Enhancement of oral moisture using tablets containing extract of Capparis masaikai Levl.

Aim of the study

This study was performed to examine the effects of tablets containing an extract of Capparis masaikai Levl. (M-tablets) on enhancing oral moisture.

Subjects and methods

The moistening effect of M-tablets was examined in 21 healthy subjects aged 25.1 ± 2.4 (mean ± S.D.) years in comparison with control tablets. After sucking tablets, the oral moisture was measured using a saliva wetness tester and a moisture checker. To evaluate the effects of the M-tablets on oral conditions, additional 50 subjects aged 30.6 ± 7.5 years were examined. The subjects recorded changes in refreshment, oral moisture, ease in speaking, and taste of water using a visual analog scale (VAS).

Results

The L-SALIVO^® value of the M-tablet increased significantly from 1.83 ± 0.17 (mean ± S.E.M.) at baseline to 3.02 ± 0.21 at 15 min (P < 0.01). The Mucus^® value of the M-tablet also increased from 37.50 ± 0.22 at baseline to 38.30 ± 0.26 at 15 min (P < 0.01). The VAS value for oral moisture increased significantly from 47.4 ± 2.0 to 69.6 ± 2.2 after taking the M-tablet (P < 0.01). The VAS value for taste of water also increased from 50.0 ± 1.1 to 66.7 ± 3.2 (P < 0.01).

Conclusion

These results suggest that M-tablets are useful for enhancing oral moisture, which leads to improvement of oral conditions.     

Hypolipidemic activity of aqueous extract of Capparis spinosa L. in normal and diabetic rats

The purpose of this study was to examine the effect of single and repeated oral administrations of the aqueous extract of Capparis spinosa L. (CS) at a dose of 20mg/kg on lipid metabolism in normal and streptozotocin-induced diabetic rats. In normal rats, the aqueous extract of CS induced a significant decrease on plasma triglycerides concentrations 1 week (p<0.05) and 2 weeks (p<0.01) after once daily repeated oral administration. A significant decrease of plasma cholesterol levels was also observed 4 days (p<0.05) and 1 week (p<0.05) after repeated oral administration. In diabetic rats, CS treatment caused a significant decrease of plasma triglycerides levels after repeated oral administration. Four days after repeated oral administration of aqueous CS extract, the plasma cholesterol levels were significantly decreased (p<0.05) and still dropped after 2 weeks (p<0.01). On the other hand, the repeated oral administration of CS aqueous extract caused a significant decrease of body weight 4 days after repeated oral treatment in diabetic rats (p<0.05). We conclude that the aqueous extract of CS (20 mg/kg) exhibits a potent lipid lowering activity in both normal and severe hyperglycemic rats after repeated oral administration of CS aqueous extract.     

Topical Aloe Vera (Aloe barbadensis Miller) Extract Does Not Accelerate the Oral Wound Healing in Rats

The effect of topical application of Aloe Vera (Aloe barbadensis Miller) extract was assessed on the healing of rat oral wounds in an in vivo model using 72 male Wistar rats divided into three groups (n = 24): control, placebo and Aloe Vera (0.5% extract hydroalcoholic). Traumatic ulcers were caused in the dorsum of the tongue using a 3‐mm punch tool. The Aloe Vera and placebo group received two daily applications. The animals were sacrificed after 1, 5, 10 and 14 days. Clinical analysis (ulcer area and percentage of repair) and histopathological analysis (degree of re‐epithelialization and inflammation) were performed. The comparison of the differences between scores based on group and experimental period, both in quantitative and semi‐quantitative analyses, was performed using the Kruskal–Wallis test. The significance level was 5%. On day 1, all groups showed predominantly acute inflammatory infiltrate. On day 5, there was partial epithelialization and chronic inflammatory infiltrate. On the days 10 and 14 total repair of ulcers was observed. There was no significant difference between groups in the repair of mouth ulcers. It is concluded that treatment using Aloe Vera as an herbal formulation did not accelerate oral wound healing in rats. Copyright © 2015 John Wiley & Sons, Ltd.     

舌苔形成的微生态学机制探讨

舌苔是由脾胃之气上熏,胃津上潮,凝聚于舌面而生。舌苔是散布于舌背的一层苔垢,由舌背脱落细胞、唾液、细菌、食物碎屑以及渗出的白细胞等填充于丝状乳头角化树的间隙内组成。舌背微生态变化是影响舌苔形成与变化的重要因素,研究舌背微生态的组成与变化规律对于阐明舌苔形成机制具有重要价值。本文就近年来舌背微生态的研究方法及与疾病的相关性进行综述,以期为研究舌背微生态变化、舌苔形成与中医证型的相关性提供依据,为中医药学的现代化研究提供新的思路和方法。     

Immunostimulant effects of Capparis zeylanica Linn. leaves

The present study was undertaken to explore the immunomodulatory activity of ethanolic and water extracts of Capparis zeylanica Linn. (family: Capparidaceae) leaves on neutrophil adhesion test, humoral response to sheep red blood cells, delayed-type hypersensitivity, phagocytic activity and cyclophosphamide-induced myelosuppression. Pre-treatment of water extract (300 mg/kg, oral) of Capparis zeylanica evoked a significant increase in neutrophil adhesion to nylon fibres. The augmentation of humoral immune response to sheep red blood cells by ethanolic and water extracts (150-300 mg/kg) is evidenced by increase in antibody titres in mice. A dose-related increase in both primary and secondary antibody titre was observed. Oral administration of ethanolic and water extracts of Capparis zeylanica leaves, at doses of 150 and 300 mg/kg in mice, dose dependently potentiated the delayed-type hypersensitivity reaction induced by sheep red blood cells. Immunomodulatory activity was also assessed by serological and haematological tests. Capparis zeylanica extracts prevented myelosuppression in mice treated with cyclophosphamide drug. The study comprised the acute toxicity and preliminary phytochemical screening of the ethanol and water extracts.     

Antinociceptive activity of methanol extract of fruits of Capparis ovata in mice

Ethnopharmacological relevance

Capparis ovata Desf. and Capparis spinosa L. have wide natural distribution in Turkey and they are consumed in pickled form. Flower buds, root bark, and fruits of the plant are used in folk medicine due to their analgesic, wound healing, cell regeneration, tonic, and diuretic effects.

Aim of the study

In this study, we attempted to identify the possible antinociceptive action of methanol extract prepared from fruits of Capparis ovata.

Materials and methods

Using tail immersion, hot plate and writhing tests, the antinociceptive effect of the methanol extract of Capparis ovata (MEC) fruits was assessed after intraperitoneal administration into mice. Morphine sulfate (5 mg/kg; i.p.) and diclofenac (10 mg/kg; i.p.) were used as reference analgesic agents. Naloxone (5 mg/kg; i.p.) was also tested.

Results

MEC was studied at the doses of 50, 100, and 200 mg/kg (i.p.) and exhibited significant antinociceptive activities in all tests used. The above-mentioned doses of the extract reduced the writhing responses by 32.21, 55.70, and 68.36%, respectively. MPE% were increased by 7.27, 12.07, 14.60% in the tail immersion, and 7.88, 11.71, 16.73% in the hot plate test at the tested doses, respectively. Naloxone antagonized antinociceptive effect at the doses of 100 and 200 mg/kg whereas partially antagonized the effect of MEC at the dose of 50 mg/kg.

Conclusions

Based on the results obtained, it can be concluded that MEC has antinociceptive effects both at the peripheral and central levels.     

电子舌用于药物掩味效果评价的研究

药物掩味效果评价对药学工作者开展药物掩味研究具有重要的意义。为了研究电子舌用于药物掩味效果评价的可行性,本实验利用盐酸小檗碱作为苦味模型药物,选择醋酸钠、2,4-二羟基甲苯酸、甜蜜素等作为苦味掩味物质,通过电子舌进行测定,根据主成分分析结果及苦距、苦度降低距、抑制率等指标对比,判断各掩味剂对盐酸小檗碱的掩味效果是否和志愿者口尝药物评判方法所得结果一致;并将掩味效果最好的甜蜜素配制成不同的浓度,对其用量进行优化。数据处理结果显示,在0.005 mg·mL-1的盐酸小檗碱溶液中,各掩味剂的掩味效果好坏依次为甜蜜素＞2,4-二羟基苯甲酸＞醋酸钠;随着甜蜜素用量的增加,其掩味效果越来越好,但0.2%以后的浓度掩味效果变化相对较小,在实际工作中,可以选择0.2%的浓度来掩味;本实验结果与口尝实验结果一致。本研究表明,在一定程度上,电子舌可作为评价药物掩味效果的一种有效的工具。     

口服制剂口感评价方法的应用进展

口感是影响口服制剂成药性和患者用药依从性的重要因素,是口服制剂处方设计和临床应用的重要考量指标,如何客观、准确、简便、高效地表征口感,是制约口服制剂口感设计与开发利用的瓶颈问题。目前,国内外常用的口服制剂口感评价方法有口尝法、电子舌法、动物味觉喜好实验、体外溶出度实验和电生理实验。口尝法是口感评价的首选,但结果的客观性和重复性较差。鉴于此,其他4种口感评价技术已作为辅助方法应用于制药行业,但都存在一定的局限性。该研究重点对上述方法的检测原理、适用性及优缺点进行评述,以期为现阶段口服制剂的矫味和口感评价研究提供方法学借鉴,提高患者服药依从性和口服制剂产品的业内竞争力,推动口服制剂工艺研究水平的进步。     

基于口尝和电子舌技术探讨味道检测在黑顺片质量评价中的实用价值

目的:通过口尝和电子舌技术,结合胆巴含量,研究味道检测在黑顺片质量评价中的实用价值。方法:通过口尝和电子舌检测饮片味道,利用主成分分析(PCA)和Fisher模型分析市售黑顺片味道差异,利用偏最小二乘法(PLS)建立口尝评价和电子舌传感器数值的关系模型,建立电子舌CTS(咸)传感器与胆巴含量线性回归方程。结果:采集的样品中有84%具有咸涩味,与《中华人民共和国药典》(以下简称《中国药典》)2015年版规定的“味淡”不一致。电子舌技术结合PCA和fisher模型可明显区分“味淡”饮片与其余27批黑顺片。电子舌CTS(咸)传感器响应值(X)与胆巴含量(Y)线性回归方程为Y=-19.013+0.025 X(r=0.9304)。结论:电子舌能够快速准确辨别黑顺片是否符合《中国药典》2015年版“味淡”的要求,由CTS(咸)传感器响应值可推测出对味道影响较大的胆巴的含量,味道检测在黑顺片质量评价中具有实用价值,可以作为中药饮片质量评价的补充。     

The discovery of Capparis spinosa L. (Capparidaceae) in the Yanghai Tombs (2800 years b.p.), NW China, and its medicinal implications

Seed clumps of Capparis spinosa L. together with shoots, leaves and fruits of Cannabis sativa L. were unearthed in the Yanghai Tombs, Turpan District in Xinjiang, China. This is the first time that plant remains of Capparis spinosa have been discovered in China and the eastern part of Central Asia. Based on the joint occurrence of Capparis spinosa and Cannabis sativa, and the pharmacological value of the seeds of Capparis spinosa, it is deduced that caper was utilized for medicinal purposes.     

Pharmacological in vivo test to evaluate the bioavailability of some St John's Wort innovative oral preparations

In this study, the optimisation of biopharmaceutical properties of a dried commercial extract of St John's Wort were evaluated employing the in vivo forced swimming test (FST). Three new dosage forms containing beta-cyclodextrin and surfactants (SDS, ASC8) were compared in the FST with the commercial extract. The commercial extract showed antidepressant activity in mice after 60 min at a dosage of 100 mg/kg. The same antidepressant activity appeared in 30 min with a micellar solution of SDS containing the same quantity of extract (100 mg/kg), while with micelles of ASC8 the effect appeared at 15 min and with a dosage of 30 mg/kg. In the case of beta-cyclodextrin the best results were obtained at 30 min, administering 60 mg/kg of the extract. Finally, the influence of the formulations on the water solubility of the constituents of the extract is reported. The tensides dramatically enhanced solubility, in particular that of the more lipophilic compounds, in the case of beta-cyclodextrin this effect was very pronounced for flavonoids and biapigenin, lower for hypericins and practically insignificant for hyperforins.     

Evaluation of anti-tussive activity of Chamaedorea tepejilote

Aim of the study

Evaluate the potential inhibition of cough in a mouse model induced by sulfur dioxide gas of methanol and chloroform extracts of aerial parts of Chamaedorea tepejilote.

Material and methods

The antitussive effect was examined using the Ogyhara method. The extracts and theobromine were orally administered to mice. Each extract was administered to one group (400 mg/Kg) and theobromine (2 mg), and negative control received PVP. The frequency of cough was measured at 60, 90 min after the administration of chloroform extract.

Results

The water extract of C. tepejilote had no effect on the pharmacological model used in this study. The effects of the methanol and chloroform extracts of this plant on sulfur-dioxide-induced cough in experimental animals show activity dose-dependently in the range between 100 to 500 mg/Kg. At doses of 400 mg/kg, the methanol and chloroform extracts inhibited cough by 41.72% and 49.1%, respectively; these results are comparable to the effect produced by the antitussive agent theobromine (53.4% inhibition).

Conclusions

Both extracts exhibited significant antitussive activity, and the effect of the chloroform extract was dose dependent. The antitussive activity of this extract was comparable to that of theobromine. The effect of chloroform extract on the trachea was also tested; it did not relax pre-contractions in guinea pig trachealis induced KCl, carbachol or histamine.     

Pharmacodynamic interaction of the sedative effects of Ternstroemia pringlei (Rose) Standl. with six central nervous system depressant drugs in mice

ETHNOPHARMACOLOGICAL RELEVANCE: The decoction of dried fruits of Ternstroemia pringlei (Rose) Standl. (Theaceae), commonly known as "Flor de Tila", is used in the Mexican traditional medicine to diminish insomnia and fear. AIM OF THE STUDY: To examine the sedative effects of the dried fruits of Ternstroemia pringlei and investigate a possible synergistic pharmacodynamic interaction between the sedative effect of aqueous extract of this plant and six central nervous system (CNS) depressant drugs. MATERIALS AND METHODS: The sedative effect was performed using the exploratory cylinder test in ICR mice. The extracts and drugs were intraperitoneally administered 30min before testing in different doses, with exception of ethanol and buspirone which were administered 5 and 20min before testing, respectively. An isobolographic analysis was used to characterize the interaction between Ternstroemia pringlei extract and six CNS depressant drugs. RESULTS: The intraperitoneal administration of the hexane, dichloromethane, methanol and aqueous extracts of Ternstroemia pringlei showed a dose-dependent sedative effect. Ternstroemia pringlei aqueous extract combined with buspirone, diazepam, diphenhydramine, haloperidol or pentobarbital exerted a super-additive (synergistic) sedative interaction. Whereas the combination Ternstroemia pringlei extract plus ethanol resulted in a sub-additive (attenuate) sedative interaction. CONCLUSIONS: These findings are in agreement with the traditional use of Ternstroemia pringlei in the treatment of insomnia, however it is a plant that interacts in a complex form with CNS depressant drugs. It may represent an advertence on the use of this plant concomitantly with other neuroactive drugs.     

小儿清热止咳口服液澄清工艺比较

目的:优选小儿清热止咳口服液的澄清工艺.方法:比较高速离心法、乙醇沉淀法、ZTC1+1Ⅲ型天然澄清剂法3种澄清工艺对小儿清热止咳口服液中收膏率、麻黄碱和黄芩苷相对含量的影响.结果:乙醇沉淀法为最佳澄清工艺,其工艺条件为药液浓度比1∶1,加95％乙醇调至含醇量60％,冷藏放置6h.结论:优选的澄清工艺稳定,可行.     

Hypoglycemic and hypolipidemic effects of the aqueous fresh leaves extract of Clerodendrum capitatum in Wistar rats

Diabetes mellitus, the most common endocrine disorder of carbohydrate metabolism, is treated in the African traditional phytotherapies with the cold water decoction of Clerodendrum capitatum (CC). In the current study, the hypoglycemic and hypolipidemic effects of fresh leaves aqueous extract of CC were studied in four groups of six adult Wistar rats per group and weighting 120-150 g, by administering graded oral doses (100, 400 and 800 mg/kg/day) of the extract for 14 days. On the 15th day, the fasted rats were anesthetized under inhaled halothane and blood samples obtained through cardiac puncture. Phytochemical analysis of CC extract was conducted using standard procedures while the preliminary acute oral toxicity study was also conducted using limit dose test of Up and Down Procedure at a limit dose of 5000 mg/kg body weight/oral route. Results of the study showed CC to cause significant (p<0.05, p<0.001) dose dependent hypoglycemic and hypolipidemic effects but had no effect on the pattern of weight gain in the treated rats. Although no lethal effect was recorded with CC oral administration for up to 5000 mg/kg body weight/oral route, but there was an associated transient somatomotor and behavioral toxicities. Phytochemical results revealed the presence of saponins, flavonoids, alkaloids, tannin, glycosides and reducing sugars in the extract. Thus, the folkloric use of Clerodendrum capitatum in the treatment of suspected type 2 diabetics has a positive correlation with scientific data generated in this study.     

Acute and chronic toxicity of a lyophilised aqueous extract of Tanacetum vulgare leaves in rodents

AIM OF THE STUDY: The present investigation was carried out to evaluate the safety of an aqueous extract of tansy (Tanacetum vulgare L.) leaves by determining its potential toxicity after acute and chronic administration in rodents. MATERIALS AND METHODS: For the acute study, a lyophilized aqueous extract of tansy leaves was administered to mice in single doses of 0-13 g/kg given by gavage as well as intraperitoneal doses of 0-4.5 g/kg. General behavior adverse effects and mortality were determined for up to 14 days. In the chronic dose study, the extract was administered orally at doses of 0, 100, 300 and 600 mg/kg daily for 90 days to rats. Biochemical and hematological parameters were determined after 30 and 60 days, and then at the end of 90 days of daily administration. RESULTS: In the acute study in mice, the crude aqueous extract of tansy leaves caused dose-dependent general behavior adverse effects and mortality. The no-observed adverse effect levels (NOAEL) of the tansy extract were 7.0 g/kg and 1.0 g/kg, and the lowest-observed adverse effect levels (LOAEL) were 9.0 g/kg and 1.5 g/kg, when given by the oral and intraperitoneal routes, respectively. Mortality increased with increasing doses, with LD(50) of 9.9 g/kg and 2.8 g/kg for the oral and intraperitonal modes of administration, respectively. In the chronic study in rats, daily oral administration of the crude aqueous extract of tansy leaves for up to 90 days did not result in death or significant changes in the biological (except for hypoglycemia) and hematological parameters. CONCLUSIONS: Because of the relatively high NOAEL values in the acute study in mice, and lack of significant effect on biological and hematological parameters in rats after 90 days of daily doses, the tansy extract does not appear to have significant toxicity. In view of the dose of tansy consumed in traditional medicine, there is a wide margin of safety for the therapeutic use of the aqueous extract of Tanacetum vulgare leaves.     

基于电子舌和多成分定量技术的厚朴“苦味”药性物质基础研究

目的：通过电子舌与多成分定量相结合的方法揭示厚朴“苦味”药性物质基础。方法：采用电子舌对20批厚朴药材的味觉进行定量化;采用多成分含量测定对20批厚朴中的紫丁香酚苷、木兰花碱、木兰箭毒碱、木兰苷A、木兰苷B、和厚朴酚、厚朴酚和辣薄荷基厚朴酚8个化学成分的含量进行分析,并测定药材电子舌测试液中除辣薄荷基厚朴酚外的7个化学成分的质量浓度;采用皮尔逊相关性分析建立化学成分与味觉传感器响应值的相关关系。根据相关性结果筛选出6个单体化合物并对其味觉进行测定。结果：厚朴药材中和厚朴酚、厚朴酚和辣薄荷基厚朴酚与电子舌苦味、苦味回味存在显著的正相关（P<0.05）;厚朴酚、和厚朴酚虽然为脂溶性化学成分,在电子舌测试液中的含量较低,但仍与苦味、苦味回味有显著正相关（P<0.05）;单体化合物的味觉测试中,厚朴酚、和厚朴酚的苦味和苦味回味的响应值均为最高。结论：厚朴酚与和厚朴酚为厚朴“苦味”药性物质基础。     

Effects of Copaiba Oil Topical Administration on Oral Wound Healing

The effects of topical copaiba oil extract and topical corticosteroid were assessed on oral wound healing in an in vivo model using 96 male Wistar rats. Traumatic ulcers were caused in the dorsum of the tongue using a 3‐mm punch tool. The animals were divided into: Control; Corticosteroid; Placebo and Copaiba oil Group. The animals received two daily applications of the products. The control group received only daily handling. Six rats in each group were euthanized at days 3, 5, 10 and 14. The animals were monitored daily to determine wound status. The weigh was assessed at day 0 and euthanasia day. The percentage of repair was calculated, and histopathological aspects were analyzed. The Kruskal–Wallis test was used to compare the results between groups and times of evaluation. Closing time was assessed through the log‐rank test. The corticosteroid group lost more weight at days 10 and 14 than the control group (p < 0.05). Moreover, the healing time of corticosteroid group was longer than the control group (p = 0.007). No differences were observed between the copaiba oil group and the control group. We concluded that topical copaiba oil, in spite of being safe, did not accelerate the process of oral wound healing. Copyright © 2017 John Wiley & Sons, Ltd.     

基于电子舌技术的生炒酸枣仁滋味比较

目的：运用电子舌技术对炒制前后酸枣仁滋味进行定量表征,建立生、炒酸枣仁滋味判别模型。方法：采用电子舌技术对生、炒酸枣仁本身味道进行检测,通过配对t检验、主成分分析(PCA)、正交偏最小二乘法-判别分析(OPLS-DA)对获取的各味道特征值进行处理,分析酸枣仁炒制前后各味道的变化情况。结果：配对t检验显示,酸枣仁炒制对AHS (酸)、CTS (咸)、NMS (鲜)、ANS (甜)、CPS (通用)、SCS (苦)味值的变化均有影响,对PKS (通用)味值影响不明显,其中SCS、NMS、CPS、AHS、ANS味值上升,CTS味值下降,炒制对各滋味的影响程度为SCS>NMS>CPS>AHS>ANS>CTS>PKS;通过PCA可以区分酸枣仁与炒酸枣仁;通过OPLS-DA可以建立酸枣仁与炒酸枣仁滋味判别模型,该模型对X矩阵的解释率(R²X)=0.900、对Y矩阵的解释率(R²Y)=0.967、预测能力(Q²)=0.965,表明该模型拟合度、预测性良好。结论：电子舌技术可以从数值上客观化体现炒制对...     

射干提取物含药血清对豚鼠离体气管平滑肌收缩功能的影响

目的:研究射干提取物含药血清对豚鼠离体气管平滑肌收缩功能的影响.方法:取豚鼠气管,在Kreb's液中制备气管平滑肌螺旋条,于恒温浴槽装置中,加入组胺(His)使其收缩,观察加入射干提取物含药血清后3,5,10 min的解痉率.结果:射干提取物含药血清对组胺引起的气管平滑肌收缩反应有一定拈抗作用,其中剂量(0.46 g?kg-1)3,5,10 min解痉率分别为44.29％,45.27％和48.30％;高剂量(0.92 g?kg-1)3,5 min解痉率分别为31.17％和31.83％,与空白对照组比较有显著性差异(P ＜0.05或P＜0.01),药物与标本接触5 min效果最好.结论:射干提取物含药血清对His引起的气管平滑肌收缩反应具有一定的拮抗作用.