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Topical application of caffeine loaded Eudragit E microspheres
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TOPICAL APPLICATION OF CAFFEINE LOADED EUDRAGIT E MICROSPHERES DCengiz, N.Tenmcr Ankara Universily.Faculty of Pharmacy. Depertment of Phaneceutical Technology,Tendogsn - 06100 Ankara, Turkey In recent years, different oollotdal psntioles such as mlcmoapsuless, mkxosphems, ltpceomes and niozomes have been used in dermel and cosmetic formulettons as drug carder systems. These new systems can lmfnwe and uwtml the drug retease from conventional toptcai formulsttons. Caffeine which Is a methylxanthlne dedvative can apply topically to stimulate llpolyses In epidermal fat cells (I). The alm of the work ls to pmpara the topical fonnulatlons containing caffetne mfcmspheres to provw the extented release of the core material in the tmatment nf cellulke. The microspheres were prepared using Eudmgt E as a coating material in various corn to wall ratios. The prepared mlcm@ems wem evaluated for drug axttent. parttde size dbblbution and diswlution studies. In vltm dissokttbn studies were patformed using the Paddle Method (USP Xmll) and a apadmphotomatrfcai method of caffeine assay was chosen (X=333). After than, me caffeine miauspheres wem Armulatad In tvm dlffemnt semlsolld bases as w/o emulsion and emulgel basas.The In bb retease of microsphered csffeine topical folmulatians wa abo studied.
TESTING THE EFFICACY OF METRONIDAZOLCONTAINING LIPOGEL IN TREATMENT OF PERIODONTAL DISEASE
Free following and sphadcal mlcrosphems wem oMainad. The in vitro mteasapmfllesofceffeinefromEudragltEmbwphemswasshewn bud affact nd folf&rtg slow mlaase. An ln~N&rtg of the corewall rat&e gave a bum dlssofmfon due to the lncreastng of the thickness ofthe rn&qham wall. The emutgel base shawn the higher mlease rate compamd to the w/o base. We atsn conctuded that the drug release was dapand on the concentratton of coating material in emalgat fomwlatton. r” Esstg D. D.L. Instill. and Van Hendd.. ‘Effects d Ceffeine lngsstionon Muscle Glywgen and Lipid During Leg Ergometer Cycling’. Int. J. Sports Medtdne, 1,6e-gq 1980.
MO”‘“,”Tg;kic-~dojicic’. Milomir Varjacic’, Irma Jovanovic’, LrkN k ‘. Institute for Pbarrnacy’, Dental Clinic2 ,“Mesanovic” yharrnacy, e o slna , ZPM and Institute for Microbiolo b?.PJ .’ 41 htaty Medical Academy, Cmotravska 17, 11& 0 Beograd, Yugoslavia The aim of our work was to test the efficacy of a newly-formulated muwadhesive compound containing 25% metronidaxol in an organic lipogel-type vehicle, in treatment of periodontal disease. Pure base metronidazol, particle size 0.15, was incorporated into the vehicle according to the manufacturing principles for suspension-type compounds. The vehicle contains a complex emulsifier, sesame oil, and an appropriate gelifying compound. Analyses showed that a compound with ambiphyl qualities is formed ex-tempore, in contact with a mucous fluid as the aqueous phase. The advantage of such compounds is their expression of slow-release characteristics due to a gradual washout of only the layer in contact with the mucus. The compound possesses tixotropic rheological characteristics enabling good tilling of periodontal pockets, and the ambiphyl layer formed expresses an exceptional muwadhesivity. In vitro testing with membrane-free diffusion method (Peptococcus anaerohius strain) show an exceptional slow-release effect of the compound. In vivo our original formulation proved to be efficient in treatment of periodontal pocket anaerobic infection within 30 days. In all patients (25) no anaerobic strain was isolated from periodontal pocket on day 30. During the study, no metronidazol-resistent anaerobic strain was isolate.
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Drug release from responsive polymer membrane T.‘, B. Svarfva?, M. Wskilahti’, M. Karhu’, P. Paronen’
RECOVERY OF POLYHYDROXYALKANOATES AND THEIR USE IN TEE CONTROLLED ANTIBIOTIC DELIVERY FOR TFIE TREATMENT OF BONE INFECTIONS F. Tilresin, i. Gtbsel, F. Ekgioglu, F. Korkusua, and V. Hasuct Middle East Technical University, Department of Biological Sciences, Biotechnology Research Unit, 06531, Ankara, Turkey
and K. Jiirvinen’ ‘Department of Pharmaceutics, University of Kuopio, Finland ‘Department of Polymer Technology&o Akademi University, Finland Permeability properties of porous poly(vinylidene fluoride) (PVDF) membranes grafted with poly(acrylic acid) (PAA) are affected by ionic strength and pH. In this study, propranolol HCI, timolol hemihydrate, atenolol, sotalol HCI and dexmedetomidine HCI were adsorbed onto the PVDF-PAA membrane by soaking the membranes in pH 7.0 phosphate buffer with different ionic strengths (0.05, 0.15 and 0.40). The release of model drugs from the PVDF-PAA membrane in pH 7.0 phosphate buffer (u = 0.05 and p = 0.40) was studied in vitro. The drug release in viva was studied by applying a circular membrane to both eyes of pigmented rabbits in the lower conjunctival sac. Tbt membranes were removed from the eyes at preset time intervals and the drug content in the membranes was determined. When propranolol HCI, timolol and dexmedetomidine HCI were adsorbed onto the membrane at constant ionic strength (p - 0.05 orp = 0.40), the release into buffer solution at u = 0.40 was significantly faster than the release into solution at p = 0.05 in vim. The release rates of propmnolol and timolol at constant ionic strength decreased with increasing ionic strength of adsorption medium both in v&o andin ViVO. In conclusion, the results clearly show that changes in environmental ionic strength affect the cation exchange process of PVDF-PAA membrane. The financial support from TEKES is gratefully acknowledged. This study was supported also by grants from The Finnish Cultural Foundation and The Save Foundation for Advanced Technology.
Polyhydroxyalkanoates (PHAs) are naturally occuring biodegradable polyesters produced by many bacteria. A random copolyester of 3hydroxybutyrate-3-hydroxyvalerate, P(3HB3HV) and 3-hydroxybutyrate -cl-hydroxybutyrate, P(3HB-W3), were produced by the fermentation of Alcaligenes eutrophur and Alcaligene~ Iarm. Polymers were extracted and purified from the microbial biomass and used in the construction of an implant containing sulperazone ss an antibiotic. In vitro release of implants with different drug loadings were conducted in PBS at 37’C. Release from 50% loaded P(3HB-3HV) and P(3HB-4HB) rods showed that the drug was completely released in less than 3 days, To retard the rate, dip coatings of these rods using the same polymer solution were done and the release profiles were obtained. Cumulative release was about 70 K of its initial content at the end of 12 days. In viva studies were conducted with male New Zealand rabbits (152.0 kg). To test the performance in vivo, the rods were implanted: i) right legs; antibiotic loaded rods, and ii) left legs; drug&e PHA rods. At 2 week intervals, the rods were retrieved and biodegradation, drug release, morphological and histopathological investigations were carried out. Following determination of performance in healthy animals, rods were implanted 3 weeks after bacterial inoculation (Sr+,v~ococcur ourens, 0.5 mL, I .0x106 CFU/mL) of right hind leg. Thereafter the rabbits were sacrificed at l”, 3’, and 6” week and radiological, histopathological and microbiological results were obtained. Preliminary results showed that PHA rods are effective in treating experimental osteomyelitis with a very mild foreign body tissue reactions at the implant site.
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TOPICAL APPLICATION OF CAFFEINE LOADED EUDRAGIT E MICROSPHERES DCengiz, N.Tenmcr Ankara Universily.Faculty of Pharmacy. Depertment of Phaneceutical Technology,Tendogsn - 06100 Ankara, Turkey In recent years, different oollotdal psntioles such as mlcmoapsuless, mkxosphems, ltpceomes and niozomes have been used in dermel and cosmetic formulettons as drug carder systems. These new systems can lmfnwe and uwtml the drug retease from conventional toptcai formulsttons. Caffeine which Is a methylxanthlne dedvative can apply topically to stimulate llpolyses In epidermal fat cells (I). The alm of the work ls to pmpara the topical fonnulatlons containing caffetne mfcmspheres to provw the extented release of the core material in the tmatment nf cellulke. The microspheres were prepared using Eudmgt E as a coating material in various corn to wall ratios. The prepared mlcm@ems wem evaluated for drug axttent. parttde size dbblbution and diswlution studies. In vltm dissokttbn studies were patformed using the Paddle Method (USP Xmll) and a apadmphotomatrfcai method of caffeine assay was chosen (X=333). After than, me caffeine miauspheres wem Armulatad In tvm dlffemnt semlsolld bases as w/o emulsion and emulgel basas.The In bb retease of microsphered csffeine topical folmulatians wa abo studied.
TESTING THE EFFICACY OF METRONIDAZOLCONTAINING LIPOGEL IN TREATMENT OF PERIODONTAL DISEASE
Free following and sphadcal mlcrosphems wem oMainad. The in vitro mteasapmfllesofceffeinefromEudragltEmbwphemswasshewn bud affact nd folf&rtg slow mlaase. An ln~N&rtg of the corewall rat&e gave a bum dlssofmfon due to the lncreastng of the thickness ofthe rn&qham wall. The emutgel base shawn the higher mlease rate compamd to the w/o base. We atsn conctuded that the drug release was dapand on the concentratton of coating material in emalgat fomwlatton. r” Esstg D. D.L. Instill. and Van Hendd.. ‘Effects d Ceffeine lngsstionon Muscle Glywgen and Lipid During Leg Ergometer Cycling’. Int. J. Sports Medtdne, 1,6e-gq 1980.
MO”‘“,”Tg;kic-~dojicic’. Milomir Varjacic’, Irma Jovanovic’, LrkN k ‘. Institute for Pbarrnacy’, Dental Clinic2 ,“Mesanovic” yharrnacy, e o slna , ZPM and Institute for Microbiolo b?.PJ .’ 41 htaty Medical Academy, Cmotravska 17, 11& 0 Beograd, Yugoslavia The aim of our work was to test the efficacy of a newly-formulated muwadhesive compound containing 25% metronidaxol in an organic lipogel-type vehicle, in treatment of periodontal disease. Pure base metronidazol, particle size 0.15, was incorporated into the vehicle according to the manufacturing principles for suspension-type compounds. The vehicle contains a complex emulsifier, sesame oil, and an appropriate gelifying compound. Analyses showed that a compound with ambiphyl qualities is formed ex-tempore, in contact with a mucous fluid as the aqueous phase. The advantage of such compounds is their expression of slow-release characteristics due to a gradual washout of only the layer in contact with the mucus. The compound possesses tixotropic rheological characteristics enabling good tilling of periodontal pockets, and the ambiphyl layer formed expresses an exceptional muwadhesivity. In vitro testing with membrane-free diffusion method (Peptococcus anaerohius strain) show an exceptional slow-release effect of the compound. In vivo our original formulation proved to be efficient in treatment of periodontal pocket anaerobic infection within 30 days. In all patients (25) no anaerobic strain was isolated from periodontal pocket on day 30. During the study, no metronidazol-resistent anaerobic strain was isolate.
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300
Drug release from responsive polymer membrane T.‘, B. Svarfva?, M. Wskilahti’, M. Karhu’, P. Paronen’
RECOVERY OF POLYHYDROXYALKANOATES AND THEIR USE IN TEE CONTROLLED ANTIBIOTIC DELIVERY FOR TFIE TREATMENT OF BONE INFECTIONS F. Tilresin, i. Gtbsel, F. Ekgioglu, F. Korkusua, and V. Hasuct Middle East Technical University, Department of Biological Sciences, Biotechnology Research Unit, 06531, Ankara, Turkey
and K. Jiirvinen’ ‘Department of Pharmaceutics, University of Kuopio, Finland ‘Department of Polymer Technology&o Akademi University, Finland Permeability properties of porous poly(vinylidene fluoride) (PVDF) membranes grafted with poly(acrylic acid) (PAA) are affected by ionic strength and pH. In this study, propranolol HCI, timolol hemihydrate, atenolol, sotalol HCI and dexmedetomidine HCI were adsorbed onto the PVDF-PAA membrane by soaking the membranes in pH 7.0 phosphate buffer with different ionic strengths (0.05, 0.15 and 0.40). The release of model drugs from the PVDF-PAA membrane in pH 7.0 phosphate buffer (u = 0.05 and p = 0.40) was studied in vitro. The drug release in viva was studied by applying a circular membrane to both eyes of pigmented rabbits in the lower conjunctival sac. Tbt membranes were removed from the eyes at preset time intervals and the drug content in the membranes was determined. When propranolol HCI, timolol and dexmedetomidine HCI were adsorbed onto the membrane at constant ionic strength (p - 0.05 orp = 0.40), the release into buffer solution at u = 0.40 was significantly faster than the release into solution at p = 0.05 in vim. The release rates of propmnolol and timolol at constant ionic strength decreased with increasing ionic strength of adsorption medium both in v&o andin ViVO. In conclusion, the results clearly show that changes in environmental ionic strength affect the cation exchange process of PVDF-PAA membrane. The financial support from TEKES is gratefully acknowledged. This study was supported also by grants from The Finnish Cultural Foundation and The Save Foundation for Advanced Technology.
Polyhydroxyalkanoates (PHAs) are naturally occuring biodegradable polyesters produced by many bacteria. A random copolyester of 3hydroxybutyrate-3-hydroxyvalerate, P(3HB3HV) and 3-hydroxybutyrate -cl-hydroxybutyrate, P(3HB-W3), were produced by the fermentation of Alcaligenes eutrophur and Alcaligene~ Iarm. Polymers were extracted and purified from the microbial biomass and used in the construction of an implant containing sulperazone ss an antibiotic. In vitro release of implants with different drug loadings were conducted in PBS at 37’C. Release from 50% loaded P(3HB-3HV) and P(3HB-4HB) rods showed that the drug was completely released in less than 3 days, To retard the rate, dip coatings of these rods using the same polymer solution were done and the release profiles were obtained. Cumulative release was about 70 K of its initial content at the end of 12 days. In viva studies were conducted with male New Zealand rabbits (152.0 kg). To test the performance in vivo, the rods were implanted: i) right legs; antibiotic loaded rods, and ii) left legs; drug&e PHA rods. At 2 week intervals, the rods were retrieved and biodegradation, drug release, morphological and histopathological investigations were carried out. Following determination of performance in healthy animals, rods were implanted 3 weeks after bacterial inoculation (Sr+,v~ococcur ourens, 0.5 mL, I .0x106 CFU/mL) of right hind leg. Thereafter the rabbits were sacrificed at l”, 3’, and 6” week and radiological, histopathological and microbiological results were obtained. Preliminary results showed that PHA rods are effective in treating experimental osteomyelitis with a very mild foreign body tissue reactions at the implant site.