Potent Preparation Research Articles

Importance and nutritional value with therapeutic properties of a traditional gulkand: A review

Rose flowers are considered an emerging nutraceutical due to their specific nutritional and medicinal properties. In ancient times, people used fresh rose petals or flowers to improve the flavor, taste and aesthetic appearance of foodstuffs. Petals of Rosa damascena, R. centifolia and R. indica, etc., are preferably used for extraction of rose oil and the making of gulkand and residual parts used as rose water. Among all the products, rose oil and gulkand are the most popular and demanding products due to their medicinal, fragrance and flavor value. It is also called rose petal jam or rose jam because the rose petals are preserved with sugar/honey/Jaggery/dry date fruit /coconut sugar and have a jam-like texture. Mostly, it is used as a laxative, tonic and flavoring purpose. The main objective of this review was to present the formulation, nutritional and medicinal value with health benefits of gulkand as it is prepared using high-value fresh rose petals and sugar with equal ratio (1:1) or different ratio (2:1) and is mainly manufactured in northern states of India. It has a rich nutraceutical value consisting of polyphenols, carbohydrates, dietary fibers, ash, vitamin C, etc. In Ayurveda, regular consumption of gulkand as a food supplement provides several health benefits and strengthens the body to fight excess heat, lethargy, muscular pain, improves eyesight and also provides relief in gastric and circulatory problems. Therefore, it is a safe and potent Ayurvedic preparation that plays a vital role in human nutrition and health and also creates self-employment opportunities. Keywords: Gulkand, Rose petals, Sugar, Nutraceutical, Health benefits.

Antifungal activity of protein hydrolysates from Thai Phatthalung Sangyod rice (Oryza sativa L.) seeds.

Fungal zoonoses are an economic and public health concern because they can cause various degrees of morbidity and mortality in animals and humans. To combat this issue, alternative natural antifungals, such as products derived from rice protein hydrolysates or rice antifungal protein/peptide are being considered because they are highly bioactive and exhibit various functional properties. Thailand is a leading rice producer and exporter. Among the various cultivated rice varieties, Sangyod rice (Oryza sativa L.) is exclusively indigenous to Thailand's Phatthalung province; it has a Thai geographical indication tag. Here, we investigated whether the Phatthalung Sangyod rice seeds have bioactive antifungal peptides. Antifungal activity in four Sangyod rice seed extracts (SYPs) - namely, (1) the crude lysate, SYP1; (2) the heat-treated lysate, SYP2; (3) the heat- and pepsin digested lysate, SYP3; and (4) the heat- and proteinase K-digested lysate, SYP4 - was analyzed. Protein concentrations in these SYPs were determined using the Bradford assay. The total phenolic compound content was determined using the modified Folin-Ciocalteu method in a 96-well microplate. Then, the SYP protein pattern was determined using the sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Subsequently, using the agar well diffusion method, the antifungal properties of these SYPs were tested against ten medically important pathogenic fungi. The minimal inhibitory concentration (MIC) and minimal fungicidal concentration values were determined for the active SYPs - SYP2-4. Finally, the clinical safety of SYP4 was determined using a hemolytic assay (using canine red blood cells [RBCs]). The crude lysate SYP1 did not show antifungal activity against any of the ten tested pathogenic fungi. Surprisingly, hydrolysates SYP2, SYP3, and SYP4 displayed antifungal properties against the ten tested pathogenic fungi. Thus, heat and enzymatic hydrolysis seem to transform the bioactivity of the crude protein extract - SYP1. Further, SYP4 shows the most effective antifungal activity. It completely inhibited Cryptococcus neoformans, Talaromyces marneffei yeast phase, Trichophyton mentagrophytes, and Trichophyton rubrum. A partial inhibitory action on Candida albicans and Microsporum gypseum was possessed while showing the least activity to C. neoformans. SYP4 was nontoxic to canine RBCs. Hemolysis of canine RBCs was undetectable at 1 × MIC and 2 × MIC concentrations; therefore, it can be safely used in further applications. These results indicate that heat and proteinase K hydrolyzed SYP is a very potent antifungal preparation against animal and human fungal pathogens and it can be used in future pharmaceuticals and functional foods.

Physicochemical, Mineral Content, Nutritional Composition and Phytochemical Properties of Careya Arborea

Background:: Roots, leaves, and bark of Careya arborea were evaluated for their physicochemical, mineral, nutritional, and phytochemical properties background: whereas the leaves had the highest acid insoluble ash value (1.4 mg/g), water-soluble ash value (2.31 mg/g), and moisture content value (10.42 mg/g) respectively. Mineral content was determined using ICP-AES and AAS methods. In the macro mineral composition, K (14.72 mg/100g), Ca (12.41 mg/100g) and Na (11.93 mg/100g) were found in the highest amounts. Objective:: The objective of this study was to explore Careya arborea roots, leaves, and bark as a nutritional, safe, and effective herbal medicine. objective: Careya arborea roots, leaves, and bark were characterized in terms of their Physico-chemical, mineral content, nutritional composition analysis, and phytochemical properties. Methods:: Stepwise physicochemical examinations, mineral content, nutritional composition, and quantitative phytochemical analysis were performed. Mineral content was determined using ICP-AES and AAS methods. Quantitative phytochemical properties were estimated on the basis of alkaloids, flavonoids, saponins, and tannins, respectively, using standard protocols. method: Mineral content was determined using ICP-AES and AAS methods. In the macro mineral composition, K (14.72 mg/100g), Ca (12.41 mg/100g) and Na (11.93 mg/100g) were found in the highest amounts. In contrast, Fe (22.82 mg/100g), Zn (8.68 mg/100g) and Cu (7.39 mg/100g) were found in the root section of C. arborea in trace mineral composition, Result:: The root had the highest water-soluble extractive value (20.7 mg/g), alcohol-soluble value (10.3 mg/g), foreign organic matter (3.4 mg/g), swelling index (4.8 mg/g), the bark had the highest total ash (12 mg/g), sulphated ash (9.49 mg/g), and leaves had the highest acid-insoluble value(1.4 mg/g), water-soluble value (2.31 mg/g), and moisture content (10.42 mg/g). Roots had higher macro-minerals and heavy metals than bark and leaves. The root contained the most carbohydrates (43.76 mg/100g), protein (14.81 mg/100g), and retinol (2.13 mg/100g), while the leaf had the most ascorbic acid (37.13 mg/100g), lutein (18.28 mg/100g), β-carotene (19.18 mg/100g), fat (7.83 mg/100g), and fibre (27.38 mg/100g). The leaves had the highest folate (61.23 μg/100g), and the root had the most calories (347.32 kcal). Qualitative phytochemical analysis of C. arborea found alkaloids, flavonoids, terpenoids, steroids, carbohydrates, protein, and phenol. In quantitative phytochemical analysis, the bark had higher alkaloid (6.32 mg/100g), tannin (7.53 mg/100g), flavonoid (7.83 mg/100g), and saponin (16.41 mg/100g) contents than C. arborea's root. Conclusion:: Hence, Careya arborea's physicochemical, mineral, nutritional, and phytochemical qualities present a potent herbal preparation and a safe, unique herbal remedy. other: None

A critical review on Gandhakadya malahara

Malahara is a potent pharmaceutical preparation for external application (Bahya Kalpana) which has Siktha Taila (mixture of sesame oil and bee-wax), Sathadhoutha Ghrita, Ghrita (ghee) as the base. It is an ointment preparation which includes herbal and mineral contents depending upon the usage. Mala-hara kalpanas are very much useful in skin disorders. Malahara has proper-ties like snehana (unctuousness), ropana (healing), lekhana (scrapping) and varnya (colouring) depending upon the drugs used in the preparation. A num-ber of Malahara Kalpanas have been mentioned in Rastarangini. Gandhakadhya Malahara is one among them mentioned in Gandhaka Vijnanam Tarangam. It is a herbo-mineral formulation comprises of Siktha taila (mixture of sesame oil and beeswax) as a base and Shudha Gandhaka (Purified Sulphur), Shudha Girisindura (Purified Mercuric Oxide), Shudha Tankana (Purified borax) are as other ingredients. Gandhakadhya malahara is intended for external application in various dermatological problems. It is specially indicated for severe Pama (a type of skin condition) as per Rasa-tarangini.

“Practice makes perfect” strategy for teaching aseptic techniques improved observational scores but not preparation potency

IntroductionStudent-compounded sterile preparations have been evaluated using observational scores, sterility testing, and potency determinations. Observational scores and potency determinations can be evaluated simultaneously, and three studies have been published using these assessment tools. One study found a significant number of students could not compound an acceptably potent preparation despite receiving very good observational scores. The previous study was judged to have an inferior instructional flaw, so a new teaching design, a “practice makes perfect” model, was utilized and was expected to increase the number of students compounding acceptably potent preparations. MethodsThe “practice makes perfect” method provided students with more practice and one-on-one instruction time in aseptic techniques. First-year pharmacy students received both group practice sessions and individualized instruction on six occasions interspersed between three compounding assessments. Observational scores and potency results were compared between this study and the previously published study. ResultsThe “practice makes perfect” strategy improved students' observational scores but showed inconsistent results in the percentage of students who compounded an acceptably potent preparation and in the potency of preparations compounded by all students. There was no correlation between observational scores and potency values or between observational scores and the percentage of students compounding acceptably potent preparations at each individual observational score. ConclusionsThe study demonstrated that there was either a systematic error in the analytical potency protocol or that the observations made during student compounding were not adequate to identify problems that led to poor potency.

Analytical Methods in Standardization of Bhasmas: A Review

Ayurveda the ancient science well known for its potential therapeutic effects with unique metallic, herbal juices/fruits in the treatment of chronic ailments. A well- known ayurvedic potent preparation, Bhasma is also known as ash which is a metallic base prepared by sophisticated pharmaceutical processes also plays a major role in acute, sub-acute, and chronic diseases. In order to determine its quality and purity to make sure the acceptability, the safety of the formulation standardization is very necessary. In this short review, an attempt has been made to present ancient methods to standardize physical characterstics like Verna, Nisvadutam, Nishchandratvam, Varitara, Unama, Rekhapurmatvam, Slakshmatvam..etc.,and chemical characterstics of bhasmas like Apurnabhavta, Niruttha, Amla Pariksha with advanced methods like SEM, TEM, and NPST, along with other natural and ancient analytical techniques.
 Keywords: Bhasmas, Standardization, Analytical methods, SEM, TEM.

Therapeutic Efficacy of Difluprednate 0.05% Versus Prednisolone Acetate 1% in Controlling Inflammation and Macular Oedema Following Phacoemulsification: An Optical Coherence Tomography-Based Study.

Background: Topical corticosteroids have been the cornerstone in the management of postoperative inflammation following cataract surgery. Due to potential side effects of the older topical steroids like prednisolone acetate and dexamethasone or betamethasone, newer potent steroids preparation like difluprednate, loteprednol or fluorometholone are now being used at lesser dose and frequency to control inflammation. There is scanty literature on the efficacy of these drugs in preventing inflammation and macular oedema in the Indian population.Purpose: The purpose of this study was to compare the efficacy of difluprednate 0.05% against prednisolone 1% eye drops for control of inflammation following phacoemulsification. The adverse effects of both drugs were also evaluated in this retrospective study.Methods: This retrospective cohort study included 181 patients operated for age-related cataracts by a single surgeon at a tertiary referral eye hospital between December 2018 and March 2019. Patients received either difluprednate 0.05% emulsion (n=90 eyes) or prednisolone acetate 1% (n=91 eyes) after phacoemulsification with the same brand intraocular lens (IOL) and same phaco machine. The topical medication was initiated one day postoperatively and continued for six weeks in tapering dosage. Pain score (Visual Analogue Scale, VAS), conjunctival hyperemia, anterior chamber (AC) cell grading, corneal oedema, central retinal thickness, subclinical cystoid macular oedema (SCME), intraocular pressures (IOP) and best-corrected visual acuity (BCVA) were examined after one week and six weeks of cataract extraction. Results: There was no statistically significant difference observed with regards to pain score (no pain in any patients after six weeks), conjunctival hyperemia (no hyperemia in any patients after six weeks), AC inflammation (no reaction in any patients), central retinal thickness (234.44 ± 35.75µ vs. 234.8 ± 34.99µ, p-value 0.946), SCME (16.67% vs. 13.19%, p-value 0.511), IOP (16.8 vs. 15.47 mmHg, p-value 0.101) and BCVA (BCVA 6/6 in 57.7% vs. 70.32%, p-value >0.05) between both groups. The mean change in IOP in both the groups at one week (0 ± 4.4 vs. 1.87 ± 3.54, p-value 0.0007) and six weeks (−0.01 ± 5.53 vs. 1.88 ± 4.01, p-value 0.004) was significant. Conclusion: Both the groups were equivalent with regards to their therapeutic efficacy in controlling postoperative inflammation and restoration of vision following phacoemulsification.

Soaking oro-pharyngeal pack with triamcinolone acetonide lowers discomfort in functional endoscopic sinus surgeries

background: Postoperative sore throat (POST) is defined as pain or discomfort in the throat following general anesthesia. Throat packs are used by many surgical subspecialties for different benifits, however they may increase the incidence of POST. Many interventions can be used to decrease incidence of POST. Triamcinolone acetonide (TA) is a moderately potent topical corticosteroid preparation. In this study, we hypothesized that soaking the throat pack with TA may decrease POST. Methods and Material: This prospective interventional comparative study was performed on 54 patients planned for Functional Endoscopic Sinus Surgeries (FEES) surgery. After endotracheal intubation, a standard length of oro-pharyngeal pack was placed, then patients were randomly allocated into: Group I: Oro-pharyngeal packs were soaked with 15 mg Triamcinolone acetonide 0.1% and Group II: packs were soaked with the same volume of lubricating gel (K-Y gel®). The patients were postoperatively asked about: sore throat, dysphagia, hoarseness of voice and nausea and vomiting. Results: Thirty minutes and 24 hours after extubation, Group I patients showed lower but statistically insignificant sore throat scores. Two to six hours after extubation, Group I showed a statistically significant reduction in sore throat scores. Six patients suffered dysphagia in group I compared with 8 patients in group II. Hoarseness of voice occurred in 1 patient in group I and 3 patients in group II. No patient complained of nausea or vomiting. Conclusión: Soaking oropharyngeal pack with triamcinolone acetonide in orabase gel was able to decrease POST in FESS patients.

Comparative Pharmacokinetics and Bioavailability of Epimedin C in Rat after Intramuscular Administration of Epimedin C, a Combination of Four Flavonoid Glycosides and Purified Herba Epimedii Extract.

Chuan-Ke-Zhi (CKZ), a purified Herba Epimedii extract, is a potent Chinese medicine preparation whose main bioactive components are a class of flavonoid glycosides such as epimedins A, B, and C and icariin. And epimedin C is far more abundant than other flavones in this extract. This study aims to investigate the pharmacokinetic and bioavailability of epimedin C and what effects, if any, other ingredients in CKZ have on its pharmacokinetics. Epimedin C, CKZ, and a combination of epimedins A, B, and C and icariin were, respectively, administrated to rats, and then the pharmacokinetic parameters of epimedin C in the three groups were calculated and compared. The result indicated that CLZ, MRT0–∞, and AUC0–∞ of epimedin C were significantly different among the three groups (P < 0.05), and compared with the epimedin C group, the absorption of epimedin C significantly increased in the CKZ group. Furthermore, in this study the absolute bioavailability of epimedin C was also investigated by comparing intramuscular and intravenous administration of epimedin C. As a result, epimedin C could be quickly absorbed with extremely high absolute bioavailability after intramuscular administration.

The activation of Epimedium polysaccharide-propolis flavone liposome on Kupffer cells

Epimedium polysaccharide-propolis flavone liposome (EPL), a potent immunological pharmaceutical preparation, was investigated for the immunomodulatory activity on Kupffer cells (KCs) in vitro. The results showed that EPL could significantly induce the secretion of chemokines (RANTES and MCP-1), promote the production of nitric oxide and induced nitric oxide synthase, improve the pinocytic and phagocytic activity of KCs, promote the mRNA expression of TNF-α and IL-1β, and enhance the expression of costimulatory molecules (CD11b and CD68) in KCs compared with Epimedium polysaccharide-propolis flavone (EP) at 30–7.5μg/mL. In addition, the abilities of KCs on stimulating lymphocytes proliferation and antigen presenting were significantly enhanced after stimulated with EPL compared with EP. These results suggested that EPL could activate KCs and possessed the stronger immunomodulatory effect, which provided the theoretical basis for further studying the mechanism of EPL on improving the immune response.

Efficacy of some colloidal silver preparations and silver salts against Proteus bacteria, one possible cause of rheumatoid arthritis

There has been increased interest in the role of anti-Proteus antibodies in the aetiology of rheumatoid arthritis (RA) and whether chemotherapeutic agents active against Proteus species might reduce the risk and/or exacerbations of RA. We examined the in vitro antibacterial effects of ten different silver preparations which were either ionic silver [Ag(I)] solutions or nanoparticulate silver (NPS) (Ag(0)) suspensions against ATCC and two wild (clinical) strains of Proteus. The data establish the low minimum inhibitory concentration and minimum bactericidal concentration of all the silver formulations tested against these four Proteus strains. In a pilot study, a potent NPS preparation ex vivo showed long-lasting anti-Proteus activity in a normal human volunteer.

Evaluation of Antitumor and Antioxidant Potential of a Polyherbal Extract on Ehrlich’s Ascites Carcinoma Xenografted Mice

Objective: Indigenous herbs alone or in combination are widely used in Indian system of medicine to treat innumerable ailments since time immemorial. Many strategies has been adopted to enhance anticarcinogenic responses and to establish therapeutic benefits. Poly herbal extracts (PHE), one of the emerging trends of modern medicine, where the assorted active principles work vibrantly to produce a maximum therapeutic activity with minimal toxicity by virtue of its additive, potentative, synergistic, agonistic or antagonistic effects. Though, Withania somnifera, Oroxylum indicum and Calotropis gigentia are independently established as potent antineoplastic agents, their antitumor and antioxidant perspective in combination is yet to be studied. The proposed study ascertains the assorted antineoplastic and antioxidant potential of the said potent herbs in PHE.Method: The antitumor potency of the PHE at a dose of 400 mg/kg body weight was screened on Ehrlich’s ascites carcinoma (EAC) xenografted swiss albino mice. The in-vivo anti-oxidant activity was investigated on the basis of hepatic anti-oxidant enzymes’ levels.Result: The PHE at the aforementioned dose showed a restoring effect on altered hematological parameters (***P&lt; 0.05 considered to be significant), down turn in ascitic tumor volume and increase in mean survival time. A significant improvement in biochemical parameters (Enzymic antioxidants) was too observed.Conclusion:The study epitomizes the PHE (400 mg/kg body weight) as a potent anti tumor and anti-oxidant preparation with synergistic effects on EAC bearing mice.

Abstract 5572: Breastin a natural product from Nerium Oleander exhibits high activity in a panel of human tumor cell lines.

Abstract Background: More than half of all registered anticancer agents were originally derived from natural sources. We isolated and screened &amp;gt;2.000 pure compounds, and purified extracts from microorganisms and plants in a panel of human tumor cell lines (Kelter et al. ENA 2008). Here we report on the activity of Breastin, a defined extract isolated from the plant Nerium Oleander in 63 human cell lines. The mode of action was elucidated by comparing the activity profile with that of known anticancer agents with defined mechanism. Methods: Breastin was isolated as cold extract from the leaves of the plant Nerium Oleander. It contains defined amounts of glycosides, flavonoides and polysaccharides. In-vitro activity was determined in 63 human tumor cell lines in a monolayer assay. 4 to 10,000 cells were seeded in 96 well plates; one day later Breastin was added at 5 concentrations and incubated with the cells for 4 days. The read-out was propidium iodide-based fluorescence. Based on IC50 and IC70 values tumor selectivity was analyzed. In the Compare Analysis the IC50 and IC70 pattern of Breastin was compared with the corresponding patterns of 180 known substances using Spearman Correlations. Results: Breastin showed a dose-dependent antitumor activity, the mean IC50 and IC70 were 1.1 and 2.7 μg/ml, respectively. It was the most potent and selective preparation out of a series of 36 extracts that were obtained with different extraction procedures. 31 / 63 cell lines investigated showed IC50 &amp;lt; 1.14 μg/ml. Breastin had a higher potency than several anticancer agents used in the clinic, e.g. Cisplatin, 5-Fluoruracil and Cyclophosphamide. The highest activity was seen in bladder, CNS, colon and NSC lung cancer cell lines as well as in pancreas and prostate models. In systematic combination studies Breastin increased the effect of the tubuline binders Paclitaxel, and Docetaxel in 4/6 cell lines, the alkylating agents Cyclophamide and Mitomycin, adriamycin and alimta. The Compare Analyses showed no similarity with 180 known anticancer agents, the coefficients of correlation were &amp;lt; 0.6 in all cases. Therefore Breastin has probably a different mechanism of action. In previous studies components of Breastin acted as specific inhibitors of the membrane Na+/K+ ATPase. This type of compounds is not included in the reference data base. Analyses of predictive biomarkers and gene patterns are ongoing. In former studies in-vivo activity was determined in murine models: B16 melanoma and Lewis-Lung-carcinoma were sensitive, leukemias L1210 and P388 were resistant. Conclusion: The evaluation of 36 extracts from Nerium Oleander identified the cold extract called Breastin as most promising anticancer agent with selective in-vitro activity found in bladder, CNS, colon and NSC lung cancer cell lines as well as in pancreas and prostate models. Moreover, in combination studies Breastin showed synergism with severall cytotoxic drugs. Citation Format: Heinz H. Fiebig, Gerhard Kelter, Armin Maier, Thomas Metz, Luay J. Rashan. Breastin a natural product from Nerium Oleander exhibits high activity in a panel of human tumor cell lines. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 5572. doi:10.1158/1538-7445.AM2013-5572

PREPARATION OF RASASINDURA BY MODIFIED PORTABLE VALUKAYANTRA VIS-À-VIS TRADITIONAL METHOD

Kupipakva Rasayana is the most potent preparation which is frequently used by Rasavaidyas. But traditional method of preparation of Kupipakva Rasayana seems to be quite complicated. Time duration, more manpower, more fu el , pollution and other obstacles add to negligence of its pre paration. T o overcome above obstacles, some alteration in the traditional method has been made without interfering concept behind the tradition. Rasasindura (Mercuric sulphide) was prepared by M odified portable Valukayantra vis - a - vis traditional method where detailed documentation of each and every step of procedure was done. To assess the quality of prepared medicine, both the samples were subjected to same Ayurvedic as well as modern parameters and results were interpreted. The study establishes efficacy and applicability of modified portable valukayantra in the preparation of Rasasindura (Mercuric sulphide).

Anti-Influenza Virus Activities of Commercial Oregano oils and their Carriers

Commercial Oregano oils with high concentrations of carvacrol have been vigorously promoted as antiviral agents effective against colds and ‘flu, including the pandemic H1N1 virus. However there seems to be no evidence to support these claims. Furthermore, since carvacrol itself is known to be toxic, so-called “carrier oils”, such as olive oil, have been included in formulations to ameliorate the potential toxic effects. We compared the antiinfluenza virus activity of several preparations, with and without “carriers”, and pure olive oil and carvacrol, by means of quantitative assays for H1N1 influenza virus, and for cytotoxicity in human lung epithelial cells. A range of concentrations was evaluated, including those relevant to consumer applications. All five Oregano oils showed significant antiviral activity, as did olive oil by itself, although their potencies were not comparable to a standardized preparation of Echinacea purpurea. Carvacrol was also very active, but it was also strongly cytotoxic. In addition all the Oregano oils were more cytotoxic than Echinacea purpurea. Thus certain commercial Oregano oils do possess anti-influenza virus activities, although these are less than a potent standardized Echinacea preparation, and furthermore the toxicity of the oils to lung epithelial cells, at doses relevant to consumer applications, is a limiting factor in their usefulness for oral applications.

A potent preparation method combining neutralization with microfluidization for rebamipide nanosuspensions and its in vivo evaluation

Backgrounds: Rebamipide (REB) is classified as a Biopharmaceutics Classification System (BCS) Class-IV compound with poor aqueous solubility and poor permeability. The local concentration in the mucosa makes REB exhibiting the therapeutic activities, and the strategy of increasing the dissolution rate has the possibility to improve the oral gastrointestinal (GI) distribution when using REB nanosuspensions.Objective: The purpose of this work was to prepare REB nanosuspensions (REB-NSs) by combining neutralization with microfluidization to improve its dissolution rate and orally pharmacokinetic properties.Methods: The feasibility of using acid-base neutralization and microfluidization to prepare REB-NSs was studied, and the preparation was optimized by central composite design (CCD). Physical states were characterized by using some technical methods, while the plasma drug concentration and GI distribution in rodents were determined.Results: The experimental results identified a formulation with 10 mg/mL REB, 0.9% (w/v) Lutrol F127, and 0.6% (w/v) Kollidon 90F. The dissolution rate of the dried REB-NSs was faster than that of Mucosta® tablets in different media, and the pharmacokinetic study showed a slight increase (1.3-fold and 1.1-fold) in the AUC0–12 h compared with unprocessed conventional suspensions (CSs) and solutions. Also, the GI distribution of REB-NSs improved compared with REB-CSs, and this would be preferable to assist in protecting GI mucosa.Conclusion: The REB-NSs prepared by the combining method exhibited a higher plasma drug concentration and superior GI distribution, thereby demonstrating positive results for preparing nanosuspensions of local effective BCS IV drugs with pH dependence such as REB by this method.

&lt;i&gt;Qidantongmai&lt;/i&gt; Protects Endothelial Cells Against Hypoxia-Induced Damage through Regulating the Serum VEGF-A Level

Qidantongmai (QDTM) is a Traditional Chinese Medicine (TCM) preparation that has long been used in folk medicine for the treatment of cardiovascular diseases. However, the underlying mechanisms are poorly understood. The present study was designed to determine the effects of QDTM on endothelial cells under hypoxic conditions both in vitro and in vivo. Primary human umbilical vein endothelial cells (HUVECs) were isolated, pretreated with QDTM medicated serum or saline control, and then cultured under hypoxia (2% oxygen) for 24 h. Sprague-Dawley rats were administered 1 ml/100 g of QDTM or saline twice a day for 4 days and treated with hypoxia (6 hours/day, discontinuous hypoxia, 360 mm Hg). QDTM not only protected HUVECs from hypoxia-induced damage by significantly retaining cell viability (P < 0.05) and decreasing apoptosis (P < 0.05) in vitro, but also protected liver endothelial cells from hypoxia-induced damage in vivo. Moreover, QDTM increased the serum VEGF-A level (P < 0.05) in rats treated with hypoxia for 7 days but suppressed the upregulation of serum VEGF-A in rats treated with hypoxia for 14 days. QDTM is a potent preparation that can protect endothelial cells against hypoxia-induced damage. The ability of QDTM to modulate the serum VEGF-A level may play an important role in its effects on endothelial cells.

Compound Cordyceps TCM-700C exhibits potent hepatoprotective capability in animal model

A herbal preparation “Compound Codyceps-TCM-700C (CC-700C)” was tested for hepatoprotective effect against the carbon tetrachloride induced liver damages in Sprague-Dawley rat model for a period of 6-weeks. Two dosage levels of CC-700C, respectively 286.2 mg/kg-bw (L-TCM) and 2862 mg/kg-bw (H-TCM), and a positive control Silymarin (Sigma) were used to compare their therapeutic effect. Both CC-700C's and Silymarin showed nontoxic in nature, as evidenced by body weight gain, organ weights and appearance including liver, spleen, and kidney. The activities of aspartate aminotransferase (AST) and alanine-aminotransferase (ALT) were more effectively suppressed by CC-700C than Silymarin. In addition, all levels of serum bilirubin, serum albumin, triglyceride (TG), total cholesterol (TC), platelet count (PLT), and prothombin time (PT) except TG were shown effectively restored to normal values by CC-700C and Silymarin. Moreover, although levels of glutathione (GSH), glutathione reductase (GSH-Rd), and superoxide dismutase (SOD) were equally maintained by these three preparations, glutathione peroxidase (GSH-Px) was suppressed only by H-TCM, and SOD only by Silymarin. In contrast, the activity of catalase efficiently recovered to control level on administration of CC-700C, being far better than Silymarin. Finally the liver collagen content, an indication of fibrosis, was also significantly suppressed by CC-700C, better effect was by L-TCM, but both levels were superior to Silymarin. Conclusively, the herbal preparation “Compound Cordyceps TCM-700C” is a potent hepatoprotective preparation. For therapeutic use, a dosage of 286.2 mg/kg-bw would be sufficiently effective.

Antimicrobial Property of a Herbal Preparation Containing Dalbergia Sissoo and Datura Stramonium with Cow Urine against Pathogenic Bacteria

In this study, a herbal preparation containing Dalbergia sissoo and Datura stramoium with cow urine (DSDS), was evaluated for its antibacterial potential against pathogenic strains of gram-positive (Staphylococcus aureus and Streptococcus pneumoniae) and gram-negative (Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae) bacteria. Antibacterial activity was compared to standard antibiotic drugs i.e. Chloramphenicol (30 mcg), Ampicillin (10 mcg), Nalidixic acid (10 mcg) and Rifampicin (30 mcg). Cow urine extract was found to be most active against both gram-positive as well as gram-negative bacteria. Clinical isolate of S. aureus showed higher sensitivity towards cow urine extract of DSDS than standard strains, and inhibited growth on most regulatory levels such as inhibition of protein, DNA, RNA and peptidoglycan synthesis. The results of the present study shows that the cow urine extract of DSDS may be used as a potent antiseptic preparation for prevention and treatment of chronic bacterial infections.

Bringing light to the dark side of insulin: a journey across the blood-brain barrier.

I think it's remarkable that only a few months after Banting introduced insulin to the world of diabetes, on the heels of one of medicine's greatest discoveries, Elliot Joslin wrote, “insulin is not a cure for diabetes, but a potent preparation alike . . . for evil and for good.” Today, 85 years later, with all the advances in insulin therapy, there is still a dark side to this potent preparation, and it is hypoglycemia. Hypoglycemia is the major barrier preventing insulin from achieving its full, therapeutic promise. My story begins 30 years ago. Bill Tamborlane came to me with a portable, battery-powered pump being used in pediatrics to infuse the iron-chelating drug desferrioxamine continuously via the subcutaneous route into children with thalassemia major. He hoped to use it to treat children with glycogen storage disease, a study we never performed. This relatively small pump, the Autosyringe Model AS2C, was at that time relatively unique. It had an “instant dose” button that allowed for bolus dose administration as well as the ability to deliver solutions continuously. In short, it was a “perfect” vehicle to infuse insulin in diabetes. Improved glucose control had been demonstrated earlier in the inpatient setting in type 1 diabetic patients given continuous intravenous insulin delivered at preprogrammed basal rates with increments before meals. Such systems were not practical outside of a controlled environment. This device, however, was small enough to be used for continuous subcutaneous insulin delivery. My enthusiasm for this idea was based on experiments Luigi Sacca and I performed 2 years earlier in the mid 1970s. We demonstrated that overnight basal insulin infusion in doses sufficient to normalize fasting glucose the next morning restored the ability of hyperglycemia to suppress hepatic glucose production in type 1 diabetic patients, despite their failure to release insulin …