ABSTRACT
Objective To compare the efficacy and safety of compound pioglitazone hydrochloririe glimepiride tablet and glimepiride tablet in the treatment of type 2 diabetic mellitus(T2DM) for evaluating the effectiveness and safety of compound pioglitazone hydrochloride glimepiride tablet for treating T2DM.Methods The random,double-blind,double-dummy,positive drugs parallel control clinical study method was adopted.Thirty-three T2DM patients with poorly controlled blood glucose were randomly assigned to the test group(n=22) and control group(n=11) by the 2 ∶ 1 ratio.The test group was given compound pioglitazone hydrochloride glimepiride tablet,while the control group received glimepiride tablet.The treatment cycle was 12 weeks.The differences of FBG,HbA1c,FINS and HOMA-IR in the two groups were compared between before and after treatment.Moreover the changes of body mass,blood pressure and blood lipids as well as adverse events occurrence were compared between the two groups.Results Thirty-one cases finished the treatment follow up(21 cases in the test group and 10 cases in the control group);the decreased amplitudes of HbA1c levels after 12-week treatment in the test group and control group were (0.99 ± 1.87)％ and (-0.02 ± 0.90) ％ respectively,which of FPG were (0.94 ± 1.87) mmol/L and (0.37 ± 2.62) mmol/L respectively.The FPG and HbA1c levels after treatment in the test group were decreased compared with before treatment,the difference was statistically significant (P＜0.01).The change difference of FPG and HbA1c in the control group had no statistical difference(P＞0.05).FINS and HOMO-IR in the test group were significantly decreased before and after treatment,the difference was statistically significant (P＜0.01).The incidence rate of hypoglycemia had no statistically significant difference between the test group and control group.Conclusion The effectiveness of compound pioglitazone hydrochloride glimepiride tablet in treating T2 DM is superior to the single use of glimepiride,while the safety is equivalent to single use of glimepiride.
ABSTRACT
To identify the related substances in pioglitazone hydrochloride by hyphenated LC-MS techniques,an Ultimate XB-C18 (250 mm × 4.6 mm,5 μm) column was used for separation of the related substances with methanol and 0.1％ ammonium acetate buffer as the mobile phases in gradient elution.Electrospray positive ionization high resolution TOF/MS was used for the determination of the accurate mass and elemental composition of parent [M + H] + ions of the related substances,and triple quadrupole tandem mass spectrometry was employed for the product mass spectra determination.Eleven major related substances were detected and identified to be one synthesis intermediate,six by-products and four degradation products,by using LC-MS determination,spectra elucidation,and further synthetic process and stress degradation mechanisms analysis.The results are useful for pioglitazone hydrochloride manufacturing processes optimization and quality control.
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The objective of the present study was to develop and evaluate pioglitazone hydrochloride loaded lipospheres for treatment of diabetes. Pioglitazone hydrochloride lipospheres were formulated by using melt dispersion (homogenization) technique using compritol®888 ATO as lipid matrix and Phospholipon 90G (P 90G), PVA, Poloxamer 188 as surfactants. Formulation was optimized by using 32 full factorial design where entrapment efficiency and particle size were dependent variables and lipid and surfactant concentration were independent variables. Optimized formulation of pioglitazone hydrochloride (PLS 5) shows 79.69± 1.35% entrapment efficiency, 94.63± 2.10% drug content and particle size was found to be 23.74± 0.35μm with spherical shaped free flowing particles. In vitro release was carried out using dissolution apparatus in 0.1N HCl and optimized formulation shows 96.06 ± 0.54 % drug release within 8 hrs. which follows quasi-fickian type of transport and was characterized by the Korsmeyer- Peppas model. Formulation was stable at 5 oC ± 3 oC for two months. Developed liposphere formulation was able to sustain the drug release and entrap the pioglitazone hydrochloride drug at high level.
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Objective:To prepare pioglitazone hydrochloride ( PGH) sustained-release pellet capsules and study the in vitro disso-lution. Methods:The preparation was prepared with a bottom spray fluidized bed, and the formula and technology were optimized by orthogonal test. Results:The method was simple and easy to operate, the reproducibility of the formula and technology was good, and the pellets had obvious sustained-release property. Conclusion:The formula and technology are easy and controllable, and the stability of sustained release pellets is good.
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A simple, specific, accurate and isocratic reversed phase liquid chromatographic method was developed and subsequently validated for the determination of metformin hydrochloride, rosiglitazone and pioglitazone hydrochloride. Separation was achieved with a Zorbax C8 column of 150×4.6 mm i.d. with 5 μm particle size and ammonium dihydrogen phosphate buffer adjusted to pH 3.0 using diluted ortho phosphoric acid and acetonitrile (65:35 v/v) as eluent at a constant flow rate of 0.7 ml per min. UV detection was performed at 215 nm. The retention time of metformin hydrochloride, rosiglitazone and pioglitazone hydrochloride were about 1.9, 3.4 and 6.7 min, respectively. This method is simple, rapid and selective and can be used for routine analysis of antidiabetic drugs in pharmaceutical preparation. It is a convenient method for separation and simultaneous determination of metformin hydrochloride, rosiglitazone and pioglitazone hydrochloride in pharmaceutical formulations.
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OBJECTIVE:To establish the method of determining the blood concentration of pioglitazone hydrochloride. METHODS:Chromatographic column was based on Hypersil C l8 (150mm?4.6mm,5?m),the mobile phase consisted of ace-tonitrile-buffer phosphate(40∶60,V/V)with a flow rate at l.0ml/min,the detecting wavelength was229nm.The blood sample was extracted with dichlormethane.RESULTS:The linear concentration range was25～4000ng/ml(r=0.9998,n=8).The lowest detecting concentration was25ng/ml.The extracting recovery rate of high,medium and low concentrations were(73.33?1.22)%,(76.92?6.57)%and(84.50?3.40)%respectively,the method recovery which were(103.26?3.31)%,(97.31?9.07)%and(99.61?6.48)%respectively.The intra-day RSD