Development of pulsatile release tablets with swelling and rupturable layers

Sungthongjeen, Srisagul; Puttipipatkhachorn, Satit; Paeratakul, Ornlaksana; Dashevsky, Andrei; Bodmeier, Roland

doi:10.1016/j.jconrel.2003.10.023

Cited by 86 publications

(37 citation statements)

References 28 publications

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“…MCC is considered as a versatile excipient in tablet manufacturing by direct compression method as it acts as both a bulking agent, dry binder, and disintegrating agent for tablets and also provides compressibility to the matrix (26). MCC facilitates the penetration of water into the core by wicking action and exerts hydrostatic pressure to disintegrate the tablets (41). The increase in the amount of MCC decreased the T rap marginally.…”

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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“…The samples were analyzed at 238nm using a UV spectrophotometer. Percentage release was determined for each formulation [13][14][15] .…”

Section: In-vitro Dissolution Methods For Core Tabletsmentioning

confidence: 99%

Untitled

2017

IJPSR

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ABSTRACT:The purpose of the present investigation is to formulate and evaluate Lercanidipine pulsatile drug delivery system by press coating method. The inner core tablets were prepared by using direct compression method by using crosscarmellose sodium (Ac-Di-Sol), sodium starch glycolate, crospovidone as super disintegrants. The drug polymer interaction was investigated by FTIR and their results directed further course of formulation. The inner core tablets were evaluated for various post compression parameters like Tablet hardness, Friability, Weight variation, Drug content and in vitro dissolution for both core and coated Tablets. The disintegration time for the core tablet was found to be 35sec and the percentage drug release for the optimized formulation (F7) was 96.1% in 30mins. The Press coat tablets containing HPMC and Ethyl cellulose as a barrier layer. The press coat tablets were evaluated for post compression parameters and were found to be in limits. The percentage drug release of optimized formulation Ethyl cellulose (F7P3) was found to 99.65% at the end of 8hrs.

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“…This can be explained by the fact that, even though different amounts of sodium starch glycolate were added before the granulation step (10, 15, 20 %), a large amount of microcrystalline cellulose was added after this step. This excipient has a good disintegration property; higher amounts of microcrystalline cellulose increased the disintegration force of the cores, leading to smaller differences between the mixtures with these amounts of sodium starch glycolate (27). Studies have shown that the lag time usually depends on the amount of sodium starch glycolate swelling polymer (28).…”

Section: Design Of Experiments Analysis In Vitro Drug Releasementioning

confidence: 99%

Piecewise function parameters as responses of the design of experiment in the development of a pulsatile release chronopharmaceutical system

Vonica-Gligor¹,

Tomuță

Leucuţa

2016

Acta Pharmaceutica

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The aim of this work was to develop a pulsatile release system with metoprolol for chronotherapeutical use by coating swellable mini-tablets with Eudragit RS. To study the influence of the formulation factors (amount of coating polymer, plasticizer percentage in film coating and swelling agent percentage in mini-tablets), a Box-Behnken design of experiment (DoE) was used. To evaluate the influence of the studied factors on the sigmoid shape of the dissolution profile, piecewise function parameters were used as the responses of DoE. The results show that higher concentrations of coating polymer and higher concentrations of plasticizer polymer led to a thicker and more elastic polymeric film, which led to a delay in drug release. Using the parameters of the piecewise function as DoE responses, an optimum formulation with a sigmoid shape dissolution profile and a 2.5-h lag time followed by rapid drug release were obtained.

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Development of pulsatile release tablets with swelling and rupturable layers

Cited by 86 publications

References 28 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

Untitled

Piecewise function parameters as responses of the design of experiment in the development of a pulsatile release chronopharmaceutical system

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