Formulation of controlled-release pelubiprofen tablet using Kollidon ® SR

Song, Seh Hyon; Chae, Bo Ram; Sohn, Se I.; Yeom, Dong Woo; Son, Ho Yong; Kim, Jin Han; Kim, Dae Jung; Lee, Sang Gon; Choi, Young Wook

doi:10.1016/j.ijpharm.2016.07.074

Cited by 14 publications

(15 citation statements)

References 33 publications

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“…In order to avoid double variable effect, the compression force was set so that the mechanical strength was constant. As shown in Figure 2A and B, Pal release increased with the tablet weight up to a value of 250 mg, due to the higher contact surface between the tablet and the dissolution media and the higher porosity created by the lactose and PVP dissolution,12 but when surpassing this value, no further changes were noticed in drug dissolution.…”

Section: Resultsmentioning

confidence: 95%

“…Hydrophilic polymers such as hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), and sodium carboxymethyl cellulose (CMCS) were used in the formulation of controlled release matrices, individually or as mixtures, and the drug transport kinetics depended on polymer hydration, swelling, and further erosion, as well as on drug dissolution and diffusion through the formed gel 10,11. On the other hand, insoluble matrices formed with hydrophobic polymers such as ethyl cellulose, Eudragit ® RS (Evonik, Essen, Germany), or Kollidon ® SR (BASF, Ludwigshafen, Germany) form porous structures upon hydration, and the dissolved active principle diffuses slowly through the pores into the liquid media 12–14…”

Section: Introductionmentioning

confidence: 99%

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Risk assessment and experimental design in the development of a prolonged release drug delivery system with paliperidone

Iurian

Turdean

Tomuță

2017

DDDT

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This study focuses on the development of a drug product based on a risk assessment-based approach, within the quality by design paradigm. A prolonged release system was proposed for paliperidone (Pal) delivery, containing Kollidon® SR as an insoluble matrix agent and hydroxypropyl cellulose, hydroxypropyl methylcellulose (HPMC), or sodium carboxymethyl cellulose as a hydrophilic polymer. The experimental part was preceded by the identification of potential sources of variability through Ishikawa diagrams, and failure mode and effects analysis was used to deliver the critical process parameters that were further optimized by design of experiments. A D-optimal design was used to investigate the effects of Kollidon SR ratio (X1), the type of hydrophilic polymer (X2), and the percentage of hydrophilic polymer (X3) on the percentages of dissolved Pal over 24 h (Y1–Y9). Effects expressed as regression coefficients and response surfaces were generated, along with a design space for the preparation of a target formulation in an experimental area with low error risk. The optimal formulation contained 27.62% Kollidon SR and 8.73% HPMC and achieved the prolonged release of Pal, with low burst effect, at ratios that were very close to the ones predicted by the model. Thus, the parameters with the highest impact on the final product quality were studied, and safe ranges were established for their variations. Finally, a risk mitigation and control strategy was proposed to assure the quality of the system, by constant process monitoring.

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Section: Resultsmentioning

confidence: 95%

Section: Introductionmentioning

confidence: 99%

Risk assessment and experimental design in the development of a prolonged release drug delivery system with paliperidone

Iurian

Turdean

Tomuță

2017

DDDT

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“…But in the formulation there was a slight change in peak temperature such as 106 °C and 180 °C ( fig. 5), also a slight change in peak area and peak shape changed, which might be due to reduction of the purity percentage of component, appearance of adjacent polymer and interaction with solvent excipients [20,21].…”

Section: Dsc Studymentioning

confidence: 99%

Formulation and Design of Extended Release Matrix Tablets of Zidovudine Hydrochloride: A Study on Effect of Various Grades of Ethocel and HPMC

Roy¹

2018

Int J Pharm Pharm Sci

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Objective: The current research was an attempt to formulate and design an extend release dosage form of zidovudine hydrochloride using various grades of ethyl cellulose (ethocel) such as ethocel 4CPS, ethocel 7 CPS and aqualon T10 Pharm EC with two grades of hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M).Methods: Pilot scale batches of nine formulations were prepared using kollidon and adopting wet granulation technique. Physiochemical properties of tablet and granules were examined prior compression to get tablet. Tablets were characterized as drug content, percentage weight variation, thickness, Hardness, percentage friability and in vitro drug release pattern and studied for 12 hour in USP Type-II apparatus using 900 ml Phosphate buffer at 37±0.5 °C. The dissolution release profile of drug in tablet was performed by various drug release kinetic modelling. Results:The result revealed formulation F8 containing ethocel 7CPS and aqualon T10 was able to delay the pure drug release for 12 h and followed Higuchi pattern. Whereas; formulations containing only ethocel 4CPS provided earlier drug release. Dissolution data of promising formulation were analysed with innovator formulation for similarity factor (f2), exhibited an acceptable value more than 50. FT-IR (fourier-transform infrared spectroscopy) and DSC (differential scanning calorimetry) study revealed no such incompatibility found between the pure drug and polymers but slight change in crystalinity were observed in XRD study (X-ray diffraction). SEM (scanning electron microscope) study revealed very rare intragranular pore and cavity. Conclusion:From that, it can be marked as viscosity and selection of ethocel have great importance in delay drug release.

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“…Assuming maximum GI tract transit time of 12 h and gastric emptying time of generally 2 h (Rawat et al, 2007;Vasavid et al, 2014), dissolution studies of SRSD (F6) was carried out at the gastric pH (pH 1.2) for 2 h and the intestinal pH (pH 6.8) for 10 h. As illustrated in Figure 2(A), while the untreated drug and PM showed fast dissolution, SRSD (F6) showed a drug release less than 7% at pH 1.2 for 2 h. After transition to the intestinal stage at pH 6.8, drug release from SRSD (F6) gradually increased, suggesting that SRSD (F6) may exhibit sustained drug release in GI tract. The pH dependency in dissolution of SRSD (F6) may be explained by the pH dependent solubility of PEL since PEL exhibits low solubility at acidic condition (Song et al, 2016). In addition, it may be also attributed to the difference in the hydration and permeability of polymer matrix in different dissolution media.…”

Section: Preparation Of Srsd and Optimization Of Formulation Compositionmentioning

confidence: 99%

Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization

et al. 2017

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The present study aimed to develop the sustained-release oral dosage form of pelubiprofen (PEL) by using the blended mixture of 3-aminopropyl functionalized-magnesium phyllosilicate (aminoclay) and pH-independent polymers. The sustained-release solid dispersion (SRSD) was prepared by the solvent evaporation method and the optimal composition of SRSD was determined as the weight ratio of drug: EudragitV R RL PO: EudragitV R RS PO of 1:1:2 in the presence of 1% of aminoclay (SRSD(F6)). The dissolution profiles of SRSD(F6) were examined at different pHs and in the simulated intestinal fluids. The drug release from SRSD(F6) was limited at pH 1.2 and gradually increased at pH 6.8, resulting in the best fit to Higuchi equation. The sustained drug release from SRSD(F6) was also maintained in simulated intestinal fluid at fasted-state (FaSSIF) and fed-state (FeSSIF). The structural characteristics of SRSD(F6) were examined by using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR), indicating the change of drug crystallinity to an amorphous form. After oral administration in rats, SRSD(F6) exhibited the prolonged drug exposure in plasma. For both PEL and PEL-transOH (active metabolite), once a day dosing of SRSD(F6) achieved oral exposure (AUC) comparable to those from the multiple dosing (3 times a day) of untreated drug. In addition, the in vivo absorption of SRSD(F6) was well-correlated with the in vitro dissolution data, establishing a good level A in vitro/in vivo correlation. These results suggest that SRSD(F6) should be promising for the sustained-release of PEL, thereby reducing the dosing frequency.ARTICLE HISTORY

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Formulation of controlled-release pelubiprofen tablet using Kollidon ® SR

Cited by 14 publications

References 33 publications

Risk assessment and experimental design in the development of a prolonged release drug delivery system with paliperidone

Risk assessment and experimental design in the development of a prolonged release drug delivery system with paliperidone

Formulation and Design of Extended Release Matrix Tablets of Zidovudine Hydrochloride: A Study on Effect of Various Grades of Ethocel and HPMC

Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization

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