ABSTRACT
The present study investigates the possibility of using poloxamers as solubility and dissolution rate enhancing agents of poorly water soluble bioactive constituent patchouli alcohol [PA] that can be used for the preparation of immediate release pellets formulation. Two commercially available grades poloxamer 188 [P 188] and poloxamer 407 [P 407] were selected, and solid dispersions [SDs] containing different weight ratio of PA and poloxamers, and the combination of P 188 and P 407 as dispersing carriers of ternary solid dispersions [tSDs] were prepared by a low temperature melting method and solidified rapidly by dropping into the 10-15 °C condensing agent atoleine. Both PA/P 188 and PA/P 407 binary solid dispersions [bSDs] could remarkably promote the dissolution rate of PA, increasing approximately 16 times in bSDs with poloxamers in comparison with pure PA within 180 min. P188 contributed to a faster dissolution rate than P 407, however, P 407 had a better solubility. It is interesting to note that the incorporation of P 188 in PA/P 407 bSD pellets could strongly enhance the dissolution rate of PA. DSC and FTIR were used to explore the characteristics of PA-SD pellets. The enhancement of dissolution from the SDs may be attributed partly to the reduction in particle size in PA crystalline due to the formation of eutectic system with poloxamers. Moreover, a simple, accurate in-vitro dissolution test method for volatility drug was established, and the process of PA-SD pellets preparation was simple, rapid, cost effective, uncomplicated and potentially scalable
Subject(s)
PoloxamerABSTRACT
<p><b>OBJECTIVE</b>To explore the mechanism of acupoint sticking of "Hua yutie" in improving ischemic stroke.</p><p><b>METHODS</b>Eighty rats were randomly divided into 5 groups, a model group, an acupoint sticking group, an acupuncture group, a Nimodipine group and a normal group. Middle cerebral artery occlusion (MCAO) was used for preparation of focal cerebral ischemic rat model. After modeling, any treatment was not given to the model group; for the acupoint sticking group, "Hua yutie" was applied at "Dazhui" (GV 14) ,"Qihai" (CV 6) and "Mingmen" (GV 4); for the acupuncture group, acupuncture was given at the same acupoints as those in the acupoint sticking group; the Nimodipine group received intragastric administration of Nimodipine. And the normal group did not receive any treatment. Their infarction volume, the cerebral water content, expression of vascular endothelial growth factor (VEGF) and the protein level were observed.</p><p><b>RESULTS</b>The infarction volume coincided with the dominative scope of the middle cerebral artery of the electric coagulation. There were significant differences in the cerebral water content as the various treatment groups compared with that of the model group (all P<0.05). The VEGF positive cell number and the protein level around the infarction area in the acupoint sticking group were increased as compared with those in the model group (P<0.01), with no significant difference as compared with the Nimodipine group and the acupuncture group (all P>0.05).</p><p><b>CONCLUSION</b>Acupoint sticking of "Hua yutie" alleviates the cerebral damage after ischemia possibly through enhancing the expression and protein level of VEGF.</p>
Subject(s)
Animals , Female , Humans , Male , Rats , Acupuncture Points , Administration, Cutaneous , Brain Ischemia , Drug Therapy , Genetics , Metabolism , Cerebral Infarction , Drug Therapy , Genetics , Metabolism , Drugs, Chinese Herbal , Gene Expression , Rats, Wistar , Vascular Endothelial Growth Factor A , Genetics , MetabolismABSTRACT
<p><b>OBJECTIVE</b>To explore the effect of compound decoction on notoginsenosides in Panax notoginseng.</p><p><b>METHOD</b>Notoginsenoside R1, Rg1, Re, Rb1 and pH were used as the parameters to investigate the changes on the content of notoginsenosides in different compound extractions by heating for two hours and their correlation with pH.</p><p><b>RESULT</b>When the pH values of solution of P. notoginseng with Fructus ligustri, P. notoginseng with Eupolyphaga seu steleophaga, P. notoginseng with Pheretima asiatica, and Zhitangjiang Fang (free of Hirudo) were rept higher than 5.7, the reserved rate (RR) of notoginsenside were higher than 90%; When the pH values of decoetion of P. notoginseng with Salvia miltiorrhiza, P. notoginseng with Paeonia lactiflora, P. notoginseng with Platycodon grandiflorum, P. notoginseng with Arctium lappa were kept 4.5-5.5, their RR of notoginsenside were 60% - 85%; When the pH values of the decotction of P. notoginseng with Hirudo nipponica was decreased to 3.4, its RR of of notoginsenside was 38.4%; When the pH values of Zhitangjiang Fang extraction was regulated by 0.1% NaOH solution to pH 6. 3, and the RR of notoginsenside increased to 97%.</p><p><b>CONCLUSION</b>The pH of other Chinese herbal medicines extraction with P. notoginseng compound is a critical effect on the stability and yields of notoginsensides.</p>
Subject(s)
Animals , Arctium , Chemistry , Cockroaches , Chemistry , Drug Combinations , Drugs, Chinese Herbal , Chemistry , Ginsenosides , Hirudo medicinalis , Chemistry , Hot Temperature , Hydrogen-Ion Concentration , Ligustrum , Chemistry , Materia Medica , Chemistry , Oligochaeta , Chemistry , Paeonia , Chemistry , Panax , Chemistry , Platycodon , Chemistry , Salvia miltiorrhiza , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To recognize changes in the contents of ingredients of Andrographis Tablet in the process of production.</p><p><b>METHOD</b>Adopting TLCS, TLC, HPLC to detect effective contents of ingredients which are produced in every stage of process of Andrographis Table's production.</p><p><b>RESULT</b>Handling with the fresh Herba Andrographis according to current pharmacopeoia's technology, it showed that only dehyandrographolide can be detected. It indicated that the main factor that leads to chemical change is the heating process in the process of production.</p><p><b>CONCLUSION</b>Avoiding heating treatment or reducing heating treatment time is the main factor to protect the effective ingredients.</p>