Due to the additional particle coalescence in the coating, changes in the dissolution profile occur over time in the formulations coated by aqueous ethylcellulose latex. Dry thermal treatment (DT) of the coating can be used as a prevention of this process. Alternatively, it is advisable to take advantage of the synergistic effect of high humidity during wet treatment (WT), which substantially accelerates the film formation. This can be a problem for time-controlled systems, which are based on the coating rupture due to the penetration of water into the core causing the increase in the system volume. This process can begin already during the WT, which may affect the coating adversely. The submitted work was focused on the stability testing of two pellet core compositions: pellets containing swelling superdisintegrant sodium carboxymethyl starch (CMS) and pellets containing osmotically active polyethylene glycol (PEG). Another objective was to identify the treatment/storage condition effects on the pellet dissolution profiles. These pellets are intended to prevent hypoglycemia for patients with diabetes mellitus and therefore, besides the excipients, pellet cores contain 75% or 80% of glucose. The pellet coating is formed by ethylcellulose-based latex, which provides the required lag time (120-360 min). The sample stability was evaluated depending on the pellet core composition (PEG, CMS) for two types of final pellet coating treatment (DT or WT). Scanning electron microscopy and Raman microspectroscopy revealed the penetration of glucose and polyethylene glycol from the core to the PEG pellet surface after WT. For the CMS sample, significant pellet swelling after WT (under the conditions of elevated humidity) was statistically confirmed by the means of stereomicroscopic data evaluation. Therefore, the acceleration of dissolution rate during the stress tests is caused by the soluble substance penetration through the coating in the case of PEG pellets or by dosage form volume increase in the case of CMS pellets. The observed mechanisms can be generally anticipated during the stability testing of the ethylcellulose coated dosage forms. The aforementioned processes do not occur after DT and the pellets are stable in the environment without increased humidity.
- MeSH
- celulosa analogy a deriváty chemie MeSH
- farmaceutická chemie MeSH
- glukosa chemie farmakologie MeSH
- hypoglykemie prevence a kontrola MeSH
- implantované léky chemie MeSH
- léky s prodlouženým účinkem MeSH
- polyethylenglykoly chemie MeSH
- pomocné látky chemie MeSH
- povrchové vlastnosti MeSH
- příprava léků metody MeSH
- rozpustnost MeSH
- škrob analogy a deriváty chemie MeSH
- stabilita léku MeSH
- uvolňování léčiv MeSH
- velikost částic MeSH
- vysoká teplota MeSH
- Publikační typ
- časopisecké články MeSH
The preparation of liquisolid systems presents a promising and innovative possibility for enhancing dissolution profiles and improving the bioavailability of poorly soluble drugs. This study aims to evaluate the differences in the properties of liquisolid systems containing combinations of 3 commercially used superdisintegrants (sodium starch glycolate, crospovidone, and croscarmellose sodium). Multiple regression models and contour plots were used to study how the amount and the type of superdisintegrant used affected the quality parameters of liquisolid tablets. The results revealed that an increased amount of crospovidone in the mixture improves disintegration and wetting time and enhances drug release from the prepared liquisolid tablets. Moreover, it was observed that a binary blend of crospovidone and sodium starch glycolate improved tablet disintegration. Considering the obtained results, it could be stated that crospovidone showed the best properties to be used as superdisintegrant for the preparation of liquisolid systems containing rosuvastatin.
- MeSH
- farmaceutická chemie metody MeSH
- farmaceutické pomocné látky chemická syntéza farmakokinetika MeSH
- lékové formy MeSH
- pomocné látky chemická syntéza farmakokinetika MeSH
- povidon chemická syntéza metabolismus MeSH
- rozpustnost MeSH
- škrob analogy a deriváty chemická syntéza farmakokinetika MeSH
- sodná sůl karboxymethylcelulosy chemická syntéza farmakokinetika MeSH
- uvolňování léčiv MeSH
- výzkumný projekt MeSH
- Publikační typ
- časopisecké články MeSH
CONTEXT: The preparation of liquisolid systems (LSS) represents a promising method for enhancing a dissolution rate and bioavailability of poorly soluble drugs. The release of the drug from LSS tablets is affected by many factors, including the disintegration time. OBJECTIVE: The evaluation of differences among LSS containing varying amounts and types of commercially used superdisintegrants (Kollidon® CL-F, Vivasol® and Explotab®). MATERIALS AND METHODS: LSS were prepared by spraying rosuvastatin solution onto Neusilin® US2 and further processing into tablets. Varying amounts of superdisintegrants were used and the differences among LSS were evaluated. The multiple scatter plot method was used to visualize the relationships within the obtained data. RESULTS AND DISCUSSION: All disintegrants do not showed negative effect on the flow properties of powder blends. The type and concentration of superdisintegrant had an impact on the disintegration time and dissolution profiles of tablets. Tablets with Explotab® showed the longest disintegration time and the smallest amount of released drug. Fastest disintegration and dissolution rate were observed in tablets containing Kollidon® CL-F (≥2.5% w/w). Also tablets with Vivasol® (2.5-4.0% w/w) showed fast disintegration and complete drug release. CONCLUSION: Kollidon® CL-F and Vivasol® in concentration ≥2.5% are suitable superdisintegrants for LSS with enhanced release of drug.
- MeSH
- anticholesteremika aplikace a dávkování chemie MeSH
- farmaceutické pomocné látky chemie MeSH
- povidon chemie MeSH
- příprava léků MeSH
- rosuvastatin kalcium aplikace a dávkování chemie MeSH
- rozpustnost MeSH
- silikáty chemie MeSH
- škrob analogy a deriváty chemie MeSH
- sloučeniny hliníku chemie MeSH
- sloučeniny hořčíku chemie MeSH
- tablety chemie MeSH
- uvolňování léčiv MeSH
- Publikační typ
- časopisecké články MeSH
Patients tend to evade the occurrence of hypoglycemic episodes by excessive carbohydrate intake. Glucose pellets with delayed release in the time of the maximum effect of insulin can not only prevent hypoglycemia but also eliminate the preventive carbohydrate intake. The pellets can be administered in a mixture with semisolid food. The cores containing glucose in combination with osmotically active agents (croscarmellose sodium, carmellose sodium, polyethylene glycol, or carboxymethyl starch) were prepared by extrusion-spheronization and coated with 15% water ethylcellulose dispersion (Surelease® B NF) in Wurster column (Medipo, Havlíčkův Brod, Czech Republic) into four coating levels (12.5, 25, 35, and 50%). Mean particle size is 0.63-0.73 for cores and 0.82-0.98 for coated pellets. Cores and coated pellets have excellent or good flow properties according to Hausner ratio and Carr index. Aspect ratio ranges from 1.78 to 2.17 for cores and from 1.73 to 2.31 for coated pellets. Dissolution was performed using pH-independent method and method with continual change of pH. The suitable pH-independent release was achieved in the samples containing carboxymethyl starch or polyethylene glycol. Glucose release is enabled by a membrane rupture caused by core swelling. It can be, therefore, assumed that the glucose release profile will not be affected by food or transit time.
- MeSH
- celulosa analogy a deriváty chemie MeSH
- diabetes mellitus farmakoterapie MeSH
- dítě MeSH
- farmaceutická chemie metody MeSH
- glukosa aplikace a dávkování MeSH
- hypoglykemie farmakoterapie MeSH
- hypoglykemika aplikace a dávkování MeSH
- implantované léky aplikace a dávkování MeSH
- lékové formy MeSH
- lékové transportní systémy metody MeSH
- léky s prodlouženým účinkem aplikace a dávkování chemie MeSH
- lidé MeSH
- polyethylenglykoly chemie MeSH
- pomocné látky chemie MeSH
- rozpustnost MeSH
- škrob analogy a deriváty chemie MeSH
- velikost částic MeSH
- Check Tag
- dítě MeSH
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Digestibility of starch has been attributed to many factors, such as starch s ource, granule size, amylose / amylopectin ratio, crystallinity. Resistant starch (RS) es- capes enzymatic digestion in the small intestine and passes into colon. The review is focused on the RS content in foods, nutritional benefits and on methods of increasing the RS/total starch ratio. Slowly digestible starch is ab- sorbed in the small intestine within 20–120 min. RS can be used in treatment of diabetes or in controlled-release drugs.
- MeSH
- amylopektin chemie MeSH
- amylosa chemie MeSH
- biologická dostupnost MeSH
- farmaceutická technologie * metody MeSH
- farmaceutické pomocné látky analýza aplikace a dávkování farmakokinetika chemie izolace a purifikace metabolismus terapeutické užití zásobování a distribuce MeSH
- glukany chemie MeSH
- intestinální absorpce MeSH
- lékové formy MeSH
- léky s prodlouženým účinkem MeSH
- lidé MeSH
- metabolismus sacharidů fyziologie MeSH
- nosiče léků * MeSH
- nutriční vědy MeSH
- potravinářská technologie MeSH
- povrchové vlastnosti MeSH
- příprava léků MeSH
- rozpustnost MeSH
- škrob * analogy a deriváty farmakokinetika fyziologie chemie izolace a purifikace klasifikace metabolismus terapeutické užití ultrastruktura MeSH
- tablety MeSH
- tobolky MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
