Properties Of Tablets Research Articles

Impact of supply chain on some tablet properties of six brands of glibenclamide marketed in Jos metropolis

Drugs are important commodities that must be handled differently from other goods. Therefore, supply chain of drugs must be monitored until it gets to the patient to maintain therapeutic efficacy. Drug properties are compromised when stipulated storage conditions are not maintained over time, and this can result in a poor therapeutic outcome. This is more impactful for glibenclamide tablets, which many diabetic patients preferentially use because of its cost-effectiveness and availability. The aim of this study was to assess the impact of supply chain on tablet properties of six glibenclamide tablet brands marketed in Jos metropolis. Glibenclamide tablets obtained from hospital and community pharmacies, and patent medicine outlets, were subjected to quality control tests such as content uniformity, friability, crushing strength, disintegration time, and dissolution test. The results were analyzed using ANOVA, fit factors (f1 and f2 ) and dissolution efficiency (DE). The results showed that all the brands passed weight uniformity, friability and disintegration tests. The ANOVA showed significant difference between the release profiles of the brands. Brands from patent medicine outlet had lower content values compared to brands from pharmacies (A1 /A3 - 102/98%; E1 /E3 - 124/108%). Brands E3 from patent vendor outlet failed f1 and f2 limits (15.3/47.9) while brands E1 and F1 from community pharmacies failed f1 , f2 and DE limits (23.6/39.4/5.91 and 17.2/46.1/8.35) respectively. Brands from hospital pharmacies showed no adverse parameters. In conclusion, private commercial enterprises engaged in drug retail may have to be monitored closely to ensure drug quality and hence public health care.Keywords: Tablet properties; Glibenclamide; Supply chain; Jos ________________________________________________

OPTIMIZATION OF STATISTICALLY DESIGNED ACECLOFENAC FAST DISSOLVING TABLETS EMPLOYING STARCH GLUTAMATE AS A NOVEL SUPERDISINTEGRANT

Objective: To optimize aceclofenac fast dissolving tablets employing starch glutamate as novel superdisintegrant by 23factorial design to improve bioavailability and enhance patient compliance.
 Methods: Starch glutamate was prepared by the esterification process. Starch glutamate physical and micromeritics properties had been evaluated and the prepared starch glutamate was used as a superdisintegrant for the formulation of the fast dissolving tablets of aceclofenac by direct compression method and optimized by employing 23factorial design. The prepared aceclofenac fast dissolving tablets were evaluated for post compression parameters as well as in vitro and in vivo release characteristics. Optimized formulation stability studies were performed at accelerated conditions for 6 mo as per ICH and WHO guidelines.
 Results: The prepared starch glutamate was amorphous, insoluble in aqueous and organic solvents were tested. Fast dissolving tablets of aceclofenac were formulated by employing starch glutamate as a superdisintegrant showed good tablet properties and showed an increased dissolution efficiency of the drug. Among all the formulations (F1 to F8), the formulation F8 containing 5% concentration of starch glutamate, croscarmellose sodium and, crospovidone as a superdisintegrants showed 99.7±0.15% of drug release within 5 min. Whereas the formulation F2 containing 5% concentration of starch glutamate, drug release characters were comparable to the formulation F8. Optimized formulation F2 attained peak plasma concentration within a short period and showed increased relative bioavailability of the drug.
 Conclusion: From the physical properties, disintegration time, in vitro dissolution studies and pharmacokinetic studies, it was concluded that fast dissolving tablets of aceclofenac tablets formulated by employing starch glutamate as a superdisintegrant enhanced the dissolution efficiency and improved the bioavailability of the drug as compared to the pure drug and stable.

Comparative analyses/evaluation of the textural properties of naproxen sodium tablets and powders prepared using microwave and other drying techniques

The properties of oral tablets are normally related to the properties of the powders they contain. Characterization of oral tablets is important for the development of tablets with rapid and safe release of the active ingredient. In this study, a new formulation of naproxen sodium was prepared and dried using microwave drying (MWD) and the following conventional drying techniques: freeze-drying (FD), vacuum drying (VD), and convective drying (CD). The reference drug powder (RDP) and dry granules MWG, CDG, VDG, and FDG, which were dried using MWD, CD, VD, and FD, respectively were compressed to form tablets labeled RF-TAB, MW-TAB, CD-TAB, VD-TAB, and FD-TAB, respectively. The dry granules and prepared tablets were characterized using Fourier transform infrared spectrometry, scanning electron microscopy, and X-ray diffraction. This study aimed to explore the correlation between the textural characteristics of the tablets and their respective powders for different drying methods. Although the morphologies of the dry particles were irregular, the prepared tablets were smooth and flat with few cracks. Drying increased the amorphous nature of the granules but decreased their crystallinity. The crystallinities of all tablets, except those prepared by VD, decreased after compression. In summary, the characteristics of the prepared tablets were acquired from their respective powders.

Pharmacokinetics and Bioequivalence Evaluation of a New Oxycodone Tamper-Resistant Tablet Administered with an Opioid Antagonist in Patients with Chronic Pain.

Oxycodone tamper resistant (OTR) is a new extended-release abuse-deterrent formulation providing improvements in the tamper resistant characteristics. This study aimed to investigate the pharmacokinetic properties of the new OTR tablets and evaluate the bioequivalence of oxycodone from OTR and the original extended release (ER) formulation tablets administered with an opioid antagonist in patients with chronic pain. In this open-label, randomized, cross-over study, the enrolled patients were randomised to receive a single dose of 40mg OTR or 40mg OXYCONTIN® (OXY) tablet administered with naltrexone blockade under fasting conditions. Serial blood samples for pharmacokinetic analysis were collected. Plasma oxycodone was quantified by a high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method. Tolerability was evaluated by monitoring adverse events, physical examinations, 12-lead ECG and laboratory tests. A total of 38 patients were enrolled and 33 subjects completed the study. After a single dose of 40mg tablets, pharmacokinetic results of the new OTR tablet were found to be similar to those of original extended-release oxycodone tablet. OTR 40mg was bioequivalent to OXY 40mg and was well tolerated in patients with chronic pain. The new OTR formulation could provide a new choice in the treatment of chronic pain and reduce the potential for oxycodone abuse. Chictr.org identifier: ChiCTR1800017253.

Importance of pressure plasticity during compression of probiotic tablet formulations

The usefulness, the high production rate and the cost effectiveness make tablets the dosage form of choice for oral probiotics. Nevertheless, probiotic bacteria undergo a lot of mechanical stress during tableting which causes damage to their cell wall and membrane and other bio-active components. This can lead to an inactivation of the probiotic bacteria and therefore in a failure of the probiotic therapy. To obtain a tablet with a sufficient amount of viable cells, research on the influence of formulation and process parameters on bacterial survival is essential. This study aimed to decipher tableting properties of the probiotic powder blends that have a major impact on survival rates. The powder blends consisted of the prototype probiotic strain Lactobacillus rhamnosus GG, a filler-binder and a suitable amount of lubricant. They were manufactured by direct compression at different compression pressures and tableting speeds. The tableting properties were analysed in detail by a 3-D modelling technique, which characterized normalized time, pressure and displacement simultaneously. The results of the 3-D modelling demonstrated the significant effect of the pressure plasticity (e) and the angle of rotation (ω) on the viability of L. rhamnosus GG during direct compression.

Controlled-Release Fine Particles Prepared by Melt Adsorption for Orally Disintegrating Tablets.

Melt adsorption is a manufacturing method that offers precise control of particle size distribution of granules and circumvents the disadvantages of conventional melt granulation. However, drug release from particles adsorbed with hydrophobic materials has not been fully investigated, and there are missing details as to whether particles manufactured by this technique can be applied to orally disintegrating tablets (ODT). In this report, we aimed to optimize process parameters and formulation to manufacture ODT containing melt adsorption-particles with the specific characteristic of sustained release. Melt adsorption particles containing Neusilin US2 as the adsorbent were prepared by using various waxes to determine the most suitable material for controlled release formulation. Glycerol fatty acid ester (Poem TR-FB: TR-FB) was the optimal wax examined because of its drug release pattern and tabletability. We then optimized manufacturing conditions by examining granulation time, disintegrant amount per tablet and compression force on the tablet for ODT that meet the criteria of controlled drug release, tensile strength and disintegration of the tablet. Multiple regression analysis revealed the effect of process parameters on tablet properties and drug release with increasing the granulation time affording sustained release of the drug. The analysis also showed that a high compression force crushed the granules coated by TR-FB, which impaired sustained drug release. From the regression model the optimal manufacturing conditions were determined, and the tablet prepared under these conditions concurred with the predicted values and met all criteria. This new technique should contribute to the development of ODT to improve medication adherence.

The Usefulness of Definitive Screening Design for a Quality by Design Approach as Demonstrated by a Pharmaceutical Study of Orally Disintegrating Tablet.

Definitive screening design (DSD) is a new class of small three-level experimental design that is attracting much attention as a technical tool of a quality by design (QbD) approach. The purpose of this study is to examine the usefulness of DSD for QbD through a pharmaceutical study on the preparation of ethenzamide-containing orally disintegrating tablet. Model tablets were prepared by directly compressing the mixture of the active pharmaceutical ingredient (API) and excipients. The five evaluated factors assigned to DSD were: the contents of API (X1) and lubricant (X2), and the compression force (X3) of the tableting process, the mixing time (X4), and the filling ratio of powder in the V-type mixer (X5). After tablet preparation, hardness and disintegration time were measured. The same experiments were performed by using the conventional design of experiments [i.e., L8 and L16 orthogonal array designs and central composite design (CCD)]. Results showed that DSD successfully clarified how various factors contribute to tablet properties. Moreover, the analysis result from DSD agreed well with those from the L8 and L16 experiments. In additional experiments, response surfaces for tablet properties were created by DSD. Compared with the response surfaces created by CCD, DSD could produce reliable response surfaces for its smaller number of experiments. We conclude that DSD is a powerful tool for implementing pharmaceutical studies including the QbD approach.

Formulation and Evaluation of Metoprolol Tartrate Sustained Release Matrix Tablets

The objective of the present work was to develop sustained release matrix tablets of Metoprolol tartrate using different polymers viz. Guar gum, Xanthan gum, Kondagogu gum and HPMC K100M. The release rates were modulated by combination of two different rates controlling material and triple mixture of two different rate controlling materials. After evaluation of physical properties of tablet, the in-vitro release study was performed in phosphate buffer pH 6.8 up to 12 hrs. Dissolution data was analyzed for release kinetics. It was observed that matrix tablets contained polymer Xanthan gum was successfully sustained the release of drug up to 12 hrs. Among all the formulations, F6 which contains 45 % of Xanthan gum, release of drug which follows zero order kinetics via, swelling, diffusion and the release profile of formulation F6 was compared with marketed product. The FTIR study revealed that there was no chemical interaction between drug and excipient.

Development and in vitro/in vivo evaluation of tamarind seed gum-based oral disintegrating tablets after fabrication by freeze drying

To overcome swallowing problems, particularly among the aging population, oral disintegrating tablets (ODTs) have been developed to disintegrate instantly in saliva. Here we developed novel diclofenac sodium ODTs by freeze drying and evaluated their efficacy using in vitro and in vivo tests. A sugar alcohol, mannitol, sorbitol, or xylitol, was used as the excipient and tamarind (Tamarindus indica) seed gum (crude or modified forms) was used as a binder in the freeze-dried tablets. Tablets with appropriate portions of the sugar alcohol (30–60 mg) and gum (50–100 mg) showed a good appearance. However, those containing mannitol had better appearance and integrity and were easier to remove from molds than those containing sorbitol or xylitol. The tablet properties thickness, diameter, and weigh variation were controlled to monitor tablet quality. The ODT formulation containing diclofenac sodium, polyethylene glycol (PEG) 4000, modified tamarind seed gum, and mannitol showed the shortest disintegration time (less than 2 min) in phosphate buffer (pH 6.8). Moreover, this formulation achieved 100% drug release in less than 6 min. These data warant the application of freeze drying using gum as a binder for the fabrication of ODTs containing heat-sensitive active pharmaceutical ingredients.

Performance Evaluation of Maize Starch as a Multifunctional Excipient in Metronidazole Tablet Formulation

Objective: The aim of this study was to evaluate the performance of maize starch as a multifunctional excipient in metronidazole tablet formulation. Methods: Metronidazole tablets were prepared by wet granulation containing maize starch as diluent (40 %), disintegrant (10 %), and binder (5 %) and compared with a reference formulation containing lactose as diluent (40 %), maize starch as disintegrant (10 %) and acacia as binder (5 %). The granules were analysed for particle size, flow properties, compressibility and moisture content. Tablets weighing 500 mg were compressed for both formulations on a Single Punch Tablet Press using a 12 mm flat-faced punches at 57.5 MPa. The tablets were kept for 24 h to allow for elastic recovery and evaluated for weight and content uniformity, thickness, crushing strength, friability, disintegration time and in vitro drug release. Results: The granule properties revealed differences in mean granule size, angle of repose, bulk and tapped densities for both formulations. Batch I tablets gave rise to better tableting properties compared to batch II tablets. Conclusion: This study confirms the suitability of maize starch as a multifunctional excipient in tablet formulation.

FORMULATION AND EVALUATION OF STATISTICALLY DESIGNED IBUPROFEN FASTDISSOLVING TABLETS EMPLOYING STARCH GLUTAMATE AS A NOVEL SUPERDISINTEGRANT

Objective: The main aim of the present work is to enhance the solubility and bioavailability of the ibuprofen by formulating it into fast-dissolving tablets employing starch glutamate as a novel superdisintegrant.
 Materials and Methods: Starch glutamate was prepared from native potato starch and glutamic acid by the esterification process. Drug-excipient compatibility studies were performed between the starch glutamate and ibuprofen with the help of Fourier transform infrared spectroscopy, and differential scanning calorimetry techniques. Ibuprofen fast dissolving tablets were formulated employing different superdisintegrants along with the starch glutamate (a novel superdisintegrant) by the direct compression method. The prepared ibuprofen fast-dissolving tablets were evaluated for various pre- and post-compression parameters along with the in vitro and in vivo release characteristics. Optimized formulation stability studies were performed at accelerated conditions for 6 months as per the International Conference on Harmonization (ICH) and WHO guidelines.
 Results: Drug-excipient compatibility studies indicated that prepared starch glutamate was compatible with ibuprofen drug, and it can be used as a superdisintegrant in the formulation of fast-dissolving tablets. Fast-dissolving tablets of ibuprofen were formulated by employing starch glutamate as a superdisintegrant showed good tablet properties and showed an increased dissolution efficiency of the drug. Among all the formulations (F1–F8), the formulation F4 which contains 5% starch glutamate and 5% croscarmellose sodium as superdisintegrants showed 99.7±0.34% drug dissolution within 5 min. Peak plasma concentration of optimized formulation F2 was achieved in a short period of time and increased relative bioavailability and F2 was found to be stable during accelerated stability testing as per the ICH stability guidelines.
 Conclusion: From drug-excipient compatibility studies, disintegration time, in vitro dissolution studies, and pharmacokinetic studies, it was concluded that starch glutamate can be used as a superdisintegrant in the formulation of fast-dissolving tablets to increase the solubility as well as bioavailability of the poorly soluble drugs.

Formulation-Development and In-Vitro-In Vivo Evaluation of Gastroretentive Floating Tablet Incorporating Clarithromycin

The objective of the work is to summarize the applicability, manufacturing possibilities, excipients and the types of floating drug delivery systems and to optimize a floating, mucoadhesive system using Clarithromycin as the drug aiming at the eradication of Helicobacter pylori having desired floating and drug release properties based on preliminary excipient examination. Direct compressed (DC) tablet was chosen as dosage form being a cost-effective technology for pharmaceutical industry requiring fewer procedures. Before the implementation of the pharmaceutical technological aims, analysis of critical factors influencing the manufacture was carried out. Reproducible manufacturing processes are required to achieve suitability and tablets uniformity to achieve the uniform properties of tablets, which could influence experimental parameters. Ishikawa diagram evaluation was created, which is a commonly used graphical method to identify factors resulting in an overall effect on product design and quality imperfection. The aim was to reveal affecting factors on uniformity of DC tablets in order to standardize all possible conditions and adjustments. Critical factors are indicated separately in particular method sections.
 Keywords: H. pylori, Clarithromycin, Floating Tablets, In Vitro Evaluation, In Vivo Evaluation.

A Novel Framework to Aid the Development of Design Space across Multi-Unit Operation Pharmaceutical Processes-A Case Study of Panax Notoginseng Saponins Immediate Release Tablet.

The fundamental principle of Quality by Design (QbD) is that the product quality should be designed into the process through an upstream approach, rather than be tested in the downstream. The keystone of QbD is process modeling, and thus, to develop a process control strategy based on the development of design space. Multivariate statistical analysis is a very useful tool to support the implementation of QbD in pharmaceutical process development and manufacturing. Nowadays, pharmaceutical process modeling is mainly focused on one-unit operations and system modeling for the development of design space across multi-unit operations is still limited. In this study, a general procedure that gives a holistic view for understanding and controlling the process settings for the entire manufacturing process was investigated. The proposed framework was tested on the Panax Notoginseng Saponins immediate release tablet (PNS IRT) production process. The critical variables and the critical units acting on the process were identified according to the importance of explaining the variability in the multi-block partial least squares path model. This improved understanding of the process by illustrating how the properties of the raw materials, the process parameters in the wet granulation and the compaction and the intermediate properties affect the tablet properties. Furthermore, the design space was developed to compensate for the variability source from the upstream. The results demonstrated that the proposed framework was an important tool to gain understanding and control the multi-unit operation process.

FORMULATION AND EVALUATION OF COLON TARGETED MATRIX TABLETS CONTAINING EXTRACT OF SOLENOSTEMMA ARGEL (HARGEL)

The objective of the present study is to formulate colon targeted matrix tablets containing Solenostemma argel extract using guar gum alone or in combination with either HPMC K15M, with Eudragit S100, or with both them. The Hargel colon targeted matrix tablets were prepared by wet granulation method. The prepared matrix tablets were evaluated for the weight variation, hardness, friability, and in-vitro drug release study in three different media. The formulations showed compliance with pharmacopial standards except that containing guar gum alone. There was no interaction between drug, polymer and other excipients. It was confirmed by FTIR studies. Among the formulations, GHE2 (i.e. containing triple polymer mixture) showed good results in release retardation and other physicochemical properties of matrix tablets when compare to other formulations. The optimum formulation (GHE2) was stable when it was stored at 450/75% RH for 3 months. The formulation GHE2 was considered the most suitable formula for targeted the colon.

Benefits of Fractal Approaches in Solid Dosage Form Development.

Pharmaceutical formulations are complex systems consisting of active pharmaceutical ingredient(s) and a number of excipients selected to provide the intended performance of the product. The understanding of materials' properties and technological processes is a requirement for building quality into pharmaceutical products. Such understanding is gained mostly from empirical correlations of material and process factors with quality attributes of the final product. However, it seems also important to gain knowledge based on mechanistic considerations. Promising is here to study morphological and/or topological characteristics of particles and their aggregates. These geometric aspects must be taken into account to better understand how product attributes emerge from raw materials, which includes, for example, mechanical tablet properties, disintegration or dissolution behavior. Regulatory agencies worldwide are promoting the use of physical models in pharmaceutics to design quality into a final product. This review deals with pharmaceutical applications of theoretical models, focusing on percolation theory, fractal, and multifractal geometry. The use of these so-called fractal approaches improves the understanding of different aspects in the development of solid dosage forms, for example by identifying critical drug and excipient concentrations, as well as to study effects of heterogeneity on dosage form performance. The aim is to link micro- and macrostructure to the emerging quality attributes of the pharmaceutical solid dosage forms as a strategy to enhance mechanistic understanding and to advance pharmaceutical development and manufacturing processes.

Pharmacokinetic profile of ivabradine hemisulfate sustained-release tablets administered in Chinese healthy volunteers: An open-label, randomized, single-dose, three-period crossover study.

We aimed to determine the pharmacokinetics and safety of three single oral doses (5, 10 and 15 mg) of ivabradine hemisulfate sustained-release tablets in healthy Chinese volunteers. A total of 12 volunteers (six males and six females) were randomized to receive a single oral dose of ivabradine hemisulfate sustained-release tablets 5, 10 or 15 mg, with a 1-week washout between periods. Blood samples were collected at regular intervals from 0 to 48 h after drug administration, and the concentrations of ivabradine and N-desmethyl ivabradine were determined by HPLC-tandem mass spectrometry. Pharmacokinetic parameters were estimated by non-compartmental analysis. After administering single doses of 5, 10 and 15 mg, the mean maximum concentration (Cmax ) levels of ivabradine were 4.36, 7.29 and 12.62 ng/mL, and the mean area under the curve from time 0 to 48 h (AUC0-48 ) values were 55.66, 101.16 and 182.09 h·ng/mL, respectively. The mean Cmax levels of N-desmethyl ivabradine were 1.05, 2.03 and 3.16 ng/mL, and the mean AUC0-48 values were 20.61, 39.44 and 65.72 h·ng/mL, respectively. The median time of maximum concentration (Tmax ) levels of ivabradine and N-desmethyl ivabradine were 5 h for all three doses tested. The pharmacokinetic properties of ivabradine hemisulfate sustained-release tablets were linear at doses from 5 to 15 mg. Ivabradine hemisulfate sustained-release tablet appears to be well tolerated in these healthy volunteers.

The influence of different mechanical stress on the release properties of HPMC matrix tablets in sucrose-NaCl media

Four types of HPMC matrix tablets were studied to investigate the influence of mechanical stress on matrix behaviour using biorelevant in vitro dissolution model, the glass bead device (GBD) and paddle apparatus (USP2), in media with various concentrations of sucrose and NaCl. High or low viscosity grade HPMC was incorporated in the matrix with soluble (lactose) and insoluble (microcrystalline cellulose) diluent. The composition of the tablets and dissolution media were selected based on available literature data, with the intention of providing a sensitive system to reflect differences in hydrodynamics and mechanical stress generated by dissolution apparatuses. Between the GBD and USP2 no substantial differences were demonstrated in low concentration media. The differences were induced in high concentration media; compared to USP2 a higher drug release was observed in GBD for each matrix type. Due to solutes in the media an incoherent gel layer is formed and therefore the matrices are more prone towards the hydrodynamic and mechanical stress of dissolution method, suggesting that motion on the surface of glass beads is an important parameter that affects the removal of the gel layer. In critical media where formation of the functional gel barrier might be compromised, the use of GBD could provide additional insight into the drug release behaviour of the matrix tablet.

Studying the Release Characteristics of Naproxen Sustained Release Matrix Tablet Using Natural Polyelectrolytes

Aim: This work involves studying the release characteristics of naproxen sustained release matrix tablet using natural polyelectrolytes and studying some variables affecting the formulation such as the effects of (PEC formation, polymer-polymer ratio, anionic polymer type, molecular weight of CS, type and amount of diluent) on the release rate of naproxen. Methods: Sixteen formula were prepared using direct compression with 500 mg total tablet weight. The release properties of naproxen sustained release matrix tablets were investigated using USP dissolution apparatus I (basket). FT-IR spectra of the complexes were studied to indicate the interactions between polyions. Results: The results showed that the release rate of naproxen was decreased in the formulas that contains PEC comparing to the formulas with single polymer. The formula containing CSh: SA prepared in the ratio of (3:1) showed the slowest release rate (68.17% of naproxen in 7 hr) and extended the release up to 15 hr. It was seen that the formula containing CSh: XG in 3:1 ratio formed the strongest PEC and the release rate extended up to 20 hr. On the other hand changing the molecular weight of CS from high to low and the type of diluent from lactose monohydrate to MCC showed a non-significant increase in the release rate. Conclusion: Polyelectrolyte complex prepared from cationic polymer CS and anionic polymer of SA, XG and CG physical mixtures was successfully formed. Formula 13 formed the strongest PEC with a ratio of CS: XG equal to (3:1) which extended the release up to 20 hr.

Importance of free water in controlling granule and tablet properties in a novel granulation method, green fluidized bed granulation (GFBG).

In the pharmaceutical field, green fluidized bed granulation (GFBG) is a novel and eco-friendly manufacturing technology used to produce desired granules via simple blending and spraying steps at ambient temperature using a standard fluidized bed granulator. However, the relations between water content and granule and tablet qualities have not yet been elucidated for GFBG. The purpose of this study was to elucidate the influence of different water quantities used in the GFBG process on granule and tablet qualities. In addition, results from the GFBG process were compared with those from the moisture-activated dry granulation (MADG) process. In terms of tablet tensile strength and disintegration time, GFBG had a wider acceptable range for added water quantity (2.0-5.0%) than did MADG. For all added water quantities, the GFBG granules were within the upper limit of water activity (a surrogate of free water amount), which was 0.61 for tensile strength and 0.55 for disintegration time. The air flow in the GFBG process may have reduced the excess free water on the granules during the absorption process. It was concluded that as compared with MADG, GFBG may be a more robust process for manufacturing granules and tablets with superior properties.

Combination of a hot-melt subcoating and an enteric coating for moisture protection of hygroscopic Sennae fructus tablets

The objective of this study was to investigate the efficiency of moisture protection of hot-melt coatings solely and in combination with an enteric coating on hygroscopic tablet cores containing a spray-dried Sennae fructus extract. Tablet cores were subcoated with different hot-melt coating materials: medium chain tryglycerides, stearic acid, Precirol® ATO 5, and Compritol® 888 ATO, at varying amounts and coated with Eudragit® L 30D-55 for enteric resistance. Subcoating penetration, tablet disintegration, dissolution times, tablet hygroscopicity, and tablet properties such as weight, height, diameter, and hardness were analyzed. 3 mg/cm2 of tablet surface seemed to be sufficient if sustained release is not required. Thereby, hot-melt coating did not adversely affect the tablet properties with regard to subsequent processing steps. Compared to the tablet cores it was possible to reduce the moisture uptake by 85% at 75% relative humidity with tablets coated with a combination of Precirol® ATO 5 and Eudragit® L 30D-55. This combination was more efficient than high amounts of Eudragit® L 30D-55. Hot-melt coating proved to be a suitable technique for the application of subcoating material to tablet cores serving as a barrier against water permeation into hygroscopic tablet cores without exceeding the required disintegration times.