The aim of this study was to evaluate Detarium microcarpum gum (DMG) as polymer in formulated mucoadhesive albendazole tablets. FTIR studies were conducted to evaluate compatibility of DMG with albendazole. Mucoadhesive albendazole tablets were prepared by non-aqueous wet granulation technique using DMG alone (30%, 20% or 10%), in combination with carbopol (15%/15%) or carbopol alone (30%) respectively as polymers. Granules prepared were evaluated for flow rate, angle of repose, bulk and tapped density, particle size distribution, Hausner’s ratio and compressibility index. The prepared tablets were evaluated for thickness, diameter, hardness, weight uniformity, friability, drug content, dissolution, swelling studies and mucoadhesive strength. The uniformity of weight for the formulated tablets ranged from 591.1±0.011 to 601.6±0.001 mg while the drug content ranged from 98.6% to 101.3%. Tablet hardness ranged from 5.10±000 to 10.77±0.01 Kgf and friability was between 0.25±0.00 and 0.42±0.02%. The mucoadhesive strength ranged from 1.293 x 10-4 to 6.45 x 10-4. Post compression parameters were within acceptable limits. The cumulative drug release for formulations F1-F3 produced using DMG (38.52 to 54.45%) were significant improvement on that produced using carbopol (11.62%) and marketed product (8.21%). The produced tablets were stable after accelerated stability studies at 40oC and 75% relative humidity. FTIR studies indicated that DMG did not show any incompatibility with albendazole. DMG at concentration of 30%w/w could be used to produce mucoadhesive albendazole tablets with prolonged and sustained release characteristics comparable to those produced using standard polymer, carbopol.
Aims: This research was done to study the effects of types and concentrations of lubricants on the dissolution and disintegration profile of metronidazole tablets formulated using Sida acuta gum as a binder. Methodology: Sida acuta gum (SAG) was extracted from powdered dried leaves of Sida acuta. Metronidazole granules were produced by wet granulation technique using different concentrations (1 and 2%) of SAG as a binder and mixed with different concentrations (0.5, 1.0, and 1.5%) of magnesium stearate (MS) or sodium lauryl sulphate (SLS) as a lubricant. The granules/lubricant -mix was compressed into tablets and evaluated for hardness, weight uniformity, drug content, disintegration time, friability and in vitro drug release. Results: The hardness for the tablets was from 4.08 to 7.97 Kgf. The friability was from 0.02±0.45 to 3.40±0.43%. Tablets from formulations A1-A3, B2, and B3 failed the friability test. Formulations prepared with 1% SAG were more friable than those formulated with 2% SAG. Disintegration time for formulations A1-A3 (1% SAG + MS) ranged from 19.07 to 63.5 min, while that of A4-A6 (2% SAG + MS) was from 39.06 to 81.48 min. Formulations B1-B3 (1% SAG + SLS) had disintegration time that ranged from 4.22 to 6.8 min while that of B4-B6 (2% SAG + SLS) was from 9.35 to 15.90 min. The % drug release at 60 min for formulations that contained SAG and MS was 76.60-104.28% and SAG and SLS was 99.89-101.35% Conclusion: Metronidazole tablets formulated using SLS as lubricant disintegrated faster than those formulated using magnesium stearate as lubricant. Percentage drug release from tablets containing SLS was slightly higher than those that contained magnesium stearate. Higher concentrations of the lubricants produced softer tablets.
Polysaccharide gums derived from Grewia spp, a medicinal plant of the Malvaceae family are reportedly useful as excipients in different pharmaceutical formulations. In this study, we investigated and evaluated the emulsifying property of this gum extract by comparing with acacia gum as an emulsifying agent in the formulation of metronidazole emulsion. First, Grewia gum was extracted from pods and characterized. Six formulations of metronidazole emulsion were then prepared from Grewia or acacia gum. Next, the emulsions were evaluated and observed for creaming index, phase separation, viscosity, pH and organoleptic properties. Study showed emulsion from Grewia gum to exhibit lower creaming index than those of acacia or a combination of both. They however showed higher viscosity than those from acacia or combination of both gums with no apparent change(s) in colour, odour and appearance throughout the period of storage. Also, the pH value of acacia emulsions proved acidic just as the Grewia gum. The gum showed a pH of 6.15 with excellent flow property. The study showed the physiochemical properties of the gum to be good and employable in the pharmaceutical industry as a stabilizer, thickener especially when high viscosity is required. Further studies that corroborate this work is recommended.
Herbal plants contain substances of medicinal values or precursors for synthesis of important drugs, however, not much have been done in terms of standardization and effective delivery system. Various routes can be employed to deliver herbs, but the topical route is the safest. In this study, aqueous and ethanolic extractions of Andrographis paniculata were carried out. Antimicrobial screening of the extract before and after incorporation into cream base was carried out using standard antimicrobial agents as positive control. Formulated creams were evaluated for organoleptic properties, pH, spreadability, viscosity and stability. Staphylococcus aureus and Candida albicans were used for the sensitivity studies. Percentage yield for ethanolic and aqueous extracts were 17.5%w/w and 13.33%w/w respectively. Both microbes were sensitive to pure ethanolic extract and creams formulated from ethanolic extract, but resistant to aqueous extract. Zones of inhibition for the ethanolic extract ranged from 7.33 ± 0.58 mm to 14.00 ± 0.00 mm (Candida albicans) and 6.00 ± 1.00 mm to 12.33 ± 0.58 mm (Staphylococcus aureus). Minimum Inhibitory Concentrations, MICs, were 25 mg/mL and 200 mg/mL for Candida albicans and Staphylococcus aureus respectively. The MIC for the formulated cream (15% w/w) was 150 mg/mL for both organisms. The pH of formulated creams ranged from 5.54 to 6.84; the viscosity, 18,800 to 60,500 mPas. The spreadability values were between 37.5 ± 0 and 75.0 ± 0.2 g.cm/s. All formulated creams were stable. Thus herbal creams formulated from Andrographis paniculata ethanolic extract retained the antimicrobial properties of the extract and as such can be applied topically for the treatment of skin diseases involving these microorganisms.
The major reason for development of new drug delivery system is based largely on promoting therapeutic outcome and minimizing toxic effect of a drug by increasing the amount and persistence of a drug in target cells areas, while reducing exposure of the drug to non-target cells. In this study, Grewia spp gum obtained from Grewia spp pods was extracted and used as binder and release retardant in the formulation of controlled release theophylline tablets. A total of six (6) batches of the tablets were produced with carried concentrations of the test gum by wet granulation technique. To produce the tablets, various granules were formulated via wet granulation and characterized by measuring flow and packing properties. Granules with adequate flow properties were compressed to tablets. Tablets so formed were evaluated for hardness, percentage friability, weight variability and drug release profiles. The percentage yield was 18.64% and the pH of the test gum was 6.15. The angle of repose, bulk density, tapped density and Carr’s index of the formulated granules ranged from 22.48±0.00 to 24.90±0.00˚, 0.53±0.03 to 0.67±0.00g/ml, 0.67±0.02 to 0.82±0.00g/ml and 18.29±0.00 to 22.06±0.26% respectively. Resultant tablets hardness values of 3.69±0.45 to 13.39±0.65kgF and friability percentage of 0.40± 0.00 to 2.56%±0.01% were also obtained. The formulated theophylline granules showed good flow properties and compressibility. Thus, the study revealed that the test gum has comparable binding effect to Eudragit RS 100 at a ratio of 2:1. We recommend further studies to rule out any interaction of Grewia spp gum with theophylline in controlled release theophylline tablets.
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