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Abstract The current research focused on screening and finding the significant independent variables in stavudine loaded tablet, followed by optimizing the best formulation using central composite design. The objective of the study to develop stavudine loaded controlled release tablet utilizing reduced factorial design, followed by optimization technique as well as characterization of prepared tablets. Preliminary trial batches were prepared using different grades of hydroxypropyl methylcellulose. The resolution-IV reduced factorial design was selected to screen the significant independent variables in the dosage form design. A total number of eight runs were prepared and responses were recorded. The signified factors identified by half-normal and Pareto chart. The prepared tablets are evaluated for various physiochemical characterizations. Three dependent responses such as hardness, dissolution at 6 hour and 12 hours are considered in optimization process. Later on, drug-polymer interaction study was carried out. The principal of the study design based on finding the best formulation with prefixed set parameter values utilizing the concept of screening technique. It observed that HPMC K15M (57.18 %), HPMC K100 (66.32 %) and PVP K30 (7.97 %) as best composition in a formulation batch would fulfill the predetermined parameter with specific values.
Subject(s)
Stavudine/administration & dosage , Process Optimization , Hypromellose Derivatives/classification , Drug Liberation , Tablets/administration & dosage , Pharmaceutical Preparations/analysisABSTRACT
Objective: To optimize the prescription of liensinine solid dispersion osmotic pump controlled release tablet and research its release characteristics in vitro. Methods: The cumulative release percent in 2, 6, and 12 h and the linear correlation coefficient of cumulative release curve were taken as evaluation indexes to select the optimal prescription by using the central composite design- response surface methodology (CCD-RSM). The main factors of influence on drug release, which were the dosage of NaCl and PEG 400, and coating agent thickness. Results: The optimal prescription for liensinine solid dispersion osmotic pump controlled release tablet were as follows: NaCl dose was 166.0 mg, PEG 400 content was 80.5%, and the coating weight gain was 3.5%. Conclusion: The prescription optimization model of liensinine solid dispersion osmotic pump controlled release tablet is optimized by CCD-RSM, and it is proved to follow zero-order release kinetics.
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Objective To observe clinical curative effect of pregabalin combined with oxycodone hydrochloride controlled-release tablets on patients with postherpetic neuralgia(PHN).Methods 84 patients with PHN were randomly divided into observation group (n=42 cases) and control group ( n=42 cases); control group was given oxycodone hydrochloride controlled-release tablets, observation group received pregabalin combined with oxycodone hydrochloride controlled-release tablets treatment; NRS, dermatology life quality index (DLQI), Pittsburgh sleep quality score (PSQI) and SAS score were recoded before and after 1,2,4 weeks treatment; 24 h duration of pain, 24 h total sleep time , pain-relief effectiveness and adverse reactions of two group were compared.Results NRS, DLQI, PSQI and SAS score of two groups after 1,2,4 weeks treatment was lower than before treatment (P<0.05), all the scores of observation group were lower than control group (P <0.05); 24 h duration of pain of observation group was obviously less than control group ( P <0.05 ) , 24 h total sleep time was longer than control group ( P <0.05 ); dose of oxycodone hydrochloride controlled-release tablets in observation group was lower than control group ( P <0.05 ); pain relief effectiveness of observation group was obviously higher than that of control group (P<0.05); adverse reactions of observation group such as dry mouth, dizziness was higher than control group (P<0.05), the rest of the adverse reactions in two groups had no significant statistical difference.Conclusions Treatment of pregabalin combined with oxycodone hydrochloride controlled-release tablets are both effective and safe significantly, and can obviously improve the patient’ s pain symptoms, improve quality of life, preferable satisfactory comprehensive curative effect.
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Objective: To optimize the formulations of microporosity osmotic pump controlled release tablet of solid dispersion for total flavonoids from Desmodium styracifolium (TFDS) by central composite design-response surface methodology. Methods: The independent variables comprised of the amount of lactose, pore-forming agent, and coating weight gain, and the dependent variables involved the cumulative release after 2, 6, and 12 h, and the linear correlation coefficient of cumulative release curve. Design-expert software was used to fit multivariate linear models and quadratic multinomial models for experimental data. Response surface was delineated according to best-fit mathematic models and the optimum formulation was selected by Numerical Optimization. Results: The correlation coefficients of quadratic multinomial models were better than those of multivariate linear models. There was close agreement between the observed and predicted values for the cumulative release, and bias were all less than 5%. Conclusion: The model established by Design-expert Software is better to predict and could be used to optimize the formulations of microporosity osmotic pump controlled release tablets of solid dispersion for TFDS.
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Objective: To prepare bi-layer osmotic pump controlled release tablet of total flavonoids from Ginkgo Folium (BOPCRT- TFGF), and to optimize its formulation by central composite design response surface methodology (CCD RSM). Methods: Single-factor test was desigined by screening the formulations of tablet core and coating film. The independent variables comprised of amount of polyethylene glycol in coating solution and coating weight gain, and the dependent variables included the percentages cumulative release of BOPCRT-TFGF after 2 and 14 h and multiple correlation coefficient of druge release profile in 1-12 h. The formulation was optimized by CCD RSM and the optimized formulation was also verified. Results: The optimized formulation was as follows: The tablet weight gain in coating was 7.58%, and PEG 4000 was 3.41 g. There was no significant difference between the measured and the predicted values. The cumulative release of the optimal osmotic pump tablets after 2 h did not appear sudden release, and the cumulative release within 14 h was over 85%. The drug release profile in 1-12 h exhibited a zero order character. Conclusion: A reliable model is established using response surface methodology and the formulation of BOPCRT-TFGF could be optimized. The BOPCRT-TFGF for administration once daily is prepared.
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[Objective] To evaluate the efficacy and safety of oxycodone controlled-release tablets in patients with advanced non-small cell lung cancer ( NSCLC ) who suffered from cancer pain and needed the treatment of docetaxel as second-line drug. [Methods] Data from 40 patients with NSCLC who suf-fered from moderate and severe cancer pain and were treated with oxycodone controlled -release tablets and docetaxel 75mg/m2 on d1 every 3 weeks from Feb 2007 to July 2011.The analgesic effects, karnofsky per-formance status scales ( KPS) and adverse effects were observed . [ Results] A group of 40 patients were available for evaluation, of whom the response rate was 27.5%,the disease control rate 60%,and the medi-an survival of all 9.35 months, with one-year survival rate being 37.5%.Compared with the condition be-fore treatment, pain in patients was greatly relieved , and the total pain relief rate was 97.5%,with the NRS score decreased significantly , and KPS score significantly raised , whose differences were statistically signifi-cant (P<0.05).The main side effect was hematologic toxicity and constipation , which could be solved af-ter treatment. [ Conclusion] Oxycodone combined with Docetaxel has satisfactory efficacy for the pa-tients with moderate to severe pain in NSCLC , thus markedly improving the quality of life of the patients .