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The aim of present work was to enhancing the solubility and dissolution rate of the aquaphobic drug Lafutidine by liquisolid technique. Lafutidine is a H2-receptor antagonist BCS class II drug. Lafutidine compatibility with excipients was evaluated by FT-IR and DSC spectrum. Preliminary trial taken to check the effect of carrier to coating material ratio (R) and non-volatile solvent (PEG- 600) on pre compression and post compression characteristic. Flowable liquid retention potential (Ø -value) and Liquid load factors (Lf) were calculated for required amount of excipients necessary to preparing Lafutidine liquisolid tablet. A 32 full factorial design was employed to check the effect of carrier to coating material ratio R (X1) and PEG- 600 (X2) on hardness (Y1), angle of repose (Y2), % of Cumulative drug release at 5 min Q5 (Y3), and disintegration time (Y4). Multiple linear regression analysis, ANOVA and graphical representation of the influence of factor by 3D plots were performing by using Design expert 7.0. In this study, the following constraints were arbitrarily used for the selection of an optimized batch: Hardness: 3 to 5.5, Angle of repose: 25 to 30, % of Cumulative Drug Release at 5 min (Q5) > 27.09 % and Disintegration time <1.3 min. The desirability value of various dependent variables calculated for determining the optimized batch of tablet and it was also found to be nearer to one. Performance of optimized batch had no shown any significant change at the end of stability study.
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We report a case of Paclitaxel-induced peripheral neuropathy successfully treated with lafutidine and tocoferol nicotinate(TN). Case Report: A 72-year-old male patient with pulmonary adenocarcinoma of left upper lobe, and metastasis of the liver. He suffered from the feelings of pins and needles of the limbs after the paclitaxel treatment, and admitted to our hospital. There was almost no remarkable change in the feelings of pins and needles with TN at 300mg per day, however, after addition of lafutidine at 20mg per day, those symptoms improved markedly, and he came to be able to walk alone. Therefore we reduced the dose of TN, those symptoms got worse. We restored TN to 300mg per day again, then these symptoms got better and he came to walk alone out of doors again. Consideration: Administration of lafutidine with TN improved the paclitaxel-induced peripheral neuropathy. Since the speed of the regeneration of the peripheral neurons is slow and changing the dose of TN affected the symptoms immediately, we considered that the improvement of the feelings of pins and needles of the limbs is due to the synergistic effect of the increase of the microvascular bloodflow of TN and lafutidine, and the effect of desensitization through the capsaicin-sensitive afferent neurons, although the hypothesis needs further investigation.
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Objective To investigate influence of lafutidine combined with omeprazole in serum pepsinogen subgroup levels of patients with chronic atrophic gastritis. Methods One hundred and thirty-eight patients with chronic atrophic gastritis were selected in the First Affiliated Hospital of Changchun Traditional Chinese Medicine University from Dec. 2010 to Dec. 2013,who were randomly divided into two groups. Sixty-nine patients treated omeprazole( oral 1 pill/times,1 times/d)as control group,and another 69 patients were treated lafutidine( oral 2 pills/times,2 times/d ) combined with omeprazole as observation group. Both Course of treatment was 8 weeks. Changes of serum pepsinogen subgroups,improvement of clinical symptoms,treatment effect and adverse reactions were compared between two groups. Results After treatment,the levels of pepsinogen I,pepsinogen I/pepsinogen II increased significantly while pepsinogen II decreased significantly in two groups. Pepsinogen I,pepsinogen I/pepsinogen II in observation group were(89. 46 ± 13. 25)μg/L,10. 21 ± 1. 27,significantly higher than control group(( 62. 34 ± 11. 90 )μg/L,6. 45 ± 0. 93;t =7. 358,9. 125;P=0. 017,0. 004). Pepsinogen II in observation group was(8. 76 ± 3. 24)μg/L,significantly lower than control group((9. 68 ± 4. 76 )μg/L,t =4. 035,P =0. 049 ). Stomachache disappearance rate,abdominal distention disappearance rate,loss of appetite disappearance rate,total efficiency in observation group were 89. 9%, 85. 5%,84. 1% and 98. 6% respectively,significantly higher than control group( 73. 9%,65. 2%,60. 9% and 82. 6%),and the differences were statistically significant( P ﹤ 0. 05 ). Incidence of adverse reaction in observation group was 5. 8%,higher than control group( 2. 9%),but the difference was not statistically significant(χ2 =0. 697,P﹥0. 05). Conclusion Lafutidine combined with omeprazole can significantly improve clinical symptoms of patients with chronic atrophic gastritis,which can also significantly improve serum pepsinogen subgroup levels. Lafutidine combined with omeprazole have significant clinical effect and high safety, which is worthy of clinical application.
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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.
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Aims: To assess the efficacy of lafutidine therapy versus rabeprazole in Indian patients with endoscopically and histologically proven gastritis and peptic ulcer. Study Design: A double blind, double dummy, randomized, comparative study. Place and Duration of Study: Global Liver and Gastroenterology Centre, Bhopal, India, between March 2010 and October 2010. Methodology: A total of 100 patients were enrolled, including 50 with endoscopically and histologically proven gastritis and other 50 with peptic ulcer (over 5 mm in diameter). Each group was randomized to receive either lafutidine or rabeprazole tablet and their corresponding competitor placebo dummy tablet, for a period of 4 weeks. Cure rate was confirmed endoscopically at the end of week 4 as compared to the baseline evaluation. Symptom response and Helicobacter pylori (H. Pylori) eradication were also compared among the two drugs at the end of the treatment period. Results: Complete cure of gastritis was observed in all the patients (100%) treated with lafutidine and 95.24% [20/21; 95% CI: 76.18 to 99.88%] patients treated with rabeprazole. Complete cure of ulcer was observed in 72.0 (18/25, 95% CI = 50.61 to 87.93%) and 79.16% (19/24, 95% CI = 57.85 to 92.87%) patients treated with lafutidine and rabeprazole respectively. There was no significant difference in gastritis/ulcer cure rate and symptom response rate between the two treatment groups at the end of the study. H pylori eradication rates was 82.61% (19/23) in lafutidine group vs 47.37% (9 /19) in rabeprazole group (Δ=35.2%, 95% CI = 3.2 to 67.3%; P= .023). Both, lafutidine and rabeprazole were well tolerated during the entire study. Conclusion: Endoscopically proven cure rate in patients suffering from gastritis and peptic ulcers is found to be comparable after 4 weeks treatment with Lafutidine and rabeprazole, but lafutidine showed better H. pylori eradication rate as compared to rabeprazole.
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Aims: To evaluate the symptomatic efficacy and safety of Lafaxid™ (lafutidine 10 mg) in Indian patients with Acid Peptic disorder (APD). Study Design: An observational, prospective, uncontrolled, open-label multi-centric study. Place and Duration of Study: Patients were recruited from 12 cities across India by 61 investigators, between October 2010 and December 2011. Methodology: We included 1500 patients (973 men, 527 women; age range 15-85 years) with Acid Peptic disorder. Lafutidine (10 mg tablets) was prescribed by the physicians as once daily dose (OD) for 28 days. The efficacy was analysed based on the change in the symptom baseline score on the 100 point Visual Analogue Scale (VAS) for individual symptoms, and the safety was determined based on adverse events reported during the study with the prescribed usage of lafutidine on day 14 and day 28 after start of the treatment. Results: Lafutidine monotherapy was given to 1378 patients. A very high reduction in the mean VAS score was observed from baseline for individual symptoms, viz. nausea, vomiting, belching, heart burn, epigastric pain, acid regurgitation, abdominal bloating & loss of appetite at the end of the study. The global mean VAS score (a sum of individual symptom VAS score) of these patients decreased from 120.34 ± 67.58 to 14.18 ± 26.97 at the end of the study (P < .001). There were 124 APD patients, previously treated but uncontrolled, with acid inhibitors like PPIs, H2RAs etc., also showed a significant reduction (157.42 ± 83.88 to 26.47 ± 46.34) in the VAS score on day 28 (P<.001). During the entire study, adverse events of mild and moderate nature were observed in 0.4% (6 patients) of the total patient population. Conclusion: The present study demonstrates that therapy with Lafaxid™ is symptomatically effective and well tolerated in patients with APDs.