The Experts below are selected from a list of 303 Experts worldwide ranked by ideXlab platform
Hangon Choi - One of the best experts on this subject based on the ideXlab platform.
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effect of sodium chloride on the gelation temperature gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium
International Journal of Pharmaceutics, 2001Co-Authors: Chul Soon Yong, Jin Suck Choi, Qizhe Quan, Jongdal Rhee, Philsoo Oh, Hangon ChoiAbstract:Liquid Suppository systems composed of poloxamers and bioadhesive polymers were easy to administer to the anus and mucoadhesive to the rectal tissues without leakage after the dose. However, a liquid Suppository system containing diclofenac sodium could not be developed using bioadhesive polymers, since the drug was precipitated in this preparation. To develop a liquid Suppository system using sodium chloride instead of bioadhesive polymers, the physicochemical properties such as gelation temperature, gel strength and bioadhesive force of various formulations composed of diclofenac sodium, poloxamers and sodium chloride were investigated. The mixtures of P 407 (15%) and P 188 (15-20%) existed as a liquid at room temperature, but gelled at physiological temperature. Diclofenac sodium significantly increased the gelation temperature and weakened the gel strength and bioadhesive force, while sodium chloride did the opposite. Furthermore, the poloxamer gels with less than 1.0% of sodium chloride, in which the drug was not precipitated, were inserted into the rectum of rabbits without difficulty and leakage, and retained in the rectum of rats for at least 6 h. Our results suggested that a thermosensitive liquid Suppository system with sodium chloride and poloxamers was a more physically stable and convenient rectal dosage form for diclofenac sodium.
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effect of additives on the physicochemical properties of liquid Suppository bases
International Journal of Pharmaceutics, 1999Co-Authors: Hangon Choi, Mikyung Lee, Moonhee Kim, Chongkook KimAbstract:To investigate the effects of additives on the physicochemical properties of in situ gelling and mucoadhesive liquid Suppository base, gelation temperature, gel strength and bioadhesive force of liquid Suppository base, poloxamer 407 (P 407) and poloxamer 188 (P 188) (15/15%) were evaluated in the presence of following additives: solvent (ethanol, propylene glycol, glycerin), ionic strength-controlling agent (sodium chloride) and pH-controlling agent (hydrochloric acid, sodium monohydrogen phosphate, sodium dihydrogen phosphate). Among the additives studied, sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate increased to a great extent the gel strength and the bioadhesive force of P 407/P 188 (15/15%) with a decrease in gelation temperature. Glycerin slightly decreased the gelation temperature and slightly increased the gel strength and bioadhesive force. However, the addition of 1% of sodium chloride, sodium monohydrogen phosphate or sodium dihydrogen phosphate caused a greater than 60-fold increase in gel strength and over a tenfold increase in bioadhesive force with 2-4 degrees C decrease of gelation temperature within optimal range, compared with P 407/P 188 (15/15%) alone. On the other hand, ethanol, propylene glycol and hydrochloric acid increased the gelation temperature and slightly decreased the gel strength and the bioadhesive force. Taken together, these findings indicate that the effect of additives on the physicochemical properties of liquid Suppository bases depends on their bonding capacities, in that additives such as sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate having strong cross-linking bonds with the components of liquid Suppository base increase the strength and bioadhesive force of a gel compared to liquid Suppository base alone, while additives such as ethanol, propylene glycol and hydrochloric acid having weaker hydrogen bonding result in a weaker response. Thus, sodium chloride and sodium phosphates appear to be promising additives for in situ gelling and mucoadhesive liquid Suppository base, if used in adequate amounts.
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development of a thermo reversible insulin liquid Suppository with bioavailability enhancement
International Journal of Pharmaceutics, 1999Co-Authors: Mi Ok Yun, Hangon Choi, Jaehee Jung, Chongkook KimAbstract:The purpose of this work is to develop a thermo-reversible insulin liquid Suppository, which undergoes a phase transition to bioadhesive gels at body temperature and enhances the bioavailability of insulin. The effects of insulin and sodium salicylate on the physicochemical properties of a liquid Suppository composed of poloxamer P 407, P 188 and polycarbophil were investigated. The pharmacodynamic study and quantitative histological assessment of the rectal mucosa of rats were carried out after the dose of insulin-loaded liquid suppositories with different amounts of sodium salicylate into streptozotocin-treated rats. Only thermo-reversible insulin liquid Suppository [insulin/P407/P188/polycarbophil/sodium salicylate (100 (IU/g)/15/20/0.2/10%)] showed the optimal physicochemical properties and good safety in rats. It gave significantly lower plasma glucose levels, AUC0→4h (the area below basal glucose level) and Cnadir (the plasma glucose levels at the nadir) than did the solid and liquid suppositories without sodium salicylate in rats, indicating that the insulin from liquid Suppository with sodium salicylate could be well absorbed in rats due to the absorption enhancing effect of sodium salicylate. It is concluded that thermo-reversible insulin liquid Suppository [insulin/P 407/P 188/polycarbophil/sodium salicylate (100 (IU/g)/15/20/0.2/10%)], which was easy to administer without any pain during insertion and remained at the administered sites, could have a potential to be developed as a more convenient, safe and effective rectal delivery system of insulin.
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in situ gelling and mucoadhesive liquid Suppository containing acetaminophen enhanced bioavailability
International Journal of Pharmaceutics, 1998Co-Authors: Hangon Choi, Chongkook KimAbstract:Solutions of poloxamers and bioadhesive polymers were previously reported to undergo a phase transition to bioadhesive gels at body temperature. For the development of a convenient acetaminophen-loaded liquid Suppository which gels in situ after rectal administration, we studied the release and pharmacokinetics of acetaminophen delivered by the liquid Suppository systems composed of poloxamer P 188, P 407 and a bioadhesive polymer, polycarbophil. The release of acetaminophen was differently affected by the components of liquid Suppository such as P 188 and polycarbophil. P 188 showed little effect on the release rates of acetaminophen from liquid suppositories. However, polycarbophil significantly delayed the release kinetics of acetaminophen from a certain concentration due to strong gel strength and bioadhesive force. The release rates of acetaminophen did not significantly differ between no polycarbophil and 0.2% polycarbophil-loaded suppositories, while they began to decrease as the concentrations of polycarbophil increased higher than 0.4%. The analysis of release mechanism showed that the release of acetaminophen was proportional to the square root of time, indicating that acetaminophen might be released from the suppositories by Fickian diffusion. Liquid Suppository A [P 407/P 188/polycarbophil/acetaminophen (15:19:0.8:2.5%)], which was strongly gelled and mucoadhesive in the rectum, showed more sustained acetaminophen release profile than did other suppositories and gave the most prolonged plasma levels of acetaminophen in vivo. Liquid Suppository A also showed higher bioavailibility of acetaminophen than did the conventional formulation. Moreover, liquid Suppository A did not cause any morphological damage to the rectal tissues and remained stable for at least 6 month during storage. These results suggest that mucoadhesive and in situ gelling liquid Suppository could be a more effective and convenient rectal delivery system of acetaminophen.
Fotios M. Plakogiannis - One of the best experts on this subject based on the ideXlab platform.
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In Vitro Release of Testosterone from Suppository Bases and In Vivo Absorption Studies in Human Males
Journal of pharmaceutical sciences, 1993Co-Authors: Ali Babar, Hani M. Fares, Fotios M. PlakogiannisAbstract:Diffusion rates of testosterone from various Suppository bases with and without surfactants were determined. In a limited study, selected Suppository formulations were evaluated for efficiency of rectal absorption of testosterone in three male volunteers ranging in age from 25 to 30 years. Significant reductions in the ratios of urinary metabolites to free testosterone were observed with polyethylene glycol 1000, esterified (C10-C18) fatty acids, and theobroma oil-based samples.
Negin Khaki - One of the best experts on this subject based on the ideXlab platform.
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assessment of clinical efficacy of intranasal desmopressin spray and diclofenac sodium Suppository in treatment of renal colic versus diclofenac sodium alone
Urology, 2010Co-Authors: Ali Roshani, Siavash Falahatkar, Iradj Khosropanah, Zahra Atrkar Roshan, Tahmineh Zarkami, Maryam Palizkar, Seyedeh Atefeh Emadi, Marzieh Akbarpour, Negin KhakiAbstract:Objectives To determine the effect of the combination of intranasal desmopressin spray and diclofenac sodium Suppository on acute renal colic and compare it with diclofenac sodium Suppository alone. Methods A total of 150 patients aged 15-65 years referred to our hospital with acute renal colic were included in a double-blind controlled clinical trial study. Patients in group 1 received desmopressin, 40 μg intranasally plus diclofenac sodium Suppository 100 mg, and patients in group 2 received diclofenac sodium Suppository 100 mg plus a placebo spray consisting of normal saline 0.9%. Results Significant differences were found in the pain scores at 15 and 30 minutes between the 2 groups ( P P Conclusions According to our results, intranasal desmopressin plus diclofenac sodium Suppository caused prompt pain relief with significant decreases in pain scores after 15 and 30 minutes. We suggest that intranasal desmopressin spray is a useful supplemental therapy for renal colic in combination with nonsteroidal anti-inflammatory drugs, especially to reduce the use of opioids.
F.a. Ogunbona - One of the best experts on this subject based on the ideXlab platform.
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The efficacy of urine data in comparative bioavailability of proguanil after oral and rectal administration in man
African Journal of Biotechnology, 2006Co-Authors: Benjamin U. Ebeshi, Oluseye O Bolaji, Obiageri O. Obodozie, F.a. OgunbonaAbstract:The bioavailability of proguanil formulated as Suppository, was compared to the tablet formulation in a bid to evaluate the utility of the Suppository dosage form as means of administering proguanil in children and high-risk groups, such as sickle cell patients, who may not tolerate oral route of administration. The study was a completely randomized cross over involving administration of 200 mg of proguanil Suppository and tablet to twelve healthy volunteers. Biological fluids such as urine and blood were collected before and at predetermined time intervals following administration of the drug. The biological samples were analyzed for the unchanged proguanil using an earlier reported method. The relative bioavailability of proguanil Suppository as compared to the tablet dosage form was found to be about 61% from both urine and plasma data. The findings showed for the first time that proguanil Suppository could be sufficiently bioavailable and may therefore be useful in chemoprophylaxis of malaria in sickle cell patients and children, particularly under such conditions that made oral route become impracticable. Key words: Proguanil, tablets, suppositories, plasma and urine data, bioavailability.
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Suppository formulation of amodiaquine - In vitro release characteristics
Drug Development and Industrial Pharmacy, 1991Co-Authors: E. O. Akala, A. Adedoyin, F.a. OgunbonaAbstract:AbstractIn vitro release characteristics of amodiaquine hydrochloride from suppositories were studied. Results showed that water soluble bases (polyethylene glycol and glycero-gelatin) and water miscible synthetic fatty base (Witepsol W45) are superior to natural fatty bases (theobroma oil and shea butter) in terms of their ability to release amodiaquine hydrochloride.The in vitro availability of amodiaquine from polyethylene glycol Suppository (the Suppository which gave the highest rate and extent of release) was compared with its in vitro availability from tablets (CamoquinR) under the same experimental conditions. Polyethylene glycol Suppository was found to be superior to the tablet.
Y. Duman - One of the best experts on this subject based on the ideXlab platform.
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The release of isoconazole nitrate from different Suppository bases: in-vivo release of drug labelled with 99mTc in rabbits.
The Journal of pharmacy and pharmacology, 1995Co-Authors: Makbule Asikoglu, Gökhan Ertan, M. T. Ercan, Y. DumanAbstract:The influence of the Suppository bases on the in-vivo release of 99mTc-labelled isoconazole nitrate was investigated. The single-dose vaginal Suppository formulations for local treatment of vaginitis were prepared by a fusion method using polyethylene glycols, Witepsol H15, Novata BD and Cremao. Prepared vaginal suppositories containing solid-labelled substance were applied to the vagina of rabbits and at 0, 2 and 24 h after administration, the amounts of radioactivity in the vagina were detected by the SPECT Gamma Camera and the release rates of the drug were calculated. The percent released was found to be in the following order; polyethylene glycol (PEG) 6000 > PEG 4000 > Witepsol > PEG 1500 > Novata BD > Cremao. The results obtained in both in-vitro and in-vivo studies indicated that the vaginal Suppository of isoconazole nitrate prepared with polyethylene glycols could confidently be used in therapy.
