A flexible technology for modified-release drugs: Multiple-unit pellet system (MUPS)

Abdul, Shajahan; Chandewar, A. V.; Jaiswal, Sunil B

doi:10.1016/j.jconrel.2010.05.014

Cited by 155 publications

(85 citation statements)

References 83 publications

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“…Failure of few units may not be as consequential as failure of a single-unit system. This is apparent in sustained-release single-unit dosage form, where a failure may lead to dose-dumping of the drug (Abdul et al, 2010). Like other multiple unit systems, minitablets can be filled into hard gelatin capsules that release these subunits (minitablets) after disintegration of capsule.…”

Section: Introductionmentioning

confidence: 99%

Design and characterization of cefuroxime axetil biphasic floating minitablets

et al. 2014

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Biphasic floating minitablets of cefuroxime axetil were prepared by melt granulation technique using two different grades of gelucire namely 50/13 and 43/01 to maintain constant plasma drug concentration. Loading dose of cefuroxime axetil was formulated as immediate release (IR) minitablets by using hydrophilic grade of gelucire 50/13. Maintenance dose was formulated as floating sustained release (SR) minitablets by using hydrophobic grade of gelucire 43/01. The prepared IR and SR granules were subjected to micromeritic studies and scanning electron microscopy. Fourier transform infrared spectroscopy (FT-IR) study revealed that drug and selected carriers were compatible. In vitro dissolution study of optimized IR minitablets showed more than 85% of loading dose dissolved within 30 min. Optimized SR minitablets showed zero lag time with floating duration more than 12 h. The drug release from SR minitablets was linear with square root of time with non-Fickian diffusion-controlled release. The optimized batch of minitablets was filled into 0 size hard gelatin capsule. In vitro dissolution study for capsule showed an immediate burst release followed by SR up to 12 h. There is no significant change in dissolution data after storage at 40 C and 75% RH for three months. Microbiological assay of dissolution samples of optimized minitablets filled in capsules showed proportionate increase in inhibition of growth against Escherichia coli up to 12 h samples. In vivo bioavailability study in albino rabbits showed three times improvement in oral bioavailability.

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Section: Introductionmentioning

confidence: 99%

Design and characterization of cefuroxime axetil biphasic floating minitablets

et al. 2014

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“…Their small size also enables them to be well distributed along the gastrointestinal tract that could improve the bioavailability, which potentially could result in a reduction in local drug concentration, risk of toxicity and side-effects [7]. Inter and intra-individual variations in bioavailability caused for example by food effects are reduced.…”

Section: Multi-particulate Dosage Formsmentioning

confidence: 99%

“…So, a dosage forms which disintegrates rapidly in the oral cavity within a small amount of saliva might be a suitable dosage form, even for infants and toddlers. This leads to a second approach for pediatric solid dosage forms: the ODT which disintegrates in the mouth in a few seconds [7]. ODTs are defined in the European Pharmacopoeia as uncoated tablets intended to be placed in the mouth where they disperse rapidly before being swallowed [8].…”

Section: Multi-particulate Dosage Formsmentioning

confidence: 99%

Multi-Particulate Dosage Forms for Pediatric Use

Martínez-Terán¹,

Hoang-Thi²,

Flament³

2017

Pediatr Ther

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In recent years, regulations on pediatric medicines have induced an increased need for research into novel childappropriate dosage forms. Indeed, children cannot be considered as « small adults » as they present different anatomical and physiological characteristics. Whatever the route of administration, the age-appropriateness of the formulation is of major importance and has to be taken into consideration. The development of new pediatric dosage forms encounters technical complexities such as dose modification, ease of administration/swallowing, tastemasking, chemical and physical stability, preservation, considerations of a multi-phase and/or multi-use product, packing, providing/designing the measuring device. Innovations are important and the research of new ways to deliver medicines tends to improve compliance, convenience and pharmacokinetic. Recently, the World Human Organization recommended that small sized solid forms or orally disintegrating solid forms should be favored. Solid multi-particulate systems such as pellets have the advantage to cover a broad range of doses for different patients. Dose adjustment can be accurately done by means of dosing device such as a multi-particulate counting device. Developing multi-particulate dosage form with fast disintegration can be useful for children as they present both advantages of solid and liquid formulations. This led to the concept of Orally Disintegrating Tablet which disintegrates rapidly in the mouth into small particles or pellets. Their small size enables them to be well distributed along the gastrointestinal tract improving the bioavailability while reducing local drug concentration, risk of toxicity and side effects. They offer easy swallowing and dose flexibility for pediatric patients and caregivers. The promising results of our fast disintegrating pellets used in multi-particulate dosage forms indicate that they might be the base of a solid platform technology for pediatric medicines.

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“…Pellets exhibit advantages over tablets such as less irritation, and a lower risk of side effects due to dose dumping at the mucosa focus site, have a lower tendency of adhering to the esophagus, provide a good distribution and smoother drug absorption profile in the GI tract due to the less variable transit times. As a result, they render reproducible drug blood levels and leave the stomach rapidly regardless of the gastric emptying rate, feeding, or nutritional state of the patient [3].…”

Section: Introductionmentioning

confidence: 99%

Comparative Evaluation of the Release Properties of Verapamil HCL and Carbamazepine From Microcrystalline Cellulose Ii Pellets

Rojas

Correa

2017

Int J Pharm Pharm Sci

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Objective: To study microcrystalline cellulose II (MCCII) as new pelletization aid for a high and low solubility drugs such as verapamil. HCl and carbamazepine, respectively. Methods:Approximately, 30 g of MCCII and drug mixtures were hydrated, passed through a # 20 mesh sieved and spheronizated at a frequency of 6 Hz and residence time of 480 s. A microscopy analysis was used to evaluate the shape and size descriptors. Pellets properties such as compressibility, friability, density, flowability and product yield were also evaluated. Drug release properties were tested according to the USP specifications and compared to those of MCCI. Results:The wetting level of the excipients depended on drug loading and drug solubility. Thus, a high drug loading (>50%) rendered pellets having a low yield, flowability and caused a detriment on size descriptors. Likewise, the regular morphology and strength of MCCII-based pellets was highly affected by increasing drug loads. Verapamil. HCl pellets were less friable and compressible and showed better flowability than carbamazepine pellets. Regardless of drug loading and drug solubility, MCCII-based pellets released more than 80% of verapamil. HCl within 10 min, whereas released more than 75% of carbamazepine within 15 min. Conversely, MCCI pellets had a satisfactory verapamil. HCl release, but ~30% carbamazepine release within 1h. Conclusion:MCCII proved to be a better excipient than MCCI to yield beads having optimal pellet characteristics, and rendered an immediate release profile for verapamil. HCl and carbamazepine.

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A flexible technology for modified-release drugs: Multiple-unit pellet system (MUPS)

Cited by 155 publications

References 83 publications

Design and characterization of cefuroxime axetil biphasic floating minitablets

Design and characterization of cefuroxime axetil biphasic floating minitablets

Multi-Particulate Dosage Forms for Pediatric Use

Comparative Evaluation of the Release Properties of Verapamil HCL and Carbamazepine From Microcrystalline Cellulose Ii Pellets

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