablet hardness. Time for 75% of drug release (T 75 ) was calculated, and formulations containing Eudragit® L 100-55 had faster release rates than tablet formulations with Methocel® K100M. Formulations with Methocel® K100M fit well in the Higuchi model as indicated by their R 2 values (>0.98). Among all the formulation factors studied, polymer type displayed the highest and statistically significant effect on compressibility index, tablet hardness, and dissolution rate. Statistical design helped in better understanding the effect of formulation factors on tablet characteristics important for designing formulations with desired characteristics.

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Section: Dissolution Profilesupporting

confidence: 72%

Influence of Formulation Factors on Tablet Formulations with Liquid Permeation Enhancer Using Factorial Design

2009

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“…The non-biodegradable polymers include the conventional cellulose derivatives (14)(15)(16)(17) and acrylic polymers (18,19). These above-mentioned polymers were purchased by the researchers for preparation of drug delivery systems with fixed polymer chain lengths, molecular weights, and drug delivery properties.…”

Section: Introductionmentioning

confidence: 99%

Application of In Situ Polymerization for Design and Development of Oral Drug Delivery Systems

Ngwuluka

2010

AAPS PharmSciTech

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Abstract. Although preformed polymers are commercially available for use in the design and development of drug delivery systems, in situ polymerization has also been employed. In situ polymerization affords the platform to tailor and optimize the drug delivery properties of polymers. This review brings to light the benefits of in situ polymerization for oral drug delivery and the possibilities it provides to overcome the challenges of oral route of administration.

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“…Waxes such as Gelucires (Montousse et al, 1999;Siepmann et al, 2006) and Compritol 888 ATO (Chi et al, 2010) were used for theophylline and ambroxol sustained-release matrix pellets. Hydrophobic polymer such as ethylcellulose (Chi et al, 2010;Kojima and Nakagami, 2002;Mayo-Pedrosa et al, 2007) and enteric-coated polymer such as Eudragit ® L 100-55 (Mehta et al, 2000(Mehta et al, , 2001 were also utilized for sustained-release matrix pellets.…”

Section: Coated Pellets For Sustained Drug Deliverymentioning

confidence: 99%

Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process

Rhee¹,

Lee²,

Lee³

et al. 2010

Journal of Pharmaceutical Investigation

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− Pellets, which are multiple-unit dosage systems, have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. This review focuses on the current status and explores extrusion-spheronization technique with special attention to controlled-release application of pellets including coated pellets for delayed release formulations, coated pellets for colon delivery, coated pellets for sustained drug delivery, sustained-release matrix pellets, pellets compressed into tablets, bioadhesive pellets, floating pellets, and pelletization with solubilization techniques.Key words − Pellets, Multiparticulates, Modified-release, Pelletization, Solubilization Pelletization process is an agglomeration process that results in agglomerates of a narrow size distribution in the range of 0.5-1.5 mm with a low intra-agglomerate porosity (about 10%) and the higher density compared to the granules. Pellets are produced by pelletization process and these agglomerates have the relatively spherical shape, low friability and free flowing properties, which facilitate the handling of pellets in the manufacturing process. Pelletization process can prevent the segregation of co-agglomerated components, resulting in an improvement of the content uniformity. Pelletization process can also avoid the dust formation resulting in an improvement of the process safety, as fine powders can cause dust explosions and respiratory health problems. Pellets are widely used in multiparticulate systems and multiparticulate systems have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. The low inter-and intra-subject variability can be achieved by multiparticulate systems because multiparticulates can pass through the pylorus immediately after administration. Moreover, less effect of food on drug absorption and rather uniform gastric emptying time than single-unit dosage systems can be attainable in multiparticulate systems. Safety concerns due to dose dumping of drugs, which have narrow therapeutic index, is minimized in multiparticulate systems, and more foreseeable drug delivery in sustained release formulation is possible because the total drug dose is divided over many units, not in a single-unit system. The small size of multiparticulates also enables them to be well dispersed along the gastrointestinal (GI) tract, enhancing drug absorption and reducing the irritant effect that single-unit systems may cause to the mucosal lining, especially if remained for an extended time at a specific site. The spherical pellets can be coated with rate-controlling polymers or compressed into tablets to achieve delayed-release, extended-release, and targeted-release profiles. Multiparticulate systems with different dose strengths can be obtained from the same batch of drug-loaded pellets without additional formulation or process modification. Pellets with different drugs or with different release profiles can be blended and formulated in a single-unit dosage form such as capsule, which promo...

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Release performance of a poorly soluble drug from a novel, Eudragit®-based multi-unit erosion matrix

Cited by 57 publications

References 5 publications

Influence of Formulation Factors on Tablet Formulations with Liquid Permeation Enhancer Using Factorial Design

Influence of Formulation Factors on Tablet Formulations with Liquid Permeation Enhancer Using Factorial Design

Application of In Situ Polymerization for Design and Development of Oral Drug Delivery Systems

Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process

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