Sustained Release of a Water-Soluble Drug from Alginate Matrix Tablets Prepared by Wet Granulation Method

Mandal, Sanchita; Basu, S.; Sa, Biswanath

doi:10.1208/s12249-009-9333-z

Cited by 48 publications

(20 citation statements)

References 23 publications

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“…8. Impact on gel layer thickness development by the polymer erosion rate for drug release also increases over time due to tablet cracking and lamination at acidic pH (23,24). Hence, a 28% change in S/V of the 120-mg strength showed negligible influence on drug release rate compared with the 240-mg strength.…”

Section: Case I: Isoptin® Sr Tabletsmentioning

confidence: 99%

“…At pH 4.5 and 6.8, sodium alginate hydrates and swells rapidly, forming a gel layer surrounding the tablet. Unlike matrices consisting of low viscosity grade HPMC, the gel layer development of alginate is significant (23,24). However, it is interesting to note that drug release at pH 4.5 was essentially governed by polymer erosion in spite of high drug solubility.…”

Section: Case I: Isoptin® Sr Tabletsmentioning

confidence: 99%

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Influence of Drug Properties and Formulation on In Vitro Drug Release and Biowaiver Regulation of Oral Extended Release Dosage Forms

Lin

Zhou

Hoag

et al. 2016

AAPS J

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Abstract. Bioequivalence (BE) studies are often required to ensure therapeutic equivalence for major product and manufacturing changes. Waiver of a BE study (biowaiver) is highly desired for such changes. Current regulatory guidelines allow for biowaiver of proportionally similar lower strengths of an extended release (ER) product provided it exhibits similar dissolution to the higher strength in multimedia. The objective of this study is to demonstrate that (1) proportionally similar strengths of ER tablets exhibiting similar in vitro dissolution profiles do not always assure BE and (2) different strengths that do not meet the criteria for dissolution profile similarity may still be bioequivalent. Four marketed ER tablets were used as model drug products. Higher and lower (half) strength tablets were prepared or obtained from commercial source. In vitro drug release was compared using multi-pH media (pH 1.2, 4.5, 6.8) per regulatory guidance. In vivo performance was assessed based on the available in vivo BE data or established in vitro-in vivo relationships. This study demonstrated that the relationship between in vitro dissolution and in vivo performance is complex and dependent on the characteristics of specific drug molecules, product design, and in vitro test conditions. As a result, proportionally similar strengths of ER dosage forms that meet biowaiver requirements per current regulatory guidelines cannot ensure bioequivalence in all cases. Thus, without an established relationship between in vitro and in vivo performance, granting biowaiver based on passing in vitro tests may result in the approval of certain bioinequivalent products, presenting risks to patients. To justify any biowaiver using in vitro test, it is essential to understand the effects of drug properties, formulation design, product characteristics, test method, and its in vivo relevance. Therefore, biowaiver requirements of different strengths of ER dosage forms specified in the current regulatory guidance should be reevaluated to assure consistent safety and efficacy among different strengths.KEY WORDS: bioequivalence; biowaiver; extended release; in vitro drug release; in vivo evaluations; proportionally similar strength.

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Section: Case I: Isoptin® Sr Tabletsmentioning

confidence: 99%

Section: Case I: Isoptin® Sr Tabletsmentioning

confidence: 99%

Influence of Drug Properties and Formulation on In Vitro Drug Release and Biowaiver Regulation of Oral Extended Release Dosage Forms

Lin

Zhou

Hoag

et al. 2016

AAPS J

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“…For F3 slight colour change was seen after 45 days at accelerated condition, but no further defects were seen till 60 days. 16,17 Marketed preparation was also tested for stability in similar conditions for 60 days. After 45 days slight colour change was observed at room temperature and accelerated conditions.…”

Section: Stability Studiesmentioning

confidence: 99%

Diclofenac Sodium Loaded Sustained Release Matrix Tablet Possessing Natural and Synthetic Polymers: Formulation and in vitro Characterization

Nagaich¹,

Bharti²,

Pal³

et al. 2014

IJPER

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Object:The objective of the present study was to investigate the effect of various concentrations of natural and synthetic polymers on in vitro drug release from sustained release matrix tablets. Materials and method: HPMC K4M and acacia gum were used as synthetic (hydrophilic) and natural (hydrophobic) polymers respectively. Diclofenac sodium was used as a model drug to study the in vitro release profile. Matrix tablets of Diclofenac sodium were fabricated by varying the concentrations of both natural and synthetic polymer via direct compression method. Result:The results of all evaluation parameters of the matrix tablet were within the acceptable limit. A significant difference was observed on in vitro drug release due to difference in polymers and their concentration. HPMC K4M in the concentration of 7% w/v showed 88.20 ± 0.056% cumulative drug release at the end of 10 h while the same concentration of acacia showed 85.22% ± 0.045%. The release mechanism of matrix tablet followed zero order release kinetics. The finding of current investigation clearly indicates that the synthetic polymer was given a more sustained release profile than natural polymer on varied concentration. Conclusion: On comparing in vitro release of optimized formulation with marketed preparation, it was concluded that F3 was found to be more efficient and promising than marketed preparation.

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“…), chemical cross-linking (with glutaraldehyde, epichlorhydrin), and ionic cross-linking (with Ca +2 , Ba +2 , Al +3 ions), offers many new functional properties to meet their needs in design of drug delivery system (3). Several polysaccharides such as alginate (4,5), guar gum (6, 7), katira gum (8), tamarind gum (9), and pectin (10,11) have been derivatized and/or cross-linked to have tailor-made products of various types for drug delivery devices.…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of Ca+ 2 Ion Cross-Linked Carboxymethyl Xanthan Gum Tablet Prepared by Wet Granulation Technique

Maity

2014

AAPS PharmSciTech

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Abstract. The objective of this work was to study the release behavior of prednisolone from calcium-crosslinked carboxymethyl xanthan gum (CMXG) tablets in dissolution medium having different pH values prevailing in the gastrointestinal lumen. Xanthan gum (XG) was derivatized to CMXG which was then cross-linked in situ with Ca +2 ion during wet massing step of tablet preparation. Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry studies did not show any drug-polymer interaction although the drug underwent solid-state transformation during compression as evident from X-ray diffraction analysis. In vitro release study demonstrated that increase in the amount of Ca +2 ion decreased the drug release, and beyond a certain amount, the drug release increased. While increase in both drug load and tablet crushing strength decreased the drug release, increase in exposure time in acid solution of pH 1.2 increased the overall release of the drug. The mechanism of drug release was nonFickian/anomalous. The results indicated that variation in the amount of Ca +2 ion can modulate the drug release from CMXG matrix tablets as needed.

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Sustained Release of a Water-Soluble Drug from Alginate Matrix Tablets Prepared by Wet Granulation Method

Cited by 48 publications

References 23 publications

Influence of Drug Properties and Formulation on In Vitro Drug Release and Biowaiver Regulation of Oral Extended Release Dosage Forms

Influence of Drug Properties and Formulation on In Vitro Drug Release and Biowaiver Regulation of Oral Extended Release Dosage Forms

Diclofenac Sodium Loaded Sustained Release Matrix Tablet Possessing Natural and Synthetic Polymers: Formulation and in vitro Characterization

Development and Evaluation of Ca+ 2 Ion Cross-Linked Carboxymethyl Xanthan Gum Tablet Prepared by Wet Granulation Technique

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