scholarly works Pharmaceutics and Industrial Pharmacy

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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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    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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    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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    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.
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    Formulation of floating metronidazole microspheres using cassava starch (manihot esculenta) as polymer
    (Springer Publications, 2017) Odeku, O. A; Aderogba, A. A.; Ajala, T. O.; Akin-Ajani, O. D.; Okunlola, A
    " Floating gastroretentive microspheres have been used to prolong the gastric residence time after oral administration and improve the local effect of metronidazole in the stomach in the treatment of peptic ulcer caused by Helicobacter pylori. In the present study, cassava starch, obtained from the tubers of Manihot esculenta has been pregelatinized and used as polymer in combination with sodium alginate for the formulation of floating gastroretentive metronidazole microspheres. Metronidazole microspheres were prepared by ionic gelation method using pregelatinized cassava starch and sodium alginate at different concentrations as polymers and calcium chloride (2% w/v) as chelating agent. Sodium bicarbonate (2% w/w) was used as gas releasing agent. Microspheres were characterized using the particle size, swelling index, floating lag time (FLT), total floating time and drug release properties. Spherical discrete microspheres with size ranging from 1.52 to 2.23 mm were obtained with FLT of less than 5min and drug entrapment efficiency of 42–60% w/w. The microsphere maintained buoyancy for over 19h and the microspheres provided controlled release of metronidazolefor up to 18h. Drug release from the microspheres, swelling index and buoyancy depended on the concentration of cassava starch in the polymer blend. Formulations containing high concentration of cassava starch showing shorter floating lag time and faster drug release. Thus, buoyancy and rate of drug release appeared to be modulated by the concentration of cassava starch in the polymer blend. The results showed that pregelatinized cassava could be useful in the formulation of floating gastroretentive metronidazole microspheres "