scholarly works Pharmaceutics and Industrial Pharmacy
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Item Development of directly compressible excipients from Phoenix dactylifera (Date) mucilage and microcrystalline cellulose using co-processing techniques(2018) Akin-Ajani, O. D; Ajala, T. O; Okoli, U. M.; Okonta, OThe objective of this study was to harness the excipient potential of date mucilage by co-grinding and co-fusing with avicel for enhanced performance in the directcompression of metronidazole. Co-grinding and co-fusing of parent polymers were done using established methods and excipients were used in the direct-compression of metronidazole tablets. The shape and surface morphology of the particles of date mucilage (DAM) and co-processed excipients were generally granular, rough and irregular. There was a significant improvement in the disintegration of tablets prepared using the coprocessed excipients in comparison to that prepared using DAM alone. The disintegration time for tablets prepared using co-fused excipients was lower than that of co-grinded additives although the differences were not significant (p > 0.05). Generally, the co-processed excipients improved the mechanical and disintegration properties of the tablets produced compared to tablets prepared using DAM alone and could be further developed as direct compression excipientsItem Application of the Gurnham equation in characterizing the compressibility of fonio and sweet potato starches and their paracetamol tablet formulations(Nigeria Association of Pharmacists in Academia, 2018-02) Akin-Ajani, O. D.; Itiola, O. A.; Odeku, O. A.Background: A number of empirical relationships have been proposed to describe the compaction of pharmaceutical materials, among them are the Heckel, Kawakita and Gurnham equations. Objective: To characterize the compressibility of fonio, sweet potato and corn starches and their paracetamol formulations using the Gurnham and Kawakita equations, and to determine the complementarity of these equations. Materials and Methods: Starches were extracted from fonio (Digitaria exilis) grains and sweet potato (Ipomea batatas) tubers and modified by acid hydrolysis for 96 h. Paracetamol formulations containing 2.5–10.0 %w/w starch binders were prepared by wet granulation. Packing and compaction properties of native and modified starches and their formulations were determined using tapping procedures. The data obtained was analyzed using the Gurnham and Kawakita equations. Results: The ranking for Gurnham compressibility, c, for the starches was sweet potatocornfonio, which was inversely related to the ranking for Kawakita maximum volume reduction, a and angle of internal flow, θ. There was no clear-cut pattern in the Gurnham compressibility of paracetamol formulation probably due to its multicomponent nature. There was correlation between c, a and θ for all the starches with the modified starches exhibiting higher compressibility than native starches. There appeared to be no correlation between c and Kawakita compressibility index, b. Conclusion: The Gurnham equation appeared useful in characterising compressibility in single component systems and could be used along with Kawakita functions, to gain a better understanding of the deformation of powdered materials under pressure.Item Chrysophyllum albidum mucilage as a binding agent in paracetamol tablet formulations.(Springer, 2016-05) Ajala, T. O; Akin-Ajani, O. D; Ihuoma-Chidi, C.; Odeku, O. AChrysophyllum mucilage obtained from the fruit of Chrysophyllum albidum (Family Sapotaceae) hasbeen characterised and evaluated as a binding agent in comparison with methylcellulose in paracetamol tabletformulations. Chrysophyllum mucilage was characterized using elemental and proximate analyses as well as material properties. The Heckel and Kawakita plots were used to assess the compressional properties and the tablet properties were evaluated using tensile strength, friability, disintegration and dissolution times. The results showed the presence of calcium, magnesium, potassium, sodium, manganese, iron, copper, zinc and absence of heavy metals from the mucilage. The mucilage exhibited excellent flow and swelling properties, but poor water solubility. The viscosity of chrysophyllum mucilage increased with decrease in temperature in a similar manner with methylcellulose. C. albidum mucilage when used as a binder in paracetamol tablet formulation induced faster onset of plastic deformation and higher amount of total plastic deformation than methylcellulose. The results of the tablet properties showed that the tensile strength, disintegration and dissolution times, increased with increase in binder concentration while friability decreased. Tablets containing chrysophyllum mucilage as binder also had lower tensile strength, disintegration and dissolution times but higher friability values than those containing methylcellulose. However, tablets containing chrysophyllum mucilage at low concentrations conformed to pharmacopeial standard on disintegration indicating its potential usefulness as binder for immediate release tablets. Thus, C. albidum mucilage could be used as an alternative binding agent in pharmaceutical tabletsItem Evaluation of the disintegrant properties of native and modified forms of fonio and sweet potato starches(Wiley Online Library, 2016-10) Akin-Ajani, O. D.; Itiola, O. A.; Odeku, O AThe effects of acid modification on the disintegrant properties of two native starches obtained from Digitaria exilis (white fonio) and Ipomea batatas (sweet potato) were evaluated in comparison with official corn starch in paracetamol tablet formulations. The starches were extracted from grains of white fonio and tubers of sweet potato, and modified by acid hydrolysis using 6% w/w hydrochloric acid for 48 h. The native and modified forms of the starches were employed as exo-disintegrants in paracetamol tablet formulations at concentrations of 2.5, 5.0, and 10.0% w/w. The disintegrant properties were assessed using crushing strength (Cs), friability (Fr), disintegration time (DT), disintegrant efficiency ratio (DER), and the dimensionless quantity DERc. The results showed that crushing strength and friability of the tablets appeared to depend on the type, concentration, and nature of disintegrant used. Disintegration time generally decreased with increase in disintegrant concentration and the values complied with the pharmacopoeial standard for uncoated tablets (_15 min). Tablets containing acid modified starches showed longer disintegration times than those containing the native starches although there were no significant differences (p>0.05) in the values. Acid modification generally increased the disintegration efficiency ratio (DER) of the formulations while the values of DERc indicated that sweet potato starch would be the most efficient disintegrant with greater ability to enhance the balance between the mechanical and disintegration properties of the tablet. Thus, the experimental starches compared well with corn starch as disintegrants and could be useful for commercial tablet formulations.Item Effect of acid modification on the material and compaction properties of fonio and sweet potato starches(Wiley Online Library, 2014-03) Akin-Ajani, O. D.; Itiola, O. A.; Odeku, O. AStarches obtained from the grains of white fonio (Digitaria exilis) and tubers of sweet potato (Ipomea batatas) have been modified by acid hydrolysis at different steeping times – (0, 24 and 96 h) and the physicochemical, material and compaction properties of the modified starches have been evaluated in comparison with official corn starch. The effect of acid modification on the compaction properties of the starches were evaluated with the aim of determining their usefulness as excipients in direct compression. The results showed that the physicochemical and material properties of the starches varied considerably depending on their botanical source. Acid modification led to an increase in solubility and relative crystallinity but decrease in swelling and viscosity of the starches. The effects were found to depend on the steeping time during acid hydrolysis. The results of the compressional properties indicated that the starches formed intact tablets at relatively low compression pressure with acid modified starches forming tablets with higher tensile strength than the natural starches. The results indicate that the physicochemical and compaction properties of white fonio and sweet potato starches were improved by acidmodification yielding starches that could be suitable as directly compressible excipient.Item Effects of pigeon pea and plantain starches on the compressional, mechanical and disintegration properties of paracetamol tablets(Taylor & Francis Group, 2006-09) Dare, K.; Akin-Ajani, D. O; Odeku, O. A; Odusote, O. M; Itiola, O. A.A study has been made of the effects of pigeon pea starch obtained from the plant Cajanus cajan (L) Millisp. (family Fabaceae) and plantain starch obtained from the unripe fruit of Musa paradisiaca L. (family Musaceae) on the compressional, mechanical, and disintegration properties of paracetamol tablets in comparison with official corn starch BP. Analysis of compressional properties was done by using density measurements, and the Heckel and Kawakita equations, whereas the mechanical properties of the tablets were evaluated by using tensile strength (T-a measure of bond strength) and brittle fracture index (BFI-a measure of lamination tendency). The ranking for the mean yield pressure, Py, for the formulations containing the different starches was generally corn < pigeon pea < plantain starch while the ranking for Pk, an inverse measure of the amount of plasticity, was pigeon pea < plantain < corn starch, which indicated that formulations containing corn starch generally exhibited the fastest onset of plastic deformation, whereas those formulations containing pigeon pea starch exhibited the highest amount of plastic deformation during tableting. The tensile strength of the tablets increased with increase in concentration of the starches while the Brittle Fracture Index decreased. The ranking for T was pigeon pea > plantain > corn starch while the ranking for BFI was corn > plantain > pigeon pea starch. The bonding capacity of the formulations was in general agreement with the tensile strength results. The disintegration time (DT) of the formulation increased with concentration of plantain and corn starches but decreased with concentration of pigeon pea starch. The general ranking of DT values was plantain < pigeon pea < corn starch. Notably, formulations containing pigeon pea starch exhibited the highest bond strength and lowest brittleness, suggesting the usefulness of pigeon pea starch in producing strong tablets with minimal lamination tendency. Plantain starch, on the other hand, would be more useful where faster disintegration of tablet is desired. The results show that the starches could be useful in various formulations depending on the intended use of the tablets with the implication that the experimental starches can be developed for commercial purposesItem 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 Flow, compaction and tabletting properties of co-processed excipients using pregelatinized ofada rice starch and HPMC(IPEC-Americas Inc., 2018) Okunlola, A.The growing popularity of direct-compression process necessitates an ideal filler–binder that can substitute two or more excipients. Pregelatinization of starches significantly improves swelling and flow properties but produces tablets with low mechanical strength. When used as a binder in many tablet formulations, hydroxyl propyl methyl cellulose (HPMC) imparts mechanical strength but because of its poor flow during high speed tablet manufacturing, granulation of HPMC-based formulations is required prior to compaction. Directly-compressible co-processed excipients were developed utilizing pregelatinized starch of the indigenous Ofada rice starch (Oryza glaberrima Steud Family Poaceae) and HPMC. Co-processed excipients of various combinations of pregelatinized Ofada rice starch and HPMC K15M (15cps) were prepared using a co-fusion method (97.5:2.5; 95:5; 92.5:7.5; 90:10; 85:15; 80:20). The flow and compaction properties of the co-processed excipients, as well as, individual excipients were evaluated using density, Hausner ratio, Carr’s index, angle of repose, angle of internal friction, the Kawakita model, consolidation index and rate. Aceclofenac tablets were formulated using direct compression with starch, HPMC and specific co-processed excipients as filler-binders. Pregelatinization produced starch with larger granules and improved flow characteristics. FTIR spectra of the co-processed excipients confirmed absence of any chemical interaction. The angle of repose, Hausner ratio, Carr’s index, angle of internal friction indicated that flow properties improved with increasing starch content of the co-processed excipients. Kawakita plots, consolidation index and consolidation rate demonstrated cohesiveness while compressibility and rate of packing were enhanced. Aceclofenac tablets containing co-processed excipients exhibited a crushing strength ≥ 66.03 ± 1.58 MNm-2; friability ≤ 1%; disintegration time ≤ 10.75 ±3.10 minutes and dissolution time (t80) ≤ 30.00 ± 3.07 minutes. The co-processed excipients of pregelatinized Ofada rice starch and HPMC could be cheaper alternatives to other synthetic excipients used in direct compression of tablets assuming the starch would meet all compendial specifications.Item 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 Development of ibuprofen microspheres using acetylated plantain starches as polymer for sustained release(Springer Publications, 2018) Okunlola, A.; Ghomorai, T.Ibuprofen has a short half-life (1–3 h) and istypically administered 3–4 times daily with subsequent adverse side effects. A good approach to reduce these effects is the preparation of sustained-release formulations of ibuprofen. Acetylated starches form water-insoluble, acid-resistant films that can substantially retard drug release. Ibuprofen microspheres were prepared using acetylated plantain starch as sustained-release polymer. Starch obtained from unripe plantain (Musa Paradisiaca normalis) were acetylated using acetic anhydride with pyridine (degrees of substitution, DS 1.5 ± 0.05 and 2.20 ± 0.10). The starches were characterized using morphology, crystallinity, swelling, density and flow properties. Ibuprofen microspheres were prepared by quasi-emulsion solvent diffusion method, using acetylated plantain starches DS 1.5 and 2.20 in comparison to Eudragit S100. Full 32 factorial experimental design was performed with polymer type (X1), polymer: drug ratio (X2) as independent factors; microsphere size, entrapment, and quantity of drug released in 12 h (Q12) were dependent variables. The data from in vitro drug release were fitted to various kinetic models. Acetylation resulted in larger starch aggregates with disruption in crystalline order. Ibuprofen microspheres were spherical with size 5.50 ± 4.00–129.90 ± 12.97μm. Drug entrapment was 43.92 ± 4.00–79.91 ± 6.15%. Values of Q12 ranged from 20.10 ± 0.55 to 54.00 ± 5.71%. Interaction between variables X1 and X2 had positive effects on size and entrapment. Drug release fitted zero order, first order and Baker-Lonsdale kinetic models. Acetylated starch of plantain with DS 2.20 was suitable as a polymer at polymer:drug ratio 4:1 for the formulation of ibuprofen microspheres with prolonged drug release.