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@#Using high performance liquid chromatography and high resolution orbital trap mass spectrometry, a two-dimensional online desalting detection method was established to determine the structure of the impurities detected under the official testing conditions of lansoprazole enteric solution preparation, and a chromatographic method compatible with mass spectrometry was established to determine and presume the structure of the impurities that could not be separated by the the official testing method.The identification of impurity was to presume its structure according to the presence of impurity reference product, so as to investigate the difference of impurity spectrum of products from different manufacturers.The one-dimensional chromatographic conditions for the 2D online desalting method were the same as those in China Pharmacopoeia (2020) under relevant substances.Two-dimensional chromatography was performed on a Waters C18 T3 column (2.1 mm × 100 mm, 1.7 μm) with 0.1% formic acid in water-acetonitrile mobile phase and gradient elution.The chromatographic conditions for the compatible mass spectra were based on an Agilent Extend C18 (4.6 mm × 150 mm, 5 μm) column with mobile phase A: 25 mmol/L ammonium acetate and B: 25 mmol/L ammonium acetate-acetonitrile (1∶4) [pH adjusted to 6.5 with glacial acetic acid], with gradient elution. Nine impurities were detected by two-dimensional online desalting method, with 5 known impurities (A-E) and 4 unknown ones.14 impurities were detected by the compatible mass spectrometry method, with 9 unknown impurities (4 consistent with the results of two-dimensional online desalting method, and 5 newly detected).The structures and sources of the unknown impurities were deduced.The two detection methods of lansoprazole preparation by high-performance liquid chromatography-high resolution orbital trap mass spectrometry have guiding significance for quality control and process evaluation.
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Cholesterol is an important precursor of many endogenous molecules. Disruption of cholesterol homeostasis can cause many pathological changes, leading to liver and cardiovascular diseases. CYP1A is widely involved in cholesterol metabolic network, but its exact function has not been fully elucidated. Here, we aim to explore how CYP1A regulates cholesterol homeostasis. Our data showed that CYP1A1/2 knockout (KO) rats presented cholesterol deposition in blood and liver. The serum levels of low-density lipoprotein cholesterol, high-density lipoprotein cholesterol and total cholesterol were significantly increased in KO rats. Further studies found that the lipogenesis pathway (LXRα-SREBP1-SCD1) of KO rats was activated, and the key protein of cholesterol ester hydrolysis (CES1) was inhibited. Importantly, lansoprazole can significantly alleviate rat hepatic lipid deposition in hypercholesterolemia models by inducing CYP1A. Our findings reveal the role of CYP1A as a potential regulator of cholesterol homeostasis and provide a new perspective for the treatment of hypercholesterolemia.
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Abstract Objective To investigate the effects of combination therapy with cholecalciferol and lansoprazole on residual β-cell function and glycemic control in children with new-onset type 1 diabetes. Methods Children aged 6-12 years with type 1 diabetes were allocated to receive cholecalciferol and lansoprazole (Group 1) or no treatment (Group 2). Children were maintained on their respective insulin regimens and kept records of blood sugar and insulin doses taken. Children were followed at three-month intervals for six months. Changes in mean fasting C-peptide and HbA1c levels, daily insulin doses, fasting blood glucose and mean blood glucose levels from baseline to end of the study were analyzed. Results Twenty-eight children (14 per group) met the eligibility criteria. Fasting C-peptide levels decreased significantly from baseline to study end in both groups (mean decrease -0.19±0.09ng/mL and -0.28±0.08ng/mL, p=0.04 and p=0.001; Group 1 and Group 2 respectively). However, fasting C-peptide level drop was significantly smaller in Group 1 compared to Group 2 (30.6% and 47.5% respectively; p=0.001). Likewise, daily insulin doses decreased significantly in both groups (-0.59±0.14units/kg and -0.37±0.24units/kg respectively; p=0.001). All patients recruited completed the study. No adverse events were reported. Conclusion Combined therapy with cholecalciferol and lansoprazole for six months was associated with smaller decline in residual β-cell function and lower insulin requirements in children with new-onset type 1 diabetes. Preliminary findings of this small-scale study need to be confirmed by larger studies. Registry of Clinical Trials (www.ctri.nic.in) under number REF/2021/03/041415 N.
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Objective@#To investigate the efficacy and safety of magnesium aluminium carbonate, lansoprazole, amoxicillin and furazolidone in the treatment of Helicobacter pylori-related gastric ulcer.@*Methods@#From March 2016 to December 2017, 120 patients with HP related gastric ulcer who met the inclusion criteria were enrolled in the digestive department of Linxi Hospital of Kailuan general hospital.They were divided into observation group and control group with random number table method, 60 cases in each group.The control group was given lansoprazole+ amoxicillin+ furazolidone triple therapy.On this basis, the observation group was added with magnesium aluminum carbonate.The clinical efficacy, clearance rate of Helicobacter pylori, the level of VEGF and EGF in gastric juice were compared between the two groups.@*Results@#The total clinical effective rate of the observation group was 95.0% (57/60), which was significantly higher than that of the control group (83.3%) (50/60). The difference between the two groups was statistically significant (χ2=4.23, P<0.05). The comprehensive symptom scores of the two groups decreased significantly with the treatment time (observation group: before treatment(9.6±2.2), treatment 2 weeks (5.5±1.5), treatment 4 weeks (4.3±1.2), treatment 6 weeks (3.1±0.8), control group (9.4±2.5), treatment 2 weeks (7.2±1.3), treatment 4 weeks (6.6±1.4), treatment 6 weeks (4.5±1.0)), and observation group syndrome scores There was significant difference between the two groups (Finter-group=23.54, Pinter-group<0.05; Fintra-group=87.62, Pintra-group<0.05; Finteraction=8.47, Pinteraction<0.05). After treatment, VEGF level in gastric juice of the two groups increased significantly after treatment.In the observation group( (429.4±128.5) pg/ml )was significantly higher than that in the control group( (380.3±137.2) pg/ml, t=2.02, P<0.05). The EGF level in gastric juice of the two groups increased significantly after treatment.In the observation group( (658.1±164.0) pg/ml )was significantly higher than that in the control group ((583.5±135.1) pg/ml, t=2.72, P<0.05). The incidence of adverse reactions was 6.7% (4/60) in the observation group and 8.3% (5/60) in the control group.There was no significant difference (χ2=0.12, P>0.05).@*Conclusion@#The treatment of Helicobacter pylori related gastric ulcer with the combination of aluminum carbonate, lansoprazole, amoxicillin and furazolidone can obviously improve the clinical symptoms and promote the regeneration of ulcer mucosa.
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Objective To observe the clinical effect of lansoprazole enteric -coated tablets combined with flupentixol and melitracen in the treatment of erosive gastritis with anxiety .Methods Eighty patients with erosive gastritis complicated with anxiety were selected , and they were randomly divided into control group ( n =40 ) and observation group( n=40) according to the digital table .The control group was treated with lansoprazole enteric -coa-ted tablets.The observation group received lansoprazole enteric -coated tablets combined with flupentixol and melitra-cen.Hamming anxiety scale ( HAMA ) and Hamilton depression scale ( HAMD ) were used to evaluate in the two groups before and after treatment .The changes of HAMA and HAMD scores were compared between the two groups .Results Before treatment,the scores of abdominal pain ,bloating,pantothenic acid and belching had no statistically significant differences between the two groups (all P>0.05).After treatment for 4 weeks,the scores of abdominal pain,bloating, pantothenic acid and belching in the observation group were ( 0.63 ±0.12 ) points, ( 0.43 ± 0.11)points,(0.30 ±0.11)points and (0.31 ±0.14)points,respectively,which were lower than those in the control group [(1.42 ±0.18)points,(1.08 ±0.15)points,(0.79 ±0.16)points,(0.98 ±0.25)points] (t=15.396, 13.285,16.758,17.492,all P<0.05).The scores of HAMA and HAMD in the observation group were (12.15 ± 2.51)points and (14.32 ±2.51) points,respectively,which were lower than those in the control group [(19.84 ± 2.65)points,(19.84 ±3.17)points](t=20.151,21.841,all P<0.05).There was no statistically significant differ-ence in the incidence rate of adverse reactions between the two groups after treatment for 4 weeks (P >0.05) .Conclusion Lansoprazole enteric -coated tablets combined with flupentixol and melitracen in the treatment of erosive gastritis with anxiety can relieve anxiety and depression ,improve clinical symptoms and treatment effect .
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Objective:To prepare lansoprazole enteric-coated pellets and compress them into orally disintegrating tablets , and e-valuate the acid resistance in the acid stage and the in vitro dissolution in the buffer stage .Methods:Lansoprazole enteric-coated pel-lets were prepared by fluid bed coating technology , and the effects of the ratio of methacrylic acid copolymer dispersion to ethyl acrylate–methyl methacrylate copolymer dispersion , the concentration of triethyl citrate and the main pressure on the acid resistance in the acid stage and the in vitro dissolution in the buffer stage were evaluated .The similarity of the self-prepared orally disintegrating tablets and the reference preparation was evaluated by using f 2 similarity factor method .Results:The average particle size of microcrystalline cellulose core was 150-180 μm, the ratio of methacrylic acid copolymer dispersion to ethyl acrylate –methyl methacrylate copolymer dispersion was adjusted to 8:2, the enteric-coated weight was 30％, 20％triethyl citrate was used and the main pressure was controlled within the range of 10-16 kN.Lansoprazole enteric-coated pellets had sufficiently flexibility and stability against the compression force . The enteric coating did not break , showing good acid resistance .The dissolution similarity factor of the self-prepared orally disintegra-ting tablets and the reference preparation was greater than 50.Conclusion: Lansoprazole enteric-coated pellets orally disintegrating tablets have good acid resistance and high similarity for the in vitro dissolution, which can be further amplified .
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OBJECTIVE:To observe therapeutic efficacy and safety of lansoprazole triple therapy in the treatment of Helicobacter pylori (Hp) associated gastric ulcer.METHODS:A total of 80 patients with Hp associated gastric ulcer were randomly divided into control group (40 cases) and combination group (40 cases).Control group was given Lansoprazole capsules 30 mg once in the morning or before bedtime,for 6 weeks.Combination group was given Lansoprazole capsules (same usage and dosage as control group)+Clarithromycin tablets 0.5 g,twice a day+Amoxicillin dispersible tablets 1 g,twice a day,for consecutive 1 week,and then given Lansoprazole capsules 30 mg once in the morning or before bedtime,for 5 weeks.Patients with amoxicillin allergy were switched to Metronidazole tablets 0.4 g,twice a day.Hp eradication rate of 2 groups were observed;recrudescence rate of Hp negative patients and the recurrence of effective patients were observed after 6,12 months of treatment.The leve1s of Th1 cytokines (IFN-γ,IL-2,IL-12) and Th2 cytokines (IL-4,IL-6,IL-10) were observed before and after treatment,and the occurrence of ADR was recorded.RESULTS:There was no statistical significance in total response rate of ulcer healing,Hp eradication rate or the incidence of ADR between 2 groups (P＞0.05).After 6 months of treatment,there was no statistical significance in recurrence rate between 2 groups (P＞0.05).The recurrence rate of combination group after 12 months of treatment and recrudescence rate of combination group after 6,12 months of treatment were significantly lower than those of control group,with statistical significance (P＜0.05).Before treatment,there was no statistical significance in Th1 type cytokines and Th2 cytokines between 2 groups (P＞0.05).After 1 week and 6,12 months of treatment,the levels of INF-γ,IL-2,IL-12 and IL-6 in 2 groups were significantly lower than before;the levels of INF-γ,IL-2 and IL-12 in combination group were significantly lower than control group after 12 months of treatment.After 1 week and 6,12 months of treatment,the levels of IL-4 and IL-10 in 2 groups were significantly higher than before;those indexes of combination group were significantly higher than those of control group after 12 months of treatment,with statistical significance (P＜0.05);but there was no statistical significance in the level of IL-6 between 2 groups (P＞0.05).CONCLUSIONS:Lansoprazole triple therapy shows significant therapeutic efficacy for Hp associated gastric ulcer,improve cytokines level and reduces recurrence rate and recrudescence rate without increasing the incidence of ADR.
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Objective To evaluate the efficacy and safety of different doses Octreotide combined with Lansoprazole in the treatment of hepatocirrhosis with upper gastrointestinal bleeding.Methods Eighty hepatocirrhosis patients with upper gastrointestinal bleeding during May.2013 to May.2016 were treated with Octreotide combined with Lansoprazole,and were divided into high dose group (40 cases) and low dose group (40 cases) according to different doses Octreotide.Before and after treatment,portalvenousmaximumvelocity (PVV) and portalveindiameter (PVD) were detected by color Doppler ultrasound respectively,and haemostatic time,blood transfusion cases and volume,rehaemorrhagia cases were recorded,and adverse reactions were observed.Results After treatment,PVV and PVD of the two groups were significantly ameliorative (P ＜ 0.05),and there were no significantly different between two groups.Haemostatic time,blood transfusiorate,blood transfusiorate volume and rehaemorrhagia rate of the high dose group were significantly less than the low dose group (P ＜ 0.05).The clinical effective rate of the high dose group was significantly higher than that of the low dose group (P ＜ 0.05).The rate of adverse reactions of the high dose group was not significantly different from that of the low dose group.Conclusions High doses Octreotide combined with Lansoprazole in the treatment of hepatocirrhosis with upper gastrointestinal bleeding have a gain on hemostatic effect,and cannot increase adverse reactions significantly.
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Objective To study and analyze the effects of triple therapy (clarithromycin, amoxicillin, and lansorazole) combined with psychological intervention in the treatment of elderly peptic gastric ulcer. Methods 100 patients with aged gastrointestinal ulcer who were admitted to the hospital from February 2015 to April 2016 were selected as the study subjects, randomly divided into the control group and the experimental group, and 50 patients in each group.The control group was treated with conventional treatment, the experimental group was treated with triple therapy (clarithromycin, amoxicillin, lansorazole) combined with psychological intervention therapy, pay attention to the psychological state of the patients, strengthen the communication and exchanges with the patient, the treatment of patients with increased confidence and treatment compliance. The treatment effect of the experimental group and the control group was compared. Results After the corresponding treatment, the effective rate of treatment in the experimental group was 96.0%, significantly higher than the control group (86.0%), the difference was statistically significant (P<0.05). No obvious adverse reactions were found in the experimental group and the control group. The recurrence rate in the control group was 400%, which was significantly higher than that in the experimental group (14.0%), the difference was statistically significant (P<0.05). Conclusion Triple therapy (clarithromycin, amoxicillin, lansorazole) combined with psychological intervention in treatment of elderly peptic ulcer effect is good, can significantly improve the treatment efficiency, the recurrence rate is low.
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Objective To study and analyze the effects of triple therapy (clarithromycin, amoxicillin, and lansorazole) combined with psychological intervention in the treatment of elderly peptic gastric ulcer. Methods 100 patients with aged gastrointestinal ulcer who were admitted to the hospital from February 2015 to April 2016 were selected as the study subjects, randomly divided into the control group and the experimental group, and 50 patients in each group.The control group was treated with conventional treatment, the experimental group was treated with triple therapy (clarithromycin, amoxicillin, lansorazole) combined with psychological intervention therapy, pay attention to the psychological state of the patients, strengthen the communication and exchanges with the patient, the treatment of patients with increased confidence and treatment compliance. The treatment effect of the experimental group and the control group was compared. Results After the corresponding treatment, the effective rate of treatment in the experimental group was 96.0%, significantly higher than the control group (86.0%), the difference was statistically significant (P<0.05). No obvious adverse reactions were found in the experimental group and the control group. The recurrence rate in the control group was 400%, which was significantly higher than that in the experimental group (14.0%), the difference was statistically significant (P<0.05). Conclusion Triple therapy (clarithromycin, amoxicillin, lansorazole) combined with psychological intervention in treatment of elderly peptic ulcer effect is good, can significantly improve the treatment efficiency, the recurrence rate is low.
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Objective To analyze the curative effect and adverse reaction of lansoprazole combined with droperidol thiadiazole melitracen treatment in patients with functional dyspepsia.Methods From December 2013 to December 2015 in our hospital and accepted treatment of 90 patients with functional digestive adverse as the research object,according to the random number table were divided into the control group and the observation group,45 cases in each group.The control group by oral administration of lansoprazole enteric coated capsules,the observation group taking oral lansoprazole and droperidol thiadiazole melitracen,course lasted for 4 weeks,efficacy and adverse occurrence was compared between two groups of patients.Results After 4 weeks of treatment,the observation group with symptoms score GSRS(postprandial fullness discomfort,early satiety,abdominal pain,epigastric burning sensation were lower than the control group with postprandial fullness discomfort early satiety,abdominal pain,epigastric burning sensation,and the difference was statistically significant(P<0.05); the patients in the observation group after 4 weeks of treatment,the total effective rate(86.7％)was higher than the control group(66.7％)significantly,and difference was statistically significant(P<0.05); symptoms of adverse reactions of two groups of patients in the process of drug use were mild and did not give special treatment,in a few days after the basic relief.Conclusion Lansoprazole combined with fluorine Pai Sai tons of Murray Song Xin can effectively eliminate or reduce the symptoms of functional dyspepsia patients clinical and no serious adverse reactions,it is safe in clinical application.
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OBJECTIVE:To observe the clinical efficacy and safety of Xiangsha yangwei pills combined with lansoprazole in the treatment of spleen deficiency and qi stagnation (SSQS) type chronic atrophic gastritis (CAG).METHODS:A total of 120 patients with SSQS type CAG were randomly divided into control group and observation group,with 60 cases in each group.Both groups received routine treatment.Control group was additionally given Lansoprazole enteric-coated capsule 30 mg,once a day,on an empty stomach in the morning.Observation group was additionally given Xiangsha yangwei pills 59 g,twice a day,on the basis of control group.Both groups were treated for consecutive 4 weeks.Clinical efficacies of 2 groups were observed and compared,and TCM syndrome score and pathological integral were observed before and after treatment.The occurrence of ADR was recorded.RESULTS:After treatment,total response rate and excellent effective rate of observation group were 95.00％ and 83.33％,which were significantly higher than those of control group (86.67％ and 57.53％),with statistical significance (P＜0.05).Before treatment,there was no statistical significance in TCM syndrome score or pathological integral between 2 groups (P＞0.05);after treatment,TCM syndrome score and pathological integral of 2 groups were significantly lower than before treatment,and those of observation group were significantly lower than those of control group,with statistical significance (P＜0.05).The incidence of ADR in observation group was significantly lower than that control group,with statistical significance (P＜0.05).CONCLUSIONS:Xiangsha yangwei pill combined with lansoprazole show good therapeutic efficacy and safety for SSQS type CAG and can significantly improve clinical and pathological symptoms.
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Objective To prepare lansoprazole biphasic release pellet capsules. Methods The pellets carrying lansoprazole were directly prepared by centrifugal making-pill method, and the pellets of enteric coating and enteric pulsatile coating were adopted by fluidized bed coating method. Then the two kinds of pellets were filled by a fixed proportion to hollow capsules. In vitro dissolution method was used for the observation of the drug release behavior. Results The optimized formulation was as follows: the magnesium carbonate level was 15%, the L-HPC level was 20% in pellets carried drug, the isolation gown level was 9%-10%, the enteric coating level was above 41% in enteric coated pellets, the swelling agent level was 50-60%, the controlled layer level was 50%, the enteric coating level was above 41% in pulsatile enteric coated pellets, and the drying time was 4 h in the end. Conclusion The method is feasible for preparation of lansoprazole biphasic release pellet capsules by encapsulating enteric-coated pellets, and able to obtain good repeatability and stable quality.
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OBJECTIVE:To systematically review the effect of CYP2C19 genetic polymorphism on lansoprazole pharmacoki-netics,and provide evidence-based reference for clinical individualized medication of lansoprazole. METHODS:Retrieved from PubMed,EMBase,Web of science,Cochrane Library and CJFD,retrospective studies about the effect of CYP2C19 genetic poly-morphism on lansoprazole pharmacokinetics were collected,Meta-analysis was performed by Rev Man 5.2 software after data ex-tract and quality evaluation. RESULTS:Totally 11 retrospective studies were included,involving 200 patients. The gene type in-cluded homozygote express metabolizers (EM),heterozygous express metabolizers (HEM) and slow metabolizers (PM). Results of Meta-analysis showed CYP2C19 polymorphism significantly affected cmax,AUC,t1/2,tmax and CL/F. The cmax and AUC in group PM were higher than group HEM and group EM;CL/F in group EM was higher than group HEM and group PM;t1/2 in group PM was higher than group HEM and group EM,while there was no significant difference in the t1/2 between group HEM and group EM;tmax in HEM and group PM were higher than group EM,while there was no significant difference in the tmax between group PM and group HEM. CONCLUSIONS:CYP2C19 genetic polymorphism shows obvious effect on lansoprazole pharmacokinetics, which is the key factor for causing efficacy of lansoprazole and individual differences among adverse reactions,and clinic should take into account individualized dose regimen of lansoprazole.
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Objective To prepare lansoprazole biphasic release pellet capsules. Methods The pellets carrying lansoprazole were directly prepared by centrifugal making-pill method,and the pellets of enteric coating and enteric pulsatile coating were adopted by fluidized bed coating method. Then the two kinds of pellets were filled by a fixed proportion to hollow capsules. In vitro dissolution method was used for the observation of the drug release behavior. Results The optimized formulation was as follows:the magnesium carbonate level was 15%,the L-HPC level was 20%in pellets carried drug,the isolation gown level was 9%-10%,the enteric coating level was above 41%in enteric coated pellets,the swelling agent level was 50-60%,the controlled layer level was 50%,the enteric coating level was above 41%in pulsatile enteric coated pellets,and the drying time was 4 h in the end. Conclusion The method is feasible for preparation of lansoprazole biphasic release pellet capsules by encapsulating enteric-coated pellets,and able to obtain good repeatability and stable quality.
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Objective To investigate the effect of lansoprazole injection on 24-hour intragastric pH in healthy volunteers. Methods The volunteers inclouding 10 women and 10 men, were divided into experitmental group and control group randomly, each group of 10 cases. After testing the pH initial value in stomach through pH determination electrode, the cases in experitmental group were drip the drug of lansoprazole injection, the cases in control group were drip the same volume of 0.9% sodium chloride solution. Then constantly determined the value of pH in the stomach for 24 h. Results The pH value in the stomach of expertimental group after injected lansoprazole was significantly higher than that before administration (P < 0.05). The pH value in the stomach of expertimental group was higher than that in control group between finished of injection and 24 h, especially in the first 12 h after administration, there were significantly differences (P < 0.01). The pH value in experimental group after injected lansoprazole for 24 h was 4.565 ± 1.109, in control group was 2.211 ± 0.263, there was significant difference (P < 0.01). The percentage of maintenance time of pH reaching 4.0 and 6.0 in stomach in experimental group were (73.36 ± 21.08)% and (53.22 ± 23.76)% , in control group were (13.28 ± 10.55)%and (3.92 ± 2.17)%, there were significant differences (P<0.01). Conclusions The strength of acid suppresion of lansoprazole injection is worthy of approving, and it can work at full capacity in treatment of patients with peptic ulcer complicated with upper gastrointestinal hemorrhage if lansoprazole is given every 12 h.
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abstract The aim of this study was to evaluate the effects of caffeine, tea polyphenol and daidzein on the pharmacokinetics of lansoprazole and its metabolites. Rats were intragastrically administered caffeine (30 mg·kg-1, once per day), tea polyphenol (400 mg·kg-1, once per day) or daidzein (13.5 mg·kg-1, once per day) for 14 days, followed by an intragastric administration of lansoprazole (8 mg·kg-1) on the 15th day. The plasma concentrations of lansoprazole and its two primary metabolites, 5-hydroxylansoprazole and lansoprazole sulfone, were determined by high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS). Tea polyphenol significantly elevated the Area Under the Curve (AUC) of lansoprazole from 680.29 ± 285.99 to 949.76 ± 155.18 μg/L.h and reduced that of lansoprazole sulfone from 268.82 ± 82.37 to 177.72 ± 29.73 μg/L.h. Daidzein increased the AUC of lansoprazole from 680.29 ± 285.99 to 1130.44 ± 97.6 μg/L.h and decreased that of lansoprazole sulfone from 268.82 ± 82.37 to 116.23 ± 40.14 μg/L.h. The pharmacokinetics of 5-hydroxylansoprazole remained intact in the presence of tea polyphenol or daidzein. Caffeine did not affect the pharmacokinetics of lansoprazole and its metabolites. The results imply that tea polyphenol and daidzein may inhibit the in vivo metabolism of lansoprazole by suppressing CYP3A.
resumo O objetivo deste estudo foi avaliar os efeitos da cafeína, do polifenol do chá e da daidzeína na farmacocinética do lansoprazol e de seus metabólitos. Administraram-se, intragastricamente, aos ratos cafeína (30 mg·kg-1, uma vez ao dia), polifenol do chá(400 mg·kg-1, uma vez ao dia) ou daidzeína (13,5 mg·kg-1, uma vez ao dia), por 14 dias, seguindo-se a administração de lansoprazol (8 mg·kg-1) no 15º. dia. As concentrações plasmáticas do lansoprazol e de seus dois metabólitos primários, 5-hidroxilansoprazol e sulfona de lansoprazol, foram determinadas por cromatografia líquida de alta eficiência acoplada com espectrometria de massas (CLAE-EM/EM). O polifenol do chá elevou, significativamente, a Área Sob a Curva (ASC) do lansoprazol de 680,29 ± 285,99 para 949,76 ± 155,18 μg/L.h e reduziu a da sulfona de lansoprazol de 268,82 ± 82,37 para 177,72 ± 29,73 μg/L.h. A daidzeína aumentou a ASC do lansoprazol de 680,29 ± 285,99 para 1130,44 ± 97,6 μg/L.h e reduziu a da sulfona de lansoprazol de 268,82 ± 82,37 para 177,72 ± 29,73 μg/L.h. A farmacocinética do 5-hidroxilansoprazol permaneceu intacta na presença de polifenol do chá ou daidzeína. A cafeína não afetou a farmacocinética do lansoprazol e de seus metabólitos. Os resultados sugerem que o polifenol do chá e a daidzeína podem inibir o metabolismo in vivo do lansoprazol por supressão da CYP3A.
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Rats , Caffeine/pharmacokinetics , Polyphenols/pharmacokinetics , Lansoprazole/pharmacokinetics , Rats , PharmacokineticsABSTRACT
Objective: The development of new delivery systems for the controlled release of drugs is one of the most innovative fields of research in pharmaceutical sciences. Nanoparticles specially designed to release the drug in the vicinity of target sites. The aim of this study was to formulate and evaluate the Lansoprazole nanoparticles to improve the therapeutic efficacy of Lansoprazole by loading in nanoparticle drug delivery system. Materials and Methods: Lansoprazole loaded chitosan nanoparticles (CNP1 to CNP10) were prepared by ionotropic gelation method. The formulated nanoparticles were evaluated for external morphological characters, determination of particle size analysis, zeta potential, drug content, entrapment efficiency and in-vitro release studies. Results: The drug content for the Lansoprazole loaded chitosan nanoparticles varied from 69.5±7.2% to 87.9±1.2%. The entrapment efficiencies were found to be minimum and maximum of 39.3±2.6% and 85.6±1.2%, the optimum entrapment efficiency was found to be 85.3±0.8%, particle size varied from 360±12nm to 814±62nm, zeta potential values were in positive and increased from 11.2±1.2mV to 18.7±0.4mV. In-vitro release of drug follows zero order and showed sustained release behavior for a period of 24 hr. Conclusion: The study demonstrated the successful preparation of sustained release polymeric nanoparticles of Lansoprazole.
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Objective:To establish the method for determining the related substances in lansoprazole for injection and qualitatively study the impurities. Methods:An HPLC method and an HPLC-MS method were used with isocratic elution and DAD as the detector. Results:The priciple impurity in all samples was impurity B. Conclusion:The method is fast, simple and sensitive, and suitable for the determination of the related substances in lansoprazole for injection.
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Objective To observe the clinical efficacy and safety of application of lafutidine treated in curing peptic ulcer.Methods Eighty-four patients with peptic ulcer were randomly assigned to receive either lafutidine(10 mg) twice daily in 42 patients of cured group or lansoprazole (30 mg) once daily for 4 weeks in 42 patients of control group.Ulcer healing rate and clinical performance were examined after treatment.Results The first,third and seventh day of peptic ulcer healing rate were 38.09％ (16/42), 71.42％ (30/42) and 90.47％ (38/42) in the lansoprazole group and 23.81％ (10/42), 76.19％ (32/42) and 85.71％ (36/42) in the lafutidine group.There were no siginificant difference between two groups (P =0.157,0.620, 0.736).Gastroscope examination showed the complete healing rate, average healing rate and general clinical effectiveness were 61.90％(26/42) ,30.95％(13/42) and 97.61％(41/42) in the lansoprazole group,while the number for lafutidine group were 57.14％ (24/42), 28.57％ (12/42) and 95.23％ (40/42).There were no siginificant difference between two groups (P =0.657, 0.811, 1.000).No severe side-effect was occurred in both groups.Conclusion Use Lafutidine to cure peptic ulcer can promote healing effectively, improve patients' clinical symptoms which is similar to lansoprazole.