Browsing by Author "Belete, Anteneh (PhD)"

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    Assessment of Non-Sterile Pharmaceutical Compounding Practices Among Selected Community and Hospital Pharmacies in Addis Ababa, Ethiopia
    (Addis Ababa University, 2017-06) Seid, Sofia; G/Mariam, Tsige(Professor); Belete, Anteneh (PhD)
    Background: The drug products available in the market are mostly ready-made finished drug products. These drugs should be manufactured in pharmaceutical industries using the standard on Good Manufacturing Practice (GMP). But, it is a common practice to prepare topical preparations in compounding laboratories in premises like hospital pharmacies and community pharmacies in order to fulfill the special needs of individual patients. These preparations, like other finished drug products, should fulfill efficacy, safety, and quality parameters. This is achieved by adherence to the established standards that guide the preparation of compounded pharmaceutical preparations. Objective: To assess the practices of non-sterile pharmaceutical compounding in selected community and hospital pharmacies in Addis Ababa. Methods: A descriptive cross-sectional study supported by qualitative study was conducted to assess the practices of non-sterile pharmaceutical compounding in community and hospital pharmacies in Addis Ababa from April 1, 2016 to May 15, 2016. The study was done in 42 community pharmacies and 3 hospital pharmacies. Results: The study revealed that the most commonly prescribed and compounded non-sterile pharmaceutical formulations in the community and hospital pharmacies in Addis Ababa were dermatological creams and ointments. Except for one community pharmacy, no community and hospital pharmacy provided on-the-job training to the pharmacy personnel involved in compounding. The compounding personnel in 41(97.6%) of the community and 2 of the hospital pharmacies were not familiar with the non-sterile pharmaceutical compounding laboratory standards developed by DACA in 2002.Twenty (47.6%) of the community pharmacies and 1 of the hospital pharmacies had no suitable place for compounding. All of the assessed hospital pharmacies had dedicated place for compounding and only authorized personnel is allowed in the specified room but 20 (47.6 %) of the community pharmacies had a compounding area with other works performed in that area. All of the hospital pharmacies and 39 (92.9%) of the community pharmacies had adequate potable water. The compounding area was maintained in a clean and sanitary condition in 25 (59.5 %) of the community pharmacies and all of the hospital pharmacies. ix Standard operating procedures were not maintained in 41 (97.6%) of the community pharmacies and 1 of the hospital pharmacies. No community and hospital pharmacy created a master formulation record the first time before compounding new preparation. The equipment and materials required by the national regulatory authority for the extemporaneous preparation were not fulfilled in 18 (42.2%) of the community pharmacies and in 1 of the hospital pharmacies. Sixteen (38%) of the community pharmacies had no compounding record at all and 26 (62%) of the community pharmacies had compounding records which only contained the name and the strength of the compounded preparations. There were containers and closures that were not suitable for the preparation compounded in 18 (42.9%) of the community pharmacies and 1 of the hospital pharmacies. Conclusions: The study revealed that, both the community and the hospital pharmacies did not fulfill most of the requirements set by the regulatory authority. However, the hospital pharmacies were found to be better than the community pharmacies in some of the requirements such as labeling of finished preparations, documentation, availability of equipments and compounding room dedication. As per the findings of this study, only one community pharmacy is practicing most of the standard requirements set for non-sterile pharmaceutical compounding. The major limiting factors for the implementation of the standard requirements set was identified to be lack of awareness on the standard set for non-sterile pharmaceutical compounding laboratories; the limited number of demands for the service; lack of on-the-job training and follow up from regulatory body and other stakeholders. Recommendations: The non-sterile pharmaceutical compounding service has to be regulated and inspected strictly. The standards of good compounding laboratories developed by the regulatory authority should be cascaded and popularized to the professionals working in the community and hospital pharmacies. On-the-job training has to be given for the personnel involved in non-sterile pharmaceutical compounding. Further research should be done on the quality of non-sterile pharmaceutical compounding practices in other parts of the country. Key words: Community pharmacy, hospital pharmacy, non-sterile pharmaceutical compounding Personnel qualification, compounding facility, equipment, documentation, quality control, Addis Ababa
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    Evaluation of Taro Boloso-I Native (Colocasia esculenta Cultivar) Starch as Disintegrant and Its Pre-Gelatinized form as Direct Compression Diluent in Paracetamol Tablets
    (Addis Ababa University, 2016-01) Balcha, Tamrat; Belete, Anteneh (PhD); Mary Joseph, Nisha(PhD)
    Taro Boloso-I is a new variety of Colocasia esculenta (L. Schott) officially released from Areka Agricultural Research Center, Areka, Ethiopia. Its cultivation out yields 67% more than a previously reported variety (Godare) in Ethiopia. It contains 85.65 ± 0.07% of carbohydrate on dry basis and higher gross energy than the existing cultivars of taro reflecting its difference from the preexisting varieties of taro. The aim of this study was to isolate, characterize the starch from this plant and evaluate its potential applications. It was also to evaluate the tablet disintegrant properties and direct compressibility of the pre-gelatinized form using paracetamol as a model drug. Starch was extracted from the C. esculenta by using saline solution (0.1N) and sodium hydroxide (0.03 N). Various 13 experimental methods were applied for characterization of the starch. Central composite design was used for optimization of the levels and hence the responses. Yield of starch from Taro Boloso-I on dry weight basis was 83.5 ± 1.6%. The native Taro Boloso-I starch (NTB1S) was characterized by lower amylose to amylopectin ratio (20.7 ± 1.8% to 77.3 ± 2.1%, w/w) higher onset, peak and endset temperatures of gelatinization than potato starch. Its granules were found to exhibit polyhedral/angular shape and A-type polymorphism comprising powder of poor flow. In all of these properties, Taro Boloso-I starch not only significantly differs from the previously reported taro varieties in Ethiopia but also shares more of cereal starches (rice starch) than the tuber starches. Paracetamol tablet (350mg) prepared by wet granulation using NTB1S (9.80%) as disintegrant and compression force of 15kN had hardness of 117.1 ± 4.93N, friability of 0.159 ± 0.02% and disintegration time of 1.31 ± 0.02 min. The hardness, friability and balance between binding and disintegration were better than potato starch, 58.1 ± 2.57 N, 1.01 ± 0.06% and 46.4 ± 4, respectively. Moreover, the tablets fulfill the disintegrant time requirements for fast dissolving tablets. The modified (optimized) Taro Boloso-I starch (PGTB1S) has comparable flow property but higher compressibility and compactibility. If used as a disintegrant in paracetamol tablets, NTB1S can result not only in better hardness and friability than the corresponding tablets with potato starch but also a kind of fast dissolving tablet. Also it was revealed that PGTB1S can be used as efficient direct compression diluent with magnesium stearate tolerance of 0.5%. Its dilution potential was also better than Starch 1500®. Key words: Starch, tablet, compression, gelatinization, disintegrant, Taro Boloso-I, Kawakita, Heckel
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    Formulation, In-vitro Evaluation and Optimization of Directly Compressible Glibenclamide Orodispersible Tablets
    (Addis Ababa University, 2016-12) Bayu, Solomon; Gebre-Mariam, Tsige(Professor); Belete, Anteneh (PhD)
    Glibenclamide (GLM) is an orally active hypoglycaemic agent which belongs to sulphonylurea group. It controls blood glucose level primarily acting on beta cells, which are the insulinproducing cells of pancreatic islet tissue to increase their sensitivity to glucose and to stimulate the production and release of more insulin. It is used for the treatment of noninsulin dependent diabetes mellitus (NIDDM). It shows poor absorption and low bioavailability from a conventional tablet, which is attributed to its poor water solubility. In this study crospovidone and sodium bicarbonateas disintegration agent and dissolution enhancer, respectively, were used to formulate and optimize orodispersible tablets (ODT) of GLM in order to minimize absorption lag time, hasten the onset of action, improve bioavailability and compliance. Tablets were prepared by direct compression technique at different levels of compression force and evaluated for physicochemical properties. Those formulations of tablets which showed better performance were optimized using central composite design. The optimized tablets were compared for their release propertieswith marketed products. The results showed simultaneous optimization of the dependent variables offered the most desirable representative optimum formulation, within the common optimum section, with hardness of 5.75 Kg/cm2, friability of 0.2%, wetting time of 16.5 sec, disintegration time of 9.4 sec and cumulative drug release of 98.0%in 30min at concentration of 9.73mg crospovidone, 30.33mg sodium bicarbonate and 16.3KN compression force. The validity of obtained optimal point was confirmed by the low magnitude of percent prediction errors of the response variables. Comparative study of the cumulative drug release of GLM within 60 min between marketed conventional tablet of GLM (Daonil®) and the optimized ODT with the model independent method revealed that there was a significant difference between the two formulations with a dissimilarity factor ƒ1value of 73.25% and similarity factor ƒ2value of 9.01%.Thus, the results of this study showed ODT of GLM possess significantly rapid disintegration and enhanced dissolution profiles. Keywords:Glibenclamide, Orodispersible tablets, crospovidone, Sodium bicarbonate, Direct compression, central composite design, Optimization
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    Isolation, Physicochemical Characterization, and Evaluation of Triticum Decocum (Ethiopian Oat) Starch As Binder and Disintegrant in Paracetamol Tablets
    (Addis Ababa University, 2014-06) Mosisa, Balisa; Gebre-Mariam, Tsige(Professor); Belete, Anteneh (PhD)
    Background: Oat is one of cereal grain which has about 10-15 species of true grasses (family Poaceae). Even though, Avena sativa L (common oat) is the most important one among cultivated oat in most parts of the globe; four other species are grown as crops of minor or regional importance of which Triticum decocum which is cultivated in Ethiopia is one. Triticum decocum is a half-weed, half-crop with erect stems which are small and fairly stiff with equilateral panicles and medium size, just very drooping. Objective: The main purpose of current work is to study the physicochemical properties of Triticum decocum starch, and evaluate its binding and disintegrating properties in paracetamol tablets. Statement of the problem: With the recent global renewed interest of natural polymers for industrial consumptions, the demand for the starch is expected to hit 230 million metric tons per year by 2015 globally. Current starch demand of Ethiopia which is more than 400 tons per year is imported from other countries. The need is escalating with industrial advancement. To cope up with these demands, potential endogenous sources of starches including, Triticum decocum starch, should be considered if being economical and sustainable supply is anticipated. Methods: Different methods previously described elsewhere were used to achieve the above objective with slight modification as its importance. Result and Discussion: The proximate composition of the starch on dry weight basis was found to be 0.23 % ash, 0.26 % protein, 1.54 % fat and 56.31 % starch. The total amylose content was 28.4 % with 20.11% apparent amylose and 29.19% lipid complexed amylose. SEM showed oval and spherical shaped granules. The particle size distributions of the starch showed monomodal normal particle size distribution with the average volumetric particle diameters being about 23.03μm, and specific surface area 0.7186 m2/g. XRD showed a pattern that is typical of A-type with a distinctive maximum peak at around 17° 2θ. At all relative humidities, its water sorption properties resemble that of Zea mays starch. It has unique swelling power and solubility in water at different temperature. Viscosity curves of 10% starch paste showed a peak viscosity of 1926cP. Its cold paste viscosity and hot paste viscosity were 4236cP and 1720 cP, respectively. The breakdown and set back of Triticum decocum starch were 206 and 2647cP, respectively. II Powder mix of the starch with paracetamol has poor flow and compressibility properties. But after wet granulation, the granules have good flow and compressibility properties. Tablet crushing strengths, friabilities, disintegration times and dissolution profiles results had shown promising results. Conclusion and Recommendation Based on the above results, Triticum decocum starch can be used both as a binding agent and disintegrant. It has a better binding ability than Zea mays starch, giving tablets of higher strength and less friability. However, tablets containing Triticum decocum starch disintegrate slightly more slowly. Different methods of extraction, modifications, and other use evaluations had better conducted on the starch. Key Words: Triticum decocum, physico-chemical properties, chemical composition, flow and compressibility.
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    Physicochemical Characterization of Acid Modified Dioscorea Starch and its Evaluation as Directly Compressible Excipient And Disintegrant in Tablet Formulations
    (Addis Ababa University, 2014-05) Tessema, Bilal; Gebre-Mariam, Tsige(Professor); Belete, Anteneh (PhD)
    Starch is one of the most important and flexible food ingredients possessing value added attributes for innumerable industrial applications. Dioscorea abyssinica (Fam. Dioscoreaceae) is a potential source of starch for large scale production in Ethiopia. Starch is usually modified either chemically or physically to augment its convenience for industrial use. The choice of excipients remains a critical factor in pharmaceutical formulations. Acid modified dioscorea starch (AMDS) has been prepared by hydrolyzing with 6% (w/w) HCl solution at ambient conditions and evaluated as a multifunctional excipient i.e, its direct compressibility and disintegrant effect in tablet formulations. Some of the physicochemical properties of AMDS such as; densities, flow, swelling power, percentage solubility, moisture sorption, and compactability were determined and compared to those of native dioscorea starch (NDS) and Starch 1500®. The comparative direct compressibility and disintegrant effects of these starches in tablet formulations were also studied using paracetamol as a model drug and the resulting tablets were evaluated for their physico-mechanical properties. The results indicated that both swelling power and percent solubility of the starches were found to increase with increase in temperature; AMDS showed higher percent solubility 68.53%. Spray dried AMDS exhibited free flowing property with 21.37 ± 1.39° angle of repose and 13.24 ± 0.76 g/sec flow rate. The compaction study revealed that the tensile strength and disintegration time of the compact increases and percent friability decreases as compression force increases. The lubricant sensitivity test showed that spray dried AMDS and Starch 1500® tablets could be used with acceptable tablet characteristics up to 1% and 0.5% of magnesium stearate concentration, respectively. With regard to dilution potential, the spray dried AMDS could accommodate up to 40% paracetamol with acceptable criteria. The results also indicated that tablets prepared with AMDS and Starch 1500® exhibited comparable characteristics. An increase in concentration of AMDS and Starch 1500® as disintegrant provided tablets with increased crushing strength and decreased disintegration time and friability. The dissolution studies of the paracetamol tablets showed that the release of the drug was within acceptable range (quantity dissolved in 30 min ≥ 80%). Thus, it can be concluded that AMDS can be used as an alternative directly compressible excipient and disintegrant in tablet formulations. Keywords: Dioscorea starch; acid modified starch; spray drying; tablet; directly compressible excipient; disintegrant; lubricant sensitivity, dilution potential, D. abyssinica.
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    Physicochemical Characterization of Plectranthus Edulis (Ethiopian Potato) Starch and its Evaluation as a Disintegrant In Paracetamol Tablet Formulations
    (Addis Ababa University, 2015-01) Assefa, Anteneh; Gebre-Mariam, Tsige(Professor); Belete, Anteneh (PhD)
    Plectranthus edulis, Vatke (P. edulis) [fam., Lamiaceae], is an ancient Ethiopian tuber crop and one of the traditional root crops indigenous to Ethiopia. It is a large (~1m high) and an erect herbaceous plant with hirsute, decumbent and glandular stems, and leaves of lanceolate to elliptic and root of swollen nodes which produces edible underground potato-like tubers. Starch from the tubers of P. edulis was isolated using 0.075% (w/v) sodium metabisulphite and it gave a yield of about 80.4% on dry weight basis. The starch was examined for the chemical composition, amylose content, physicochemical properties and evaluated for its applicability as a pharmaceutical disintegrant in tablet formulations. The proximate composition of the starch on dry weight basis was found to be 0.14% ash, 0.21% lipid, 0.43% protein, and 99.22% starch. The amylose content was 30.6%. Its true density, moisture content and pH values were 1.47 g/ml, 11.2% and 6.6, respectively. Scanning electron microscopy (SEM) of the starch granules showed characteristic morphology that was oblong (elliptical) with some oval in shapes. The starch showed a monomodal normal granule size distribution with a mean particle size of 36.2 μm and specific surface area of 0.302 m2/g. The DSC thermograms of P. edulis starch exhibited higher T0 (69.2 oC), Tp (74.3 oC) and Te (83.3 oC) values than potato starch. X-Ray Diffraction pattern of the starch was typical B-type with a distinctive maximum peak at 17.5o 2θ. The FTIR spectral features of the starches show characteristic peaks at 3325, 2930, 1462, 1377, 1155, 860 cm-1 attributed to various stretching and bending vibrations of O–H, C–H, C–O, or C–O–C bonds for starches. It has typical swelling power, solubility and moisture sorption pattern at different conditions of temp and relative humidities. It possesses higher values relative to potato starch, but its solubility values are lower than potato starch at all temp studied. The comparative disintegrant abilities of these starches in paracetamol tablet formulations prepared by wet granulation method were studied. The granules prepared with the starches (P. edulis starch and potato starch) at different disintegrant concentrations were characterized for particle size distribution and flow properties. The excellent flow property of the granules was manifested by the weight uniformity of tablets. The crushing strength, friability, disintegration time, and dissolution rate of the tablets were studied using standard methods. The results II indicated that the properties of paracetamol tablets formulated with both starches as disintegrants were affected by their concentration and the compression force (CF). Increasing the concentration of the starches reduced the crushing strength and disintegration time of the tablets and increased the percent friability of the tablets. Conversely, increasing the CF increased crushing strength and disintegration time of the tablets and reduced the percent friability of tablets. The results have shown that P. edulis starch has favorably competed with potato starch as a disintegrant in the paracetamol tablet formulations. The optimization study of P. edulis starch as a disintegrant in paracetamol tablets was carried out by selecting the CF (X1) and P. edulis starch concentration (X2) as factors, and crushing strength, percent friability and disintegration time as response variables; and employing central composite statistical design (CCD). Design-Expert 8.0.7.1 software was utilized in the experimental design, statistical analysis and optimization process. Using the software several statistical parameters were compared, quadratic model for all the three responses were selected, and the adequacy of the models were checked by analysis of variance (ANOVA). The ANOVA results revealed that quadratic model is significant for the terms (factors) and responses studied. A quadratic mathematical model was developed; and the optimum formulation of paracetamol tablet containing P. edulis starch as a disintegrant was obtained by simultaneous optimization of the responses. From the optimum region, a CF (X1) of 14.40 KN and a disintegrant concentration (X2) of 5.96% was selected to check the validity and predictability of the design. The predicted values of crushing strength, friability and disintegration time of the formulation at the aforementioned levels of factors closely matched with the results of actual experimentation. Thus, the optimization technique provided the optimum formulation of paracetamol tablet containing P. edulis starch as a disintegrant. The results of the physicochemical characterization of P. edulis starch, as well as the comparative and optimization study of the starch as a disintegrant in the tablet formulations indicate that P. edulis can be used as an alternative source of starch for applications in the pharmaceutical industry. Keywords: Plectranthus edulis, Starch, Differential scanning calorimetry, Scanning electron microscopy, X-ray diffraction, Tablet disintegrant, Optimization, Central Composite Design