New formulation of in situ gelling Metolose-based liquid suppository

E. Pásztor, Á Makó, G. Csóka, Zs Fenyvesi, R. Benko, M. Prosszer, S. Marton, I. Antal, I. Klebovich

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

Context: An in situ gelling liquid suppository is liquid at room temperature but forms a gel at body temperature. In our work, Metolose® SM-4000 (methylcellulose) is studied that basically shows thermal gelation at 68°C (2, ww). Objective: The objective was to study the potency of different factors (concentration, pH, additives) to change the value of thermal gelation temperature (Tt) for Metolose® to form an in situ gelling liquid suppository. Materials and methods: We studied the effect of Metolose® concentration, pH, and salts (sodium chloride, potassium chloride, sodium hydrogen carbonate, and sodium monohydrogen phosphate) on Tt by viscosimetry. To choose the appropriate compound, in vitro drug release was examined. Rectal safety test was performed on rats in vivo after 12-hour application. Results: Increasing the Metolose® concentrations (0.54, ww), Tt can be decreased, but it also altered the consistency of gel. pH does not affect the Tt. The water-soluble salts allowed reducing the gelation temperature to 37°C. Sodium monohydrogen phosphate in 4.5 concentration was found to be the most appropriate. The impact of examined factors on in vitro drug release of piroxicam from the in situ-formed gel was characterized according to Fickian diffusion. Metolose® and the chosen salt did not cause any morphological damage on the rectal tissues. Discussion: According to our study, Metolose® has the physical and chemical potential to be used as base for liquid suppositories.

Original languageEnglish
Pages (from-to)1-7
Number of pages7
JournalDrug Development and Industrial Pharmacy
Volume37
Issue number1
DOIs
Publication statusPublished - Jan 2011

Fingerprint

Suppositories
Temperature
Liquids
Gelation
Salts
Gels
Hot Temperature
Piroxicam
Sodium
Phosphates
Sodium Bicarbonate
Methylcellulose
Potassium Chloride
Body Temperature
Saline water
Chemical potential
Sodium Chloride
Pharmaceutical Preparations
Rats
Safety

Keywords

  • In situ gelling suppository
  • Metolose®
  • Piroxicam

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Organic Chemistry

Cite this

New formulation of in situ gelling Metolose-based liquid suppository. / Pásztor, E.; Makó, Á; Csóka, G.; Fenyvesi, Zs; Benko, R.; Prosszer, M.; Marton, S.; Antal, I.; Klebovich, I.

In: Drug Development and Industrial Pharmacy, Vol. 37, No. 1, 01.2011, p. 1-7.

Research output: Contribution to journalArticle

Pásztor, E, Makó, Á, Csóka, G, Fenyvesi, Z, Benko, R, Prosszer, M, Marton, S, Antal, I & Klebovich, I 2011, 'New formulation of in situ gelling Metolose-based liquid suppository', Drug Development and Industrial Pharmacy, vol. 37, no. 1, pp. 1-7. https://doi.org/10.3109/03639045.2010.489558
Pásztor, E. ; Makó, Á ; Csóka, G. ; Fenyvesi, Zs ; Benko, R. ; Prosszer, M. ; Marton, S. ; Antal, I. ; Klebovich, I. / New formulation of in situ gelling Metolose-based liquid suppository. In: Drug Development and Industrial Pharmacy. 2011 ; Vol. 37, No. 1. pp. 1-7.
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