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Disintegration and then dissolution yield the compositions' medicinal efficacy. The proper disintegrant must be used in tablets and capsules in order to provide the best bioavailability. Disintegrants are the ingredients that break down tablets or capsules quickly into tiny pieces so they dissolve faster than they would if they didn't have them. Conversely, However, superdisintegrants, which are, as their name implies, superior to disintegrants, are compounds that speed up or assist disintegration even at low concentrations, usually 1–10% by weight in relation to the dosage unit's total weight. These are employed to boost the potency of solid dosage forms. Over the past ten years, there has been a steady increase in the market for fast-disintegrating tablets (FDTs), and the pharmaceutical sector has seen a significant expansion in this field. MDTs are solid unit Dosage forms that quickly dissolve in the mouth without the need for chewing or water. For elderly and paediatric patients who have trouble swallowing, FDTs, orally disintegrating tablets, offer benefits over traditional capsules and pills. This review describes the classification of superdisintegrants, its advantage, disadvantage, how it can be employed for preparing MDT, their mechanism of action, factors affecting disintegration and the recent development of superdisintegrants and finally application.

Risk control for nitrosamine impurities in drug products is currently a major challenge in the industry. Nitrosamines can form during drug product manufacturing and storage through the reaction of nitrites with amine-containing APIs or impurities. The level of nitrites in excipients and the rate of reaction often control the build-up of nitrosamine. Although the variability in nitrite levels across excipient types and suppliers is well recognized, the impact of excipient selection on the level of nitrosamine formed has not been systematically studied. This gap of knowledge is addressed in the current work. We present theoretical case studies of formulations where microcrystalline cellulose (MCC), or lactose supplier, or superdisintegrant type are changed in pursuit of lower levels of nitrite. The impact of the average, maximum, and minimum levels of nitrites in each excipient on nitrosamine formation in the dosage form is calculated. The input data for this calculation are the formulation composition, nitrosamine molecular weight (MW), percentage of conversion, and nitrite levels per excipient. The percentage of conversion (based on the formulation and manufacturing variables) and nitrite levels were taken from the recent literature. We show that changing the supplier of a single excipient, or of the three most critical excipients, can reduce nitrosamine formation by up to −59% and −89%, respectively. We also show that high-risk formulations, e.g., high MW nitrosamines, high dosage weights, and high percentages of conversion (e.g., wet granulation), can often be de-risked below regulatory acceptable daily intake via careful excipient selection. Finally, we provide an open-access tool that enables users to calculate the theoretical formation of nitrosamines in their specific formulations. This calculation template can be used for (i) the preliminary screening of the risk of nitrosamine formation in drug products and (ii) the preliminary assessment of the impact of excipient selection for risk mitigation.

AIM: Prasugrel is used to treat heart attack and strokes in persons with heart disease (recent heart attack). It helps keep blood flowing smoothly in your body. Objective: Difficulty in swallowing (dysphasia) is a common problem of all age groups, especially the elderly and pediatrics, because of physiological changes associated with these groups.

This study examines the influence of crospovidone (CP) manufacturer variability on the dissolution profiles of hydrochlorothiazide (HCTZ) tablets. Four CP batches from different manufacturers were characterized using pharmacopeial and physicochemical tests, including infrared absorption, loss on drying, and scanning electron microscopy (SEM). Significant differences were observed in the particle size distribution, wetting time, and water absorption capacities of the CP batches. Tablets were formulated using both direct compression and wet granulation methods. For the latter, the superdisintegrant was either added to the binder solution or incorporated intra- or extra-granularly. Disintegration and dissolution tests revealed that both CP concentration and the method of incorporation significantly affected tablet performance. Poly Kovidone and Max-Povidon exhibited superior performance at lower concentrations, while differences between brands became less pronounced at higher concentrations. The extra-granular method notably enhanced drug release profiles. Statistical analyses, including f 2 similarity factors and MANOVA with Principal Component Analysis (PCA), highlighted significant differences in dissolution behavior among the formulations. These findings emphasize the importance of controlling excipient variability to ensure consistent product performance. The study concludes that a 2% CP concentration is optimal for mitigating source variability and that the extra-granular addition of CP in wet granulation is recommended for enhancing its functional properties. Graphical Abstract

Telmisartan (Tel) is a potent antihypertensive drug with a very poor aqueous solubility, especially in pH ranging from 3 to 9 (i.e., biological fluids) that results in poor bioavailability. Our aim was to improve Tel solubility and dissolution rates without the need for expensive multistep procedures, and without inclusion of alkalinizers. This study adopted the use of surface solid dispersions (SSDs) employing superdisintegrants, hydrophilic polymers and combined carriers including a superdisintegrant with a hydrophilic polymer. Tel-SSDs were formulated using thesolvent evaporation method. Compatibility between Tel and different carriers was examined via FT-IR. Tel-SSDs were evaluated optically and thermally to reveal a complete loss of the crystalline nature of the drug. Both drug content and percentage yield were calculated to judge the efficiency of the preparation technique used. Saturation, aqueous solubility, and dissolutions rates were determined. Dissolution profiles were studied using model dependent and independent approaches and were subjected to the pair-wise procedure using the DDsolver software program. Effect of aging was studied by comparing the drug content and dissolution profiles of freshly prepared SSDs with aged samples. All Tel-SSDs showed acceptable physical properties. Tel-SSDs showed pertinent enhancement related to the carrier used. Combined surface solid dispersions employing superdisintegrant croscarmellose sodium with either hydrophilic polymer PEG 4000 or Poloxamer 407 gave remarkable enhancement in solubility and dissolution rates of Tel where more than 90% of the drug was released within 20 min. The effect of aging results proved a non-significant difference in the drug content and dissolution profiles between fresh and aged samples. Formulation of Tel SSDs using combined carriers proved to be effective in enhancing the aqueous solubility and dissolution rates of Tel, as well as showing good stability upon aging.

PurposeOrodispersible tablets (orally disintegrating tablets, ODTs) have been used in pharmacotherapy for over 20 years since they overcome the problems with swallowing solid dosage forms. The successful formula manufactured by direct compression shall ensure acceptable mechanical strength and short disintegration time. Our research aimed to develop ODTs containing bromhexine hydrochloride suitable for registration in accordance with EMA requirements.MethodsWe examined the performance of five multifunctional co-processed excipients, i.e., F-Melt® C, F-Melt® M, Ludiflash®, Pharmaburst® 500 and Prosolv® ODT G2 as well as self-prepared physical blend of directly compressible excipients. We tested powder flow, true density, compaction characteristics and tableting speed sensitivity.ResultsThe manufacturability studies confirmed that all the co-processed excipients are very effective as the ODT formula constituents. We noticed superior properties of both F-Melt’s®, expressed by good mechanical strength of tablets and short disintegration time. Ludiflash® showed excellent performance due to low works of plastic deformation, elastic recovery and ejection. However, the tablets released less than 30% of the drug. Also, the self-prepared blend of excipients was found sufficient for ODT application and successfully transferred to production scale. Outcome of the scale-up trial revealed that the tablets complied with compendial requirements for orodispersible tablets.ConclusionsWe proved that the active ingredient cannot be absorbed in oral cavity and its dissolution profiles in media representing upper part of gastrointestinal tract are similar to marketed immediate release drug product. In our opinion, the developed formula is suitable for registration within the well-established use procedure without necessity of bioequivalence testing.

Background/Objectives: Enteric coating protects active pharmaceutical ingredients from gastric degradation, but conventional tablets may present swallowing difficulties in geriatric and pediatric patients. Hence, this study intended to develop pH-responsive multiparticulates, formulated into orally disintegrating tablets (ODTs), for targeted intestinal drug delivery in individuals with dysphagia. Methods: Multiparticulates were developed via sequential seal coating, drug layering, sub-coating, and enteric coating on inert cores using a fluidized bed coater (Pam Glatt, India; bottom spray). Selected enteric-coated batches were directly compressed into ODTs using microcrystalline cellulose (Avicel PH102) and mannitol (Pearlitol SD 160) as fillers, with Explotab®, Ac-Di-Sol®, or crospovidone M® as superdisintegrants. Results: Multiparticulates exhibited mean diameters of 197.671–529.511 μm and span values of 0.603–0.838. Span value < 1, indicating a narrow size distribution. Electron microscopy confirmed the spherical morphology of Batches 7a and b. Enteric-coated batches (5b, 6, 7a, 7b) released ≤10% of the drug in 0.1 N HCl at 2 h. Optimized formulation ODT 7b released 7.904% of the drug under gastric conditions and 79.749% in phosphate buffer (pH 6.8) within 2.5 h, following first-order drug release kinetics. ODT 7b demonstrated hardness (2.538 ± 0.144 kg/cm2), wetting time (11.17 ± 1.051 s), friability (0.712%), and drug content (99.81 ± 1.01%) within acceptable limits. Conclusions: The pH-dependent multiparticulates provided sustained intestinal drug release and, when incorporated into ODTs, yielded a dosage form with a rapid wetting time and acceptable mechanical properties. This dosage form can offer a promising approach for improving compliance and therapeutic efficacy in patients with swallowing difficulties (dysphagia).

The characteristics of sago starch exhibit remarkable resemblances to those of cassava, potato, and maize starches. This review intends to discuss and summarize the synthesis and characterization of sodium starch glycolate (SSG) from sago starch as a superdisintegrant from published journals using keywords in PubMed, Scopus, and ScienceDirect databases by Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA 2020). There are many methods for synthesizing sodium starch glycolate (SSG). Other methods may include the aqueous, extrusion, organic solvent slurry, and dry methods. Sago starch is a novel form of high-yield starch with significant development potential. After cross-linking, the phosphorus content of sago starch increases by approximately 0.3 mg/g, corresponding to approximately one phosphate ester group per 500 anhydroglucose units. The degree of substitution (DS) of sodium starch glycolate (SSG) from sago ranges from 0.25 to 0.30; in drug formulations, sodium starch glycolate (SSG) from sago ranges from 2% to 8% w/w. Higher levels of sodium starch glycolate (SSG) (2% and 4% w/w) resulted in shorter disintegration times (within 1 min). Sago starch is more swellable and less enzymatically digestible than pea and corn starch. These investigations demonstrate that sago starch is a novel form of high-yield starch with tremendous potential for novel development as superdisintegrant tablets and capsules.

Tablet disintegration is an important pre-requisite for drug dissolution and absorption. The disintegration test is typically conducted at 37 °C, but the intragastric temperature may vary due to meals or fever. This study investigated the effects of temperature and compaction pressure on tablet disintegratability to gain deeper insights into superdisintegrant sensitivity and function. Tablets with either sodium starch glycolate or crospovidone as disintegrant were prepared at various compaction pressures and subjected to the disintegration test using different medium temperatures. Preheating of tablets was also employed to establish instant temperature equilibrium between the tablet and the disintegration medium. Liquid penetration and disintegration were faster as the medium temperature increased or compaction pressure decreased. Swelling or strain recovery disintegrants exhibited similar sensitivity to variations in the medium temperature. Preheating of the tablets resulted in slower disintegration, but this effect was reversible upon cooling, hence the slower disintegration was unlikely to be attributed to changes in the disintegrant physical state. The temperature difference between the tablet and the disintegration medium likely affected the rate of fluid flow into tablets and influenced disintegration. Understanding disintegrant temperature sensitivity would help to avoid unacceptable fluctuations in disintegration due to temperature variations. The temperature difference effect could also be harnessed to boost disintegrant performance.