Influence of excipients, drugs, and osmotic agent in the inner core on the time‐controlled disintegration of compression‐coated ethylcellulose tablets

Lin, Shan‐Yang; Lin, Kung-Hsu; Li, Mei-Jane

doi:10.1002/jps.10197

Cited by 23 publications

(14 citation statements)

References 17 publications

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“…Even slight seepage of water through the gel layer may develop high osmotic pressure in the core that acts radically outwards to rupture the coat or surrounding membrane (42). The lag time of drug release from compression-coated ethyl cellulose tablets has been reported to decrease markedly due to the presence of NaCl as osmogen in the core tablets (43).…”

Section: Discussionmentioning

confidence: 99%

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Maity

2015

AAPS PharmSciTech

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Abstract. This work was envisaged to develop compression-coated tablets using a blend of Ca +2 ion crosslinked carboxymethyl xanthan gum (CMXG) and sodium alginate (SAL) for delayed release of immediate pulse release tablets of prednisolone (PDL) in the colon without the need of colonic bacterial intervention for degradation of the polysaccharide coat. The core tablets containing PDL and other compatible excipients were prepared by direct compression method and subsequently compression coated with different ratios of CMXG and SAL. Long T lag , the time required to restrict the drug release below 10%, and short T rap , the time required for immediate release following the T lag , were considered as suitable release parameters for evaluation of colon targeting of PDL tablets. Among the various compression coats, a blend of CMXG and SAL in a ratio of 1.5:3.5 provided T lag of 5.12±0.09 h and T rap of 6.50±0.05 h. The increase in microcrystalline cellulose (MCC) and crospovidone (CP) in the core tablets did not change T lag significantly although decreased the T rap marginally. Inclusion of an osmogen in the core tablets decreased the T lag to 4.05±0.08 h and T rap to 3.56±0.06 h. The increase in coat weight to 225 mg provided a reasonably long T lag (6.06±0.09 h) and short T rap (4.36±0.20 h). Drug release from most of the formulations followed the Hixson-Crowell equation and sigmoidal pattern as confirmed by the Weibull equation. In conclusion, tablets, compression coated with CMXG and SAL in a ratio of 1.5:3.5 and having 225-mg coat weight, were apparently found suitable for colon targeting.

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Section: Discussionmentioning

confidence: 99%

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Maity

2015

AAPS PharmSciTech

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“…[22][23] An inner core of drug tablet (sodium diclofenac 100 mg, 7 mm in diameter) was previously direct-compacted at a pressure of 200 kg/cm 2 for 1 minute. Different weight ratios (wt/wt) of EC/excipient mixtures were previously prepared as follows: 280 mg/0 mg (100%/0%), 250 mg/30 mg (89.3%/10.7%), 200 mg/80 mg (71.4%/28.6%), 150 mg/130 mg (53.6%/46.4%), 100 mg/180 mg (35.7%/64.3%), and 0 mg/280 mg (0/100%).…”

Section: Preparation Of Press-coated Tabletsmentioning

confidence: 99%

“…The amount of drug release was measured at the suitable time interval and was then determined spectrophotometrically at 276 nm (UV-160 A; Shimadzu Co, Tokyo, Japan). [22][23] Cumulative percentage drug release was calculated using an equation obtained from a standard curve. The release studies were conducted in triplicate, the mean values were plotted vs time with standard deviations (SD) of less than 3%, indicating the reproducibility of the results.…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

“…21 This function can be further and effectively controlled by modifying the compression force applied to the outer shell, the amount of outer shell used, and the excipients added to the inner core tablet. [22][23] Many studies have reported that the type and amount of excipients used might affect the drug release profile of controlledrelease tablets to influence the drug bioavailability. [24][25][26] Our previous study results have proven that the type of excipients in the inner core tablet might significantly influence the induction period of the time-controlled disintegration or rupture of a compression-coated tablet.…”

Section: Introductionmentioning

confidence: 99%

“…[24][25][26] Our previous study results have proven that the type of excipients in the inner core tablet might significantly influence the induction period of the time-controlled disintegration or rupture of a compression-coated tablet. 23 The purpose of this study was to investigate the influence of the type and amount of excipients mixed with micronized EC powder in the outer shell on the time-lag and time-controlled disintegrating or rupturing function of press-coated tablets. Two model excipients, spray-dried lactose (SDL) and hydroxypropyl methylcellulose (HPMC), were used.…”

Section: Introductionmentioning

confidence: 99%

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Hydrophilic excipients modulate the time lag of time-controlled disintegrating press-coated tablets

Lin

2004

AAPS PharmSciTech

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An oral press-coated tablet was developed by means of direct compression to achieve the time-controlled disintegrating or rupturing function with a distinct predetermined lag time. This press-coated tablet containing sodium diclofenac in the inner core was formulated with an outer shell by different weight ratios of hydrophobic polymer of micronized ethylcellulose (EC) powder and hydrophilic excipients such as spray-dried lactose (SDL) or hydroxypropyl methylcellulose (HPMC). The effect of the formulation of an outer shell comprising both hydrophobic polymer and hydrophilic excipients on the time lag of drug release was investigated. The release profile of the press-coated tablet exhibited a time period without drug release (time lag) followed by a rapid and complete release phase, in which the outer shell ruptured or broke into 2 halves. The lag phase was markedly dependent on the weight ratios of EC/SDL or EC/HPMC in the outer shell. Different time lags of the press-coated tablets from 1.0 to 16.3 hours could be modulated by changing the type and amount of the excipients. A semilogarithmic plot of the time lag of the tablet against the weight ratios of EC/SDL or EC/HPMC in the outer shell demonstrated a good linear relationship, with r = 0.976 and r = 0.982, respectively. The predetermined time lag prior to the drug release from a presscoated tablet prepared by using a micronized EC as a retarding coating shell can be adequately scheduled with the addition of hydrophilic excipients according to the time or site requirements.

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2.5 Forward Osmosis and Forward Osmosis Membranes

Dou

et al. 2017

Comprehensive Membrane Science and Engineering

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Influence of excipients, drugs, and osmotic agent in the inner core on the time‐controlled disintegration of compression‐coated ethylcellulose tablets

Cited by 23 publications

References 17 publications

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Hydrophilic excipients modulate the time lag of time-controlled disintegrating press-coated tablets

2.5 Forward Osmosis and Forward Osmosis Membranes

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