Effect of Different Meltable Binders on the Disintegration and Dissolution Behavior of Zolmitriptan Oromucosal Fast Melt Tablets Pages 13-23

Effect of Different Meltable Binders on the Disintegration and Dissolution Behavior of Zolmitriptan Oromucosal Fast Melt Tablets
Pages 13-23

Doaa Ahmed El-Setouhy, Emad B. Basalious and Nevine Shawky Abdelmalak

DOI: https://doi.org/10.6000/1927-5951.2017.07.01.3
Published: 14 February 2017

Abstract: Objective: Fast melt tablets and sublingual route have been widely used for providing quick onset of action with the avoidance of first pass metabolism. The objective of this work was to compare the effect of different meltable binders namely; polyethylene glycol (PEG) 4000, pluronic F127 and pluronic F68 on the performance of fast release tablets of the model drug zolmitriptan prepared using the melt granulation technique regarding disintegration time (DT) and dissolution rate (DR) as criteria for rapid absorption and hence quick onset of action. Zolmitriptan is a potent antimigraine drug. Current oral zolmitriptan tablets suffer fromslow onset of action, poor bioavailability and large inter-subject variability.

Methods: 33 factorial design was adopted. The effect of binder type, binder concentration and croscarmellose sodium (disintegrant) concentration were studied on DT and DR.

Results: The three factors were found to significantly affect the DR and the inverse square root of DT and significant interactions were elucidated.

Conclusion: Although satisfactory results were obtained regarding DR, modifications using different excipients and or preparation methods should be considered to comply with pharmacopoeia requirement for DT.

Keywords: Melt granulation technique, fast release sublingual tablets, meltable binders, intragranular desintegrant, PEG4000, F68, F127.

Effects of Quercetin and Omega-3 Combination on Nuclear Factor Kappa B (NFκB) Expression Level in Pancreatic Tissue of Rats with Type-2 Diabetes Mellitus Pages 1-5

Effects of Quercetin and Omega-3 Combination on Nuclear Factor Kappa B (NFκB) Expression Level in Pancreatic Tissue of Rats with Type-2 Diabetes Mellitus
Pages 1-5
Asri Hendrawati and Mujiyanto Winardi
DOI: https://doi.org/10.6000/1927-5951.2017.07.01.1
Published: 14 February 2017

Abstract: Background: Hyperglycemia increases nuclear factor kappa B (NFκB) expression and promotes cellular injury. Quercetin and omega-3 are expected to regulate NFκB expression. This study aims to measure the effect of combination therapy with quercetin and omega-3 in lowering the expression of NFκB in the pancreatic tissue of rats with type-2 DM as compared to those treated with monotherapy with either agent.

Methods: This experimental study involved the use of a paraffin block of pancreatic tissue from 24 male Wistar rats aged 3 months, weighing between 250 g and 350 g. All rats underwent induction of type-2 DM and were divided into 4 groups: K1 (treated daily with placebo), K2 (treated with quercetin at 20 mg·kgBW-1·d-1), K3 (treated with omega-3 at 100 mg·kgBW-1·d-1), and K4 (treated with quercetin at 20 mg·kgBW-1·d-1 and omega-3 at 100 mg·kgBW-1·d-1). Treatments were administered orally for four weeks. Once the treatment was completed, samples of pancreatic tissue were collected for the measurement of the percentage of NFκB expression using immunohistochemical (IHC) staining.

Results: The average level of NFκB expression in the pancreatic nuclei of DM rats treated with the combination of omega-3 and quercetin was significantly lower than that of those treated with placebo, quercetin only, or omega-3 only (p < 0.05).

Conclusion: The combination of quercetin at 20 mg·kgBW-1·d-1 and omega-3 at 100 mg·kgBW-1·d-1 is significantly more effective in lowering the percentage of NFκB in pancreatic nuclei than monotherapy with either agent.

Keywords:Quercetin, omega-3, type-2 diabetes mellitus, immunohistochemistry, nuclear factor kappa B (NFκB).

In Silico Comparison of Disulfide-Bearing and Disulfide-Free Phytases among Microorganisms – Pages 24-34

In Silico Comparison of Disulfide-Bearing and Disulfide-Free Phytasesamong Microorganisms
Pages 24-34
Shirin Ebrahimi, Rashid Jamei, Abdolmajid Ghasemian and Seyyed Khalil Shokouhi Mostafavi

DOI: https://doi.org/10.6000/1927-5951.2017.07.01.3
Published: 14 February 2017

Abstract: Phytases are degrading enzymes that hydrolyze phytate (myo inositol hexa kis phosphate) to release a series of lower phosphate esters of myoinositol and orthophosphate. Phytase successfully used as an animal feed additive to increase the bioavailability of phosphate from phytic acid in the grain-based diets of poultry and swine. In order to investigate structural relationships between disulfide-bearing phytases and disulfide-free phytases, 9 phytases with resolved three-dimensional (3D) structure were retrieved as pdb and FASFA format from Protein Data Bank server and were analyzed using various tools and software. The results showed that 6 out of 9 phytases carry three or more disulfid bonds while the others lack any disulfide bonds. Our results also demonstrated that there is a remarkable correlation between the presence of disulfide bond and the number of amino acid in each phytase which means the larger enzymes contain three or more disulfide bonds whereas the enzymes containing less than 400 amino acids lack any disulfide bond. Additionally, in order to dig out the structure of phytases, some chemical and physical characteristics of phytases such as aliphatic index (AI), isoelectric pH (PI), amino acids percentage, molecular weights (MW) and 3D structure of phytases were analyzed. Results showed that phytases containing disulfide bonds have some identical characteristic including glycine percentage, AI, and 3D structure rather than disulfide-free phytases do. Moreover, evolutionary surveys by means of alignment studies and evaluations were conducted. Evolutionary analysis represented that phytases with disulfide bond most probably exhibited the same evolutionary course.

Keywords: In silico analysis, phytase, disulfide bond, protein stability.

Effect of Different Meltable Binders on the Disintegration and Dissolution Behavior of Zolmitriptan Oromucosal Fast Melt Tablets – Pages 13-23

Effect of Different Meltable Binders on the Disintegration and Dissolution Behavior of Zolmitriptan Oromucosal Fast Melt Tablets
Pages 13-23

Doaa Ahmed El-Setouhy, Emad B. Basalious and Nevine Shawky Abdelmalak

DOI: https://doi.org/10.6000/1927-5951.2017.07.01.3
Published: 14 February 2017

Abstract: Objective: Fast melt tablets and sublingual route have been widely used for providing quick onset of action with the avoidance of first pass metabolism. The objective of this work was to compare the effect of different meltable binders namely; polyethylene glycol (PEG) 4000, pluronic F127 and pluronic F68 on the performance of fast release tablets of the model drug zolmitriptan prepared using the melt granulation technique regarding disintegration time (DT) and dissolution rate (DR) as criteria for rapid absorption and hence quick onset of action. Zolmitriptan is a potent antimigraine drug. Current oral zolmitriptan tablets suffer fromslow onset of action, poor bioavailability and large inter-subject variability.

Methods: 33 factorial design was adopted. The effect of binder type, binder concentration and croscarmellose sodium (disintegrant) concentration were studied on DT and DR.

Results: The three factors were found to significantly affect the DR and the inverse square root of DT and significant interactions were elucidated.

Conclusion: Although satisfactory results were obtained regarding DR, modifications using different excipients and or preparation methods should be considered to comply with pharmacopoeia requirement for DT.

Keywords: Melt granulation technique, fast release sublingual tablets, meltable binders, intragranular desintegrant, PEG4000, F68, F127.

Preemptive Effects of Administration of Tualang Honey on Inflammatory Responses in Adult Male Rats – Pages 6-12

Preemptive Effects of Administration of Tualang Honey on Inflammatory Responses in Adult Male Rats
Pages 6-12
Che Aishah Nazariah Ismail, Che Maraina Che Hussin, Mahaneem Mohamed and Che Badariah Abd Aziz
DOI: https://doi.org/10.6000/1927-5951.2017.07.01.2
Published: 14 February 2017

Abstract: Background: Honey was reported to reduce pain and inflammation from burn wound. To date, no study has compared between the effects of Tualang honey and prednisolone on inflammatory responses in rats. This study has examined the effects of Tualang honey and prednisolone on inflammatory pain and its associated inflammatory responses secondary to formalin injection.

Methods: Twenty-one Sprague-Dawley male rats were randomised into control, Tualang honey (1.2 g/kg) or prednisolone (10 mg/kg)groups. Formalin test was conducted and the rats were sacrificed at four-hours post-formalin injection. Serum was collected for measurement of leukocytecounts and interleukins level. All data were analysed using one-way ANOVA with post-hoc Scheffe’s or Dunnet’s C test. Significance level was taken as less than 0.05.

Results: Tualang honey and prednisolone groups had significantly reduced pain behaviour and paw edema compared to control group. Tualang honey group demonstrated a significant increase in blood neutrophil count while prednisolone group had significant reduction in blood lymphocyte and monocyte counts compared to control group. Only interleukin-6 level was significantly reduced in honey group. Both interleukin-6 and -8 levels were significantly reduced in prednisolone group.

Conclusions: Tualang honey is comparable to prednisolone in modulating the inflammatory pain responses in rats; however, with regards to local and systemic inflammatory responses, it has differential effects compared to prednisolone.

Keywords:
Tualang honey, prednisolone, pain, inflammation, interleukin-6, interleukin-8.

Preemptive Effects of Administration of Tualang Honey on Inflammatory Responses in Adult Male Rats Pages 6-12

Effects of Quercetin and Omega-3 Combination on Nuclear Factor Kappa B (NFκB) Expression Level in Pancreatic Tissue of Rats with Type-2 Diabetes Mellitus
Pages 1-5
Asri Hendrawati and Mujiyanto Winardi
DOI: https://doi.org/10.6000/1927-5951.2017.07.01.1
Published: 14 February 2017

Abstract: Background: Honey was reported to reduce pain and inflammation from burn wound. To date, no study has compared between the effects of Tualang honey and prednisolone on inflammatory responses in rats. This study has examined the effects of Tualang honey and prednisolone on inflammatory pain and its associated inflammatory responses secondary to formalin injection.

Methods: Twenty-one Sprague-Dawley male rats were randomised into control, Tualang honey (1.2 g/kg) or prednisolone (10 mg/kg)groups. Formalin test was conducted and the rats were sacrificed at four-hours post-formalin injection. Serum was collected for measurement of leukocytecounts and interleukins level. All data were analysed using one-way ANOVA with post-hoc Scheffe’s or Dunnet’s C test. Significance level was taken as less than 0.05.

Results: Tualang honey and prednisolone groups had significantly reduced pain behaviour and paw edema compared to control group. Tualang honey group demonstrated a significant increase in blood neutrophil count while prednisolone group had significant reduction in blood lymphocyte and monocyte counts compared to control group. Only interleukin-6 level was significantly reduced in honey group. Both interleukin-6 and -8 levels were significantly reduced in prednisolone group.

Conclusions: Tualang honey is comparable to prednisolone in modulating the inflammatory pain responses in rats; however, with regards to local and systemic inflammatory responses, it has differential effects compared to prednisolone.

Keywords:Tualang honey, prednisolone, pain, inflammation, interleukin-6, interleukin-8.