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11Experiment 3 batches, the results total jiegumu glycosides RSD was 0.653%, morroniside RSD was 1.5%. Thereby determining the optimum purification process Sambucus williamsii Hance.The most of the ethanol extract of Sambucus williamsii Hance polar impurities than morroniside, Use macroporous resin column is intended to be morroniside with these large polar impurities separation. This article on macroporous resin type, maximum sample volume, the best elution flow rate were screened. Conclusions
Best purification processes:In 1.5BV / h flow rate of water was eluted through the AB-8 type macroporous resin column chromatography, the water eluate discarded 20BV, collect 10% ethanol eluate was lyophilized to obtain total jiegumu glycosides.The three batches of validation tests showed that macroporous resin purification process stability, resulting elderberry total glucosinolate content of total glycosides (in morroniside meter) reached more than 51% recovery rate of 80% or more,This is the total jiegumu glucosides purification process. References
1. National Herbal Writing Group of the National Herbal Compendium (first volume) [M]. People's Health Press, 1975; 738.
2. Lu Fang. Thesis "elderberry chemical constituents of the root bark" Heilongjiang University of Chinese Medicine, 2002.
3. Han hua Elderberry root bark promote healing effective part of the chemical composition and pharmacological effects of Heilongjiang University of Chinese Medicine Doctoral Dissertation, 2006.
4. Han hua, Kuang Haixue, Li Zhenyu, etc. orthogonal test morroniside extraction process [J] Medicine Information, 2011,28 (4) :33-35.
Study on Preparation Technology of Total Jiegumu glycosides tablet
LU Qing-xiu,Yang Liu,Jiang Hai,Wang Qiu-hong,Yang Bing-you,Kuang Hai-xue*
Key Laboratory of Chinese Materia Medica,Heilongjiang University of Chinese Medicine,Ministry of Education,Key Laboratory of Traditional Chinese Medicine and Natural Medicine Pharmacodynamic Material Base,Harbin 150040, China
Abstract: Objective To establish the preparation of total jiegumu glycosides tablet . Method Using single factor method excipients were screened for the molding process studied for total jiegumu glycosides tablet.Result. Sambucus williamsii Hance
glycosides32g;lactose288g;MCC32g;PVPP7g;magnesiumstearate3.5g;Forming process is as following:fully combine the extract of total jiegumu glycosides and adjuvant as formula, and then filter the mixture, sieved, tabletting, ie.Conclusion Our group determine total jiegumu glycosides tablet that is the preparation technology scientific and stable .The chip can develop total jiegumu glycosides tablet and provide the basis for new drugs.
Key words: morroniside; total jiegumuglycosides tablet;preparation process
Sambucus williamsii Hance(jiegumu) known as hippurate show,big bone Dan and so on.Derived from Sambucus species of Caprifoliaceae[1].The main efficacies of jiugumu include fractures, bruises, swelling and bleeding trauma.The root of jiegumu have significantly promote fracture healing, and to clarify the material basis for total jiegumu glycosides.Task Force will total jiegumu glycosides prepared into tablets for clinical patients taking.Decoction is characterized oral dose, long home easily moldy. But there is an accurate dose tablets, stable quality, good
bioavailability, etc., are commonly used traditional Chinese medicine formulations drug research[2].The preparation is mainly used in clinical fractures in patients, an effective daily dose of 0.2g or so, can achieve the requirements of the tablet; Therefore, the effective part of the elderberry (Sambucus total glycosides) prepared into tablets for clinical patients taking.
1 Materials and Methods
1.1 Materials
LB-881C six Disintegration Tester (Wu Xi Keda Instrument);ZP170 Rotary Tablet Press;CS-3 friability tester;Soluble starch;lactose;microcrystalline cellulose;cross-linked povidone (U.S. ISP Corp.);Hard magnesium stearate.
1.2 Methods
1.2.1TheChoice of diluents Total jigumu glycosides have a strong moisture absorption, it is necessary to add diluent to reduce its moisture absorption.Design 5 prescriptions,1(starch 80%),2(dextrin 80%),3(lactose 80%),4(MCC 80%),5(100% tital jiegumu glycosides).Selected hygroscopicity as an index to investigate diluent hygroscopicity of starch,dextrin, lactose,MCC.Accurately weighed total jiegumu glycosides and different thinners,mixing,and placing 20°C,humidity of 75% RH conditions, respectively,12hN 24hN 36hand48h weighed to calculate the absorption rate. Moisture absorption rate(%)=(mass powder after moisture-absorbent powder mass before)/absorbent powder mass*100% Table 1 The diluents dilution of different time
Prescription No. 12hAbsorptio n rate (%) 24hAbsorption rate (%) 36hAbsorption rate (%) 48hAbsorption rate (%)
1 4.68% 4.80% 4.79% 4.79%
2 4.19% 5.38% 6.50% 6.50%
3 2.61% 2.64% 2.68% 2.68%
4 4.67% 4.72% 4.75% 4.75%
5 9.93% 10.51% 10.57% 10.57%
From Table1,comparison of diluents,the prescription of lactose(3) have the weakest hygroscopicity. According to the literature[3-5],lactose have good formability,widely used,and so lactose was chosen as the primary diluen.
1.2.2 TheScreening for proportion of the amount of lactose and microcrystalline cellulose.Alone choose lactose as diluent,wet granulation soft material too close,and the particals too tough,so consider adding a certain percentage of MCC. Table 2 The prescription of different proportions of lactose and MCC
Prescriptio n No total jiegumu glycosides (g) Lactose (g) MCC(g) Magnesium stearate
1 3 30 Amount
2 3 27 3 Amount
3 3 21 9 Amount
4 3 15 15 Amount
According to Table 2 is designed to prescription,granulation. In ease of granulation, particle characteristics, tablet properties, the disintegration time as the evaluation index.
Table 3 The result of dosage proportion of lactose and MCC
Prescriptio n No Granulation difficulty Grain traits Tablets traits Disintegration time (min)
1 difficult excellent slight pitting 8
2 easy moderation uniform 7
3 easy moderation uniform 5
4 easy slightly loose a few loose pieces 3
Table 3 shows, only choose lactose as diluent, made of soft material is more difficult, and the particle excellent, adding MCC has been greatly improved. Since MCC expensive and less hygroscopic lactose, and ultimately determine the proportion of diluent is lactose and MCC 9:1 1.2.3 Thescreening of thinner Different amount of diluent will make moisture different.So different proportions of diluents were added to total jiegumu glycosides. Table 4 The dosage prescription of thinners
Prescripti on No total jiegumu glycosides (g) Thinner total (g) Lactose (g) MCC (g)
1 0.1 0.6 0.54 0.06
2 0.1 0.8 0.72 0.08
3 0.1 1.0 0.90 0.10
4 0.1 1.2 1.08 0.12
Table 5 The screening result of dosage of thinners
Prescription No 10h 24h 36h 48h 60h
1 1.41% 1.89% 2.02% 2.07% 2.07%
2 1.06% 1.48% 1.63% 1.69% 1.69%
3 0.89% 1.24% 1.34% 1.40% 1.40%
4 0.69% 1.12% 1.18% 1.27% 1.27%
According to Table 4,were accurately weighed total jiegumu glycosides and thinners, mix,placed 20°C,humidity of 75% RH conditions,respectively weighed in 10h, 24h, 36h, 48h and to calculate absorption rate .Accoarding to Table 5 determined the total jiegumu glucosides diluent ratio of 10:1.
1.2.4 Wetting agents and disintegrants As total jiegumu glycosides have good water solubility and a good viscosity,70% ethanol is the most suitable wetting agents; To considering finish and friability of sided, so choice appropriate amount PVPP. as a disintegrant agent.
1.2.5 Screening lubricant Built particlesby total jiegumu glycosides: lactose: MCC 1:9:1 ratio, Said four copies, one copy without lubricant, and the other three parts adding 0.5% different lubricants, The results showed that a small angle of repose of magnesium stearate, a lubricant is preferably.
1.2.6 The amount of magnesium stearate With total jiegumu glycosides: lactose: MCC 1:9:1 ratio pellet,said four were added magnesium stearate 0.1%, 0.5%, 1.0%, 1.5%, measured angle of repose. The angle of repose results were 39.5,37.3,34.7,33.4 that showed with the increase in the amount of magnesium stearate and liquidity is gradually improving.Determining the lubricant magnesium stearate, the amount of 1%.
Results and discussion
The proportions of elderberry prescription glycosides with lactose, MCC, PVPP mixing, granulating 70% ethanol, dried, whole, plus magnesium stearate, mixing, tabletting. Examine tablet weight variation, disintegration time, friability, hardness. Experiment 3 batchesD Table 6 The verification results of preparation process
Experime nt No. Weight difference Disintegratio n time Friability (%) Hardness (kg.cm-1)
1 0.3615±0.05 17 0.6 3.6±0.2
2 0.3594±0.08 19 0.6 3.5±0.2
3 0.3611±0.04 16 0.5 3.8±0.1
The results showed that the average tablet weight of the preparation, disintegration time, friability, hardness are in line with the requirements under pharmacopoeia tablets, process stability, can be used as total jiegumu glycosides tablet formulation process.
Conclusions
Determine the preparation process:total jiegumu glycosides 32g,lactose 288g,MCC 32g, PVPP 7g full mixing, over 80 mesh sieve, soft material made of 70% ethanol, 20 mesh sieve granulation, drying, whole, plus stearin magnesium 3.5g,mix make total jiegumu glycosides tablet.The research of total jiegumu glycosides tablet that is the preparation technology scientific and stable .The chip can develop total jiegumu glycosides tablet and provide the basis for new drugs.
References
1.Jiangsu New Medical Editor. Chinese Dictionary (two volumes) [M]. Shanghai Science and Technology Press, 1985:2093.
2. Zhao Xiaohong, Chen Di hua, SI Jian-yong, etc. Traditional Chinese Drug Research tablet formability ideas and methods [J] Chinese Journal of Clinical Pharmacology, 2002,13 (5) :327-329.
3. Armando Caceres, Brenda R. Lopez, Melba A. Giron and Heidi Logemann. Plants used in guatemal for the treatment of dermiatophytic infection. 1.screening for antimycotic activity of 44 plant extracts. Journal of Ethnopharmacology, 1991, 31(3): 263-276.
4. Liu Zheng, Wu Jingsheng, Wang Minwei. Elderberry oil lipid-lowering and anti-aging effect of [J]., Shenyang Pharmaceutical University, 1995, 12: 127-129.
5. Mlinaric A, Kreft S, Umek A, Strukelj B. Screening of selected plant extracts for in vitro inhibitory activity on HIV-1 reverse transcriptase(HIV-1 RT). Pharmazie,
Study onQuality Standard of Total Jiegumuglycosides tablet
LU Qing-xiu,Yang Liu, Jiang Hai,Wang Qiu-hong, Yang Bing-you, Kuang Hai-xue*
Key Laboratory of Chinese Materia Medica,Heilongjiang University of Chinese Medicine,Ministry of Education,Key Laboratory of Traditional Chinese Medicine and Natural Medicine Pharmacodynamic Material Base,Harbin 150040, China
Abstract:Objective: To study the quality standard of total jiegumu glycosides tablet.Method: Ast ragalus morroniside were identified by TLC method;The content of total jiegumu glycosides tablet was determined by HPLC and determine the dissolution of morroniside in total jiegumu glycosides tablet by slurry. According to the 2010 edition of "Chinese Pharmacopoeia"provisions of the relevant tablets, firstly, we established inspection methods of
