scholarly works Pharmaceutics and Industrial Pharmacy

Permanent URI for this collectionhttps://repository.ui.edu.ng/handle/123456789/560

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Start date: 2010End date: 2019

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    Formulation of Diclofenac Sodium Emulsion Using Colocynthis Citrullus L. (Melon) Seed Oil
    (West African Postgraduate College of Pharmacists (WAPCP), 2019) Akin-Ajani, O. D.; Ajala T. O.; Ogunnubi M. A
    Background: Melon seed obtained from the fruit of Colocynthis citrullus L. is widely used in Nigeria as a soup thickener. The seed has a high oil yield (42-57%) which has been largely unexplored as excipient in pharmaceutical formulations. Objectives: To evaluate melon seed oil as a drug carrier in emulsion using diclofenac as a model drug. Methods: Melon seed oil was extracted and the physicochemical properties were characterised. The emulsions were prepared using the traditional wet and dry gum methods, and all the emulsions were evaluated using viscosity measurements, creaming rate, and in-vitro drug release. Results: Melon seed oil had a pale yellow colour, with characteristic taste, and a neutral pH. Melon seed oil exhibited higher acid, saponification and ester values than castor oil but lower iodine value indicating an edible non-drying oil, unsusceptible to auto-oxidation. Both oils achieved a great degree of emulsification with globule size < 15mm μm. Emulsions of melon seed oil were generally less viscous with a higher degree of creaming compared to castor oil emulsions. Diclofenac emulsions prepared with melon seed oil, however, were more viscous and gave the highest release of diclofenac irrespective of the method of preparation. Only diclofenac emulsion prepared with melon seed oil using the wet gum method had > 70 % release within 45 minutes thus meeting the official specification. Conclusion: Melon seed oil functioned as a drug carrier for diclofenac. Thus, it will find application in pharmaceutical emulsions.
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    Date Mucilage as Co-Polymer in Metformin-loaded Microbeads for Controlled Release
    (International Pharmaceutical Excipients Council (IPEC), 2019-03) Akin-Ajani O. D.; Ajala T. O.; Ikehin, M.
    Mucilage from the fruit of the date palm (Phoenix dactylifera) was characterized and evaluated for use as a polymer in controlled release metformin-loaded microbeads. Metformin-loaded (1% w/w) microbeads were formed by the ionotropic gelation method using blends (2% w/v) of date mucilage: sodium alginate in varying concentrations (20:80 C4, 25:75 C3, 33:67 C2, 50:50 C1) using zinc chloride (10% w/v) as a crosslinking agent. Bead size and morphology, swelling index, entrapment efficiency and release properties were then measured. The dissolution profiles were fitted to kinetic equations to determine the kinetics and mechanisms of drug release while the similarity factor, ƒ2 was used to determine formulations with similar drug release patterns. The results showed that the date mucilage had crude fat content of 2.5%. The microbeads formed were spherical with bead sizes ranging from 0.44 to 1.99 mm except for the one prepared using blend C4 which was ellipsoidal. Drug entrapment efficiency ranged between 25.0 and 91.1%w/w with alginate alone giving the least entrapment. Microbeads formulated with blends C2 and C3 had the slowest dissolution rates at t15 < 9% in 240 minutes. C3, however, had a higher entrapment efficiency and was considered the optimum formulation. All microbead formulations fitted the Korsmeyer-Peppas’ model with super case II transport mechanism except for the one made of sodium alginate alone, which had an anomalous (non-Fickian) diffusion. Secondary parameters of the Korsmeyer-Peppas’ model showed that microbead formulations C2 and C3 provided controlled release for longer than 24 hours. Similarity factor, ƒ2 showed comparable release profiles between C2 and C3 (ƒ2=94.2). This study shows that mucilage from the date fruit could potentially be used as a polymer in the formulation of controlled release metformin-loaded microbeads.
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    Date Mucilage as Co-Polymer in Metformin-loaded Microbeads for Controlled Release
    (Natural Product Research Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria, 2019) Akin-Ajani, O. D; Odeku O. A.; Babalola Y.
    The World Health Organization (WHO) has recognized the use of rectal preparations for certain indications in children as an alternative to parenteral. However, challenges of stability in tropical countries have limited its application. Furthermore, adverse effects arise in the use of some excipients in infants and neonates. In this study, paediatric paracetamol suppositories using two plant-derived fats - shea butter and dika fat - and their combination as suppository bases in comparison with cocoa butter were formulated. Shea butter and dika fat were purified and characterised using acid, iodine and saponification values, refractive index and relative density. Paracetamol suppositories were formulated by fusion method and evaluated using appearance, weight uniformity, melting point range, solidification point, crushing strength, disintegration time and dissolution test. Physicochemical properties showed shea butter and dika fat as stable with minimal susceptibility to oxidation with melting point ranges of 32 - 35C and 37 - 39C respectively. Base mixtures yielded melting point ranges of 32 - 39C. The suppositories had crushing strengths  31 N and disintegration times ranged between 3 - 21 min. Paracetamol release from the single bases ranked cocoa butter >dika fat > shea butter. Paediatric paracetamol suppositories using these plant-derived fats compared well with cocoa butter. Paracetamol suppositories with mixtures of either shea butter or dika fat with cocoa butter had superior release properties compared to cocoa butter alone. Thus, could serve as an alternative to cocoa butter in the formulation of suppositories.
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    Formulation of Diclofenac Sodium Emulsion Using Colocynthis Citrullus L. (Melon) Seed Oil
    (West African Postgraduate College of Pharmacists (WAPCP), 2019) Akin-Ajani, O. D.; Oluyemi T. T.; Odeku O. A
    Background: Melon seed obtained from the fruit of Colocynthis citrullus L. is widely used in Nigeria as a soup thickener. The seed has a high oil yield (42-57%) which has been largely unexplored as excipient in pharmaceutical formulations. Objectives: To evaluate melon seed oil as a drug carrier in emulsion using diclofenac as a model drug. Methods: Melon seed oil was extracted and the physicochemical properties were characterised. The emulsions were prepared using the traditional wet and dry gum methods, and all the emulsions were evaluated using viscosity measurements, creaming rate, and in-vitro drug release. Results: Melon seed oil had a pale yellow colour, with characteristic taste, and a neutral pH. Melon seed oil exhibited higher acid, saponification and ester values than castor oil but lower iodine value indicating an edible non-drying oil, unsusceptible to auto-oxidation. Both oils achieved a great degree of emulsification with globule size < 15mm μm. Emulsions of melon seed oil were generally less viscous with a higher degree of creaming compared to castor oil emulsions. Diclofenac emulsions prepared with melon seed oil, however, were more viscous and gave the highest release of diclofenac irrespective of the method of preparation. Only diclofenac emulsion prepared with melon seed oil using the wet gum method had > 70 % release within 45 minutes thus meeting the official specification. Conclusion: Melon seed oil functioned as a drug carrier for diclofenac. Thus, it will find application in pharmaceutical emulsions.
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    Formulation of Diclofenac Sodium Emulsion Using Colocynthis Citrullus L. (Melon) Seed Oil
    (2019) Akin-Ajani, O. D.; Oluyemi T. T.; Odeku O. A
    Background: Melon seed obtained from the fruit of Colocynthis citrullus L. is widely used in Nigeria as a soup thickener. The seed has a high oil yield (42-57%) which has been largely unexplored as excipient in pharmaceutical formulations. Objectives: To evaluate melon seed oil as a drug carrier in emulsion using diclofenac as a model drug. Methods: Melon seed oil was extracted and the physicochemical properties were characterised. The emulsions were prepared using the traditional wet and dry gum methods, and all the emulsions were evaluated using viscosity measurements, creaming rate, and in-vitro drug release. Results: Melon seed oil had a pale yellow colour, with characteristic taste, and a neutral pH. Melon seed oil exhibited higher acid, saponification and ester values than castor oil but lower iodine value indicating an edible non-drying oil, unsusceptible to auto-oxidation. Both oils achieved a great degree of emulsification with globule size < 15mm μm. Emulsions of melon seed oil were generally less viscous with a higher degree of creaming compared to castor oil emulsions. Diclofenac emulsions prepared with melon seed oil, however, were more viscous and gave the highest release of diclofenac irrespective of the method of preparation. Only diclofenac emulsion prepared with melon seed oil using the wet gum method had > 70 % release within 45 minutes thus meeting the official specification. Conclusion: Melon seed oil functioned as a drug carrier for diclofenac. Thus, it will find application in pharmaceutical emulsions.
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    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, O
    The 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 excipients
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    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 potatocornfonio, 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.
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    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. A
    Chrysophyllum 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 tablets
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    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 A
    The 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.
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    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. A
    Starches 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.