Efficacy and safety of three plant extracts based formulations of vagitories in the treatment of vaginitis: a randomized controlled trial.

Aim There are more and more herbal preparations that are used for the purpose of treatment and improvement of the clinical manifestation of vaginitis not only by patients themselves, but also by healthcare professionals. Plant species, St. John's wort, chamomile, calendula, yarrow, shepherd's purse and tea tree oil are all well known for their anti-inflammatory, antimicrobial and wound healing activity. This paper presents the results of a clinical study in which three herbal formulations/vagitories, based on extracts of St. John's wort, chamomile, calendula, yarrow, shepherd's purse and tea tree oil, were investigated for their effectiveness on vaginitis. Methods This was a randomized controlled clinical study that included 210 women with diagnosed vaginitis. Patients were divided into two basic groups, women in reproductive period and postmenopausal period. Three subgroups including 30 patients each received one of the three vagitorie formulations for 5 days, after which the effects on subjective and objective symptoms were monitored. Results Three types of vagitories based on plant extracts had a positive effect in the treatment of vaginitis. Vagitories based on tea tree oil showed better efficiency compared to vagitories with St. John's wort and vagitories based on extracts of five plants. Women in postmenopausal group reported better tolerability of St. John's wort-based and five herbs-based vagitories compared to tea tree oil based vagitories. Conclusion Investigated vagitories showed a positive effect on both objective and subjective symptoms of vagitnis. No serious side effects were reported.

Dissolution Profile of Nimesulide from Pharmaceutical Preparations for Oral Use.

Nimesulide belongs to the group of semi-selective COX-2 inhibitors, widely used in solid oral formulations. In the present work the influence of surfactants among other drug excipients, as well as particle size of the active substance and the effects of medium pH on the dissolution rate of nimesulide from solid pharmaceutical forms. For that purpose, four different preparations containing 100 mg nimesulide per tablet and available in the market of Bosnia and Herzegovina (labeled here as A, B, C and D) were studied. The test for the assessment of dissolution profiles of the formulations was performed in surfactant-free dissolution medium pH 7.5. The dissolution profiles were compared by calculating difference (f1), and similarity (f2) factors. The increasing dissolution medium pH value from 7.5 to 7.75 resulted in a significant increase of nimesulide dissolution rate from the examined formulations. Also, the results showed that particle size affects to a great extent the dissolution rate and the best results were achieved with micronized nimesulide. The presence of the surfactants among the other excipients expressed a negligible effect on the dissolution profile.

Dissolution studies of physical mixtures of indomethacin with alpha- and gamma-cyclodextrins.

Oral administration of indomethacin has been limited by its poor water solubility. Cyclodextrins have been recognized as potential candidates to overcome the poor solubility of indomethacin through the formation of inclusion complexes. The aim of our study was to compare the dissolution profiles of pure indomethacin and its mixtures with α- and γ-cyclodextrins The inclusion complexes of indomethacin with α- and γ-cyclodextrins were prepared by direct mixing in dissolution vessel. Fixed volumes of the dissolution medium were withdrawn at 0,5; 1 and 4 hours. Dissolution tests were performed on the USP Apparatus 2, rotating speed 100 rpm at 37±0.5 ° C, 500 ml, distilled water and 0,1 M HCl solution). Quantification of dissolved indomethacin was performed by UV/VIS spectrophotometric method at the absorption maximum around 320 nm. The results were expressed as relative dissolution rate (ratio between indomethacin dissolved from its physical mixtures with α- and γ-cyclodextrins and that dissolved the pure drug). Relative dissolution rates of indomethacin in combination with α- and γ-cyclodextrins at the end of testing were in the range of 91,66 to 337,14 % (for α- cyclodextrin) and in the range of 128,57 to 301,92 % (for γ-cyclodextrin). The complexation of indomethacin with α- and γ-cyclodextrins resulted in the enhancement of dissolution rate.

Impairment of the in vitro release of carbamazepine from tablets.

Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. The present study deals with the formulations of immediate release tablets of poorly soluble carbamazepine. As model tablets for this investigation, two formulations (named "A" and "B" formulations) of carbamazepine tablets labeled to contain 200 mg were evaluated. The aim of this study was to establish possible differences in dissolution profile of these two formulations purchased from the local market. The increased crystallinity together with enlarged particle size, enhanced aggregation and decreased wettability of the drug, resulted in insufficient dissolution rate for formulation "B". From the dissolution point of view, this formulation was inferior to the formulation "A", due to the solubilization effect.

Influence of splitting on dissolution properties of metoprolol tablets.

The objective of this work was to compare several profiles of dissolution data for metoprolol controlled release tablet formulations in order to identify possible changes in dissolution profiles of whole and scored tablets. Adequate design of score lines (on one or both sides) as well as the technology of preparation of tablet mixtures ensure forming a score line of adequate thickness, shape, size, curvature. According to the obtained results, this type of extended release formulation is eligible for splitting and use in therapy either as a whole or scored tablets.

Influence of type and neutralisation capacity of antacids on dissolution rate of ciprofloxacin and moxifloxacin from tablets.

Dissolution rate of two fluoroquinolone antibiotics (ciprofloxacin and moxifloxacin) was analysed in presence/absence of three antacid formulations. Disintegration time and neutralisation capacity of antacid tablets were also checked. Variation in disintegration time indicated the importance of this parameter, and allowed evaluation of the influence of postponed antacid-fluoroquinolone contact. The results obtained in this study showed decreased dissolution rate of fluoroquinolone antibiotics from tablets in simultaneous presence of antacids, regardless of their type and neutralisation capacity.

Stability of anthocyanins from commercial black currant juice under simulated gastrointestinal digestion.

Anthocyanins are effective antioxidants but they have also been proposed to have other biological activities independent of their antioxidant capacities that produce health benefits. Examples range from inhibition of cancer cell growth in vitro, induction of insulin production in isolated pancreatic cells, reduction of starch digestion through inhibition of a-glucosidase activity, suppression of inflammatory responses as well as protection against age-related declines in cognitive behavior and neuronal dysfunction in the central nervous system. However, to achieve any biological effect in a specific tissue or organ, anthocyanins must be bioavailable; i.e. effectively absorbed from the gastrointestinal tract (GIT) into the circulation and delivered to the appropriate location within the body. In this study, we assess the stability of anthocyanins from commercial Black currant (Ribes nigrum L.) juice using an in vitro digestion procedure that mimics the physiochemical and biochemical conditions encountered in the gastrointestinal tract (GIT). The main objective of this work was the evaluation of stability of anthocyanins during in vitro digestion in gastric and intestinal fluid regarding whether appropriate enzyme (pepsin or pancreatin) was added or not. Anthocyanins present in commercial black currant juice remain stable during in vitro digestion in gastric fluid regardless whether pepsin was added into the medium or not. Also, they remain stable during in vitro digestion in simulated intestinal fluid without pancreatin. The stability studies of anthocyanins in the intestinal fluid containing pancreatin indicated reduced stability, which also mainly contribute to slight reduction of total anthocyanins content (-1.83%) in commercial black currant juice.

Study of the applicabilty of content uniformity and dissolution variation test on ropinirole hydrochloride tablets.

When considering single-dose preparations, it is fundamental that the patient receives in his individual dose an amount of drug close to that claimed on the label. Since drug content and content uniformity of single-dose preparations depend on a number of processes associated with their manufacture, it is obviously unrealistic to expect every unit of product to possess exactly the same amount of the active ingredient. For that reason, pharmacopeial standards and specifications have been established to provide limits for permissible variations in the amount of active ingredient of individual single-dose units. The aim of our study was to determine the applicability of content uniformity and dissolution variation test on ropinirole hydrochloride tablets. According to the results obtained, we may conclude that analyzed ropinirole hydrochloride tablets satisfied pharmacopeial requirements concerning content uniformity and dissolution testing. In this case RSD tended to increase with the decrease of the labeled strength. It is obvious from the R2 value, as well. On the other side, if consider larger number of lots, analyzed by different assay methods and various sample preparation procedures this correlation is less pronounced. This may be a consequence of different assay techniques applied, HPLC, UV-D1 or UV.

Stability of cefuroxime axetil oral suspension at different temperature storage conditions.

Stability testing of an active substance or finished product provides information of the variation of drug substance or final product with time influenced by a variety of environmental factors such as temperature, humidity and light. Knowledge gained from stability studies enables understanding of the effects of the environment on the drugs. The aim of our study was to determine the stability of cefuroxime axetil oral suspension at different temperature storage conditions (stored at room /20 degrees C/ and refrigerated /5 degrees C/ conditions). Determination of cefuroxime (as cefuroxime axetil) was performed by dissolution testing. Fractions of the released cefuroxime axetil were compared using f2 value. After interpolating data for dissolution profiles at room and refrigerated conditions the following f2values were obtained: 62,56; 56,32 and 36,18 on 3rd, 6th and 10th day, respectively. These values indicate similarities in drug release from analyzed cefuroxime axetil oral suspension on 3rd, 6th day, and differences on 10th day. Based on our results, we may assume that cefuroxime axetil oral suspension preserves its stability for 10 days after reconstitution under room and refrigerated conditions. It is obvious, according to the f2 value obtained on the 10th day, that there is a difference between the released cefuroxime axetil from oral suspension at room (87,68%) and refrigerated (92,35%) conditions. Concentration changes can be caused by the mechanisms associated with drug release and hydrolytical decomposition of the sample and higher temperatures during longer period of storage.

Comparison of some physical parameters of whole and scored lisinopril and lisinopril/hydrochlorthiazide tablets.

Tablets are one of the most popular and preferred solid dosage forms because they can be accurately dosed, easily manufactured and packaged on a large scale, have good physical and chemical stability, and can contribute to good patient compliance given their ease of administration. The ability to match doses to patients depends on the availability of multiple dose sizes and adequate dose-response information. These are not always provided, so splitting of the tablets is sometimes necessary. Tablet splitting is an accepted practice in dispensing medication. It has been used when a dosage form of the required strength is not available commercially. The aim of our study was to compare some physical parameters of whole and scored lisinopril and lisinopril/hydrochlorthiazide tablets and to accept or exclude their influence on the obtaining of required dosage. According to the results obtained, we may conclude that tablets from batch "I", "II", "III" and "IV" satisfied pharmacopeial requirements concerning crushing strength, friability, disintegration time and mass uniformity. The hardness testing showed acceptable reproducibility and indicate that the data variation was primarily from the irreversible changes in the structure of tablet samples. The act of compacting powders stores energy within the tablets, by shifting or compressing the intermolecular bonds within the particles. The tablets have a natural tendency to relax once pressure is removed, and this tendency works against the interparticle bonding formed during compression. Hardness testing procedure causes irreversible changes in this structure.

Influence of tablet splitting on content uniformity of lisinopril/hydrochlorthiazide tablets.

Dose-related adverse effects of medications are a major problem in modern medical practice. The "correct" dose, based on drug company guidelines in package inserts, may not be correct for many patients. Tablet splitting or dividing has been an accepted practice for many years as a means of obtaining the prescribed dose of medication. As model tablets for this investigation, two batches of lisinopril- hydrochlorothiazide scored tablets labeled to contain 20/12.5 mg were used. The aim of this study was to establish possible influence of tablet splitting on content uniformity of lisinopril/hydrochlorthiazide tablets. Determination of the content uniformity of lisinopril and hydrochlorthiazide in our batches, was carried out by HPLC method. The results of content uniformity studies for halves of tablets containing combination of lisinopril-hydrochlorthiazide (supposed to contain 50% of stated 20/12.5 mg in the whole tablet) were: 49.60 +/-3.29% and 49.29+/-0.60 % (lisinopril); 50.33+/-3.50% and 50.69+/-1.95% (hydrochlorthiazide) for batch I and II, respectively. We can conclude that the results obtained in this study support an option of tablet splitting, which is very important for obtaining the required dosage when a dosage form of the required strength is unavailable, and for better individualization of the therapy.

Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.

Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

Formulation ingredients for toothpastes and mouthwashes.

In order to achieve the multi-claim products required for the dental care category, it is necessary for the formulator to use a variety of different ingredients. This places a number of demands on the development process. Innovations in the areas of pharmaceutical technology have contributed to the formulation of the products having superior efficacy as well as other attributes that may contribute to clinical response and patient acceptability. Improved clinical efficacy and tolerability, along with conditioning signals, should encourage patient compliance with oral hygiene further complementing professional efforts directed at disease prevention. The most effective way of preventing the development of dental disease is in controlling the production of dental plaque. It is formed by microbial action. The removal of plaque from the teeth and related areas is essential for the maintenance of a healthy mouth. In this paper we have presented the main components of toothpastes and mouthwashes. For the active ingredients, their supposed effect as therapeutic agents is also explained.