Evaluation of the Direct Compression Properties of Microcrystalline Cellulose Obtained from Cassava Fermentation Waste in Paracetamol Tablet Formulations

Background: Natural materials have gained a lot of significance in the field of drug delivery because of their cost effectiveness and ready availability.Purpose: The study aimed at evaluating the direct compression property of microcrystalline cellulose from cassava fermentation waste in directly compressed paracetamol tablet formulations.Methods: Alkali delignification of the dried cassava fermentation fibres, followed by bleaching and acid depolymerisation was employed in the extraction of α-cellulose and conversion to microcrystalline cellulose (MCC). The MCC obtained and Avicel® were used at different concentrations (5.0-15 %w/w) to formulate batches of paracetamol tablets by directed compression. A comparative evaluation of the formulated paracetamol granules and tablets properties were undertaken.Results: The paracetamol granules formulated showed good flowability with Hausner’s ratios of 1.15-1.25, Carr’s indices of 13.10-20.00 % and angles of repose ≤ 34.41°. The formulated tablets showed good hardness (> 5.0 kgf) and disintegration time within 10 min. Only tablets containing 5.0 and 7.5 %w/w of the test MCC failed the BP dissolution test specification for tablets which stipulates that at least 70 % of the drug should be in solution after 30 min.Conclusion: This study has shown that the extracted MCC has direct compression ability evidenced in the mechanical strength of the formulated paracetamol tablets. The tablet properties of the formulated paracetamol tablets revealed pharmaceutically acceptable tablets though they were not comparable with Avicel® at all concentrations and the MCC may serve as an alternative local source for direct compression excipient. Keywords: Cassava, microcrystalline cellulose, direct compression, paracetamol, tablet

Modulatory effect of high molecular weight polyethylene glycols on drug release from ibuprofen matrix tablets

The work aim at investigating the channeling or modulatory effects of polyethylene glycol (PEG) (MW 4000 and 6000) on drug release from ibuprofen sustained release formulation. Different batches of ibuprofen matrix granules and tablet were prepared by melt granulation using different concentrations of carnauba wax and PEG at different ratios. The granule flow properties and various tablets parameters were evaluated using standard procedures. Drug release kinetics and mechanisms from the tablets were investigated as well as DSC and FTIR drug-excipients compatibility. The granules showed increasingly close packing with increase in the amounts of PEG incorporated. All the tablets did not meet compendial specifications with regard to crushing strength and friability. The release rate and extent of release were found to be influenced by the amount of PEG used as well as the carnauba wax concentration. PEG combination of equal amounts produced the highest release of 91 % in the formulation prepared with 12.20 %w/w of carnauba wax while a 1:2 combination in tablets prepared with 24.40 %w/w of carnauba wax gave a maximum drug release of 83 %. Drug release kinetic and mechanism were most consistent with the Higuchi model hence the release was diffusion mediated. DSC and FTIR studies showed no interactions between ibuprofen and the excipients. Carnauba wax-PEG system can be used successfully as a matrix former to sustain the release of ibuprofen for over 6 h. The studies indicate that the proper balance between a matrix former and a channeling agent can produce a desired drug dissolution profile.Keywords: carnauba wax, PEG, granulation, release modifier, ibuprofen, tablet

The effects of a blend of croscarmellose sodium and microcrystalline cellulose on the brittle fracture tendency of paracetamol tablets

Background: Capping and lamination are major problems encountered in tablet production and they are indicators of the brittle fracture tendency of a tablet formulation.Objective: The study aimed at determining the effect of a blend of two super-disintegrants on the brittle fracture tendency of paracetamol tablet.Methods: Batches of paracetamol granules and tablets (B1-B5) were prepared by wet granulation using a blend of croscarmellose sodium and microcrystalline cellulose (MCC) at different ratios. The formulated granules’ pre- and post-compression parameters such as weight uniformity, dimensions, friability, crushing strength disintegration time, brittle fracture index (BFI) and dissolution studies were evaluated.Results: Granules of the different batches of the formulations exhibited excellent flow properties. All of the formulated tablets met official compendial specifications for tablets except batch B4 tablets with tablet friability value of 1.35 %. The BFI of the paracetamol tablets with MCC alone (B5) had the lowest value (0.420), closely followed by the B3 tablets value (0.421) with 2 parts MCC and 1 part croscarmellose sodium. The highest BFI value of 0.582 was obtained from the B1 batch of tablets containing equal parts of the superdisintegrants.Conclusion: The blend of superdisintegrants adversely affected the brittle fracture tendency of the paracetamol tablets by increasing the BFI of the tablets though to a lesser degree. The choice of two or more superdisintegrants in the formulation of fast disintegrating tablets should be undertaken with a careful study to avoid producing tablets that are prone to capping or lamination during tablet-die ejection.Keywords: Superdisintegrants, Blend, Tablets properties, BF

Transdermal delivery of bovine serum albumin using snail mucin

The study aimed at evaluating the bioadhesion properties and penetration enhancing effect of mucin-based bovine serum albumin (BSA) transdermal patches. Mucin was extracted from the giant African snail Archachatina maginata by differential precipitation with acetone and alum. Various batches of BSA loaded transdermal film patches were prepared with the precipitated mucin and varying volumes (0, 0.2 and 0.5 mL) of polyethylene glycol (PEG) as plasticizer. Prepared patches were evaluated for weight uniformity, patch thickness, folding endurance, moisture content and uptake, bioadhesion, drug content and in vitro and ex vivo diffusion studies. Differential scanning calorimetry analysis showed no interaction between BSA and mucin. Mean weight range from 0.11±0.02 to 0.13±0.05 g, moisture content (32 %) and moisture uptake was highest with patches prepared with acetone-precipitated mucin (up to 129 %) and decreased as PEG concentration increased. All the patches showed bioadhesion values between 1.70 - 1.98 g/sec. Drug diffusion across treated rat skin was 47 % after 12 h from patches prepared from acetone-precipitated mucin. Thus, snail mucin showed promise as a transdermal drug delivery base in the formulation of BSA patches because of its bioadhesion property and penetration enhancing effect.Keywords: Bioadhesion, drug diffusion, proteins, mucin, transdermal deliver

An investigation of the direct compression properties of pre-gelatinized African bitter yam and cassava starches in acetylsalicylic acid tablet formulations

The direct compression ability of pre-gelatinized African bitter yam and cassava starches in acetylsalicylic acid tablet formulation was investigated. Starches from the African bitter yam and cassava tubers were extracted following standard procedures. The starch powders were subjected to some physicochemical evaluations and pre-gelatinized. Batches of acetylsalicylic acid granules and tablets were formulated with the native and pregelatinized forms of both the test and maize starches and microcrystalline cellulose at 5.0 and 10 %w/w by direct compression. Granules were evaluated for their flow properties and drug-excipient compatibility using DSC and FTIR while the tablets were investigated for their tablet parameters. The extracted starches were off-white to white in colour, insoluble in water, smooth in texture with particle sizes ranging from 5.0-10 μm that are oval to elliptical in shapes. The powders showed a swelling capacity ≤ 2.15, hydration capacity ≥ 1.20 and a moisture content ≤ 14.3 %. The granules exhibited good to fair flowability. Only tablets formulated with 10 %w/w of the pre-gelatinized starches and MCC met compendial requirements in their crushing strengths and friability. All the tablets disintegrated within 15 min with the pre-gelatinized cassava starches giving the shortest times of < 1.0 min. The 10 %w/w pre-gelatinized starches tablets compared favourably with MCC in their drug release profiles. Compatibility studies revealed no interaction between drug and excipients. The study show that the pre-gelatinized test starches compared favourably with MCC, a known direct compression excipient in their direct compression ability and drug release profiles especially at a concentration of 10 %w/w.Keywords: bitter yam, cassava, starches, pre-gelatinized, drug formulatio

Physicochemical Characterization of Sus scrofa domesticus Fat and a Preliminary Evaluation of its Potential as a Matrix Former in Ibuprofen Granules

Background: There is an increasing interest and search for local and natural sources as active pharmaceutical excipients.Purpose: The study aimed at investigating the physicochemical characteristics of Sus scrofa domesticus (SSD) fat and its potential as a matrix former in ibuprofen granule formulations.Methods: SSD fat was extracted from the domestic pig by wet rendering and purified. The fat was characterized for its organoleptic and physicochemical properties and used in the formulation of batches of ibuprofen granules by melt granulation using varying concentrations (5.0-15%w/w). Conventional granules were formed with maize starch (15%w/w) for control. Formulated granules were evaluated for flow properties, encapsulated in hard gelatin capsules and subjected to in-vitro drug release studies.Results: SSD fat was snow white in colour. Soluble in organic solvents but insoluble in water. pH of the fat was 7.4, viscosity (147.4 millipascal), peroxide value (11.0 meq/kg), acid value (3.4) and saponification value (196.3). Granules formulated with SSD fat exhibited poor flowability and their dissolution profiles showed retardation in ibuprofen release with increase in fat concentrations. Granules formulated with 5.0 and 10%w/w of the fat exhibited 43 and 27% ibuprofen release within 4 h while the conventional granules showed a drug release of 98% within 1.0 h.Conclusion: The physicochemical properties of SSD fat was found to possess favourable potential properties relevant in the formulation of a drug delivery system. The retardation of ibuprofen release from the granules showed that SSD fat has a potential application as a matrix former in controlled release formulation. Keywords: Sus scrofa domesticus, ibuprofen, matrix granules, dissolution profile

Influence of Incorporation of Pleurotus tuber-regium Powder on the Release Characteristics of Acetaminophen Tablets formed with certain Acrylate Methacrylate Copolymers as Binders

This study investigated the effects of incorporation of Pleurotus tuber-reguim powder on the release profiles of acetaminophen tablets. Pleurotus tuber-reguim powder was prepared from the mushroom sclerotium. The powdered sclerotia was bleached with 3.5% w/v sodium hypochlorite solution, slurred with ethanol, washed with water and dried at 50°C for 24 h. Using wet granulation technique, varying concentrations of the fine powder (0-25% w/w) were used intra- and extra-granularly to prepare various batches of acetaminophen tablets with 5% w/v Eudragit RL-100 or RS PO as binder. The tablets were evaluated for hardness, friability, disintegration and dissolution. The tablets formed hard compact with acceptable hardness values ranging from 5.0-9.7 kp which decreased with increasing concentration of P. tuber-regium powder. Only the batches of tablets without disintegrants met the official specification for friability with values ≥ 0.69 %. Pleurotus tuber-regium powder inclusion lowered the disintegration times of the matrix tablets with increasing concentrations. There was marked increase in the release of the drug from the matrix tablet with increase in the concentrations of the P. tuber-regium powder irrespective of the mode of disintegrant incorporation or polymer type. The intra-granular incorporated batches of tablets exhibited a higher drug release within 6 h when compared with the extra-granular incorporated tablets. P. tuber-regium powder serving as a swelling agent when incorporated intragranularly in matrix tablet system has the potential application for modulating or enhancing drug release at appropriate concentrations.Keywords: P. tuber-regium, excipients, disintegrants incorporation, drug releas

Evaluation of Dacryodes edulis (Burseraceae) exudate as a binding agent in paracetamol matrix tablet formulation

The binding ability of the stem bark exudate of Dacryodes edulis (Buseraceae) in paracetamol matrix tablet formulation was compared with that of Eudragit L-100. Crude exudates were purified by differential precipitation with water in acetone and petroleum ether and air-dried. Varying concentrations (1-10 %w/v) of the purified exudate or Eudragit L-100 were dissolved in acetone and used to form paracetamol matrix granules while 15 % w/v maize starch was used to form conventional granules by wet granulation. Drug excipient compatibility was carried out and the granules compressed into tablets. Tablet properties were evaluated and the data analyzed statistically using the student t-test (p < 0.05). Results showed a 71 % yield of the purified exudate. The exudate functioned perfectly as binder in the formulation of tablets at concentrations > 2.5 %w/v and compared favourably with Eudragit L-100. Tablets formed did not disintegrate within 15 min except for those formed with maize starch mucilage. The dissolution data fitted into the Higuchi equation with r2-values ≥ 0.95. Dacroydes edulis exudate extended the release profile of paracetamol up to 70 % within 5 h.Keywords: Dacroydes edulis, exudate, binder, Eudragit L-100, tablet

Some Physical Properties of Vernonia amygdalina and Garcinia kola Microspheres Prepared with High Molecular Weight Polyethylene Glycols

The effect of polymer concentrations on some of the physicochemical properties of Vernonia amygdalina (Linn) and Garcinia kola (Heckel) extracts loaded microspheres was evaluated. Microspheres of the aqueous extracts was prepared by emulsion solvent evaporation using polyethylene glycol (PEG) mixtures of molecular weight 4000 and 6000 at different ratios of 1:0, 0:1, 1:1, 1:2 and 2:1 while the amounts of the extracts incorporated was constant for all ratios. The microspheres were evaluated for their particles sizes, yield, flavonoid content, loading efficiency, moisture loss and flow properties. In-vitro release studies were carried out by monitoring flavonoid release rate from the microspheres. The microspheres were spherical and uniformly shaped and exhibited good flow characteristics. Their size range, yield, loading efficiency, moisture loss and flavonoid content were 76 - 83 \u3bcm, 49 - 76 %, 47 - 82 %, 2.18 - 4.60 % and 17.10 - 23.80 mg%, respectively for V. amygdalina and 144 - 160 \u3bcm, 50 - 68 %, 51 - 68 %, 3.00 - 4.41 % and 20.00 - 28.70 mg%, respectively for G. kola. Flavonoids release from the microsphere was up to 90 % within 1 h and it followed a matrix release kinetic model with a super case-II transport mechanism. The concentrations of the polymers affected the yield, loading efficiency, moisture loss and the extent of flavonoid release of the microspheres but had no effect on their particle sizes and flavonoid content. These results may find useful application in the delivery of V. amygdalina and G. kola extracts since the combination of PEG of different molecular weights resulted in microspheres with good physicochemical and release properties

Antimicrobial activities of creams prepared with methanol and aqueous leaf extracts of Ricinus communis L. (Euphorbiaceae)

The aqueous and methanol crude extracts of the leaves of Ricinus communis L. (Euphorbiaceae) have been reported to possess antimicrobial activity. This study was carried out to investigate the antimicrobial activity of the cream formulations of these leaf extracts against some pathogens. The extract of R. communis was obtained by maceration of the blended leaf using methanol or distilled water. Topical creams were prepared by mixing 6 g of cetomacrogol ointment BP with an aqueous phase prepared by dispersing 4 g of the extract in 10 mL of purified water. Agar well diffusion method was used to determine the antimicrobial activity of the creams against test organisms using diameter of zones of inhibition as a measure of activity. Plain creams formulated and a commercial antimicrobial cream were also tested. The yield of the extraction was 7.27 and 6.73 % with methanol and water respectively. Extracts were dark green in colour with a pungent odour. The colours of the creams formulated were also dark green while their pH values range from 2.54-5.01. Diameter of zones of inhibition produced against gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) and gram-negative bacterium (Pseudomonas aeruginosa) were 26, 18 and 14 mm for the methanol extract and 16, 13 and 11 mm for the aqueous extract. Escherichia coli and Candida spps were not inhibited by both extracts. The antimicrobial microbial activity of the methanol extract cream was comparable to that of the commercial cream. The plain creams showed no antimicrobial effect on all test organisms. The creams of methanol and aqueous extract of R. communis L. leaf have significant antimicrobial activity against test organisms except E. coli and Candida spps. The methanol extract cream would be useful in skin infections where the pathogen S. aureus is implicated.Keywords:  Ricinus communis, zones of inhibition, cetomacrogol emulsifying ointment BP, maceratio