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Merck

Pharmacokinetic study of hydroxypropylmethylcellulose microparticles loaded with cimetidine.

Advances in clinical and experimental medicine : official organ Wroclaw Medical University (2013-03-08)
Rozina Kousar, Mahmood Ahmad, Ghulam Murtaza, Shujaat A Khan, Sabiha Karim, Izhar Hussain
ZUSAMMENFASSUNG

The objective of this study was to assess the pharmacokinetic behavior of floating hydroxypropylmethylcellulose microparticles loaded with cimetidine (FMC) prepared using the non-solvent addition coacervation technique. Based on the physico-chemical characteristics of three formulations (FMC1, FMC2 and FMC3), FMC2 having a 1:3 ratio of cimetidine:HPMC was found optimum. For in vivo analysis, a new HPLC analytical method was developed and validated. The optimized formulations were subjected to in vivo studies to calculate the various pharmacokinetic parameters for developed optimized microparticulate formulation FMC3. The developed floating microparticles of cimetidine were further evaluated by in vivo experimentation. The bioavailability parameters were found as: Cmax 1508.79 ± 37.95 ng/ml, Tmax 3.67 ± 0.17 h and AUC 14366.19 ± 377.64 ng h /mL. For prolonged drug release in the stomach, developed floating microparticles of cimetidine (FMC3) may be used, thereby improving the bioavailability and patient compliance.

MATERIALIEN
Produktnummer
Marke
Produktbeschreibung

Sigma-Aldrich
Methylzellulose, viscosity: 4,000 cP
Sigma-Aldrich
(Hydroxypropyl)methylcellulose, viscosity 2,600-5,600 cP, 2 % in H2O(20 °C)(lit.)
Sigma-Aldrich
Methylzellulose, viscosity: 15 cP, BioReagent, suitable for cell culture
Sigma-Aldrich
Methylzellulose, viscosity: 1,500 cP
Sigma-Aldrich
(Hydroxypropyl)methylcellulose
Sigma-Aldrich
(Hydroxypropyl)methylcellulose, average Mn ~10,000
Sigma-Aldrich
Methylzellulose, viscosity: 15 cP
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(Hydroxypropyl)methylcellulose, viscosity 80-120 cP, 2 % in H2O(20 °C)(lit.)
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(Hydroxypropyl)methylcellulose, viscosity 40-60 cP, 2 % in H2O(20 °C)(lit.)
Sigma-Aldrich
(Hydroxypropyl)methylcellulose, average Mn ~86,000
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(Hydroxypropyl)methylcellulose, average Mn ~120,000
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Methylzellulose, viscosity: 25 cP
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Cimetidin
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(Hydroxypropyl)methylcellulose, average Mn ~90,000
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Methylzellulose, 27.5-31.5% (Methoxyl content), viscosity: 400 cP
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Hypromellose, meets USP testing specifications
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Methocel® A15 LV, 27.5-31.5% methoxyl basis
Sigma-Aldrich
Methylzellulose, meets USP testing specifications, 26.0-33.0% (methoxyl group, on Dry Basis), viscosity: 400 cP
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Methocel® A4M, viscosity 3000-5500 mPa.s, 2 % in H2O(20 °C)
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Methocel® MC, medium viscosity, Methoxyl content 27.5-31.5 %
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Methylzellulose, 26.0-33.0% (Methoxy group (dry basis)), meets USP testing specifications, viscosity: 1,500 cP
Supelco
Cimetidin, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Methylzellulose, tested according to Ph. Eur.