Evaluation of antioxidant, photoprotective and antinociceptive activities of Marcetia macrophylla extract: potential for formulation of sunscreens

The antioxidant, photoprotective and antinociceptive Marcetia macrophylla active extract was investigated as an active ingredient in a sunscreen cream formulation. Thus, the M. macrophylla extract showed IC50 of 3.43 mg/ml of the antioxidant (DPPH∙ scavenging test) and Sun Protection Factor of 20.25 (SPF/UV-B, at 250 µg/ml) and UV-A of 78.09% (photobleaching trans-resveratrol test). The antinociceptive activity was superior to all standards tested using the in vivo acetic acid-induced writhing test (99.14% at the dose of 200 mg/kg) and the high-performance liquid chromatography coupled with diode array detector and mass spectroscopy multi-stage (HPLC-DAD-MS/MS) enabled the structural characterization of the quercetin-3-O-hexoside, quercetin-3-O-pentoside and quercetin-3-O-desoxihexoside. The pharmaceutical formulation containing the Marcetia macrophylla crude active extract was prepared and the physicochemical tests (organoleptic characteristics, pH analysis and centrifugation), the in vitro UVB (sun protection factor, SPF) and UVA (β-carotene) using the spectroscopic method were investigated. The formulation showed satisfactory results concerning the physicochemical parameters evaluated and active against the UV test. Thus, M. macrophylla showed biological activities with potential use in pharmaceutical preparations.

The Alternative Voltammetric Method for the Determination of Nicotine and Its Metabolite Nicotine N-Oxide

In the present paper, for the first time, the electrochemical behaviour of nicotine metabolite nicotine N-oxide (NNO) on static mercury dropping electrode (SMDE) and mercury meniscus modified silver solid amalgam electrode (m-AgSAE) has been reported. Nicotine N-oxide is reduced forming one peak at the potential -0.78 V on SDME and -0.86 V on m-AgSAE in Britton-Robinson buffer medium at pH 4.5 using cyclic voltammetry (CV). One electron and one proton take part in the reaction of NNO reduction. Calibration graphs for NNO determination using linear sweep voltammetry (LSV) on SDME and square-wave voltammetry (SWV) and differential pulse voltammetry (DPV) on m-AgSAE were obtained. Limit of detection (LOD) is 0.13 μM on SDME, and 0.16 μM (SWV) and 0.29 μM (DPV) on m-AgSAE. Since NNO can be used as an analytical form for nicotine voltammetric determination, so the developed methods were applied for the analysis of pharmaceutical preparations, and the recoveries from 97.3 to 104.6 % were achieved. Also, the elaborated methods were used in the analysis of biological fluids, and tobacco products. The obtained results were compared to those indicated in the certificates of drugs analysis, and to the results, obtained by reference methods (HPLC and GC).

AN EXPERIMENTAL DESIGN IN THE OPTIMIZATION OF VARIOUS TABLET EXCIPIENT FORMULATIONS = A CONCISE REVIEW

The use of an experimental design technique in the development of various pharmaceutical preparations, including tablet preparations, has become the latest trend. Because of their ease of use, tablet formulations are popular among both producers and patients. To increase the usage of tablets in diverse circles and settings, researchers are working to develop a variety of tablet excipients for various functions. Fast dissolving tablets (FDT), effervescent tablets, modified-release tablets, oral mucoadhesive tablets, gastroretentive tablets, and colon targeted tablets are some of the tablet formats that have been developed in addition to traditional tablets. This review will look at how formulation optimization in tablet preparations has been done during the previous ten years using specific literacies. The articles for this review were found using the keywords tablet, excipient, matrices, formulation, and QBD in specialized databases such as Elsevier, Pubmed, and Cambridge. Other options include Springer publications, material from the Internet, and articles published online by The Lancet Respiratory Medicine, Medscape, and Statpearls. The formulation design strategy is based on the experimental design approach carried out on the kind of tablet preparation, which has distinct important quality parameters.

Qualitative and Quantitative Analysis of Phenolic Compounds in Spray-Dried Olive Mill Wastewater

The processing of olives for oil production generates the most abundant agro-industrial by-products in the Mediterranean area. The three-phase olive oil extraction process requires the addition of a large amount of water to the system, which is difficult to dispose of for its load of toxic pollutants. On the other hand, olive mill wastewater is a rich source of bioactive substances with various biological properties that can be used as ingredients in the food industry for obtaining functional and nutraceutical foods as well as in the pharmaceutical industry. In this study, we present the results relative to the phenolic compounds detected in dried olive mill wastewaters obtained using a spray dryer. Qualitative and quantitative analyses were obtained by high-pressure liquid chromatography–tandem mass spectrometry (HPLC–MS/MS). In particular, the compounds here discussed are: apigenin (9.55 mg/kg dry weight), caffeic acid (2.89 mg/kg dry weight), catecol (6.12 mg/kg dry weight), p-cumaric acid (5.01 mg/kg dry weight), diosmetin (3.58 mg/kg dry weight), hydroxytyrosol (1.481 mg/kg dry weight), hydroxytyrosyl oleate (564 mg/kg dry weight), luteolin (62.38 mg/kg dry weight), luteolin-7-O-glucoside (88.55 mg/kg dry weight), luteolin-4-O-glucoside (11.48 mg/kg dry weight), oleuropein (103 mg/kg dry weight), rutin (48.52 mg/kg dry weight), tyrosol (2043 mg/kg dry weight), vanillin (27.70 mg/kg dry weight), and verbascoside (700 mg/kg dry weight). The results obtained highlighted that the use of dehumidified air as a drying medium, with the addition of maltodextrin, appears to be an effective way to produce a phenol-rich powder to be included in food formulations as well as in pharmaceutical preparations having different biological properties.

Bioactivity and Mycochemical Profile of Extracts from Mycelial Cultures of Ganoderma spp.

Fungal mycelium cultures are an alternative to natural sources in order to obtain valuable research materials. They also enable constant control and adaptation of the process, thereby leading to increased biomass growth and accumulation of bioactive metabolites. The present study aims to assess the biosynthetic potential of mycelial cultures of six Ganoderma species: G. adspersum, G. applanatum, G. carnosum, G. lucidum, G. pfeifferi, and G. resinaceum. The presence of phenolic acids, amino acids, indole compounds, sterols, and kojic acid in biomass extracts was determined by HPLC. The antioxidant and cytotoxic activities of the extracts and their effects on the inhibition of selected enzymes (tyrosinase and acetylcholinesterase) were also evaluated. The total content of phenolic acids in the extracts ranged from 5.8 (G. carnosum) to 114.07 mg/100 g dry weight (d.w.) (G. pfeifferi). The total content of indole compounds in the extracts ranged from 3.03 (G. carnosum) to 11.56 mg/100 g d.w. (G. lucidum) and that of ergosterol ranged from 28.15 (G. applanatum) to 74.78 mg/100 g d.w. (G. adspersum). Kojic acid was found in the extracts of G. applanatum and G. lucidum. The tested extracts showed significant antioxidant activity. The results suggest that the analyzed mycelial cultures are promising candidates for the development of new dietary supplements or pharmaceutical preparations.

Development of Immediate Release Tablets Containing Calcium Lactate Synthetized from Black Sea Mussel Shells

Nowadays, the use of marine by-products as precursor materials has gained great interest in the extraction and production of chemical compounds with suitable properties and possible pharmaceutical applications. The present paper presents the development of a new immediate release tablet containing calcium lactate obtained from Black Sea mussel shells. Compared with other calcium salts, calcium lactate has good solubility and bioavailability. In the pharmaceutical preparations, calcium lactate was extensively utilized as a calcium source for preventing and treating calcium deficiencies. The physical and chemical characteristics of synthesized calcium lactate were evaluated using Fourier Transform Infrared Spectroscopy, X-ray diffraction analysis and thermal analysis. Further, the various pharmacotechnical properties of the calcium lactate obtained from mussel shells were determined in comparison with an industrial used direct compressible Calcium lactate DC (PURACAL®). The obtained results suggest that mussel shell by-products are suitable for the development of chemical compounds with potential applications in the pharmaceutical domain.

Crude Extract of Terminalia Chebula Fruit Effect on Gastro Intestinal Disorders Using Different Animal Models

Terminalia chebula is an ancient medicinal herb. it is also known as Haritaki, Yellow myrobalan, Chebulic myrobalan, Yellow myrobalan, and Terminalia chebulabe longs to Combretaceae family is a major Ayurvedic medicine that is native to South Asia, predominantly from India. Apart from Ayurveda, it is commonly used in Unani and Homeopathic medicine systems. Because of the broad variety of pharmacological activities connected with the biologically active constitutents found throughout this herb, it is included in conventional medicine. The fruit contains main pharmacological activities such as Hepatoprotective activity, Cytoprotective activity Cardioprotective activity, Antidiabetic and renoprotective activity, Antibacterial activity, Antifungal activity, Antiviral activity, Antiprotozoal activity, Anti-inflammatory and anti-arthritic activity, antioxidant and free radical scavenging activity, Anticarcinogenic activity, Antimutagenic, radioprotective and Chemopreventive activity, Hypolipidemic and hypocholesterolemic activity, Adaptogenic and anti anaphylactic activities, Gastrointestinal motility improving and anti-ulcerogenic activity, Antispasmodic activity, Wound healing activity, Anticaries activity, Immunomodulatory activity any many are reported with scientific evidence. All these ancient applications of Terminalia chebula as home remedies have been confirmed in preclinical trials. The current evidence on the effect of Terminalia chebula intake or consumption on gastrointestinal disorders and diseases is scientifically based on preclinical and clinical trials. All these ancient applications of Terminalia chebula as home remedies have been confirmed in preclinical trials. The current evidence on the effect of Terminalia chebula intake or consumption on gastrointestinal disorders and diseases is scientifically based on preclinical and clinical trials. Study indicates different dosage of Terminalia chebula is effective to get relief from gastrointestinal troubles. Due to less number of gastrointestinal studies, there is no scientific report to consume a specific amount of dose. To prove that Terminalia chebula and its standard extracts are effective as a gastroprotective agent, more comprehensive preclinical and clinical trials are required. To reliably evaluate the appropriate dosages for specific disorders and preparation of extract of Terminalia chebula fruit in prospective human trials procedures, dose-finding preclinical studies should be conducted. There is an evident need for more patient and physician education concerning specific therapies, legislation to regulate the quality of pharmaceutical preparations, and, in particular, more clinical and pre-clinical trials to determine the value and safety of such medicaments in digestive and other disorders.

Kaolin in pharmaceutical preparations: a review

Background: Kaolin is a clay mineral with Al2Si2O5(OH)4 structure which can be found in sedimentary rocks also known as clay stones. Kaolin consists of clay materials such as quartz, illite, smectite, and hematite, with the largest constituent component being kaolinite. Kaolin is one of the most common minerals with an abundant presence in the earth's crust compared to other minerals, especially in Indonesia. In the pharmaceutical sector, this clay mineral is widely used in Indonesia. Kaolin is known to be a good adsorbent and has good physical, chemical, and surface physicochemical properties. Objective: This review article aims to provide information about the uses of kaolin in the pharmaceutical industry. Methods: This review article was written by conducting a literature search study method in the PubMed, ScienceDirect, and Google Scholar databases. Results: In the pharmaceutical field, kaolin is used as an excipient in various types of medicinal preparations, one of which is as a suspension agent because of its ability to stabilize suspensions in a deflocculated state as an emulsifying agent, crushing agent, filling agent, and drug carrier. As an active substance, kaolin is widely used because it has a therapeutic activity. In the cosmetic industry, kaolin can be administered in a variety of topical dosage forms which act as skin protective agents or sunscreens. Conclusion: Based on the results of the review, it was found that kaolin, with its abundant presence on earth and its great potential in the pharmaceutical field, is used as an active medicinal substance, excipient ingredient, and in the cosmetic field as a sunscreen. Keywords: Kaolin, excipient, active pharmaceutical ingredient, cosmetics

CHARACTERISTICS AND SUBSTANTIATION OF THE USE OF PELLETS AS A MODERN DOSAGE FORM ON THE MARKET OF UKRAINE

currently, omeprazole pellets are one of the most common pellet formulations on the pharmaceutical market of Ukraine (Gorobets, Matyash, Pekhenko & Barna, 2019). This medication is available in capsule form. Pellets are multi particular dosage forms that have several advantages over monoparticular dosage forms; therefore, pellets are promising oral delivery systems for active pharmaceutical ingredients (APIs). Pellets are used when the stability of the active substance changes with fluctuations in the pH of the environment, when irritation of the gastric mucosa is possible, to facilitate swallowing (especially important for patients with dysphagia, elderly patients, and children). When using polymers in the shell, it is possible to regulate the release in a certain part of the gastrointestinal tract, this allows you to get a point pharmacological effect. In addition, pellets can be of different sizes (from 0.1 to 2 mm), because of their shape, pellets exhibit abrasion resistance and are more fluid. Omeprazole is a synthetic substance. The active ingredient suppresses gastric acid secretion. In refers to the pharmaceutical group of proton pump inhibitors, it prescribes drugs in this group to treat active duodenal ulcers, gastric ulcers, gastro-oesophageal reflux disease (GERD), severe erosive esophagitis, pathological hypersecretory conditions, for example, Zollinger Ellison syndrome. Among the most commonly used methods for the production of pellets are: stage-by-stage spraying of solutions or suspensions (the second name is stage-by-stage layering); direct pelletization (the second name is extrusion-spheronization); spray drying and spray cooling of melts; agglomeration-spheronization. Unfortunately, at the moment, none of the Ukrainian manufacturers is manufactured enteric pellets on their own (they buy ready-made pellets), while there are medicines of both foreign and Ukrainian origin on the domestic market. The article contains an overview of pharmaceutical preparations as pellets, systematization of information on production methods, a review of omeprazole drugs as pellets, presented on the pharmaceutical market of Ukraine. The purpose of this study was to summarize the cases when the use of such a form as pellets is the most reasonable; make an overview of medicines in Ukraine containing pellets; summarize modern methods of pellet production.

Mussel Shells, a Valuable Calcium Resource for the Pharmaceutical Industry

(1) Background: The mussel (Mytilus edulis, Mytilus galloprovincialis) is the most widespread lamellibranch mollusk, being fished on all coasts of the European seas. Mussels are also widely grown in Japan, China, and Spain, especially for food purposes. This paper shows an original technique for mussel shell processing for preparation of calcium salts, such as calcium levulinate. This process involves synthesis of calcium levulinate by treatment of Mytilus galloprovincialis shells with levulinic acid. The advantage of mussel shell utilization results in more straightforward qualitative composition. Thus, the weight of the mineral component lies with calcium carbonate, which can be used for extraction of pharmaceutical preparations. (2) Methods: Shell powder was first deproteinized by calcination, then the mineral part was treated with levulinic acid. The problem of shells generally resulting from the industrialization of marine molluscs creates enough shortcomings, if one only mentions storage and handling. One of the solutions proposed by us is the capitalization of calcium from shells in the pharmaceutical industry. (3) Results: The toxicity of calcium levulinate synthesized from the mussel shells was evaluated by the method known in the scientific literature as the Constantinescu phytobiological method (using wheat kernels, Triticum vulgare Mill). Acute toxicity of calcium levulinate was evaluated; the experiments showed the low toxicity of calcium levulinate. (4) Conclusion: The experimental results highlighted calcium as the predominant element in the composition of mussel shells, which strengthens the argument of capitalizing the shells as an important natural source of calcium.