Hard Capsules Research Articles

Carboxyl-modified nanocellulose (cNC) enhances the stability of cNC/pullulan bio-nanocomposite hard capsule against moisture variation

The quality of polysaccharide-based films and hard capsules is often affected by changes in relative humidity, manifesting as unstable water content, and changes in mechanical strength that make them brittle or soft. Herein, carboxyl-modified nanocellulose (cNC) was prepared and used as a new component to successfully improve the moisture resistance of cNC/pullulan/high-acyl gellan bio-nanocomposite hard capsules (NCPGs). Homogenously dispersed cNC in the pullulan/high-acyl gellan matrix could render the formation of more hydrogen bonds that provided additional water-binding sites and limited the free movement of pullulan and high-acyl gellan molecular chains within NCPGs. This contributed to a decreased amount of pooling adsorption water and an increased amount of Langmuir adsorption water in NCPGs, as compared to pullulan/high-acyl gellan hard capsules (PGs) without cNC. Therefore, the equilibrium moisture content (EMC) values of NCPGs decreased at 83 % relative humidity and increased at 23 % relative humidity compared to those of PGs. Together with enhanced mechanical and barrier properties, NCPGs effectively protected encapsulated amoxicillin and probiotic powder from changes in the outside humidity. Additionally, NCPGs exhibited faster drug release. This study presents a new mechanism and strategy for fabricating films and hard capsules with enhanced stability against moisture variation.

Comprehensive characterisation of tilapia fish gelatine under varied extraction conditions for the advancement of hard capsule production

SummaryHard capsules are a frequently used oral medication delivery form. This study aims to evaluate the potential of tilapia fish gelatine as a suitable material for hard capsules, by analysing various gelatine properties under different extraction temperatures (50, 60, 70, and 80 °C) and extraction periods (6 and 12 h). The results showed a range of values for the gelatine yield (22–33% (w/w)), gel strength (141–360 g), molecular weight distribution (140–300 kDa), and amino acid composition (185–220/1000 residues). FG70‐12 (296) and FG60‐6 (266) were found to have gel strength between 200 and 300 g thus suitable to be used as hard capsule material. Interestingly, the strongest gelatine having 360 g gel strength obtained from FG50‐6 (fish gelatine extracted at 50 °C for 6 h) became the essential ingredient for preparing hard capsules because two times dipping was enough to obtain the standard weight and thickness. A slight loss of moisture was identified during drying and rapid dissolution (4–8 min) detected from fish gelatine capsule at pH 6.8 or below. Therefore, hard capsules for pharmaceutical applications could be developed from fish gelatine as an alternative gelatine with similar properties as commercial hard capsules and satisfying the pharmacopoeia standard.

Comparison of Mini-Tablets and Pellets as Multiparticulate Drug Delivery Systems for Controlled Drug Release

Mini-tablets made into hard capsules or administered using special dosing units, as well as pellets in hard capsules or compressed into tablets, offer the advantages of multiparticulate drug delivery systems and are suitable for controlled drug release using polymer coatings. Four different kinds of solid drug preparations were manufactured and investigated concerning drug release. Inert pellets were coated with the model drug sodium benzoate and, in a second step, with the insoluble polymer ethylcellulose. The coated pellets were compressed into mini-tablets and into normal tablets. Another kind of mini-tablet was compressed from a sodium benzoate compression mixture and finally coated with ethylcellulose. The coating of the tablets was performed using fluidized bed technology. The sodium benzoate release plots of the coated pellets show a lag time and retarded release according first-order kinetics. The mini-tablets and normal tablets compressed from pellets release sodium benzoate according to first-order kinetics as well, but without the lag time due to distinct ethylcellulose layer destruction during tableting. The release is retarded with increasing ethylcellulose layer thickness on directly compressed mini-tablets. The different formulations of coated pellets, mini-tablets, and normal tablets offer a broad choice for variable drug release kinetics depending on the biopharmaceutical and pharmacological requirements.

In Vivo Evaluation of a Gastro-Resistant Enprotect® Capsule under Postprandial Conditions.

Ready-to-fill enteric hard capsule shells are an evolving field of oral drug and nutraceutical products. Lonza Capsugel® Enprotect® capsules were recently proven to provide reliable release in the small intestine after fasted intake, but robustness against postprandial intake needed to be proven. In this study, the capsules were administered to 16 healthy young subjects after intake of a light meal. The Enprotect® capsules were labelled with 5 mg black iron oxide and 25 mg 13C3-caffeine. Magnetic Resonance Imaging was used to identify the localization and visual dispersion of the capsule filling. The salivary appearance of caffeine was considered a second independent and sensitive marker for the initial release. Whereas the fasted gastric residence time of the capsules amounted to 43 ± 32 min, it was increased to 158 ± 36 min after postprandial intake. Therefore, the mean dispersion time according to MRI and the mean caffeine appearance time were increased to 196 ± 37 min and 189 ± 37 min, respectively. But, similar to fasted administration, no capsule disintegration or leakage was observed in the stomach and 38% of the capsules disintegrated in the jejunum and 62% in the ileum. The mean dispersion time after gastric emptying and the mean caffeine appearance time after gastric emptying amounted to 38 ± 21 min and 31 ± 17 min, respectively. Both did not relevantly change compared to the fasted intake. Only the absolute dispersion time and caffeine appearance were prolonged due to the increased gastric residence and no relevant influence of the light meal was observed on the disintegration or release behavior of Enprotect® capsules after gastric emptying. The capsules also showed robust enteric properties after postprandial administration.

Formulation and Acute Toxicity, Anti-Inflammatory, Analgesic Effects of Hard Capsules of Herba Siegesbeckiae Orientalis Dry Extract in Experimental Animals

This study aimed to investigate the acute toxicity, analgesic and anti-inflammatory effects of hard capsules containing dry extract from Siegesbeckia orientalis L. (CKHT) in animal models. Hard capsules were prepared using the volumetric method, with Avicel PH 102 as the diluent excipient and magnesium carbonate as the adsorbent excipient. The acute toxicity of CKHT was assessed on white mice at a dose of 2,400 mg/kg body weight. The anti-inflammatory effect was evaluated using a carrageenan-induced paw edema model in rats, while the analgesic effect was tested using an acetic acid-induced writhing model in mice. The results showed that CKHT administered at the doses of 102.2 mg/kg/day, 204.4 mg/kg/day, and 408.8 mg/kg/day had significant anti-inflammatory effect on the carrageenan-induced rat paw edema model by reducing the paw volume and increasing the percentage of edema inhibition compared to the untreated group (p < 0.001). The dose of CKHT 408.8 mg/kg/day showed anti-inflammatory effects that similar to aspirin at the dose level of 200 mg/kg/day (p > 0.05). In the analgesic study, mice treated with CKHT at the doses of 188.7 mg/kg/day, 377.4 mg/kg/day, and 754.8 mg/kg/day had significant reduction in acetic acid-induced writhing within 30 minutes compared to the untreated group (p < 0.001). Furthermore, CKHT did not show acute toxicity (no LD50) at the dose of 2,400 mg/kg body weight. These results suggested that CKHT exhibited acute analgesic and anti-inflammatory effects in animal models.
 Keywords: Dried extract from Siegesbeckia orientalis L.; capsules; anti-inflammatory; analgesic. 
 

RESEARCH ON FORMULATION OF HARD CAPSULES CONTAINING EXTRACTS OF HOUTTUYNIA CORDATA THUMB (SAURURACEAE), MORUS ALBA L. (MORACEAE), AND CARICA PAPAYA L. (CARICACEAE)

Background: previous studies have demonstrated that Houttuynia cordata Thumb (Saururaceae), Morus alba L. (Moraceae), and Carica papaya L. (Caricaceae) are effective against various viruses, especially the SARS-CoV-2 virus. In Vietnam, even though the three of these plant species are grown quite popularly and are pretty commonly consumed by residents regularly, there have not been any applications to the dosage forms to promote their full potential effects and make these dosage forms easy to use and preserve. Furthermore, no research has been conducted on a capsule form that combines all three of these medicinal herbs. Objectives: the research focuses on the composition of a hard capsule formula containing the extracts of Houttuynia cordata, Morus alba, and Carica papaya as well as the development of testing standards for prepared hard capsules. Materials and methods: the ratio of adsorbents and fillers in the formula was investigated so that the granules had low moisture, a suitable flow rate, and the appropriate apparent density for packaging; standards for testing capsules were developed according to current regulations. Results: the selected adsorbent was light MgCO3, with a ratio of plant extract: filler: adsorbent of 10: 5: 0.5 and a ratio of Avicel: Starch 1500 of 1: 3. Conclusions: a hard capsule containing medicinal plant extract was formulated with a moisture content of < 5% and well-flowing granules that had the suitable apparent density for packing the capsule size of 0. Capsules met standards in terms of appearance, weight uniformity, disintegration, heavy metal and microorganisms, with a quercetin content of 74.45 ± 0.23 mg. The result of the study is considered one of the most essential bases for further research on determining the effectiveness of medicines derived from medicinal plants and applied to support the treatment of COVID-19, which is still happening in a quite complicated way at the moment.

Developing oral chronotherapy for cortisol replacement in congenital adrenal hyperplasia.

The sun imposes a 24-h periodicity to life and circadian rhythms have evolved to maintain homoeostasis through the day/night cycle. In humans, there is a central clock that controls the sleep/wake cycle which is paralleled metabolically by a fast/feed cycle. The clock maintains homoeostasis by synchronising metabolism to the time of feeding. Loss of synchrony between the clock and hormonal rhythms results in loss of homoeostasis as evidenced by obesity, depression, and diabetes in people undertaking shift work. Cortisol has a distinct circadian rhythm; peaking on waking and low at sleep onset. Loss of this rhythm in adrenal insufficiency is associated with a poor quality of life and increased mortality. To replace the cortisol rhythm requires chronotherapy and for this you need to define the key parameters of the target rhythm, create a formulation to replicate that rhythm, and then prove clinical benefit. The physiology of hormones is more complex than that of nonnative drugs. Hormones are secreted with varied rhythms, bound to multiple cognate binding proteins, and actively transported and cleared through enzymatic pathways in multiple organs. We have examined the diurnal rhythm of cortisol in healthy volunteers, created physiologically-based pharmacokinetic models, and tested various oral delayed and sustained formulations of hydrocortisone (development name, Chronocort) in clinical trials. The outcome from this work was the manufacture of modified-release hydrocortisone hard capsules (tradename Efmody, Diurnal Ltd), that replicate the cortisol diurnal rhythm and improve the disease control of congenital adrenal hyperplasia the commonest hereditary form of adrenal insufficiency.

The Rapid Detection of Pork Gelatin in Hard Shell Capsule on Supplement Products Using FTIR and PCA

This study aimed to develop a fast and low-cost detection method to determine the difference between hard shell capsule on supplement products containing pork or non-pork gelatin by using Fourier Transform Infrared (FTIR) spectroscopy and Partial Component Analysis (PCA). Twelve samples of hardshell capsules were used, among which Eight samples were pure made from pork and some of them adulterated with cow. The samples were detected before using real-time PCR to determine the identity of the samples. All the gelatin samples were measured with the FTIR spectrophotometer in the reflection mode. Spectra were collected in the wavenumber range from 4000-650 cm-1. The results show that the PCA model with the data were pre-processed before PCA was performed. The absorbance data from FTIR were pre-processed using Savitsky-Golay smoothing technique and continued with normalization by peak normalize before subjected to PCA. This newly developed method is fast, involves simple sample preparation and is low cost.

FORMULASI CANGKANG KAPSUL DARI PEKTIN KULIT BUAH NANGKA (Artocarpus heterophyllus Lam) DAN UJI WAKTU HANCUR KAPSUL

Capsule is capsule preparations which consisting of a drug in a soft capsule and hard capsule sell. Capsule is the preparations that most people used to discover the unpleasant taste of the drug. Most of capsule sell are made of gelatin, but it can also made with starch or other ingredients. The other ingredients which can substitute gelatin is pectin. Pectin is an ingredient belong to the class of carbohydrates. This study aim to find others alternative that can be used as new ingredients of capsule sell, which is jack fruit peels. Dissolved 20 mg jack fruit peels in 1000 ml of distilled water and, added 5% of citric acid. Then extracted on a hot plate with a stirring speed 600 rpm, temperature of 85ͦC, for 120 minutes. The yield obtained was 0.319%. The best formulations results were 2 (0.7 gram pectin, 5.00 gram carrageenan, 100ml disttiled water). The result of the evaluation of capsule sell standards with a body diameter of 6,2 mm, 6,3 mm, of a lid diameter, a body length of 15,2 mm, a lid length of 07.8 mm, and those that are unqualified with 0.09 gram of capsule weights. The organleptic results are light brown color, texture a little loud and there is no fragrance. The capsule sell disintegration should meet the requirements set by the Indonesian Pharmacopoeia V edition, is 13 minutes 47 seconds.Keywords: jackfruit skin (Artocarpus heterophyllus Lam), pectin, capsule shell

Pembuatan Cangkang Kapsul Keras dari Glukomanan Biji Salak (Salacca zalacca) dengan Penambahan Enzim α-Amilase Buah Kelor

The purpose of this study was to examine the results of the fabrication and disintegration time of hard capsule shells made from salak seed glucomannan with and without the inclusion of α-amylase moringa fruit enzymes. To determine the effect of time, temperature, and the optimal concentration on the production of rigid capsule shells from glucomannan from zalacca seeds. This study makes use of both independent and dependent variables. The data was examined using functional group analysis using an FTIR spectrophotometer, and the hemicellulose from the seeds of the salak fruit was converted to glucomannan with the addition of the moringa α-amylase enzyme. The viscosity of the glucomannan gel variations of zalacca seeds differed, with gels from glucomannan flour with concentrations of 8%, 9%, and 10% (w/v) having viscosity values of 32.5 cP, 2049.75 cP, and 8007, 89 cP, respectively. While glucomannan with the Moringa fruit α-amylase enzyme The viscosity value gradually lowered with the addition of Moringa fruit extract. It reduced at 300°C temperature variation of 11221.02 cP, 400°C temperature variation of 11097.14 cP, and 500°C temperature variation of 10754.37 cP. The viscosity value gradually decreased after the addition of the αamylase moringa fruit enzyme. The 10 minute mixing time variation yielded the greatest viscosity value, 10261.74 cP, while the 50 minute mixing time variation yielded the lowest, 8681.76 cP. Furthermore, physical specifications with the inclusion of the α-amylase enzyme in Moringa fruit produced capsule shells that were thinner in color and conformed to conventional capsule shells.

Manufacturing classification system for oral solid dosage forms of traditional Chinese medicines(Ⅳ): classification of hygroscopicity behaviors of capsules

Hard capsules of traditional Chinese medicine(TCM) have different degrees of hygroscopicity, which affects the stability and efficacy of drugs. In this paper, 30 kinds of commercially available TCM capsules were used as the research object. The hygroscopicity curves of capsule contents, capsule shells, and capsules were tested respectively, and the first-order kinetic equation was used for fitting. The results show that during the 24 h hygroscopicity process, the capsule shell can reduce the weight gain caused by the hygroscopicity of the contents by 0.80%-53.0% and the hygroscopicity rate of the capsule contents by 1.74%-91.3%, indicating that the capsule shell has a strong delay effect on the hygroscopicity of the contents of the TCM capsules. Seven physical parameters of the contents of 30 kinds of TCM capsules were determined, and 14 prescription process-related parameters were sorted out. A partial least squares model for predicting the hygroscopicity rate of the contents of TCM capsules(with shell) for 24 h was established. It is found that the hygroscopicity rate of the capsule shell is positively correlated with the hygroscopicity of the contents of TCM capsules(with shell), suggesting that the capsule shell with a low hygroscopicity rate is helpful for moisture prevention. In addition, the pre-treatment process route of the preparation and the type of molding raw materials affect the hygroscopicity. A larger proportion of the extract in the capsule content and a smaller proportion of the fine powder of the decoction pieces indicate stronger hygroscopicity of the capsule content. The 24 h hygroscopicity rate of 15% was used as the classification node of hygroscopicity strength, and the hygroscopicity rate constant of 0.58 was used as the classification node of hygroscopicity speed. The classification system of hygroscopicity behaviors of TCM capsules was established: the varieties with strong and fast hygroscopicity accounted for about 6.67%, while those with strong and slow hygroscopicity accounted for about 33.3%; the varieties with weak and fast hygroscopicity accounted for about 26.7%, while those with weak and slow hygroscopicity accounted for about 33.3%. The classification system is helpful to quantify and compare the hygroscopicity behavior of different TCM capsules and provides a reference for the quality improvement, moisture prevention technologies, and material research of TCM capsules.

Myocardial infarction model induced by isoproterenol in rats and potential cardiovascular protective effect of a nattokinase-containing hard capsule

BackgroundTD.HK01® consists of a Japanese traditional medicine: Nattokinase (derived from soybean) and three other natural components, namely dried Hirudo medicinalis, Semen Mucuna interrupta and Huperzia carinata. ObjectivesTD.HK01® is potentially aimed to the preventive treatment of cardiovascular disease (CVD) in general, and myocardial infarction (MI) in particular. MethodsIn this study, a non-invasive method has been used to induce MI in rats, preceded by oral administration of TD.HK01® for 30 consecutive days to determine the potential cardiovascular effect of this pretreatment. Rats were divided into four groups: normal control group, ISO-induced group (isoproterenol (ISO), 150 mg/kg, s.c.) and two groups treated by TD.HK01® in different doses (0.31 and 0.92 g/kg, orally + ISO 150 mg/kg, s.c.). ResultsTD.HK01® treated groups showed significant improvement as in abnormal electrocardiography (ECG) alteration ratio, in decreased biochemical specific markers troponin T and in decreased non-specific biochemical markers (LDH and AST) between each of TD.HK01® treated groups and ISO-induced group. The effect on vascular system was also evaluated through serum eNOS quantification and a notable increase in an anti-oxidative enzyme catalase. All three groups, except the normal control one, had pathological lesions in histopathology in different levels - modest injuries in treated groups and more severe in ISO-induced group. ConclusionsIt is concluded on the basis of the findings that isoproterenol induced MI in all three groups and TD.HK01® did have its potential protective effect in vivo on cardiovascular system.

A Review on Gelatin Production and a Special Type of Hard Gelatin Capsules With Their Packaging and Storage

In this review it is explained about production of gelatin and a special type of hard gelatin capsules with their packaging and storage. Capsules are solid dosage preparations that contain a soft soluble shell of gelatin that encloses the drug substance(s) and/or excipients whereas hard capsules are made up of two pieces that resemble cylinders that are closed at one end: the longer piece is called the "body," and the shorter piece is called the "cap." A variety of formulation types, the majority of which are meant for oral administration, can be filled into capsules. Special applications include capsules that can be added to diagnostic kits, loaded into dry powder inhalers and occasionally soft-shell capsules meant to be inserted as suppositories into the vagina or the rectal cavity. Gelatin or another appropriate polymeric material is typically used to create the sell, which produces an elegant, tasteless, odourless, simple, and easily swallowed dosage form without the need for a second coating step. Capsules can be categorized as hard or soft depending on the makeup of the capsule shell. There was also emphasis on the different packaging and storage techniques.

Self-emulsifying drug delivery systems and the application in drugs and cosmetics

Self-emulsifying drug delivery systems (SEDDS) have the potential to enhance the bioavailability and therapeutic impact of active ingredients that are poorly water-soluble, low pemeability and unstable. The active ingredient, oil, surfactant, co-surfactant and/or co-solvent are the main elements of SEDDS. Supersaturable SEDDS have been developed to increase the efficiency of active ingredient loading by incorporating precipitation inhibitors (PIs) into SEDDS that help maintain the supersaturated state, preventing drug precipitation in the gastrointestinal tract. Due to these benefits, SEDDS have been studied and applied in drugs and cosmetics in various dosage forms including solidification (S-SEDDS) by different techniques to create powder, granules, pellets to apply to tablets, hard capsules as well as soft capsules, lotions, and some other semi-solid dosage forms... This review mainly focuses on the components, formulation, and applications of SEDDS in the pharmaceutical and cosmetic products.

Simultaneous determination of 11 nootropic substances potentially adulterated in dietary supplements for improving brain function using ultra-performance liquid chromatography and liquid chromatography–quadrupole-time-of-flight mass spectrometry

Recently, the demand for improved brain function and concentration has increased in the dietary supplement market. However, to artificially enhance their pharmacological efficacy, dietary supplements may be illegally adulterated with unauthorised substances. Therefore, we developed a rapid and accurate method to simultaneously determine 11 nootropic substances using an ultra-high-performance liquid chromatography (UPLC) system equipped with a photodiode array (PDA) detector. In addition, sample preparation procedures were semi-optimised for various types of matrices, including solid (hard capsule, tablet, powder, and pill) and liquid (oil and extract) samples. The method was validated to determine the limit of detection (LOD), limit of quantification (LOQ), method detection limit (MDL), method quantitation limit (MQL), specificity, linearity, precision, accuracy, recovery, stability, and matrix effects. The validation results satisfied international validation guideline requirements. To test the applicability of the method, 55 real samples advertised as effective brain health, memory, and cognition supplements were analysed. Among the real samples, vinpocetine (2.483 and 7.296 µg/g), and kavain (69–44.056 µg/g) were detected. In addition, the detected compounds were confirmed by comparing their fragmentation patterns with those of the reference standards using liquid chromatography–quadrupole-time-of-flight mass spectrometry (LC-QTOF/MS). In conclusion, the UPLC-PDA method not only rapidly and accurately quantifies illegal nootropics but also enables the pre-emptive investigation and identification of 11 nootropic substances in illegal dietary supplements to protect public health.

Development of a potential carrageenan-based hard capsule as the alternative of conventional capsules by implementing the oligomerization reaction

Carrageenan-based (CRG) hard capsules have a slower disintegration rate compared to that of gelatin capsules. Therefore, there is an urgent need to optimize the performance of this material using the oligomerization process. The preparation was conducted by oligomerizing CRG, cross-linking it with maltodextrin (MD), and plasticizing it with sorbitol (SOR). Based on our research, we found that the capsule prepared with the code CRG(O)-MD/SOR had an ash content of 11.80% and a water content of 17.20 ± 1.20 %. No microbes or yeast were found in the capsule, and only negligible amounts of heavy metal traces were present. Scanning electron microscopy (SEM) morphology analysis of the capsule surface showed that no pores were observed, even at a magnification of 10,000 times. This result was supported by the BET-BJH analysis, which showed that the pores had an average diameter of 49.26 Ǻ. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) showed that the Tg of the prepared capsules was at 51.4 °C. Fourier-transform infrared spectroscopy (FTIR) analysis showed that the presence of citric acid as the oligomerization agent had changed the chain composition of the carrageenan. Acute toxicity analysis showed that the capsule was safe even at a dose of 3,000 mg/bw. The Young's modulus of CRG(O)-MD/SOR was determined to be 1.500 ± 0.52 MPa. In vitro disintegration testing of CRG(O)-MD/SOR showed that the capsule required 20.01 ± 1.13 mins, 23.13 ± 1.14 mins, and more than 120 mins to disintegrate at pH 1.2, 4.5, and 6.8, respectively. Release kinetics analyses showed that the drugs paracetamol (PCT) and salicylamide (SCA) followed the zeroth-order model at pH 1.2 and 4.5, while they were best described by the Peppas-Sahlin model at pH 6.8. Finally, the maximum swelling degree of the CRG(O)-MD/SOR hard capsule was determined to be 708.88%, which was reached in 15.22 mins. This capsule has the potential to be used as an alternative to conventional hard capsules on a broader scale. Furthermore, this work supports Sustainable Development Goals (SDGs) point 3, good health and well-being, by providing a capsule made from biomaterial.

Drying Process of HPMC-Based Hard Capsules: Visual Experiment and Mathematical Modeling.

Using plant-based polysaccharide gels to produce hard capsules is a novel application of this technology in the medicinal field, which has garnered significant attention. However, the current manufacturing technology, particularly the drying process, limits its industrialization. The work herein employed an advanced measuring technique and a modified mathematical model to get more insight into the drying process of the capsule. Low field magnetic resonance imaging (LF-MRI) technique is adopted to reveal the distribution of moisture content in the capsule during drying. Furthermore, a modified mathematical model is developed by considering the dynamic variation of the effective moisture diffusivity (Deff) according to Fick's second law, which enables accurate prediction of the moisture content of the capsule with a prediction accuracy of ±15%. The predicted Deff ranges from 3 × 10-10 to 7 × 10-10 m2·s-1, which has an irregular variation with a time extension. Moreover, as temperature increases or relative humidity decreases, there is an increased acceleration of moisture diffusion. The work provides a fundamental understanding of the drying process of the plant-based polysaccharide gel, which is crucial for enhancing the industrial preparation of the HPMC-based hard capsules.

Analysis of trends in the positioning of pharmaceutical drugs of the SGLT-2 class of gliflozin derivatives at the pharmaceutical market and the application prospects

Aim – is to analyze trends in the use and positioning of pharmaceuticals of the class of gliflozin derivatives on the Ukrainian pharmaceutical market.
 Materials and methods. In the conducted research, the methods of systematic and comparative analysis, generalization, statistical processing and synthesis were used in determining the projected perspectives, tabular and graphic means of presenting the results. To implement the goal and objectives of the research, software and electronic resources of ATX (Anatomical-Therapeutically-Chemical), ATC (Anatomical Therapeutically Chemical Classification System), BSC (Biopharmaceutical Classification System), Vidal, Compendium, and the State Register of Medicinal Products of Ukraine were used.
 Results of the research. The results of a systematic analysis of application trends and a comparative analysis of marketing research on the positioning of pharmaceuticals of the class of gliflozin derivatives on regulated markets and the Ukrainian pharmaceutical market are presented. A steady trend in the positioning of the number of appointments in the segments of mono and combined drugs and the number of sales on regulated markets was revealed. It is established that as of the end of 2022, the total number of pharmaceuticals from API class SGLT-2 pharmaceutically acceptable of gliflozin derivatives in the form of solid dosage forms, which are positioned on regulated markets and pharmaceutical campaign research on the pharmaceutical development of new dosage forms of mono and combined drugs is 35, the number of registered pharmaceutical drugs in Ukraine is 4 mono and 2 combined drugs. The segment of this group of drugs - mono and combined drugs - has been systematized, according to the ATX classification by active substances - API - pharmaceutically acceptable salts of gliflozin derivatives on regulated markets and on the pharmaceutical market of Ukraine.
 Conclusions. The analysis of positioning on regulated markets and statistics of R&D research of pharmaceutical companies for the development of new dosage forms of mono and combined drugs provides grounds to generalize and conclude that SGLT-2 inhibitors are the newest and promising class of antidiabetic drugs, which, according to evidence-based medicine, are used in combination with with insulin and other antidiabetic drugs in the treatment of diabetes mellitus (DM) of I and II types, in combined regimens with metformin and DPP-4 inhibitors, as well as in combinations of all three and TZD drugs. SGLT-2 inhibitors are the second largest group of antidiabetic agents by the volume of clinical trials, which is 12%.
 Recommended for use by FDA regulatory authorities, EMA is an API of the SGLT-2 class of pharmaceutically acceptable derivatives of gliflozin: canagliflozin, dapagliflozin, empagliflozin, ertugliflozin, ipragliflozin, luseogliflozin, tofogliflozin, sotagliflozin, as well as pharmaceutically acceptable salts; remogliflozin etabonate; sergliflozin etabonate.
 It has been established that SGLT-2 API drugs of pharmaceutically acceptable derivatives of gliflozin have a constant trend of positioning the number of appointments in the segments of mono and combined drugs and the number of sales on regulated markets, the total amount is 35 in the form of solid dosage forms. Distribution by volume of sales of solid dosage forms of pharmaceutical preparations with API class SGLT-2 of pharmaceutically acceptable of gliflozin derivatives is: tableted monopreparations – 59.2%; combined – 37.2%; mono preparations, hard capsules - 3.6%.
 The number of registered pharmaceutical drugs in Ukraine is 4 mono and 2 combined drugs, the level of prices from a pharmacoeconomic point of view, according to the results of price comparison of other antihyperglycemic drugs, are not affordable for Ukrainian patients who need systemic use. Therefore, the increase in the range of SGLT-2 class API drugs of pharmaceutically acceptable gliflozin derivatives on the Ukrainian pharmaceutical market and competitive manufacturers will contribute to the availability of use for the treatment of DM in Ukrainian patients.
 Key words: trends; positioning; application; pharmaceutically acceptable derivatives of gliflozin; drug support; best practice; evidence-based medicine; rational pharmacotherapy.

Fish sperm cryopreservation using biodegradable containers: New low-cost and environment-friendly methodology.

The containers used in cell cryopreservation are essential to maintain cell integrity and viability after thawing. This paper reveals the methodology of using biodegradable containers for fish sperm cryopreservation. Cryopreserved sperm in biodegradable containers showed high fertility capability. Biodegradable capsules could be alternative containers to plastic straws for sperm cryopreservation. Containers used to cryopreserve sperm are made with non-biodegradable plastic compounds, having a high monetary and environmental cost. Therefore, the development of biodegradable alternative containers for cell cryopreservation is necessary. Thus, this study aimed to evaluate the efficiency of hard-gelatin and hard-hydroxypropyl methylcellulose (HPMC) capsules as low-cost and biodegradable alternative containers for sperm cryopreservation. Sperm from 12South American silver catfish Rhamdia quelen were individually cryopreserved in plastic straws 0.25 mL (as control), hard-gelatin, and hard-HPMC capsules. The quality of post-thaw sperm cryopreserved in the different containers was checked by measuring spermatozoa membrane integrity, kinetic parameters, mitochondrial activity, fertilization, hatching, and normal larvae rates. The samples cryopreserved in straws showed a higher percentage of membrane integrity (68%) than those frozen in hard-gelatin (40%) and hard-HPMC capsules (40%). However, we did not observe differences between the samples stored in straws and hard capsules for the rest of the tested sperm parameters. Thus, based on the high sperm fertility capability, both capsules were efficient as cryopreservation containers for maintaining sperm functionality.

Management of obesity

Journal of Prescribing PracticeVol. 5, No. 5 Calculation SkillsManagement of obesityStephen BennettStephen BennettE-mail Address: [email protected]Advanced Specialist Paediatric Pharmacist(Cardiology/CriticalCare/ECMO Glenfield Hospital and De Montfort UniversitySearch for more papers by this authorStephen BennettPublished Online:17 May 2023https://doi.org/10.12968/jprp.2023.5.5.193AboutSectionsView articleView Full TextPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack Citations ShareShare onFacebookTwitterLinked InEmail View article References Centers for Disease Control and Prevention. Measurement Units Formula and Calculation Kilograms and meters (or centimeters). 2023. https://www.cdc.gov/healthyweight/assessing/bmi/childrens_BMI/childrens_BMI_formula.html (accessed 3 March 2023) Google ScholarDavies A. Half of world on track to be overweight by 2035. BBC, 3 March 2023. https://www.bbc.co.uk/news/world-64831848 (accessed 3 March 2023) Google ScholarDonovan L, Hignet J. Food Fact Sheet. British Dietetic Association, 2023. https://www.bda.uk.com/uploads/assets/84f584f6-9294-4a5f-8012bf20e7bedd56/Fat-food-fact-sheet.pdf (accessed 3 March 2023) Google ScholarGlaxoSmithKline Consumer Healthcare. Alli 60 mg hard capsules - Summary of Product Characteristics (SmPC) - (emc), June 2017. https://www.medicines.org.uk/emc/product/6533/smpc#gref (accessed 3 March 2023) Google ScholarNeon Healthcare. Xenical SPC. Xenical 120 mg hard capsules - Summary of Product Characteristics (SmPC) - (emc), Neon Healthcare, July 2008. https://www.medicines.org.uk/emc/product/2592/smpc#gref. (accessed 3 March 2023) Google ScholarNational Institute for Health and Care Excellence. Recommendations: Obesity: identification, assessment and management. London: NICE; 2014 Google Scholar FiguresReferencesRelatedDetails 2 May 2023Volume 5Issue 5ISSN (print): 2631-8385ISSN (online): 2631-8393 Metrics History Published online 17 May 2023 Published in print 2 May 2023 Information© MA Healthcare LimitedPDF download