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A randomized openly comparative study between rifaximin suspension versus rifaximin pills for the eradication of Helicobacter pylori.

BACKGROUND: It has been recently shown that Rifaximin, although given as a suspension, plus omeprazole, may be a promising antibiotic against Helicobacter pylori (H pylori) and worthy of further study. AIM: We have therefore evaluated Rifaximin suspension versus Rifaximin pills, in a randomly openly allocated fashion study, in H pylori positive patients. METHODS: Twenty patients with upper gastrointestinal symptoms (M/F: 13/7, age range 28-68; mean 49.6 yrs) were found to have H. pylori associated gastritis. They were allocated in an open randomized study to two different treatment groups for two weeks: (A) Rifaximin suspension 1800 mg three times a day plus Omeprazole 20 mg twice a day (n = 10), (B): Rifaximin pills 1800 mg three times a day plus Omeprazole twice a day (n = 10). Symptoms such as pirosis, bloating, epigastric pain and nausea were recorded by diary card and were evaluated before and four weeks after stopping treatment. Patients were assessed by endoscopy, histology and urease testing at entry and four weeks after stopping treatments. All the twenty patients were available four weeks after stopping treatment. RESULTS: A statistically significant improvement of the symptoms were found overall after Rifaximin treatments for pirosis, bloating, epigastric pain (p < 0.001 respectively). A significant difference in the symptom's score at the end of the two treatments were recorded between the two groups for bloating alone (p < 0.070). A different and major fall in the neutrophils, between the two treatments was observed with Rifaximin pills compared to Rifaximin suspension. The same observation was obtained according to the intensity of H. pylori reaching an eradication rate of 40% and 60% for Rifaximin suspension versus Rifaximin pills plus omeprazole respectively. In conclusion, these data suggest that Rifaximin pills may be an effective antibiotic against H pylori and worthy of further study.

Adult↗

Stability of propylthiouracil in extemporaneously prepared oral suspensions at 4 and 25 degrees C.

The stability of propylthiouracil in two extemporaneously prepared suspensions at 4 and 25 degrees C was studied. Commercially available 50-mg propylthiouracil tablets were used to prepare suspensions in 1:1 Ora-Sweet:Ora-Plus and in 1:1 1% methylcellulose:Simple Syrup, NF, to yield a propylthiouracil concentration of 5 mg/mL. Each suspension was stored in 10 amber plastic prescription bottles, 5 of them at 4 degrees C and the other 5 at 25 degrees C. Three samples were taken from each bottle at 0, 7, 14, 28, 42, 56, 70, and 91 days for assay by stability-indicating high-performance liquid chromatography. More than 90% of the initial propylthiouracil concentration was retained in both suspensions for 70 days at 25 degrees C and for 91 days at 4 degrees C. There were no changes in physical appearance, color, or odor, and the pH remained essentially unchanged. Propylthiouracil 5 mg/mL in two extemporaneously prepared oral suspensions was stable for at least 70 days at 25 degrees C and for at least 91 days at 4 degrees C.

Antithyroid Agents↗

Effect of estrogen and tail-suspension on expression of osteocalcin mRNA in femur of ovariectomized rats.

We investigated the effect of estrogen (E2) and tail-suspension on expression of osteocalcin (OC) mRNA in the femur of ovariectomized rats. Five-week-old female Wistar rats were ovariectomized and divided into two groups: one group received estradiol dipropionate (OVX-E2), and the other received the vehicle (OVX). Each group was further divided into two subgroups, tail-suspended (S) and non-suspended (N), giving a total of four groups: OVX-E2-S, OVX-E2-N, OVX-S and OVX-N. After a 7-day suspension, femurs were excised, and OC mRNA levels were determined by Northern blot analysis. A significant decrease of OC mRNA in OVX-E2-N was observed when compared with that of OVX-N, indicating that E2 decreases the OC expression. Interestingly, tail-suspension further decreased the mRNA levels in both OVX-S and OVX-E2-S when compared with the levels of OVX-N and OVX-E2-N, respectively. Since glucocorticoids have been shown to decrease OC expression, we also measured the urinary excretion of corticosterone during the suspension period that reflects the serum levels of corticosterone, and found that it was increased by E2 and further increased by tail-suspension. These results indicate that estrogen and glucocorticoids exert additive effects in inhibiting OC expression in the rat femur.

Animals↗

Vaginal distribution of miconazole nitrate suspension from administration of a single vaginal insert.

OBJECTIVE: To perform a phase IV, open-label study of OVULE (Personal Care Products, Skillman, New Jersey) using magnetic resonance imaging (MRI) to describe the release, vaginal distribution and retention of a suspension containing miconazole nitrate in healthy female volunteers. STUDY DESIGN: Three parous and 3 nulligravid women were enrolled. Each subject self-inserted the OVULE on the MRI table and remained recumbent after insertion. MRI images were obtained every 15 minutes for 1 hour and then at predetermined intervals following suspension insertion until the suspension was no longer identified. RESULTS: Placement of the OVULE was in the upper vagina in 4 subjects and in the lower vagina in 1 subject, and the Ovule was expelled in 1 subject. Average time to capsule shell dissolution was 36 minutes. Average time to maximum vaginal mucosal coverage by the suspension was 49 minutes. The average time at which the suspension was last seen in the vagina was 5 hours and 53 minutes. CONCLUSION: MRI can be used to noninvasively quantify the intravaginal spread of a therapeutic antifungal agent. Understanding the intravaginal spread of antifungal agents may lead to further optimization of antifungal preparations as well as to better patient instructions.

Administration, Intravaginal↗

Studies on the development of taste-masked suspension of chloroquine.

A non-bitter chloroquine suspension formulation for pediatric use was prepared in the form of an ion-pair of chloroquine with pamoic acid. Various parameters involved in the formulation of a stable and palatable suspension have been optimized. The suspension was characterized for particle size analysis, viscosity, physical and chemical stability and taste. Release of chloroquine from the ion-pair conducted as dissolution rate studies in simulated gastric media showed near to 100% release instantaneously. In-vivo bioavailability study conducted in albino rats indicated comparable bioavailability of chloroquine from the suspension with that of chloroquine phosphate syrup taken as standard. Stability study conducted over a period of 3 months showed the intactness of the ion-pair and the tasteless behavior of the suspension throughout the period of storage.

Animals↗

Effect of two-week tail suspension on forelimb and hindlimb [correction of hindlimd] small arteries in rats.

This study was aimed at comparing the effect of 2-week tail suspension on the characteristics of median artery and saphenous artery isolated from forelimb and hindlimb, accordingly. The segments of arteries were mounted in two-channel myograph for recording their isometric wall tension. In post-suspension rats segments of saphenous artery showed augmented sensitivity to noradrenaline and serotonin. More than two-fold decreased of EC50 was observed both before and after endothelium removal. Along with that, the sensitivity of median artery segments to vasoconstrictors was similar in post-suspension and control rats. However, the diameter of relaxed median artery in post-suspension rats was increased. Relaxation to acetylcholine compared to controls was augmented in both vascular regions of post-suspension rats being more pronounced in saphenous artery preparations.

Acetylcholine↗

Canine kidney cells: I. Neutral lipids, phospholipids and fatty acids of SV40 transformed canine kidney cells in suspension and monolayer culture.

Differences in lipid composition and the effects of monolayer and suspension culture on SV40 virus transformed canine kidney cells and their plasma membranes were studied. Plasma membranes from monolayer and suspension cultures of SV40 transformed canine kidney cells were isolated by the Warren fluorescein-mercuric acetate technique. Free cholesterol was the major neutral lipid extracted from the whole cells and plasma membranes of all these cultures. Triglyceride increased about 6- to 50-fold in suspension grown whole cells and their plasma membranes compared to those from monolayer cultures. The mu moles of total neutral lipids and phospholipids are elevated in plasma membranes compared to whole cells from monolayer cultures but are similar in suspension cultures. The distribution of fatty acids in the major lipid classes of plasma membranes and whole cells generally follow the composition of calf serum used in the culture media. INDEX WORDS: SV40, plasma membranes, transformed cells, canine kidney cells, neutral lipids, phospholipids, monolayer culture, suspension culture.

Animals↗

[A new method of preparation of doxorubicin-in-oil suspension using ultrasonificator attached with Cuphorn].

The property of selective deposition of oily contrast medium, Lipiodol (LPD), in tumor tissue was utilized for targetting intraarterial infusion chemotherapy for hepatic cancers. For this therapy anti-cancer agents need to be suspended in LPD. In this report the new suspension device using ultrasonificator attached with Cuphorn was studied. Doxorubicin (Dx) was stable to ultrasonification for 1 hour. Ten mg/ml of Dx was mixed with LPD and this mixture was treated 2 times for 5 minutes with the ultrasonification method. This procedure was simple and sterile, as the commercially used Dx vials into which LPD was injected were set in the Cuphorn and ultrasonificated just as sealed. Microscopic examination of the suspension showed uniform dispersion of Dx particles without formation of aggregates. Dx particles were finely and regularly fragmented. In vitro the suspensions showed a gradual release of Dx from LPD to water phase. In one case with hepatocellular carcinoma received intraarterial infusion of this suspension, the size of the tumor and serum level of alpha-fetoprotein was prominently decreased. This ultrasonification method was simple and convenient to prepare Dx-in-oil suspension.

Carcinoma, Hepatocellular↗

[The possible use of PKZh-type devices (liquid purity control devices) in the analysis of cell suspensions].

PKZh means "device for liquid purity control". A possibility is considered to use the native PKZh type device for carrying out quantitative analyses of cellular suspension components, for routine bacterial suspension, agglutinated bacterial suspension and erythrocyte suspension. The flowing photometric principle of particle recording, used in the device, allows to analyse biological suspensions with small amounts of components. The device provides a differential count of some cells and their conglomerates in six dimensional ranges, within the frames of 1-25 micron or higher. The time consumption for one sample analysis is 10-15 seconds.

Animals↗

A comparative trial of clotrimazole troches and oral nystatin suspension in recipients of renal transplants. Use in prophylaxis of oropharyngeal candidiasis.

An open study designed to compare the effectiveness and safety of clotrimazole troches with nystatin oral suspension in the prevention of oropharyngeal candidiasis was conducted. This study was performed as the troche form of clotrimazole was easier to administer and less costly than nystatin oral suspension. Sixty assessable patients were randomized to receive either clotrimazole troches (n = 32) or nystatin oral suspension (n = 28) for a 60-day period after receiving a renal allograft. The two groups were comparable in age, sex, type of transplant, and amount of immunosuppression. Both regimens were 100% effective in preventing the development of thrush in the patients studied. Adverse effects were infrequently seen in either group (one case of mild nausea in the clotrimazole group and three cases in the nystatin group). One patient chose to withdraw from the clotrimazole group, and eight patients withdrew from the nystatin group before completing 60 days of therapy (P = .002). Reasons given for withdrawal were the unpleasant taste of the drugs, or an inability to comply with the protocol. The cost of clotrimazole troches in the prophylactic doses given in this study was approximately one tenth that of nystatin oral suspension. Clotrimazole troches are effective, less expensive, and easier to self-administer than nystatin oral suspension.

Administration, Topical↗

Effect of pectin and kaolin on bioavailability of co-trimoxazole suspension.

Bioavailability of co-trimoxazole suspension was determined with and without concurrent administration of pectin and kaolin in 8 volunteers. Twenty ml suspension of co-trimoxazole containing 160 mg trimethoprim (TMP) and 800 mg sulphamethoxazole (SMX) and co-trimoxazole suspension along with 20 ml of pectin-kaolin suspension were administered in a random order with 7 days interval. Plasma estimation of trimethoprim and sulphonamide was carried out at serial intervals. Area under curve (AUC) and Cmax of TMP were significantly higher when co-trimoxazole suspension alone was used. No statistically significant changes were observed in case of sulphamethoxazole. Clinical study is necessary to verify whether concurrent administration of co-trimoxazole and pectin-kaolin leads to loss of antibacterial efficacy.

Adult↗

Stability of propranolol hydrochloride suspension compounded from tablets.

The stability of a propranolol hydrochloride suspension compounded from commercially available tablets was studied. Propranolol hydrochloride 10-mg tablets were triturated to a powder and incorporated into a commercially available suspension vehicle to yield a suspension with a theoretical propranolol hydrochloride concentration of 1 mg/mL. The suspension was divided into portions and stored in amber glass bottles at either room (25 degrees C) or refrigerated (2 degrees C) temperature for four months. The concentration of propranolol hydrochloride in the samples was determined by a stability-indicating, high-performance liquid chromatographic (HPLC) assay at 0, 30, 60, 90, and 120 days. Also at these times, the pH of the samples was measured, and the samples were inspected visually for evidence of microbial growth and ease of resuspension. The concentration of propranolol hydrochloride in the samples remained within 90% of the initial concentration throughout the study period. No important changes in the pH of the samples and no visible evidence of microbial growth were noted. This extemporaneous suspension of propranolol hydrochloride compounded from commercially available tablets is stable for at least four months when stored at room or refrigerated temperature.

Chromatography, High Pressure Liquid↗

Stability of ampicillin trihydrate suspension in amber plastic oral syringes.

The stability of ampicillin trihydrate oral suspension stored in amber plastic oral syringes was studied. Commercially available ampicillin trihydrate powder for oral suspension was reconstituted according to manufacturer's instructions and drawn into 5-mL amber polypropylene plastic oral syringes. The syringes were divided into groups and stored at -20, 4, 25, 60, or 80 degrees C. Powder from two additional lots was similarly reconstituted and packaged and stored at 80 degrees C only to assess interlot variability. Immediately after reconstitution and at specified times during storage, three syringes at each storage temperature were removed and their contents analyzed for ampicillin trihydrate concentration by a spectrophotometric assay. Samples stored at frozen (-20 degrees C) or refrigerated (4 degrees C) temperature retained at least 90% of the initial ampicillin concentration throughout the 47-day study period. Samples stored at room temperature retained at least 90% of the initial ampicillin concentration for 30 days and exhibited an apparent zero-order degradation rate. Samples stored at heated temperatures (60 and 80 degrees C) exhibited an apparent first-order degradation process, with the concentration of ampicillin decreasing to less than 90% of initial concentration within two hours. Reconstituted ampicillin trihydrate powder for oral suspension is stable for at least 30 days when stored at room, refrigerated, or frozen temperature in the amber plastic oral syringes studied. The expiration dates recommended by the manufacturer for ampicillin trihydrate suspension stored in its original container can also be used for reconstituted suspension stored in these amber plastic syringes.

Ampicillin↗

Methods of infesting sheep with gastro-intestinal nematodes after cryopreservation: dosing of larvae in gelatin capsules compared to dosing of larvae in water suspension.

Cryopreservation of the infective larvae (L3) of nematodes is being used increasingly for the routine maintenance of pure strains of nematodes in the laboratory. Gelatin capsules are frequently used to administer the L3 of nematodes to sheep, but with some nematode species this method usually does not give good results with cryopreserved larvae. The development in sheep of cryopreserved L3 of Trichostrongylus spp. and other ovine nematodes was compared when the larvae were administered either in a suspension or in gelatin capsules with or without the use of CuSO4 to stimulate the oesophageal groove reflex. Significantly larger numbers of cryopreserved L3 developed when dosed per os in suspension than when the L3 were dosed in gelatin capsules. Stimulation of the oesophageal groove did not appear to affect the numbers of worms that developed from L3 dosed in suspension. It is speculated that L3 in suspension bypass the rumen to go directly into the abomasum, while those in gelatin capsules enter the rumen, thus closely approximating the natural infestation of grazing ruminants. In these trials, however, only cryopreserved L3 were used. Sufficient numbers of cryopreserved L3 of Trichostrongylus falculatus and T. colubriformis in suspension developed, so that it seems unlikely that laparotomy will be required for routine infestations in the laboratory.

Animals↗

Bioavailability of sulfathiazole from flocculated and deflocculated suspensions and its implications.

Flocculation is commonly used to stabilize pharmaceutical suspensions. Flocculated and deflocculated suspensions of sulfathiazole were administered to healthy human volunteers. Bioavailability from these two types of suspensions was studied from urinary free drug excretion. Bioavailability was significantly lower from flocculated suspensions. The study indicates the necessity of studying all flocculated drug suspensions for bioavailability data.

Biological Availability↗

Stability of sterile dexamethasone acetate suspensions and dexamethasone sodium phosphate injections submitted by U.S. hospitals.

The stability of sterile dexamethasone acetate suspensions and dexamethasone sodium phosphate injections that had been stored in hospital pharmacies across the United States was studied. Through a voluntary FDA drug stability program, all hospital pharmacies in the United States were asked in October 1981 to complete a response card indicating information about the sterile dexamethasone acetate suspensions and dexamethasone sodium phosphate injections they had in stock. Based on the responses, FDA selected 21 samples of sterile dexamethasone acetate suspensions (representing two manufacturers) and 114 samples of dexamethasone sodium phosphate injection (representing 11 manufacturers). These samples were analyzed for identification, pH, and strength. All samples of sterile dexamethasone acetate suspension met USP requirements. Eleven samples of dexamethasone sodium phosphate injection representing 10 lots from three manufacturers failed USP assay requirements for strength. All samples that failed to meet strength requirements showed evidence of degradation by oxidation. Sterile dexamethasone acetate suspensions appear to be stable when stored under actual marketplace conditions, but there is a problem with the shelf-life stability of dexamethasone sodium phosphate injections made by some manufacturers.

Dexamethasone↗

A comparison of the quantitative suspension tests for the assessment of disinfectants.

The germicidal effect of two disinfectant standards has been determined by three quantitative suspension tests: the Dutch Standard-Suspension Test, the French AFNOR test, and the in vitro test. Particularly in case of Pseudomonas aeruginosa the germicidal-effect values found according to the three methods differ in a significant way (Tables 1 and 2). The only factors that could explain these differences, since they are not the same in the three techniques, are the preparation of the bacterial suspension and the diluent of the disinfectant solution. Through this the composition of the reaction mixture is different: in the in vitro test only 0.0085% NaC1 and 0.001% Tryptone are contained, in the AFNOR test the same constituants are ten times more concentrated and in the Standard-Suspension Test 0.882% NaC1 and 0.0306% albumin are present. If in the same trial these substances have been incorporated in the final concentration above-mentioned, then germicidal-effect values equal to those of the original tests have been obtained (Table 3). The disinfectant diluent and the bacterial suspension fluid have to be the main factors responsible for the differences in activity found by the three testing methods. In our opinion the in vitro test gives the clearest picture of the anti-bacterial properties of a disinfectant since in this test the less addition of extraneous matter is encountered.

Albumins↗

Comparative bioavailability of chlorpropamide tablet and suspension formulations.

The bioavailability of a chlorpropamide tablet formulation chlorpropamide tablet formulation was assessed by comparing it to a reference suspension of chlorpropamide. Eighteen healthy adult men received chlorpropamide 250 mg as a tablet (Diabinese, Pfizer) and suspension in an open two-way crossover study of Latin-square design with a 14-day washout period between treatments. Serial blood samples were obtained by venipuncture for 96 hours for chlorpropamide serum concentration determinations. Serum glucose concentrations were determined at 0, 0.5, 1, 2, and 4 hours. The area under the serum chlorpropamide concentration-time curve (AUC), peak serum chlorpropamide concentration (Cmax), time to Cmax, and mean glucose concentration at each time point for each treatment were compared using a two-tailed Student's t test for paired data (p less than 0.05). Microrate constants for a two-compartment model for oral absorption computed using nonlinear regression were also compared. There were no significant differences between the two formulations regarding AUC, Cmax, time to Cmax, and hypoglycemic response. The absorption rate for the tablet was significantly greater than for the suspension. The results suggest that the oral chlorpropamide tablet and reference suspension are bioequivalent. Although the tablet had a faster absorption rate than the suspension, this probably is not clinically important since both formulations similarly decreased serum glucose concentration.

Adult↗