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1.
Article in Chinese | WPRIM | ID: wpr-350640

ABSTRACT

<p><b>OBJECTIVE</b>To prepare ligustrazine (TMPZ) ocular sustained-release implant, and investigate its in vitro drug release, pharmacokinetics in rabbit vitreum and in vitro correlation.</p><p><b>METHOD</b>Ligustrazine ocular sustained-release implants were prepared by micro-twin conical screw mixers with hot-melting extrusion method, with polyactic-co-glycolic acid (PLGA) as the matrix. HPLC was adopted to determine the concentration in vitreum after ligustrazine was implanted in rabbit eyes, in order to examine its in vivo sustained-release behavior, and study the correlation between in vitro and in vivo.</p><p><b>RESULT</b>Ligustrazine implants were prepared with a drug-loading rate between 10% and 30%, which was in conformity to the pharmacopoeia in terms of the content uniformity. Its in vitro release was in conformity to the zero-order release model. With PLGA 5050, 2. 5A as a vector, ligustrazine implants with a drug-loading rate of 30% could slowly release drug for more than 3 weeks, indicating a good correlation between in vitro and in vivo release.</p><p><b>CONCLUSION</b>Ligustrazine ocular implants prepared with hot-melting extrusion method is practicable. Ligustrazine ocular implants release drug smoothly in rabbit vitreous vitreums, suggesting good sustained-release effect.</p>


Subject(s)
Animals , Biological Availability , Drug Implants , Eye , Female , Male , Polyglycolic Acid , Chemistry , Pyrazines , Chemistry , Pharmacokinetics , Rabbits , Vitreous Body
2.
Chinese Journal of Surgery ; (12): 44-48, 2013.
Article in Chinese | WPRIM | ID: wpr-247893

ABSTRACT

<p><b>OBJECTIVE</b>To study the clinical effect of arthroscopic anterior cruciate ligament (ACL) construction with different transplants.</p><p><b>METHODS</b>From March 2006 to April 2009, 86 patients including 60 male and 26 female undergoing arthroscopic ACL reconstruction were prospectively randomized consecutively into autograft group (44 patients, using autogeneic hamstring tendons) and allograft group (42 patients, using allogenic lower extremity tendons). The age of those patients were 22 - 56 years, averaging (32 ± 7) years. The operations were made by the same doctor with the standard technology. The postoperative effects were assessed by the range of motion and tibia forward distance, Lachman test, pivot shift test, Daniel test, IKDC scores systems, Lysholm-Tegner scores.</p><p><b>RESULTS</b>Seventy-nine patients were followed up, 41 patients in autograft groups averaged 39.6 months and 38 patients in allograft group averaged 37.4 months. The operation time of autograft group was (87 ± 11) minutes, that of allograft group was (55 ± 10) minutes (t = 15.732, P < 0.05). The time of postoperative fever of autograft group was (3.2 ± 1.4) days, that of allograft groups was (7.6 ± 5.3) days (t = 5.740, P < 0.05). The Lysholm scores of autograft group was 42 ± 7 before operation, and 89 ± 8 at final follow-up. The Lysholm scores of allograft group was 44 ± 6 before operation, and 87 ± 9 at final follow-up. There was statistic difference in both groups between before operation and final follow-up (t = 13.534 and 17.768, P < 0.05).But no statistic difference existed between the two groups (P > 0.05). The Tegner scores of autograft group was 2.9 ± 2.1 before operation, and 7.7 ± 1.2 at final follow-up. The Tegner scores of allograft group was 2.7 ± 1.4 before operation, and 7.1 ± 1.6 at final follow-up. There was statistic difference in both groups between before operation and final follow-up (t = 16.004 and 12.338, P < 0.05).No statistic difference existed between the two groups (P > 0.05). The KT2000 results showed that the anterior displacement of autograft groups was (10.7 ± 3.5) mm before operation and (5.0 ± 2.7) mm at final follow-up, the anterior displacement of allograft groups was (10.9 ± 2.9) mm before operation and (6.5 ± 2.4) mm at final follow-up, there was statistic difference between before and after operation in anterior displacement in two groups (t = 16.354 and 13.296 P < 0.05). There was no difference between two groups before operation and at final follow-up. Compared to before operation, the IKDC scores were improved greatly after operation (P < 0.05).</p><p><b>CONCLUSION</b>The clinical effect of arthroscopic ACL construction with allograft transplants is near to autograft.</p>


Subject(s)
Adult , Anterior Cruciate Ligament Reconstruction , Arthroscopy , Female , Humans , Knee Injuries , General Surgery , Male , Middle Aged , Prospective Studies , Tendons , Transplantation , Transplantation, Autologous , Transplantation, Homologous , Young Adult
3.
Acta Pharmaceutica Sinica ; (12): 1410-1415, 2009.
Article in Chinese | WPRIM | ID: wpr-344061

ABSTRACT

To prepare cyclosporine A (CyA) loaded block copolymer micelles and observe its release behaviors in vitro and pharmacokinetics in rats, methoxylpoly (ethylene glycol)-poly (D, L-lactide-co-glycolide) (mPEG-PLGA) was synthesized by ring-opening copolymerization of lactide and glycolide in the presence of methoxylpoly (ethylene glycol) (mPEG) as initiator. The structure of the mPEG-PLGA copolymer was confirmed with 1H NMR and FT-IR. The cyclosporine A loaded micelles (CyA-PM) were prepared by solvent evaporation method and their morphology was observed by the transmission electron microscope (TEM). The mean size and size distribution were determined by dynamic light scattering (DLS). The release behaviors in vitro and pharmacokinetics in rats were investigated by HPLC method using cyclosporine A injection commercial agent, sandimmune, as the reference. The obtained CyA-PM showed spherical shape with the core-shell structure, the mean particle sizes are in the range of 136.1-141.9 nm. The drug loading amount and entrapment efficiency were increased and the particle size became smaller with decreasing the ratio of acetone to water. With the increasing of the amount of cyclosporine A fed the drug loading increased, entrapment efficiency decreased and the particle size had no change. CyA-PM showed significant sustained release behave in vitro compared with sandimmune and only 9.7% of encapsulated cyclosporine A was released after 12 hours, the release characteristics was well fitted with Higuchi equation (r = 0.999). The Pharmacokinetics study at equal administration dosage (5 mg x kg(-1)) in rats showed the half-life (t1/2) of CyA-PM extended and the area under concentration-time curve (AUC) increased compared to sandimmune. The results also showed that cyclosporine A concentration-time data were all in accord with two compartment model. Cyclosporine A loaded mPEG-PLGA micelles showed obviously solubility enhancement, sustained release and overcome the side effect and toxicity of sandimmune resulted from solubiling agent-polyoxyethylene castor oil (Cremophor EL) and might be developed as a novel dosage form of cyclosporine A.


Subject(s)
Animals , Area Under Curve , Cyclosporine , Pharmacokinetics , Delayed-Action Preparations , Drug Carriers , Pharmacokinetics , Drug Compounding , Half-Life , Immunosuppressive Agents , Pharmacokinetics , Male , Micelles , Particle Size , Polyesters , Pharmacokinetics , Polyethylene Glycols , Pharmacokinetics , Polymers , Pharmacokinetics , Rats , Rats, Sprague-Dawley
4.
Acta Pharmaceutica Sinica ; (12): 756-760, 2008.
Article in Chinese | WPRIM | ID: wpr-277800

ABSTRACT

To optimize the formulation and preparation method of multivesicular liposome of thymopentin and to investigate its pharmacokinetics in rats, the multivesicular liposome of thymopentin was prepared by double emulsification method and the formulation was optimized by orthogonal design. The release characteristics of thymopentin from multivesicular liposome in PBS (pH 7.4) and in plasma were investigated. The multivesicular liposome of thymopentin labeled with fluorescein isothiocyanate was prepared by double emulsification method. Its pharmacokinetics was evaluated following intramuscular injection in rats. The optimal formulation of multivesicular liposome of thymopentin were formulated with 7.5% glucose in aqueous phase and 2.25 mol x L(-1) triolein, 2.68 mol x L(-1) DPPG and 16.96 mol x L(-1) DOPC in organic phase. The entrapment efficiency of the multivesicular liposome of thymopentin was above 85% and the mean particle size was about 22 microm. The in vitro release of thymopentin from multivesicular liposome in PBS (pH 7.4) and in plasma was found to be in a sustained manner. The release curves were fitted to Higuchi equation. The pharmacokinetics following intramuscular injection of the multivesicular liposome of thymopentin labeled with fluorescein isothiocyanate in rats showed that the peak concentration of thymopentin was lower and elimination of it was slower significantly than that of thymopentin labeled with fluorescein isothiocyanate solution in the same dose. The plasma concentration of thymopentin maintained above quantitative limitation at 120 h after administration of multivesicular liposome of thymopentin. The optimized formulation and preparation technology of multivesicular liposome of thymopentin with higher entrapment efficiency are feasible with good reproducibility. Multivesicular liposome of thymopentin showed significant sustained-release property following intramuscular injection in rats.


Subject(s)
Adjuvants, Immunologic , Pharmacokinetics , Animals , Area Under Curve , Delayed-Action Preparations , Drug Carriers , Drug Compounding , Drug Delivery Systems , Glucose , Chemistry , Liposomes , Chemistry , Male , Particle Size , Phosphatidylcholines , Chemistry , Phosphatidylglycerols , Chemistry , Rats , Rats, Sprague-Dawley , Thymopentin , Pharmacokinetics , Triolein , Chemistry
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