Gastroprotective effect of standardized extract of Amukkara choornam on experimental gastric ulcer in rats.

Amukkara choornam ethanolic extract (ACE) was investigated for phytochemical screening, content of total phenolics and flavonoids, in vitro radical scavenging activity (RSA), quantification of various antiulcer marker compounds (i.e., eugenol, piperine, trans-caryophyllene, and withaferine A) by a validated HPTLC method, and evaluated for its in vivo gastroprotective ability against ethanol (EtOH)-induced and pylorus ligation (PL)-induced ulcer models in rats. Phytochemical screening revealed the presence of flavonoids, saponins, phenols, bitter principles, and steroids. Total phenolic and flavonoid content was found to be 61.12 ± 0.72 mg GAE/g of ACE and 24.06 ± 1.07 mg RE/g of ACE, respectively; this was found to be very high in plant extracts showing very good antioxidant and antiulcerogenic effect. RSA of ACE appeared significantly (p < 0.05) lower than that of ascorbic acid (AA), but higher than that of ranitidine (RAN). In vivo the pretreatment of rats with RAN (100 mg/kg) and 50, 100, and 200 mg/kg doses of ACE significantly reduced the ulcer index in a dose-dependant manner in both the models by blocking lipid peroxidation and by significant increases in superoxide dismutase and catalase activity. But rats treated with AA (200 mg/kg) did not have any effect on the ulcer induced by EtOH or PL as it has very good in vitro and in vivo antioxidant activity. HPTLC analysis showed the presence of 0.198 ± 0.01 µg/g, 0.754 ± 0.06 mg/g, 3.50 ± 0.04, and 0.854 ± 0.04 µg/g of eugenol, piperine, trans-caryophyllene, and withaferine A per gram of Amukkara choornam (AC). So the antiulcerogenic activity of ACE might be due to a possible synergistic antioxidant, supported by the holistic approach of polyherbal formulations, i.e., systematism, multi-target and multi-channel owing to their complex chemical constituents and antihistaminic-like effects.

[Comparative evaluation of the anionic superdisintegrant incorporation mode on the quality of ranitidine tablets]. / Evaluarea comparativa a modului de încorporare al unui superdezagregant anionic asupra calitatii comprimatelor cu ranitidina.

UNLABELLED: The present study was based on the impact of the superdisintegrants incorporation mechanism on the immediate realese of the tablets final performances. The aim was the selection of the working method to obtain Ranitidine 150 mg tablets with the desiderate quality and in reproducible conditions. MATERIAL AND METHODS: The effect of the incorporation mode of sodium starch glycolate on the aspect, granules size distribution and flowing properties of the lubricated product, and also the weight uniformity, hardness, disintegration, friability, and dissolution of the Ranitidine 150 mg tablets prepared by dry granulation was studied. The addition mode of the disintegrant was realized in three ways: intragranular, extragranular, and distributed equally between the two phases. The distribution range for the tablets weight was established. Relative standard distribution was calculed for the weight and hardness of the uncoated tablets. RESULTS: The powder flow and, implicit, the weight uniformity of the uncoated tablets was positive influenced by the extragranular incorporation of the superdisintegrant. The disintegration time was identical for all the three disintegrant addition modes, and the hardness and the friability were not significantly influenced by working method, the obtained values were similar. For the developed formulations, the percent of the ranitidine dissolution was high, but higher in the extragranular incorporation. CONCLUSIONS: For the product quality the extragranular addition mode seemed the best method to incorporate the superdisintegrant.

Gastroprotective effect of standardized leaf extract from Argyreia speciosa on experimental gastric ulcers in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Argyreia speciosa (L.f), Sweet (Family Convolvulaceae) is used traditionally in Indian System of Medicine as aphrodisiac, rejuvenating agent, intellect promoting agent, brain tonic and in the therapy of hepatomegaly, diabetes and chronic ulcer. AIM OF THE STUDY: To study the gastroprotective effect of standardized butanol fraction of Argyreia speciosa leaf (ASE). MATERIALS AND METHODS: The butanol fraction of Argyreia speciosa leaf (ASE; 50, 100 and 200mg/kg body weight) was administered orally, twice daily for 5 days for prevention from Aspirin (ASP)-, ethanol (EtOH)-, cold-restraint stress (CRS) - and pylorus ligation (PL)-induced ulcers. Estimation of antioxidant enzymes activity was carried out in CRS-induced ulcer model, and various gastric secretion parameters like volume of gastric juice, acid output, and pH value were estimated in PL-induced ulcer model. RESULT: ASE showed dose-dependent ulcer protective effect in ASP 23.64-58.76% (p<0.01 to p<0.001), EtOH 15.45-58.45% (p<0.001), CRS 19.39-78.36% (p<0.001) and PL 19.67-69.04% (p<0.05 to p<0.01), respectively. The percentage of protection by standard drug ranitidine was 77.77-84.32% (p<0.01 to p<0.001) in various gastric ulcer models. The gastric wall mucus was significantly (p<0.001) enhanced by ASE and is regarded as the first line of defence against EtOH-induced gastric ulcers showing cytoprotective property. ASE showed a marginal decrease in volume, acid pepsin concentration and acid pepsin output. However, ASE reduced the ulcer index with significant decrease in LPO level (p<0.001), and SOD level (p<0.01 to p<0.001) as compared with CRS-induced group. A gradual and significant increase in CAT values were observed at 100 and 200mg/kg dose levels (p<0.01 to p<0.001). CONCLUSIONS: The results of our study revealed that Argyreia speciosa possess significant dose dependent gastroprotective activity, probably due to its free radical scavenging activity.

Generic omeprazole delayed-release capsules: in vitro performance evaluations.

BACKGROUND: After the patent on omeprazole delayed-release capsules expired, Food and Drug Administration (FDA) approved several generic omeprazole delayed-release capsule applications. FDA has received some complaints concerning a lack of therapeutic effect of the generic omeprazole delayed-release capsules. AIM: To investigate the quality of five different marketed generic omeprazole delayed-release capsules. METHOD: The dissolution characteristics of these generic omeprazole delayed-release capsules were determined according to the United States Pharmacopeia (USP). Additional dissolution studies under simulated in vivo physiological conditions were also conducted to determine whether generic omeprazole capsules would perform similarly under these conditions. RESULTS: The experimental data show that all the generic omeprazole delayed-release capsules met the USP standards. The in vitro dissolution of generic drugs is similar to that of the brand omeprazole product. CONCLUSIONS: There is no scientific evidence to support the claims that the generic omeprazole delayed-release capsules perform differently from the brand omeprazole product in vitro.

Assessment of the pharmaceutical quality of omeprazole capsule brands marketed in Egypt.

The pharmaceutical quality of 7 local omeprazole capsule brands in Egypt was assessed relative to the proprietary product (Losec). Drug content, content uniformity, drug release (using USP test for enteric coated articles and a modified release test) were determined. Products were subjected to a 3-month stability study. Of the 7 brands, 6 had satisfactory drug content and content uniformity. All brands passed the USP drug release test. The modified release test proved to be more discriminative. After 3 months storage, drug content of 3 brands remained > 90% and 2 of these brands maintained drug release above 75%. Changes in pellet appearance during storage were indicative of omeprazole chemical degradation.

Ranitidine preparations on the Belgian market: a comparative study.

Ranitidine preparations formulated as tablets and granules were evaluated with different tests including in vitro dissolution and assay. Previously the analytical methods of these tests were validated according to the guidelines of the European network of Official Medicines Control Laboratories (OMCLs). All examined products complied to the requirements as described in the European, the British and the US Pharmacopoeia and consequently they can be considered as pharmaceutically equivalent.

Efficacy and safety measurements of proton pump inhibitors in infants and children.

The design of studies to evaluate the efficacy of acid-lowering drugs in children differs significantly from study designs in adult populations. Efficacy measurements may be less extensive than those used in adult studies because of limitations that exist secondary to concerns for patient safety, parental and institutional review board acceptance of efficacy end points, and existing standards of care within the pediatric gastroenterology community. Study designs involving patients who would routinely receive acid-lowering therapy have been successfully used to characterize the pharmacokinetics and pharmacodynamics of acid-lowering therapies (H2 receptor antagonists) and have led to pediatric labeling for these drugs. This approach may likewise be used in the study of newer acid-lowering agents, such as proton pump inhibitors.

Switching omeprazole in Sweden and the United States.

This article compares the Swedish Medical Products Agency's (MPA) decision to switch omeprazole from prescription (Rx) to over-the-counter (OTC) status with the US Food and Drug Administration (FDA) advisory panel's decision not to authorize the switch. The agencies' differing perspectives on efficacy, safety, labeling, and clinical trial requirements are evaluated with regard to the Rx-to-OTC switch process in general and omeprazole's case in particular. The FDA and MPA regulatory policies on switches are substantially divergent. The FDA maintains a stricter set of switch guidelines and requirements than the MPA. One could infer from this that the FDA is more risk-averse than the MPA. Nevertheless, the omeprazole switch in Sweden appears to be an exception in that it contrasts with the MPA's historical reluctance to switch the Rx status of medications. Cost considerations appear to have triggered the omeprazole switch, making it a special case. The lessons to be drawn from this case study are both specific and general. At the specific level, this case study suggests the MPA's decision to switch omeprazole was prompted by economic considerations, whereas the FDA's mandate did not allow cost to affect its decision on omeprazole. At a general level, this case study indicates that the differences between the FDA and MPA with respect to their regulatory policies on switches and their mandates apply not only to omeprazole but also to the dozens of switches currently under consideration by the respective regulatory agencies.

Solid state assay of ranitidine HCl as a bulk drug and as active ingredient in tablets using DRIFT spectroscopy with artificial neural networks.

PURPOSE: A new, simple, sensitive and rapid method was developed to analyse the polymorphic purity of crystalline ranitidine-HCI as a bulk drug and from a tablet formulation. METHODS: Diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy was combined with Artificial Neural Networks (ANNs) as a data modelling tool. A standard feed-forward network, with backpropagation rule and with single hidden layer architecture was chosen. Reduction and transformation of the spectral data enhanced the ANN performance and reduced the complexity of the ANNs model. Spectral intensities from 1738 wavenumbers were reduced into 173 averaged spectral values. These 173 values were used as inputs for the ANN. Following a sensitivity analysis the number of inputs was reduced to 30, or 35, these being the input windows which had most effect on the output of the ANN. RESULTS: For the bulk drug assay, the ANN model had 30 inputs selected from a sensitivity analysis, one hidden layer, and two output neurons, one for the percentage of each ranitidine hydrochloride crystal form. The model could simultaneously distinguish between crystal forms and quantify them enabling the physical purity of the bulk drug to be checked. For the tablet assay, the ANN model had 173 averaged spectral values as the inputs, one hidden layer and five output neurons, two for the percentage of the two ranitidine hydrochloride crystal forms and three more outputs for tablet excipients and additives. The ANN was able to solve the problem of overlapping peaks and it successfully identified and quantified all components in tablet formulation with reasonable accuracy. CONCLUSIONS: Some of the advantages over conventional analytical methods include simplicity, speed and good selectivity. The results from DRIFT spectral quantification study show the benefits of the neural network approach in analysing spectral data.

Use of a urea breath test to evaluate short-term treatments for cats naturally infected with Helicobacter heilmannii.

OBJECTIVE: To evaluate efficacy of 3 short-term treatments in cats naturally infected with Helicobacter heilmannii. ANIMALS: 29 cats infected with H heilmannii that had positive results for a urea breath test, rapid urease test, and Helicobacter species-specific polymerase chain reaction test. PROCEDURES: Cats anesthetized for routine surgical procedures were randomly allocated to 4 groups: group 1, control cats; group 2, cats treated with azithromycin, tinidazole, ranitidine, and bismuth once daily for 4 days; group 3, cats treated with clarithromycin, metronidazole, ranitidine, and bismuth twice daily for 4 days; and group 4, cats treated with clarithromycin, metronidazole, ranitidine, and bismuth twice daily for 7 days. Efficacy was determined on the basis of results of a urea breath test performed 10 and 42 days after end of treatment. RESULTS: Ten days after treatment, 0 of 4, 4 of 6, 11 of 11, and 8 of 8 cats in groups 1 to 4, respectively, had a negative result for a urea breath test. Forty-two days after treatment, 0 of 4, 3 of 6, 7 of 11, and 4 of 8 cats in groups 1 to 4, respectively, still had a negative result. CONCLUSIONS AND CLINICAL RELEVANCE: Treatments used in this study regularly suppressed breath 13CO2 production. However, although 23 of 25 (92%) cats had negative results for a urea breath test 10 days after treatment, only 14 of 25 (56%) cats still had negative results 42 days after treatment. It is difficult to achieve a definitive long-term cure in cats naturally infected with H heilmannii.