Prilling of fatty acids as a continuous process for the development of controlled release multiparticulate dosage forms

Objective: This study was aimed to obtain a new excipient that can be used as a polymer matrix for the formulation of controlled release dosage forms.Methods: This study used coprocessing and crosslinking methods on amylose and xanthan gum (XG) to obtain a new excipient that can be usedfor controlled release matrix of pharmaceutical dosage forms. The coprocessing step was conducted by drum drying, and the crosslinking step wasprepared using 6 and 12% sodium trimetaphosphate (STMP). The produced novel excipients were characterized in terms of infrared (IR) spectrum,substitution degree, moisture content, swelling index, and gel strength.Results: Our results showed that amylose–XG excipients crosslinked using 6% STMP have greater gel strength and better swelling indexes thanexcipients crosslinked using 12% STMP. All coprocessed excipients exhibited no differences in their IR spectra, whereas the crosslinked excipientsdid, indicating a structural change due to the addition of phosphate groups. Crosslinking amylose–xanthan-coprocessed excipients using 6% STMPproduced degrees of substitution (DSs) of 7–8 phosphates per 100 monomeric subunits. The excipients had a moisture content of 8.21–12.85%, andthe pH of a 1% solution of excipients was 6.21–6.43. In addition, the swelling index and gel strength of the excipient where both amylose and XG werecrosslinked together Were more than 1 where only amylose was crosslinked.Conclusion: The crosslinking amylose–xanthan-coprocessed excipient using 6% STMP is more suitable for use in controlled release dosage forms,particularly when the polymer ratio is 1:1.

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Production of Unsaturated Fatty Acids Concentrate Tablets from Sardinella sp. Oil

E3S Web of Conferences ◽

10.1051/e3sconf/202014703008 ◽

2020 ◽

Vol 147 ◽

pp. 03008

Author(s):

Rodiah Nurbaya Sari ◽

Hari Eko Irianto ◽

Ema Hastarini

Keyword(s):

Fatty Acids ◽

Flow Rate ◽

Unsaturated Fatty Acids ◽

Dosage Forms ◽

Raw Material ◽

Solid Dosage Forms ◽

Fixed Angle ◽

Pharmaceutical Ingredients ◽

Solid Dosage ◽

Size Uniformity

Tablets are medicinal ingredients in solid dosage forms which are usually prepared with suitable pharmaceutical ingredients. In this study, unsaturated fatty acids concentrate from Sardinella sp. oil was used as raw material and then it was microencapsulated. The microcapsule was formulated into a tablet with proportion of 250 mg concentrated unsaturated fatty acids for each 450 mg tablet. Tablet granules were analyzed for compressibility, flow rate, and fixed angle. While, the tablets were determined for weight uniformity, released time, hardness, and tablet size uniformity. The results showed that compressibility, flow rate and fixed angle of the tablet granules were 5.6%; 10.36 g/sec; and 32.4° respectively. Tablets had 447.85 mg weight uniformity; 48’12” released time; and 0.775 kg hardness. In addition, the tablet size uniformity with diameter 10 mm and thickness 4 mm was 2.5. Based on the pharmacopoeia, the tablets of unsaturated fatty acids concentrate from Sardinella sp. oil had met these requirements, but optimization was still needed for improving the released time and hardness of the tablet.

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Report of the Workshop on Controlled Release Dosage Forms: Issues and Controversies: Academy of Pharmaceutical Sciences American Society for Clinical Pharmacology 3 Therapeutics Drug Information Association and Food and Drug Administration

Clinical Research Practices and Drug Regulatory Affairs ◽

10.3109/10601338809028596 ◽

1988 ◽

Vol 6 (1) ◽

pp. 1-15

Author(s):

Jerome P. Skelly ◽

William H. Barr ◽

Leslie Z. Benet ◽

James T. Doluisio ◽

Arthur H. Goldberg ◽

...

Keyword(s):

Clinical Pharmacology ◽

Controlled Release ◽

Drug Administration ◽

Drug Information ◽

Food And Drug Administration ◽

Dosage Forms ◽

Pharmaceutical Sciences ◽

American Society ◽

Information Association

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An in Vivo Single- and Multiple-Dose Study of Several Marketed Brands of Conventional and Controlled-Release Theophylline

Drug Intelligence & Clinical Pharmacy ◽

10.1177/106002808401800212 ◽

1984 ◽

Vol 18 (2) ◽

pp. 147-153 ◽

Cited By ~ 3

Author(s):

Jeffrey A. Kotzan ◽

Joseph V. Vallner ◽

James T. Stewart ◽

Irwin L. Honigberg ◽

W.J. Brown

Keyword(s):

Single Dose ◽

Controlled Release ◽

Multiple Dose ◽

Healthy Adult ◽

Dosage Forms ◽

Adult Males ◽

Single Dose Study ◽

Multiple Dose Study ◽

Dose Study ◽

Release Tablet

In a single-dose study, 18 healthy adult males consumed each of six dosage forms of theophylline. A conventional-release tablet, a syrup, and four competing brands of controlled-release theophylline were studied. Serial serum samples were obtained and analyzed via high pressure liquid chromatography (HPLC). After achieving steady state, 15 healthy adult males consumed each of five dosage forms of theophylline in a multiple-dose study. Serial blood samples were obtained between 0 and 72 hours and subjected to analysis with HPLC. The results indicated that the controlled-release products were not bioequivalent, although they achieved longer time-to-peak values than did the immediate-release syrup and the conventional-release tablet. A single sustained-release product was uniquely different on most pharmacokinetic parameters when compared with the remaining three controlled-release products. In general, the dosage form variation exceeded the individual subject variation on the single-dose study, but the opposite was true for the multiple-dose study.

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