[Study on biopharmaceutics classification system of Chinese materia medica for Gegen Qinlians Tablets based on anti-inflammatory activity].

The research on biopharmaceutics classification system of Chinese materia medica( CMMBCS) should be finally implemented to the holistic research level of traditional Chinese medicine compounds,while the overall biopharmaceutical properties of traditional Chinese medicine compounds are not only the sum of solubility and permeability of each component. In this study,Gegen Qinlian Tablets was used as the research object,and the contents of 12 representative components,i.e. puerarin,daidzin,baicalin,daidzein,wogonoside,baicalein,wogonin,glycyrrhizic acid,coptisine hydrochloride,epiberberine,berberine hydrochloride and palmatine hydrochloride,were simultaneously determined by HPLC to obtain the mass weight of each component. The in vitro lipopolysaccharide( LPS)-induced RAW264. 7 cells inflammation model was established to investigate the anti-inflammatory effects of 12 representative components and obtain the efficacy weight of each component. In order to obtain the number of doses and effective permeability coefficient which can represent the overall biopharmaceutical properties of Gegen Qinlian Tablets,mass weight was combined with efficacy weight to integrate the solubility and permeability data of each component determined by typical shake flask method and in situ single pass intestinal perfusion model respectively. The results indicated that Gegen Qinlian Tablets should be categorized Ⅳ drug of the CMMBCS with low solubility and low permeability.

[Study on formulation of naoxuekang dispersible tablets].

OBJECTIVE: To study the formulation of Naoxuekang dispersible tablets. METHODS: The formulation was determined by pre-processing leech extractum prior to a series of experiments used to screen excipients like bulking agents and disintegrants and so on, and by adding disintegrants within and without. RESULTS: Microcrystalline cellulose was determined as the bulking agent, and carboxymethyl cellulose and low-substituted hydroxypropyl cellulose were determined as the disintegrants of Naoxuekang dispersible tablet formula. The average disintegration time and nitrogen content of one tablet were 52 seconds and 5.47 milligrams, respectively. Also disperse homogeneity, weight variation and microbial limit all met the requirements in Ch. P. CONCLUSION: The prepared Naoxuekang dispersible tablet is reasonable in formula, feasible in technology, which meets the quality standards.

A case of oesophageal ulcer developed after taking homeopathic pill in a young woman.

Oesophageal ulcers occur mainly as a result of gastro-oesophageal reflux disease (GERD). However, pill-induced oesophageal ulcers are a fairly common event. The lesion is mainly due to entrapment of the pill and/or its chemical composition thereof. This case report describes an oesophageal mucosa ulcer occurred in a healthy 35-year old woman who had no previous history of oesophageal disorders and received homeopathic medication. The present case reveals that pill entrapment can occur even in the oesophagus of healthy young individuals and that oesophageal mucosal ulcer can be triggered by substances generally thought devoid of any potentially mucosal aggressive effect.

[Optimization of formulation matrix proportion and preparation technology of realgar floating tablets for gastric retention by uniform design and correlation analysis].

OBJECTIVE: To optimize the different components proportions of the Realgar floating tablets for gastric retention by uniform design and correlation analysis. METHOD: With the different dosage of hydroxypropyl methyl cellulose (HPMC) as the tablets frame matrix, uniform design and correlation analysis were used to optimize the best component proportions of formula, and to measure the dissolution of the tablets in vitro. RESULT: Dissolution of the tablets in vitro was conformed to the expectation of experiment. The drug-release mechanism was by diffusion and corrosion at the same time. CONCLUSION: The Realgar floating tablets for gastric retention achieved the goal of design, which demand sustained release and safety.

PAT: From Western solid dosage forms to Chinese materia medica preparations using NIR-CI.

Near-infrared chemical imaging (NIR-CI) is an emerging technology that combines traditional near-infrared spectroscopy with chemical imaging. Therefore, NIR-CI can extract spectral information from pharmaceutical products and simultaneously visualize the spatial distribution of chemical components. The rapid and non-destructive features of NIR-CI make it an attractive process analytical technology (PAT) for identifying and monitoring critical control parameters during the pharmaceutical manufacturing process. This review mainly focuses on the pharmaceutical applications of NIR-CI in each unit operation during the manufacturing processes, from the Western solid dosage forms to the Chinese materia medica preparations. Finally, future applications of chemical imaging in the pharmaceutical industry are discussed.

Comparison of solid and liquid forms of homeopathic remedies for tonsillitis.

The efficacy of three plants used in homeopathy to treat acute tonsillitis was evaluated. A fixed combination of three plant substances (Phytolacca americana, Guajacum officinale, Capsicum annuum) was used in either solid (tablet) or liquid (drop) formulation: 107 patients were treated and no antibiotics were used. The objective and subjective symptoms of acute tonsillitis were noted. A significant decrease in symptoms was observed as early as 2.5 days after treatment startup; no serious adverse effects were reported. It was concluded that acute tonsillitis can be treated with a homeopathic remedy characterized by its immunomodulatory, analgesic, and anti-inflammatory properties.

[Application of colorimetric-equal value derivative spectrometry to the determination of cholic acid in niuhuang jiedu pian (tablet)].

A colorimetric-equal value derivative spectrometry for the quantitative analysis of cholic acid in Niuhuang Jiedu Pian(tablet)containing 8 crude drugs is reported. The method is free from the interferuce of borneol rhubarb and other components without separation. The average recovery of cholic acid is 99.75 +/- 0.79% (X +/- CV).

Remineralizing efficacy of Calcarea Fluorica tablets on the artificial carious enamel lesions using scanning electron microscope and surface microhardness testing: in vivo study.

CONTEXT: Remineralization is defined as the process whereby calcium and phosphate ions are supplied from a source external to tooth to promote ion deposition into crystal voids in demineralized enamel to produce net mineral gain. The remineralization produced by saliva is less and also a slow process, therefore remineralizing agents are required. AIMS: The study was planned to evaluate the effectiveness of homeopathic Calcarea Fluorica (calc-f) tablets as remineralizing agents on artificial carious lesions using scanning electron microscope (SEM) and surface microhardness (SMH) testing. SUBJECTS AND METHODS: A total of 24 patients needing removable orthodontic treatment were included in the study. They were divided into two groups of 12 patients each. The Group I consisted of patients in whom no tablets were given while Group II consisted of patients in whom calc-f tablets were given in a dosage of 4 tablets twice a day. Four enamel samples with the artificial carious lesions were then embedded in the removable appliance for a period of 6 weeks. After 6 weeks, the enamel samples were retrieved and evaluated by SEM and SMH. STATISTICAL ANALYSIS USED: One-sample Kolmogorov-Smirnov test and Student's t-test were applied to analyze the difference in the Vickers microhardness number (VHN) values of remineralized enamel obtained from control and experimental group. RESULTS: The signs of remineralization such as reduction in depth prismatic holes or decrease in porosity, variable sized uneven distribution of deposits and amorphous deposits were seen in enamel samples of both the groups. The mean SMH of remineralized enamel sample of Group I and Group II were 270.48 and 302.06, respectively, and the difference was statistically significant. CONCLUSIONS: (1) Remineralization occurred in both the groups as indicated by SEM and the increase in surface hardness values in both the groups. (2) Remineralization of enamel samples in the control group as indicated by SEM and also by increase in VHN values indicated that the saliva has a tendency of remineralizing the early carious lesions. Conclusions drawn from the study are that the calc-f tablets can be used as safe and cost effective remineralizing agent.

Development and validation of an ICP-OES method for quantitation of elemental impurities in tablets according to coming US pharmacopeia chapters.

May 1, 2014 the United States Pharmacopeia (USP) will implement two new chapters stating limit concentrations of elemental impurities in pharmaceuticals applying inductively coupled plasma methods. In the present work an inductively coupled plasma optical emission spectrometry (ICP-OES) method for quantitation of As, Cd, Cu, Cr, Fe, Hg, Ir, Mn, Mo, Ni, Os, Pb, Pd, Pt, Rh, Ru, V and Zn in tablets according to the new USP chapters was developed. Sample preparation was performed by microwave-assisted acid digestion using a mixture of 65% HNO3 and 37% HCl (3:1, v/v). Limits of detection and quantitation were at least a factor of ten below the USP limit concentrations showing that the ICP-OES technique is well suited for quantitation of elemental impurities. Excluding Os, spike recoveries in the range of 85.3-103.8% were obtained with relative standard deviations (%RSD) ranging from 1.3 to 3.2%. Due to memory effects the spike recovery and %RSD of Os were 161.5% and 13.7%, respectively, thus the method will need further development with respect to elimination of the memory effect of Os. The method was proven to be specific but with potential spectral interference for Ir, Os, Pb, Pt and Rh necessitating visual examination of the spectra. Hg memory effect was handled by using lower spike levels combined with rinsing with 0.1M HCl. The tablets had a content of Fe and Pt of 182.8 ± 18.1 and 2.8 ± 0.2 µg/g, respectively and did therefore not exceed the limit concentration defined by USP. It is suggested that the developed method is applicable to pharmaceutical products with a composition and maximal amount of daily intake (g drug product/day) similar to the tablets used in this work.

Pharmacokinetics and safety of repirinast tablets in healthy Chinese subjects

ABSTRACT Repirinast is a new, synthetic, disodium cromoglycate-like antiallergic agent for oral administration in humans. This study evaluated the safety, tolerability and pharmacokinetics of repirinast tablets in healthy Chinese volunteers. This was a phase I, open-label, randomized, single- and multiple-dose study. Subjects were assigned to receive a single dose of repirinast tablet at either 150, 300, or 450 mg, or multiple doses of 150 mg twice daily for 5 days. Plasma samples were analyzed with LC-MS/MS. Pharmacokinetic parameters of active metabolite MY-1250 (deesterified repirinast) were calculated using non-compartmental analysis with WinNonlin software. Statistical analysis was performed using SPSS software. All adverse events (AEs) were mild and of limited duration. No serious adverse event (SAE), death or withdrawal from the study was observed. In the single-dose study, Cmax was reached at about 0.75 hour, and the mean t1/2 was approximately 16.21 hours. Area under curve (AUC) and Cmax increased with dose escalation, but dose proportionality was not observed over the range of 150 to 450 mg. In the multiple-dose study, the steady-state was reached within 3 days with no accumulation. Repirinast tablet was well tolerated in healthy Chinese subjects.

Study of the variables which influence the impregnation of globules, compressed tablets and tablet triturates used in homeopathy

Globules, compressed tablets and tablet triturates are solid dosage forms used in homeopathy. Divergences can be noted between the preparation techniques described in official compendiums as well as those applied in homeopathic pharmacies. The difficulty associated with standardization of the impregnation of these dosage forms occurs due to the lack of detail provided for the techniques in the literature, leaving it up to each pharmacy to decide on the exact method of preparation. The objective was to optimize the impregnation technique, through investigating the variables that influence the impregnation of globules, compressed tablets and tablet triturates, applying the statistical tool of factorial design. The independent variables were the dosage form, percentage and type of impregnation and drying temperature, and the dependent variables were the mass gain, disintegration time, friability and hardness. For the globules, the greatest mass gain was for 10% impregnation and drying at 20 ºC. For the tablet triturates and compressed tablets the greatest mass gain was for 15% impregnation and there was no difference between the results obtained using simple and triple impregnation or different drying temperatures. The results can contribute to improving the final product quality, besides aiding in the establishment of standardized techniques for the official compendiums.

Glóbulos, comprimidos e tabletes são formas farmacêuticas sólidas utilizadas em homeopatia. Constatam-se divergências entre técnicas de preparação descritas nos compêndios oficiais, bem como em farmácias homeopáticas. A dificuldade de padronização na impregnação destas formas farmacêuticas também ocorre devido à falta de detalhamento das técnicas na literatura existente, deixando para cada farmácia a escolha de como executá-las. O objetivo foi otimizar a técnica de impregnação, através do estudo de variáveis que interferem na impregnação de glóbulos, comprimidos e tabletes, aplicando como ferramenta estatística planejamento fatorial. As variáveis foram forma farmacêutica, percentual e tipo de impregnação e temperatura de secagem, sendo o ganho de massa, tempo de desintegração, friabilidade e dureza as variáveis dependentes. Para os glóbulos, observou-se maior ganho de massa quando impregnados a 10% e secagem realizada a 20 ºC. Para os tabletes e comprimidos, constatou-se maior ganho de massa quando impregnados a 15%, sendo que não houve diferença na impregnação simples ou tríplice nem nas diferentes temperaturas de secagem. Os resultados obtidos podem contribuir para a melhoria da qualidade do produto final, além de auxiliar no estabelecimento de técnicas padronizadas para os compêndios oficiais.

Pain relief after inguinal hernia repair: a randomized double-blind study.

A randomized double-blind study was undertaken using 0.5 per cent bupivacaine ilioinguinal field block and oral papaveretum-aspirin tablets to assess pain relief after hernia surgery. A consecutive series of 200 men undergoing repair of a unilateral inguinal hernia underwent random allocation into one of the four groups to receive: bupivacaine and papaveretum-aspirin (group 1), bupivacaine and oral placebo (group 2), saline and papaveretum-aspirin (group 3), or saline and oral placebo (group 4). Patients were prescribed postoperative opiates to be given on demand. Pain levels and mobility were assessed at 6 and 24 h after operation. Patients in group 1 reported significantly less pain, required less additional opiates and had better mobility than those in group 4 (pain score P < 0.001 at 6 h and P = 0.002 at 24 h) and group 3 (P = 0.002 for pain and mobility scores at 6 h). Bupivacaine alone provided good immediate postoperative pain relief (P = 0.002 group 2 versus group 4 at 6 h). The combination of bupivacaine and papaveretum-aspirin provided the best results and is suitable for day-case postoperative analgesia.

Avaliação do perfil de dissolução de comprimidos de ciprofloxacino 250 mg comercializados como similares no Brasil / Dissolution profile evaluation of ciprofloxacin 250 mg tablets marketed as similar drugs in Brazil

O presente trabalho avaliou, in vitro, oito especialidades farmacêuticas contendo ciprofloxacino (250 mg), sendo o produto C, o medicamento referência (Cipro®) fabricado pela Bayer® S.A. e A, B, D, E, F, G e H medicamentos considerados similares. Além do teste de dissolução preconizado pela Farmacopéia americana, foi traçado o perfil de dissolução de cada amostra a partir do qual foram calculados parâmetros de eficiência de dissolução (ED). O preço máximo ao consumidor também foi levantado, para que fosse possível compará-lo com o desempenho dos produtos. Os resultados obtidos demonstram que todas as amostras atendem aos critérios especificados pelo teste de dissolução descrito na USP 24 ed., mas somente os produtos B, C, E e H foram aprovados no primeiro estágio (S1)...