Current Issue : January-March Volume : 2024 Issue Number : 1 Articles : 5 Articles
Background. Among all the pharmaceutical dosage forms, tablets are still the most preferred and the most commonly used option because of their advantages. The direct compression method of tablet preparation exempts several steps needed in the granulation method. Therefore, the pursuit of better direct compression tablet excipients is evident in contemporary research endeavors. Pregelatinized Taro Boloso-I starch has comparable flow properties and higher compressibility and compactibility than Starch 1500®. However, there is no evidence in the literature regarding the lubricant sensitivity and dilution potential of pregelatinized Taro Boloso- I starch. This study was aimed at performing the in vitro evaluation of paracetamol tablets prepared using pregelatinized Taro Boloso- I starch as a direct compression excipient using paracetamol as a model drug. Methods. Taro Boloso-I starch was pregelatinized, and its properties including amylose to amylopectin ratio, densities, flow properties, swelling power, water solubility index, particle morphology, moisture content, and moisture sorption profile were evaluated. Furthermore, the lubricant sensitivity test, dilution potential study, and compatibility test with the paracetamol drug using ATR spectroscopy were performed. The properties of the directly compressed tablets prepared accordingly were evaluated. The majority of evaluations were performed in comparison with Starch 1500®. Results and Discussion. PGTBIS had a significantly lower amount of amylose than Starch 1500®. In the ATR-IR spectra of the mixture of the paracetamol and pregelatinized PGTBIS, all the major absorbance peaks of the drug were maintained indicating the absence of chemical modifications. PGTBIS showed better flow properties than Starch 1500®. The modified starch was shown to withstand magnesium stearate up to 0.5% concentration. Conclusion. PGTBIS could accommodate higher drug cargo than Starch 1500® with acceptable tablet properties. Accordingly, PGTBIS starch could be taken as a potential direct compression excipient....
In this study, we developed a tamsulosin pellet-loaded orally disintegrating tablet (ODT) that is bioequivalent to commercially available products and has improved patient compliance using microcrystalline cellulose (MCC) and mannitol. Utilizing the fluid bed technique, the drug, sustained release (SR) layer, and enteric layer were sequentially prepared by coating MCC pellets with the drug, HPMC, Kollicoat, and a mixture of Eudragit L and Eudragit NE, respectively, resulting in the production of tamsulosin pellets. The tamsulosin pellet, composed of the MCC pellet, drug layer, SR layer, and enteric layer at a weight ratio of 20:0.8:4.95:6.41, was selected because its dissolution was equivalent to that of the commercial capsule. Tamsulosin pellet-loaded ODTs were prepared using tamsulosin pellets and various co-processed excipients. The tamsulosin pellet-loaded ODT composed of tamsulosin pellets, mannitol–MCC mixture, silicon dioxide, and magnesium stearate at a weight ratio of 32.16:161.84:4.0:2.0 gave the best protective effect on the coating process and a dissolution profile similar to that of the commercial capsule. Finally, no significant differences in beagle dogs were observed in pharmacokinetic parameters, suggesting that they were bioequivalent. In conclusion, tamsulosin pellet-loaded ODTs could be a potential alternative to commercial capsules, improving patient compliance....
Being biocompatible, less toxic, cheap, easily available, and environmentally friendly, there is an increased trust in natural polymers in the drug delivery system. Mucilages, among the natural polymers, are the primary metabolites of plants that have been widely utilized in pharmaceutical manufacturing for different purposes, and mucoadhesive is one among them. The present study was designed to investigate the use of LSM as a mucoadhesive polymer using ibuprofen as a model drug. The mucilage was extracted following an aqueous extraction method and its percentage yield was found to be 13.2% w/w. Besides, three microsphere formulations of ibuprofen were prepared using synthetic polymer hydroxyl propyl methyl cellulose (HPMC) K100M and the LSM in polymer to drug ratios of 1 : 1, 1 : 5, and 3 : 5 by applying ionotropic gelation followed by solvent evaporation methods. The microspheres were evaluated for various micromeritic properties and all the formulations exhibited free-flowing properties. Optical microscopic pictures of almost all the microspheres except F3 and F6 (which had more or less spherical shapes) were found to have irregular and discrete shapes. Besides, the surfaces of all the formulations were rough in texture. The drug entrapment efficiency of the microspheres was found to be between 52.08% ± 0.80 and 87.97% ± 0.72. The in-vitrowash-off test evidenced that almost 50 percent (especially F3) of the microspheres were able to adhere up to 18 h and showed remarkable bioadhesion properties. The in-vitro drug release profile indicated that all the formulations were able to prolong their drug release up to 12 h with a non-fickian release mechanism, except for F4, which followed a fickian release. Therefore, based on the findings of this study, LSM can be used as a potential alternative mucoadhesive excipient for sustained release formulations....
The stomach and upper part of the small intestine are where furosemide is primarily absorbed when treating edema brought on by congestive heart failure (CHF), hepatic cirrhosis, renal impairment, and nephrotic syndrome. This narrow absorption window is responsible for furosemide’s limited oral bioavailability. So creating a gastroretentive floating tablet could be beneficial. Natural polymers are advised for use in medication delivery because they are readily available in nature, biodegradable, relatively inexpensive, biocompatible, and nontoxic. Olibanum is a natural plant-based polymer obtained from Boswellia genus of trees and mainly composed of alcohol-soluble resin (65-85%). Ethiopia is rich in Boswellia species, with Boswellia papyrifera being the most important oleo-gum resin-producing tree species. In order to formulate a gastroretentive floating matrix tablet of furosemide, this study looked at the use of naturally occurring, locally available B. papyrifera resin as a matrix-forming polymer. By directly compressing B. papyrifera resin and HPMC K4M as matrix-forming polymers and sodium bicarbonate as a gas-generating agent, floating matrix tablets were created. The effects of the formulation variables polymer type, polymer concentration, polymer ratio, and percentage of the floating agent on the floating lag time, total floating time (duration), and cumulative drug release in 12 hours were investigated. Furosemide floating tablets formulated employing higher (40%) polymer concentrations (olibanum resin, HPMC K4M, or in combination) and 10% sodium bicarbonate as gas-generating agent demonstrated a floating lag time of less than 6 minutes and a sustained release with a total floating time of more than 12 hours. Comparing the release characteristics of floating tablets made with 40% of a total polymer and 10% of NaHCO3 revealed that the medicine is released very slowly when polymers were combined. The matrix-forming polymer, olibanum resin, obtained from B. papyrifera, was effectively used to make furosemide floating matrix tablets. The olibanum resin from B. papyrifera can therefore be used as a potential substitute matrix-forming polymer in the production of effervescent floating matrix tablets....
Binders are ingredients used in tablet granulation process for tablet cohesiveness which confirms that the tablet remains intact after compression. Natural gums have been employed as disintegrants, emulsifying agents, suspending agents, and binders in tablets. Even though Ficus vasta gum is claimed as a possible pharmaceutical excipient by some phytochemical studies, literature is scanty on its efficacy as a tablet binder. The purpose of this study was to isolate, characterize, and comparatively evaluate Ficus vasta gum as a potential binder in tablet formulation. Gum was extracted from Ficus vasta tree, characterized for physicochemical properties, and applied as a binder in paracetamol granule and tablet formulation. Granules were prepared using 4%, 6%, 8%, and 10% w/w concentration of the gum and standard binders (polyvinylpyrrolidone K-30 and Starch@1500) by wet granulation. The formulated tablets were then evaluated for tablet quality parameters, and comparison between the test and standard binders was done by ANOVA. The dried crude gum yielded 50.63% (w/w) of a brownish yellow purified gum. The angle of repose, Carr’s index, and the Hausner ratio all complied with the pharmacopoeial recommendations. The gum is compatible with the model drug, paracetamol. The paracetamol granules prepared with Ficus gum binder demonstrated an optimum size range and size distribution with substantial flow and compressibility properties. Ficus gum binder demonstrated significantly higher disintegration time and strength properties than that of similar concentrations of Starch@1500 but lower than polyvinylpyrrolidone (p < 0:05). Ficus gum has better binding properties than starch but lower than polyvinylpyrrolidone. Hence, Ficus vasta gum can be used as an alternative tablet binder in tablet manufacturing....
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