Concentration Of Magnesium Stearate Research Articles

The Design and Optimization of Fast-dissolving Oral Drug Delivery System (ODDS) of Valproic Acid (VLA) an Anti-epileptic Category Drug

Objective: Develop and optimize a fast-dissolving oral drug delivery system (ODDS) for Valproic acid (VLA), an anti-epileptic drug, using Design of Experiments (DoE). Methodology: DoE, a powerful tool for optimizing formulations, was employed to investigate the impact of various factors on the dissolution rate of VLA ODDS. Key factors studied included superdisintegrants (sodium starch glycolate, crospovidone), diluents (lactose, microcrystalline cellulose), and lubricants (magnesium stearate). A Box-Behnken design was used to create experimental runs, and the dissolution rate at 30 minutes was chosen as the response variable. Results: The DoE analysis revealed significant interactions between factors affecting the dissolution rate. The formulation containing sodium starch glycolate, lactose, and low magnesium stearate concentration exhibited the fastest dissolution rate (Q30 > 85% in 10 minutes). Conclusion: This study successfully designed and optimized a fast-dissolving ODDS for VLA using DoE. The optimized formulation offered rapid drug release, potentially improving patient compliance and therapeutic efficacy. This approach demonstrates the effectiveness of DoE in optimizing pharmaceutical formulations for enhanced performance. The findings indicated that the RSM was effectively utilized in developing valproic acid fast dispersible tablets, thus representing a significant progress in the treatment of epileptic seizures.

Study of compaction tools and parameters on critical quality attributes of high drug load minitablets

Minitablets are prepared using multiple die openings and multi–tip punches for greater productivity. With multiple tips on the punch barrel, the overall compaction force to be applied is commonly estimated by multiplying the desired compaction force per tip by the number of punch tips. Few researchers have however examined this proportionality and the effects of the number of punch tips and punch face geometry on the critical quality attributes (CQAs) of high drug load minitablets. In this study, the minitablets prepared by multi–tip tools exhibited greater weight variation than those prepared by single–tip tools. Their compaction was accompanied by a longer dwell time that led to a higher minitablet tensile strength and consequently a longer disintegration time. The compaction forces required to achieve a consistent set of minitablet CQAs were not directly proportional to the number of punch tips used. In comparison, the effect of punch face geometry was negligible. Increasing concentration of magnesium stearate (as lubricant) from 0.75 to 1.25 %, w/w reduced weight variation, especially of minitablets prepared by the multi-tip tools. It also increased the disintegration time but had no significant effect on the tensile strength of the minitablets regardless of type of tools used. The adjustment of compaction speed was an effective compensatory method to mitigate the differences in dwell time and tensile strength between minitablets prepared by single–tip and multi–tip standard concave tools. A larger reduction in compaction speed of the single-tip tools was required at higher compaction pressures.

Lubricant Sensitivity of Direct Compression Grades of Lactose in Continuous and Batch Tableting Process.

Modern pharmaceutical manufacturing based on Quality by Design and digitalisation is revolutionising the pharmaceutical industry. Continuous processes are promoted as they increase efficiency and improve quality control. Compared to batch blending, continuous blending is easier to scale and provides advantages for achieving blend homogeneity. One potential challenge of continuous blending is the risk of over-lubrication. In this study, blending homogeneity and lubricant sensitivity are investigated for both batch and continuous processes. Given their distinct chemical structures and morphologies, anhydrous lactose and granulated lactose are expected to exhibit varying sensitivities to changes in process settings across both technologies. The findings suggest that both lactose grades provide highly stable blends that can be safely utilised in both batch and continuous modes. Optimisation should focus on process variables, such as the quality of loss-in-weight feeders used for dosing low doses of ingredients. The most significant process parameter for lubricant sensitivity was the type of lactose used. Anhydrous lactose produced harder tablets than the more porous granulated lactose but was more sensitive to lubrication at the same settings. The magnesium stearate content and its interaction with the type of lactose are also critical factors, with magnesium stearate having a counterproductive impact on tabletability.

Exploring the influence of magnesium stearate content and mixing modality on the rheological properties and in vitro aerosolization of dry powder inhaler

Since carrier-based dry powder inhalers (DPIs) suffer from inadequate drug deposition in the lung, an increasing number of marketed products have added magnesium stearate (MgSt) to improve the aerosolization, dispersion, and stability against moisture of DPI. However, for carrier-based DPI, there is a lack of examination of the optimal MgSt content as well as the mixing modality, and there is also a need to verify the applicability of rheological properties to predict the in vitro aerosolization of DPI formulations containing MgSt. Therefore, in this work, DPI formulations were prepared using fluticasone propionate as a model drug and commercial crystalline lactose Respitose® SV003 as a carrier within 1% MgSt content, the effect of MgSt content on the rheological and aerodynamic properties were investigated. After the optimal MgSt content was determined, the effects of mixing modality, mixing order, and carrier size on formulation properties were further investigated. Meanwhile, correlations were established between rheological parameters and in vitro drug deposition parameters, and the contribution of rheological parameters were determined using principal component analysis (PCA). The results showed that the optimal content of MgSt in DPI formulations is 0.25%-0.5% under both high-shear and low-shear, using medium-sized carriers (D50 around 70 μm) and low-shear mixing are beneficial for improving in vitro aerosolization. Good linear relationships between powder rheological parameters such as basic flow energy (BFE), specific energy (SE), Permeability and fine particle fraction (FPF) were established, PCA showed that both flowability and adhesion are key properties affecting FPF. In conclusion, both MgSt content and mixing modality can influence rheological properties of the DPI, which can be used as a screeing tool for DPI formuluation and preparation process optimization.

Optimasi Formulasi Tablet Lepas Lambat Ekstrak Seledri (Apium graveolens L.) Menggunakan Polimer Xanthan Gum dan Lubrikan Magnesium Stearat dengan Metode Simplex Lattice Design (SLD)

Antihypertensive drugs undergo first-pass metabolism and therefore have low oral bioavailability. It causes an increase in the frequency of drug use and concentration fluctuations that affect patient comfort. The sustained release tablet formulation was chosen because it can deliver the active substance with good bioavailability. An active antihypertensive substance that can be used is celery extract because it contains flavonoids, so a sustained release tablet formulation was made using xanthan gum and magnesium stearate to produce a constant and controlled release rate. This study aims to knowing the results of celery extract sustained release tablet evaluation using different concentrations of xanthan gum and magnesium stearate, and also obtains the optimal formulation. The manufacture of tablets uses the direct compression method. Powder evaluations include flow property through a funnel, angle of repose, compressibility index, and moisture content. Tablet evaluations include organoleptic, weight uniformity, size uniformity, hardness, friability, disintegration time, and dissolution tests. The evaluation results data were analyzed using Simplex Lattice Design. The powder evaluation result of all formulations meets the requirements of flow property through a funnel, angle of repose, compressibility index, and moisture content. Physical evaluation of the tablets shows all formulations meet the requirement of weight uniformity, hardness, and friability tests. On the size uniformity test, all formulations do not meet the requirement. The disintegration time test results show that F1 does not meet the requirement. Meanwhile, the dissolution test results show that F4 is the best formula because it shows constant and controlled release rate. Based on analyzed using Simplex Lattice Design, the F4 is the most optimal formula with xanthan gum 52 mg and magnesium stearate 3 mg.

A compactibility-based lubricant dispersion model describing the effect of formulation and paddle speed

In rotary tablet presses, the powder flow into the dies is typically facilitated by paddle feeder. For internally lubricated formulations, the shear forces exerted by the paddle rotation can result in a considerable decrease in tablet strength due to the dispersion of lubricant agglomerates. Available models to describe the lubricant dispersion in paddle feeder allow only a limited quantitative description and transferability of the process. This study introduces an empirical dispersion kinetic which is able to precisely describe the reduction of compactibility due to the shear stresses inside the paddle feeder, even for inhomogeneously flowing material. Additionally, by blending different grades of magnesium stearate at three levels of lubricant concentration with two different grades of microcrystalline cellulose, the impact of bulk properties on the lubrication dispersion in the feed frame was investigated. It was shown, that for a given formulation, the kinetics of compactibility reduction are comparable for different magnesium stearate concentrations. Additionally, the bulk properties of the applied magnesium stearate grade critically affect the dispersion kinetics as well as the maximum compactibility reduction inside the feed frame. In summary, the developed model represents a meaningful extension of the currently available process models for pharmaceutical tablet lubrication.

FORMULATION DEVELOPMENT AND EVALUATION OF IMMEDIATE RELEASE TABLET OF PARACETAMOL AND ORPHENADRINE CITRATE BY DIRECT COMPRESSION METHOD

The objective of this research work was to formulate, develop and evaluate immediate release tablet of paracetamol and orphenadrine citrate by direct compression method. Paracetamol which is antipyretic and orphenadrine citrate is skeletal muscle relaxant. The drug paracetamol and orphenadrine citrate was taken and formulated with different concentration of cross-povidone, mannitol, micro-crystalline cellulose, magnesium stearate and talc. Where cross-povidone as a superdisintegrant, mannitol as diluent, micro-crystalline cellulose as binder, magnesium stearate as lubricant and talc as a glidant used. the preformulation parameters such as bulk density, tapped density, compressibility index and hausner’s ratio were analysed. The thickness, hardness, friability, weight variation, disintegration time & drug content uniformity was evaluated. the in-vitro drug release studied were performed in the usp type (ii) paddle using 0.1N HCl as a dissolution media at 75 rpm speed and temperature of 37±0.5ºC. The % drug release at different time interval was estimated using UV method. Based on the evaluation result f9 trial was selected as the best formulation. The in-vitro drug release profile of the drugs was compared with marketed reference product. All the evaluated result was found to be satisfied with the reference products.

FORMULATION AND EVALUATION OF THYROID HORMONE(T3) IMMEDIATE RELEASE TABLETS

The study was aimed to formulate and evaluate Thyroid hormone (T3) immediate release tablets of a model Reference Listed Drug (RLD). The objective was to develop a cost effective immediate release tablet formulation and to optimize the formula in product development same that of the reference product. The ingredients used were API (thyroid hormone), lactose monohydrate (diluent), acacia (binder), maize starch (disintegrant), sodium chloride (alkalinizing agent) and magnesium stearate (lubricant). The concentration of maize starch and magnesium stearate were altered to reach the objective. Totally five formulations (F1 - F5) were prepared by direct compression method. The plan of work involved involved in the study was1 Selection of drug and excipients, 2Physico–chemical characterization and drug identification, 3Preformulation parameters of the drug, 4Pre–compression parameters for the tablet blend, 5Formulation and development of the tablet dosage form, 6Post compression parameters of the tablet and 7Stability study. The stability studies were performed as per ICH guidelines. Among all the formulations F5 was found to be the best as it showed better results than the other formulations. In vitro disintegration time and percentage drug release results shown satisfactory results. Stability study results showed no significant changes in the formulation. Keywords: Thyroid hormone (T3), Immediate release tablets, Direct compression, Dissolution.

Formulation Development and Evaluation of Doxofylline Sustained-Release Tablets by Using Chitosan and Guar Gum

The sustained-release dosage form is a well-characterized and reproducible dosage form that is designed to control drug release profile at a certain rate to reach desired drug concentration in blood plasma or at the target site. There is immense demand in the market for new sustained-release formulations used for new drug molecules which release the drug at a sustained rate. Doxofylline is one of the widely useful drugs in the market and needs to be given in a single dose for a long duration of time. For the same, we have prepared a sustained released Doxofylline tablet.
 Aim: This research was done to design, formulate and evaluate Doxofylline sustained-release tablets by using different concentrations of Chitosan and Guar Gum. 
 Methods: The factorial design was used to prepare Doxofylline sustained-release tablet. Doxofylline sustained-release tablets were prepared to employ different concentrations of Chitosan, Guar Gum, Lactose, and Magnesium Stearate in different combinations by wet granulation technique. Total 9 formulations were designed, formulated, and evaluated for the hardness, thickness, friability, % drug content, and in-vitro drug release.
 Results: A study of the release of drug by in-vitro found that F8 is to be the best efficient formulation which consists of both Chitosan and Guar Gum helped in delayed the release of drug up to 24 hours and performs excellent release of drug in starting hours of drug release in the body. The drug released from the F8 formulation indicates the kinetic model of First Order, by anomalous diffusion. The formulation F8 shows optimum thickness, hardness and at 40ºC±2 99.35% drug release after 24 hours shows optimum formulation. 
 Conclusion: This study concludes that better drug release was observed by using natural polymers. Doxofylline with natural polymer shows good release and better dissolution rate as compared with a single synthetic polymer. Synthetic drug with natural polymer shows more future scope and this work will help the researcher in the future.

A QbD assisted modified release formulation of Midodrine Hydrochloride for management of long-term hypotension

Midodrine Hydrochloride (MDH) is primarily utilized for the treatment of orthostatic hypotension. The main objective of this research work is to study the effect of the ratio of Methocel 4M to 100M, PVP K-30, and magnesium stearate in extended-release (ER) layer of bilayer tablets of MDH. Bilayer tablets of MDH were optimized by the design of experiment (DoE) using response surface face centre (α = 1), the central composite design having three independent variables at three levels. Bilayer tablets of MDH were administered once a day to reduce dosing frequency and improve patient compliance. Midodrine Hydrochloride tablets contain a drug layer and extended-release layer, which is further compressed into bilayer tablets. Based on the results of in-vitro %drug release it can be concluded that the ratio of Methocel 4M to 100M in MDH bilayer tablets shows a significant impact on % drug release whereas the concentration of PVP K-30 and concentration of magnesium stearate does not shows significant impact on % drug release. As the increase in the ratio of Methocel 4M to 100M, increase in the % drug release and as a decrease in the ratio of Methocel 4M to 100M, decrease in the % drug release. The optimized formulation of MDH bilayer tablets with 6% of Methocel 4M as an extended-release polymer, 24% of Methocel 100M as an extended-release polymer, 5% of PVP K-30 as a binder and 0.5% of magnesium stearate as a lubricant exhibits extended drug release up to 12 hours.

The Effects of Lubricants on the Disintegration and Dissolution Profile of Metronidazole Tablets Formulated Using Sida acuta Gum as a Binder

Aims: This research was done to study the effects of types and concentrations of lubricants on the dissolution and disintegration profile of metronidazole tablets formulated using Sida acuta gum as a binder.
 Methodology: Sida acuta gum (SAG) was extracted from powdered dried leaves of Sida acuta. Metronidazole granules were produced by wet granulation technique using different concentrations (1 and 2%) of SAG as a binder and mixed with different concentrations (0.5, 1.0, and 1.5%) of magnesium stearate (MS) or sodium lauryl sulphate (SLS) as a lubricant. The granules/lubricant -mix was compressed into tablets and evaluated for hardness, weight uniformity, drug content, disintegration time, friability and in vitro drug release.
 Results: The hardness for the tablets was from 4.08 to 7.97 Kgf. The friability was from 0.02±0.45 to 3.40±0.43%. Tablets from formulations A1-A3, B2, and B3 failed the friability test. Formulations prepared with 1% SAG were more friable than those formulated with 2% SAG. Disintegration time for formulations A1-A3 (1% SAG + MS) ranged from 19.07 to 63.5 min, while that of A4-A6 (2% SAG + MS) was from 39.06 to 81.48 min. Formulations B1-B3 (1% SAG + SLS) had disintegration time that ranged from 4.22 to 6.8 min while that of B4-B6 (2% SAG + SLS) was from 9.35 to 15.90 min. The % drug release at 60 min for formulations that contained SAG and MS was 76.60-104.28% and SAG and SLS was 99.89-101.35%
 Conclusion: Metronidazole tablets formulated using SLS as lubricant disintegrated faster than those formulated using magnesium stearate as lubricant. Percentage drug release from tablets containing SLS was slightly higher than those that contained magnesium stearate. Higher concentrations of the lubricants produced softer tablets.

EFFECT OF VARIATION OF LUBRICANT CONCENTRATION (MAGNESIUM STEARATE) ON THE PHYSICAL QUALITY OF METOCLOPRAMID HCl TABLETS WITH DIRECT PRINTING METHOD

Metoclopramide HCl is used to relieve nausea and vomiting. Market availability in the form of tablets, syrup and injection. The most preferred drug use by patients is oral medication because of its ease of use. Chewable tablets are a new product as an alternative for treatment in pediatric and adult patients who have difficulty swallowing drugs. This study aims to formulate the chewable tablet preparations of metoclopramide HCl using variations in lubricant concentrations. The variations of magnesium stearate with concentrations of 1%, 2%, and 3% using the direct printing method made to obtain a better physical quality test including organoleptics, weight uniformity, uniformity of size, tablet hardness, tablet brittleness, tablet crush time, uniformity of content. The results of the physical quality test were statistically analyzed using one way ANOVA to determine the effect of variations in the concentration of lubricants on the characteristics of chewable tablets. The results showed that variations in the concentration of magnesium stearate lubricant in the manufacture of metoclopramide HCl chewable tablets had an effect on the physical quality of metoclopramide HCl chewable tablets. The concentration of magnesium stearate which produces metoclopramide HCl chewable tablets with good physical properties is 2%.

A New Flame AAS Application for Magnesium Determination in Solid Pharmaceutical Preparations as an Active Ingredient and an Excipient

Objective: A new application of Atomic Absorption Spectroscopy (AAS) has been carried out to determine magnesium in its solid preparations (effervescent and uncoated compressed tablets) as an active ingredient and/or excipient.
 Methodology: The linear range of magnesium was determined. A sample of magnesium effervescent tablets was analyzed. Magnesium stearate concentration was also indirectly determined in commercial paracetamol tablets using two digestion methods. Finally, a sample of drug-free tablets (only contain excipients) was analyzed to study the effect of talc on total magnesium content of the sample.
 Results: Linear range was observed in concentrations between 0.08-0.40 ug/mL of magnesium. Effervescent tablets samples were recovered in the range between 98.66-103.00% which indicates that the product meets specifications. For paracetamol tablets, the content of magnesium stearate was in average of 0.2% and there is no differences between the two digestion methods (t=0.454). Our work on the drug-free sample proved a significant increase of magnesium concentrations in the presence of talc.
 Conclusion: The AAS method is a simple and rapid technique that can be employed for the simultaneous estimation of magnesium in in-process and final products analyses.

Evaluation of an external lubrication system implemented in a compaction simulator.

The internal blending of magnesium stearate is often associated with decreasing tensile strengths and longer disintegration and dissolution times. Therefore, external lubrication has gained interest in the pharmaceutical industry as these negative effects could be minimized using this method. In this study, an external lubrication system implemented in a compaction simulator was investigated. The influence of 2 process parameters related to the external lubrication system, spraying time and atomizing pressure, on the responses was studied using 4 common fillers and 2 model drugs. While the parameters of the external lubrication system had a significant impact on the ejection forces, no negative effect was observed on the tensile strength and disintegration time as similar values were obtained compared to non-lubricated experiments. Moreover, equal or lower ejection forces were obtained for external lubrication using a lower concentration of magnesium stearate compared to internal lubrication, where a decrease in tensile strength and prolonged disintegration was noticed for most formulations. The observed results could be correlated to the wall friction angle, compaction properties and tablet brittleness index of the raw materials and blends. This study showed the potential of external lubrication as an alternative lubrication method for lubricant-sensitive formulations.

Evaluation of the Disintegration Action of Soy Polysaccharide by Image Analysis.

Here we investigated the disintegration action of the natural superdisintegrant soy polysaccharide (SP) and benchmarked it against sodium starch glycolate (SSG) and crospovidone (XPVP). Kinetics and mechanism of disintegration of various tablet formulations were monitored using a USB microscope connected to a computer, followed by image analysis. SP acts mainly by a swelling mechanism and it is most effective at concentrations of 4-8%. Its disintegration action is comparable with that of SSG and XPVP, in most cases. However, SP underperforms compared with these superdisintegrants, in extremely hard tablets containing a hydrophobic component. Moreover, it is more negatively affected by the concentration of magnesium stearate than SSG and XPVP. The disintegration action of SP is not affected by pH and ionic strength of the medium, but it is compromised by the presence of ethanol. This indicates that the concomitant administration of alcoholic beverages might hamper the disintegration of SP-containing tablets. Overall, SP is a promising tablet disintegrant for pharmaceutical and nutraceutical products.

Solving manufacturing problems for L-carnitine-L-tartrate to improve the likelihood of successful product scale-up.

L-carnitine-L-tartrate, a non-essential amino acid, is hygroscopic. This causes a problem in tablet production due to pronounced adhesion of tablets to punches. A 33 full factorial design was adopted to suggest a tablet formulation. Three adsorbents were suggested (Aerosil 200, Aerosil R972, talc) to reduce stickiness at three concentrations (1, 3 and 5 %), and three fillers (mannitol, Avicel PH 101, Dibasic calcium phosphate) were chosen to prepare 27 formulations. Micromeritic properties of formulations were studied, and tablets were prepared by wet granulation. Absence of picking, sticking or capping, recording of sufficient hardness, acceptable friability and tablet ejection force indicated formulation success. The resulting formulation prepared using Avicel PH 101 and 1 % Aerosil 200 was submitted to further investigation in order to choose the most suitable compression conditions using a 33 full factorial design. Variables included compression force, tableting rate and magnesium stearate (lubricant) concentration. The formulation prepared at compression force of 25 kN, using 2 % magnesium stearate, at a production rate of 30 tablets/ minute, was found to be the most appropriate scale up candidate.

Characterizing the powder punch-face adhesive interaction during the unloading phase of powder compaction

The objective of this work is to measure the adhesive force profile between a punch face and powder compact in-die during the decompression phase of a tablet compaction process. An instrumented punch was developed for use on a single station compaction fixture mounted on a universal testing machine. Adhesive force-displacement profiles were measured for acetaminophen, ibuprofen, lactose, mannitol, several grades of micro-crystalline cellulose, and blends containing magnesium stearate as a lubricant. The degree of compact solid fraction, the number of compacts produced in a row, and concentration of magnesium stearate in the blends affected the adhesive force profiles. The maximum adhesive force increased with increasing compact solid fraction and decreasing magnesium stearate concentration. An increase in the number of compression cycles increased the adhesive force between the powder compact and punch face, but the compression speed did not play a significant role in the adhesive interaction, at least over the range of speeds examined in the current work.

Investigation into the Manufacture and Properties of Inhalable High-Dose Dry Powders Produced by Comilling API and Lactose with Magnesium Stearate.

The aim of the study was to understand the impact of different concentrations of the additive material, magnesium stearate (MGST), and the active pharmaceutical ingredient (API), respectively, on the physicochemical properties and aerosol performance of comilled formulations for high-dose delivery. Initially, blends of API/lactose with different concentrations of MGST (1-7.5% w/w) were prepared and comilled by the jet-mill apparatus. The optimal concentration of MGST in comilled formulations was investigated, specifically for agglomerate structure and strength, particle size, uniformity of content, surface coverage, and aerosol performance. Secondly, comilled formulations with different API (1-40% w/w) concentrations were prepared and similarly analyzed. Comilled 5% MGST (w/w) formulation resulted in a significant improvement in in vitro aerosol performance due to the reduction in agglomerate size and strength compared to the formulation comilled without MGST. Higher concentrations of MGST (7.5% w/w) led to reduction in aerosol performance likely due to excessive surface coverage of the micronized particles by MGST, which led to failure in uniformity of content and an increase in agglomerate strength and size. Generally, comilled formulations with higher concentrations of API increased the agglomerate strength and size, which subsequently caused a reduction in aerosol performance. High-dose delivery was achieved at API concentration of >20% (w/w). The study provided a platform for the investigation of aerosol performance and physicochemical properties of other API and additive materials in comilled formulations for the emerging field of high-dose delivery by dry powder inhalation.

Application of Terahertz Attenuated Total Reflection Spectroscopy to Detect Changes in the Physical Properties of Lactose during the Lubrication Process Required for Drug Formulation.

Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we used terahertz attenuated total reflection (THz-ATR) spectroscopy to detect differences in the physical characteristics of the lubricated powder. We applied a simple formulation prepared by blending granulated lactose as filler with magnesium stearate as lubricant. A flat tablet was prepared using the lubricated powder to acquire sharp THz-ATR absorption peaks of the samples. First, we investigated the effects of lubricant concentration and compression pressure on preparation of the tablet and then determined the effect of the pressure applied to samples in contact with the ATR prism on sample absorption amplitude. We focused on the differences in the magnitudes of spectra at the lactose-specific frequency. Second, we conducted the dynamic lubrication process using a 120-L mixer to investigate differences in the magnitudes of absorption corresponding to the lactose-specific frequency during lubrication. In both studies, enriching the lubricated powder with a higher concentration of magnesium stearate or prolonging blending time correlated with higher magnitudes of spectra at the lactose-specific frequency. Further, in the dynamic lubrication study, the wettability and disintegration time of the tablets were compared with the absorption spectra amplitudes at the lactose-specific frequency. We conclude that THz-ATR spectroscopy is useful for detecting differences in densities caused by a change in the physical properties of lactose during lubrication.

Assessment of Tablet Surface Hardness by Laser Ablation and Its Correlation With the Erosion Tendency of Core Tablets

Surface erosion of uncoated tablets results in processing problems such as dusting and defects during coating and is governed by the strength of particle bonding on tablet surface. In this study, the correlation between dusting tendency of tablets in a coating pan with friability and laser ablation surface hardness was assessed using tablets containing different concentrations of magnesium stearate and tartaric acid. Surface erosion propensity of different batches was evaluated by assessing their dusting tendency in the coating pan. In addition, all tablets were analyzed for crushing strength, friability, modified friability test using baffles in the friability apparatus, and weight loss after laser ablation. Tablets with similar crushing strength showed differences in their surface erosion and dusting tendency when rotated in a coating pan. These differences did not correlate well with tablet crushing strength or friability but did show reasonably good correlation with mass loss after laser ablation. These results suggest that tablet surface mass loss by laser ablation can be used as a minipiloting (small-scale) tool to assess tablet surface properties during early stages of drug product development to assess the risk of potential large-scale manufacturing issues.