Preparation and quality evaluation of Leonurine hydrochloride tablets / 中国药房

OBJECTIVE To prepare Leonurine hydrochloride tablets and evaluate the quality. METHODS The wet granulation technology was adopted ；leonurine hydrochloride was used as the crude drug ，and the types of fillers ，disintegrants，binders and lubricants were screened by single-factor experiments. Combined with orthogonal experiments ，using the cumulative dissolution rate within 15 minutes（using water as dissolution media ）as index ，the proportion of disintegrants ，the mass fraction of binder solution，and the proportion of lubricants were screened and verified. The in vitro dissolution behavior of the prepared Leonurine hydrochloride tablets （dissolution media were hydrochloric acid solution of pH 1.2，acetic acid-sodium acetate solution of pH 4.5， phosphate buffer solution of pH 6.8，water），tablet appearance ，hardness，friability and content uniformity were tested according to the general principles in 2020 edition of Chinese Pharmacopoeia （part Ⅳ）. RESULTS The optimal formulation of Leonurine hydrochloride tablets included leonurine hydrochloride crude drug of 500 mg，dextrin of 9 250 mg，crosslinking polyving y- pyrrolidone of 200 mg，magnesium stearate of 50 mg，1％ hydroxypropyl methyl cellulose solution of 4 mL. The average 15-minute cumulative dissolution rate of the three batches of tablets was 81.25％（RSD＝1.12％，n＝3）. In above 4 dissolution media，the dissolution equilibrium of prepared tablets could be reached within 30 minutes，and the cumulative dissolution rates exceeded 85％. The prepared tablets had uniform beige in color ，smooth surface ，complete edge ，no mottle ，spot，foreign matter ， etc.，hardness of 57.3 N（n＝6），weight loss rate of 0.15％. The content uniformity was in accordance with relevant provisions in 2020 edition of Chinese Pharmacopoeia （part Ⅳ）. CONCLUSIONS Leonurine hydrochloride tablets are successfully prepared ， and the quality comply with relevant regulations.

Controlled release of glaucocalyxin - a self-nanoemulsifying system from osmotic pump tablets with enhanced bioavailability.

OBJECTIVE: The purpose of this study was to develop a new formulation to enhance the bioavailability simultaneously with controlled release of glaucocalyxin A (GLA). MATERIAL AND METHODS: In this study, controlled release of GLA was achieved by the osmotic release strategy taking advantage of the bioavailability enhancing capacity of self-nanoemulsifying drug delivery systems (SNEDDS). The formulation of GLA-SNEDDS was selected by the solubility and pseudoternary-phase diagrams studies. The prepared GLA-SNEDDS formulations were characterized for self-emulsification time, effect of pH and robustness to dilution, droplet size analysis and zeta potential. The optimized GLA-SNEDDS were used to prepare GLA-SNEDDS osmotic pump tablet via direct powder compression method. The effect of formulation variables on the release characteristic was investigated. GLA-SNEDDS osmotic pump tablets were administered to beagle dogs and their pharmacokinetics were compared to GLA and GLA-SNEDDS as a control. RESULTS: In vitro drug release studies indicated that the GLA-SNEDDS osmotic pump tablet showed sustained release profiles with 90% released within 12 h. Pharmacokinetic study showed steady blood GLA with prolonged Tmax and mean residence time (MRT), and enhanced bioavailability for GLA-SNEDDS osmotic pump tablet. CONCLUSION: It was concluded that simultaneous controlling on GLA release and enhanced bioavailability had been achieved by a combination of osmotic pump tablet and SNEDDS.

Controlled release of ziprasidone solid dispersion systems from osmotic pump tablets with enhanced bioavailability in the fasted state.

OBJECTIVE: The purpose of this work was to develop a controlled release of ziprasidone with no food effect by the osmotic release strategy. METHODS: The solution of ziprasidone and poloxamer188 (P188) with different weight ratios was spray-dried to form solid dispersion of ziprasidone (SD-ZIP). The SD-ZIP was characterized using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (X-RD) and solubility testing. The SD-ZIP osmotic pump tablets were prepared by wet granulation method. The effect of formulation variables on the release characteristic was investigated. The SD-ZIP osmotic pump tablets were administered to fasted and fed beagle dogs and their pharmacokinetics were compared to commercial formulation Zeldox® as a control. RESULTS: The results of DSC and X-RD indicated that ziprasidone resides in P188 with no crystalline changes. Solubility studies demonstrated that the solubility of SD-ZIP was substantially improved compared to ziprasidone and physical mixtures of ziprasidone and P188. The optimized formulation and drug release profiles of SD-ZIP osmotic pump tablets in different medium were obtained which showed typical osmotically controlled release and could fitted to zero-order kinetics with good linear correlation. Pharmacokinetic studies in beagle dogs showed ziprasidone with prolong actions and no food effect was achieved simultaneously in SD-ZIP osmotic pump tablet compared with Zeldox®. CONCLUSION: The SD-ZIP osmotic pump tablet could be able to enhance the bioavailability in the fasted state and showed sustained release with prolonged actions.

The first pathogenetic feature and the analysis of misdiagnosis about the multiple sclerosis / 中国基层医药

Objective To investigate the first pathogenetie feature and the reason of misdiagnosis about the multiple sclerosis(MS). Methods To review and analyze 62 eases with the first pathogenetic medical record of MS. Results The most frequent clinical manifestation pf the first pathogenetie MS are the limbs paraesthesia(18 eases, 29.0%) ,dyskinesia(16 cases,25.8%) and visual disorder(11 cases, 17.7%), and the other clinical manifestation are the ataxia, epileptic seizure ,dyasarthria, dysuria, itch of skin, mental anomaly, vertigo and so on. The total of misdi-agnosis is 24 cases (38.7 %). Conclusion Except the main clinical manifestation, there are diversity, complexity forfirst pathogenetic MS,what's more the misdiagnosis rate is very high.

Influence of Gastroesophageal Reflux Disease Morbidity Rate by High Salt Diet in Mare Island Area / 医学研究杂志

12,9.41%(148/1578);RDQ≤12,91.58%(1430/1578).Logistic multiple regression analysis of gastroesophageal reflux correlation factor studied:OR= 2.781.Conclusions The results showed:there were close correlation of high salt diet and GERED.

Research on the curative effect of cerebrospinal fluid replacement combining intravenous drips and intrathecal injection of amphotericin B in the treatment of cryptococcal neoformans meningitis / 中国基层医药

Objective To study the curative effect of cerebrospinal fluid replacement combining intravenous drips and intrathecal injection of amphotericin B in the treatment of cryptococcal neoformans meningitis(CNM for short).Methods 28 CNM patients were randomly divided into two groups.Group A was the treatment group,and the treatment method was cerebrospinal fluid replacement combining intravenous drips and intrathecal injection of amphotericin B.Group B was the control group,and the treatment method was only intravenous drips and intrathecal injection of arnphotericin B.The period of treatment was 16 weeks.The curative effect was assessed in terms of symptoms,physical features,CSF routine examination,CSF cultivation and smear examination.Results The cura- tive effect of treatment group was better than that of the control group.There were remarkable differences between these two groups(P