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pH-responsive CAP-co-poly(methacrylic acid)-based hydrogel as an efficient platform for controlled gastrointestinal delivery: fabrication, characterization, in vitro and in vivo toxicity evaluation

Shah SA, Sohail M, Minhas MU, Nisar-Ur-Rehman, Khan S, Hussain Z, et al.

Drug Deliv Transl Res, 2019 Apr;9(2):555-577.
PMID: 29450805 DOI: 10.1007/s13346-018-0486-8

Cellulose acetate phthalate-based pH-responsive hydrogel was synthesized for fabrication of polymeric matrix tablets for gastro-protective delivery of loxoprofen sodium. Cellulose acetate phthalate (CAP) was cross-linked with methacrylic acid (MAA) using free radical polymerization technique. Fourier transform infrared (FTIR) spectra confirmed the formation of cross-linked structure of CAP-co-poly(methacrylic acid). Thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) confirmed the thermal stability of polymeric networks, and scanning electron microscopy (SEM) and energy-dispersive X-ray spectrum (EDS) images unveiled that the prepared formulations were porous in nature and thus the developed formulations had shown better diffusibility. Swelling and in vitro drug release was performed at various pHs and maximum swelling and release was obtained at pH 7.4, while swelling and release rate was very low at pH 1.2 which confirmed the pH-responsive behavior of CAP-co-poly(MAA). CAP-co-poly(MAA) copolymer prevents the release of loxoprofen sodium into the stomach due to reduced swelling at gastric pH while showing significant swelling and drug release in the colon. Cytotoxicity studies revealed higher biocompatibility of fabricated hydrogel. Acute oral toxicity studies were performed for the evaluation and preliminary screening of safety profile of the developed hydrogels. Matrix tablets were evaluated for release behavior at simulated body pH. The investigations performed for analysis of hydrogels and fabricated matrix tablets indicated the controlled drug release and gastro-protective drug delivery of CAP-co-poly(MAA) hydrogels and pH-sensitive matrix tablets for targeted delivery of gastro-sensitive/irritative agents. Graphical abstract.

Matched MeSH terms: Tablets
Use of prebiotics in oral delivery of bioactive compounds: a nanotechnology perspective

Heidarpour F, Mohammadabadi MR, Zaidul IS, Maherani B, Saari N, Hamid AA, et al.

Pharmazie, 2011 May;66(5):319-24.
PMID: 21699064

The oral route is considered the most patient-convenient means of drug administration. In recent years there has been a tendency to employ smart carrier systems that enable controlled or timed release of a bioactive material, thereby providing a better dosing pattern and minimizing side effects. Nano-encapsulation systems (nanocarriers) offer important advantages over conventional drug delivery techniques. Nanocarriers can protect the drug from chemical/enzymatic degradation and enhance bioavailability. Prebiotics are ideal ingredients for the nano-encapsulation and oral drug delivery due to their natural ability to protect the encapsulated compound in the upper gasterointestinal (GI) tract. Here the potential of prebiotics for oral delivery of drugs and other bioactives is reviewed.

Matched MeSH terms: Tablets, Enteric-Coated
Fulltext Treating More with Less: Effectiveness and Event Outcomes of Antituberculosis Fixed-dose Combination Drug versus Separate-drug Formulation (Ethambutol, Isoniazid, Rifampicin and Pyrazinamide) for Pulmonary Tuberculosis Patients in Real-world Clinical Practice

Lai JML, Yang SL, Avoi R

J Glob Infect Dis, 2019 3 1;11(1):2-6.
PMID: 30814828 DOI: 10.4103/jgid.jgid_50_18

Introduction: Conventionally, a combination of four separate drugs (ethambutol, isoniazid, rifampicin, and pyrazinamide [EHRZ]) is the first-line pharmacotherapy for pulmonary tuberculosis (TB). In recent years, fixed-dose combination (FDC) formulation, where a single tablet contains the active ingredients of four aforementioned drugs, is gaining popularity due to its ease of administration.
Objective: To compare the real-world effectiveness of EHRZ and FDC treatment groups on a cohort registry by investigating the sputum conversion rate and treatment outcomes of both groups.
Methods: A total of 11,489 patients' data were extracted from the Sabah TB registry between January 2012 and June 2016, including EHRZ (n = 4188) and FDC (n = 7301) patients. Then, 1:1 propensity score matching was adopted to reduce the baseline bias. Caliper matching was conducted with maximum tolerance score set at 0.001. Confounders included in the propensity score matching were gender, nationality, diabetes, HIV status, smoking status, and chest X-ray status. Successful matching provided 4188 matched pairs (n = 8376) for final analysis.
Results: In this matched cohort of 4188 pairs, the 2-month sputum conversion rate of FDC group was significantly higher than the EHRZ group (96.3% vs. 94.3%; P < 0.001) whereas 6-month sputum conversion of both groups showed no significant difference. Treatment outcomes such as noncompliance rate, failure rate, and success rate have no significant difference (P > 0.05) in both the treatment groups. There was an incidental finding of reduced death rate among FDC group compared to the EHRZ group (0.2% vs. 0.5%; P = 0.034).
Conclusion: The FDC formulation has better sputum conversion rate at 2 months compared to conventional EHRZ regime as separate-drug formulation. It was also observed that FDC has a slight protective effect against all-cause death among TB patients. This protective effect of FDC, however, still needs to be proven further.

Matched MeSH terms: Tablets
Topologically directed confocal Raman imaging (TD-CRI): Advanced Raman imaging towards compositional and micromeritic profiling of a commercial tablet components

Muthudoss P, Kumar S, Ann EYC, Young KJ, Chi RLR, Allada R, et al.

J Pharm Biomed Anal, 2022 Feb 20;210:114581.
PMID: 35026592 DOI: 10.1016/j.jpba.2022.114581

Particle size distribution (PSD), spatial location and particle cluster size of ingredients, polymorphism, compositional distribution of a pharmaceutical product are few of the most important attributes in establishing the drug release-controlling microstructural and solid state properties that would be used to (re)design or reproduce similar products. There are numerous solid-state techniques available for PSD analysis. Laser diffraction (LD) is mostly used to study PSD of raw materials. However, a constraint of LD is the interference between the active pharmaceutical ingredients (API) and excipients, where it is very challenging to measure API size in a tablet. X-ray powder diffraction (XRPD) is widely employed in establishing the polymorphism of API and excipients. This research examined a commercial osmotic tablet in terms of extracting solid state properties of API and functional excipient by Raman Imaging. Establishing repeatability, reproducibility, and sample representativeness when the samples are non-uniform and inhomogeneous necessitates multiple measurements. In such scenarios, when employing imaging-based techniques, it can be time-consuming and tedious. Advanced statistical methodologies are used to overcome these disadvantages and expedite the characterization process. Overall, this study demonstrates that Raman imaging can be employed as a non-invasive and effective offline method for assessing the solid-state characteristics of API and functional excipients in complex dosage forms like osmotic tablets.

Matched MeSH terms: Tablets
Three-ways crossover bioequivalence study of cephalexin in healthy Malay volunteers

Liew KB, Peh KK, Loh GO, Tan YT

Drug Dev Ind Pharm, 2014 Sep;40(9):1156-62.
PMID: 23688276 DOI: 10.3109/03639045.2013.798805

Although the general pharmacokinetics of cephalexin is quite established up-to-date, however, no population-based study on Cephalexin pharmacokinetics profile in Malay population has been reported yet in the literature.

Matched MeSH terms: Tablets/pharmacokinetics
Thermal sintering: a novel technique used in the design, optimization and biopharmaceutical evaluation of propranolol HCl gastric floating tablets

Venkata Srikanth M, Songa AS, Nali SR, Battu JR, Kolapalli VR

Drug Dev Ind Pharm, 2014 Jan;40(1):33-45.
PMID: 23317339 DOI: 10.3109/03639045.2012.744416

The objective of the present investigation was to study the applicability of thermal sintering technique for the development of gastric floating tablets of propranolol HCl. Formulations were prepared using four independent variables, namely (i) polymer quantity, (ii) sodium bicarbonate concentration, (iii) sintering temperature and (iv) sintering time. Floating lag time and t95 were taken as dependent variables. Tablets were prepared by the direct compression method and were evaluated for physicochemical properties, in vitro buoyancy and dissolution studies. From the drug release studies, it was observed that drug retarding property mainly depends upon the sintering temperature and time of exposure. The statistically optimized formulation (PTSso) was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry studies, and no significant chemical interaction between drug and polymer was observed. Optimized formulation was stable at accelerated conditions for a period of six months. PTSso was evaluated for in vivo buoyancy studies in humans for both fed and fasted states and found that gastric residence time of the floating tablets were enhanced by fed stage but not in fasted state. Optimized formulation PTSso and commercial formulation Ciplar LA 80 were subjected to bioavailability studies in healthy human volunteers by estimating pharmacokinetic parameters such as Cmax, Tmax, area under curve (AUC), elimination rate constant (Kel), biological half-life (t1/2) and mean residence time (MRT). There was a significant increase in the bioavailability of the propranolol HCl from PTSso formulation, which was evident from increased AUC levels and larger MRT values than Ciplar LA 80.

Matched MeSH terms: Tablets
Thermal sintering: a novel technique in the design of gastroretentive floating tablets of propranolol HCl and its evaluation

Meka VS, Songa AS, Nali SR, Battu JR, Kukati L, Kolapalli VR

Invest Clin, 2012 Sep;53(3):223-36.
PMID: 23248967

The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50 degrees C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used.

Matched MeSH terms: Tablets*
Fulltext The use of Hibiscus esculentus (Okra) gum in sustaining the release of propranolol hydrochloride in a solid oral dosage form

Zaharuddin ND, Noordin MI, Kadivar A

Biomed Res Int, 2014;2014:735891.
PMID: 24678512 DOI: 10.1155/2014/735891

The effectiveness of Okra gum in sustaining the release of propranolol hydrochloride in a tablet was studied. Okra gum was extracted from the pods of Hibiscus esculentus using acetone as a drying agent. Dried Okra gum was made into powder form and its physical and chemical characteristics such as solubility, pH, moisture content, viscosity, morphology study using SEM, infrared study using FTIR, crystallinity study using XRD, and thermal study using DSC and TGA were carried out. The powder was used in the preparation of tablet using granulation and compression methods. Propranolol hydrochloride was used as a model drug and the activity of Okra gum as a binder was compared by preparing tablets using a synthetic and a semisynthetic binder which are hydroxylmethylpropyl cellulose (HPMC) and sodium alginate, respectively. Evaluation of drug release kinetics that was attained from dissolution studies showed that Okra gum retarded the release up to 24 hours and exhibited the longest release as compared to HPMC and sodium alginate. The tensile and crushing strength of tablets was also evaluated by conducting hardness and friability tests. Okra gum was observed to produce tablets with the highest hardness value and lowest friability. Hence, Okra gum was testified as an effective adjuvant to produce favourable sustained release tablets with strong tensile and crushing strength.

Matched MeSH terms: Tablets
The influence of different plasticizers on some physical and mechanical properties of hydroxypropyl methylcellulose free films

Saringat HB, Alfadol KI, Khan GM

Pak J Pharm Sci, 2005 Jul;18(3):25-38.
PMID: 16380341

Coating has been widely used in pharmaceutical manufacture either as non-functional or a functional entity. The objectives of the present study were to investigate the effect of plasticizers such as PEG400, PEG1000 and triacetin on mechanical properties, glass transition temperature and water vapor transmission of free films prepared from HPMC and/or HPMC:PVA blends, to develop suitable coating system for tablets, and to determine the release profiles of the coated tablets. The tensile strength of plasticized HPMC films was generally lower than that of control HPMC film and could be attributed to increased crystallinity and segmental chain mobility of HPMC. This effect increased as the concentration of plasticizer increased. Generally the addition of both grades of polyethylene glycol (PEG400 & PEG1000) increased the moisture permeability of HPMC films but the films containing triacetin provided a more rigid barrier to moisture compared to unplasticized HPMC films. The dissolution profiles of paracetamol tablets coated with 7% w/v HPMC coating-solutions containing PEG400, PEG1000 and triacetin, and those containing PEG400 & PVA together showed that HPMC had weak water resistance. The presence of PEG400 and 1000 in HPMC films further weakened its resistance to solubility while the presence of triacetin caused a little increase in HPMC water resistance. From the results it was concluded that HPMC at 7%w/w concentration was suitable for film-coating intended for non-functional coating. Presence of the PEG 400, PEG1000 and triacetin as well as the presence of PVA and PEG400 together improved the coating properties of HPMC films and made it more suitable as a non-functional coating material.

Matched MeSH terms: Tablets*
The influence of consumers' preferences and perceptions of oral solid dosage forms on their treatment

Ibrahim IR, Ibrahim MI, Al-Haddad MS

Int J Clin Pharm, 2012 Oct;34(5):728-32.
PMID: 22744843 DOI: 10.1007/s11096-012-9667-6

BACKGROUND: Beyond the direct pharmacological effect of medicines, preferences and perceptions toward a particular oral solid dosage form (OSDF) play a crucial role in recovery and may reduce adherence to the prescribed treatment.
OBJECTIVES: This study conducted to investigate the most preferred OSDF and the degree to which swallowing solid medication is an issue, to assess perceptions of the therapeutic benefits of the OSDF, and to find predictors of the most preferred OSDF.
METHOD: A cross-sectional study, through convenience sample method, was conducted to survey consumers visiting community pharmacies in Baghdad, Iraq. Data was collected by self-administered and pre-piloted questionnaires, and analyzed using Statistical Package for Social Science. Multiple logistic regression analysis and Chi-square tests were used at alpha level = 0.05.
RESULTS: A total of 1,000 questionnaire were included in the analysis. Of all respondents, 52.9 % preferred capsule among other OSDF and this preference varied significantly with a number of socio-demographic factors. Ease of swallowing solid medication was the main issue which resulted in preferences for a particular form. A negative perception of the therapeutic benefits of the OSDF was found among 89.1 % of the consumers. Multiple logistic regression analysis indicated that gender, ease of swallowing, and perceptions of the therapeutic benefits of the OSDF were significant predictors of capsule preferences.
CONCLUSIONS: Given the fact that consumers are the end users of medicines and their preferences may influence response to the treatment, efforts are worthwhile by the prescribers and medicines' manufactures to understand consumers' preferences of a particular dosage form in order to achieve successful therapy outcomes.

Matched MeSH terms: Tablets/administration & dosage
Fulltext Tell tale of tablets in bronchus

Shimpi T, Chawla A, Shikhare S

Med J Malaysia, 2015 Feb;70(1):36-7.
PMID: 26032528

Foreign body (FB) aspiration is an emergency of concern at all ages. However, in adults, it can present with atypical symptoms such as shortness of breath, wheezing or rarely cyanosis. Aspiration of oral medications is seen in the elderly population with impairment of protective airway mechanism. Treatment of choice is endoscopic removal of the foreign body. We report such a case of foreign body aspiration (potassium chloride tablet), diagnosed on imaging and subsequently developed bronchostenosis. There are a very few reported cases of oral potassium supplement aspiration and associated complications in the literature.

Matched MeSH terms: Tablets
Taste-masked and affordable donepezil hydrochloride orally disintegrating tablet as promising solution for non-compliance in Alzheimer's disease patients

Liew KB, Tan YT, Peh KK

Drug Dev Ind Pharm, 2015 Apr;41(4):583-93.
PMID: 24495273 DOI: 10.3109/03639045.2014.884130

Manufacturing process and superdisintegrants used in orally disintegrating tablet (ODT) formulation are often time discussed. However, the effect of suitable filler for ODT formulation is not explored thoroughly.

Matched MeSH terms: Tablets
Tableting Properties and Compression Models of Labisia pumila Tablets

Etti CJ, Yusof YA, Chin NL, Mohd Tahir S

J Diet Suppl, 2017 Mar 04;14(2):132-145.
PMID: 27487244

The tableting properties of Labisia pumila herbal powder, which is well known for its therapeutic benefits was investigated. The herbal powder was compressed into tablets using a stainless steel cylindrical uniaxial die of 13-mm- diameter with compaction pressures ranging from 7 to 25 MPa. Two feed weights, 0.5 and 1.0 g were used to form tablets. Some empirical models were used to describe the compressibility behavior of Labisia pumila tablets. The strength and density of tablets increased with increase in compaction pressure and resulted in reduction in porosity of the tablets. Smaller feeds, higher forces and increase in compaction pressure, contributed to more coherent tablets. These findings can be used to enhance the approach and understanding of tableting properties of Labisia pumila herbal powder tablets.

Matched MeSH terms: Tablets/chemistry*
Suspected-target and non-targeted screenings of phosphodiesterase 5 inhibitors in herbal remedies using liquid chromatography-quadrupole time-of-flight-mass spectrometry

Mohd Yusop AY, Xiao L, Fu S

Drug Test Anal, 2021 May;13(5):965-976.
PMID: 32441056 DOI: 10.1002/dta.2861

The lucrative market of herbal remedies spurs rampant adulteration, particularly with pharmaceutical drugs and their unapproved analogues. A comprehensive screening strategy is, therefore, warranted to detect these adulterants and, accordingly, to safeguard public health. This study uses the data-dependent acquisition of liquid chromatography-quadrupole time-of-flight-mass spectrometry (LC-QTOF-MS) to screen phosphodiesterase 5 (PDE5) inhibitors in herbal remedies using suspected-target and non-targeted strategies. For the suspected-target screening, we used a library comprising 95 PDE5 inhibitors. For the non-targeted screening, we adopted top-down and bottom-up approaches to flag novel PDE5 inhibitor analogues based on common fragmentation patterns. LC-QTOF-MS was optimised and validated for capsule and tablet dosage forms using 23 target analytes, selected to represent different groups of PDE5 inhibitors. The method exhibited excellent specificity and linearity with limit of detection and limit of quantification of <40 and 80 ng/mL, respectively. The accuracy ranged from 79.0% to 124.7% with a precision of <14.9% relative standard deviation. The modified, quick, easy, cheap, effective, rugged, and safe extraction provided insignificant matrix effect within -9.1%-8.0% and satisfactory extraction recovery of 71.5%-105.8%. These strategies were used to screen 52 herbal remedy samples that claimed to enhance male sexual performance. The suspected-target screening resulted in 33 positive samples, revealing 10 target analytes and 2 suspected analytes. Systematic MS and tandem MS interrogations using the non-targeted screening returned insignificant signals, indicating the absence of potentially novel analogues. The target analytes were quantified from 0.03 to 121.31 mg per dose of each sample. The proposed strategies ensure that all PDE5 inhibitors are comprehensively screened, providing a useful tool to curb the widespread adulteration of herbal remedies.

Matched MeSH terms: Tablets
Fulltext Survei penjagaan kanta sentuh di kalangan pemakai di Kuala Lumpur

Norhani Mohidin, Bakyah Lorenza Zaimuri

Jurnal Sains Kesihatan Malaysia, 2012;10(1):41-48.
MyJurnal

Kanta sentuh merupakan alat optikal yang sepatutnya selamat digunakan untuk pembetulan ralat refraksi atau kosmetik. Namun demikian terdapat permasalahan berkaitan kesihatan mata yang timbul akibat sikap pemakai yang tidak patuh kepada garis panduan penjagaan kanta yang disaran oleh pengamal kesihatan mata. Justeru itu satu soal selidik berkaitan penjagaan kanta sentuh dilakukan di kalangan pemakai kanta sentuh di sekitar Kuala Lumpur. Ia berdasarkan 22 set soalan terfokus kepada penjagaan kanta sentuh termasuklah tatacara pembersihan dan disifeksi, rawatan enzim, penggunaan agen pembasah dan kekerapan menghadiri pemeriksaan lanjutan. Di samping itu, terdapat enam soalan yang diaju untuk meninjau pengetahuan pemakai berkaitan penjagaan kanta sentuh yang selamat. Seramai 104 pemakai kanta sentuh mengambil bahagian dalam kajian ini. Lebih kurang 86% daripada mereka adalah wanita dengan min umur 24 ± 6 tahun. Lebih setengah daripada mereka memakai kanta sentuh jenis pakai buang. Hampir kesemuanya (98%) menggunakan sistem disinfeksi kimia. Hanya 68% pemakai yang dikaji mencuci kanta mereka setiap kali sebelum memakai dan selepas menanggalkannya. Tiga puluh peratus (30%) pemakai kanta sentuh menggunakan agen pembasah dan 40% menggunakan tablet protein. Enam puluh satu peratus (61%) daripada mereka menyatakan tidak membuat temu janji untuk pemeriksaan lanjutan. Enam soalan tertumpu kepada pengetahuan pemakai mengenai penjagaan kanta yang selamat dan min jawapan yang betul ialah 61.4%. Sebahagian pemakai kanta sentuh tidak mengikut arahan penjagaan kanta sentuh seperti yang disaran oleh pengamal kesihatan mata. Ramai yang tidak faham akan garis panduan pemakaian kanta yang selamat. Kajian ini menunjukkan sebahagian daripada pemakai kanta sentuh tidak mempunyai pengetahuan yang cukup mengenai risiko dan bahaya ke atas mata mereka kerana ketidakpatuhan pada arahan yang disaran oleh pengamal kesihatan mata. Pengamal kanta sentuh perlu memikirkan semula strategi untuk memastikan pemakai patuh kepada arahan berkaitan penjagaan kanta sentuh supaya komplikasi dapat dikurangkan.

Matched MeSH terms: Tablets
Stability-indicating micellar electrokinetic chromatography method for the analysis of sumatriptan succinate in pharmaceutical formulations

Al Azzam KM, Saad B, Tat CY, Mat I, Aboul-Enein HY

J Pharm Biomed Anal, 2011 Dec 15;56(5):937-43.
PMID: 21873014 DOI: 10.1016/j.jpba.2011.08.007

A micellar electrokinetic chromatography method for the determination of sumatriptan succinate in pharmaceutical formulations was developed. The effects of several factors such as pH, surfactant and buffer concentration, applied voltage, capillary temperature, and injection time were investigated. Separation took about 5 min using phenobarbital as internal standard. The separation was carried out in reversed polarity mode at 20 °C, 26 kV and using hydrodynamic injection for 10s. Separation was achieved using a bare fused-silica capillary 50 μm×40 cm and background electrolyte of 25 mM sodium dihydrogen phosphate-adjusted with concentrated phosphoric acid to pH 2.2, containing 125 mM sodium dodecyl sulfate and detection was at 226 nm. The method was validated with respect to linearity, limits of detection and quantification, accuracy, precision and selectivity. The calibration curve was linear over the range of 100-2000 μg mL(-1). The relative standard deviations of intra-day and inter-day precision for migration time, peak area, corrected peak area, ratio of corrected peak area and ratio of peak area were less than 0.68, 3.48, 3.28, 2.97 and 2.83% and 2.01, 5.50, 4.46, 4.92 and 4.07%, respectively. The proposed method was successfully applied to the determinations of the analyte in tablet. Forced degradation studies were conducted by introducing a sample of sumatriptan succinate standard solution to different forced degradation conditions using neutral (water), basic (0.1 M NaOH), acidic (0.1 M HCl), oxidative (10% H(2)O(2)) and photolytic (exposure to UV light at 254 nm for 2 h). It is concluded that the stability-indicating method for sumatriptan succinate can be used for the analysis of the drug in various samples.

Matched MeSH terms: Tablets
Stability indicating HPLC method for simultaneous quantification of sildenafil citrate and dapoxetine hydrochloride in Pharmaceutical products

Liew KB, Peh KK

Pak J Pharm Sci, 2018 Nov;31(6):2515-2522.
PMID: 30473526

A stability-indicating HPLC-UV method for the simultaneous determination of sildenafil citrate and dapoxetine hydrochloride in solution and tablet was developed. The mobile phase was comprised of acetonitrile and 0.2M ammonium acetate buffer. The analyte was eluted at 3.392min and 7.255min for sildenafil citrate and dapoxetine HCl respectively using gradient system at a flow rate of 1.5mL/min. The theoretical plates count was>2000, tailing factor

Matched MeSH terms: Tablets
Fulltext Solubility enhancement studies on lurasidone hydrochloride using mixed hydrotropy

Madan JR, Pawar KT, Dua K

Int J Pharm Investig, 2015 Apr-Jun;5(2):114-20.
PMID: 25838997 DOI: 10.4103/2230-973X.153390

Low aqueous solubility is a major problem faced during formulation development of new drug molecules. Lurasidone HCl (LRD) is an antipsychotic agent specially used in the treatments of schizophrenia and is a good example of the problems associated with low aqueous solubility. Lurasidone is practically insoluble in water, has poor bioavailability and slow onset of action and therefore cannot be given in emergency clinical situations like schizophrenia. Hence, purpose of this research was to provide a fast dissolving oral dosage form of Lurasidone. This dosage form can provide quick onset of action by using the concept of mixed hydrotropy. Initially, solubility of LRD was determined individually in nicotinamide, sodium citrate, urea and sodium benzoate at concentration of 10, 20, 30 and 40% w/v solutions using purified water as a solvent. Highest solubility was obtained in 40% sodium benzoate solution. In order to decrease the individual hydrotrope concentration mixed hydrotropic agents were used. Highest solubility was obtained in 15:20:5 ratio of Nicotinamide + sodium benzoate + sodium citrate. This optimized combination was utilized in the preparation of solid dispersions by using distilled water as a solvent. Solid dispersions were evaluated for X-ray diffraction, differential scanning calorimetry and Fourier-transform infrared to show no drug-hydrotropes interaction has occurred. This solid dispersion was compressed to form fast dissolving tablets. Dissolution studies of prepared tablets were done using USP Type II apparatus. The batch L3 tablets show 88% cumulative drug release within 14 min and in vitro dispersion time was 32 min. It was concluded that the concept of mixed hydrotropic solid dispersion is novel, safe and cost-effective technique for enhancing the bioavailability of poorly water-soluble drugs. The miraculous enhancement in solubility and bioavailability of Lurasidone is clear indication of the potential of mixed hydrotropy to be used in future for other poorly water-soluble drugs in which low bioavailability is a major concern.

Matched MeSH terms: Tablets
Solubility enhancement effect at absorption site on bioavailability of ritonavir using liquisolid technique

Bonthagarala B, Dasari V, Kotra V

Ther Deliv, 2019 May 01;10(5):295-310.
PMID: 31094300 DOI: 10.4155/tde-2019-0020

Aim: The present study revolved around determining the effect of increase in the solubility of these drugs at the absorption site using ritonavir as a drug model. Materials & methods: Ritonavir per-oral tablets were prepared using versatile and nonionic surfactants having high solubilization rate, which were further marked with high rate of dissolution. The high rate of dissolution formula applied to the solid state characterization by means of transition electron microscopy, differential scanning calorimetry, scanning electron microscopy, X-ray diffraction and infrared spectroscopy. Results & conclusion: The drug bioavailability was seen to increase expressively by administration of liquisolid tablets as compared with conventional tablets.

Matched MeSH terms: Tablets
Smart nanocrystals of artemether: fabrication, characterization, and comparative in vitro and in vivo antimalarial evaluation

Shah SM, Ullah F, Khan S, Shah SM, de Matas M, Hussain Z, et al.

Drug Des Devel Ther, 2016;10:3837-3850.
PMID: 27920499

Artemether (ARTM) is a very effective antimalarial drug with poor solubility and consequently low bioavailability. Smart nanocrystals of ARTM with particle size of 161±1.5 nm and polydispersity index of 0.172±0.01 were produced in <1 hour using a wet milling technology, Dena(®) DM-100. The crystallinity of the processed ARTM was confirmed using differential scanning calorimetry and powder X-ray diffraction. The saturation solubility of the ARTM nanocrystals was substantially increased to 900 µg/mL compared to the raw ARTM in water (145.0±2.3 µg/mL) and stabilizer solution (300.0±2.0 µg/mL). The physical stability studies conducted for 90 days demonstrated that nanocrystals stored at 2°C-8°C and 25°C were very stable compared to the samples stored at 40°C. The nanocrystals were also shown to be stable when processed at acidic pH (2.0). The solubility and dissolution rate of ARTM nanocrystals were significantly increased (P<0.05) compared to those of its bulk powder form. The results of in vitro studies showed significant antimalarial effect (P<0.05) against Plasmodium falciparum and Plasmodium vivax. The IC50 (median lethal oral dose) value of ARTM nanocrystals was 28- and 54-fold lower than the IC50 value of unprocessed drug and 13- and 21-fold lower than the IC50 value of the marketed tablets, respectively. In addition, ARTM nanocrystals at the same dose (2 mg/kg) showed significantly (P<0.05) higher reduction in percent parasitemia (89%) against P. vivax compared to the unprocessed (27%), marketed tablets (45%), and microsuspension (60%). The acute toxicity study demonstrated that the LD50 value of ARTM nanocrystals is between 1,500 mg/kg and 2,000 mg/kg when given orally. This study demonstrated that the wet milling technology (Dena(®) DM-100) can produce smart nanocrystals of ARTM with enhanced antimalarial activities.

Matched MeSH terms: Tablets

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