The embodiment of the strategy of “using active chemicals as excipients” in compound preparation
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Excipient
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Excipients are inactive substances that are included in pharmaceutical formulations alongside active ingredients. These substances are added to pharmaceutical products for various purposes, including improving stability, enhancing bioavailability, aiding in the manufacturing process, enhancing the appearance or taste, and facilitating administration or delivery of the active ingredient. We summarized a recent study published in science. This work suggests a systematic method to identify such active “inactive ingredients,” including the detection of allergenic and immunogenic properties. The examined excipient activity by combining large-scale computational screening with targeted experimental testing. They identified 38 excipients with activities against 44 targets. Although most excipients deserve their status as inert, many approved excipients may directly modulate physiologically relevant targets. This review increases our understanding of the relationship between drug excipients and active sites and provides more comprehensive theoretical support for future excipient selection.
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Excipients form a major component of pharmaceutical formulations and are classified as any ingredient other than the active ingredient which is included within the product formulation to improve drug product performance. Functional uses of excipients include improving solubility and stability, safety and efficacy, as bulking agents in lyophilized formulations, tonicity agents, and aiding in controlled or prolonged drug delivery. Parenteral formulations are sterile, pyrogen-free; free of particulate matter and by-pass the body's natural defense mechanisms. Excipients may demonstrate a synergistic effect when combined with an active ingredient but may also lead to unwanted reactions with the drugs and packaging components. Ideal excipients are required to be considered safe, inert and multifunctional. Contrary to the past, safety of excipients needs to be well established in order for their use in the pharmaceutical formulations. Therefore, careful consideration should be given while selecting an excipient. This review article provides an overview of the excipients used exclusively in small molecule and biological parenteral products including solutions, suspensions, and lyophilized formulations, information on the possible drug-excipient and drug-packaging interactions and the regulatory requirements for the use of pharmaceutical excipients. The readers will be able to have a comprehensive understanding of the excipients used in parenteral formulations.
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The extraction method has a great influence on the yield, quality, chemical structure, and biological activities of active ingredients. Safe and efficient extraction of active ingredients is one of the important problems facing the food and pharmaceutical industry. As a pretreatment approach for the extraction of active ingredients, dynamic high pressure microfluidization (DHPM) is a promising strategy that can not only effectively increase the yield of active ingredients but also strengthen the bioactivities of active ingredients, and take the advantages of mild operating temperature and environmental friendliness. In this review, the research progress of DHPM-assisted extraction of active ingredients from plant materials in recent ten years is overviewed. The DHPM equipment, strengthening mechanism, operating procedure, critical factors and application of DHPM-assisted extraction are introduced in detail, together with the advantages and disadvantages. Furthermore, its future development trend is discussed at the end. DHPM-assisted extraction is considered as the ideal technique of better homogenization effects, less solvent consumption, more reliable operation, and so on, making it a promising method to acquire active ingredients efficiently. Therefore, this technique is worthy of further theoretical research and experimental operation.
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Acne vulgaris is one of the most prevalent dermatological diseases. Proper cosmetic treatment can significantly improve the condition. When choosing an active ingredient for a cosmetic product, it is important to evaluate the cost-effectiveness ratio. The aim of this study was to perform a cost-effective analysis of selected cosmetic complexes for the treatment of acne in order to make the right choice when developing a new cosmetic product. Bulgarian and foreign literature was searched to select active cosmetic complexes. For the analysis, four active complexes (A, B, C and D) were selected for which an in vitro efficacy test was performed - inhibition of 5α-reductase. The results from the cost-effectiveness analysis showed that the active complex B dominated over the remaining complexes in respect of the cost-effectiveness ratio. Complex C was superior to active complexes D and A. Active complex D is dominated byactive complex A. Active complex B, which is an osmotic gel with oleanolic acid from olive leaf and nordihydroguaiaretic acid, could be considered as a cost-effective alternative in the choice of an active ingredient when developing a cosmetic product.
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The stability - indicating method is an analytical procedure used to detect a decrease in the amount of an active pharmaceutical ingredient present due to degradation. According to FDA guidelines, stability - indicating method is defined as a validated analytical procedure that accurately and precisely measures active ingredients free from potential interferences like degradation products, process impurities, excipient or other potential impurities. During stability studies, liquid chromatography is used routinely to separate and determine the analyses of interest. For implementing the stability - indicating method, several steps are needed. An active pharmaceutical substance is firstly subjected to the forced degradation studies followed with the investigations of its interactions with the excipient from the pharmaceutical preparation, the optimization of chromatographic conditions and the method validation.
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Fast Dissolving/Disintegrating Dosage Forms (FDDFs) are a group of dosage forms which dissolve or disintegrate quickly, leading to fast distribution of active ingredients at the site of administration; thereby providing ease of oral ingestion of solid unit dosage forms and have the potential to enhance transmucosal absorption. With time, the use of FDDFs in alternative systems has significantly increased. Homeopathic systems and traditional Chinese medicine have embraced FDDFs for the delivery of active compounds. Most of the patents in this area are from China or by the Chinese innovators. In Europe and US, FDDFs have been extensively studied for the delivery of natural active compounds. It was fascinating to know that some new dosage forms and new routes of delivering active compounds are also making their way to the family of FDDFs. The dose of active compound, size of dosage forms, standardization of extracts, polyherbal mixtures, stability of active compounds, safety, efficacy and pharmacokinetics are challenging issues for developing FDDF herbal formulations or phytopharmaceuticals.
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Studies on stability of active ingredients are fundamental and critical for the rational development of Traditional Chinese Medicine (TCM) in view of its modernization and worldwide use. The stability of both active and marker constituents of plants used in TCM is reviewed for the first time. More than 100 papers, mostly written in Chinese, have been reviewed. Studies concerning plant constituents were analyzed according to their chemical classification of active ingredients. In addition, several crude drugs of animal origin are also reported. Stability of active ingredients is summarized during extraction and/or storage of the herbal drug preparations, and under stress conditions (pH, temperature, solvents, light, and humidity) and in the presence of preservatives, antioxidants, and metals.
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