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Objective: To prepare diphenidol hydrochloride push-pull osmotic pump tablets and in-vestigate the influence of differ-ent factors on in-vitro drug release. Methods: The cumulative release of different formulas was detected. Using the cumulative release and similarity factor f2as the evaluation criterion, single factor experiment was applied to screen the core formula and coating process. Results: The drug release behavior was affected by the content of PEO in the drug containing layer, the content of NaCl and the weight gain of the coating layer. After the formula was optimized, the NaCl content in the drug containing layer was 10mg, the PEO-N10 con-tent was 15mg. In the push layer, the content of PEO-WSR303 was 60 mg, that of NaCl was 20 mg. The optimized coating liquid for-mula contained 1. 25 g·L-1PEG4000 and the coating weight gain was 7% of the core. The optimized formula fitted a zero-order equa-tion within 2-12h with the drug release equation of Q=6. 308t-2. 5037(r=0. 995 8). Conclusion: The preparation technology of di-phenidol hydrochloride push-pull osmotic pump tablets is stable, and the in-vitro drug release fits zero-order model.
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Objective:To optimize the formula of aprepitant nanocapsules. Methods: The central composite design–response surface methodology was used. The amounts of hydroxg propyl cellulose(HPC-SL) and sodium dodecyl sulfate(SDS) were set as the independent variables;the dissolution of aprepitant capsules at 15min and 30min, and the dissolution after accelerated at 40℃ and 75% RH for 6 months were set as the dependent variables. Quadratic polynomial mathematic models were used to evaluate the relation-ship between the independent and the dependent variables. According to the mathematic models,an effect graph was drawn. The opti-mized formula was chosen from the overlap of the contour graphs of the dependent variables. The similarity of in vitro dissolution curve was evaluated by using f2factor. Results:The correlation coefficient of quadratic polynomial mathematic model and the reliability was high. The measured values of the optimized formula were within the expected ranges. Conclusion: Aprepitant nanocapsules with the optimized formula by central composite design-response surface methodology meet the requirements. The results can provide evidence for the next industrial production.
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OBJECTIVE: To explore the similarity of the dissolution curves of self-made and original telmisartan /hydrochlorothiazide tablets and provide basis for the prescription and process screening of self-made preparation and the quality similarity evaluation with original preparation. METHODS: The dissolution curves of telmisartan and hydrochlorothiazide from self-made and original preparations in four different dissolution media were determined using HPLC. The HPLC method was performed on Welch Ultimate XB-C8 column (4.6 mm × 250 mm, 5 μm) with mobile phase A consisting of ammonium dihydrogen phosphate solution (2.0 g ammonium dihydrogen phosphate was dissolved in 1 L water then adjusted to pH 3.0 with phosphoric acid) and mobile phase B consisting of acetonitrile- methanol (50:50) at a flow rate of 1.2 mL•min-1. The detection wavelength was set at 270 nm. The injection volume was 20 μL. Then f2 factor method was used to evaluate the similarity. RESULTS: The dissolution curves of self-made and original preparations of telmisartan /hydrochlorothiazide tablets in different dissolution media showed similarity, with the f2 factor ≥50 or the dissolution rate within 15 min≥85%. CONCLUSION: The dissolution behaviors of self-made and original telmisartan /hydrochlorothiazide tablets are basically similar, which indicates that the prescription and technology of self-made preparation are reasonable and feasible.
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Objective To compare the dissolution curves of reference preparation and self-prepared Iloperidone Tablets in four different pH dissolution media (0.1 mol/L HC1 solution,pH 4.5 acetate buffer solution,pH 6.8 phosphate buffer solution,and water).Methods The solubility of Iloperidone in different pH solutions was measured,the dissolution curves of two preparations in four different pH dissolution media were determined by HPLC,and the similarity was investigated according to the f2 factor method.Results The f2 factors between reference preparation and self-prepared Iloperidone Tablets in four different media were more than 50.Conclusion The two preparations are equivalent in four different pH dissolution media in vitro.
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Objective To establish a method for determining the dissolution of isoniazid tablet in vitro and evaluate the dissolution profiles.Methods The paddle method was used for the dissolution test and the rotation rate was set at 50 r/min.The hydrochloric acid solution (pH 1.2),acetate buffer solution (pH 4.5),phosphate buffer solution (pH 6.8) and water (900 mL) were used as the dissolution media.HPLC was used for the determination of dissolution quantity.Results There was a good linear relationship between the quality concentration of i soniazid and peak area in the range of 0.1981-0.9904μg (r =0.9993).The average recovery was 100.2％.Precision,reproducibility,and specificity tests were good.Among the determination of 16 manufactures,the dissolution profiles in water of four manufactures were not similar with Sandoz reference preparation.Conclusion The HPLC method is simple.The accuracy and specificity of determination of isoniazid dissolution are improved.There is significant difference in the dissolution profiles between different manufactures.The method can be used for the determination of dissolution curves for isoniazid tablets.
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Objective To compare the dissolution behavior between domestic trepibutone tablets and original reference product, and provide a basis for evaluating the quality consistency of generic drugs. Methods Four dissolution media recommended by Japanese Orange Book and a domestic standard dissolution media were selected to determined the dissolution profile,and f2 factor was calculated to investigate the consistency of stripping curves. Results In water,pH 4.0 and pH 1.2,the f2 of domestic formulation and reference formulation was under 50,and the dissolution profile was inconsistent.Dissolution behavior of domestic preparations of different manufacturers was dissimilar.In water,the f2 of domestic preparations of different batches of the same manufacturer was over 99.9,and the dissolution behavior was similar. Conclusion The dissolution method of existing domestic standard can not distinguish the dissolution behavior of different products,and it should be revised and completed.There is still great difference in quality between the domestic preparations and reference preparations.
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Objective:To study the difference in dissolution behavior of clozapine tablets in four different media between the do-mestic preparations and original preparation to compare the internal quality of the tablets from various manufacturers and provide refer-ence for the drug control. Methods:Referring to the methods of in vitro dissolution test, the dissolution profiles of 46 batches of sam-ples from 18 pharmaceutical enterprises were determined in four kinds of dissolution media with different pH values, and the results were compared with that of the original drug by the method of f2 similarity factor. Results: Totally 46 dissolution profiles were drawn out. The profiles of two batches of samples from one pharmaceutical enterprise were similar to that of the original drug, which account-ing for 4%, and that of the other samples showed notable difference from that of the original drug. Conclusion:The preparation tech-nology of the tablets from domestic has great difference, which leads to significant difference in dissolution behavior. The screening and optimization of the production process in domestic pharmaceutical enterprises should be strengthened to improve the preparation technol-ogy of clozapine tablets.
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OBJECTIVE:To establish a method for the dissolubility determination of Manidipine Hydrochloride tablet and eval-uate the quality consistency of generic and original preparation. METHODS:HPLC was performed on the column of Waters Sym-metry C18 column with mobile phase of potassium phosphate monobasic solution (potassium phosphate monobasic 6.8 g was well-mixed with water 1 000 ml,and pH was adjusted to 4.6 by potassium hydroxide solution)-acetonitrile (49∶51,V/V) at flow rate of 1.0 ml/min,detection wavelength was 228 nm,column temperature was 25℃,and the injection volume was 20μl. The dis-solution mediums were 0.1 mol/L hydrochloric acid solution,acetic acid-sodium acetate buffer solution(pH 4.0)and phosphate buf-fer solution [pH 6.8,adding into 0.5% sodium dodecyl sulfonate(SDS)],volume of dissolution medium was 900 ml and rotating rate was 50 r/min,and the dissolubility of Manidipine hydrochloride tablet generic and original preparation was investigated and the similarity of dissolution profile was evaluated by calculating similar factor (f2). RESULTS:The linear range of manidipine hydro-chloride was 0.625-20 μg/ml;RSDs of instrument precision and stability tests were lower than 2.0%;recoveries of 3 dissolution mediums were 92.86%-102.97%(RSD=1.9%,1.8% and 2.7%,n=9),respectively. The dissolubility of 3 batches of Manidipine hydrochloride tablet generic and original preparations was higher than 85% in 0.1 mol/L hydrochloric acid solution in 15 min;f2 was >50 in acetic acid-sodium acetate buffer solution (pH 4.0) and phosphate buffer solution (pH 6.8,adding into 0.5% SDS). CONCLUSIONS:The method is suitable for the dissolubility determination of Manidipine hydrochloride tablet;meanwhile,the dis-solution profile in vitro of Manidipine hydrochloride tablet generic and original preparations has similarities,so the quality consis-tency is good.
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Objective: To evaluate the quality consistency of the original product ( DIOVAN ) and generic valsartan capsules ( VSC) . Methods:The dissolution of the two capsules in four media was monitored by the UV method described in Chinese Pharmaco-poeia ( ChP 2010 edition) . The f2 similarity factor approach was used to evaluate the dissolution similarity between DIOVAN and VSC and the production quality of the enterprises. Meanwhile, the homogeneity in the same batch was studied by dissolution precision and the reproducibility in the different batches were also evaluated by a similar equivalent limit method to show the production quality of the manufacturers. Results:The dissolution of VSC and Diovan in pH 6. 8 phosphate buffer medium was both above 85% in 15 min. The f2 similarity factors in the other three media ( water, pH 4. 5 acetate buffer and 0. 1 mol·L-1 HCl) were all above 50. The relative standard deviation ( RSD) of precision in the same batch was less than 10%. Among the different batches, dissolution limit value ( Q) was within the range of the upper and lower limit value of probability levels (δ) . Conclusion:The f2 similarity factor results indicate the in vitro dissolution of the reference drug ( DIOVAN) and generic drug ( VSC) is consistent in the four media. The production quali-ty of generic manufacturer is also good with promising homogeneity and reproducibility evaluation results.
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Objective To evaluate the similarity of dissolution profiles of self-produced and original drug cefuroxime axetil tab-lets.Methods Based on the dissolution detection method in the Chinese Pharmacopoeia,the dissolution behaviors of the self-pro-duced preparation and original drug were investigated in pure water,0.1 mol/L hydrochloric acid,0.05 mol/L hydrochloric acid, pH4.5 and pH6.8 medium and the rotation speed of 50,25,75 r/mim.The stripping curves were evaluated by the f2 factor method. Results In the rotation speed of 50 r/min,the f2 factors in different mediums were 57.65,79.17,73.56,66.83 and 62.33 respec-tively;the medium was 0.1 mol/L hydrochloric acid with the rotation speed of 25,75 r/min,the f2 factors were 65.35 and 78.48 re-spectively.Conclusion The stripping curves of self-produced preparation and original drug are similar under various conditions.