Optimization Studies on Design and Evaluation of Orodispersible Pediatric Formulation of Indomethacin

In the present study, the aim was to optimize an orodispersible formulation of indomethacin using a combined approach of subliming agent and superdisintegrant. The tablets were made by non-aqueous wet granulation technique with superdisintegrant incorporated both intragranularly and extragranularly. A 2³ factorial design was used to investigate the effects amount of subliming agents namely camphor and ammonium bicarbonate and taste masking and soothening hydrophilic agent mannitol as independent variables and disintegration time and crushing strength as dependent responses. The volatilization time of eight hours at 50°C was optimized by conducting solid-state kinetic studies of optimized formulations. Optimized orodispersible tablets were evaluated for wetting time, water absorption ratio, porosity and in vitro and in vivo disintegration tests. Results show that higher levels of camphor and mannitol and a lower level of ammonium bicarbonate is desirable for orodispersion. Scanning electron microscopy (SEM) revealed the porous surface morphology and kinetic digital images substantiated the orodispersible property. Differential Scanning Calorimetry (DSC) studies exhibited physiochemical compatibility between indomethacin and various excipients used in the tablet formulation. Stability studies carried out as per ICH Q₁ A guidelines suggested the stable formulations for the tested time period of 6 months. The systematic approach of using subliming and disintegrating agents helped in achieving a stable, optimized orodispersible formulation, which could be industrially viable.     

Chitosan and Enteric Polymer Based Once Daily Sustained Release Tablets of Aceclofenac: <Emphasis Type="BoldItalic">In Vitro</Emphasis> and <Emphasis Type="BoldItalic">In Vivo</Emphasis> Studies

The purpose of this study was to develop a once daily sustained release tablet of aceclofenac using chitosan and an enteric coating polymer (hydroxypropyl methylcellulose phthalate or cellulose acetate phthalate). Overall sustained release for 24 h was achieved by preparing a double-layer tablet in which the immediate release layer was formulated for a prompt release of the drug and the sustained release layer was designed to achieve a prolonged release of drug. The preformulation studies like IR spectroscopic and differential scanning calorimetry showed the absence of drug–excipient interactions. The tablets were found within the permissible limits for various physicochemical parameters. Scanning electron microscopy was used to visualize the surface morphology of the tablets and to confirm drug release mechanisms. Good equivalence in the drug release profile was observed when drug release pattern of the tablet containing chitosan and hydroxypropyl methylcellulose phthalate (M-7) was compared with that of marketed tablet. The optimized tablets were stable at accelerated storage conditions for 6 months with respect to drug content and physical appearance. The results of pharmacokinetic studies in human volunteers showed that the optimized tablet (M-7) exhibited no difference in the in vivo drug release in comparison with marketed tablet. No significant difference between the values of pharmacokinetic parameters of M-7 and marketed tablets was observed (p > 0.05; 95% confidence intervals). However the clinical studies in large scale and, long term and extensive stability studies at different conditions are required to confirm these results.     

Ultrasound Transmission Technique as a Potential Tool for Physical Evaluation of Monolithic Matrix Tablets

The aim of this study was to investigate the effects of tablet porosity and particle size fraction of compacted Starch acetate powders, with and without model drug caffeine, on acoustic properties of tablets. The ultrasound velocity was determined from the transmission measurements. Tablets of starch acetate (SA DS 2.7) powder with two particle size fractions of 0–53 and 0–710 μm were compressed with a compaction simulator. Porosities of tablets varied in the range from 12% to 43% for both particle size fractions. Strong associations were found between the ultrasound velocity and physical properties of the tablets such as porosity and particle size fraction. Interestingly, ultrasound velocity was practically insensitive to inclusion of the model drug caffeine with the concentrations used. Based on this study ultrasound transmission method is a potential non-destructive tool for studying structural changes of tablets and other solid dosage forms.     

甲磺酸多沙唑嗪控释片联合中药坐浴治疗老年非细菌性前列腺炎的临床疗效

目的:探讨甲磺酸多沙唑嗪控释片联合中药坐浴治疗老年非细菌性前列腺炎的临床疗效。方法:选取我院泌尿男科收治的老年非细菌性前列腺炎患者60例,随机分配为实验组和对照组,每组各30例,对照组患者使用甲磺酸多沙唑嗪控释片进行治疗,实验组患者在对照组的治疗基础上加用中药坐浴进行治疗,两组患者均治疗1个月。治疗结束后对患者前列腺液中的WBC水平进行检测,并应用美国国家卫生研究院慢性前列腺炎症状指数(NIH-CPSI)表对患者的前列腺功能进行评分,同时比较治疗结束后两组患者临床总有效率。结果:与治疗前相比,两组患者WBC计数及NIH-CPSI评分均有所降低(P0.05);与对照组相比,实验组患者治疗后WBC计数及NIH-CPSI评分较低(P0.05);临床总有效率较高(P0.05)。结论:甲磺酸多沙唑嗪控释片联合中药坐浴能够提高老年非细菌性前列腺炎患者的前列腺功能,降低炎症反应,临床疗效更好。     

Effect of lipid lowering tablet on blood lipid in hyperlipidemia model rats

Observe the effect of lipid-lowering tablets on body weight, liver index and serum biochemical indexes of hyperlipidemia rats. The hyperlipidemia rat model was replicated successfully. Compared with the model group, high, medium and low dose lipid-lowering tablets group could significantly increase the body weight of rats with hyperlipidemia (P?<?0.01, P?<?0.05); High and middle dose lipid-lowering tablets group could significantly reduce the liver index of high fat rat (P?<?0.01); High, medium and low dose lipid-lowering tablets group could significantly decrease levels of TC, TG, LDL-C, AST, ALT, ALP, Y-GT in serum (P?<?0.01, P?<?0.05), and significantly increase the level of HDL-C (P?<?0.01). Lipid-lowering tablets can effectively regulate the body lipid metabolism of rats, and have a certain therapeutic effect on hyperlipidemia.     

Hydrophilic excipients modulate the time lag of time-controlled disintegrating press-coated tablets

An oral press-coated tablet was developed by means of direct compression to achieve the time-controlled disintegrating or rupturing function with a distinct predetermined lag time. This press-coated tablet containing sodium diclofenac in the inner core was formulated with an outer shell by different weight ratios of hydrophobic polymer of micronized ethylcellulose (EC) powder and hydrophilic excipients such as spray-dried lactose (SDL) or hydroxypropyl methylcellulose (HPMC). The effect of the formulation of an outer shell comprising both hydrophobic polymer and hydrophilic excipients on the time lag of drug release was investigated. The release profile of the press-coated tablet exhibited a time period without drug release (time lag) followed by a rapid and complete release phase, in which the outer shell ruptured or broke into 2 halves. The lag phase was markedly dependent on the weight ratios of EC/SDL or EC/HPMC in the outer shell. Different time lags of the press-coated tablets from 1.0 to 16.3 hours could be modulated by changing the type and amount of the excipients. A semilogarithmic plot of the time lag of the tablet against the weight ratios of EC/SDL or EC/HPMC in the outer shell demonstrated a good linear relationship, withr=0.976 andr=0.982, respectively. The predetermined time lag prior to the drug release from a press-coated tablet prepared by using a micronized EC as a retarding coating shell can be adequately scheduled with the addition of hydrophilic excipients according to the time or site requirements.     

Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution

The aims of this study are (1) to compare the disintegration efficiency, and (2) to develop a discriminating test model for the 3 classes of superdisintegrants represented by Ac-Di-Sol, Primojel, and Polyplasdone XL10. Using a digital video camera to examine the disintegration process of tablets containing the same wt/wt percentage concentration of the disintegrants, Ac-Di-Sol was found to disintegrate tablets rapidly into apparently primary particles; Primojel also apparently disintegrated tablets into primary particles but more slowly; Polyplasdone XL10 disintegrated tablets rapidly but into larger masses of aggregated particles. The differences in the size distribution generated in the disintegrated tablets likely contribute to the drug dissolution rate differences found for aspirin tablets with similar disintegration rates. The aspirin tablet matrix is proposed as a model formulation for disintegrant efficiency comparison and performance consistency testing for quality control purposes. Published: December 12, 2005     

Movement of different-shaped particles in a pan-coating device using novel video-imaging techniques

The purpose of this study was to investigate the effects of particle shape on the movement of particles in a pan-coating device using novel video-imaging techniques. An area scan CCD camera was installed inside a 24-in pan coater at the same location as that of a spray nozzle, and the movement of particle was tracked using machine vision. A white tracer particle was introduced inside a bed of black-coated particles. The effects of pan loading, pan speed, and particle shape on the movement of particles was studied. The response variables were circulation time, surface time, projected area of particle per pass, dynamic angle of repose, cascading velocity, and dispersion coefficient. Experiments were conducted at 3 different pan speeds, 6, 9, and 12 rpm, and 2 fill levels (ratio of bed depth to pan diameter), one eighth and one quarter, and data were collected over a 30-minute time period. The differences in circulation times of spheres and tablets, with similar volume equivalent diameter as that of the sphere, were found to be insignificant at the 95% confidence interval. The circulation time ranged from 2.8 to 10.8 seconds depending on the operating condition and increased with increasing pan load and decreasing pan speed. The distributions of circulation time, surface time, and projected surface area were found to be nonnormal. The dynamic angle of repose for tablets was higher than for spheres. Also, the bed surface for spheres was much flatter in comparison with tablets where the bed shape attained a “wave-like” form. The average velocity of tablets in the cascading layer was found to be significantly higher than spheres. A linear model (R ²>0.98) best described the variation of velocity as a function of pan speed for all of the operating conditions. Published: October 6, 2005     

氨基酮戊酸光动力联合一清片治疗中重度痤疮效果及对血清学指标的影响

摘要 目的：观察氨基酮戊酸光动力联合一清片治疗中重度痤疮疗效以及对血清学指标的影响。方法：将93例中重度痤疮患者进行随机分组,31例为治疗组,31例为参照组1,31例为参照组2。治疗组采用氨基酮戊酸光动力联合一清片治疗,参照组1采用氨基酮戊酸光动力治疗,参照组2采用一清片治疗,观察三组治疗前、后患者痤疮严重程度分级系统(GAGS)评分、痤疮特异性生活质量量表（Qol-Acne）评分变化及性激素结合球蛋白（SHBG）、游离睾酮（FT）、雌二醇（E₂）、补体C3、免疫球蛋白IgG、IgM水平,比较三组临床疗效。结果：治疗组FT水平低于参照组1和参照组2（P＜0.05）,治疗组SHBG、E₂水平高于参照组1和参照组2（P＜0.05）,治疗组补体C3、IgG、IgM水平低于参照组1和参照组2（P＜0.05）,治疗组Qol-Acne评分较参照组1和参照组2高（P＜0.05）,治疗组GAGS评分较参照组1和参照组2低（P＜0.05）,治疗组总有效率（93.55%）高于参照组1（77.42%）和参照组2（64.52%）（P＜0.05）。结论：氨基酮戊酸光动力联合一清片治疗中重度痤疮患者,可调节患者内分泌,改善性激素水平及免疫状态,缓解患者痤疮症状,提升生活质量及临床疗效。