Conversion of traditional Chinese medicine (TCM) into nanomedicine:application of theory of unification of medicines and excipients / 中国中药杂志

In recent years, the use of active substances as excipients or as substitutes for other excipients in the design of modern drug delivery systems has received widespread attention, which has promoted the development of the theory of unification of medicines and excipients in the design of traditional Chinese medicine(TCM) preparations. Adopting the theory of unification of medicines and excipients to design drug delivery systems can reduce the use of excipients and thus the cost of preparations, reduce drug toxicity, increase drug solubility and biocompatibility, enhance synergistic effect, and realize targeted delivery and simultaneous delivery of multiple components. However, the research on the application of this theory in the modern drug delivery system of TCM preparations is still insufficient, with few relevant articles. In addition, the TCM active substances that can be used as the excipients remain to be catalogued. In this paper, we review the types and applications of the drug delivery systems with TCM active substances as excipients and describe their common construction methods and mechanisms, aiming to provide references for the in-depth research on the modern drug delivery systems for TCM preparations.

Characterization of the critical quality attributes for hydroxypropyl methylcellulose with different sources and analysis of the release of sustained-release tablets in vitro / 药学学报

The quality difference of pharmaceutical excipients from different sources affects the molding properties of the powder, resulting in changes in the properties of the final product. In this study, the critical quality attributes of hydroxypropyl methylcellulose (HPMC) with different specifications from two manufacturers (manufacturer A and manufacturer B) were characterized including particle size, physical morphology, viscosity and powder physical quality attributes. Aminophylline, diclofenac sodium, and metformin hydrochloride were utilized as model drugs with different solubility to prepare sustained-release tablets, and the effect of HPMC from different sources on drug release of sustained-release tablets in vitro was investigated. The results showed that HPMC with the same viscosity specification from different sources had outstanding differences in the physicochemical properties (including particle size, physical morphology, viscosity, dimension, compressibility and powder flow), which could change the hardness and friability of the sustained-release tablets. The differences in the physicochemical properties of HPMC had different effects on the dissolution of different sustained-release tablets in vitro. It had no significant effect on the release of easily soluble aminophylline and metformin hydrochloride, but had a greater impact on the release of poorly soluble diclofenac sodium. Compared with manufacturer A, the sustained-release effect of matrix tablets prepared by HPMC from manufacturer B was more excellent. The results of this study will provide a theoretical reference on selecting the appropriate excipients for formulation design.

Research progress on new dosage forms of progesterone and its preparation methods / 药学学报

Progesterone is currently the first-line drug for the treatment and prevention of threatened abortion and habitual abortion. With the gradual liberalization of China's childbirth policy, the number of elderly parturients has increased significantly. As a result, the market demand for progesterone and the individual requirements have been continuously improved. Clinical studies have found that the indications of progesterone are not limited to gynecological diseases, but can also be used for the treatment of renal colic, traumatic brain injury and other diseases. Existing progesterone preparations include oral capsules, intramuscular injections, vaginal gels, etc., but they can no longer meet the current market situation and the increase of indications. Improving existing preparations, developing new preparations, and opening up new routes of administration have become one of the directions of progesterone drug research. This article will review the research progress of new dosage forms in existing administration, new routes of administration and related preparation methods of progesterone.

Application Characteristics of Prescription Preparations for External Use in Chinese pharmacopoeia 2020 Edition / 中国实验方剂学杂志

ObjectiveTo analyze the clinical application characteristics of prescription preparations for external use in the Chinese pharmacopoeia 2020 edition （hereafter abbreviated as the Pharmacopoeia）. MethodThe topical functions， usage， dosage， dosage form， application method， and prescription of the preparations for external use in the Pharmacopoeia were analyzed. ResultThe Chinese pharmacopoeia 2020 edition includes a total of 138 prescription preparations for external use， the specific clinical usage， dosage， administration method， and efficacy evaluation of which remain unclear. These preparations can be used to treat a wide range of diseases. Specifically， the use in orthopedics and traumatology （36 preparations， accounting for 26.09%） is dominant， followed by that in internal medicine， surgery， and throat. The major application method is directly applying to the diseased area （35 preparations， 25.36%）. The main dosage forms are ointment （40 preparations， 28.99%） and powder （24 preparations， 17.39%） and others include liniments， suppositories， tinctures， and sprays. The clinical usage and dosage of these preparations are mostly unclear. Only 48 preparations （34.78%） are recorded with clear dosage and frequency of use， and 45 preparations （32.61%） have neither clear dosage nor frequency of use. The 138 prescription preparations for external use include 211 single medicines， of which 44 single medicines can be used alone. The single medicines are mostly used for heat clearing （48 preparations， 22.75%）. ConclusionThe Chinese pharmacopoeia 2020 edition （Volume I） records a large number of prescription preparations for external use， and the number shows an increasing trend. However， the usage， dosage， and efficacy evaluation criteria of these preparations remain to be improved and need in-depth research.

Comparison of Serum 25-Hydroxyvitamin D Levels After A Single Oral Dose of Vitamin D3 Formulations in Mild Vitamin D3 Deficiency

Objective:To compare the levels of serum 25 Hydroxyvitamin D levels after a single large oral dose (60,000 IU) of different vitamin D3 formulations. Materials and Methods: Ninety?one volunteers with mild vitamin D deficiency (18–29 ng/ml) were selected and randomly assigned to three parallel groups. Groups-I received liquid, Group-II received sachet, and Group-III received tablet formulation of cholecalciferol as a single dose of 60,000 IU orally after 8–10 h of overnight fasting. Serum 25(OH) D concentrations were measured at baseline, 24 h, 7 days, and 14 days after drug administration. Various hematology and biochemical parameters were also assessed for baseline safety evaluation. Results: Baseline serum 25(OH) D concentrations in Groups I (liquid), II (sachet), and III (tablet) was 24.75 ± 4.77 ng/mL, 23.25 ± 4.15 ng/mL, and 23.18 ± 5.52 ng/mL, respectively. After supplemented with three formulations, only tablet group after 24 h showed increase in serum 25-OH-D concentration of 8.07 units from its baseline. Whereas after 7th day, no significant difference in absorption was observed but after 14 th day, all three groups showed increase in serum 25-OH-D concentration, in which tablet group (50.10 ± 94.99 ng/ml) showed highest increase in absorption (26.92 units) from their baseline values. During intergroup comparison between three formulations at the time of investigation, only liquid group after 24 h showed increased serum concentration by P values (0.03, 0.02) as compared to sachet and tablet group. However, After 7th and 14th day, there was no statistically difference was observed between three groups. Conclusion: Single oral dose of 60,000 IU dose of vitamin D liquid formulation has higher absorption value as after 24 h and tablet formulation showed higher absorption after 7th days. In emergency paucity of vitamin D, these observations findings can have critical conclusions to state the suitable dietary formulation of vitamin D.

Are the release characteristics of Erzhi pills in line with traditional Chinese medicine theory? A quantitative study / 中西医结合学报

OBJECTIVE@#Traditional Chinese medicine (TCM) has been widely used throughout China to prevent and cure diseases for thousands of years, and now it is a part of the integrative medicine field that is available in Western societies. To ensure the safety and quality of the herbal medicines that are a major part of the TCM tradition, they must be held to modern pharmaceutical standards. Erzhi pill (EZP) is a Chinese Pharmacopeia-listed herbal preparation that is used in the long-term clinical management of post-menopausal symptoms, osteoporosis and menstrual disorders. Until now, whether the drug release mechanism of EZP is in line with its intended TCM usage has not been studied.@*METHODS@#The release of specnuezhenide from three EZPs (self-made, Leiyunshang and Renhe) in simulated gastric fluid (SGF), acetate buffer (pH 4.5 buffer) and simulated intestinal fluid (SIF) was investigated in a dissolution test. The water uptake capacity and erosion extent of the three EZPs were investigated using swelling and erosion studies. The drug release mechanism was further assessed through statistical model fitting, using DDSolver software.@*RESULTS@#The release of specnuezhenide from all three EZPs in SGF was less than 50% within a 4 h period. However, over 70% of the specnuezhenide was released from each EZP in both pH 4.5 buffer and SIF in the same time. Analysis of the swelling and erosion behaviors and the drug release mechanism of the three EZPs confirmed that the release rate from EZP followed a sustained release profile, which was an interactive combination of swelling and erosion.@*CONCLUSION@#This study showed that the release pattern from the pills was in line with the intended TCM use of EZP. TCM had not only theoretically considered sustained release from the pills, but also formulated them to achieve this release pattern. When establishing quality control standards for pills, the theoretical TCM usage and the actual release patterns need to be considered.

The Design And Development Of Carvedilol Gastroretentive Floating Drug Delivery Systems Using Hydrophilic Polymers And In Vitro Characterization

Objective: The primary aim of the present examination was to create carvedilol phosphate floating tablets using factorial designs and for retention in the upper portion of the gastrointestinal (GI) tract to sustain the dissolution where the solubility of carvedilol phosphate is more in an acidic medium. Methods: The floating tablets of carvedilol phosphate were ready to employ different concentrations and a combination of these polymers of Na-alginate, Carbopol 934P, and sodium carboxymethyl cellulose (NaCMC) with lubricants magnesium stearate by direct compression technique. In the present experiment, involved sodium bicarbonate and citric acid as a gas-producing agent. Fifteen formulations structured and judged for pre-compression components like the angle of repose, bulk and tapped density, Hausner’s ratio, compressibility index, and post-compression factors are weight uniformity, hardness, drug content, friability, in vitro buoyancy, dissolution studies, and Fourier transforms infrared spectroscopy (FTIR). Results: The drug released 90.02% in 12 h by combining NaCMC (7.5 mg) and Na-alginate (7.5 mg) in the formulation F14 towards the achievement of sustained release. Batch F14 selected as optimized, as provided desired zero-order release profile as well as floating lag time 20 s and total floating time>12 h, and the mechanism of drug release observed (n = 1.098, super case-II transport). Conclusion: From the results fulfilled that all the preparation found to be within the pharmacopeia limits and was the best dosage form to treat moderate heart failure and hypertension. The in vitro dissolution profiles of all formulations placed into various kinetic models, the statistical parameters like slope, regression coefficient and intercept determined. The gastro-retentive dosage form to maintain the sustain drug delivery, which would improve the maximum therapeutic efficacy and patient compliance.

Dosage form and specification analysis on electrolytes and antipyretic analgesics in 2018 National Essential Medicines List / 药学实践杂志

Objective To provide data reference for improving the selection criteria of the dosage forms and specifications of the electrolytes and antipyretic analgesics in the Essential Medicines List, and to improve the applicability of these medicines to children and the availability of essential medicines. Methods The market and prices of electrolytes and antipyretic analgesics were retrieved by the system. The data were processed by Excel software, and the different dosage forms were compared and analyzed. Results 8 medication classes were included for adjusting water, electrolytes and acid-base balance, and another 16 classes were analgesic, antipyretic, anti-inflammatory, anti-rheumatic and anti-gout drugs. Those medications were characterized with many registered approval numbers, manufacturers and some considerations for pediatric uses. The proper prices were given for different dosage forms and specifications. There is a room for improvement regarding the specifications of potassium, glucose injections, and acetaminophen preparations. Conclusion The selection of pharmaceutical dosage forms and specifications in the Essential Medicines List should be comprehensively evaluated from the registered approval numbers of base medicines, the manufacturers and related prices in pharmaceutical procurement platforms from various provinces, and the clinical needs for special populations. It is recommended that 10 ml: 1 g potassium chloride injection, 50 ml glucose injection，acetaminophen suppositories and drops were included in the Essential Medicines List.

Historical Evolution of "Formula" and "Preparation" of Zixue as One of Three Classic Antipyretic Preparations / 中国实验方剂学杂志

Zixue was first recorded in detail in Qianjin Yifang, and practitioners of later generations renamed it as Zixuesan and Zixuedan, which is the representative prescription of antipyretic preparations and has high clinical application and research value. At present, there have been many studies on the pharmacological effect and clinical application of Zixue, but the medical books of the past dynasties have slightly different records on Zixue, which has brought some difficulties to the reasonable clinical application and research of this prescription. In addition to the introduction of Zixuesan, which is different from the ancient recipe, the researchers have questions about which development method can reasonably inherit and develop the classical preparation. The authors intend to summarize the historical evolution of "formula" and "preparation" of Zixue, in order to clarify its historical context, which can provide a reference for the modern research and development of this formula, and provide a new ideas for the in-depth exploration of other classic preparations.

Analysis on Application of Salviae Miltiorrhizae Radix et Rhizoma Related Health Food / 中国实验方剂学杂志

With the improvement of living standard and enhancement of health consciousness, Salviae Miltiorrhizae Radix et Rhizoma, as a common medicinal material that can be widely used in health food, is focused an increasing number of scholars′ attention at home and abroad. Based on Salviae Miltiorrhizae Radix et Rhizoma health food published by the food website of National Medical Products Administration (NMPA), this paper combs and analyzes their dosage forms, functional components, health-care functions and prescriptions of traditional Chinese medicine (TCM). Meanwhile, the Apriori algorithm module in SPSS Modeler 15.0 is used to explore the formulation rules of Salviae Miltiorrhizae Radix et Rhizoma health food. The results showed that capsules was the most common (about 55.34%), and the infusions and beverages were rare. In the aspect of health-care function, it is mainly used to auxiliary hypolipidemic, auxiliary protective function to chemical liver injury, enhance immunity and dispel chloasma. Among 92 cases of the health food with auxiliary hypolipidemic, the common combination of TCM was Salviae Miltiorrhizae Radix et Rhizoma-Gynostemmatis Pentaphylli Herba-Puerariae Lobatae Radix. Among 55 cases of the health food with auxiliary protective function to chemical liver injury, the common combination of TCM was Salviae Miltiorrhizae Radix et Rhizoma-Puerariae Lobatae Radix-Schisandrae Chinensis Fructus. Among 54 cases of the health food with immune-enhancing, the common combination of TCM was Salviae Miltiorrhizae Radix et Rhizoma-Astragali Radix-Lycii Fructus. Among 46 cases of the health food with dispelling chloasma, the common combination of TCM was Salviae Miltiorrhizae Radix et Rhizoma-Angelicae Sinensis Radix-grape seeds. The selection of prescription compatibility of Salviae Miltiorrhizae Radix et Rhizoma health food with different health-care functions is basically consistent with the TCM treatment with syndrome differentiation theory and modern medical theory. This article interprets the application of Salviae Miltiorrhizae Radix et Rhizoma health food from the perspective of dosage forms, functional components, health-care functions and compatibility of prescriptions, which can provide a basis and reference for precise and efficient research and development of this kind of health food.

Development and Revision of Dosage Forms General Chapters of Chinese Pharmacopeia 2020 Edition Volume / 中国药学杂志

OBJECTIVE: To guide pharmaceutical manufacturing to pay full attention to and implement the quality control and overall requirements of preparation production based on the analysis of the revision work and major changes of the Dosage Forms General Chapters of the 2020 edition of the Chinese Pharmacopoeia. METHODSE: This article mainly introduces the compilation progress of the Dosage Forms General Chapters of the 2020 edition of the Chinese Pharmacopoeia. RESULTS: The analysis is helpful to improve the integrity, advancement and readability of the Dosage Forms General Chapters of the 2020 edition of the Chinese Pharmacopoeia. CONCLUSION: The improvement of the Dosage Forms General Chapters of the 2020 edition of the Chinese Pharmacopoeia will play an important role in improving the overall level of Chinese pharmacopoeia standards, strengthening drug quality control and improving drug quality.

In vitro comparison test for chemical solid oral generic drugs administered by nasogastric tubes / 国际药学研究杂志

At present, the dosage and administration items in the marketing instructions of some oral solid brand drugs approved in China include related contents for administration via nasogastric tube. In order to achieve consistency with the original drugs in quality and efficacy, the generic drugs investigators should confirm whether the generic drugs and the original drugs have the same in vitro characteristics under the conditions of administration by nasogastric tube. The purpose is to eliminate the clinical risks brought by the way of administration. This article summarizes the experimental design and evaluation points for the in vitro comparative study of the solid oral generic drugs which can be administered by nasogastric tube, while referring to the individual drug guidelines issued by FDA and the related literature published, so as to provide a reference for the technical system construction for the consistency evaluation of oral solid dosage forms.

Pharmacological effects and clinical application of tetrandrine: research advances / 国际药学研究杂志

Tetrandrine(TET)is a bisbenzyl isoquinoline alkaloid extracted from the plant Stephania tetrandra. TET is one of the important active ingredients of S.tetrandra, showing pharmacological effects mainly on the circulatory, respiratory and locomotor systems, such as the anti- inflammatory, anti-tumor, anti-arrhythmia, anti-hypertensive, anti-silicosis and fibrosis effect, and thus has a high clinical application value. This article reviews research achievements of the pharmacological effects, action mechanisms, dosage forms and clinical applications of TET, in order to provide reference for related research.

Development And Validation Of Hplc Method For Simultaneous Estimation Of Sertaconazole Nitrate And Zinc Pyrithione In Combined Dosage Form

Drugs like Sertraconazole nitrate and Zinc Pyrithion were analyzed by manymethods individually viz HPLC (High performance liquid chromatography) etc but there is nosingle method reported for the simultaneous determination of Sertraconazole nitrate and ZincPyrithion in combination. Although Sertraconazole nitrate is official in British Pharmacopoeiabut Zinc Pyrithion is not official in any Pharmacopoeia. Hence a proper research work is wellaimed to develop and validate a new analytical method for simultaneous estimation ofSertraconazole nitrate and zinc Pyrithion in Pharmaceutical Dosage form.

Research Progress of Vaginal Mucosal Drug Delivery System / 中国实验方剂学杂志

Because it can not only directly reach the lesion site to play a local therapeutic effect, but also avoid the liver first pass effect and play a systemic therapeutic effect, vaginal mucosal administration has attracted more and more attention from domestic and foreign scholars in the treatment of vaginitis, cervicitis and other diseases. This article introduces the physiological characteristics of the vagina and discusses the factors affecting drug absorption. The vaginal mucosal drug-administered preparations, which are contained in the drug database of U.S. Food and Drug Administration(FDA) and China Food and Drug Administration(CFDA), and listed in the 2015 edition of Chinese Pharmacopoeia, are taken as the research objects. And the application of their dosage forms, indications and other aspects were sorted out and analyzed. The related literature on vaginal mucosal drug delivery systems in recent years was reviewed, and the dosages forms and in vitro and in vivo evaluation were summarized. Some problems in the study of vaginal mucosal drug preparations have been pointed out:①the western medicine preparations are widely used, and the related Chinese medicine preparations have been developed less; ②the majority of dosage forms are tablets, suppositories and other conventional dosage forms; ③there are few studies on the evaluation of vaginal mucosal preparations in vitro and in vivo. It is suggested that the future development of vaginal mucosal drug delivery system can be a useful attempt in the application of new technologies and methods, such as combination of drugs, high adhesion excipients, liposomes, etc;so as to provide reference for the application and improvement of vaginal mucosal drug delivery system.

Lipid regulation mechanism and dosage form selection of Xixian Tongshuan Preparation based on molecular simulation methods / 中国中药杂志

Atherosclerosis is the main cause of stroke, and dyslipidemia is the most important risk factor for atherosclerosis. In this paper, pharmacophore and molecular docking models of eight key lipid-lowering targets, namely NPC1 L1, HMG-CoA reductase, SQS, MTP, CETP, PPARα, LXRα and LXRβ, were used to screen out the small molecular database of traditional Chinese medicine(TCM), which was made up of ingredients of thirteen Chinese herbal medicines contained in Xixian Tongshuan Preparation. The screening results indicated that the preparation could showed an effect in regulating lipid on target NPC1 L1, HMG-CoA reductase, LXRβ and SQS through four groups of potential active compounds, namely prupersin A in peach kernel and suffruticoside A in gastrodiaelata, limocitrin-β-D-glucoside in Ligusticum chuanxiong, 2'-(2,3-dihydroxybenzoyl)-sweroside in Pinellia ternate and quercitrin in Panax notoginseng, 4-tert-butyl-2-[(5-tert-butyl-2-hydroxy-phenyl)methoxy-methyl]-6-(hydroxymethyl)phenol in Gastrodia elata. Moreover, the properties and extraction process of the most potentialactive compounds were consistent with the preparation process of Xixian Tongshuan Capsules, which indicated that the capsule had more advantages than the pill in the existing two dosage forms of Xixian Tongshuan Preparation. This study analyzed the pharmacodynamic basis and mechanism of Xixian Tongshuan Capsules in regulating lipid for treating stroke, and provided evidence for its further research and clinical application.

Evaluating the discriminatory power of a dissolution assay for rosuvastatin calcium capsules: Solid-state properties and dissolution media

We propose to evaluate the dissolution properties of rosuvastatin calcium (ROSC) capsules in different media to characterize the discriminatory power of the assay method. Dissolution assays were performed in media with different pH, and including the surfactant sodium dodecyl sulfate (SDS). Several immediate-release formulations were manufactured using the commercial raw material characterized as amorphous solid. The hydrophobic adjutant magnesium stearate was employed in some formulations due to its negative effect in the wettability and dissolution efficacy of solid dosages. These formulations showed the lower dissolution efficacy values in media without surfactant; however, when SDS was added to the medium, the dissolution efficacy increased, and the discriminatory power was lost. In spite of micellar solubilization does not increase the ROSC solubility, it modifies the discriminatory power of the assay method, increasing the wettability of the powder mixtures. The crystalline form M of ROSC was recrystallized in our laboratory, and it showed lower solubility in water than amorphous solid. However, its dissolution properties were not influenced by SDS. These results are important to develop dissolution assays for other hydrophilic drugs with increased water solubility, once that dissolution media with surfactants increase the wettability of the formulations, leading to an overrated dissolution rate.

Evaluation of capsule labelling for its wall contents as gelatin or non gelatin

Background: Capsules are the most commonly used solid drug dosage form and are made up of gelatin or non gelatin. Currently the gelatin based capsules drug formulations are more used. However, current issue of vegetarian and non vegetarian capsules has come up due to recent Indian government initiative to promote vegetarian capsules.Methods: There were 100 capsule dosage forms were examined for the gelatin or HPMC wall contents and nature of medicine contained in capsules, whether ayurvedic or allopathic.Results: Out of 100 capsules studied 55 had gelatin wall base while 25 had HPMC and 20 capsule labels did not mention the nature of capsule wall constituent. Out of 55 gelatin capsules 30 were of allopathic while 25 capsules were of ayurvedic medicines. Among HPMC, 15 were ayurvedic while 10 allopathic. 20 capsules had no mention of its constituent and among these non labelled capsule formulations had 11 from ayurvedic and 9 from allopathic medicines.Conclusions: The current study revealed that gelatin capsules forms bulk in Indian market. Even the gelatin capsules contained ayurvedic medicines while 10% of HPMC capsules contained allopathic medicines. Non labelled capsules formed 20% of total capsules. These findings suggest wider scope for promotion of HPMC based capsules.

Comparative Analysis of In-use Period after First Opening or Reconstitution of European Union Imported Sterile Products and Domestic Sterile Products in Our Hospital / 中国药师

Objective: To provide reference and suggestions for improving the in-use period information of sterile products after first opening or reconstitution in China. Methods: The package inserts of sterile products in our hospital were investigated. The sterile products needed to be reconstituted before use and with multiple-dose package were selected. The in-use period information of European imported sterile products and domestic sterile products were comparatively analyzed. Results: The presentation rate of in-use period in the package inserts of domestic sterile products was 32. 25% , which was less than 55. 56% of the other imported sterile products, and significantly less than 93. 55% of European imported sterile products. Conclusion: The relevant content of in-use period of sterile products after first opening or reconstitution is supplemented relatively late in China's stability testing guidance for drug substances and products, moreover, the specific technical proposals are absent. It is suggested that the drug administrative department and its techni-cal supportive agencies should improve the relevant guidance and guide pharmaceutical research enterprises and manufacturing enterpri-ses to carry out in-use stability studies, furthermore, gradually improve the relevant in-use period information in package inserts.

Electrostatic Dry Powder Coating for Pharmaceutical Solid Dosage Forms / 中国药学杂志

Derived from industrial dry powder coatings, electrostatic dry powder coating for pharmaceutics gained numbers of attentions in recent years. In this technology, powdered coating materials are directly sprayed onto the surface of the solid dosage through an electrostatic gun without using any solvent or water, followed by a curing step to allow those deposited coating particles to coalesce together and form a coating film. The electrostatic dry powder technology has many advantages compared with solvent or aqueous coating such as higher coating efficiency with better coating film, less energy consumption and shorter processing time, which is a promising alternative of liquid coatings used in the present pharmaceutical industry.The objective of this review is to introduce the development background, fundamental principles, technological superiority of the electrostatic powder coating for solid dosage forms,and to summarize and discuss those reported results, giving prospects for the future industrial applications.