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Article in Chinese | WPRIM | ID: wpr-906408


This review made a systematic textual research on the historical evolution and changes of the origin, producing areas and quality, harvest time and processing methods, and cultivation technique of Poria in famous classical formulas from the Catalogue of Ancient Famous Classical Formulas (the First Batch) by referring to the literature of ancient materia medica and medical books combining with the modern literature in CNKI, Wanfang Data and other databases, which could provide reference for the development and research of the famous classical formulas containing Poria. According to the research, the origin of Poria in ancient times was the dried sclerotia of Poria cocos. The producing area of Poria is widely distributed in China, mainly produced in Anhui, Hubei, Henan and Yunnan provinces. The quality of Poria from Yunnan is better, and the yield is larger in Anhui and Hubei provinces. The quality evaluation of Poria is basically the same from ancient to modern, which has the characteristics of large block, heavy weight, thin and wrinkled skin, and white and delicate cross section. The harvesting period of Poria is usually in August of the lunar calendar. The initial processing has undergone the evolution from drying in shade in the ancient time to drying in shade after sweating in the modern time. From ancient times to the present, Poria has been processed by cutting to prepare the Fuling lumps and Fuling slices. The cultivation technique has experienced the evolution process of "wild Poria-inoculation of live pine root-basswood cultured". At present, Poria is mainly cultivated by artificial basswood with mature technical methods and abundant yields, which can meet the research and development needs of the famous classical formulas.

Acta Pharmaceutica Sinica ; (12): 1115-1122, 2019.
Article in Chinese | WPRIM | ID: wpr-780169


In this paper, a new type of preparation for treatment of initial dry eye disease, thermosensitive in situ gel, was prepared using levocarnitine as a model drug. Poloxamer 407 and poloxamer 188 were used as the gel matrix, and sodium hyaluronate and sodium carboxymethylcellulose were used as bioadhesive materials. Gelation temperature was determined by a rotor method and the prescription was optimized by central composite design-response surface methodology. The pH value, viscosity value and gelation temperature of the optimal prescription were measured. The release of the drug in vitro was examined by dialysis membrane permeation, and retention time of the thermosensitive in situ gel preparation on the rabbit's ocular surface was observed by a slit lamp microscope. The results showed that the dosage of the poloxamer 407 and poloxamer 188 were 20.81% and 3.46%, respectively, and sodium hyaluronate was 0.02%, sodium carboxymethyl cellulose was 0.10% of the optimal formulation of levocarnitine thermosensitive in situ gel. The pH value was 6.90 ± 0.06 at room temperature and the viscosity value started to rise sharply at 27 ℃ of the optimal formulation. The gelation temperature of the optimal preparation before and after dilution by simulated tear fluid were (26.37 ± 0.06) ℃ and (33.57 ± 0.21) ℃, respectively. In the first 240 min, in vitro release rate per unit area of levocarnitine thermosensitive in situ gel was lower than that of solution (P<0.05), and after 600 min, the cumulative release rate of levocarnitine thermosensitive in situ gel could reach more than 80%. The retention time of the thermosensitive in situ gel preparation on rabbit's ocular surface reached about 25 min, at least 5 times as much as that of the solution. The animal experiment was conducted following the National Institutes of Health Guidelines for the use of experimental animals, and approved by the Ethics Committee of the Experimental Animal Center of Beijing University of Chinese Medicine. The levocarnitine thermosensitive in situ gel showed good characteristics and sustained release property and significantly improved the retention time of the drug on the rabbit's ocular surface.

Article in Chinese | WPRIM | ID: wpr-801716


Objective: To investigate the effect of varying concentrations of polyethylene glycol(PEG)400 in receiving solution on in vitro transdermal test of drugs. Method: 5-Fluorouracil(5-FU) was selected as a model drug,by preparing different concentrations of PEG400-phosphate buffer solution(PBS) as the receiving solution,the receiving chamber did not add drug,the excised rat skins were treated with various additives for 12 h,then replaced by PBS and added the saturated model drug into the donor compartment to determine the transdermal parameters of the drug.Meanwhile,scanning electron microscopy(SEM) was employed to monitor the effect of PEG400 with different concentration on the stratum corneum of rat skin. Result: The 10%,15% and 40% PEG400-PBS groups had no significant effect on in vitro transdermal absorption parameters of the 5-FU.The steady transdermal rate and cumulative penetration rate of the drug in 20% and 30% PEG400-PBS groups were significantly higher than that in the PBS group(PPConclusion: In the rat skin transdermal test,the concentration of PEG400 in receiving solution should be controlled below 20%.

Article in Chinese | WPRIM | ID: wpr-775412


Usnic acid and its derivatives, a group of organic molecules with great importance, are characteristic to lichens, possessing pharmacological activities such as anti-virus, anti-bacteria, anti-humor, anti-inflammatory, analgesic, and anaesthetic effects. Many of them have been widely used as medicine, but also bring side effects such as dermatitis and liver damages. In the past decades, great efforts by isolation, organic synthesis, and structure modification methods were put on discovery of UA derivatives with higher biological activities or less side effects. This paper describes herein the most progress on natural sources, isolation and structure elucidation, structural characteristics, synthesis and modification results, pharmacological activities and toxicities of UA and its derivatives, hopefully to provide valuable reference for further research.

Benzofurans , Chemistry , Pharmacology , Biological Products , Lichens , Chemistry
Article in Chinese | WPRIM | ID: wpr-707162


Objective To optimize ambi-extracting and inclusion process of volatile oil from Chuanxiong Rhizoma and Angelicae Sinensis Radix. Methods With yield ratio of volatile oil and ferulic acid content in water extract as evaluation indexes, single factor experiments were used to study the extraction process. With the inclusion rate of volatile oil and yield of inclusion as evaluation indexes, saturated aqueous solution was used to L9(34) orthogonal experiments to reach optimum inclusion process. Results The optimum extraction process of Chuanxiong Rhizoma and Angelicae Sinensis Radix was extracted for 8 hours with 8 folds the amount of water, and without soaking. The validation experiments of extraction of volatile oil and ferulic acid content in water extract were 1.23 mL and 0.387 9 mg/g. The optimum conditions of inclusion process were as follows: volatile oil (mL): β-CD (g) was 1:8;inclusion temperature was 40 ℃; inclusion time was 3 hours. The validation experiments of inclusion rate of volatile oil and yield of inclusion were 74.89% and 72.81%. Conclusion Optimum ambi-extracting and inclusion process of volatile oil from Chuanxiong Rhizoma and Angelicae Sinensis Radix are feasible and stable, witch can provide certain supporting data for preparation production.

Article in Chinese | WPRIM | ID: wpr-250476


Sixteen compounds were isolated from lichen Usnea longissima using of various chromatographic techniques including silica gel, Sephadex LH-20, ODS, and semi-preparative HPLC. By spectroscopic data analyses, their structures were identified by as useanol(1), lecanorin(2), 3-hydroxy-5-methylphenyl 2-hydroxy-4-methoxy-6-methylbenzoate(3), lecanorin E(4), 3'-methylevernic acid(5), evernic acid(6), barbatinic acid(7), 3,7-dihydroxy-1,9-dimethyldibenzofuran(8), orcinol(9), O-methylorcinol(10), methyl orsellinate(11), methyl everninate(12), 2,5-dimethyl-1,3-benzenediol(13), 2-hydroxy-4-methoxy-3,6-dimethyl benzoic acid(14), ethyl everninate(15), and ethyl 2,4-dihydroxy-6-methylbenzoate(16). Compound 1 was obtained as a natural product for the first time, and 3,4, 8,10,12, and 13 were isolated from Usneaceae family for the first time. Compound 1, 8, and 13 showed significant anti-inflammatory activity against NO production in RAW 267.4 cells with IC₅₀ values of 6.8, 3.9 and 4.8 μmol•L⁻¹, respectively, compared with the positive controls curcumin(IC₅₀ 15.3 μmol•L⁻¹) and indomethacin(IC₅₀ 42.9 μmol•L⁻¹).