Lactose Tablets Research Articles

The interplay of brain neurotransmission and mental fatigue: A research protocol.

Mental fatigue (MF) significantly affects both cognitive and physical performance. However, the precise mechanisms, particularly concerning neurotransmission, require further investigation. An implication of the role of dopamine (DA) and noradrenaline (NA) is stated, but empirical evidence for this theory still needs to be provided. To address this gap, we aim to investigate the role of brain neurotransmission in elucidating if, and how prolonged cognitive activity induces MF and its subsequent impact on cognitive performance. This study (registration number: G095422N) will adopt a randomized cross-over design with sixteen healthy participants aged 18-35 years. The sessions include a familiarization, two experimental (DA: 20mg Methylphenidate; NA: 8mg Reboxetine) conditions, and one placebo (lactose tablet: 10mg) condition. A 60-minute individualized Stroop task will be used to investigate whether, and how the onset of MF changes under the influence of reuptake inhibitors. Attention and response inhibition will be assessed before and after the MF-inducing task using a Go/NoGo task. The integration of physiological (electroencephalography, heart rate), behavioral (attention, response inhibition), and subjective indicators (scales and questionnaires) will be used to detect the underlying mechanisms holistically. Data analysis will involve linear mixed models with significance at p<0.05. The integration of diverse techniques and analyses offers a comprehensive perspective on the onset and impact of MF, introducing a novel approach. Future research plans involve extending this protocol to explore the connection between brain neurotransmission and physical fatigue. This protocol will further advance our understanding of the complex interplay between the brain and fatigue.

Evaluation of binders in twin-screw wet granulation – Optimization of tabletability

The influence of hydroxypropyl cellulose type (HPC-SSL SFP, HPC-SSL), concentration (2 %, 3.5 %, 5 %) and filler (lactose, calcium hydrogen phosphate (DCP)/microcrystalline cellulose (MCC)) on twin-screw wet granulation and subsequent tableting was studied. The aim was to identify the formulation of the highest tabletability which still fulfills the requirements of the disintegration. Lactose combined with 5 % binder enabled a higher tabletability and a faster disintegration than DCP/MCC. It was found that tabletability of lactose formulations can be increased by higher binder concentration and higher compression pressure while tabletability of DCP/MCC formulations can be only increased by higher compression pressure. It was observed that batches containing DCP/MCC failed the disintegration test, if the highest binder concentration and the highest compression pressure were used. To ensure a fast disintegration, the compression pressure or at least the binder concentration had to be low. Changing the disintegrant and its localization improved the DCP/MCC formulation, resulting in faster disintegration than lactose tablets. However, it also resulted in a lower tabletability. In this study best tablets were achieved with 3.5 % or 5 % binder and lactose as filler. These tablets presented the highest tabletability but still disintegrated in less than 500 s.

Investigations on Compaction Behavior of Kollidon®SR-Based Multi-component Directly Compressed Tablets for Preparation of Controlled Release Diclofenac Sodium.

The physics of tablets mixtures has gained much attention lately. The purpose of this work is to evaluate the compaction properties of Kollidon® SR (KSR) in the presence of different excipients such as Microcrystalline cellulose (MCC), Monohydrous lactose (MH Lactose), Poly (vinyl acetate) (PVA100), and a water-soluble drug Diclofenac sodium (DNa) to prepare once daily formulation. Tablets were prepared using direct compression and were compressed into flat-faced tablets using hydraulic press at various pressures. The combination of MCC and KSR in the tablets showed reduced porosity, and almost constant low Py values as KSR levels increased; also, KSR-DNa tablets had higher percentage porosity and crushing strength values than KSR-MH Lactose tablets. The crushing strengths of KSR-MCC tablets were larger than those of KSR-DNa tablets. Ternary mixture tablets comprised of KSR-MCC-DNa showed decreased porosities and low Py values as the percentage of KSR increased especially at high compression pressures but had higher crushing strengths compared to KSR-DNa or MCC-DNa binary tablets. KSR-MH Lactose-DNa ternary tablets experienced lower porosities and crushing strengths compared to KSR-MCC-DNa tablets. Quaternary tablets of KSR-PVA100-MCC-DNa showed lower porosity and Py values than quaternary tablets obtained using similar proportion of MH Lactose instead of MCC. In conclusion, optimum quaternary tablets were obtained with optimum crushing strengths, relatively low Py, and moderate percentage porosities among all prepared quaternary tablets. The drug release of the optimum quaternary tablets demonstrated similar in vitro release profile compared to that of the marketed product with a mechanism of release that follows Korsmeyer-Peppas model.

Technological Processing of Dried Powdered Rosehips to Tablets Through Wet Granulation

Abstract The pseudo-fruits of Dog Rose are a rich source of L-ascorbic acid and several other active substances, which means their high supportive therapeutic potential. The study aimed to examine the impact of the chosen technological procedure for the preparation of tablets containing rosehip powder on the amount of L-ascorbic acid in the final pharmaceutical form. Drying of the plant drug was performed at room temperature to avoid possible thermal degradation of this heat-sensitive compound. Similarly, drying of the granules after wet granulation in the oven was replaced by natural drying at room temperature. The composition of two types of prepared granule formulations differed in the filler – lactose (LAC) or microcrystalline cellulose (MCC). Apart from the disintegration test, they meet the technological requirements for granules or tablets. Lactose was confirmed as a more suitable filler, which despite the unsuccessful disintegration of the granules, ensures the disintegration of tablets within 15 minutes even without the addition of a special excipient acting as a disintegrant. The content of L-ascorbic acid detected using isotachophoresis – capillary zone electrophoresis was 87.16 ± 5.06 µg in LAC tablets and 63.33 ± 2.83 µg in MCC tablets.

Comparative evaluation of three methods for quantifying tablet brittleness

A low value of deformation before crushing is an obvious and understandable measure of brittleness of materials including tablets. In this article, three methods based on deformation measurement in a flexure tester are compared. The simplest one is a plain measurement of distance from contact or selected start point till fracture. Next the brittle-ductile method (BDI), where the distance is established by normalisation of the force–displacement curve based on the work of failure (WOF). The third method is the tablet brittleness index (TBI) by Gong and Sun, where the reciprocal of a linear distance is proposed as a brittleness quantity. The study is based on data from a previous investigation, where tablets of microcrystalline cellulose and lactose in different combinations and with four different crushing forces were utilised. The investigation shows that the BDI method is preferable. It is easy to compute without data manipulation, the sensitivity to the fracture force is negligible and it provides an independent characteristic of the brittleness of a compacted material.

Evaluation of binders in twin-screw wet granulation – Optimal combination of binder and disintegrant

The influence of localization (intragranular, split or extragranular) of three superdisintegrants (croscarmellose sodium, crospovidone, sodium starch glycolate) on granules and tablets after twin-screw granulation was studied. The aim was to find a suitable disintegrant type and disintegrant localization for lactose tablets manufactured with different hydroxypropyl cellulose (HPC) types. The disintegrants were found to decrease the particle size in granulation, where sodium starch glycolate had the lowest influence. The tablet tensile strength was not influenced strongly by the disintegrant type or localization. By contrast, the disintegration was dependent on the disintegrant type as well as the localization, where sodium starch glycolate performed worst. Intragranular croscarmellose sodium and extragranular crospovidone were identified as beneficial for chosen conditions because a satisfying tensile strength in combination with the fastest disintegration was found. These findings were achieved for one HPC type and the suitability of the best disintegrant-localization-combinations was confirmed for another two HPC types.

Effect of feed frame on lubricant sensitivity during upscaling from a compaction simulator to a rotary tablet press

Internal lubrication can be associated with reduced tabletability. Deformation mechanism, lubricant type, lubricant blending time and paddle speed (PS) of the forced feeder are known to be influenceable factors. This study investigated the effect of lubricant blending time and PS of forced feeders on the tensile strength of lubricated microcrystalline cellulose (MCC) and lactose tablets. Magnesium stearate (MgSt), sodium stearyl fumarate (SSF) and stearic acid (SA) were used as lubricants. Tablets were produced on a compaction simulator and a rotary tablet press to investigate lubricant sensitivity during upscaling. Lubricant sensitivity was found higher for MCC compared to lactose which was attributed to the higher plasticity of MCC. The reduction in tensile strength upon lubricant addition followed the order: MgSt > SSF > SA; which could be linked to particle size, specific surface area and particle shape of the lubricants. Although differences in tensile strength were observed between the lubricant types, comparable ejection forces were obtained. The impact of PS on tensile strength was higher compared to lubricant blending time for both tableting machines. A good correlation of tensile strength and lubricant sensitivity between the compaction simulator and rotary tablet press was observed based on the calculation of paddle passes (NPP).

Porous Lactose as a Novel Ingredient Carrier for the Improvement of Quercetin Solubility In Vitro.

In this work, quercetin was loaded in the highly-porous lactose via the adsorption of quercetin molecules in ethanol. The method aims to improve the quercetin solubility and the loading capacity of lactose. The method relates to the synthesis of the highly-porous lactose with a particle size of ∼35 μm, a mean pore width of ∼30 nm, a BET surface area of 35.0561 ± 0.4613 m2/g, and a BJH pore volume of ∼0.075346 cc/g. After the quercetin loading in ethanol, BET surface area and BJH pore volume of porous lactose were reduced to 28.8735 ± 0.3526 m2/g and 0.073315 cc/g, respectively. The reduction rate was based on the quercetin loading efficiency of highly-porous lactose. DSC analysis and XRD analysis suggest that the sediments of quercetin in the nanopores of porous lactose are crystalline. FTIR spectroscopy results suggest that there is no significant interaction between quercetin and lactose. The highly-porous lactose had a higher loading efficiency of 20.3% (w/w) compared to the α-lactose (with 5.2% w/w). The release rates of quercetin from the highly-porous lactose tablets were faster compared to the conventional α-lactose carrier.

Hydroxychloroquine in Nonhospitalized Adults With Early COVID-19.

LettersMarch 2021Hydroxychloroquine in Nonhospitalized Adults With Early COVID-19FREEAnusuya Bhattacharyya, MBBS, DO, DNB (Ophthalmology), Phulen Sarma, MBBS, MD, DM (Clinical Pharmacology), PDCR, Hardeep Kaur, MSc, Bikash Medhi, MBBS, MD, MAMSAnusuya Bhattacharyya, MBBS, DO, DNB (Ophthalmology)Government Medical College & Hospital, Chandigarh, IndiaSearch for more papers by this author, Phulen Sarma, MBBS, MD, DM (Clinical Pharmacology), PDCRPostgraduate Institute of Medical Education and Research, Chandigarh, IndiaSearch for more papers by this author, Hardeep Kaur, MScPostgraduate Institute of Medical Education and Research, Chandigarh, IndiaSearch for more papers by this author, Bikash Medhi, MBBS, MD, MAMSPostgraduate Institute of Medical Education and Research, Chandigarh, IndiaSearch for more papers by this authorAuthor, Article, and Disclosure Informationhttps://doi.org/10.7326/L21-0001 SectionsAboutVisual AbstractPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissions ShareFacebookTwitterLinkedInRedditEmail TO THE EDITOR: Skipper and colleagues' multicenter trial (1) was conducted in 2 locations (the United States and Canada) with the intention of evaluating the absolute therapeutic efficacy of HCQ in symptomatic, nonhospitalized adults with COVID-19. Patients were randomly assigned to either the HCQ or placebo group. While evaluating the composition of the placebo regimen, we noted that a folic acid tablet, 400 mcg, was used as placebo in the U.S. population and a lactose tablet in the Canadian population.In in silico studies, folic acid acted as a good binder against severe acute respiratory syndrome coronavirus 2 furin (which is required for viral entry to the host cell) (2). In clinical studies, Itelman and associates (3) reported lower blood folic acid levels among patients with severe disease than in their counterparts with mild disease. Pregnant women seem to be less likely to require hospitalization for COVID-19 (4), and Acosta-Elias and Espinosa-Tanguma (4) postulated that folic acid uptake may be the protective factor. Use of Angiovit (Altayvitaminy), an agent containing folic acid and vitamin B12, has been associated with a shorter duration of “hospital stay” and “fever” compared with mainstay therapy (5). Several trials evaluating folic acid as a therapeutic agent in COVID-19 are currently under way (https://clinicaltrials.gov/ct2/show/NCT04354428 and https://covid-19.cochrane.org/studies/crs-15322074).Skipper and colleagues concluded that there was no statistically significant difference in “COVID-19–related symptoms,” “incidence of hospitalization,” and “death” between both groups. This comparable efficacy does not indicate the absolute efficacy of HCQ; rather, it indicates the comparative efficacy between HCQ and folic acid, and both performed equally. Again, rather than describing this trial as “placebo controlled,” it would be better classified as a “head-on” comparison between HCQ and folic acid.

In vivo, ex vivo and in vitro Mucoadhesive Strength Assessment of Potential Pharmaceutical Bio-resource Polymer from Diospyros melonoxylon Roxb seeds

In this study, an oral bio-based mucoadhesive polymer was developed from Diospyros melonoxylon Roxb (Ebenaceae) seed mucilage and evaluated for mucoadhesive strength. The mucilage showed shear stress results (0.140 ± 0.0007N), with comparable adhesiveness to HPMC E5 (0.098 ± 0.0008N). Force of adhesion required to detach the seed mucilage and HPMC E5 tablets from the mucin of intestinal tissue were 0.0509 ± 0.0007 (N) and 0.0049 ± 0.0006 (N). Seed mucilage revealed significant higher detachment time, erosion time, in vitro wash off time and ex vivo residence compared to HPMC E5 and lactose tablets (p&lt;0.01). In vivo test indicated that seed mucilage tablets possessed good mucoadhesive strength compared to HPMC E5 and resisted disintegration for ≤ 8 h. The swelling index and wetting time showed comparable results between the mucilage and synthetic polymer tablets. Mucilage demonstrated high moisture absorption, percentage hydration, and matrix erosion of 20.0 ± 0.037, 53.66 ± 0.127, and 20.00 ± 0.077 compared to HPMC E5 10.0 ± 0.079, 36.00 ± 0.089, and 1.26 ± 0.085. The mucoadhesive properties of seeds mucilage were comparable to guar gum and HPMC E5. Thus, seed mucilage of D. melonoxylon can be exploited for usage as pharmaceutical excipient in oral bioadhesive drug delivery systems.

The relevance of granule fragmentation on reduced tabletability of granules from ductile or brittle materials produced by roll compaction/dry granulation.

Roll compaction/dry granulation often results in loss of tabletability. The two main hypotheses for this are granule hardening and granule size enlargement. The aim of this study was to investigate the effect of granule size, roll compaction force, and granule fragmentation upon tableting and its effect on tabletability of granules constituting a ductile or brittle material. Plastically deforming microcrystalline cellulose (MCC) and fragmenting lactose monohydrate (lactose) were roll compacted at five roll compaction forces ranging from 2 to 16 kN/cm. Granule size fractions of 250-355 and 500-710µm were blended with 10% magnesium stearate (MgSt), compressed into tablets and ground to obtain compressed granules. The predominant deformation behaviour of the particles constituting the granules directly impacted granule deformation upon tableting, as lactose granules fractured extensively upon tableting, whereas MCC granules predominantly deformed by plastic deformation. Increased roll compaction force resulted in more granule hardening of both materials and thereby granules less susceptible to fragmentation upon tableting. Granule hardening accounted for the largest loss of tabletability of MCC granules upon roll compaction. Roll compaction force and granule size had no or negligible effect on tabletability of lactose tablets without MgSt, whereas increased roll compaction force and larger granules decreased tensile strength of tablets containing lactose granules blended with MgSt. This was explained by inter-particle and inter-granular bonds contributing equally to the tensile strength of lactose tablets without MgSt. However, after addition of MgSt, the decreased fragmentation tendency of larger granules compacted at higher roll compaction forces resulted in greater MgSt coverage of the granules upon tableting, thereby decreasing tabletability.

Bio-based Polymer Isolated from Seeds of Buchanania lanzan Spreng with Potential Use as Pharmaceutical Mucoadhesive Excipient

This study was aimed to develop an oral bio-based mucoadhesive polymer from seeds mucilage of Buchanania lanzan spreng, belongs to family anacardiaceae. Isolated mucilage was evaluated for mucoadhesive strength and compared with existing polymer. The mucilage showed shear stress results (0.099 ± 0.0001N), with comparable adhesiveness to methocel E5 (0.098 ± 0.0008N). Force of adhesion required to detach the seed mucilage and methocel E5 tablets from the mucin of intestinal tissue were 0.0276 ± 0.0019 (N) and 0.0049 ± 0.0006 (N), respectively. Seed mucilage revealed significant (P&lt;0.01) higher detachment time, erosion time, in-vitro wash-off time and ex-vivo residence compared to methocel E5 and lactose tablets. In vivo test indicated that seed mucilage tablets possessed good mucoadhesive strength compared to methocel E5 and resisted disintegration for ≤ 8 h. The swelling index and wetting time showed comparable results between the mucilage and synthetic polymer tablets. Mucilage demonstrated high moisture absorption, percentage hydration, and matrix erosion of 18.57 ± 0.036, 50.00 ± 0.051, and 8.30 ± 0.155 compared to methocel E5 10.0 ± 0.079, 36.00 ± 0.089, and 1.26 ± 0.085, respectively. Mucoadhesive properties of seeds mucilage were comparable to guar gum and methocel E5, thus seed mucilage of B. lanzan can be potentially exploited for usage as a bioadhesive pharmaceutical excipient.

Understanding the impact of magnesium stearate variability on tableting performance using a multivariate modeling approach

The objective of this research is to understand how the properties of magnesium stearate (MgSt) affect product performance in a quantitative manner using a multivariate modeling approach. In addition, we explored the feasibility of using NIR and Raman spectra as a surrogate measurement of physiochemical properties in prediction of performance in tablet direct compression. Partial least square models to predict performance attributes (PAs) from MgSt properties or spectra were developed and validated. The model input variables are MgSt physiochemical properties, spectra, key formulation and process parameters. Material physiochemical properties include fatty acid composition, loss on drying, densities, particle size distribution, specific surface area, and solid state properties. The key formulation and process parameters include MgSt concentration, filler type and compression force. The output variables are PAs including tablet ejection force, breaking force and disintegration time. It was found that the prediction of MgSt performance from its properties greatly depends on filler type and PAs of interest. NIR spectra successfully predicted lubricant performance in lactose tablet; however, predictions from Raman spectra were not acceptable. In the cases that the contributing physiochemical properties in performance prediction are sufficiently captured in the spectra, the spectra can be used as an alternative tool to predict excipient performance.

Anti-counterfeiting DNA molecular tagging of pharmaceutical excipients: An evaluation of lactose containing tablets.

The licensed pharmaceutical industry and regulators use many approaches to control counterfeiting, but it remains a very difficult task to differentiate between counterfeit and real products. Moreover, there is a lack of techniques available for providing a batch specific molecular bar code for tablets that has the required traceability, specificity and sensitivity to be fit for purpose. The aim of this study was to evaluate DNA molecular tags as a potential anti-counterfeiting technology in tablets. Lactose tablets (400 mg) were used as a model to investigate incorporation DNA molecular tag into a solid dosage form: DNA authentication was carried out on an Applied DNA SigNify® qPCR instrument. Tablet batches were subjected to accelerated stability conditions (40 °C and 75% RH) for up to 6 months. All batches passed the monograph specifications of the British Pharmacopoeia (hardness, friability and mass uniformity) throughout the storage period. In all of recovery plots, the number of cycles required for DNA detection (Cq values) increased as a function of storage time, which indicated a reduction in tag levels, but it should be noted for all storage experiments the tag was clearly detected. It would appear that DNA molecular tags could feasibly be applied within the pharmaceutical development cycle when a new solid dosage form is brought to the market so as to mitigate the risk and dangers of counterfeiting.

Modified equation for particle bonding area and strength with inclusion of powder fragmentation propensity

The paper considers a novel, modified equation for evaluation of relationship between tablet tensile strength, bonding area and bonding strength with inclusion of fragmentation as particle deformation mechanism. Four types of lactose particles for direct compression were assessed for their micromeritic and mechanical properties (compressibility and compactibility), with particular focus on fragmentation behaviour, bonding area and bonding strength. Compressibility properties were assessed using three established models. Walker and Kuentz-Leuenberger models distinguished lactose plastic properties more effectively in contrast to the Heckel model. Spherical agglomerates of lactose were most prone to fragmentation as determined with the fragmentation propensity coefficient and the number of interparticulate bonds. Fragmentation, together with plastic deformation were found to be the governing factors for tablet tensile strength in α-lactose samples, while high bonding force primarily controlled the tablet tensile strength of anhydrous lactose. Tensile strength of all lactose tablets showed best correlation to the ratio of fragmentation propensity and Walker compressibility coefficient, which is proposed as better deformation index, intended to describe the overall deformation properties of lactose more precisely. A novel expression for determining bonding area is proposed, established on the enhanced deformation index, which includes both plastic deformation and fragmentation as bond formation mechanisms.

Comparative impact of different binder addition methods, binders and diluents on resulting granule and tablet attributes via high shear wet granulation

This study investigated comparative impact of different binder addition methods (pouring, dripping, spraying), binders and diluents on resulting granule and tablet attributes via high shear wet granulation. Lactose monohydrate and mannitol as diluents, and hydroxypropyl methylcellulose (HPMC E5) and polyvinylpyrrolidone (PVP K30) as binders were used. Granules were characterized for morphology, bulk-density, tapped-density, flow, size, segregation-potential and friability. To determine granule friability, procedure described in European Pharmacopoeia was slightly modified to reduce manual-variations and obtain appreciable discrimination between the formulations. Binder-diluent affinity was assessed by measuring contact angles of diluent-dispersion droplets on binder films over a period of time. All blends were pressed at the same compression force and resulting tablets were characterized for pharmacotechnical properties. Results revealed that the binder addition methods altered granule-shape, which predominantly governed the granule flow. The binder addition by spraying increased fines, blend segregation-potential, granule friability, tablet tensile-strength and tablet disintegration-time; binder addition by pouring showed an opposite impact. Mannitol granules exhibited lower bulk density, superior flow, lower segregation-potential and higher friability than their lactose counterparts. Amongst binders, PVP produced more friable granules compared to HPMC. The high polydispersity-index of polymer-binder induced non-homogeneity facilitating the blend segregation-potential. Due to higher affinity, HPMC was suitable binder for mannitol, and PVP for lactose to promote granule growth. The binder-diluent affinity dominated viscosity and surface tension of binder solution to improve granule size. Increase in granule size decreased granule-friability, which subsequently decreased tablet hardness, tensile-strength and disintegration-time. Mannitol produced harder tablets, and lactose tablets disintegrated faster by all binders and binder addition methods.

Efficacy and safety of oral vitamin D (cholecalciferol) supplement therapy in Stage I primary hypertension; a prospective, randomized, double-blind, placebo controlled, clinical trial in a tertiary care hospital in central India.

Introduction : Hypertension is one of the most common cardiovascular disorders. Almost all targets in its therapy are exploited and there is a growing need to search for newer targets. Vitamin D is gaining increasing attention in treatment of primary hypertension. Objectives : To study the efficacy and safety of Vitamin D supplementation on systolic and diastolic BP in patients of primary hypertension (JNC 7 stage I) receiving conventional antihypertensive medications (namely Tab atenolol 50mg or Tab amlodipine 5mg). Methods : It was a prospective, randomized, double blind, parallel, placebo controlled clinical trial with 2 groups of 33 patients each. Both groups had patients receiving conventional antihypertensives (Tab atenolol50mg or Tab amlodipine 5mg). Group A patients were given placebo (lactose tablets) and Group B were given oral Vitamin D 3 (60,000 IU) once weekly at bedtime after meals, repeated every fortnightly for 12 weeks. Results : Patients belonging to Group B showed a statistically significant (p < 0.0001) decline in both systolic blood pressure after 12 weeks of receiving vitamin D supplementation. There was no significant change in the safety parameters. Conclusions : Thus, our study shows that Vitamin D supplementation has some role in safely reducing systolic blood pressure after 12 weeks of supplementation and hence it should be supplemented with antihypertensive drugs to the patients with hypertension.

Efficacy of Silodosin in Expulsive Therapy for Distal Ureteral Stones: A Randomized Double-blinded Controlled Trial.

To evaluate the efficacy of silodosin in the medical expulsive therapy for symptomatic distal ureteral stones. This prospectively randomized controlled trial was carried out from May 2011 to December 2014. In all, 198 patients with radiopaque distal ureteral stones &lt;10 mm in size were eligible: 61 patients in the control group and 62 patients in the silodosin group. The silodosin group received silodosin 8 mg daily, and the control group received lactose tablets. The primary outcome was the expulsion rate. The secondary outcomes the expulsion time, analgesic consumption, lower urinary tract symptoms, colic episodes, and adverse effects. Statistical analyses were performed using a Mann-Whitney U-test and chi-square test. The final analysis was conducted with 61 control and 62 silodosin patients as the denominator in each randomization arm. The average expulsion times were 6.31 &plusmn; 2.13 days for the silodosin group and 9.73 &plusmn; 2.76 days for the control group (P &lt; .001). Treatment with silodosin proved to be safe and effective, as demonstrated by the increased stone expulsion rate, the reduced expulsion time, and the reduced analgesics consumption.&nbsp.

Improvement of mechanical properties of pellet containing tablets by thermal treatment

Batches of partially spray-dried lactose tablets with three different initial tensile strength (∼20N, ∼35N, ∼50N) were made. Changes along a 24h long thermal treatment at 100°C in tensile strength, friability, individual mass, water content, disintegration time, average free volume and wetting properties were evaluated. Caffeine containing gastroresistant pellets were gained by drug layering and filmcoating of inert microcrystalline cellulose pellet cores in fluid bed equipment. Shape, size, mechanical properties, drug content and dissolution profile of the coated pellets were determined. Batches of pellet containing tablets with three different pellet-filler ratios were compressed where partially spray-dried lactose was used as a filler-binder material.Characteristics of pellet containing tablets were evaluated before and after a 24h long thermal treatment at 100°C. Results shown that the poor initial mechanical properties (friability, tensile strength) were improved by thermal exposure while there were no remarkable alterations in drug release profiles.

Gastroretentive Matrix Tablets of Boswellia Oleogum Resin: Preparation, Optimization, In Vitro Evaluation, and Cytoprotective Effect on Indomethacin-Induced Gastric Ulcer in Rabbits.

Currently available anti-ulcer drugs suffer from serious side effects which limited their uses and prompted the need to search for a safe and efficient new anti-ulcer agent. Boswellia gum resin (BR) emerged as a safe, efficient, natural, and economic potential cytoprotective agent. Thus, it is of medical importance to develop gastroretentive (GR) formulations of BR to enhance its bioavailability and anti-ulcer efficacy. Early attempts involved the use of organic solvents and non-applicability to large-scale production. In this study, different tablet formulations were prepared by simple direct compression combining floating and bioadhesion mechanisms employing hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (SCMC), pectin (PC), and/or carbopol (CP) as bioadhesive polymers and sodium bicarbonate (SB) as a gas former. The prepared tablets were subjected for assessment of swelling, floating, bioadhesion, and drug release in 0.1 N HCl. The optimized GR formulation was examined for its protective effect on the gastric ulcer induced by indomethacin in albino rabbits compared with lactose tablets. The obtained results disclosed that swelling, floating, bioadhesion, and drug release of the GR tablets of BR depend mainly on the nature of the matrix and the ratio of polymer combinations. Moreover, a combination of SCMC-CP in a ratio of 2:1 (SCP21) exhibited desirable floating, bioadhesion, swelling, and extended drug release. Also, a 6-h pretreatment with SCP21 tablets decreased the severity of inflammation and number of bleeding spots among ulcer-induced rabbits in comparison to those treated with lactose tablets.