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1.
Acta Pharmaceutica Sinica ; (12): 1049-1058, 2023.
Article in Chinese | WPRIM | ID: wpr-978766

ABSTRACT

Sirolimus self-microemulsion-mesoporous silicon sustained release tablets were prepared in order to improve the dissolution of the insoluble drug sirolimus and reduce its side effects. Firstly, sirolimus self-microemulsion was prepared and cured with mesoporous silicon. Secondly, the suitable excipients were selected according to the appearance, hardness and in vitro release rate. The sustained-release tablets with hydroxypropyl methylcellulose (HPMC) as skeleton material were prepared by powder direct pressing method, and the formulation was optimized by central composite design-response surface method to investigate the drug release in vitro. Finally, the pharmacokinetics was carried out in beagle dogs using the commercial sirolimus tablets as references. The final formulation of sustained-release tablets is as follows: 162 mg of sirolimus self-microemulsion-mesoporous silica (1∶1, w/w), 80 mg of HPMC K4M and 80 mg of carboxymethyl starch sodium, the microcrystalline cellulose is 168 mg. The results of in vitro release test showed that the self-made sustained-release tablets released slowly within 12 h, which conformed to the Ritger-Peppas model. The in vivo test results showed that compared with the commercial sirolimus tablets, the Cmax of the sustained-release tablets decreased by 49.47%, the Tmax of the sustained-release tablets was prolonged by 5.1 times, and the relative bioavailability was 105.81%. Sirolimus self-microemulsion-mesoporous silicon sustained-release tablets have good sustained-release effects in vitro and in vivo, which provides a reference for the solubilization of other insoluble drugs and the research and development of sustained-release preparations. Animal experiments and welfare processes were reviewed and approved by the Animal Ethics Committee of the 900TH Hospital of the Joint Logistics support Force.

2.
Chinese Pharmaceutical Journal ; (24): 382-389, 2019.
Article in Chinese | WPRIM | ID: wpr-858055

ABSTRACT

OBJECTIVE: To investigate the effect of the critical quality attributes of hypromellose (HPMC) on the release profile of diclofenac sodium sustained-release tablets in vitro. METHODS: The characteristics including appearance, particle size, density, compression and specific surface area of HPMC K15M from three manufacturers (A, B and C) were studied and evaluated comprehensively. The compression data of HPMC K15M were non-linear fitted via the pressure-tensile strength curve method, Kawabe equation and Hasano equation. Sustained-release tablets were prepared by using diclofenac sodium as the active ingredient with different HPMC as gel matrix, and the in vitro release behavior of the tablets was determined in order to identify the critical quality attribute of HPMC that affect the in vitro release profile of diclofenac sodium sustained-release tablets. RESULTS: The release rate of diclofenac sodium sustained-release tablets was correlated with the substitution type of HPMC, viscosity, density and specific surface area, but less affected by particle size. CONCLUSION: Substitution, viscosity, density and specific surface area of HPMC are the CQAs factors influencing the release profile of diclofenac sodium sustained- release tablets.

3.
Chinese Pharmaceutical Journal ; (24): 468-472, 2017.
Article in Chinese | WPRIM | ID: wpr-858775

ABSTRACT

OBJECTIVE: To investigate the influencing mechanism of the particle size of hydroxypropyl methylcellulose (HPMC) on the release behavior of nifedipine from a sustained-release tablet system based on the compaction properties of HPMC. METHODS: The compaction properties of HPMC K4M of different particle sizes were determined. Hydrophilic matrix sustained-release tablets were prepared using nifedipine as the active ingredient and HPMC K4M as a hydrophilic matrix former. The effect of compaction properties of HPMC K4M on the porosity, release, and other properties of nifedipine hydrophilic matrix sustained-release tablets were also studied. RESULTS: The decrease of the particle size of HPMC K4M resulted in higher bulk density, tap density, compressibility index, and tensile strength and smaller elastic recovery of HPMC K4M, which all led to the decrease of thickness and porosity and the increase of HPMC concentration per unit volume of nifedipine hydrophilic matrix sustained-release tablets. These factors resulted in faster gelation rate of nifedipine sustained-release tablets and decreased water ingress and polymer swelling, so the release of nifedipine from the delivery system was prolonged. CONCLUSION: The obviously different compaction properties of HPMC of different particle sizes influence the porosity and gelation rate and then the release of hydrophilic matrix nifedipine sustained-release tablets.

4.
China Pharmacy ; (12): 3129-3132, 2017.
Article in Chinese | WPRIM | ID: wpr-618157

ABSTRACT

OBJECTIVE:To prepare the Compound anisodamine and neostigmine sustained-release tablet and study the in vitro drug release behavior. METHODS:Using raceanisodamine and neostigmine methyl sulfate as main medicines,hydroxypropyl meth-yl cellulose as sustained release skeleton material,magnesium stearate as the lubricant,polyvinyl pyrrolidone as the adhesive,pre-gelatinized starch as the thinner,microcrystalline cellulose as the disintegrant and filler,Compound anisodamine and neostigmine sustained-release tablet was prepared by wet granulation method and direct compression method. The in vitro cumulative release rate within 12 h of the 2 main medicines was detected by HPLC method. RESULTS:Compound anisodamine and neostigmine sus-tained-release tablet was successfully prepared,and the in vitro release was basically completed within 12 h,with accumulative re-lease rate of 91.3% for anisodamine and 96.5% for neostigmine. CONCLUSIONS:Compound anisodamine and neostigmine sus-tained-release tablet that can cumulatively release for 12 h is successfully prepared.

5.
Chinese Journal of Biochemical Pharmaceutics ; (6): 45-46, 2017.
Article in Chinese | WPRIM | ID: wpr-611320

ABSTRACT

Objective To study the effect of Snsong Yangxin capsule and metoprolol sustained release tablet on the curative effect and the levels of BNP and HR in the elderly coronary heart disease (CHD) arrhythmia patients. Methods It selects 108 patients with coronary heart disease and arrhythmia in elderly patients were divided into observation group (54 cases) and control group (54 cases). The control group was treated with metoprolol sustained-release tablets, and the observation group was treated with Shensong Yangxin capsule and metoprolol sustained-release tablets. The curative effect of two groups and the changes of BNP and HR levels before and after treatment were observed and compared. Results The treatment effect, times of contraction, frequency of cardiac fibrillation, frequency of defect, load, time, blood pressure and BNP of the observation group were significantly better than those of the control group (P<0.05). Conclusion For elderly patients with coronary heart disease arrhythmia, the treatment of Shensong Yangxin capsule combined with metoprolol sustained release tablets is effective. It can significantly improve the patient's heart rate, restore the blood supply to the heart, improve the blood pressure and BNP, with less adverse reactions, safe and reliable, and worthy of promotion.

6.
China Pharmacy ; (12): 3565-3568, 2017.
Article in Chinese | WPRIM | ID: wpr-611004

ABSTRACT

OBJECTIVE:To optimize the formulation of Cilnidipine sustained-release tablet,and study its drug-release mecha-nism. METHODS:Solvent method was adopted to prepare the cilnidipine solid dispersion,then Cilnidipine sustained-release tablet was prepared by using hypromellose K4M(HPMC K4M)as release material. Using comprehensive scores of cumulative release de-gree in 2,6,12 h as indexes,single factor method and Box-Behnken response surface method were used to screen the amounts of HPMC K4M and ethyl cellulose (EC),lactose-microcrystalline cellulose (MCC) ratio in formulation of Cilnidipine sustained-re-lease tablet,and verification test was conducted. The drug-release mechanism of Cilnidipine sustained-release tablet was investigat-ed by model fitting way. RESULTS:The optimal formulation was as follow as 25% of cilnidipine solid dispersion,30% of HPMC K4M,10% of EC,lactose-MCC ratio of 1:1(m/m). The adhesive was 5% PVPP ethanol solution and the lubricant was 0.5%magnesium stearate. The cumulative release degrees of prepared sustained-release tablet in 2,6,12 h were(21.4±3.3)%,(62.9± 2.8)%,(85.4±0.5)%(n=3),relative error of which to predicted value 25%,60%,90%were 14.4%,4.8%and 5.1%. Release curve showed the highest fitting degree with the first-order release model,conforming to non-Fick diffusion. CONCLUSIONS:Cil-nidipine sustained-release tablet with sustained-release effect is successfully prepared by optimized formulation.

7.
China Pharmacy ; (12): 4872-4875, 2017.
Article in Chinese | WPRIM | ID: wpr-663586

ABSTRACT

OBJECTIVE:To improve the original preparation technology,imitate Lamotrigine sustained-release tablets,and study its in vitro release behavior. METHODS:Hydroxypropylmethylcellulose (HPMC) E4M CR and HPMC K100LV CR were used to prepare the sustained-release matrix core. Using Eudragit? L30D-55 as enteric coating material,Lamotrigine sustained-re-lease tablets were prepared. Using the similar factor f2 of in vitro release rate of original preparation as index,single factor was used to screen the amount of lactose,mass ratio of HPMC E4M CR and HPMC K100LV CR,amount of HPMC and weight of coating layer in the formulation. RESULTS:The formulation of matrix core was as follow as lamotrigine 50 mg,HPMC K100LV CR 40 mg,HPMC E4M CR 61.4 mg,lactose 128 mg,and the optimal weight of coating layer of 3%. The in vitro release of self-made and original preparations were similar in pH 6.8 phosphate buffer containing 0.5% sodium dodecyl sulfate,pH 4.5 acetic acid sodi-um acetate buffer and water. CONCLUSIONS:Lamotrigine sustained-release tablets are successfully imitated,and the technology is more simple and feasible than original preparation.

8.
China Pharmacy ; (12): 3969-3972, 2017.
Article in Chinese | WPRIM | ID: wpr-662031

ABSTRACT

OBJECTIVE:To screen the formulation of 5-fluorouracil (5-FU) polylactic acid (PLA) sustained-release discs (5-FU-PLA-DS),and study its in vitro drug-release mechanism. METHODS:UV spectrophotometry was used to determine the 5-FU content in the release medium. Using simulate body fluid as release medium,in vitro drug-release test was conducted under 37℃water bath. Using PLA with molecular weight of 3000,6000,10000,15000,20000,15 species of round 5-FU-PLA-DS with drug containing of 1.5,2.5,3.0 mg/piece and 3.0 mm in diameter and 1.0 mm in thickness were prepared. Using effective con-centration sustained release time and cumulative release rate as indexes, the optimal formulation was screened. The form of 5-FU-PLA-DS was observed by scanning electron microscopy after release,and its release mechanism was evaluated. RESULTS:In the optimal formulation, the PLA molecular weight was 20000 and drug containing was 3.0 mg/piece. The prepared 5-FU-PLA-DS can release for 119 d,with cumulative release degree of 100.63% and effective concentration sustained for 91 d. Scanning electron microscopy showed that the microspheres at the surface were degraded to the release medium first,and then the microspheres of inner layer exposed and release drug gradually after PLA degraded. The main mechanism of drug-release was melt-ing and diffusion. CONCLUSIONS:5-FU-PLA-DS is successfully prepared,with long release time in effective concentration,can be degraded step by step from outside to inside and achieve non-synchronous drug-release of microspheres at different layers.

9.
China Pharmacy ; (12): 3969-3972, 2017.
Article in Chinese | WPRIM | ID: wpr-659254

ABSTRACT

OBJECTIVE:To screen the formulation of 5-fluorouracil (5-FU) polylactic acid (PLA) sustained-release discs (5-FU-PLA-DS),and study its in vitro drug-release mechanism. METHODS:UV spectrophotometry was used to determine the 5-FU content in the release medium. Using simulate body fluid as release medium,in vitro drug-release test was conducted under 37℃water bath. Using PLA with molecular weight of 3000,6000,10000,15000,20000,15 species of round 5-FU-PLA-DS with drug containing of 1.5,2.5,3.0 mg/piece and 3.0 mm in diameter and 1.0 mm in thickness were prepared. Using effective con-centration sustained release time and cumulative release rate as indexes, the optimal formulation was screened. The form of 5-FU-PLA-DS was observed by scanning electron microscopy after release,and its release mechanism was evaluated. RESULTS:In the optimal formulation, the PLA molecular weight was 20000 and drug containing was 3.0 mg/piece. The prepared 5-FU-PLA-DS can release for 119 d,with cumulative release degree of 100.63% and effective concentration sustained for 91 d. Scanning electron microscopy showed that the microspheres at the surface were degraded to the release medium first,and then the microspheres of inner layer exposed and release drug gradually after PLA degraded. The main mechanism of drug-release was melt-ing and diffusion. CONCLUSIONS:5-FU-PLA-DS is successfully prepared,with long release time in effective concentration,can be degraded step by step from outside to inside and achieve non-synchronous drug-release of microspheres at different layers.

10.
China Pharmacy ; (12): 1395-1398, 2017.
Article in Chinese | WPRIM | ID: wpr-515335

ABSTRACT

OBJECTIVE:To optimize the formulation of Budesonide sustained-release tablet. METHODS:Using the cumula-tive releases in 2,4,8 h as investigation indexes,central composite design-response surface method was used to optimize the amount of hydroxypropylcellulose L(HPC-L),amount of soybean phosphatides,and filler(fixed total 200 mg)lactose- micro-crystalline cellulose mass ratio in the formulation of Budesonide sustained-release tablet,and the verification test was conducted. The release behaviors of prepared sustained-release tablet and original preparation in pH 7.2,7.0,6.8 phosphate buffer were com-pared. RESULTS:The optimal formulation was as follow as budesonide of 9 mg,HPC-L of 46.49 mg,soybean phosphatides of 9.23 mg,filler lactose-microcrystalline cellulose mass ratio of 1:2.9;the cumulative releases in 2,4,8 h were 21.9%,50.1%, 99.5%,the relative errors with predicted values (22.0%,50.0%,98.5%) were 0.45%,0.20%,1.02%(n=3),respectively. Compared with cumulative release of original preparation,the f2 was higher than 50. CONCLUSIONS:Budesonide sustained-re-lease tablet is successfully prepared,which shows similar release behavior to original preparations.

11.
Drug Evaluation Research ; (6): 174-178, 2017.
Article in Chinese | WPRIM | ID: wpr-515052

ABSTRACT

Objective To establish a method for determining the dissolution oftorasemide sustained-release tablet in vitro and study the methodology of the determination.The consistency of the in vitro release behavior between self-prepared torasemide sustained-release tablet and original preparation were evaluated by constructed method.Methods HPLC method was applied to detect the cumulative release percentage of self-prepared torasemide sustained-release tablet and original preparation in five kinds of release media (water,0.1 mol/L hydrochloric acid solution,pH 4.5 acetate buffer,pH 6.8 phosphate buffer,and 0.1 mol/L hydrochloric acid solution turn to pH 6.8 phosphate buffer).Similarity factor (f2) was used to evaluate the similarity of release curves.Results There was a good linear relationship between the quality concentration of torasemide and peak area in the range of 1.0-12.0 μg/mL (r =0.9995).Results of precision and stability tests were good,and the RSDs for probational liquid were all lower than 2.0%.The average recovery of accuracy test was 100.04%,and RSD was 0.54% (n =12).The homogeneity of within group of self-prepared preparation met the technical requirement,RSDs of each sampling points in six Dissolution Vessels were lower than 10.0%.The f2 factors of self-prepared torasemide sustained-release tablet and original preparation were 72,60,77,66,and 60 in five kinds of release media.Conclusion The method in the paper is suitable for the release test of torasemide,meanwhile,the self-prepared tablet shows consistent in vitro release behavior with that of the original preparation.

12.
China Pharmacy ; (12): 1080-1084, 2017.
Article in Chinese | WPRIM | ID: wpr-514927

ABSTRACT

OBJECTIVE:To compare Paliperidone sustained-release tablet and Paliperidone palmitate injection in the treatment of schizophrenia in respects of medium-term and long-term efficacy,safety,insight,medication compliance and social function of patients,so ad to provide reference for drug selection in the clinic.METHODS:Eighty-four schizophrenia patients selected from our center during Mar.2015-Jun.2016 were divided into Paliperidone sustained-release tablet group (group H,44 cases) and Paliperidone palmitate injection group (group Z,40 cases).Group H was given Paliperidone sustained-release tablet orally with initial dose of 3 mg/d,gradually increasing to 9 mg/d 2 weeks later according to disease condition;the drug dose was adjusted and ranged 3-12 mg/d according to disease condition.Group Z was given Paliperidone palmitate injection intramuscularly,150 mg on 1st day,100 mg on 8th day,and then given injection once a month,drug dose was adjusted according to disease condition (75,100,150 mg).Treatment course of 2 groups lasted for 12 months.Before treatment,1,2,3,6,9,12 months after treatment,Positive and Negative Syndrome Scale (PANSS) was used to evaluate therapeutic efficacy;Scale to Assess Unawareness of Mental Disorder (SAUMD) was used to evaluate the cognition of patients to disease;Medication Adherence Rating Scale (MARS) was used to evaluate medication compliance;Personal and Social Performance Scale (PSP) was used to evaluate patient's social function.The occurrence of ADR was observed during treatment.RESULTS:3,2 patients withdrew from group H,Z during treatment.Before treatment,there was no statistical significance in PANSS,SAUMD,MARS,PSP scores between 2 groups (P>0.05).1,2,3,6,9,12 months after treatment,PANSS and SAUMD scores of 2 groups were decreased significantly,while MARS and PSP scores were increased significantly,compared to before treatment,with statistical significance (P<0.05).9,12 months after treatment,PANSS and SAUMD scores of group Z were decreased significantly,while MARS and PSP scores were increased significantly,compared to group H,with statistical significance (P<0.05).There was no statistical significance in the occurrence of ADR between 2 groups (P>0.05).CONCLUSIONS:For schizophrenia,Paliperidone palmitate injection is better than Paliperi done sustained-release tablet in respects of medium-term and long-term efficacy,patient's insight,medication compliance,social function recovery;the longer the time,the more prominent the superiority.There is no significant difference in safety between them.

13.
China Pharmacy ; (12): 110-114, 2017.
Article in Chinese | WPRIM | ID: wpr-507736

ABSTRACT

OBJECTIVE:To optimize the formulation of Mirabegron sustained-release tablets. METHODS:Using polyethylene oxide(PEO)and hydroxypropylmethyl cellulose(HPMC K4M)as the sustained release matrix,Mirabegron sustained-release tab-lets were prepared by powder direct compression technology. Using 1,3,5,7 h accumulative release rate as indexes,the amounts of PEO,HPMC K4M and OPADRY? were optimized by composite design-response surface method,and then validated. Accumula-tive release rates of sustained-release tablet and original tablet (MyrbetriqTM) were compared in different pH mediums (water,pH 1.0 simulated gastric fluid,pH 4.5 acetate buffer solution,pH 6.8 phosphate buffer solution) at different rotation rates (100,50 r/min),and similiar factor f2 was calculated to fit drug release model of sustained-release tablet. RESULTS:In the optimized firmu-lation each Mirabegron sustained-release tablet contained mirabegron 25 mg,PEO 108.02 mg,HPMC K4M 21.69 mg,OPADRY? 2.27%. Relative error of accumulative release rates at 1,3,5,7 h to predicted value were 4.78%,3.48%,0.69% and -1.41%, respectively. f2 of release curves of sustained-release tablet and original tablet were higher than 65 in different pH medium at differ-ent rotation rates. The drug release of sustained-release tablet was fitted to zero-order release equation. CONCLUSIONS:Mirabe-gron sustained-release tablet by optimized technology is similar to original tablet in drug release behavior.

14.
Journal of International Pharmaceutical Research ; (6): 1145-1150, 2016.
Article in Chinese | WPRIM | ID: wpr-845455

ABSTRACT

Objective To optimize the recipe of rhynchophylline sustained release tablet in order to provide a reference for industrial production of the formulation. Method With the release degree as index, the influences of single factors on the release, such as hydroxypropyl methyl cellulose(HPMC)used as an skeleton materials, ethyl cellulose(EC)as blockers and the mass fraction of polyvinylpyrrolidone (PVP)as adhesive, were evaluated to screen the optimal preparation by central composite design and response surface methodology based on the single factor investigation. Result The optimal preparation was as follows: rhynchophylline 9.5%, HPMC: 19%, EC: 7%, PVPP:2.2%, starch:61.5% and talcum powder: 0.8%. The sustained release tablet prepared by the optimized recipe of rhynchophylline had no sudden release effect and the release degree in 12 h was more than 84%. Conclusion The optimized recipe is reasonable and meets the requirements of sustained release formulation, which means it can provide a reference for industrial production of the formulation.

15.
Chinese Pharmaceutical Journal ; (24): 1483-1487, 2016.
Article in Chinese | WPRIM | ID: wpr-858989

ABSTRACT

OBJECTIVE: To establish a simple, sensitive method of liquid chromatographic-tandem mass spectrometric (LC-MS/MS) for determination of mirabegron in dog plasma, and to evaluate the pharmacokinetics for single dose of different formulations of mirabegron sustained-release tablets in dogs. METHODS: The analyte mirabegron and internal standards (IS) tolbutamide were separated on a BEH C18 column (2.1 mm×50 mm, 1.7 μm) with mobile phase of 0.1% formic acid water solution-0.1% formic acid methyl cyanides solution using a gradient elution mode at a flow rate of 450 μL·min-1. In accordance with randomized two-period self crossover study, eight dogs were given single oral dose of the test preparation and reference preparation, then the concentration of mirabegron in plasma was determined, the pharmacokinetic parameters were calculated and the difference of the two preparations were evaluated. RESULTS: The linear range of mirabegron in Beagle dogs plasma was 1-1000 ng·mL-1. The accuracy and the precisions of intra-day and inter-day also were qualified. After a single dose administration of the test preparation and reference preparation, the pharmacokinetic parameters were as follow: t1/2 were (7.14±1.59) vs (7.13±1.78) h, pmax were (144.4±77.5) vs (130.3±39.2) ng·mL-1, tmax were (3.72±1.87) vs (4.64±1.55)h, AUC0→8 were (1021±439) vs (989±299)ng·h·mL-1, AUC0→∞ were (1043±441) vs (1010±301)ng·h·mL-1. CONCLUSION: The LC-MS/MS method is suitable for pharmacokinetic study of mirabegron. Moreover, there is no significant difference in the pharmacokinetic profiles between the two preparations of mirabegron.

16.
Journal of International Pharmaceutical Research ; (6): 1145-1150, 2016.
Article in Chinese | WPRIM | ID: wpr-509097

ABSTRACT

Objective To optimize the recipe of rhynchophylline sustained release tablet in order to provide a reference for in?dustrial production of the formulation. Method With the release degree as index,the influences of single factors on the release,such as hydroxypropyl methyl cellulose(HPMC)used as an skeleton materials,ethyl cellulose(EC)as blockers and the mass fraction of polyvinylpyrrolidone(PVP)as adhesive,were evaluated to screen the optimal preparation by central composite design and response surface methodology based on the single factor investigation. Result The optimal preparation was as follows:rhynchophylline 9.5%, HPMC:19%,EC:7%,PVPP:2.2%,starch:61.5%and talcum powder:0.8%. The sustained release tablet prepared by the optimized recipe of rhynchophylline had no sudden release effect and the release degree in 12 h was more than 84%. Conclusion The opti?mized recipe is reasonable and meets the requirements of sustained release formulation,which means it can provide a reference for in?dustrial production of the formulation.

17.
Chinese Traditional and Herbal Drugs ; (24): 3514-3519, 2015.
Article in Chinese | WPRIM | ID: wpr-853839

ABSTRACT

Objective: To optimize the formulation of Haimeng Zhisuan gastric floating sustained-release tablets and to investigate its in vitro release properties. Methods: Plackett-Burman design was used to screen three most influential factors, i.e. matrices, floating material, and fillers which had significant impact on the preparation of floating sustained-release tablet by evaluating the cumulative release rate of CaCO3 at 2, 4, and 12 h; The levels of non-important factors were also determined. A 3-factor, 3-level Box-Behnken design was led to optimize the formulation, using cumulative release rate as index. The experiment result was optimized and the drug release kinetics equation was fitted by response optimizer. Results: The optimized tablet formulation was as follows: cuttlebone 225.0 mg, Montmorillonite 25.0 mg, HPMC K100M 100.0 mg, MCC 48.3 mg, EC 25.0 mg, searyl alcohol 74.7 mg, and 5% PVP-K30 ethanol solution as adhesive. The experimental data of optimized tablet were similar to the predicted values. The floating duration was over 12 h in simulated gastric fluid. Data of the in vitro release were fitted to the first-order equation. Conclusion: Formulation of Haimeng Zhisuan floating sustained-release tablet is found to be reasonable. The preparation technology is feasible. The tablet shows good in vitro release properties within 12 h.

18.
China Pharmacy ; (12): 4351-4353, 2015.
Article in Chinese | WPRIM | ID: wpr-501115

ABSTRACT

OBJECTIVE:To study the effects of Clebopride(CBP)bioadhensive sustained-release tablets on experimental gas-tric ulcer and gastrointestinal motility disorder. METHODS:Gastric ulcer rat model was induced by ethanol and aspirin,and then divided into model group (normal saline),common tablet (CBP tablet 0.072 mg/kg) and sustained-release tablet high-dose and low-dose groups (CBP bioadhensive sustained-release tablet 0.072,0.036 mg/kg);normal rats were included in normal control group (normal saline);they were given relevant medicine intragastrically,twice a day for sustained-release tablet,three times a day for other. Ulcer area were observed 2 and 4 days after medication to calculate healing rate of ulcer(n=6). Gastrointestinal mo-tility disorder mice model was induced by atropine,and then divided into model group (normal saline),common tablet group (CBP tablet 0.1 mg/kg)and sustained-release tablet high-dose,medium-dose and low-dose groups(CBP bioadhensive sustained-re-lease tablet 0.1,0.05,0.025 mg/kg);normal mice were included in normal control group(normal saline);they were given rele-vant medicine intragastrically,once a day,for consecutive 3 days. The rate of gastric emptying and small intestinal propulsion were detected (n=6). RESULTS:Compared with normal control group,ulcer area of rats increased in model group;compared with model group,that of rats decreased in common tablet group and sustained-release tablet high-dose,low-dose groups,with statisti-cal significance (P<0.01);healing rates of gastric ulcer were 32.35%-48.24% 2 days after medication,and those were above 70% 4 days after medication. Compared with normal control group,the rate of gastric emptying and small intestinal propulsion in mice decreased in model group;compared with model group,those of mice increased in common tablet group and sustained-re-lease tablet high-dose,medium-dose,low-dose groups. The effects of sustained-release tablet high-dose and medium-dose groups were better than that of common tablet group;those difference had statistical significance (P<0.01 or P<0.05). CONCLU-SIONS:CBP bioadhensive sustained-release tablets have im-provement effects against gastric ulcer of rats and gastrointesti-nal motility disorder of mice.

19.
Chinese Journal of Infection Control ; (4): 38-41, 2015.
Article in Chinese | WPRIM | ID: wpr-462105

ABSTRACT

Objective To explore the efficacy and adverse reactions of diminishing scheme of cefaclor sustained re-lease tablets in the treatment of recurrent urinary tract infection(RUTI).Methods 60 RUTI patients in a hospital were divided into treatment group(n=30)and control group (n=30),patients in treatment group were treated with diminishing scheme of cefaclor sustained release tablets,patients in control group were treated with diminishing scheme of levofloxacin tablets,clinical therapeutic efficacy and adverse reactions of two groups were observed. Results The curative rate in treatment group was higher than control group ([80.00%,n =24]vs [53.33%,n =16])(χ2 =4.80,P =0.028).The incidence of RUTI in treatment group was lower than control group ([6.67%,n=2]vs [26.67%,n=8])(χ2 =4.32,P =0.038).Incidence of adverse reactions in treatment group was lower than control group (16.67% vs 50.00%)(χ2 =7.50,P =0.006).Conclusion The diminishing scheme of cefaclor sus-tained release tablets in the treatment of RUTI has good curative efficacy,low recurrence rate,fewer adverse reac-tions,and can be used for the treatment of recurrence of RUTI.

20.
Chinese Journal of Clinical Oncology ; (24): 600-602, 2015.
Article in Chinese | WPRIM | ID: wpr-467268

ABSTRACT

Oxycodone sustained-release tablet is a new formulation of potent opioids, which are characterized by their exact anal-gesic effect, high safety for oral administration, and slight adverse drug reaction. Oxycodone improves the quality of life of patients with cancer pains and is among the selected drugs used for controlling moderate and severe cancer pains. Relief from prolonged pain is achieved by adjusting the dose of Oxycontin (oxycodone hydrochloride) sustained-release tablet according to its pharmacological char-acteristics. The details are reviewed in this article.

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