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Development and Evaluation of Dual Cross-Linked Pulsatile Beads for Chronotherapy of Rheumatoid Arthritis.

Bansal AK, Pande V - J Pharm (Cairo) (2012)

Bottom Line: Lornoxicam dual cross-linked beads were prepared by dropping dispersed phase of lornoxicam, pectin, and sodium alginate into the dispersion phase of different concentrations of calcium chloride solution followed by aluminium chloride solution.The formulated beads were further coated by Eudragit L & S 100 in the ratio 1 : 2 w/w in order to achieve desired lag time.In vitro release study showed lag time of 5-8 h before release of lornoxicam from the formulated beads.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, H.R. Patel Institute of Pharmaceutical Education and Research, Dhule, Shirpur 425405, Maharashtra, India.

ABSTRACT
In the present investigation, pulsatile release beads were prepared by ionic gelation technique. Lornoxicam dual cross-linked beads were prepared by dropping dispersed phase of lornoxicam, pectin, and sodium alginate into the dispersion phase of different concentrations of calcium chloride solution followed by aluminium chloride solution. The formulated beads were further coated by Eudragit L & S 100 in the ratio 1 : 2 w/w in order to achieve desired lag time. In vitro release study showed lag time of 5-8 h before release of lornoxicam from the formulated beads. Thus, formulated dual cross-linked beads when administered at bed time may release lornoxicam when needed most for chronotherapeutics of early morning rheumatoid arthritis attacks in chronic patients.

No MeSH data available.


Related in: MedlinePlus

Effect of Eudragit solution concentration on lag time.
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Related In: Results  -  Collection


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fig7: Effect of Eudragit solution concentration on lag time.

Mentions: USP dissolution apparatus 1 (Basket type) was used to perform the drug release study at 50 rpm and temperature maintained at  37 ± 0.5°C. In vitro drug release studies of formulation fabricated with enteric coated as well as uncoated gelatin capsule shell were performed. The bare pectin alginate beads showed immediate drug release while, when the beads are filled in the enteric gelatin capsule there was a pH dependent drug release after the dissolution of the capsule shell. Drug release was inversely related to the concentration of sodium alginate and cross-linking of beads. The decrease in drug release resulted in increase in sodium alginate concentration and increasing the cross-linking time. With the increase in the concentration of the Eudragit S100 and Eudragit L100 in the coating solution there is considerable increase in the lag time for drug release, namely, when 2% Eudragit was used for coating. The lag time was observed to be 6 hrs while 4% and 6% Eudragit showed lag time 8 hrs to 9 hrs, respectively. Hence, we optimized the Eudragit concentration as 2% to get the desired lag time for the drug release (Figure 7). The effective sustained release was obtained from different formulations. The uncoated formulations P1, P4, P6, and P7 showed much sustained drug release than formulation P2, P3, and P5. Moreover, amongst this formulation P6 and P7 gave more sustained drug release due to the formation of the rigid gel structure dual with AlCl3+ which reduces the drug release from gel matrix of beads, so overcome the burst release of drug from the pectin alginate beads by formulating the dual cross-linked beads.


Development and Evaluation of Dual Cross-Linked Pulsatile Beads for Chronotherapy of Rheumatoid Arthritis.

Bansal AK, Pande V - J Pharm (Cairo) (2012)

Effect of Eudragit solution concentration on lag time.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595973&req=5

fig7: Effect of Eudragit solution concentration on lag time.
Mentions: USP dissolution apparatus 1 (Basket type) was used to perform the drug release study at 50 rpm and temperature maintained at  37 ± 0.5°C. In vitro drug release studies of formulation fabricated with enteric coated as well as uncoated gelatin capsule shell were performed. The bare pectin alginate beads showed immediate drug release while, when the beads are filled in the enteric gelatin capsule there was a pH dependent drug release after the dissolution of the capsule shell. Drug release was inversely related to the concentration of sodium alginate and cross-linking of beads. The decrease in drug release resulted in increase in sodium alginate concentration and increasing the cross-linking time. With the increase in the concentration of the Eudragit S100 and Eudragit L100 in the coating solution there is considerable increase in the lag time for drug release, namely, when 2% Eudragit was used for coating. The lag time was observed to be 6 hrs while 4% and 6% Eudragit showed lag time 8 hrs to 9 hrs, respectively. Hence, we optimized the Eudragit concentration as 2% to get the desired lag time for the drug release (Figure 7). The effective sustained release was obtained from different formulations. The uncoated formulations P1, P4, P6, and P7 showed much sustained drug release than formulation P2, P3, and P5. Moreover, amongst this formulation P6 and P7 gave more sustained drug release due to the formation of the rigid gel structure dual with AlCl3+ which reduces the drug release from gel matrix of beads, so overcome the burst release of drug from the pectin alginate beads by formulating the dual cross-linked beads.

Bottom Line: Lornoxicam dual cross-linked beads were prepared by dropping dispersed phase of lornoxicam, pectin, and sodium alginate into the dispersion phase of different concentrations of calcium chloride solution followed by aluminium chloride solution.The formulated beads were further coated by Eudragit L & S 100 in the ratio 1 : 2 w/w in order to achieve desired lag time.In vitro release study showed lag time of 5-8 h before release of lornoxicam from the formulated beads.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, H.R. Patel Institute of Pharmaceutical Education and Research, Dhule, Shirpur 425405, Maharashtra, India.

ABSTRACT
In the present investigation, pulsatile release beads were prepared by ionic gelation technique. Lornoxicam dual cross-linked beads were prepared by dropping dispersed phase of lornoxicam, pectin, and sodium alginate into the dispersion phase of different concentrations of calcium chloride solution followed by aluminium chloride solution. The formulated beads were further coated by Eudragit L & S 100 in the ratio 1 : 2 w/w in order to achieve desired lag time. In vitro release study showed lag time of 5-8 h before release of lornoxicam from the formulated beads. Thus, formulated dual cross-linked beads when administered at bed time may release lornoxicam when needed most for chronotherapeutics of early morning rheumatoid arthritis attacks in chronic patients.

No MeSH data available.


Related in: MedlinePlus