Evaluation of swelling processes of various natural polymer matrix tablets by X-ray computed tomography and controlled drug release

Abstract

BACKGROUND:

The swelling properties and the drug-release sustainability of pre-gelatinized starches (𝛼-starch) tablets depend on the polymer characteristics.

OBJECTBS:

In order to clarify the drug release form, the natural polymers (NPs) were investigated. The relationship between drug release and swelling of natural polymers (NPs), the swelling processes of various starch polymers, were investigated using a drug-release test (DRT) and X-ray computed tomography (XCT). NPs consisting of various starches such as glutinous rice starch (GRS), corn starch (CS), and tapioca starch (TS) were used as additives for sustained drug-release tablets. Tablets consisted of 5% theophylline, 94% 𝛼-starch, and 1% magnesium stearate and were compressed at 6 kN. DRTs were measured in distilled water at 37 °C, and the drug concentrations were measured using UV (271 nm). Swelling ratio (R) profiles of the tablets during DRTs were evaluated based on XCT images.

RESULTS:

The order of the drug-release rate constant of the tablets was TS < GRS < CS. XCT images of the tablets were measured during the DRTs, and CS, GRS, and TS tablets swelled and showed increased gel-layers, and then finally disintegrated at 6, 9, and 11 h, respectively.

CONCLUSION:

The relationship between R profile and the % drug release of the tablets differed depending on the kind of NP used.

Keywords

Natural polymers X-ray computed tomography sustained drug release kinetics gelatinized starches swelling property polymer matrices tablets

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References

Aulton

M.E.

, Pharmaceutics: “The Science of Dosage Form Design”, 2nd edn, Churchill Livingstone, Edinburgh, 2002.

Hillery

A.M.

and Lloyd

A.W.

, Drug Delivery and Targeting for Pharmacists and Pharmaceutical Scientists Swarbrick

(ed.), Taylor and Francis, London, 2001.

Kumar

M.N.V.R.

and Kumar

, Polymeric controlled drug-delivery systems: Perspective issues and opportunities, Drug Dev. Ind. Pharm. 27 (2001), 1–30.

Melia

C.D.

, Hydrophilic matrix sustained-release systems based on polysaccharide carriers, Crit. Rev. Ther. Drug Carrier Syst. 8 (1991), 395–421.

Colombo

Bettini

Santi

and Nikolaos

A.P.

, Swellable matrices for controlled drug delivery: Gel-layer behaviour, mechanisms and optimal performance, Pharm. Sci. Technol. Today 3 (2000), 198–204.

Nerurkar

Jun

H.W.

Price

J.C.

and Park

M.O.

, Controlled-release matrix tablets of ibuprofen using cellulose ethers and carrageenans: Effect of formulation factors on dissolution rates, Eur. J. Pharm. Biopharm. 61 (2005), 56–68.

Kiortsis

Kachrimanis

Broussali

and Malamataris

, Drug release from tabletted wet granulations comprising cellulosic (HPMC or HPC) and hydrophobic component, Eur. J. Pharm. Biopharm. 59 (2005), 73–83.

Ebube

N.K.

and Jones

A.B.

, Sustained release of acetaminophen from a heterogeneous mixture of two hydrophilic non-ionic cellulose ether polymers, Int. J. Pharm. 272 (2004), 19–27.

Roy

D.S.

and Rohera

B.D.

, Comparative evaluation of rate of hydration and matrix erosion of HEC and HPC and study of drug release from their matrices, Eur. J. Pharm. Sci. 16 (2002), 193–199.

10.

Williams

R.O.

Reynolds

T.D.

Cabelka

T.D.

Sykora

M.A.

and Mahaguna

, Investigation of excipient type and level on drug release from controlled release tablets containing HPMC, Pharm. Dev. Technol. 7 (2002), 181–193.

11.

Levina

and Rajabi-Siahboomi

A.R.

, The influence of excipients on drug release from hydroxypropyl methylcellulose matrices, J. Pharm. Sci. 93 (2004), 2746–2754.

12.

Huang

and Brazel

C.S.

, Review, On the importance and mechanisms of burst release in matrix-controlled drug delivery systems, J. Controlled Release 73 (2001), 121–136.

13.

Simoda

and Wada

, Revised Cooking Studies, Nutritionist Training Series, Koseikan Co. Ltd., Tokyo, Japan , 1998, p. 156, ISBN 4-332-70126-7.

14.

Traini

Loretit

Jones

A.S.

and Young

, X-ray computed microtomography for the study of modified release systems, Microscopy and Analysis 22 (2008), 13–15.

15.

Chauve

Raverielle

and Marchessault

R.H.

, Comparative imaging of a slow-release starch excipient tablet: Evidence of membrane formation, Carbohydr. Polym. 70 (2007), 61–67.

16.

Inman

S.J.

Briscoe

B.J.

and Pitt

K.G.

, Topographic characterization of cellulose bilayered tablets interfaces, Chem. Eng. Res. Des. 85(A7) (2007), 1005–1012.

17.

Kojima

and Nakagami

, Investigation of water mobility and diffusivity in hydrating micronized low-substituted hydroxypropyl cellulose, hydroxypropylmethyl cellulose, and hydroxypropyl cellulose matrix tablets by magnetic resonance imaging (MRI), Chem. Pharm. Bull. 50 (2002), 1621–1624.

18.

Baumgartner

Lahajnar

Sepe

and Kristl

, Quantitative evaluation of polymer concentration profile during swelling of hydrophilic matrix tablets using 1H NMR and MRI methods, Eur. J. Pharm. Biopharm. 59 (2005), 299–306.

19.

Laity

P.R.

Mantle

M.D.

Gladden

L.F.

and Cameron

R.E.

, Magnetic resonance imaging and X-ray microtomography studies of a gel-forming tablet formulation, European Journal of Pharmaceutics and Biopharmaceutics 74 (2010), 109–119.

20.

Zeitler

J.A.

and Gladden

L.F.

, In-vitro tomography and non-destructive imaging at depth of pharmaceutical solid dosage forms, European Journal of Pharmaceutics and Biopharmaceutics 71 (2009), 2–22.

21.

http://www.nichidene.com/mamechishiki.htm, 2 February 2017.

22.

Higuchi

, Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices, J. Pharm. Sci. 52 (1963), 1145.

23.

Yamana

and Tsuji

, Kinetics of Pharmaceutical Preparations, Nankodo Press Co., Tokyo, 1979, p. 40.

24.

Keiji

, Structure and physical properties of gel prepared from a-amylase-treated cassava starch, Ph.D. Thesis, Graduate School of Agriculture, Meiji University, 2015.

25.

Thérien-Aubin

Zhu

X.X.

Ravenelle

and Marchessault

R.H.

, Membrane formation and drug loading effects in high amylose starch tablets studied by NMR imaging, Biomacromolecules 9 (2008), 1248–1254.