Displaying publications 41 - 60 of 128 in total

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  1. Bioequivalence of cefalexin in healthy Chinese subjects
    Lv X, Zhong G, Yao H, Wu J, Ye S
    Int J Clin Pharmacol Ther, 2021 Nov;59(11):725-733.
    PMID: 34448694 DOI: 10.5414/CP203986
    OBJECTIVE: An earlier three-way crossover study evaluating bioequivalence of 3 cefalexin formulations (capsule for reference, capsule and tablet for test) in healthy subjects in Malaysia showed that the intra-individual coefficients of variation were 9.25% for AUC0-t, 9.54% for AUC0-∞, and 13.90% for Cmax. It is preliminarily stated that cefalexin is not a high-variation product. The here-presented clinical study in China was carried out to analyze the pharmacokinetic properties of two preparations in fasting and postprandial condition to assess the bioequivalence of the test preparation and reference preparation when administered on a fasting and postprandial basis in healthy Chinese subjects and to observe the safety of the test preparation and reference preparation in healthy Chinese subjects.

    MATERIALS AND METHODS: In this trial, a total of 56 eligible subjects were randomly assigned to the fasting group and the postprandial group. The two groups were given 250 mg of the test and reference preparation, respectively. Liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was applied to determine the plasma concentration of cefalexin. PhoenixWinNonlin software (V7.0) was used to calculate the pharmacokinetic parameters of cefalexin using the non-compartmental model (NCA), and the bioequivalence and safety results were calculated by SAS (V9.4) software.

    RESULTS: The main pharmacokinetic parameters of the test and reference preparations were as follows, the fasting group: Cmax 12.59 ± 2.65 μg/mL, 12.72 ± 2.28 μg/mL; AUC0-8h 20.43 ± 3.47 h×μg/mL, 20.66 ± 3.38 h×μg/mL; AUC0-∞ 20.77 ± 3.53 h×μg/mL, 21.02 ± 3.45 h×μg/mL; the postprandial group: Cmax 5.25 ± 0.94 μg/mL, 5.23 ± 0.80 μg/mL; AUC0-10h 16.92 ± 2.03 h×μg/mL, 17.09 ± 2.31 h×μg/mL; AUC0-∞ 17.33 ± 2.09 h×μg/mL, 17.67 ± 2.45 h×μg/mL.

    CONCLUSION: The 90% confidence intervals of geometric mean ratios of test preparation and reference preparation were calculated, and the 90% confidence intervals of geometric mean ratios of Cmax, AUC0-10h, and AUC0-∞ were within the 80.00% ~ 125.00% range in both groups. Both Cmax and AUC met the pre-determined criteria for assuming bioequivalence. The test and reference products were bioequivalent after administration under fasting as well as under fed conditions in healthy Chinese subjects. This study may suggest that successful generic versions of cefalexin not only guarantee the market supply of such drugs but can also improve the safety and effectiveness and quality controllability of cefalexin through a new process and a new drug composition ratio.

    Matched MeSH terms: Tablets
  2. Investigation of the Effects of Excipients in the Compounding of Amlodipine Besylate Orally Disintegrating Tablets
    Azmi NHS, Ming LC, Uddin ABMH, Sarker ZI, Bin LK
    Int J Pharm Compd, 2022 1 27;26(1):80-87.
    PMID: 35081048
    Oral drug delivery has been recognized as the most desirable drug administration method among other drug delivery routes due to its ease of administration, long shelf life, and low cost. Orally disintegrating tablets disintegrate within seconds in the mouth without the need of water for swallowing. This unique feature of orally disintegrating tablets is favorable to special populations such as geriatric and pediatric patients. Formulation optimization is significant to obtain the optimal combination of tablet constituents, as the tablet composition is influential on dosage-form characteristics. The objective of this study was to investigate the effect of different types of fillers and percentage on the physical properties of orally disintegrating tablets by using amlodipine as the model drug. Blank orally disintegrating tablets containing different fillers, namely, Sorbolac 400, Granulac 200, and CombiLac with different percentages, were prepared using the wet granulation method and were evaluated based on weight variation, hardness, thickness, friability, and disintegration time. Formulation 5 that consists of 25% Granulac 200 showed the optimal result among all formulations with the fastest disintegration time (96.17 s Å} 18.40) and sufficient tablet hardness (4.59 kg Å} 0.70). Hence, formulation 5 was selected as the optimal formulation and incorporated with amlodipine. From this study, it can be concluded that excipients have an essential role in determining the physical properties of orally disintegrating tablets.
    Matched MeSH terms: Tablets
  3. Fulltext A Longitudinal Analysis of Daily Pill Burden and Likelihood of Optimal Adherence to Antiretroviral Therapy Among People Living With HIV Who Use Drugs
    Mohd Salleh NA, Richardson L, Kerr T, Shoveller J, Montaner J, Kamarulzaman A, et al.
    J Addict Med, 2018 3 10;12(4):308-314.
    PMID: 29521670 DOI: 10.1097/ADM.0000000000000403
    OBJECTIVES: Among people living with HIV (PLWH), high levels of adherence to prescribed antiretroviral therapy (ART) is required to achieve optimal treatment outcomes. However, little is known about the effects of daily pill burden on adherence amongst PLWH who use drugs. We sought to investigate the association between daily pill burden and adherence to ART among members of this key population in Vancouver, Canada.

    METHODS: We used data from the AIDS Care Cohort to Evaluate Exposure to Survival Services study, a long-running community-recruited cohort of PLWH who use illicit drugs linked to comprehensive HIV clinical records. The longitudinal relationship between daily pill burden and the odds of ≥95% adherence to ART among ART-exposed individuals was analyzed using multivariable generalized linear mixed-effects modeling, adjusting for sociodemographic, behavioural, and structural factors linked to adherence.

    RESULTS: Between December 2005 and May 2014, the study enrolled 770 ART-exposed participants, including 257 (34%) women, with a median age of 43 years. At baseline, 437 (56.7%) participants achieved ≥95% adherence in the previous 180 days. Among all interview periods, the median adherence was 100% (interquartile range 71%-100%). In a multivariable model, a greater number of pills per day was negatively associated with ≥95% adherence (adjusted odds ratio [AOR] 0.87 per pill, 95% confidence interval [CI] 0.84-0.91). Further analysis showed that once-a-day ART regimens were positively associated with optimal adherence (AOR 1.39, 95% CI 1.07-1.80).

    CONCLUSIONS: In conclusion, simpler dosing demands (ie, fewer pills and once-a-day single tablet regimens) promoted optimal adherence among PLWH who use drugs. Our findings highlight the need for simpler dosing to be encouraged explicitly for PWUD with multiple adherence barriers.

    Matched MeSH terms: Tablets
  4. Fulltext Continuous Monitoring of the Hydration Behavior of Hydrophilic Matrix Tablets Using Time-Domain NMR
    Tsuji T, Ono T, Taguchi H, Leong KH, Hayashi Y, Kumada S, et al.
    Chem Pharm Bull (Tokyo), 2023;71(7):576-583.
    PMID: 37394606 DOI: 10.1248/cpb.c23-00214
    Time-domain NMR (TD-NMR) was used for continuous monitoring of the hydration behavior of hydrophilic matrix tablets. The model matrix tablets comprised high molecular weight polyethylene oxide (PEO), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG). The model tablets were immersed in water. Their T2 relaxation curves were acquired by TD-NMR with solid-echo sequence. A curve-fitting analysis was conducted on the acquired T2 relaxation curves to identify the NMR signals corresponding to the nongelated core remaining in the samples. The amount of nongelated core was estimated from the NMR signal intensity. The estimated values were consistent with the experiment measurement values. Next, the model tablets immersed in water were monitored continuously using TD-NMR. The difference in hydration behaviors of the HPMC and PEO matrix tablets was then characterized fully. The nongelated core of the HPMC matrix tablets disappeared more slowly than that of the PEO matrix tablets. The behavior of HPMC was significantly affected by the PEG content in the tablets. It is suggested that the TD-NMR method has potential to be utilized to evaluate the gel layer properties, upon replacement of the immersion medium: purified (nondeuterated) water is replaced with heavy (deuterated) water. Finally, drug-containing matrix tablets were tested. Diltiazem hydrochloride (a highly water-soluble drug) was employed for this experiment. Reasonable in vitro drug dissolution profiles, which were in accordance with the results from TD-NMR experiments, were observed. We concluded that TD-NMR is a powerful tool to evaluate the hydration properties of hydrophilic matrix tablets.
    Matched MeSH terms: Tablets
  5. Optimised neem oil-bilayer tablets: A safe, effective and stable tool for the prevention of vector-borne disease outbreaks by Aedes albopictus
    Swathy KK, Sarath Chandran C, Mukundan M, Sreejith KR, Sourav K, Jafna MC, et al.
    Exp Parasitol, 2023 Aug;251:108550.
    PMID: 37230323 DOI: 10.1016/j.exppara.2023.108550
    The control of mosquito breeding is an essential step towards the reduction of vector-borne disease outbreaks. Synthetic larvicidal agents produce resistance in vectors and cause safety concerns in humans, animals and aquatic species. The drawback of synthetic larvicides opened a new avenue for natural larvicidal agents, but poor dosage accuracy, need for frequent applications, low stability and sustainability are the major challenges with them. Hence, this investigation aimed to overcome those drawbacks by developing bilayer tablets loaded with neem oil to prevent mosquito breeding in stagnant water. The optimised batch of neem oil-bilayer tablets (ONBT) had 65%w/w hydroxypropyl methylcellulose K100M and 80%w/w ethylcellulose in its composition. After the completion of 4th week, 91.98 ± 0.871% azadirachtin was released from the ONBT, which was followed by a subsequent drop in the in vitro release. ONBT reported long-term larvicidal efficacy (>75%) and a good deterrent effect which was better than neem oil-based marketed products. The acute toxicity study on a non-target fish model (Poecilia reticulata), OECD Test No.203 confirmed the safety of the ONBT on non-target aquatic species. The accelerated stability studies predicted a good stability profile for the ONBT. The neem oil-based bilayer tablets can be used as an effective tool for the control of vector-borne diseases in society. The product may be a safe, effective and eco-friendly replacement for the existing synthetic as well as natural products in the market.
    Matched MeSH terms: Tablets
  6. Design and In-vitro Evaluation of Sustained Release Floating Tablets of Metformin HCl Based on Effervescence and Swelling
    Senjoti FG, Mahmood S, Jaffri JM, Mandal UK
    Iran J Pharm Res, 2016;15(1):53-70.
    PMID: 27610147
    An oral sustained-release floating tablet formulation of metformin HCl was designed and developed. Effervescence and swelling properties were attributed on the developed tablets by sodium bicarbonate and HPMC-PEO polymer combination, respectively. Tablet composition was optimized by response surface methodology (RSM). Seventeen (17) trial formulations were analyzed according to Box-Behnken design of experiment where polymer content of HPMC and PEO at 1: 4 ratio (A), amount of sodium bi-carbonate (B), and amount of SSG (C) were adopted as independent variables. Floating lag time in sec (Y1), cumulative percent drug released at 1 h (Y2) and 12 h (Y3) were chosen as response variables. Tablets from the optimized formulation were also stored at accelerated stability condition (40°C and 75% RH) for 3 months to assess their stability profile. RSM could efficiently optimize the tablet composition with excellent prediction ability. In-vitro drug release until 12 h, floating lag time, and duration of floating were dependent on the amount of three selected independent variables. Optimized tablets remained floating for more than 24 h with a floating lag time of less than 4 min. Based on best fitting method, optimized formulation was found to follow Korsmeyer-Peppas release kinetic. Accelerated stability study revealed that optimized formulation was stable for three months without any major changes in assay, dissolution profile, floating lag time and other physical properties.
    Matched MeSH terms: Tablets
  7. Fulltext Development and evaluation of a novel modified-release pellet-based tablet system for the delivery of loratadine and pseudoephedrine hydrochloride as model drugs
    Zeeshan F, Bukhari NI
    AAPS PharmSciTech, 2010 Jun;11(2):910-6.
    PMID: 20496016 DOI: 10.1208/s12249-010-9456-2
    Modified-release multiple-unit tablets of loratadine and pseudoephedrine hydrochloride with different release profiles were prepared from the immediate-release pellets comprising the above two drugs and prolonged-release pellets containing only pseudoephedrine hydrochloride. The immediate-release pellets containing pseudoephedrine hydrochloride alone or in combination with loratadine were prepared using extrusion-spheronization method. The pellets of pseudoephedrine hydrochloride were coated to prolong the drug release up to 12 h. Both immediate- and prolonged-release pellets were filled into hard gelatin capsule and also compressed into tablets using inert tabletting granules of microcrystalline cellulose Ceolus KG-801. The in vitro drug dissolution study conducted using high-performance liquid chromatography method showed that both multiple-unit capsules and multiple-unit tablets released loratadine completely within a time period of 2 h, whereas the immediate-release portion of pseudoephedrine hydrochloride was liberated completely within the first 10 min of dissolution study. On the other hand, the release of pseudoephedrine hydrochloride from the prolonged release coated pellets was prolonged up to 12 hr and followed zero-order release kinetic. The drug dissolution profiles of multiple-unit tablets and multiple-unit capsules were found to be closely similar, indicating that the integrity of pellets remained unaffected during the compression process. Moreover, the friability, hardness, and disintegration time of multiple-unit tablets were found to be within BP specifications. In conclusion, modified-release pellet-based tablet system for the delivery of loratadine and pseudoephedrine hydrochloride was successfully developed and evaluated.
    Matched MeSH terms: Tablets*
  8. Enantioselective analysis of primaquine and its impurity quinocide by capillary electrophoresis
    Elbashir AA, Saad B, Ali AS, Saleh MI, Aboul-Enein HY
    Biomed Chromatogr, 2009 Mar;23(3):295-301.
    PMID: 18816453 DOI: 10.1002/bmc.1113
    A capillary electrophoretic (CE) method for the baseline separation of the enantiomers of primaquine diphosphate (PQ) and quinocide (QC) (a major contaminant) in pharmaceutical formulations is proposed. Both components were separated under the following conditions: 50 mm tris phosphate buffer (pH 3.0) containing 15 mm hydroxypropyl-gamma-cyclodextrin (HP-gamma-CD) as background electrolyte; applied voltage, 16 kV; capillary temperature, 25 degrees C; detection wavelength, 254 nm; hydrostatic injection, 10 s. The separations were conducted using a 35 cm length and 50 microm i.d. uncoated fused silica capillary column. Under the optimized conditions, the components were successfully separated in about 5 min. Intraday precision of migration time and corrected peak areas when expressed as relative standard deviation ranged from 0.17 to 0.45 and 2.60 to 3.94%, respectively, while the interday precision ranged from 2.59 to 4.20 and 3.15 to 4.21%, respectively. After the validation exercise, the proposed method was applied for the determination of QC impurity in PQ formulations.
    Matched MeSH terms: Tablets/chemistry
  9. The influence of different plasticizers on some physical and mechanical properties of hydroxypropyl methylcellulose free films
    Saringat HB, Alfadol KI, Khan GM
    Pak J Pharm Sci, 2005 Jul;18(3):25-38.
    PMID: 16380341
    Coating has been widely used in pharmaceutical manufacture either as non-functional or a functional entity. The objectives of the present study were to investigate the effect of plasticizers such as PEG400, PEG1000 and triacetin on mechanical properties, glass transition temperature and water vapor transmission of free films prepared from HPMC and/or HPMC:PVA blends, to develop suitable coating system for tablets, and to determine the release profiles of the coated tablets. The tensile strength of plasticized HPMC films was generally lower than that of control HPMC film and could be attributed to increased crystallinity and segmental chain mobility of HPMC. This effect increased as the concentration of plasticizer increased. Generally the addition of both grades of polyethylene glycol (PEG400 & PEG1000) increased the moisture permeability of HPMC films but the films containing triacetin provided a more rigid barrier to moisture compared to unplasticized HPMC films. The dissolution profiles of paracetamol tablets coated with 7% w/v HPMC coating-solutions containing PEG400, PEG1000 and triacetin, and those containing PEG400 & PVA together showed that HPMC had weak water resistance. The presence of PEG400 and 1000 in HPMC films further weakened its resistance to solubility while the presence of triacetin caused a little increase in HPMC water resistance. From the results it was concluded that HPMC at 7%w/w concentration was suitable for film-coating intended for non-functional coating. Presence of the PEG 400, PEG1000 and triacetin as well as the presence of PVA and PEG400 together improved the coating properties of HPMC films and made it more suitable as a non-functional coating material.
    Matched MeSH terms: Tablets*
  10. Comparison studies on the percolation thresholds of binary mixture tablets containing excipients of plastic/brittle and plastic/plastic deformation properties
    Amin MC, Fell JT
    Drug Dev Ind Pharm, 2004;30(9):937-45.
    PMID: 15554218
    Percolation theory has been used with great interest in understanding the design and characterization of dosage forms. In this study, work has been carried out to investigate the behavior of binary mixture tablets containing excipients of similar and different deformation properties. The binary mixture tablets were prepared by direct compression using lactose, polyvinyl chloride (PVC), Eudragit RS 100, and microcrystalline cellulose (MCC). The application of percolation theory on the relationships between compactibility, Pmax, or compression susceptibility (compressibility), gamma, and mixture compositions reveals the presence of percolation thresholds even for mixtures of similar deformation properties. The results showed that all mixture compositions exhibited at least one discreet change in the slope, which was referred to as the percolation threshold. The PVC/Eudragit RS100 mixture compositions showed significant percolation threshold at 80% (w/w) PVC loading. Two percolation thresholds were observed from a series of binary mixtures containing similar plastic deformation materials (PVC/MCC). The percolation thresholds were determined at 20% (w/w) and 80% (w/w) PVC loading. These are areas where one of the components percolates throughout the system and the properties of the tablets are expected to experience a sudden change. Experimental results, however, showed that total disruption of the tablet physical properties at the specified percolation thresholds can be observed for PVC/lactose mixtures at 20-30% (w/w) loading while only minor changes in the tablets' strength for PVC/MCC or PVC/Eudragit RS 100 mixtures were observed.
    Matched MeSH terms: Tablets*
  11. Preparation and in vitro evaluation of mebeverine HCl colon-targeted drug delivery system
    Abdullah GZ, Abdulkarim MF, Chitneni M, Mutee AF, Ameer OZ, Salman IM, et al.
    Pharm Dev Technol, 2011 Aug;16(4):331-42.
    PMID: 20429815 DOI: 10.3109/10837451003739255
    Mebeverine HCl is a water soluble drug commonly used to treat irritable bowel syndrome by acting directly on the smooth muscles of the colon. This work was aimed at the formulation and in vitro evaluation of a colon-targeted drug delivery system containing mebeverine HCl. Matrix tablets were prepared using ethyl cellulose (EC), Eudragit RL 100 either solely or in combination by wet granulation technique. Dissolution was carried out in 0.1 N HCl for 2?h followed by pH 6.8 phosphate buffer for eight hours. Uncoated forms released more than 5% drug in 0.1 N HCl therefore, Eudragit L100 was used as a coat. The results indicated very slow release profile. As a result, single retardant was used to prepare the matrix and coated by Eudragit L 100. The matrix containing 7% Eudragit RL 100 and 6% of binder was subjected to further studies to assess the effect of different coats (Eudragit L 100-55 and cellulose acetate phthalate) and different binders (pectin and sodium alginate) on the release profile. Eudragit L 100 and pectin were the best coating agent and binder, respectively. The final formula was stable and it can be concluded that the prepared system has the potential to deliver mebeverine HCl in vivo to the colon.
    Matched MeSH terms: Tablets, Enteric-Coated/pharmacokinetics; Tablets, Enteric-Coated/chemistry*
  12. Fulltext Formulation and in vitro, in vivo evaluation of effervescent floating sustained-release imatinib mesylate tablet
    Kadivar A, Kamalidehghan B, Javar HA, Davoudi ET, Zaharuddin ND, Sabeti B, et al.
    PLoS One, 2015;10(6):e0126874.
    PMID: 26035710 DOI: 10.1371/journal.pone.0126874
    Imatinib mesylate is an antineoplastic agent which has high absorption in the upper part of the gastrointestinal tract (GIT). Conventional imatinib mesylate (Gleevec) tablets produce rapid and relatively high peak blood levels and requires frequent administration to keep the plasma drug level at an effective range. This might cause side effects, reduced effectiveness and poor therapeutic management. Therefore, floating sustained-release Imatinib tablets were developed to allow the tablets to be released in the upper part of the GIT and overcome the inadequacy of conventional tablets.
    Matched MeSH terms: Tablets/pharmacokinetics; Tablets/chemistry*
  13. Fulltext Novel swellable polymer of orchidaceae family for gastroretentive drug delivery of famotidine
    Razavi M, Nyamathulla S, Karimian H, Noordin MI
    Drug Des Devel Ther, 2014;8:1315-29.
    PMID: 25246773 DOI: 10.2147/DDDT.S68517
    This study aimed to develop hydrophilic, gastroretentive matrix tablets of famotidine with good floating and swelling properties. A novel gastroretentive drug delivery formulation was designed using salep, also known as salepi, a flour obtained from grinding dried palmate tubers of Orchis morio var mascula (Orchidaceae family). The main polysaccharide content of salep is glucomannan, highly soluble in cold and hot water, which forms a viscous solution. Salep was characterized for physicochemical properties, thermal stability, chemical interaction, and surface morphology using X-ray diffraction analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, and scanning electron microscopy. Ten different formulations (S1-S10) were prepared using famotidine to salep ratios from 1:0.5 to 1:5. Results demonstrated that all formulations were able to sustain the drug release for more than 24 hours. The S5 formulation, with a famotidine to salep ratio of 1:2.5, had the shortest floating lag time of 35 seconds and 100% drug release within 24 hours. The dissolution data were fitted into popular mathematical models to assess the mechanism of drug release. S5 showed Zero order release (R=0.9746) with Higuchi diffusion (R=0.9428). We conclude that salep, a novel polymer, can be used in controlled release formulations to sustain release for 24 hours, due to inherent swelling and gelling properties.
    Matched MeSH terms: Tablets
  14. Fulltext Formulation development and optimization of sustained release matrix tablet of Itopride HCl by response surface methodology and its evaluation of release kinetics
    Bose A, Wong TW, Singh N
    Saudi Pharm J, 2013 Apr;21(2):201-13.
    PMID: 23960836 DOI: 10.1016/j.jsps.2012.03.006
    The objective of this present investigation was to develop and formulate sustained release (SR) matrix tablets of Itopride HCl, by using different polymer combinations and fillers, to optimize by Central Composite Design response surface methodology for different drug release variables and to evaluate drug release pattern of the optimized product. Sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: hydroxy propyl methyl cellulose (HPMC) and polyvinyl pyrolidine (pvp) and lactose as fillers. Study of pre-compression and post-compression parameters facilitated the screening of a formulation with best characteristics that underwent here optimization study by response surface methodology (Central Composite Design). The optimized tablet was further subjected to scanning electron microscopy to reveal its release pattern. The in vitro study revealed that combining of HPMC K100M (24.65 MG) with pvp(20 mg)and use of LACTOSE as filler sustained the action more than 12 h. The developed sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.
    Matched MeSH terms: Tablets
  15. Comparative bioavailability of two risperidone orodispersible tablet products after single dose administration
    Tassaneeyakul W, Kumar S, Gaysonsiri D, Kaewkamson T, Khuroo A, Tangsucharit P, et al.
    Int J Clin Pharmacol Ther, 2010 Sep;48(9):614-20.
    PMID: 20860915
    OBJECTIVES: To compare the bioavailability of two risperidone orodispersible tablet products, Risperidone 1 mg Mouth dissolving tablet, Ranbaxy (Malaysia) Sdn. Bhd., Malaysia, as a test product and Risperdal 1 mg Quicklet, Janssen Ortho LLC, Gurabo, Puerto Rico, as a reference product, in healthy male volunteers under fasting condition.

    MATERIALS AND METHODS: A randomized, 2-treatment, 2-period, 2-sequence, single dose, crossover with a washout period of 2 weeks, was conducted in 24 healthy Thai male volunteers. Blood samples were collected at 0, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72 and 96 h following drug administration. Plasma concentrations of risperidone and 9-hydroxyrisperidone were determined using a validated LC-MS-MS method. The pharmacokinetic parameters of risperidone and 9-hydroxyrisperidone were determined using a non-compartmental model.

    RESULTS: The geometric means ratios (%) and 90% confidence interval (CI) of the test and reference products for the log-transformed pharmacokinetic parameters, Cmax, AUC0-t and AUC0-inf of risperidone were 104.49 % (92.79% - 117.66%), 100.96 % (92.15% - 110.61 %) and 97.99 % (90.72% - 105.85%). The 90% CI of geometric means ratios of the test and reference products for the log-transformed pharmacokinetic parameters, Cmax, AUC0-t and AUC0-inf of 9-hydroxyrisperidone were 97.00%, 96.97% and 97.49%.

    CONCLUSIONS: The 90% CI for the geometric means ratios (test/reference) of the log-trasformed Cmax, AUC0-t and AUC0-inf of risperidone and its major active metabolite were within the bioequivalence acceptance criteria of 80% - 125% of the US-FDA.

    Matched MeSH terms: Tablets
  16. Efficacy of a Bacillus thuringiensis israelensis tablet formulation, vectobac DT, for control of dengue mosquito vectors in potable water containers
    Benjamin S, Rath A, Fook CY, Lim LH
    Southeast Asian J. Trop. Med. Public Health, 2005 Jul;36(4):879-92.
    PMID: 16295540
    VectoBac DT, a tablet formulation of Bacillus thuringiensis israelensis (Bti) was evaluated for the potential control of dengue vectors in various types of potable water containers. On introduction to containers, the tablet sinks to the bottom and the Bti toxins are found concentrated at the sides and the base, while the treated water column is free of Bti toxins within 24 hours after tablet introduction. In a simulated study, earthen, HDPE and plastic containers were kept covered and laboratory-bred larvae were introduced to determine the control by the tablet. The efficacy and persistence of the tablet, with a control of > 90%, was significantly longer in earthen containers in comparison to the HDPE and plastic containers. Efficacy and persistence were observed in earthen containers for a minimum period of 5.5 months (166 days) both without water replenishment and with weekly, 50% water volume, replenishment, and for a maximum period of 2.2 months (66 days) with daily, 50% water volume, replenishment. In plastic and HDPE containers, the tablet activity had a persistence of 2.1 months (63 days) without water replenishment and 1.8 months (54 days) with weekly water replenishment. The efficacy and persistence of the VectoBac DT was significantly longer in the earthen containers, with or without regularly treated water exchange, due to the Bti toxins being embedded in the porous earthen container surfaces, which protects them from rapid degradation. Lesser toxin amounts are removed from the water column during water exchange. The efficacy of VectoBac DT was also evaluated for the control of natural infestation of Aedes larvae which were resistant to temephos at the WHO diagnostic dosage of 0.012 mg/l. The tablet significantly reduced the pupal density by 8 fold in earthen containers for 67 days and 5 fold in HDPE containers for 55 days in comparison to untreated containers (p < 0.05). However, the tablet was effective for a shorter period of 25 days post-tablet-introduction due to fungal infestation in the treated plastic containers. There is a need to determine the capacity of the VectoBac DT to reduce the dengue vector population to a threshold which will prevent dengue outbreaks in dengue endemic areas.
    Matched MeSH terms: Tablets
  17. Fulltext Comparative pharmacokinetics of a proliposome formulation of Ginkgo biloba extract and Ginaton in rats by a sensitive ultra performance liquid chromatography-tandem mass spectrometry method
    Zheng B, Xing G, Bi Y, Yan G, Wang J, Cheng Y, et al.
    Saudi J Biol Sci, 2016 Jan;23(1):54-65.
    PMID: 26858539 DOI: 10.1016/j.sjbs.2015.08.009
    As a novel oral drug delivery system, proliposome was applied to improve the solubility of active components of Ginkgo biloba extract (GbE). There are currently few reports focusing on the pharmacokinetic characteristics of proliposome of GbE (GbP). A rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the simultaneous quantification of active components of GbP and a commercial tablet product (Ginaton) in rat plasma was developed and successfully validated. The method was applied to the comparative pharmacokinetic evaluation of GbP and Ginaton in rat plasma. The results indicated that GbP has a significant effect on absorption, elimination and bioavailability of flavonoids and terpenoid lactones in comparison with Ginaton. The obtained results would be helpful for evaluating the absorption mechanism in the gastrointestinal tract in pharmacokinetic level and guiding the development of the novel oral drug delivery system.
    Matched MeSH terms: Tablets
  18. Formulation and optimization of gastric floating drug delivery system using Central composite design and its biopharmaceutical evaluation
    Meka VS, Thing LK, Gorajana A, Kolapalli VR
    Pak J Pharm Sci, 2015 Jul;28(4):1373-87.
    PMID: 26142528
    The present work investigates the formulation and biopharmaceutical estimation of gastric floating drug delivery system (GFDDS) of propranolol HCl using semi-synthetic polymer carboxymethyl ethyl cellulose (CMEC) and a synthetic polymer polyethylene oxide (PEO). A central composite design was applied for optimization of polymer quantity (CMEC or PEO) and sodium bicarbonate concentration as independent variables. The dependent variables evaluated were: % of drug release at 1 hr (D1hr), % drug release at 3 hr (D3hr) and time taken for 95% of drug release (t95). Numerical optimization and graphical optimization were conducted to optimize the response variables. All observed responses of statistically optimized formulations were in high treaty with predicted values. Accelerated stability studies were conducted on the optimized formulations at 40 ± 2°C/75% ± 5% RH and confirm that formulations were stable. Optimized formulations were evaluated for in vivo buoyancy characterization in human volunteers and were found buoyant in gastric fluid. Gastric residence time was enhanced in the fed but not the fasted state. The optimized formulations and marketed formulation were administered to healthy human volunteers and evaluated for pharmacokinetic parameters. Mean residence time (MRT) was prolonged and AUC levels were increased for both optimized floating tablets when compared with marketed product. High relative bioavailability obtained with optimized gastric floating tablets compared to commercial formulation, indicated the improvement of bioavailability.
    Matched MeSH terms: Tablets
  19. Chloroquine polymeric membrane electrodes: Development and applications
    Saad B, Kanapathy K, Ahmad MN, Hussin AH, Ismail Z
    Talanta, 1991 Dec;38(12):1399-402.
    PMID: 18965315
    Three main types of PVC solvent polymeric membrane ion-selective electrodes for chloroquine are described. They are based on three ion-pairing agents namely dipicrylamine (DPA), tetraphenylborate (TPB) or tetrakis(4-chlorophenyl)borate (TCPB) with either dioctylphenyl phosphonate (DOPP) or trioctyl phosphate (TOP) solvent mediator. All electrodes exhibit Nernstian responses, fast dynamic response times and a wide useful pH range. The best all-round electrode is based on TPB and TOP plasticizing solvent mediators with a limit of detection of 7.1 x 10(-6)M and was utilized for the assay of chloroquine in tablets. Direct potentiometric determinations with either the analyte addition method or the normal calibration method gave results comparable to the official method.
    Matched MeSH terms: Tablets
  20. Suspected-target and non-targeted screenings of phosphodiesterase 5 inhibitors in herbal remedies using liquid chromatography-quadrupole time-of-flight-mass spectrometry
    Mohd Yusop AY, Xiao L, Fu S
    Drug Test Anal, 2021 May;13(5):965-976.
    PMID: 32441056 DOI: 10.1002/dta.2861
    The lucrative market of herbal remedies spurs rampant adulteration, particularly with pharmaceutical drugs and their unapproved analogues. A comprehensive screening strategy is, therefore, warranted to detect these adulterants and, accordingly, to safeguard public health. This study uses the data-dependent acquisition of liquid chromatography-quadrupole time-of-flight-mass spectrometry (LC-QTOF-MS) to screen phosphodiesterase 5 (PDE5) inhibitors in herbal remedies using suspected-target and non-targeted strategies. For the suspected-target screening, we used a library comprising 95 PDE5 inhibitors. For the non-targeted screening, we adopted top-down and bottom-up approaches to flag novel PDE5 inhibitor analogues based on common fragmentation patterns. LC-QTOF-MS was optimised and validated for capsule and tablet dosage forms using 23 target analytes, selected to represent different groups of PDE5 inhibitors. The method exhibited excellent specificity and linearity with limit of detection and limit of quantification of <40 and 80 ng/mL, respectively. The accuracy ranged from 79.0% to 124.7% with a precision of <14.9% relative standard deviation. The modified, quick, easy, cheap, effective, rugged, and safe extraction provided insignificant matrix effect within -9.1%-8.0% and satisfactory extraction recovery of 71.5%-105.8%. These strategies were used to screen 52 herbal remedy samples that claimed to enhance male sexual performance. The suspected-target screening resulted in 33 positive samples, revealing 10 target analytes and 2 suspected analytes. Systematic MS and tandem MS interrogations using the non-targeted screening returned insignificant signals, indicating the absence of potentially novel analogues. The target analytes were quantified from 0.03 to 121.31 mg per dose of each sample. The proposed strategies ensure that all PDE5 inhibitors are comprehensively screened, providing a useful tool to curb the widespread adulteration of herbal remedies.
    Matched MeSH terms: Tablets
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