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OBJECTIVE:To prepare Fluconazole adhesive gel.METHODS:Using carbopol934p,glycerine and other inor?ganic solvents as adjuvant,the Fluconazole adhesive gel was prepared.Then the pharmaceutic study and quality standard es?tablishment were carried out.RESULTS&CONCLUSION:The Fluconazole adhesive gel was simple in preparation and stable in property.The adhesive gel may become an ideal antifungal preparation for topical application.
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Objective: To study the pharmacokinetics of diclofenac sodium microemulsions in human. Methods: According to the crossover design, each volunteer was orally given diclofenac sodium microemulsion and diclofenac sodium tablet. The serum concentrations were determined by RP-HPLC with UV-detector. The concentration-time data were analyzed using 3P87 Pharmacokinetic Program and the pharmacokinetics parameters were compared by paired t-test. Results: It was found that diclofenac sodium in serum was linear within the range of 50-8 000 μg/L. The minimum detection concentration was 30 μg/L. The mean rate of recovery was (100.55±1.56)%. After a single oral dose, AUC0～∞ were 5.563，7.891 μg*h/ml, MRT 5.489， 5.387 h for dispersible diclofenac sodium microemulsion and tablet respectively. Conclusion: Absorption progress of diclofenac sodium microemulsion in human may be special.
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Objective To evaluate the in vivo behaviour of the pulsed tablet in six scintigraphic studies.Methods The lag time and the anatomical position at the time of release were detected by scintigraphic evaluation.Results The different types pulsed release tablets all can achieve the lag time in vivo.Conclusion Scintigraphic study is the first considered method to evaluate the in vivo behaviour of the new formulation.
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Objective: To prepare silibinin solid dispersion and measure its dissolution in vitro .Methods: Silibinin solid dispersions were obtained with urea, PVP and poloxamer188 as carriers by melting and coevaporation methods. Differential thermal analysis and powder X ray diffraction were used to determine the status of drug in carriers, and the dissolution characteristics in vitro were studied in simulated gastric juice. Results: In PVP silibinin solid dispersions drug was amorphous; in poloxamer188 silibinin solid dispersions, drug existed as fine crystal, while in urea silibinin solid dispersions most of silibinin existed as crystal, only a little as molecule. Poloxamer188 was the better carrier in improving the solution and dissolution rate of the drug. Conclusion: Poloxamer188 is a very useful carrier in improving the solubility and dissolution of silibinin. [
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Objective: To prepare ibuprofen dispersible tablet and compare its pharmacokinetics and bioavailability with market tablets in rabbits. Methods: According to inspection of factors and orthogonal design, optimal formulation was decided. A randomized crossover and self control design was used. Eight healthy rabbits were single oral dosed with 100 mg ibuprofen dispersible tablet or market tablet, respectively. The plasma drug concentration was determined by HPLC method. The pharmacokinetic parameters were calculated by 3P87 program and the bioequivalence was assessed by NDST5.0 program. Results: A one compartment open model was adopted and the pharmacokinetic parameters of dispersible tablet and market tablet were as follows: c max were (9.79?2.25) and (4.54?1.50) ?g/ml; t max were (0.27?0.07) and (2.03?0.53) h; t 1/2 were (6.65? 2.14) and (9.17?4.38) h; AUC 0~∞ were (94.11?28.38) and (65.20?18.38) ?g?h?ml -1 , respectively. Ralative bioavailability of the dispersible tablet was 164.11% compared to market tablet. Conclusion: Ibuprofen dispersible tablet is administrated easily and absorbed quickly, and its bioavailability is far more better than the market one. [
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Objective: To compare the pharmacokinetics and bioavailability of verapamil hydrochloride pulsed release tablets with core tablets. Methods: Latin test was employed in the single oral administration of the Ⅲ,Ⅳ type of pulsed release tablets and core tablets in 8 volunteers. The pharmaceutics behavior of the tablet in vivo was evaluated by the lag time, c max ,AUC and so on. Results: The pharmacokinetics results demonstrated that the Ⅲ type of pulsed tablet in humans could be released after about 4 h lag time. In a proper range, pulsed release tablets only changed the beginning time while c max and AUC were not different from the core tablets. Conclusion: A new system to reduce the early morning symptoms of ischemic heart disease is prepared. [
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Objective: To study the pharmacokinetic progress of diclofenac sodium microemulsions in rabbits. Methods: Diclofenac sodium microemulsion and diclofenac sodium suspension were single orally given to rabbits. Diclofenac sodium concentrations in plasma were measured by HPLC method. Results: AUC 0 ∞ , c max1 and t max1 were 13.456 ?g?h?ml -1 , 2.852 ?g/ml and 1.438 h after po diclofenac sodium microemulsion and 10.584 ?g?h?ml -1 , 3.145 ?g/ml and 0.750 h after po diclofenac sodium suspension. Conclusion: The absorption of diclofenac sodium microemulsions in rabbits is slower and can keep a higher concentration in plasma for a long time compared with those of the suspension. [
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Lappaconitine hydrobromide can remove inflammation and swelling, lower temperature and relieve heat. It also can be used for local anesthesia. Clinically lappaconitine hydrobromide can be applied via i.v., i.m. or p.o. for analgesic treatment. Lappaconitine has better effect for moderate pain than for severe pain, which may be associated with the low dose. Future efforts should be made in increasing dosage, combining lappaconitine hydrobromide with other drugs and improving drug delivery technique.
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Objective: To clone and express Treponema pallidum (TP) specific antigens P15 and P47 and use them in clinical examination. Methods: P15 and p47 genes synthesized were inserted into a GST fusion expression vector. The recombinant antigens were purified by affinity chromatography and then coated on microplates to establish an ELISA kit. Using this kit, national TP standards, sera of normal persons and patients with TP and other diseases were tested. Results: The synthesized p15 and p47 genes sequenced were identical with those of GenBank. National TP standards were tested by ELISA kit which coated with these recombinant antigens, and the results accorded with the standards. High sensitivity and specificity was showed when 2 recombinant antigens were used in ELISA to detect the sera of normal persons and patients with TP and other diseases. Conclusion: The recombinant TP specific antigen P15 and P47 are suitable for establishment of ELISA kit in clinical examination.
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To prepare bio-degradable albumin microspheres containing carboplatin. METHODS: Bovin serum albumin microspheres containing carboplatin were prepared by using emulsion-direct heat cross linking techniques. RESULTS: The microsphere was yellow, powdery, with a mean diameter of 58.2 μm. The microphere loaded (11.26±0.48)% carboplatin. The trapping efficiency was (84.5±3.6)%. The pattern of drug releasing from the microspheres in vitro fitted to zero order release plot, with an initial burst in the first 2 hours. The releasing rate can be expressed by the follow equation: Q=21.90+8.50 t (d), r=0.995 8. t50=3 d. Stored at 4 ℃ and 37 ℃ respectively for 3 months, the microspheres did not alter much in shape, size and drug content. CONCLUSIONS: This method is simple, reproducible, having high drug trapping efficiency. The microsphere obtained is stable and release drug at a consistant rate in vitro, leading to a prosperity in clinical use.
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Ketoprofen is widely used as non-steroidal anti-inflammatory drug. A potential sustained release ketoprofen tablet formulation was designed by orthogonal experiment on formulations composed of differential common excipients and homemade polymerides, and was screened by dissolution in vitro. The dissolution rate (%) of the ketoprofen tablet in simulated intestinal fluid was 16.6, 26.7, 42.2, 63.6, 83.1, 93.4, at 30min, 1, 2, 4, 6, 8 h, respectively. The plasma ketoprofen concentrations in six male volunteers were assayed after administration of a single oral dose (100 mg) of the sustained release tablet. It was found that the tablet formulation screened in vitro had sustained release effect in vivo too. This study suggests that there was a close correlation between the dissolution of sustained release ketoprofen tablet in vitro and the percent of dose absorbed in vivo, and the correlation coefficient was 0.9689. The influence of tablet hardness on the release rate of ketoprofen was also observed..
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Objective: To investigate the difference between the uptake of different hydrophobe drugs into the O/W microemulsion systems and micellar solutions. Methods:Based on the phase diagram,the incorporation of 3 poorly water soluble drugs into Cremophor RH-40-alchohol-isopropyl myristate-water microemulsions and Cremophor RH-40 surfactant systems were examined. Results: There was no significant difference between miconazole nitrate and indometacin into the O/W microemulsion systems and micellar preparation.There was,however,a significant increase in the micellar solutions of ibuprofen amount than in the microemulsion systems. Conclusion:Improvement of solubility by O/W microemulsion and micellar system depends on the solubility of the drug in the dispersed oil phase and is significant only for high lipophilic drugs.
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Bioavailable studies were performed based on plasma concentrations of captopril in 5 Beagle dogs and 5 male healthy volunteers after a single oral administration of captopril sustained-release tablet and sugar-coated tablet. A one-compartment model was adopted. Relative bioavailability of sustained-release tablet to sugar-coated one was 131.6% for dogs and 111.0% for humans. Their mean residence times (MRTs) were 4.52 h and 1.96 h in dogs, 4.28 h and 2.77 h in humans, respectively. The maximum concentrations were 995.9 ng/ml and 2470.8 ng/ml in dogs, 126.2 ng/ml and 251.2 ng/ml in humans for two kinds of tablets, respectively. The duration time, in which plasma concentration staved above 50% inhibitory concentration of angiotensin converting enzyme activity, was more than 10 h for sustained-release tablets and 6h for sugar-coated tablets at the same dose (37.5 mg). consequently, it could be expected that the sustained-release tablet dosed twice a day should have a greater efficiency than marketed sugar-coated tablet taken 3 times daily.
