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1.
Clin Pharmacol Drug Dev ; 11(2): 165-172, 2022 02.
Artículo en Inglés | MEDLINE | ID: mdl-34453416

RESUMEN

Tadalafil is an effective, reversible, and competitive phosphodiesterase 5 inhibitor mainly used to treat erectile dysfunction. This study investigated the bioequivalence of generic and marketed formulations of 10-mg tadalafil tablets under fasted and fed conditions. This open-label, randomized, single-dose, 2-period crossover study included 53 healthy Chinese men (aged 20-43 years). Plasma samples were collected from 0.5 hours before treatment to 72 hours after each dose and analyzed using ultra-high-performance liquid chromatography coupled with tandem mass spectrometry. Pharmacokinetic parameters were calculated using noncompartmental analysis. Safety assessments were performed throughout the study. For the fasted state, the 90% confidence intervals of the geometric mean ratios between the generic and marketed formulations were 86.1% to 99.1% for the maximum plasma concentration and 88.4% to 100.3% for the area under the plasma concentration-time curve from time 0 to infinity, and the corresponding values under the fed state were and 99.9% to 108.4% and 95.7% to 104.3%, respectively. All data were within the accepted bioequivalence range of 80% to 125%. After consuming high-fat, high-calorie meals in the fed condition, the time to the maximum plasma concentration was similar between the formulations, and area under the plasma concentration-time curve from time 0 to infinity and maximum plasma concentration were 10.2% and 6.55% higher, respectively, for the marketed formulation. Thus, food had no clinically relevant effect on tadalafil exposure following a single oral dose in healthy Chinese men. No serious adverse reactions were reported. These results indicated that the analyzed generic and marketed tadalafil tablets were bioequivalent with similar safety profiles.


Asunto(s)
Ayuno , Adulto , China , Estudios Cruzados , Humanos , Masculino , Comprimidos , Tadalafilo/efectos adversos , Equivalencia Terapéutica , Adulto Joven
2.
AAPS PharmSciTech ; 23(7): 251, 2022 Sep 07.
Artículo en Inglés | MEDLINE | ID: mdl-36071254

RESUMEN

Trazodone hydrochloride (TZN) is a serotonin reuptake inhibitor that treats a major depressive disorder. It exhibits a short plasma half-life of 4.1 h and shows pH-dependent solubility. Above its pKa (6.74), solubility of TZN is very low, affecting its dissolution in the lower part of GIT. Hence, the present work aimed to develop gastro-retentive floating tablet of TZN. Central composite design was employed to optimize the formulation. Formulation variables like the concentration of HPMC-K100M, Polyox WSR 303 Leo, and sodium bicarbonate were evaluated for the responses like floating lag time and drug release. X-ray imaging study was performed on rabbits to determine the in vivo gastric retention of the optimized formulation. The accelerated stability study was conducted on optimized tablets as per ICH guidelines. Floating lag time and f2 value of the optimized formulation were found to be 2.51±0.02 min and 62.79, respectively. X-ray imaging studies in rabbits determined the in vivo gastro retention time. After 12 h of administration, tablet remained in the gastric region, indicating better retentive power. Accelerated stability studies showed sufficient formulation stability even after 3 months of storage. All these studies depict that the floating gastro-retentive system could be used as an alternative to the innovator formulation.


Asunto(s)
Trastorno Depresivo Mayor , Trazodona , Animales , Preparaciones de Acción Retardada , Conejos , Solubilidad , Comprimidos
3.
Comput Math Methods Med ; 2022: 9803552, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36132547

RESUMEN

Aims: To observe the clinical efficacy of self-made Lifei Dingchuan decoction combined with western medicine in the treatment of cough variant asthma (phlegm-heat accumulation in the lung syndrome). Materials and Methods: The clinical data of 90 patients with cough variant asthma who were hospitalized in the Department of Respiratory Medicine of our hospital from January 2020 to April 2022 were selected as the research objects, and they were equally divided into the observation group and the reference group according to different treatment methods, 45 cases in each group. The group was treated with traditional montelukast sodium chewable tablet and salmeterol fluticasone mixed powder inhalation, and the observation group was treated with self-made Lifei Dingchuan decoction on the basis of the control group, saturation, pH, partial pressure of oxygen in arterial blood, partial pressure of carbon dioxide, length of stay, and hospitalization costs. Results: After the patients underwent self-made Lifei Dingchuan decoction, there were significant differences between the observation group and the reference group in terms of heart rate, respiratory rate, blood oxygen saturation, pH value, arterial blood oxygen partial pressure, carbon dioxide partial pressure, and within the group. There was a statistical difference (P < 0.05). The adverse reactions in patients with cough variant asthma after treatment showed that the red throat, shortness of breath, chest tightness, and dry mouth in the observation group were significantly different from those in the control group (P < 0.05). After investigation, follow-up, and statistics, the hospitalization time, hospitalization cost, asthma exacerbation control time, effective rate, and recurrence rate were compared between the two groups, and the differences between the two groups were statistically significant (P < 0.05). Conclusion: The study on the clinical efficacy and low hospitalization cost of the self-prepared lung and asthma-restorative soup in patients with cough variant asthma significantly improved the patients' arterial oxygen saturation, acid-base value, arterial partial pressure of oxygen, and partial pressure of carbon dioxide and effectively controlled the heart rate and respiratory rate with high safety, which is worth further promotion.


Asunto(s)
Asma , Tos , Acetatos , Asma/tratamiento farmacológico , Dióxido de Carbono , Tos/tratamiento farmacológico , Ciclopropanos , Fluticasona/uso terapéutico , Humanos , Oxígeno , Polvos/uso terapéutico , Quinolinas , Xinafoato de Salmeterol/uso terapéutico , Sulfuros , Comprimidos/uso terapéutico
4.
J Pharm Biomed Anal ; 220: 115019, 2022 Oct 25.
Artículo en Inglés | MEDLINE | ID: mdl-36084472

RESUMEN

Primary goal of any space mission is to keep astronauts healthy and fit during entire mission. One of the important challenges for that is providing a safe and effective pharmacy with the capabilities to address both scheduled and unanticipated medical conditions that may arise during spaceflight. Extended exposure to space environmental conditions may trigger drug deterioration, impacting quality, effectiveness, and safety. To assess the influence of space ionizing radiations on the stability of medicines launched aboard spacecraft, a preliminary ground-based ionizing radiation drug interaction study was carried out at different doses in the present work. Four different types of radiations - proton, neutron (thermal, fast), gamma and heavy ions (56Fe) were used to irradiate selected drugs namely diclofenac, ciprofloxacin and metoprolol along with their formulations. Chemical stability of each irradiated sample was checked using high performance liquid chromatographic method. Significant degradation was observed in even solid-state during proton irradiation in both Active Pharmaceutical Ingredient (API) and tablet dosage form. Solution of active pharmaceutical ingredient and liquid dosage forms were prone to degradation in presence of gamma radiation. No physical and chemical changes observed after neutron and 56Fe irradiation. Irradiation of the same drug with different radiations demonstrated varying HPLC chromatographic profiles in terms of %degradation as well as proportion of same degradation products. This indicates possibility of different degradation pathways to generate degradation products.


Asunto(s)
Protones , Vuelo Espacial , Ciprofloxacina , Diclofenaco , Metoprolol , Radiación Ionizante , Comprimidos
5.
J Tradit Chin Med ; 42(5): 671-680, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-36083472

RESUMEN

OBJECTIVE: To investigate the effectiveness and safety of tripterygium glycosides (TG) tablet for the treatment of Lupus nephritis (LN). METHODS: Several databases were systematically searched including PubMed, Embase, Cochrane, Wiley, China National Knowledge Infrastructure Database, SinoMed and Wanfang Library till June 20, 2020. Revman5.3 was utilized to analyze the data according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses Statement. RESULTS: In total, 8 randomized controlled trials involving 583 participants were identified. Meta-analyses showed that, compared with glucocorticoids (GC) alone, the combination with TG tablet provided a statistically significant improvement in total remission (TR) ( = 1.27, 95% : 1.08-1.50, = 0.004), complete remission (CR) ( = 1.61, 95% : 1.05-2.47, = 0.03) and C3 levels ( = 0.27, 95% : 0.14-0.39, < 0.000 1), C4 levels ( = 0.12, 95% : 0.07-0.17, < 0.000 01). No significant differences were seen in TR, CR, proteinuria, serum creatinine, C3 and C4 (TR: = 1.00, 95% : 0.87-1.16, = 0.95; CR: = 1.10, 95% : 0.78-1.56, = 0.58; proteinuria levels: = -0.06, 95% : -0.13 to 0.01, = 0.10; serum creatinine levels: = -0.01, 95%: -7.36 to 7.35, = 1.00; C3 levels: = 0.01, 95%: -0.06 to 0.07, = 0.84; C4 levels: = -0.01, 95%: -0.03 to 0.01, = 0.49) between azathioprine (AZA) / leflomit (LEF) + GC and TG tablet + GC. Adverse events (hepatic dysfunction, nausea, vomitting) showed no statistical differences between the TG tablet + GC group and the GC group. There were more new onset of irregular menstruation in the TG tablet + GC group than those in the AZA + GC ( = 3.57, 95% : 1.40-9.11, = 0.008) /LEF+ GC ( = 6.69, 95% : 2.42-18.46, = 0.000 2) group, but leucopenia lower than those in AZA + GC group ( = 0.38, 95% : 0.17-0.85, = 0.02) and alopecia ( = 0.14, 95% : 0.03-0.77, = 0.02) and rash ( = 0.09, 95% : 0.01-0.69, = 0.02) lower than those in LEF + GC group. CONCLUSIONS: This review indicates that TG tablet maybe effective in LN treatment. Nevertheless, adverse events cannot be ignored. Large sample, multi-center, high-quality clinical studies are needed to verify the exact effects and safety of TG tablet in treatment of LN.


Asunto(s)
Nefritis Lúpica , Tripterygium , Creatinina , Femenino , Glicósidos/uso terapéutico , Humanos , Nefritis Lúpica/tratamiento farmacológico , Proteinuria/tratamiento farmacológico , Ensayos Clínicos Controlados Aleatorios como Asunto , Comprimidos/uso terapéutico , Tripterygium/química
6.
J Tradit Chin Med ; 42(5): 810-817, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-36083490

RESUMEN

OBJECTIVE: To investigate the clinical efficacy of Fufang Huangqi decoction in combination with pyridostigmine bromide tablets, prednisone, and tacrolimus in the treatment of type I and II myasthenia gravis (MG) through changes in the clinical symptom scores of 100 patients with type I and II MG. This study also aimed to examine dose reductions and dis-continuation of these 3 Western medicines after administration of Fufang Huangqi decoction. METHODS: The clinical data on 100 patients with type I or II MG who were treated in the outpatient department of the Affiliated Hospital of Liaoning University of Traditional Chinese Medicine, China, between June 2017 and June 2020 were collected. The patients were divided into 4 groups based on whether they had taken pyridostigmine bromide tablets, prednisone, and/or tacrolimus at the time of their hospital visit: the Fufang Huangqi decoction group (group A), the pyridostigmine bromide tablets + Fufang Huangqi decoction group (group B), the pyridostigmine bromide tablets + prednisone + Fufang Huangqi decoction group (group C), and the pyridostigmine bromide tablets + tacrolimus + Fufang Huangqi decoction group (group D). The average treatment time was (15.6 ± 11.5) months (range: 0.5-55 months). Changes in the clinical symptom scores of the 4 groups of patients after medication administration and dose reductions and discontinuation of the 3 Western medicines were analyzed. RESULTS: An overall effectiveness rate of 86.00% was achieved in the 100 patients after treatment for (15.6 ± 11.5) months (range 0.5-55 months). The effectiveness rates were 85.71% in group A, 88.24% in group B, 76.92% in group C, and 80.00% in group D. The dosage of pyridostigmine bromide was reduced for 69.12% of the patients in group B for the first time after (4.2 ± 4.1) months, and 45.59% of the patients in group B discontinued pyridostigmine bromide after (8.8 ± 6.1) months. The dosage of pyridostigmine bromide was reduced for 46.15% of the patients in group C for the first time after (5.3 ± 3.4) months, and 23.08% of the patients in group C discontinued pyridostigmine bromide after (19.8 ± 11.0) months; 76.92% reduced hormone dosage after (2.8 ± 1.9) months, and 23.08% discontinued hormone treatment after (6.7 ± 2.9) months. The dosage of pyridostigmine bromide was reduced for 1 patient in group D after 1 month; this patient discontinued pyridostigmine bromide after 3 months and reduced tacrolimus dosage after 5 months. One patient in group D discontinued pyridostigmine bromide and tacrolimus on his own initiative at 0.5 months and took Fufang Huangqi decoction for 2 months without discontinuing Western medicine. CONCLUSION: Fufang Huangqi decoction is effective for the treatment of type I and II MG and improves the associated clinical symptoms. Moreover, this agent is conducive to dose reductions and discontinuation of basic Western medicines, thereby reducing the side effects experienced by patients.


Asunto(s)
Miastenia Gravis , Tacrolimus , Reducción Gradual de Medicamentos , Medicamentos Herbarios Chinos , Hormonas/uso terapéutico , Humanos , Miastenia Gravis/tratamiento farmacológico , Prednisona/uso terapéutico , Bromuro de Piridostigmina/uso terapéutico , Comprimidos/uso terapéutico , Tacrolimus/uso terapéutico
7.
Biomed Pharmacother ; 153: 113425, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-36076546

RESUMEN

Naoqingzhiming, whose active ingredient is echinacoside, is the first new Class I natural medicine approved for clinical trials for the therapeutic potential of vascular dementia in China. We report randomized, double-blind, placebo-controlled trials to evaluate the safety, tolerability and pharmacokinetics of single ascending doses of Naoqingzhiming tablet after oral administration in healthy Chinese subjects. The single ascending dose of Naoqingzhiming tablet (180-2160 mg) were well tolerated in all enrolled subjects, without serious adverse events and adverse events leading to withdrawal from the study. The most common drug-related treatment-emergent adverse events were elevated blood bilirubin and serum uric acid. No clinically significant findings were found in the physical examinations, vital signs or electrocardiograms. After single-dose administration of Naoqingzhiming tablet, echinacoside was absorbed with a Tmax at 1.25-1.75 h and declined with a t1/2 of 2.42-3.33 h. However, the proportionality coefficients for Cmax, AUC0-t and AUC0-∞ of echinacoside were not fully contained in the pre-defined 90 % CI criterion (0.91-1.09). As a result, the dose proportionality could not be concluded statistically within the dosage range of this study. Overall, the safety profile and PK properties support further development and use of Naoqingzhiming in vascular dementia.


Asunto(s)
Demencia Vascular , Área Bajo la Curva , Demencia Vascular/tratamiento farmacológico , Relación Dosis-Respuesta a Droga , Método Doble Ciego , Voluntarios Sanos , Humanos , Comprimidos , Ácido Úrico
8.
Int J Pharm Compd ; 26(5): 358-362, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36053761

RESUMEN

In 2016, the National Institute for Occupational Safety and Health (NIOSH) published a list of hazardous drugs in healthcare. The handling of such drugs must be conducted using closed system devices according to United States Pharmacopeia General Chapter <800> and other regulations, such as Directive (EU) 2022/431 of the European Parliament and of the Council of 9 March 2022 amending Directive 2004/37/EC on the protection of workers from the risks related to exposure to carcinogens or mutagens at work. There are approximately 90 enterally administered drugs on the NIOSH list. In this list, NIOSH established that crushing tablets or making solutions from them causes an unacceptable risk at hospitals. Furthermore, United States Pharmacopeia <800> and European regulations impose the use of closed system devices and plastic pouches to contain any dust or particles generated during these operations. While there are several marketed closed system drug-transfer devices for intravenous treatments, there is no single system to crush, disperse, and administer hazardous drugs safely via enteral. This poses a great risk for patients who cannot swallow properly or are fed by an enteral tube. To solve this problem, we developed a new medical device to protect caregivers from such risks. We patented a new device that allows a safe administration and reduces exposure risk and environmental pollution at pharmacy departments (cross-contamination in cabinets), nursery units, and even at patients' homes to protect caregivers and relatives. This initiative by a hospital pharmacist aims to solve a daily problem and provide an example of our potential in healthcare innovation.


Asunto(s)
Antineoplásicos , Exposición Profesional , Salud Laboral , Servicios Farmacéuticos , Excipientes , Humanos , Exposición Profesional/análisis , Exposición Profesional/prevención & control , Comprimidos , Estados Unidos
9.
Int J Pharm Compd ; 26(5): 370-377, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36053763

RESUMEN

The cost of research and development for a single new treatment that reaches the market is enormous and rising, with estimates ranging from $1 billion to $2 billion. Because of the high cost of development and the need to quickly access multiple technologies, it is more cost-effective (clinically and financially) to optimize existing drugs for potency, selectivity, drug metabolism, and dosing convenience before they reach the market. This has resulted in the development of orally disintegrating tablets. Orally disintegrating tablets are patient-oriented pharmaceutical preparations which aim to enhance the safety and efficacy of the drug molecule by formulating a dosage form which disintegrates or dissolves in a few seconds after placement in the mouth. This dosage form has gained popularity among the general public because it is easily administered to geriatrics patients, pediatric patients, patients with poor physiological abilities (e.g., patients suffering from mental disorders), and patients with physical abilities (e.g., patients suffering from dysphagia), traveling patients that may not have ready access to water, and to patients that are in a situation where swallowing conventional solid oral-dosage forms presents difficulties. These tablets can be prepared in many ways like direct compression, freeze drying, sublimation, molding, and spray drying by using single or combinations of superdisintegrants or subliming agents.


Asunto(s)
Solubilidad , Administración Oral , Niño , Humanos , Comprimidos
10.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 44(4): 555-562, 2022 Aug.
Artículo en Chino | MEDLINE | ID: mdl-36065686

RESUMEN

Objective To explore the therapeutic effect of ethambutol tablets (EMB) on pulmonary tuberculosis (PTB) in rats and whether the action mechanism of EMB is related to Janus kinase (JAK)/signal transducer and activator of transcription (STAT) signaling pathway. Methods Sixty SD rats were assigned into a control group,a PTB group,a PTB+EMB group (30 mg/kg),and a PTB+EMB+Colivelin (JAK/STAT pathway activator) group (30 mg/kg+1 mg/kg) via the random number table method,with 15 rats in each group.The rats in other groups except the control group were injected with 0.2 ml of 5 mg/ml Mycobacterium tuberculosis suspension to establish the PTB model.After the modeling,the rats were administrated with corresponding drugs for 4 consecutive weeks (once a day).On days 1,14,and 28 of administration,the body weights of rats were measured and the Mycobacterium tuberculosis colonies were counted.Hematoxylin-eosin staining was carried out to detect the pathological changes in the lung tissue.Enzyme-linked immunosorbent assay was employed to measure the levels of interleukin(IL)-6,tumor necrosis factor-α (TNF-α),IL-1ß,and interferon-γ (IFN-γ) in the serum.Flow cytometry was used to determine the levels of T lymphocyte subsets CD3+,CD4+,CD8+,and CD4+/CD8+.The 16S rRNA sequencing was performed to detect the relative abundance of the intestinal microorganisms.Western blotting was employed to determine the expression of the proteins in the JAK/STAT pathway. Results Compared with the control group,the modeling of PTB reduced the rat body weight (on days 14 and 28),increased Mycobacterium tuberculosis colonies,caused severe pathological changes in the lung tissue,and elevated the levels of IL-6,TNF-α,and IL-1ß in serum and CD8+.Moreover,the modeling increased the relative abundance of Bacteroides,Peptococcus,Clostridium,Actinomyces,Lactobacillus,Verrucomicrobium,and Veillonella in the intestine,up-regulated the protein levels of phosphorylated JAK2 and phosphorylated STAT3 in the lung tissue,and lowered the levels of CD3+,CD4+,CD4+/CD8+,and IFN-γ levels (all P<0.001).Compared with the PTB group,PTB+EMB increased the rat body weight (on days 14 and 28),reduced Mycobacterium tuberculosis colonies,alleviated the pathological damage in lung tissue,lowered the levels of IL-6,TNF-α,and IL-1ß in serum and CD8+.Moreover,the treatment decreased the relative abundance of Bacteroides,Peptococcus,Clostridium,Actinomyces,Lactobacillus,Verrucomicrobium,Veillonella in the intestine,down-regulated the protein levels of phosphorylated JAK2 and phosphorylated STAT3 in the lung tissue,and elevated the levels of CD3+,CD4+,CD4+/CD8+,and IFN-γ (all P<0.001).Colivelin weakened the alleviation effect of EMB on PTB (all P<0.001). Conclusion EMB can inhibit the JAK/STAT signaling pathway to alleviate the PTB in rat.


Asunto(s)
Mycobacterium tuberculosis , Tuberculosis Pulmonar , Animales , Peso Corporal , Etambutol/farmacología , Interferón gamma/metabolismo , Interferón gamma/farmacología , Interleucina-6/metabolismo , Quinasas Janus/metabolismo , Quinasas Janus/farmacología , Mycobacterium tuberculosis/metabolismo , ARN Ribosómico 16S , Ratas , Ratas Sprague-Dawley , Factores de Transcripción STAT/metabolismo , Factores de Transcripción STAT/farmacología , Transducción de Señal , Comprimidos/farmacología , Tuberculosis Pulmonar/metabolismo , Factor de Necrosis Tumoral alfa/metabolismo
11.
Comput Intell Neurosci ; 2022: 3990427, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36045965

RESUMEN

Objective: To investigate the effects of loratadine tablets in combination with other drugs on nasal physiological function and T lymphocyte subsets in patients with allergic rhinitis (AR). Methods: A total of 120 AR patients treated in our hospital from February 2018 to February 2021 were randomly divided into control group and research group. The control group was given mometasone furoate nasal spray combined with loratadine tablets, while the research group was given budesonide combined with loratadine. The efficacy, duration of clinical symptom remission, immune function indicators, T lymphocyte subset, nasal physiological function, and incidence of adverse reactions were compared between the two groups. Results: The efficacy results of the two groups showed that the effective rate of the research group was 96.67%, while the effective rate of the control group was 83.33%. The effective rate in the research group was higher compared to the control group (χ 2: 5.925 P < 0.05). The results of clinical symptom relief time showed that the clinical symptom relief time of nasal congestion, itching, runny nose, and sneezing in the research group was lower than that in the control group, and the difference was statistically significant (P < 0.05). The results of the comparison of immune function indicators showed that the IL-6, IL-8, and IgE of the research group were lower than those of the control group, while the Th1/Th2 of the research group were higher than those of the control group. There were no statistically significant differences in T lymphocyte subsets before nursing, but after treatment, the T lymphocyte subsets of the two groups decreased, and the level of CD3+, CD4+, CD8+, CD4+, and CD4+/CD8+ lymphocytes in the research group was lower than that of the control group, and the difference was statistically significant (P < 0.05). Before treatment, there exhibited no significant difference in nasal physiological function, but after treatment, the nasal physiological function of the two groups was enhanced, and the MTT, NR, and MCR of the research group were lower than those of the control group, and the difference was statistically significant (P < 0.05). Finally, the incidence of adverse reactions in the research group was lower compared to the control group, and the difference was statistically significant (P < 0.05). Conclusion: Budesonide and loratadine are effective in improving patient efficacy, T lymphocyte subsets, and nasal physiological function, and are safer.


Asunto(s)
Antialérgicos , Rinitis Alérgica , Administración Intranasal , Antialérgicos/uso terapéutico , Budesonida/uso terapéutico , Humanos , Loratadina/efectos adversos , Rinitis Alérgica/inducido químicamente , Rinitis Alérgica/tratamiento farmacológico , Subgrupos de Linfocitos T , Comprimidos/uso terapéutico
12.
Biomed Res Int ; 2022: 2467574, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36046453

RESUMEN

Ondansetron tablets that are directly compressed using crospovidone and croscarmellose as a synthetic super disintegrant are the subject of this investigation. A central composite, response surface, randomly quadratic, nonblock (version 13.0.9.0) 32 factorial design is used to optimize the formulation (two-factor three-level). To make things even more complicated, nine different formulation batches (designated as F1-F9) were created. There were three levels of crospovidone and croscarmellose (+1, 0, -1). In addition to that, pre- and postcompressional parameters were evaluated, and all evaluated parameters were found to be within acceptable range. Among all postcompressional parameter dispersion and disintegration time, in vitro drug release experiments (to quantify the amount of medication released from the tablet) and their percentage prediction error were shown to have a significant influence on three dependent variables. Various pre- and postcompression characteristics of each active component were tested in vitro. Bulk density, tap density, angle of repose, Carr's index, and the Hausner ratio were all included in this analysis, as were many others. This tablet's hardness and friability were also assessed along with its dimension and weight variations. Additional stability studies may be conducted using the best batch of the product. For this study, we utilised the Design-Expert software to select the formulation F6, which had dispersion times of 17.67 ± 0.03 seconds, disintegration times of 120.12 ± 0.55 seconds, and percentage drug release measurements of 99.25 ± 0.36 within 30 minutes. Predicted values and experimental data had a strong correlation. Fast dissolving pills of ondansetron hydrochloride may be created by compressing the tablets directly.


Asunto(s)
Ondansetrón , Povidona , Excipientes , Solubilidad , Comprimidos
13.
Zhongguo Zhong Yao Za Zhi ; 47(15): 4221-4237, 2022 Aug.
Artículo en Chino | MEDLINE | ID: mdl-36046913

RESUMEN

The efficacy of six commonly used Chinese patent medicines for replenishing Qi and activating blood in the treatment of chronic heart failure was evaluated systematically by network Meta-analysis. Randomized controlled trials(RCTs) about the treatment of chronic heart failure were searched against CNKI, Wanfang, SinoMed, PubMed, and Cochrane library. Network Meta-analysis was performed in Stata 16. A total of 154 RCTs involving 15 620 patients were eventually included. The network Meta-analysis showed that Qili Qiangxin Capsules+conventional western medicine had the highest total effective rate, followed by Tongxinluo Capsules+conventional western medicine, Qishen Yiqi Drop Pills+conventional western medicine, Naoxintong Capsules+conventional western medicine, Shexiang Tongxin Drop Pills+conventional western medicine, Yangxinshi Tablets+conventional western medicine, and conventional western medicine. As for left ventricular ejection fraction(LVEF), Yangxinshi Tablets+conventional western medicine had the highest value, followed by Shexiang Tongxin Drop Pills+conventional western medicine, Qili Qiangxin Capsules+conventional western medicine, Tongxinluo Capsules+conventional western medicine, Qishen Yiqi Drop Pills+conventional western medicine, Naoxintong Capsules+conventional western medicine, and conventional western treatments. As for N-terminal pro-B type natriuretic peptide(NT-proBNP), Qishen Yiqi Drop Pills+conventional western medicine was the most effective treatment, followed by Yangxinshi Tablets+conventional western medicine, Shexiang Tongxin Drop Pills+conventional western medicine, Qili Qiangxin Capsules+conventional western medicine, Tongxinluo Capsules+conventional western medicine, and conventional the most effective treatment was. As for left ventricular end-diastolic diameter(LVEDD), Naoxintong Capsules+conventional western medicine was the best therapy, followed by Tongxinluo Capsules+conventional western medicine, Shexiang Tongxin Drop Pills+conventional western medicine, Yangxinshi Tablets+conventional western medicine, Qili Qiangxin Capsules+conventional western medicine, Qishen Yiqi Drop Pills+conventional western medicine, and conventional western medicine. In summary, the combination of Chinese patent medicines for replenishing Qi and activating blood with western medicines is superior to conventional western medicine alone in the treatment of chronic heart failure. It effectively improves cardiac function indicators such as LVEF, NT-proBNP, and LVEDD, and thus is worthy of popularization in clinical practice. The results of this study provide evidence-based options for the clinical treatment of chronic cardiac failure by combining the Chinese patent medicines for replenishing Qi and activating blood with western medicine.


Asunto(s)
Medicamentos Herbarios Chinos , Insuficiencia Cardíaca , Cápsulas , China , Medicamentos Herbarios Chinos/uso terapéutico , Insuficiencia Cardíaca/tratamiento farmacológico , Humanos , Metaanálisis en Red , Medicamentos sin Prescripción/uso terapéutico , Qi , Volumen Sistólico , Comprimidos , Función Ventricular Izquierda
14.
Chem Pharm Bull (Tokyo) ; 70(9): 628-636, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36047234

RESUMEN

Mini-tablets (MTs) contain a small amount of active pharmaceutical ingredients in one small tablet. MTs are advantageous because they can be fine-tuned according to the age and weight of pediatric patients and they are easy for children and the elderly to swallow. However, there are manufacturing concerns such as the difficulty in achieving both hardness and disintegration of a small tablet and it is difficult to keep the tablet weight and drug content consistent in MTs because the mold used for its production is special. In this study, we aimed to determine if an additive such as cellulose nanofibers (CNF), which has been studied in various fields in recent years, could be used to manufacture MTs without difficulties. In this study, an MT was manufactured using a rotary tableting press with a compression force of 2, 5, and 8 kN, and the weight variation, drug content variation, tensile strength, friability, disintegration time, and drug dissolution were evaluated. Of note, the tensile strength of MTs produced with a compression force of ≥5 kN was ≥1.3 MPa, which was comparable to that of an ordinary tablet with an 8 mm diameter and a hardness of ≥30 N. The disintegration time of the MT which was 20-30% CNF was ≤30 s at any compression force. MTs with CNF showed similar disintegration to MTs with other common disintegrants. Therefore, we found that CNF is a functional additive capable of manufacturing MTs by direct powder compression which has both strength and disintegration.


Asunto(s)
Celulosa , Nanofibras , Anciano , Niño , Composición de Medicamentos , Dureza , Humanos , Polvos , Comprimidos , Resistencia a la Tracción
15.
AAPS PharmSciTech ; 23(7): 246, 2022 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-36050431

RESUMEN

Compared to traditional drug release monitoring with manual sampling and testing procedures, low-field nuclear magnetic resonance (LF-NMR) imaging is a one-step, visual, non-destructive, and non-invasive measurement method. Here, we reported the application of LF-NMR to image the morphology, component, sub-diffusion, and spatial distribution of a solid oral formulation, Biyankang tablets, during dissolution in vitro. The drug ingredients with characteristic relaxation times were distinguished and localized based on the signal of standards, such as patchouli oil, Xanthium strumarium extract, and starch. The hydration, swelling, disintegration, and sub-diffusion of tablets in simulated gastric fluids (SGF) were visualized statically. All tablets showed similar expansion (37.4-42.0%) along the direction of thickness at 25 min and reached a full disintegration at 145 min, at pH 1.80-6.15, indicating pH-independent swelling and disintegration. Compared to that static immersion within 20 mL SGF, the tablet disintegration time was shortened by ~ 11% in 30 mL SGF. The application of shear reduced the time by ~ 28%, suggesting a major role of hydrodynamic condition in tablet dissolution. The ability to simultaneously visualize, distinguish, and localize drug ingredients using LF-NMR is expected to provide valuable information to develop drug release monitoring systems in vitro and potentially in vivo using small animal studies.


Asunto(s)
Hidrodinámica , Imagen por Resonancia Magnética , Animales , Liberación de Fármacos , Espectroscopía de Resonancia Magnética , Solubilidad , Comprimidos/química
16.
BMC Pharmacol Toxicol ; 23(1): 69, 2022 09 13.
Artículo en Inglés | MEDLINE | ID: mdl-36100946

RESUMEN

BACKGROUND: Hypolipidemic agents have been shown to be helpful in the primary and secondary prevention of cardiovascular disease. Most often, statins are prescribed to treat hyperlipidemia. There are a number of statins available in the market today, but atorvastatin is the most widely prescribed. It is essential that the drugs should have the appropriate amount of active pharmaceutical ingredient and meet the necessary physical properties. The main purpose of the study was to evaluate the quality of different marketed brands of atorvastatin calcium tablets available in Saudi Arabia. METHODS: In this study, innovator product coded as (AS-1) and five generics brands (coded as AS-2 to AS-6) of atorvastatin tablets 20 mg available in Saudi Arabia were evaluated for in vitro dissolution test, weight variations, friability and hardness tests. The analysis of drug was carried out by "high-performance liquid chromatography" (HPLC) method using C18 column (4.6 × 150 mm, 5 µm). The mobile phase was consisted of acetonitrile and HPLC water (pH 2.1, adjusted with orthophosphoric acid) in ratio of 52:48 v/v, the flow rate was 1.0 ml/min. Atorvastatin was detected at a wavelength of 254 nm. RESULTS: According to the results of the dissolution study, the investigated products released more than 90% of atorvastatin in 15 min. Within 60 min, the brands AS-1, AS-3, AS-5, and AS-6 depicted nearly 100% atorvastatin release, while the brand AS-2 displayed 91.69% drug release. According to our findings, the investigated atorvastatin innovator (AS-1) and generic brands such as AS-2 to AS-6 were of good pharmaceutical quality. CONCLUSIONS: All generic brands of atorvastatin tablets available in the Saudi Arabian market met the pharmacopoeia's consistency checks such as weight variation, friability, hardness and in vitro dissolution. Hence, focusing on their in vitro release properties, it was determined that these brands could be used interchangeably.


Asunto(s)
Inhibidores de Hidroximetilglutaril-CoA Reductasas , Atorvastatina , Medicamentos Genéricos , Glicolatos , Control de Calidad , Arabia Saudita , Comprimidos
17.
Sensors (Basel) ; 22(16)2022 Aug 18.
Artículo en Inglés | MEDLINE | ID: mdl-36015966

RESUMEN

Naftazone is a quinone-semi carbazone drug that possesses a strong orange color, and hence it was usually analyzed colorimetrically or by HPLC-UV. However, these methods are not sensitive enough to determine naftazone in biological samples. Naftazone lacks intrinsic fluorescence and does not possess easily derivatizable functional groups. In this contribution, we introduced the first spectrofluorimetric method for naftazone assay through reduction-elicited fluorogenic derivatization through the reduction of its quinone-semicarbazone moiety to the corresponding quinol-semicarbazide derivative by potassium borohydride as a reduction probe. The solvent-dependent fluorescence of the reaction product was studied in various protic and aprotic solvents. Eventually, the fluorescence of the reduced naftazone was measured in 2-propanol at λemission of 350 nm after excitation at λecxitation of 295 nm. The relative fluorescence intensity was linearly correlated to the drug concentration (r = 0.9995) from 10.0 to 500 ng/mL with high sensitivity, where the lower detection limit was 2.9 ng/mL. Hence, the method was effectively applied for naftazone tablets quality control with a mean %recovery of 100.3 ± 1.5, and the results agreed with those of the comparison HPLC-UV method. Furthermore, a new salting-out assisted liquid-liquid extraction (SALLE) method was established for naftazone extraction from human serum, followed by its determination using the developed reduction-based fluorogenic method. The developed SALLE method showed excellent recovery for naftazone from human serum (92.3-106.5%) with good precision (RSD ≤ 6.8%). Additionally, the reaction of naftazone with potassium borohydride was kinetically monitored, and it was found to follow pseudo-first-order kinetics with an activation energy of 43.8 kcal/mol. The developed method's greenness was approved using three green analytical chemistry metrics.


Asunto(s)
Naftoquinonas , Semicarbazonas , Humanos , Hidroquinonas , Semicarbacidas , Solventes , Espectrometría de Fluorescencia , Comprimidos
18.
Chin J Nat Med ; 20(8): 589-600, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-36031231

RESUMEN

Recent studies have showed that thrombosis is closely related to leucocytes involved in immunity. Interfering with the binding of leukocyte integrin Mac-1 and platelet GPIbα can inhibit thrombosis without affecting physiological coagulation. Mac-1-GPIbα is proposed as a potential safety target for antithrombotic agents. Guanxinning tablet (GXNT) is an oral Chinese patent medicine used for the treatment of angina pectoris, which contains phenolic acid active ingredients, such as salvianolic acids, ferulic acid, chlorogenic acid, caffeic acid, rosmarinic acid, tanshinol, and protocatechualdehyde. Our previous studies demonstrated that GXN exhibited significant antithrombotic effects, and clinical studies suggested that it did not increase bleeding risk. In addition, GXN exerted a significantly regulatory effect on immune inflammation. In the current study, we intended to evaluate the effects of GXN on bleeding events and explore the safety antithrombotic mechanism of GXN based on leukocyte-platelet interaction. First, we established a gastric ulcer model induced by acetic acid in rats and found that GXN not only did not increase the degree of gastrointestinal bleeding when gastric ulcer occurred, but also had a certain promoting effect on the healing of gastric ulcer. Second, in vitroexperiments showed that after pretreatment with GXN and activation by phorbol 12-myristate-13-acetate (PMA), the adhesion and aggregation of leukocytes with human platelets were reduced. It was also found that GXN reduced the expression and activation of Mac-1 in leucocytes, and inhibited platelet activation due to leukocyte engagement via Mac-1. Overall, the results suggest that GXN may be a safe antithrombotic agent, and its low bleeding risk mechanism is probably related to inhibited leukocyte-platelet aggregation and its interaction target Mac-1-GPIbα.


Asunto(s)
Úlcera Gástrica , Trombosis , Animales , Fibrinolíticos , Humanos , Integrinas , Leucocitos , Antígeno de Macrófago-1 , Ratas , Comprimidos
19.
Drugs R D ; 22(3): 235-243, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35918587

RESUMEN

BACKGROUND: Melatonin is an endogenous substance which plays a key role in sleep induction by reducing sleep onset latency; it has been approved by the European Food Safety Authority as a food supplement for exogenous administration. Oniria® is a food supplement formulated as 1.98 mg of prolonged-release melatonin tablets; it displays a dual dissolution profile in vitro. OBJECTIVES: The main objective of the present study was to evaluate the relative oral bioavailability of Oniria®, in comparison with immediate-release tablets (IRT) with a similar melatonin content as a reference. We also attempted to characterize the circadian rhythm of endogenous melatonin. METHODS: We performed an open-label, cross-over, randomized, phase I clinical study with two sequences and three periods involving 14 healthy volunteers. We characterized the endogenous melatonin circadian profile (period 1) and pharmacokinetics (PK) of both Oniria® and the reference melatonin (periods 2 and 3). RESULTS: Two phases were clearly differentiated in the PK profile of Oniria®. An initial one, from dosing up to 2 h, and a delayed one from 2 to 11 h post-administration. During the initial phase, both melatonin formulations were equivalent, with a Cmax value close to 4000 pg/mL. However, in the delayed phase, Oniria® showed significantly higher melatonin concentrations than the IRT (three times higher at 4-6 h post-administration). Moreover, Oniria® exhibited concentrations above the endogenous melatonin peak of 80 pg/mL for up to 2.5 h versus the reference formulation, potentially suggesting an effect of Oniria®, not only in the induction of sleep, but also in the maintenance. CONCLUSION: Oniria® could be a highly promising food supplement, not only for sleep induction but also for the maintenance of sleep.


Asunto(s)
Melatonina , Disponibilidad Biológica , Estudios Cruzados , Preparaciones de Acción Retardada , Voluntarios Sanos , Humanos , Comprimidos
20.
J Chem Inf Model ; 62(16): 3695-3703, 2022 08 22.
Artículo en Inglés | MEDLINE | ID: mdl-35916486

RESUMEN

An autoencoder architecture was adopted for near-infrared (NIR) spectral analysis by extracting the common features in the spectra. Three autoencoder-based networks with different purposes were constructed. First, a spectral encoder was established by training the network with a set of spectra as the input. The features of the spectra can be encoded by the nodes in the bottleneck layer, which in turn can be used to build a sparse and robust model. Second, taking the spectra of one instrument as the input and that of another instrument as the reference output, the common features in both spectra can be obtained in the bottleneck layer. Therefore, in the prediction step, the spectral features of the second can be predicted by taking the reverse of the decoder as the encoder. Furthermore, transfer learning was used to build the model for the spectra of more instruments by fine-tuning the trained network. NIR datasets of plant, wheat, and pharmaceutical tablets measured on multiple instruments were used to test the method. The multi-linear regression (MLR) model with the encoded features was found to have a similar or slightly better performance in prediction compared with the partial least-squares (PLS) model.


Asunto(s)
Espectroscopía Infrarroja Corta , Calibración , Análisis de los Mínimos Cuadrados , Espectroscopía Infrarroja Corta/métodos , Comprimidos
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