Plain Tablets Research Articles

Applying Box-Behnken Design in Herbal Product Development: Semha-Pinas Plain Tablets

Phlegm production is a common symptom of upper respiratory tract infections and some allergies. A traditional Thai herbal formula called Semha-Pinas offers an alternative treatment option for managing this symptom. This study aimed to optimize the formulation of Semha-Pinas plain tablets using the Box-Behnken design. Three factors were identified as potentially influencing tablet properties: compressional force, quantity of spray-dried lactose, and quantity of croscarmellose sodium. Initial screening with a one-factor-at-a-time approach helped narrow down the relevant ranges for each factor. Subsequently, the Box-Behnken design was employed with compressional forces ranging from 1,500 to 2,500 psi, spray-dried lactose quantities from 0 to 10%, and croscarmellose sodium quantities from 2 to 4%. Results showed that the optimal formulation, achieving a hardness of 5 to 8 kP, disintegration time of at least 0.5 minutes, and friability of not more than 0.4%, was found at 1,500 psi compressional force, 6% spray-dried lactose, and 3% croscarmellose sodium. This optimized formulation exhibited the following characteristics: tablet weight of 381.23 ± 0.80 mg, diameter of 9.66 ± 0.01 mm, thickness of 4.20 ± 0.04 mm, hardness of 7.50 ± 0.41 kP, disintegration time of 0.67 ± 0.07 minute, and friability of 0.22% ± 0.04%. Verification data confirmed the accuracy of the predictions, with all percent errors falling below 10%. In conclusion, this study successfully applied the Box-Behnken design to develop Semha-Pinas plain tablets that meet the relevant pharmacopoeial criteria.

Quality by design approach in the formulation of vaginal tablet of fluconazole solid dispersion

Vaginal Candidiasis had caused quite frequent gynecological medical consultations. Fluconazole is an antifungal drug that has poor solubility that hinders dissolution and antifungal activity. The study aimed to formulate the sustained release vaginal tablet of Fluconazole solid dispersion through the Design of Experiment approach to guarantee no compromise with the quality. In the first step, Plackett Burman Design was employed for the preliminary screening of the essential factors that would affect the tablet’s property. The significant factors were used further in applying the 32 factorial design and the responses were studied. The drug release, bioadhesive strength and swelling index were taken as the responses and considered as the vital critical quality attributes of the vaginal tablet. The design space was determined through the contour and response surface plots. The tablet was prepared within the design space with the drug release (99.97±0.1%), bioadhesive strength (1671.62±43.23 dynes/cm2), and swelling index (342.47±5 %) that suggested the values lie within the quality target product profile determined previously. The antifungal activity against C. albicans resulted in a larger inhibition zone for the solid dispersion-based tablet (51±3 mm) than the plain drug-based tablet (36±2 mm).

Design and optimization of liquisolid compact based vaginal sustained release tablet of antifungal agent for vaginal candidiasis

Antifungal therapy is causing an alarming drug resistance problem during the treatment of Vaginal Candidiasis and also many of the antifungal vaginal marketed formulations have reported major side-effect of the irritation. Hence the quest for natural therapy is currently booming. Lawsone is having poor aqueous solubility and its antifungal activity is therefore hindered. Therefore, the present research work aimed to formulate the liquisolid compact based vaginal tablet of Lawsone to improve its solubility and dissolution rate. The tablet was optimized by 32 full factorial design. The independent factors selected were carrier (Neusilin US2): coating material (Aerosil 200) ratio (R) and concentration of the mucoadhesive polymer (HPMC K4M) while the dependent factors studied were in vitro release (6 h and 12 h) and mucoadhesive strength. The drug was dispersed in nonvolatile solvent (polyethylene glycol 400) to prepare the liquid medicament that was further used for liquisolid compact. The FTIR, DSC and XRD studies revealed no incompatibility between Lawsone and the excipients of the tablet and suggested that the drug was dispersed completely into the liquid medication and therefore transformed from crystalline to amorphous state. In vitro release study suggested sustained release with enhanced dissolution of optimized liquisolid compact tablet LT7 (94.92%) than the plain tablet (61.16%). The in vitro antifungal activity against C. albicans, C. glabrata and C. krusei for liquisolid tablet and the marketed tablet formulation showed insignificant difference.

Formulation and in vitro Evaluation of Effervescent Bilayer Floating Controlled Release Tablets of Clarithromycin and Famotidine

The development of floating tablets with required buoyancy, lag time, and controlling release behaviour of drugs at target site is truly interesting and challenging task for researchers. Current study is concerned with the designing of effervescent floating controlled release tablets of clarithromycin and famotidine to treat peptic ulcer due to Helicobacter pylori (H. pylori) infection. Five formulations (F1-F5) were prepared, among which three formulations were of bilayered tablets while the remaining were included as plain tablets. These tablets were prepared by direct compression method using hydroxypropyl methylcellulose (HPMC) K100M, HPMC K4M and sodium bicarbonate as swelling and floating agents respectively. The qualitative tests such as thickness, hardness, weight variation, friability and uniformity of content were performed to ensure the quality of prepared tablets. The floating lag time of all formulations ranged from 14 to 20 seconds. The effervescent floating tablets with HPMC K4M (F1, F3 & F5) attained the total floating time of more than 12 hours, while tablets prepared with HPMC K100M (F2 & F4) achieved the total floating time of less than 7 hours. This difference in floating behaviour could be due to the variation in compaction and flow properties of the two polymers. The formulations with HPMC K100M (F2 & F4) have comparatively more sustained drug release properties when compared to F1, F3 and F4 using HPMC K4M as swelling and floating polymers. This could be attributed to better compaction of HPMC K100M. The prepared tablets follow non-Fickian diffusion kinetics. Overall, these floating controlled release effervescent bilayer and plain tablets may enhance the compliance and therapeutic outcomes of clarithromycin and famotidine in treatment of H. pylori.

Preparation and Characterization of Cellulose and Microcrystalline Cellulose from Sugarcane Bagasse and Assessment of the Microcrystalline Cellulose as a Directly Compressible Excipient

Cellulose, the most abundant biomass material in nature finds wide applications in the pharmaceutical industry. Sugarcane bagasse (SCB) is one of the main agricultural lignocellulose byproducts. The objective of this study was to prepare and characterize native and microcrystalline cellulose (MCC) from SCB and evaluate the MCC as a directly compressible pharmaceutical excipient. Cellulose was extracted from SCB by chlorine-free methods with or without dewaxing. MCC was prepared from the cellulose by hydrolysis using hydrochloric acid, and subsequently oven-dried (OD) or spray-dried (SD). The as-obtained cellulose and MCC were characterized in terms of yield, degree of polymerization (DP), chemical functionality, crystallinity, morphology and thermal stability. The chemical composition, particle size, densities and direct compressibility of MCCs were also determined. Cellulose yields on a dry weight basis were found to be 42.8 ± 1.10% and 43.5 ± 0.5% from non-dewaxed and dewaxed SCB, respectively. Dewaxed SCB cellulose (DSCBC) provided higher yield of MCC (DSCB-MCCOD, 83 ± 0.74%) than non-dewaxed SCB cellulose (SCBC) (SCB-MCCOD; 78 ± 1.07%). The DP of SCBC and DSCBC were 580.56 and 592.75, respectively, while the DP of MCC ranged from 230.10 - 251.40. The FTIR spectra of both cellulose and MCC were similar with that of Avicel PH-101. The degree of crystallinity of the dewaxed cellulose (77.34%) and MCCOD (79.56%) and MCC-SD (81.87%) were higher than non-dewaxed cellulose (74.50%) and MCC-OD (78.11%) and MCC-SD (79.62%). Scanning electron micrographs (SEM) showed a fibrous structure for DSCBC and rod-shaped for DSCB-MCC. Thermogravimetric analysis (TGA) revealed dewaxed products exhibited better thermal stability than non-dewaxed products. All MCC samples exhibited monomodal normal particle size distributions. The Hausner ratio and Carr’s index of DSCB-MCCOD and Avicel PH-101 were not significantly different (p < 0.05) indicating similar flow property and compressibility of the materials, respectively. Also, plain tablets prepared from SCB-MCC showed reasonably high crushing strengths (MCC-SD > MCC-OD), although tablets of Avicel PH-101 showed the highest crushing strengths. Thus, SCB could be an alternative source of cellulose and MCC for pharmaceutical applications.

Comparative Evaluation of Porous Carriers for Dissolution Improvement of BCS Class II Drug

The objective of present investigation was comparison of porous carriers to increase the dissolution properties of BCS class II drug Ziprasidone. Solvent evaporation method was used for the adsorption of ziprasidone on various porous carriers. Three different porous carriers namely Florite, Neusilin US2, Sylysia 350 were used in the study. Prepared microparticles were characterised for invitro drug release, SEM, XRD and DSC. The optimized formulation containing ziprasidone: florite microparticles had high drug release (94.88% in 45 min) than plain ziprasidone tablets (21.13% in 45 min) which is due to increase in surface area and decrease in crystallinity of drug after adsorption onto porous carrier.

Formulation and in Vitro Evaluation of Valsartan Flash Tablet

Introduction: Flash tablet is one of the newer technologies that recently have been focused on flash tablet offers many advantages such as fast disintegration and dissolution. However, it has many issues and drawbacks such as fragility of the final tablet and difficult manufacturing process. In this work valsartan (the antihypertensive medication) was fabricated as lyophilized tablets to improve its dissolution profile and bring about all the advantages of this drug delivery system, such as rapid disintegration. Materials and Methods: Mannitol, hydroxylpropyl methyl cellulose (HPMC 5E) and tween 80 were used as matrix, binder, and dissolution enhancer; respectively. The effect of their concentrations on physiochemical properties were evaluated in vitro by conducting mechanical strength test, content uniformity, weight variation test, and the dissolution profile. Results: The hardness and friability have shown using HPMC 5E at concentration 5% will yield a better mechanical property and the best disintegration time. Dissolution profile have shown that using tween 80 at concentration 1% would improve valsartan dissolution significantly. Conclusion: Valsartan flash tablet offers a good alternative to plain tablet with acceptable pharmaceutical properties. How to Cite this Article Pubmed Style Sattar M, Alshawi MA, Mosa MN. and in Vitro Evaluation of Valsartan Flash Tablet. SRP. 2020; 11(10): 213-219. doi:10.31838/srp.2020.10.36 Web Style Sattar M, Alshawi MA, Mosa MN. and in Vitro Evaluation of Valsartan Flash Tablet. http://www.sysrevpharm.org/?mno=16475 [Access: March 30, 2021]. doi:10.31838/srp.2020.10.36 AMA (American Medical Association) Style Sattar M, Alshawi MA, Mosa MN. and in Vitro Evaluation of Valsartan Flash Tablet. SRP. 2020; 11(10): 213-219. doi:10.31838/srp.2020.10.36 Vancouver/ICMJE Style Sattar M, Alshawi MA, Mosa MN. and in Vitro Evaluation of Valsartan Flash Tablet. SRP. (2020), [cited March 30, 2021]; 11(10): 213-219. doi:10.31838/srp.2020.10.36 Harvard Style Sattar, M., Alshawi, . M. A. & Mosa, . M. N. (2020) and in Vitro Evaluation of Valsartan Flash Tablet. SRP, 11 (10), 213-219. doi:10.31838/srp.2020.10.36 Turabian Style Sattar, Mohammed, Malathe A. Alshawi, and Mazin Nadhim Mosa. 2020. and in Vitro Evaluation of Valsartan Flash Reviews in Pharmacy, 11 (10), 213-219. doi:10.31838/srp.2020.10.36 Chicago Style Sattar, Mohammed, Malathe A. Alshawi, and Mazin Nadhim Mosa. Formulation and in Vitro Evaluation of Valsartan Flash Tablet. Systematic Reviews in Pharmacy 11 (2020), 213-219. doi:10.31838/srp.2020.10.36 MLA (The Modern Language Association) Style Sattar, Mohammed, Malathe A. Alshawi, and Mazin Nadhim Mosa. Formulation and in Vitro Evaluation of Valsartan Flash Tablet. Systematic Reviews in Pharmacy 11.10 (2020), 213-219. Print. doi:10.31838/srp.2020.10.36 APA (American Psychological Association) Style Sattar, M., Alshawi, . M. A. & Mosa, . M. N. (2020) and in Vitro Evaluation of Valsartan Flash Reviews in Pharmacy, 11 (10), 213-219. doi:10.31838/srp.2020.10.36

Multiple Unite Pellet Systems (MUPS) as Drug Delivery model

Multiparticulate drug delivery systems are mainly oral dosage form, consist of small discrete units that exhibit different characteristics especially in release pattern and drug bioavailability. These systems are represented by granules, pellets, microspheres, microcapsules, and minitablets. Pellets offer high flexibility in the design, formulation, and development of oral dosage forms such as sachet, suspension, capsule, and tablet. Multiparticulate tablets manufactured by compaction of multiple unite pellets is one of the latest and, yet, challenging technologies. Multiparticulate tablets combine the benefits of both a tablet and a pellet-filled capsule in one dosage form but their manufacturing experience many difficulties. The oral multiparticulate products consist of polymer-coated subunits or pellets, which are embedded in an inert excipients’ matrix, formulated to overcome the difficulty in administering capsules and improve the physicochemical stability of suspension and offer predictable release and uniform distribution in the gastro-intestinal tract compared to the plain tablet. This review discusses the advantages and drawbacks of MUPS, the properties of an ideal MUPS, various pharmaceutical applications of MUPS, the challenges and key variables that to be considered in the tableting process for successful production of MUPS
 Keywords: MUPS®, Pellets, Multiparticulate tablets.

Evaluation of the Properties of Encapsulated Stavudine Microparticulate Lipid-based Drug Delivery System in Immunocompromised Wistar Rats.

Lipid-based formulations have been confirmed to lower some side effects of drugs and can be tailor-made to offer sustained drug release of drugs with short half-life like stavudine. This study aimed to evaluate the immunomodulatory properties of stavudine-loaded solid lipid microparticles (SLMs) using immunocompromised Wistar rats. The SLMs were formulated by the homogenization method. The optimized batches were used for further in vivo studies. The effect of formulation on the CD4 count and the haematological properties of immunocompromised Wistar rats were studied. The particle size range was 4 -8 μm, EE range was 85-93 % and maximum drug release was observed at 10 h. The CD4 cells increased from 115 ± 3.17 cell/mm3 at day zero to 495 ± 5.64 cell/mm3 at day 14 of treatment and 538 ± 6.31 cell/mm3 at day 21. The red blood cells increased from 2.64 ± 1.58 (x 106/mm3) at day zero to 6.96 ± 3.47 (x 106/mm3) at day 14 and 7.85 ± 3.64 (x 106/mm3) at day 21. PCV increased significantly (p < 0.05) to about 42-50 % at day 21 in the groups that received the SLMs formulations. White blood cells (WBC) also were 12 x 103/mm3, for SLM formulations, while the rats that received plain stavudine exhibited WBC of 9.6 x 103/mm3 at day 21. The histopathological studies revealed that oral stavudine-loaded SLMs had no significant damage to the kidney, liver, spleen and the brain of Wistar rats. The formulations exhibited significantly higher immunomodulatory properties than plain stavudine (p<0.05) and showed good properties for once daily oral administration and could be a better alternative to plain stavudine tablets for the management of patients living with HIV.

Formulation development and characterization of cellulose/ polyacrylic acid – based polymers on the release of celecoxib from extended release tablets

The study was aimed to formulate an extended release matrix tablets of celecoxib and to investigate the influence of different types and concentration of polymers on release of drug. Six formulations namely F1 – F6 were manually designed using different proportions of polymers. The matrix tablets formulations (F1 – F5) were composed of using different polymers such as, hydroxypropyl methylcellulose (HPMC-K4M), carboxymethyl cellulose (CMC), ethylcellulose (EC-10 cps) and Carbopol-940, whereas plain tablets formulation (F6) without polymer contained microcrystalline cellulose (MCC), lactose monohydrate, sodium lauryl sulfate (SLS) and polyvinylpyrrolidone (PVP-K30). The MCC, SLS and PVP-K30 were used in a fixed quantity in all formulations except F6 i.e. 20.7%, 6.7%, and 2%, respectively. Multiple point dissolution was performed in phosphate buffer of pH 7.4. Dissolution profiles indicated that formulations F2 and F3 extended the drug release up to the desired time period of 12 h. DD Solver (an add-in software for MS Excel) was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Higuchi and Korsmeyer–Peppas models. However, formulation (F3) containing HPMC – K4M as a matrix former showed concentration-independent drug release as highest linearity was observed when zero-order model was applied (R2 = 0.933). Release mechanism of formulations F3 was super case-II transport. Fourier transform infrared spectroscopy (FTIR) was used to assess the drug polymers compatibility and no drug– excipients interaction was found. The present study accomplished that ethylcellulose and HPMC can be used successfully to develop an extended release matrix tablet formulation.

Enhancement of Dissolution Rate of Telmisartan by Solid Dispersion Technique

Telmisartan is an angiotensin II type-1 receptor antagonist, used in the treatment of essential hypertension. Telmisartan belongs to class II under biopharmaceutical classification system, characterized by low solubility and high permeability. Oral absorption of Telmisartan is dissolution rate limited and it requires enhancement of solubility and dissolution. The main objective of the present study is to increase the solubility and dissolution rate of telmisartan through solid dispersion technology using various concentrations of water soluble carriers such as poly vinyl pyrrolidone, polyethylene glycol 4000 and poloxomer 407. Solid dispersions were prepared by solvent evaporation technique using methanol as solvent. The enhancement of dissolution rate depends on the nature and concentration of the carrier. The order of increasing dissolution rate with water soluble carriers was poloxomer 407 > polyethylene glycol 4000 > polyvinyl pyrrolidone. Increasing dissolution may be due to the reduced particle size of the drug, enhanced wettability of the drug by hydrophilic carriers. The formulations were evaluated by fourier transform infrared spectroscopy. Telmisartan tablets formulated employing selected solid dispersions gave higher dissolution than the plain tablets.

AB096. Cause analysis of double J tube retention and the study of endoscopic minimally invasive management

BackgroundTo analyze the common causes of double J tube retention and to explore the safety and effectiveness of endoscopic minimally invasive management of double J tube retention.MethodsThe clinical data of 34 patients with difficult extubation of double J tube under conventional cystoscope from November 2012 to March 2018 in our center were retrospectively analyzed, including 22 cases of double J tube indwelling in the operation of upper urinary calculi and 12 cases due to ureteral stenosis and obstruction. Patients were diagnosed as double J tube retention according to the medical history, combined with abdominal plain tablets (KUB) plain film, total abdominal CT and other imaging findings. Among them, double J tube was located in the left side of ureter in 15 cases, right side in 15 cases, bilateral in 4 cases, with an average retention time of 10.64 months (0.5 to 72 months). The minimally invasive endoscopic technique was performed alone or in combination with cystoscopy, ureteroscopy and percutaneous nephrolithotomy.ResultsSeventeen cases with peri-tube stone formation and 10 cases of double J tube displacement resulting in retention and difficulty in extubation. Four patients had forgotten extubation after discharge. Two patients with severe urinary tract infection underwent stents replacement after anti infection treatment. One case of severe hematuria accompanied by bladder spasm led to failure of extubation. All stranded double J tubes were successfully removed, of which 14 cases were removed by ureteroscopy, 12 by cystoscopy or ureteroscopic lithotripsy, and 8 cases were removed by the combination of cystoscopy, ureteroscopy and percutaneous nephroscope. The average operation time was 68.5 minutes (14 to 275 minutes). No case was transferred to open surgery. Except for a small amount of hematuria, there were no severe complications such as ureteral perforation, laceration and nephrectomy. Two patients developed hyperthermia after operation and the body temperature returned to normal with active anti-infection treatment. Residual stones were found in 4 patients after operation. The average postoperative hospital stay was 2.7 days (1 to 12 days).ConclusionsThe peri-tube stone formation and displacement of double J tube after long term indwelling are the main reasons for the retention of double J tube. According to the patient’s condition, it is safe and effective to remove the stranded double J tube through minimally invasive endoscopic technique alone or in combination with cystoscopy, ureteroscopy and percutaneous nephroscopy. Moreover, it is necessary to strengthen the management of patients with double J tube indwelling, so as to avoid double J tube being left behind.

Solid dispersion adsorbate technique for improved dissolution and flow properties of lurasidone hydrochloride: characterization using 32 factorial design

The aim of the present study was to improve the dissolution and flow properties of lurasidone hydrochloride (LH) by solid dispersion adsorbate (SDA) technique. Solid dispersions (SDs) of LH were prepared by fusion method using Poloxamer P188. The melt dispersion was adsorbed onto the porous carrier Florite (calcium silicate). A 32 factorial design was employed to quantify the effect of two independent variables, namely ratio of carrier (Poloxamer 188) and LH in SD and ratio of adsorbent (Florite) to SD. SDA granules of LH were studied for flow properties and characterized using differential scanning calorimetry, scanning electron microscopy, and X-ray diffraction. Tablets of optimized composition of SDA granules (equivalent to 20 mg of drug) and plain tablets were prepared by direct compression method. The dissolution studies were carried out in Mcllvaine buffer (pH 3.8) as per USFDA guidelines and characterized for parameters such as percent dissolution efficiency, t50, and Q30. Tablets prepared from SDA granules showed almost four-fold increase in cumulative percentage drug release as compared to tablets prepared from plain LH. The value of dissolution efficiency was enhanced from 49.60% for plain tablets to 94.15% for SDA tablets. SDA granules did not show any change in drug release and X-ray diffraction pattern after storage at 40 °C/75% of RH for 3 months, which confirms that Florite prevented conversion of drug from amorphous form to crystalline form improving physical stability of the amorphous state of LH.

Formulation and Clinical Evaluation of Orphenadrine citrate as a Plain Tablet

Orphenadrine is an anticholinergic ,antimuscarinic , centrally acting skeletal muscle relaxant .It presents in the form of citrate and HCl salts which are used in treatment of the symptoms of mild Parkinson's disease and also it is used as adjuvant with other drugs in the therapy .&#x0D; Many trials were made to formulate Orphenadrine citrate as a plain tablet using wet granulation or direct compression technique in order to get a satisfactory formula through studying the effect of various factors such as binders , diluents and disintegrants types .&#x0D; The best formula was obtained by using Poly Vinyl Pyrolidine (PVP) as a binder also the results indicated that starch and mannitol gave acceptable physical properties to the tablets when they were used as diluents . At the same time , the results showed that Avicel which was used as a disintegrant gave an acceptable disintegration and dissolution time in comparison with the reference tablet DISIPAL Ò. In addition , the selected formula was used to study the effect of method of incorporation of disintegrant on the physical properties of tablets .It was found that the intragranular incorporation resulted in a shorter disintegration and dissolution times .The stability of Orphenadrine citrate prepared tablets was also studied upon storage at 50°C, 60°C and 70°C for four months .The drug was fairly stable and the expiration date for the prepared tablet was considered to be equal for 5 years .On the other hand , the results of clinical study on patients suffering from Parkinson's disease indicated that patients with tremor (regular rhythmic oscillation of extremities especially hand and finger ) and mild symptoms of Parkinson's disease showed a good response to the prepared tablets , but it had no effect on patients of dystonia ( fixed upward gaze , neck twisting ,clenching jaws ) and akinesia ( slow down of movement of voluntary muscle and difficulty of initiation of movement ).&#x0D; The overall results of this study indicate that the drug can be prepared as tablets , which fit the requirements of British Pharmacopoeia since the prepared tablets gave satisfactory results .

The Effect of some Variables on the Formulation of Captopril as Tablets Shaymaa Nazar Al – Sammarrai

Captopril is an angiotensin converting enzyme inhibitor (ACEI) used to treat hypertension,congestive heart failure, and myocardial infraction.The only dosage form available for captopril is the plain tablet in strength of 12.5,25,50 and 100mgtablet.This investigation is concerned with factors affecting the formulation of captopril as a plaintablet dosage form of 50mg. Many trials were made to prepare satisfactory tablets for the drug byusing wet – granulation methods with various additives. It was found that poly vinyl pyrrolidone(P.V.P.) as binder gave the most satisfactory tablets. At the same time a shorter disintegrantion timeand slower dissolution rate were obtained with the addition of starch intragranular.While the distintegration time and dissolution rate were faster for explotab when it was usedintragranular in comparison with starch.A comparative study on the physical properties of the prepared tablets with Capoten®(Squibb), Miniten® (APM), and Capocard® (DAD) tablets, showed that the release of drug from theselected formula was similar to that obtained from Miniten® at 0.1N HCl and 37C.The stability of the prepared tablet was also studied at 50C, 60C, and 70C for 4 months andthe calculated shelf – life was about 3.5years at 25C.

Novel Salted Anionic-Cationic Polymethacrylate Polymer Blends for Sustained Release of Acidic and Basic Drugs.

Since a unique matrix tablet formulation that independently controls the release of various drug types is in a great demand, the objective of this research was to develop a sustained release matrix tablet as a universal dosage form using a binary mixture of the salt forms of Eudragit polymers rather than their interpolyelectrolyte complexes. Tablets were prepared by wet granulation and compressed at different compression forces, depending on drug type. Dissolution tests were conducted using USP XXII rotating paddle apparatus at 50 rpm at 37°C in consecutive pH stages. Tablets containing Ibuprofen (IB) as a model acidic drug and Metronidazole (MD) as a model basic drug showed controlled/sustained release behavior. For IB tablets containing 80% Ibuprofen and 5% (w/w) polymeric combination; the time for 50% of the drug release was about 24 hours compared to 8.5 hours for plain tablets containing 80% IB. In case of MD, the drug release extended to about 7 hours for tablets containing 80% MD and 5% (w/w) polymeric combination, compared to about 1 hour for plain tablets containing 80% MD. In terms of extending the release of medications, the dissolution profiles of the tablets containing polymeric salts forms were found to be statistically superior to tablets prepared by direct compression of the polymers in their powdered base forms, and superior to tablets containing the same polymers granulated using isopropyl alcohol. The findings indicated the significance of combining the polymers in their salt forms in controlling the release of various drug types from matrices.

Failed Commemoration: A Royal Tomb and Its Afterlife

Visitors to St. George’s Chapel, Windsor, are often surprised to discover that two of England’s most recognizable kings, Henry VIII and Charles I, are buried together in a vault beneath a rather plain tablet in the choir. Christopher Highley’s essay tells the story of how this strange postmortem pairing came to be and how writers of different religious and political persuasions after 1649 drew inferences from it about the nation’s past, present, and future. By exploring this marginal site on the map of royal England, the essay offers insights into the cultural processes of remembering and forgetting, and the political uses of the past.

Influence of Differing Analgesic Formulations of Aspirin on Pharmacokinetic Parameters.

Aspirin has been used therapeutically for over 100 years. As the originator and an important marketer of aspirin-containing products, Bayer’s clinical trial database contains numerous reports of the pharmacokinetics of various aspirin formulations. These include evaluations of plain tablets, effervescent tablets, granules, chewable tablets, and fast-release tablets. This publication seeks to expand upon the available pharmacokinetic information concerning aspirin formulations. In the pre-systemic circulation, acetylsalicylic acid (ASA) is rapidly converted into its main active metabolite, salicylic acid (SA). Therefore, both substances are measured in plasma and reported in the results. The 500 mg strength of each formulation was chosen for analysis as this is the most commonly used for analgesia. A total of 22 studies were included in the analysis. All formulations of 500 mg aspirin result in comparable plasma exposure to ASA and SA as evidenced by AUC. Tablets and dry granules provide a consistently lower Cmax compared to effervescent, granules in suspension and fast release tablets. Effervescent tablets, fast release tablets, and granules in suspension provide a consistently lower median Tmax compared to dry granules and tablets for both ASA and SA. This report reinforces the importance of formulation differences and their impact on pharmacokinetic parameters.

Evaluation of various processes for simultaneous complexation and granulation to incorporate drug–cyclodextrin complexes into solid dosage forms

Insoluble drugs often formulated with various excipients to enhance the dissolution. Cyclodextrins (CDs) are widely used excipients to improve dissolution profile of poorly soluble drugs. Drug–CD complexation process is complex and often requires multiple processes to produce solid dosage form. Hence, this study explored commonly used granulation processes for simultaneous complexation and granulation. Poorly soluble drugs ibuprofen and glyburide were selected as experimental drugs. Co-evaporation of drug:CD mixture from a solvent followed by wet granulation with water was considered as standard process for comparison. Spray granulation and fluid bed processing (FBP) using drug:CD solution in ethanol were evaluated as an alternative processes. The dissolution data of glyburide tablets indicated that tablets produced by spray granulation, FBP and co-evaporation–granulation have almost identical dissolution profile in water and 0.1% SLS (>70% in water and >60% in SLS versus 30 and 34%, respectively for plain tablet, in 120 min). Similarly, ibuprofen:CD tablets produced by co-evaporation–granulation and FBP displayed similar dissolution profile in 0.01 M HCl (pH 2.0) and buffer pH 5.5 (>90 and 100% versus 44 and 80% respectively for plain tablets, 120 min). Results of this study demonstrated that spray granulation is simple and cost effective process for low dose poorly soluble drugs to incorporate drug:CD complex into solid dosage form, whereas FBP is suitable for poorly soluble drugs with moderate dose.

Proniosomal oral tablets for controlled delivery and enhanced pharmacokinetic properties of acemetacin.

Free-flowing proniosomal powders of acemetacin (AC) were prepared using the slurry method and maltodextrin as carrier. Positively charged proniosomes composed of 70:20:10 of Span 60/cholesterol (Chol)/stearylamine (SA), respectively, were successively compressed into tablets using direct compression method. The tablets were characterized for weight variability, friability, hardness, drug content uniformity, and dissolution properties. The in vivo evaluation of the prepared proniosomes (powder or tablet forms) after oral administration was investigated by the determination of AC and its active metabolite indomethacin (IND) in the blood of albino rabbits. Results indicated that the increase of Chol from 10% to 20% markedly reduced the efflux of the drug. Further Chol addition from 30% to 50% led to increased AC release rates. The proniosome tablets of AC showed greater hardness and disintegration time and less friability than AC plain tablets. The dissolution of proniosomal tablets indicated a lower drug release percentage compared to powdered proniosomes and AC plain tablets. The mean pharmacokinetic parameters of AC and IND from different formulations indicated increased t 1/2 and area under the curve (AUC) of both AC and IND for proniosomal tablets compared with both proniosomal powders and AC plain tablets. This study suggested the formulation of AC proniosomal powder into tablets to control and extend its pharmacologic effects.