Crude Drug Research Articles

Validation of a Novel Supercritical Fluid Extractor/Dryer Combo Instrument.

The current pharmaceutical manufacturing scenario involves different techniques for the processing of materials. For example, the extraction unit is one of the essential aspects of plant-based pharmaceuticals. Recently, various kinds of extraction techniques have been used for analytical and preparative scales; among them, a supercritical fluid extractor (SCFE) is the most widely used technique for extraction. It is used for an extensive range of crude drugs and can be possible with the help of SCFE by varying temperature/pressure. Notably, it uses carbon dioxide (CO2) for extraction instead of other solvents. Simultaneously, lyophilization is an important technique used at different processing steps along with other methods. In lyophilization, CO2 is used as a cooling agent in the shelves of lyophilized equipment. It behaves as a supercritical fluid at critical pressure (Pc) of 72.7 atm and critical temperature (Tc) of 31°C. Considering the criteria mentioned earlier, there is a possibility that liquid CO2 or supercritical carbon dioxide (SC-CO2) can be used as a cooling agent in a lyophilizer and extraction solvent in SCFE. This review presents a brief outline for the possible validation parameters of the proposed novel processor; that is, SCFE/Dryer combo instrument containing Design Qualification, Installation Qualification, Operational Qualification, and Performance Qualification.

A Preliminary Phytochemical, Pharmacognostic and Physicochemical Evaluation of Endemic Thymus spathulifolius (Lamiaceae)

Aim of study: The members of the genus Thymus are widely used in Turkey as herbal teas, spices and salads for different purpose and the herbs of Thymus spathulifolius are reported to have medicinal value. Therefore, in this study various pharmacognostic parameters, physicochemical properties and anatomical characters of Thymus spathulifolius Hausskn. & Velen., is a medicinal plant and endemic to Turkey, were investigated. Area of study: T. spathulifolius was dried and stored according to herbarium techniques in the Herbarium of Pharmacy Faculty, Trakya University, collected from Sivas, Turkey. Material and methods: The total ash, moisture content, and physicochemical tests on the different extracts obtained from the endemic T. spathulifolius aerial parts collected from Sivas province were determined according to the World Health Organization (WHO) standards for crude drugs. Main results: The moisture content and total ash amount of the drug obtained from this plant is in accordance with the WHO standards. Phytochemical screening for secondary metabolites showed the presence of carbohydrates, antraquinone glycosides, steroids, flavonoids and coumarins, while other phytochemicals such as alkaloids and saponins were absent. Besides, the cross-sections of root, stem and leaf were examined and detailed. The total ash value was found as 7.36 ± 0.21% and acid insoluble ash was 0.14 ± 0.72%. Highlights: The present study provided important information for correct authentication and standardization of this plant material.

Optimization of the Epimedii Folium Mutton-Oil Processing Technology and Testing Its Effect on Zebrafish Embryonic Development.

As a traditional Chinese medicine (TCM), Epimedii folium (EF) has a history in medicine and food that is > 2,000 years old. Clinically, EF processed with mutton oil is often used as a medicine. In recent years, reports of safety risks and adverse reactions of products that use EF as a raw material have gradually increased. Processing can effectively improve the safety of TCM. According to TCM theory, mutton-oil processing can reduce the toxicity of EF and enhance its tonifying effect on the kidneys. However, there is a lack of systematic research and evaluation of EF mutton-oil processing technology. In this study, we used the Box-Behnken experimental design-response surface methodology to optimize the key parameters of the processing technology by assessing the contents of multiple components. The results showed that the optimal mutton-oil processing technology of EF was as follows: heating the mutton oil at 120 °C ± 10 °C, adding the crude EF, stir-frying it gently to 189 °C ± 10 °C until it is evenly shiny, and then removing it and cool. For every 100 kg of EF, 15 kg of mutton oil should be used. The toxicities and teratogenicities of an aqueous extract of crude and mutton-oil processed EF were compared in a zebrafish embryo developmental model. The results showed that the crude herb group was more likely to cause zebrafish deformities, and its half-maximal lethal EF concentration was lower. In conclusion, the optimized mutton-oil processing technology was stable and reliable, with good repeatability. At a certain dose, the aqueous extract of EF was toxic to the development of zebrafish embryos, and the toxicity was stronger for the crude drug than for the processed drug. The results showed that mutton-oil processing reduced the toxicity of crude EF. These findings can be used to improve the quality, uniformity, and clinical safety of mutton oil-processed EF.

Pharmacokinetic study about compatibility of Eucommia ulmoides and Psoralea corylifolia

ObjectiveThe compatibility of Eucommia ulmoides (Eu) and Psoralea corylifolia (Pc) on the pharmacokinetic (PK) properties in the rat was explored in this study. MethodsEu extract, Pc extract and the combined extracts (crude drug ratio was 2:1) was administered by gavage, respectively. Two PK experiments were conducted. In first one, the blood samples were collected via the occuli chorioideae vein to get the PK properties of the components. In second one, the blood samples were simultaneously collected via the internal jugular vein or portal vein at different time points and the concentrations of target ingredients were detected by LC/MS/MS to clear the location where the interaction of Eu and Pc took place in vivo. ResultsEight of 11 ingredients in Eu and Pc extract were determined in rat plasma. The exposure levels of geniposidic acid (GPA), aucubin (AU), geniposide (GP), pinoresinol diglucoside (PDG), psoralen glycosides (PLG) and isopsoralen glycosides (IPLG) were decreased 1/5–2/3 after administration of combined extracts. Comparing to the combined administration, the exposure of GPA and AU in plasma of single Eu administration collected via the portal vein were decreased 1/3–2/3, and the values of AUC0-24h and AUC0-∞ of GP collected from the portal vein or internal jugular vein were double increased. The other components’ parameters were not significantly changed. ConclusionIn summary, the Pc and Eu combined administration could affect the exposure of the main components of Eu extract in rats due to the changed intestinal absorption. The research on the compatibility of Pc and Eu was helpful to guide the clinical administration of Eu and Pc simultaneously.

Zhuyeqing liquor promotes longevity through enhancing stress resistance via regulation of SKN-1 and HSF-1 transcription factors in Caenorhabditis elegans

Zhuyeqing liquor (ZYQL) is well-known traditional functional liquor in China that contains twelve crude drugs. Studies have shown that ZYQL has many beneficial effects, but its anti-aging effect has not been reported. Here, we found that ZYQL had excellent antioxidant activity in vitro. In C. elegans, ZYQL could significantly extend the lifespan, and decreased aging related phenotype including accumulation of lipofuscin and the decrease of food intake and motility. Further, ZYQL significantly reduced ROS level and enhanced the antioxidant defense in C. elegans. ZYQL increased transcriptional activity of transcription factors HSF-1 and SKN-1, and ZYQL-mediated longevity was dependent on these factors. Taken together, the data suggested that ZYQL enhanced the transcriptional activity of transcription factors HSF-1 and SKN-1, which in turn increased oxidative/heat stress resistance to exert its anti-aging effect in C. elegans. Our results provide new insights into the beneficial effects and underlying mechanisms of ZYQL, which might be useful for further developing ZYQL into health or anti-aging beverages.

Ethnopharmacological Study of Medicinal Plants Used in the Treatment of Skin Burns in the Arab World.

Traditional healers are often practiced in rural areas owing to cultural beliefs and are known to provide various forms of healthcare and home remedies. Patients in the Mediterranean region rely on traditional medicine to cure a variety of health concerns, like skin burns. This study was conducted to identify the various practices used by traditional healers for treating skin burns. The survey was conducted in 18 Arab countries, including Syria, Iraq, Jordan, Saudi Arabia, Egypt, United Arab Emirates, Algeria, Bahrain, Palestine, Kuwait, Oman, Qatar, Lebanon, Yemen, Tunisia, Oman, Morocco, and Sudan. Between September 2020 and July 2021, an online questionnaire was administered to 7530 participants from 12 Asian and 5 African countries. The survey was designed to gather information from common medicinal plant users and herbalists on their practices as specialists in using various herbal and medicinal plant products for diagnosis and treatment. Among the participants, 2260 had a scientific background in plant application, and the study included one phytotherapeutic professional. The crude-extraction technique was favored, by Arabic folk, for plant preparation over the maceration and decoction method. Olive oil was the most commonly used product among participants as an anti-inflammation and for scar reduction. Aloe vera, olive oil, sesame, Ceretonia siliqua, lavender, potato, cucumber, shea butter, and wheat flour are used as crude drugs to reduce pain because of their analgesic and cooling effects. The present study is the first database of medicinal plants with burn-healing properties conducted in Arab countries. These plants can be employed in the search for new bioactive substances through pharmacochemical investigations, as well as in the development of new formulations containing a combination of these plants.

Comparison of ephedrine and pseudoephedrine contents in 34 Kampo extracts containing Ephedrae Herba used clinically in Japan.

Ephedrae Herba is among the important crude drugs prescribed in Kampo medicine for the treatment of cold, flue, rhinitis, nasal congestion, cough, and asthma. The active ingredients of Ephedrae Herba, ephedrine (E) and pseudoephedrine (PE), are potent sympathomimetic compounds that stimulate α-, β1-, and β2-adrenoceptors resulting in dilatation and alleviation of nasal mucosal hyperemia. Hypertension, palpitations, insomnia, and dysuria are the main adverse effects of E and PE, which can be avoided by determining the actual contents of these alkaloids in Kampo extracts containing Ephedrae Herba. However, the extraction efficiencies of E and PE from Ephedrae Herba contained in Kampo formulas in combination with other crude drugs remain unknown. Therefore, we comprehensively determined the E and PE contents of 34 Kampo extracts containing Ephedrae Herba used clinically in Japan. The E and PE contents per daily dosage in Kampo extracts were generally proportional to the compounding amount of Ephedrae Herba. In contrast, the extraction efficiencies of E or PE were not constant and not influenced by the pH of the extracts. We assume that the extraction efficiencies of E and PE may be independently affected by other constituent crude drugs. Thus, it is necessary to investigate the cause and mechanism in the future. In conclusion, these results show that the E and PE content of each Kampo formulation can be estimated from the compounding amount of Ephedrae Herba. Therefore, the amount of Ephedrae Herba should be carefully considered to ensure the safe use of Kampo formulations containing Ephedrae Herba.

Yunpi Qushi Jiangzhuo Recipe Alleviates Lipid Deposition and Reduces Liver Damage in Mice with Non-alcoholic Fatty Liver Disease

Non-alcoholic fatty liver disease (NAFLD) is a multifactorial liver metabolic disease, which affects nearly a quarter of the world's population. Yunpi Qushi Jiangzhuo Recipe (QSJZR) is a traditional Chinese medicine compound, which is composed of Amomum kravanh Pierre ex Gagnep, Coix lacryma-jobi L.var.ma-yuen (Roman.) Stapf, Prunus armeniac a L.var.ansu Maxim, Salvia miltiorrhiza Bge, Nelumbo nucifera Gaertn, Alisma plantago-aquatica Linn, Polyporus umbellatus ( Pers.) Fries, Poria cocos ( Schw.) Wolf, and Artemisia capillaris Thunb. QSJZR has a certain therapeutic effect on NAFLD patients, but its specific mechanism is not clear. To investigate the effect of QSJZR on high-fat diet (HFD)-fed NAFLD mice and its mechanism. Twenty-four SPF female C57BL/6J mice (21.0±0.5 g) were randomly divided into normal diet group, HFD group and QSJZR group. ND group was given basal diet, while the other two groups were given HFD. Meanwhile, each mouse in QSJZR group was given 0.2 mL/day (containing 2.27g crude drug per mL) QSJZR, ND group and HFD group were given the same amount of normal saline for 13 consecutive weeks. Then, the serum was collected for biochemical assay, and the liver was removed for pathological examination and biochemical analysis. Body weight and white fat weight of the HFD-induced NAFLD mice significantly decreased after ministration with QSJZR, while liver weight had no significant change. QSJZR also significantly reduced liver and serum triglyceride levels, and alleviated hepatocyte lipid deposition by regulating genes and proteins expression related to lipid metabolism, including AMPK, SREBP1C, CPT1A and ACC. In addition, compared with HFD group, liver malondialdehyde (MDA) content was lower in QSJZR group, while glutathione peroxidase (GPx) content was higher. Serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were lower in QSJZR group than those in HFD group. Treatment with QSJZR significantly alleviated liver injury by increasing BCL2/BAX protein ratio and down-regulating ASK1/JNK pathway. Administration of QSJZR to NAFLD mice once daily for 13 weeks can decrease lipid levels, and alleviate liver damage. These results suggest that QSJZR might be used to treat NAFLD, although more studies need to be conducted for further verification. Yunpi Qushi Jiangzhuo Recipe (QSJZR) is a traditional Chinese medicine compound QSJZR. It reduces fatty liver and reduces liver damage by inhibiting lipogenesis and promoting lipid oxidation, providing a beneficial effect in the HFD-induced NAFLD mouse model.

System optimization and validation to improve thin-layer chromatography of roselle calyces (Hibiscus sabdariffa L.) required by the Indonesian Herbal Pharmacopoeia Edition II

Context: Roselle (Hibiscus sabdariffa L.) is one of the traditional crude drugs monographed in the Indonesian Herbal Pharmacopoeia Edition II (IHP II). As per IHP II requirements, a TLC pattern should be used in its authentication. However, the TLC system described for this purpose does not produce a clear reference chromatogram, often leading to inconclusive results. Aims: To develop and validate TLC systems of H. sabdariffa calyces for a better-quality chromatogram than those listed in the IHP II, thereby facilitating crude drugs authentication. Methods: To optimize TLC for H. sabdariffa, sixteen systems, differing in stationary phase, mobile phase composition, and/or visualization reagent were tested. The TLC system was then validated using several parameters such as analyte stability during chromatography, analyte stability in the extract solution and on the TLC plate, stability of the derivatization result, and precision on a plate as well as intermediate precision. Results: Two systems (I and II) were successfully designed and applied to evaluate H. sabdariffa quality. System I used Si gel 60 F254 for the stationary phase, ethyl acetate-formic acid-glacial acetic acid-water (100:11:11:2) for the mobile phase, H. sabdariffa’s ethanol extract (5%, 20 µL) for the test solution, cyanidin 3-O-glucoside (100 ppm, 4 µL) as a reference, no derivatization, and detection with visible light. System II combined Si gel 60 F254 for the stationary phase, ethyl acetate-formic acid-glacial acetic acid-toluene-water (80:11:11:20:19), H. sabdariffa’s ethanol extract (5%, 20 µL) for the test solution, chlorogenic acid (1000 ppm, 2 µL) and caffeic acid (50 ppm, 2 µL) as references, the visualizing reagent NP/PEG, and investigation under 366 nm UV light. Conclusions: Both systems are simple but have good stability and precision, thus facilitating H. sabdariffa calyx authentication and paving the way for developing content analysis methods for H. sabdariffa markers.

Phytochemical Screening, Antibacterial, Antifungal, Anti-Biofilm and Antioxidant Activity of Azadiracta Indica A. Juss. Flowers.

The present study involves investigation of Azadiracta Indica flowers with respect to its pharmacognostic properties, phytochemical screening, and its application as anti-oxidant, anti-biofilm, and anti-microbial agent. The Pharmacognostic characteristics were evaluated with respect to moisture content, total ash content, acid, and water-soluble ash content, swelling index, foaming index, and metal content. The macro and micronutrient content of the crude drug was estimated by AAS and Flame photometric methods and it gives the quantitative estimation of minerals, where calcium is present in abundance (88.64 mg/L). Soxhlet extraction was carried out in the increasing order of polarity of the solvent viz Petroleum Ether (PE), Acetone (AC), and Hydroalcohol (20 %) (HA) to extract the bioactive compounds. The characterization of the bioactive compounds of all the three extract have been carried out using gcms and lcms. The presence of 13 major compounds have been identified in PE extract and 8 compounds in AC extract using gcms studies. The HA extract is found to contain polyphenols, flavanoids, and glycosides. The antioxidant activity of the extracts was evaluated by DPPH, FRAP, and Phosphomolybdenum assay. This reveals that HA extract shows good scavenging activity than PE and AC extracts which is well correlated with the bioactive compounds, especially phenols which are present as a major component in the extract. The anti-microbial activity was investigated via Agar well diffusion method for all the extracts. Among all the extracts HA extract shows good antibacterial activity with MIC of 25 μg/mL and AC extract shows good anti-fungal activity with MIC of 25 μg/mL. The antibiofilm assay confirms that the HA extract shows good biofilm inhibition about 94 % among other extracts when tested on human pathogens. The results confirm that the HA extract of A. Indica flowers will be an excellent source of natural anti-oxidant and also antimicrobial agents. This paves the way for its potential uses in herbal product formulation.

Characterization and quantification of chemical constituents in Angong Niuhuang Pill using ultra-high performance liquid chromatography tandem mass spectrometry

Material basis researches and quality evaluation of traditional Chinese medicine preparations (TCMPs) face great challenges due to the complex composition and abundant unexpected interference. Angong Niuhuang Pill (ANP), one of the most famous TCMPs in China, containing 11 crude drugs has been commonly used for the treatment of febrile diseases. However, previous literatures of comprehensive chemical constituents in ANP were still limited. Herein, Ultra-high performance liquid chromatography-ion mobility-quadrupole time-of-flight mass spectrometry (UHPLC-IM-QTOF MS) method was established to effectively recognize the chemicals in Angong Niuhuang Pill (ANP). A total of 205 compounds, containing 72 confirmed with reference standards, were characterized from ANP with the application of a systematic strategy integrated polygonal mass defect filtering (MDF) and diagnostic fragment ion filtering (DFIF)/neutral loss filtering (NLF). Additionally, 68 major constituents in 8 batches of ANP samples were simultaneously determined by ultra-performance liquid chromatography-triple quadrupole tandem mass spectrometry (UPLC-QQQ MS/MS) within 40 min. The quantitative method was validated regarding linearity, precision, repeatability, stability, and accuracy. These findings proved the established liquid chromatography-mass spectrometry (LC-MS) method was efficient and dependable for qualitative and quantitative chemical profiling of ANP. Besides, this research could provide the material basis for further pharmacological researches and quality control of ANP.

Profiling aromatic constituents of Chimonanthus nitens Oliv. leaf granule using mass spectrometry.

The chemical constituents of Chinese patent medicine are usually different from those of crude medicine because of specific preparation processes. Chimonanthus nitens Oliv. leaf granule is widely used for prevention against COVID-19 in China. However, no research has been reported on the chemical constituents of the granule and their variation during the preparation process. Fragmentation patterns of reference compounds were investigated using electrospray ionization mass spectrometry, and the new gas-phase reaction wasdemonstrated by electronic and steric effects and calculated chemistry. Then, a strategy based on new fragmentation patterns was used to profile aromatic constituents. In addition, based on untargeted metabolomics analytical workflow, a comparison was made on the chemical constituents of the leaf and granule. New fragmentation patterns related to two competing reactions, ring-opening and ring-closing reactions for coumarin, have been proposed and investigated in depth. The newly established diagnostic ion at m/z 81.0331 worked strongly in the assignment of OH-7 and substituent at C-8 of coumarin. McLafferty rearrangement occurring in coumarin glycoside whilesugar grouplocating at C-4 was first observed, and new diagnostic ions at m/z 147.0440, 119.0488, and 91.0543wereconstructed. Aromatic constituents of the granule were first profiled. A total of 114 aromatic compounds were identified; of these 85 compounds were identified first. Kaempferol-7-O-neohesperidoside and its homologues were mostly enriched in the granule. Considering their reported bioactivities, these analogues possibly contribute greatly to clinical efficacy. Our results provided a new fragmentation theory for coumarins and a new material basis for the quality control of the granule.

Kampo herbal ointments for skin wound healing.

The management of skin wound healing problems is a public health issue in which traditional herbal medicines could play a determining role. Kampo medicine, with three traditionally used ointments, provides interesting solutions for these dermatological issues. These ointments named Shiunkō, Chuōkō, and Shinsen taitsukō all have in common a lipophilic base of sesame oil and beeswax from which herbal crude drugs are extracted according to several possible manufacturing protocols. This review article brings together existing data on metabolites involved in the complex wound healing process. Among them are representatives of the botanical genera Angelica, Lithospermum, Curcuma, Phellodendron, Paeonia, Rheum, Rehmannia, Scrophularia, or Cinnamomum. Kampo provides numerous metabolites of interest, whose content in crude drugs is very sensitive to different biotic and abiotic factors and to the different extraction protocols used for these ointments. If Kampo medicine is known for its singular standardization, ointments are not well known, and research on these lipophilic formulas has not been developed due to the analytical difficulties encountered in biological and metabolomic analysis. Further research considering the complexities of these unique herbal ointments could contribute to a rationalization of Kampo's therapeutic uses for wound healing.

Comparative Pharmacognostic and Powder Microscopic Studies of the Bark of Four Ficus Species (Nalpamaram)

Nalpamaram is widely used in traditional Ayurvedic system for the treatment of several ailments. It is very effective for the treatment of skin diseases like pigmentation, wrinkles and dark circles. This has a brown texture and a unique aroma. Nalpamaram is a mixture of four plant species of the family Moraceae - Ficus religiosa (Asvattha), Ficus benghalensis (Nyagrodha), Ficus racemosa (Udumbara) and Ficus microcarpa (Plaksah). The barks of the species are usually interchanged or adulterated with other species of Ficus because of the limited knowledge in identification and differentiation. Therefore, a detailed comparative pharmacognostic evaluation of the four species has been carried out with the aim to establish the diagnostic keys of these important drugs based on the pharmacognostic and powder macroscopic profiles. Pharmacognostic study of all these shows differences in values. Total ash is low in F. racemosa and high in F. benghalensis Acid insoluble ash is low in F. benghalensis and high in F. racemosa. Water soluble extractive is low in F. benghalensis and high in F. racemosa. Alcohol soluble extractive is low in F. benghalensis and high in F. racemosa. Unique identification features like stone cells and prismatic crystals of calcium oxalate were found in the powder of all four species. The information from the present study provide data which is useful for the development of suitable monograph, determining the quality and purity of a crude drug and laying down Pharmacopoeia standards for Nalpamaram.

Integrative Medicine in the Treatment of COVID-19: An Indian Perspective

Background: Over recent years, evidence-based modern medicine has overshadowed the use and efficacy of natural and traditional medicines. However, in the wake of the pandemic, the interest in the quest for therapeutic resources linked to traditional, complementary, and integrative medicine has substantially increased. This has further facilitated the research and development of potential therapeutic crude drugs or their formulations in the management of COVID-19 and the symptoms associated with the latter. This article attempts to provide a comprehensive review of the various traditional medicines used as integrative medicines in alleviating symptoms attributed to the COVID-19 infection. Methods: The literature was thoroughly browsed for recent research articles, systematic reviews, case studies, and review articles on ScienceDirect, PubMed, and Google Scholar using keywords like complementary medicine, alternative medicine, and holistic approach to enlist a few. Subsequently, they were thoroughly screened to include only recent studies and evidence. Additionally, the official guidelines published by the Government and other regulatory bodies were also sought to be included in the article. Study Design: The review article follows the narrative literature review method. However, the primary data was skimmed for relevance and only recent shreds of evidence, pertinent to the review were included. Results: The review elucidated the pharmacological activity of various treatment regimens in different systems of medicine, with available supportive clinical evidence. Additionally, it also underscored the importance of holistic health interventions, and how these traditional and integrative systems of medicine cater to the same. Conclusions: The recent evidence presents a broad-spectrum effect of these therapeutic interventions, primarily in the fields of mental health, mild to moderate, and even severe forms of the infection, employing various pharmacological pathways. These studies primarily include studies and statistics pertaining to the SARS-CoV-2 (Severe Acute Respiratory Syndrome Corona Virus 2) but may include supporting evidence from other respiratory viruses. This information may prove imperative in guiding new research, and also to design and support an integrative treatment regimen. Conclusively, any suspicion pertaining to the COVID-19 infection should be sought by following the protocols recommended by the concerned health authorities of the respective region/country.

Extraction and identification of bioactive compound embelin from embelia ribes fruits

Embelia ribes is the most widely used plant in numerous Ayurvedic preparations to treat various disorders. The most commonly used plant parts like leaves and fruit are in the Indian traditional system for CNS (Central Nervous System) disease, Anti-bacterial Anthelmintic, and Anti-ulcer activity. The proposed work aimed to optimize different extraction parameters (Part of Crude drug, Solvent and Temperature) to increase the extraction yield of the Embelin from Embelia ribes fruits. Extraction was done by using Chloroform as a solvent, and extraction yield was optimized by using independent variables, such as solvent, drug parts, time and temperature, with the help of the design of expert software. One part of the crude drug kept in 3 parts of Chloroform for 34 mins at 49 oC temperature gives the maximum yield (38.73±1.13%) of Embelin. HPTLC was done by using the mobile phase of Chloroform: Ethyl acetate: Formic acid (5:4:0.5 v/v/v). A single band appeared in the TLC plate exhibiting the Isolation of a Single compound, further the Isolated compound was identified and characterized by using Ultraviolet Spectroscopy (UV), Fourier Transform Infra-Red (FTIR), and Nuclear Magnetic Resonance Spectroscopy (NMR). The results obtained from the analytical techniques reveal that the Isolated compound was Embelin.

The preparation and relative bioavailability of an artemisin in self-emulsifying drug delivery system

The aim of this study is to demonstrate a method for improving the solubility and relative bioavailability of artemisinin using a self-emulsifying drug delivery system (SEDDS). The self-emulsifying drug load, solubility, and emulsifying time were used as the evaluation indices, based on a solubility test and a ternary phase diagram. Optimal Mixture Design in Design-Expert software was used to optimize the prescription of the artemisinin SEDDS. By determining the water distribution coefficient in vitro, combined with the drug concentration–time curve in vivo, a comparison was made of the relative oral bioavailability of the artemisinin SEDDS and the crude drug. The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the artemisinin SEDDS was 0.5:0.2:0.3 (wt/wt/wt), with a drug loading capacity of 41.556 mg/g, a solubility of 1.997 mg/mL, and a self-emulsification time of 214 s. The optimal prescription was transparent, slightly yellow, and oil-like. The average loading capacity of artemisinin was 41.912 mg/g, the emulsification time was 231 s, the average particle size was 128.0 nm, the average Zeta potential was –4.29 mV, and the solubility of artemisinin SEDDS in water was 1.997 mg mL–1. It is 33.85 times of the solubility of artemisinin in water, which achieves the purpose of increasing the solubility of artemisinin. The comparison of the oil/water distribution coefficient of the artemisinin SEDDS with that of the crude drug in vitro showed that SEDDS could improve the permeability of artemisinin and promote the absorption in vivo, and the relative bioavailability of the SEDDS agent was at least 1.47 times higher than that of the crude drug. The artemisinin SEDDS could significantly improve the solubility and relative bioavailability of artemisinin.

FORMULATION AND EVALUATION OF HERBAL CREAM

The aim of the present study was to formulate and evaluate the herbal cream having properties of moistening, nourishing, anti-acne and antiinflammatory effect on the skin using different crude drugs like Azadirachta indica (Neem), Aloe barbadensis (Aloe Vera), Ocimum tenuiflorum (Tulsi). The cream was prepared by using the cream base i.e. bee’s wax, liquid paraffin, borax, methyl paraben, distilled water, rose oil, Aloe Vera gel, aqueous extract of neem and tulsi. The cream was prepared by homogeneous mixing of all the excipients and the herbal extract. By using this method, we have prepared six batches F1, F2, F3, F4, F5, and F6. Formulations were evaluated for different parameters like physical evaluation, irritancy study observation, wash ability, spread ability, PH, Viscosity, phase separation, greasiness observations, dye test, homogeneity, acid value, saponification value. All the six formulations F1, F2, F3, F4, F5, and F6 showed good appearance, PH, adequate viscosity and no phase separation was observed. All the six formulations F1, F2, F3, F4, F5, and F6 were stable and can be safely use on the skin.

Quantitative Differences in Alkaloids, the Ingredients for Crude Drug, and Other Useful Compounds in <i>Uncaria rhynchophylla</i> among Various Tissue Parts

Quantitative Differences in Alkaloids, the Ingredients for Crude Drug, and Other Useful Compounds in <i>Uncaria rhynchophylla</i> among Various Tissue Parts

Inhibitory effect of extracts of hainosan (painongsan) and its constituent crude drugs on production of monocyte chemoattractant protein‐1 and interleukin‐6 in murine fibroblasts treated with Porphyromonas gingivalis

AbstractAimHainosan (painongsan), composed of Platycodon grandiflorum root (PG), Paeonia lactiflora root (PL), and Citrus aurantium immature fruit (AF), is a formula used in traditional Japanese (Kampo) and Chinese medicine to treat purulent diseases, including gingivitis. In this study, we investigated the anti‐inflammatory effects of hainosan extract (HNS) using both traditional direct and serum pharmacological techniques.MethodsBALB/c mice were orally treated with HNS or extracts of its constituent crude drugs for one week. Murine RCB2767 fibroblasts were incubated with a medium containing heat‐killed Porphyromonas gingivalis and HNS, extracts of the constituent crude drugs, or serum samples collected from mice orally treated with these extracts. The monocyte chemoattractant protein 1 (MCP‐1) and interleukin (IL)‐6 in the medium were measured by enzyme‐linked immunosorbent assay (ELISA). The effect of HNS and its constituent crude drugs on the proliferative potential of fibroblasts was evaluated by radioisotope‐labeled thymidine uptake capacity.ResultsThe concentrations of MCP‐1 and IL‐6 in the culture supernatants were significantly increased by treatment with heat‐killed bacteria. In addition, PG and PL extracts significantly inhibited MCP‐1 and IL‐6 production. Furthermore, supplementation of serum samples from mice orally treated with the extracts to the culture medium resulted in significant inhibition of induction of these cytokines. HNS, extracts of PG, PL and AF, and serum samples collected from mice treated with these extracts significantly augmented 3H‐thymidine uptake in fibroblasts.ConclusionOur results demonstrated that HNS has anti‐inflammatory effects in murine fibroblasts and that PL and PG could contribute to the effects of hainosan.