Solidified Reverse Micellar Solution (SRMS)-Based Indomethacin Sustained-Release Tablets: Formulation and In vitro Evaluation

Purpose: To formulate and evaluate sustained-release indomethacin tablets based on solidified reverse micellar solution (SRMS).Methods: SRMS consisting of mixtures of phospholipid (Phospholipon® 90H) and triglyceride (Softisan® 154) were prepared in the ratios of 1:1, 2:1 and 1:2, respectively. SRMS-based tablets containing 75 mg of indomethacin each were prepared using a validated plastic mould. The physicochemical properties of the tablet formulations were studied. In vitro release study was carried out in simulated intestinal fluid (SIF, pH 7.5).Results: The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix used (p < 0.05). Tablet hardness ranged from 5.00 ± 0.39 to 5.60 ± 0.36 kgf for tablets formulated with SRMS 1:2 and 2:1 (N3 and N2), respectively. The tablets exhibited friability of < 1 % (p < 0.05). Erosion time in SIF ranged from 124.0 ± 0.5 to 180.0 ± 1.1 min while drug release from the tablets reached a maximum in 8 – 11 h for all thebatches.Conclusion: Indomethacin tablets based on SRMS exhibited good sustained-release properties and can be further developed to achieve once daily administration for improved patient adherence to therapy.Keywords: Solidified reverse micellar solution, Phospholipid, Triglyceride, Indomethacin, Sustained release

FORMULATION AND EVALUATION OF NOVEL HERBOSPHERES DELIVERY SYSTEM OF LEAF EXTRACT OF VERNONIA AMYGDALINA DEL (ASTERACEAE)

Objectives: The objectives of the study were to formulate herbospheres of V. amygdalina leaf-extract and to study the in vitro and antibacterial properties of the formulationsVernonia amygdalina, Del (Asteraceae) is a tropical shrub used throughout West Africa for the management of diabetes and other metabolic diseases associated with the liver. The plant has acquired special relevance recently, having been proved in human medicine to possess potent antimalarial, antihelmintic, and antitumorigenic properties.Methods: Herbospheres were formulated with lipid matrices consisting of goat fat (70%) and Phospholipon® 90H (30%) by melt homogenization and characterized for taste masking, particle size, pH, encapsulation efficiency, and loading capacity. Inhibition zone diameter of the herbospheres was studied.Results: Phytochemical analysis showed the presence of alkaloids, saponins, tannins, carbohydrates, reducing sugars, protein, steroids, flavonoids, and cardiac glycosides in substantial quantities. Acid compounds and oils were, however, absent. The particle size of herbospheres ranged from 6.90±0.2 to 28.50±0.71 μm and was significantly affected by the type of surfactant used (p < 0.05). The pH ranged from 5.6 to 5.9 at day 1 and 4.1 to 4.4 at 30 days. Highest EE of 90–92 % was obtained and was significantly affected by surfactant used (p<0.05). Formulations exhibited significantly higher inhibition of Staphylococcus aureus than tetracycline pure sample used as the reference drug (p<0.05).Conclusion: V. amygdalina herbospheres formulations had antibacterial properties in addition to taste masking and high encapsulation of the extract

In vitro and In vivo Characterisation of Piroxicam-Loaded Dika Wax Lipospheres

Purpose: To formulate piroxicam-loaded lipospheres and evaluate their in vitro and in vivo properties.Method: Piroxicam-loaded lipospheres were prepared by hot  homogenization technique using dika wax and Phospholipon® 90G (1:1, 1:2 and 2:1) as the lipid matrix. Characterisation, based on particle sizeand morphology, pH, drug content and encapsulation efficiency, were carried out on the lipospheres. In vitro release was evaluated in simulated intestinal fluid (pH 7.5). Anti-inflammatory and ulcerogenic properties of the piroxicam-loaded lipospheres were studied using healthy, adult Wistar rats.Result: Photomicrographs revealed spherical particles in the range of 1.66 – 3.56 ìm. The results also indicated that lipospheres formulated with lipid matrix 1:1 and containing 0.25 % piroxicam had the highest encapsulation efficiency of 84 %. In vitro release data showed that lipospheres formulated with lipid matrix having higher concentration of dika wax exhibited the fastest drug release of drug with maximum release time between 60 - 70 min. The lipospheres exhibited good anti-inflammatoryproperties with 58.6 % oedema inhibition at 5 h. Piroxicam-loaded liposheres had an ulcer index of zero while, the reference (plain piroxicam) had an ulcer index of 15.00 ± 1.23 (p < 0.05).Conclusion: Piroxicam lipospheres formulated with a mixture of dika wax and phospholipid exhibited good in vitro and in vivo properties.Keywords: Dika wax, Lipospheres, Piroxicam, Phospholipid, Ulcerogenicity, Anti-inflammator

Clinical effects of Garcinia kola in knee osteoarthritis

<p>Abstract</p> <p>Objectives</p> <p>Over the past years, there has been a growing number of knee osteoarthritis (KOA) patients who are not willing to comply with long-term non-steroidal anti-inflammatory drugs (NSAID) treatment and wish to use herbal anti- rheumatic medicine. This study assessed the clinical effects of <it>Garcinia kola </it>(GK) in KOA patients.</p> <p>Patients and methods</p> <p>Prospective randomized, placebo controlled, double blind, clinical trial approved by the institutional medical ethics review board and written informed consent obtained from each patient. All KOA patients presenting at the Obafemi Awolowo University Teaching Hospital complex were recruited into the study. The patients were grouped into four (A = Placebo, B = Naproxen, C = <it>Garcinia kola</it>, D = Celebrex). The drugs and placebo were given twice a day per oral route. Each dose consisted of 200 mg of <it>G. kola</it>, Naproxen (500 mg), Celebrex (200 mg) and Ascorbic acid (100 mg). The primary outcome measure over six weeks study period was the change in mean WOMAC pain visual analogue scales (VAS). Secondary outcome measures included the mean change in joint stiffness and physical function (mobility/walking).</p> <p>Results</p> <p>143 patients were recruited, 84 (58.7%, males – 24, females – 60) satisfied the selection criteria and completed the study. The effect of knee osteoarthritis bilateralism among the subjects was not significant on their outcome (p > 0.05). The change in the mean WOMAC pain VAS after six weeks of <it>G. kola </it>was significantly reduced compared to the placebo (p < 0.001). Multiple comparisons of the mean VAS pain change of <it>G. kola </it>group was not lowered significantly against the naproxen and celebrex groups (p > 0.05). The onset of <it>G. kola </it>symptomatic pain relief was faster than the placebo (p < 0.001). However, it was slower than the active comparators (p > 0.05). The duration of therapeutic effect of <it>Garcinia kola </it>was longer than the placebo (p > 0.001). <it>G. kola </it>period of effect was less than naproxen and celebrex (p < 0.001). <it>G. kola </it>subjects had improved mean change mobility/walking after six weeks better than the control group(p < 0.001). The mean change in mobility of the <it>G. kola </it>group when compared to the active comparators was not significantly better (p < 0.05). The mean change of knee joint stiffness (p < 0.001) and the change of mean WOMAC score (p < 0.001) were improved on <it>Garcinia kola </it>as compared to the placebo. The mid term outcome of eleven <it>Garcinia kola </it>subjects after cessation of use had a mean pain relief period of 17.27 +/- 5.15 days (range: 9–26 days). There was no significant cardiovascular, renal or drug induced adverse reaction to <it>Garcinia kola</it>.</p> <p>Conclusion</p> <p><it>Garcinia kola </it>appeared to have clinically significant analgesic/anti-inflammatory effects in knee osteoarthritis patients. <it>Garcinia kola </it>is a potential osteoarthritis disease activity modifier with good mid term outcome. Further studies are required for standardization of dosages and to determine long-term effects.</p

An evaluation of the bioadhesive performance and release of bioerodable metronidazole tablets

The bioadhesive performance and some other physical properties of the tablets were evaluated. The tablets showed higher bioadhesive strength than the polymers in dispersion. However, tablets formulated with SCMC had higher bioadhesive strength than the Detarium based tablets. The bioadhesion of the tablets increased with an increase in binder concentration. The tablets showed satisfactory hardness and friability values. However all the tablets failed the disintegration time test. The disintegration times of the tablets formulated with Detarium gum were lower in 0.1N HCI than the tablets prepared with SCMC while the reverse was the case in Simulated Intestinal Fluid (SIF). Moreover, the rate of drug dissolution was higher in 0.1N HCI for the tablets formulated with Detarium gum. Key Words: Bioadhesive, Strength, Hardness, Friability, Disintegration Time and Dissolution Rate. Journal of Biomedical Investigation Vol.1 2003: 18-2

Some physical properties of tabletted Bridelia ferrugnea leaf extract

This paper is an attempt to formulating an indigenous medicinal plant into a modern pharmaceutical tablet dosage form. The dried lead extract of B. ferruginea was formulated into tablets dosage forms using three standard binders at concentration levels of 2–8%w/w. Some physical properties of the tablets such as hardness, friability, disintegration time, dissolution rate and content uniformity were evaluated. The tablets had satisfactory physical properties with exception of those batches containing 4–8%w/w SCMC that failed the disintegration test. Tablets containing SCMC also showed the highest hardness and least friability. Since most of the tablet batches had satisfactory physical properties, it is possible to employ the named binders in the formulation of the conventional tablets of B. ferruginea. Bio-Research Vol. 3(1) 2005: 85-8

Formulation of Croton penduliflorus seed into tablet dosage form

No Abstract. Global Journal of Medical Sciences Vol. 5(1) 2006: 29-3

Binding Properties Of A Polymeric Gum From Cola accuminata

The binding properties of a polymeric gum obtained from the pods of Cola accuminata was studied. The tablets produced with the new gum showed good weight uniformity, friability and hardness profiles. However all the tablets produced with 1 % w/w binder; Sodium carboxyl methyl cellulose (SCMC) and Cola accuminata failed the hardness test. Hardness increased while friability decreased as tablet binder concentration increased. However, the tablets produced with Cola accuminata gum had long disintegration times similar to the tablets produced with SCMC. Only the tablets produced with low binder concentrations of Cola accuminata and SCMC (1 – 2 % w/w) passed the disintegration time test. Moreover at 1-2 % w/w binder concentrations, tablets produced with Cola accuminata recorded higher drug release rates than the tablets containing SCMC. However at 4-6 % w/w binder concentrations, it showed drug release rates comparable with the tablets formulated with the standard binder SCMC. KEY WORDS: Cola accuminata, binding property, disintegration time, Dissolution rate. Global Journal of Pure and Applied Sciences Vol.11(2) 2005: 233-23

Some physicochemical properties and application of A. Cellulose from Pennisetum purpureum as a disintegrant in tablet formulation

No abstract availabl

SOME PHYSICOCHEMICAL PROPERTIES AND APPLICATION OF &alpha; -CELLULOSE FROM PENNISETUM PURPUREUM AS A DISINTEGRANT IN TABLET FORMULATION

This study was undertaken to process a locally available tablet disintegrant from Pennisetum purpureum inorder to reduce importation of such pharmaceutical excipients into the country. Some physicochemical and flow properties of the processed &alpha;-cellulose were studied. The &alpha;-cellulose was also employed as disintegrant in some tablet formulations. Some of the physicochemical and flow properties evaluated were, moisture content, bulk density, packed density, Carrs compressibility, angle of repose and Hausner quotient. The tablet properties studied were, disintegration time, hardness, friability and dissolution rate. The prepared &alpha;-cellulose had poor flow properties since it recorded high values of angle of repose, Carr's compressibility and Hausner's quotient. All the batches of tablets passed the weight uniformity test. Tablets formulated with the &alpha;-cellulose showed lower disintegration and dissolution times than the tablets containing maize starch as disintegrant. Hence the processed &alpha;- cellulose could be employed as a locally available substitute to maize starch as a tablet disintegrant. Global Jnl Pure & Applied Sciences Vol.10(1) 2004: 95-10