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Item Evaluation of freeze-dried pregelatinized Chinese yam (Dioscorea oppositifolia) starch as a polymer in floating gastroretenive metformin microbeads.(2010) Okunlola, A.; Patel, R. P.; Odeku, O. A.Pregelatinized Chinese yam (Dioscorea oppositifolia) starch has been evaluated as a polymer for the formulation of floating gastroretentive beads for the controlled delivery of metformin hydrochloride. Floating microbeads were prepared by the ionotropic gelation method using a blend of modified Chinese yam starch and sodium alginate at different ratios. Sodium bicarbonate was added as a gas-generating agent. The floating microbeads were characterized by SEM, DSC, FTIR analyses and the drug entrapment efficiency and floating ability was evaluated. Drug release was investigated using in vitro dissolution test and the results were fitted to various kinetic models to determine the mechanism(s) of release. Spherical, discrete and free flowing microbeads were obtained from the modified starch-alginate blends. Minimum lag time (< 20 s) was observed for the floating microbeads containing starch and buoyancy was maintained for 12 h. The release of MET from the floating microbeads appeared to be controlled by varying the starch to alginate polymer ratio. In general, the formulations followed diffusion and erosion mechanisms of drug release. The results suggest that modified Chinese yam starch-sodium alginate blend can be useful for the formulation of floating gastroretentive system for metformin hydrochlorideItem Formulation of metronidazole tablets using hydroxypropylated white yam (dioscorea rotundata) starch as the binding agent(IPEC-Americas Inc, 2017) Okunlola, A.; Alade, O. O.; Odeku, O. A.White yam starch obtained from the tubers of Dioscorea rotundata Poir was modified by hydroxypropylation and used as a binding agent in a metronidazole tablet formulation and compared with corn starch BP. The quantitative effects of the novel starch binder on the mechanical (tensile strength and friability) and release properties (disintegration and dissolution times) of the metronidazole tablet was analyzed using a full 23 factorial experimental design. The individual and interaction effects of type of starch binder (X1), concentration of binder (X2) and relative density (X3) on tensile strength, friability, disintegration time and dissolution time (t90) were determined. The ranking of the coefficients was X3 > X2 > X1 on T, X1 > X3 > X2 on F and X3 > X1 > X2 on DT and t90 (time for 90% drug release) indicating that the formulation variables influence the properties of metronidazole tablets to varying degrees. This indicates that the type and concentration of starch binder as well as the compression pressure employed in table formulation need to be carefully selected to obtain tablets with the desired mechanical and drug release properties. Hydroxypropyl white yam starch could be more useful as a binder especially when tablets require high mechanical strength and faster drug release are desired.Item Design of cissus–alginate microbeads revealing mucoprotection properties in anti-inflammatory therapy(Elsevier B.V., 2015) Okunlola, A.; Odeku, O. A.; Lamprech, A.; Oyagbemi, A. A.; Oridupa, O. A.; Aina, O. O.Cissus gum has been employed as polymer with sodium alginate in the formulation of diclofenac microbeads and the in vivo mucoprotective properties of the polymer in anti-inflammatory therapy assessed in rats with carrageenan-induced paw edema in comparison to diclofenac powder and commercial diclofenac tablet. A full 23 factorial experimental design has been used to investigate the influence of concentration of cissus gum (X1); concentration of calcium acetate (X2) and stirring speed (X3) on properties of the microbeads. Optimized small discrete microbeads with size of 1.22 ± 0.10 mm, entrapment efficiency of 84.6% and t80 of 15.2 ± 3.5 h were obtained at ratio of cissus gum:alginate (1:1), low concentration of calcium acetate (5% w/v) and high stirring speed (400 rpm). In vivo studies showed that the ranking of percent inhibition of inflammation after 3 h was diclofenac powder > commercial tablet = cissus > alginate. Histological damage score and parietal cell density were lower while crypt depthand mucosal width were significantly higher (p < 0.05) in the groups administered with the diclofenac microbeads than those administered with diclofenac powder and commercial tablet, suggesting the mucoprotective property of the gum. Thus, cissus gum could be suitable as polymer in the formulation of non-steroidal anti-inflammatory drugs ensuring sustained release while reducing gastric side effects.Item Potentials of natural polymers as nanomaterials for pharmaceutical drugs delivery(2013) Bablola, O. C.; Okunlola, A.; Odeku, O. A.During the last decades, pharmaceutical technology has taken advantage of the advent of nanotechnology for its application in four broad areas of the pharmaceutical industry: drug delivery, diagnostic products, biomarker discovery and product packaging. Of all the potential pharmaceutical applications of nanotechnology, drug delivery is currently the most developed and seems to be the most promising for the long-term. Of great advantage is the concept and ability to manipulate molecules and supramolecular structures to produce drug delivery devices with great potential for improving the efficacy of drug delivery systems. Polymeric nanoparticles are colloidal carriers which usually consist of synthetic, semi-synthetic or natural polymers, and depending on the materials used and their manufacturing methods, nanoparticles can adopt diverse shapes and sizes with distinct properties. Natural polymers such as gelatin, albumin, alginate and chitosan have great potentials because of their inherent properties such as biocompatibility, non-immunogenicity, non-toxicity and biodegradability. In addition, they can be subjected to physical and chemical modifications to alter their physic-chemical properties resulting in a wide range of functional properties that may permit their application as polymers for the formulation of nanoparticles. Moreover, they have been found to issues and relatively inexpensive when compared to the synthetic polymers. This paper is a review of some natural polymers that have shown promise as biodegradable polymers for the formulation of nanoparticulate drug delivery system.Item Microbead design for sustained drug release using four natural gums(Elsevier, 2013) Odeku, O. A.; Okunlola, A.; Lamprecht, AFour natural gums, namely albizia, cissus, irvingia and khaya gums have been characterized and evaluated as polymers for the formulation of microbeads for controlled delivery of diclofenac sodium. The natural gums were characterized for their material properties using standard methods. Diclofenac microbeads were prepared by ionotropic gelation using gel blends of the natural gums and sodium alginate at different ratios and zinc chloride solution (10%w/v) as the crosslinking agent. The microbeads were assessed using SEM, swelling characteristics, drug entrapment efficiencies and release properties. Data obtained from in vitro dissolution studies were fitted to various kinetic equations to determine the kinetics and mechanisms of drug release, and the similarity factor, f2, was used to compare the different formulations. The results showed that the natural gum polymers varied considerably in their material properties. Spherical and discrete microbeads with particle size of 1.48–2.41μm were obtained with entrapment efficienciesof 44.0–71.3%w/w. Drug release was found to depend on the type and concentration of polymer gumused with formulations containing gum:alginate ratio of 3:1 showing the highest dissolution times. Con-trolled release of diclofenac was obtained over for 5 h. Drug release from the beads containing the polymer blends of the four gums and sodium alginate fitted the Korsmeyer–Peppas model which appeared to be dependent on the nature of natural gum in the polymer blend while the beads containing alginate alone fitted the Hopfenberg model. Beads containing albizia and cissus had comparable release profiles to thosecontaining khaya (f2> 50). The results suggest that the natural gums could be potentially useful for the ormulation controlled release microbeads.Item Evaluation of starches obtained from four dioscorea species as binding agent in chloroquine phosphate tablet formulations(Elsevier, 2011-01) Okunlola, A.; Odeku, O. A.Starches obtained from four Dioscorea species namely Dioscorea dumetorum (Bitter), Dioscorea oppositifolia (Chinese), Dioscorea alata (Water), and Dioscorea rotundata (White) have been evaluated as binding agents in chloroquine phosphate tablet formulations in comparison with official corn starch. The compressional properties of the formulations were analyzed using density measurements and the Heckel and Kawakita equations. The mechanical properties of the tablets were assessed using tensile strength, brittle fracture index (BFI), and friability tests while the drug release properties of the tablets were assessed using disintegration and dissolution times. The results indicate that the four starches vary considerably in their physicochemical properties. The ranking for the tensile strength and the disintegration and dissolution times for the formulations was Chinese> Bitter > Corn> White > Water while the ranking was reversed for BFI and friability. The results suggest that Water, White, and Corn could be useful when faster disintegration time of tablets is desired while Chinese and Bitter could be more useful when bond strength is of concern and in minimizing the problems of lamination and capping in tablet formulationItem Effects of water yam and corn starches on the interacting variables influencing the disintegration of chloroquine phosphate tablets(Medwell Journals, 2010) Okunlola, A.; Odeku, O. A.The individual and interaction effects of nature (X) and concentration (Y) of disintegrant and the relative density (Z) on the mechanical and release properties of chlor-oquine phosphate tablets were studied using a 23 factorial experiment design. Water yam starch (low level) and corn starch (high level) were used as disintegrants at concentrations of 5.0 and 20.0% w/w .The mechanical properties were assessed using the Crushing Strength (CS) and Friability (F) and the release properties by the Disintegration Time (DT) and dissolution time (t80). Increasing the concentration of disintegrants and the relative density of tablets resulted in increase in CS but decrease in F, DT and t80. The ranking of the individual coefficient values was Z>X>Y for CS, Z>X>Y for F and DT and Y>X>Z for t80, while that for the interaction coefficient was X-Z>Y-Z>X-Y for CS, Y-Z>X-Z>X-Y for F, Y-Z>X-Y>X-Z for DT and t80. Changing the disintegrant from corn starch to water yam starch resulted in decrease in CS, DT and t80 but increase in F. The results show considerable interaction between the variables employed and suggest that water yam could be an alternative disintegrant to corn starch particularly where with faster disintegration and release are required.Item Generic versus innovator: Analysis of the pharmaceutical qualities of paracetamol and ibuprofen tablets in the Nigerian market(2009) Okunlola, A.; Adegoke, O. A.; Odeku, O. A.The physicochemical equivalence of twenty-two brands of paracetamol and nine brands of ibuprofen tablets sourced from retail Pharmacy outlets in the Nigerian market to their respective innovator brands were investigated. The uniformity of weight, friability, crushing strength, disintegration and dissolution times and assay of active paracetamol ingredient were used as assessment parameters. All the brands of paracetamol and ibuprofen tablets complied with the official specifications for uniformity of weight. However, five brands of paracetamol failed the friability test, one brand of paracetamol and two brands of ibuprofen failed the disintegration test and three brands of paracetamol and four brands of ibuprofen failed the assay of active ingredients. The study shows that not all the brands of paracetamol and ibuprofen tablets are physico-chemically equivalent to their innovator brands. There is therefore the need for constant market surveillance to ascertain their compliance with official standards and equivalence to the innovator products.Item Comparative evaluation of starches obtained from dioscore species as intragranular tablet disintegrant(Editions de Sante, 2008) Okunlola, A.; Odeku, O. A.Starches from four Dioscorea species namely Dioscorea dumetorum (bitter yam), D. oppositifolia (Chinese yam), D. alata (water yam) and D. rotundata (white yam) have been evaluated as disintegrants in chloroquine phosphate tablet formulations in comparison with official corn starch. The mechanical and drug release properties of the tablets were assessed. The results showed that the ranking of the effectiveness of the starches as intragranular disintegrant was water > white > corn > Chinese> bitter. The disintegrant concentration had significant (p < 0.001) effects on the disintegrant efficiency. The four experimental starches compared favorably and in some cases showed better efficiency as intragranular disintegrant than corn starch and could be further developed for use in commercial tablet formulation.Item Evaluation of pharmaceutical and microbial qualities of some herbal medicinal products in South Western Nigeria(Pharmacotherapy group, Faculty of Pharmacy, University of Benin, Benin City, 2007-03) Okunlola, A.; Adewoyin, B. A; Odeku, O. A.Purpose: The aim of the present study was to investigate the pharmaceutical and microbial qualities of 21 different (of various dosage forms) Herbal Medicinal Products (HMPs) sourced from some traditional medicine sales outlets and retail pharmacy outlets in south western Nigeria. Method: The pharmaceutical qualities evaluated include tablet crushing strength, friability, disintegration time; density of the solutions and suspensions; particle size and angle of repose of the powders. Phytochemical tests were carried out to assess the class of compounds present in the formulations and the microbial quality of the products was also evaluated. Results: The results show that twelve (57.1 %) of the products had their manufacturing and expiry dates stated, nine (42.9%) products have been registered by NAFDAC and ten (47.6%) did not have their content stated but had their therapeutic claims indicated on the container. The tablet formulation (Product A) showed acceptable crushing strength and friability but failed the test for disintegration time. The angle of repose of the powder dosage forms were considerably high showing that the powders were highly cohesive and not free flowing. The microbial load of the products varied considerably. Ten (47.6%) of the samples were contaminated by E. coli, seven (33%) were contaminated by Salmonella, fifteen (71.4%) were contaminated by Staphylococcus aureus and twelve (57.1%) were contaminated by fungi. Conclusion: There is need for constant monitoring and control of the standards of herbal medicines available in the Nigerian market.