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At least 487 records · Page 27Linked to original sources

PubMed2001

A novel method for analyzing thick tablets by near infrared spectroscopy.

A near-infrared (NIR) spectroscopic method to determine content uniformity of a large, thick tablet using an approach that could facilitate future validations has been developed. A CT ibuprofen 800-mg tablet weighs about 1150 mg and is about 18.6 mm wide and 7.6 mm thick. The FT NIR spectrometer was optimized for transmission spectra of the tablets by moving it to the sample compartment and placing it immediately behind the tablet. In spite of this dedicated setup, the transmission spectra obtained were very poor, indicating that the NIR radiation was not reaching the detector. The spectra of the tablet improved with use of a simple preparation in which a flat-face die applies pressure of 20 000 psi to the tablet; this reduced the thickness of the tablet from 7.6 mm to 3.6 mm. A calibration model was developed for tablets with drug content ranging from 70% to 130% of label. The calibration model was tested using a validation set of tablets with a drug content of 752, 800, and 848 mg. The results obtained were within 1.5% of the known drug content of the validation set tablets. Even with the sample preparation, the content uniformity results of 10 tablets could be determined using this method in less than 1 hour. The approach described in this article could also be used to validate NIR content uniformity methods for other formulations.

Calibration↗

PubMed2004

Nondestructive and on-line monitoring of tablets using light-induced fluorescence technology.

A system using light-induced fluorescence (LIF) technology was developed for rapid and nondestructive analysis of active pharmaceutical ingredients on tablet surfaces. Nonhomogeneous tablets with defined layer of active ingredients were made by 3-Dimensional Printing technology to determine penetration depths of the light source and the resultant fluorescence responses. The LIF method of analysis showed penetration to depths of up to 3 mm into tablets. A correlation between LIF signals from analysis of tablet surfaces and the total drug content of the respective tablets was established. This method of surface analysis was verified with UV spectrometric methods for the total drug content of each respective tablet. The results from a small sample population of tablets made from both homogeneous and nonhomogeneous powder mixtures established good correlation between LIF surface monitoring and total tablet content. The use of on-line monitoring of the individual tablet for surface content demonstrated consistent LIF profiles from simulated production rates up to 3000 tablets a minute. The instrument was also field tested successfully on a tablet analyzer.

Chemistry, Pharmaceutical↗

PubMed2004

Comparative in vitro and in vivo evaluation of matrix, osmotic matrix, and osmotic pump tablets for controlled delivery of diclofenac sodium.

The aim of this investigation was preparation and comparative evaluation of fabricated matrix (FM), osmotic matrix (OM), and osmotic pump (OP) tablets for controlled delivery of diclofenac sodium (DS). All formulations were evaluated for various physical parameters, and in vitro studies were performed on USP 24 dissolution apparatus II in pH 7.4 buffer and distilled water. In vivo studies were performed in 6 healthy human volunteers; the drug was assayed in plasma using HPLC, and results were compared with the performance of 2 commercial tablets of DS. Various pharmacokinetic parameters (ie, C(max), T(max), area under the curve [AUC(0-24)], and mean residence time) and relative bioavailability were compared. All fabricated formulations showed more prolonged and controlled DS release compared with commercial tablets studied. The OM and OP tablets, however, performed better than the matrix tablets. The rate and extent of drug release from FM1 matrix tablets (single polymer) was significantly different from that of FM2 (admixed polymers). Type of porosigenic agents and osmogens also influenced the drug release. Analysis of in vitro data by regression coefficient analysis revealed zero-order release kinetics for OM and OP tablets, while FM tablets exhibited Higuchi kinetics. In vivo results indicated prolonged blood levels with delayed peak and improved bioavailability for fabricated tablets compared to commercial tablets. It was concluded that the osmotic matrix and osmotic pump tablets could provide more prolonged, controlled, and gastrointestinal environmental-independent DS release that may result in an improved therapeutic efficacy and patient compliance.

Adult↗

PubMed2005

In vitro and in vivo evaluation of guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride.

The objective of the study was to develop guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride. Matrix tablets of diltiazem hydrochloride, using various viscosity grades of guar gum in 2 proportions, were prepared by wet granulation method and subjected to in vitro drug release studies. Diltiazem hydrochloride matrix tablets containing either 30% wt/wt low-viscosity (LM1), 40% wt/wt medium-viscosity (MM2), or 50% wt/wt high-viscosity (HM2) guar gum showed controlled release. The drug release from all guar gum matrix tablets followed first-order kinetics via Fickian-diffusion. Further, the results of in vitro drug release studies in simulated gastrointestinal and colonic fluids showed that HM2 tablets provided controlled release comparable with marketed sustained release diltiazem hydrochloride tablets (D-SR tablets). Guar gum matrix tablets HM2 showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40 degrees C/relative humidity 75% for 6 months. When subjected to in vivo pharmacokinetic evaluation in healthy volunteers, the HM2 tablets provided a slow and prolonged drug release when compared with D-SR tablets. Based on the results of in vitro and in vivo studies it was concluded that that guar gum matrix tablets provided oral controlled release of water-soluble diltiazem hydrochloride.

Administration, Oral↗

PubMed2006

Effect of formulated ingredients on rapidly disintegrating oral tablets prepared by the crystalline transition method.

The aim of this article was to determine the optimal ingredients for the rapidly disintegrating oral tablets prepared by the crystalline transition method (CT method). The effect of ingredients (diluent, active drug substance and amorphous sugar) on the characteristics of the tablets was investigated. The ingredients were compressed and the resultant tablets were stored under various conditions. The oral disintegration time of the tablet significantly depended on diluents, due to differences in the penetration of a small amount of water in the mouth and the viscous area formed inside the tablet. The oral disintegration time was 10-30 s for tablets with a tensile strength of approximately 1 MPa, when erythritol, mannitol or xylitol was used as the diluent. The increase in the tensile strength of tablets containing highly water-soluble active drug substances during storage was as large as that of tablets without active drug substances, while the increase in the tensile strength of tablets containing low water-soluble active drug substances was small. It was therefore found that highly water-soluble active drug substances were more suitable for the formulation prepared by the CT method than low water-soluble active drug substances. Irrespective of the type of amorphous sugar (amorphous sucrose, lactose or maltose) used, the porosity of tablets with 1 MPa of tensile strength was 30-40%, and their oral disintegration time was 10-20 s. The optimal ingredients for rapidly disintegrating oral tablets with reasonable tensile strength and disintegration time were therefore determined from these results.

Absorption↗

PubMed2002

[Fast-disintegration oral tablets having sustained release property].

Fast-disintegrating (FD) tablets containing nicorandil-loaded dry emulsions were prepared and their controlled-release properties were examined and compared with the plain FD tablets (FD tablets without dry emulsions) and commercial tablets. The dry emulsions were prepared with myristyl alcohol and stearyl alcohol and their property was modified by mixing the ratio of the two alcohols. Disintegration time of the prepared FD tablets was sufficiently fast (i.e., 12 to 23 s). In vitro release of nicorandil from the FD tablets containing the dry emulsions was sustained over 6 h, while that from plain FD and commercial tablets was complete within 5 min. In vivo absorption of nicorandil from the tablets was evaluated by oral administration in beagle dogs. FD tablets containing dry emulsions showed a similar AUC, lower Cmax, and delayed Tmax compared to the plain FD and commercial tablets. These results suggest that the dry emulsion-loaded FD tablets can be utilized to improve the sustained-release property of active drugs.

Administration, Oral↗

PubMedDate not supplied

Lack of medication dose uniformity in commonly split tablets.

OBJECTIVE: To divide 11 commonly split tablets and evaluate the resulting half-tablets for content uniformity. DESIGN: Pre-post comparison. SETTING: Laboratory. INTERVENTIONS: A trained individual split tablets of 11 products using a single-edged razor blade and 3 products by hand alone. MAIN OUTCOME MEASURES: The Uniformity of Dosage Units test published in the United States Pharmacopeia 24 (USP), which applies to whole tablets, was adapted liberally to assess the dose uniformity of the resulting split tablets. RESULTS: Of the 11 razor-split products, 8 failed the liberal adaptation of the USP uniformity test. No visible tablet features (e.g., scoring) predisposed a product's split tablets to pass or fail the uniformity test. All three hand-split tablets failed the uniformity test and yielded worse results than did razor-split tablets. CONCLUSION: The majority of the 11 drug products we tested, when assessed for their ability to be split into half-tablets of equal dose, failed a liberally interpreted USP uniformity test. The practice of dividing tablets to save costs or to improve a dosage regimen may not cause problems for patients using drugs with low toxicity and relatively flat dose-response relationships, but it is not recommended for patients using drugs with more substantial toxicity and steep dose-response efficacy curves.

Drug Compounding↗

PubMed2006

Compression physics in the formulation development of tablets.

The advantages of high-precision dosing, manufacturing efficiency, and patient compliance make tablets the most popular dosage forms. Compaction, an essential manufacturing step in the manufacture of tablets, includes compression (i.e., volume reduction and particle rearrangement), and consolidation (i.e., interparticulate bond formation). The success of the compaction process depends not only on the physico-technical properties of drugs and excipients, especially their deformation behavior, but also on the choice of instrument settings with respect to rate and magnitude of force transfer. This review discusses various properties of drugs and excipients, such as moisture content, particle size and distribution, polymorphism, amorphism, crystal habit, hydration state, and lubricant and binder level of the blend that have an influence on compaction. Tableting speed and pre/main compression force profile, also have a bearing on the quality of the final tablet. Mechanistic aspects of tableting can be studied using, instrumented punches/dies, instrumented tableting machines, and compaction simulators. These have potential application in pharmaceutical research and development, such as studying basic compaction mechanism, process variables, scale-up parameters, trouble shooting problem batches, creating compaction data bank, and fingerprinting of new active pharmaceutical ingredients (APIs) or excipients. Also, the mathematical equations used to describe compaction events have been covered. These equations describe density-pressure relationships that predict the pressures required for achieving an optimum density. This understanding has found active application in solving the analytical problems related to tableting such as capping, lamination, picking, sticking, etc. Mathematical models, force-time, force-distance, and die-wall force parameters of tableting are used to describe work of compaction, elasticity' plasticity, and time dependent deformation behavior of pharmaceuticals. Various indices of tableting performance such as the bonding index, brittle fracture index, and strain index can be used to predict compaction related problems. Compaction related physico-technical properties of commonly used tableting excipients have been reviewed with emphasis on selecting suitable combination to minimize tableting problems. Specialized tools such as co-processing of API and excipients can be used to improve their functionality.

Chemistry, Pharmaceutical↗

PubMedDate not supplied

Effect of cation content of certain ammoniomethacrylate copolymers type A (RL) and B (RS) on their binder property in tableting.

Tablets of salicylic acid (drug model) have been formed using two analogous acrylatemethacrylate copolymers designated here as A and B as binders. A and B differ only in their content of quaternary ammonium (cationic) groups in the ratio 2:1 (A:B). The aim was to investigate the effect of the cationic groups on the tableting characteristics of the formed granules. In the procedure, aqueous dispersions of the polymers of concentrations 1 to 5% w/v were used in a separate experiment for granulation of the salicylic acid powder and then tableted. The final concentration of the binder in the tablets varied from 0.4 to 2% w/w. The parameters assessed were the tablet tensile strength (T) and their brittle fracture index (BFI) which are indicative of the plasto-elasticity of the granules; for instance, a high T value together with a low BFI value are indicative of a high plasto-elasticity. A and B generally displayed a strong binder property as they individually produced hard tablets even at the low concentration 0.4% w/w. As the binder concentration in the tablets increased to 2% w/w. tensile strength (MNm(-2)) increased from 1.08 to 1.80 (tablets of polymer A), 1.08 to 2.02 (tablets of polymer B). BFI values decreased from 0.24 to 0.06 (tablets of polymer A) and 0.16 to 0.04 (tablets of polymer B). These results indicate that the presence of the cationic groups in the polymer structure promoted elastic rather than plastic compression.

Acrylic Resins↗

PubMed1995

[Problems when swallowing tablets. A questionnaire study from general practice].

Dysphagia, or difficulty in swallowing tablets, may greatly affect compliance. This report presents the results of our survey, which was undertaken to determine the proportion of a general practitioner's patient population who had difficulty in swallowing tablets, and to identify the reasons for the difficulty. 6,158 questionnaires were received from patients who consulted a general practitioner. More than 1/4 (26%) of the total patient population (or 1,576) said they had problems in swallowing tablets. A prominent complaint was the size of the tablet, followed by the surface, form and taste of the tablet. Twice as many women as men experienced swallowing problems. Elderly patients (> 70 years) had less difficulty than younger patients when taking tablets. To achieve good compliance and optimal pharmacotherapy, it is important for medical practitioners and pharmaceutical personnel to be aware of the general problems connected to swallowing tablets, to enable them to select the correctly formulated drug for their patients. New and novel oral drug formulations, such as tablets that dissolve in seconds on the tongue without water, may alleviate the problem of swallowing tablets. They offer substantial advantages over ordinary tablets, are more convenient to administer, and enhance the potential for improved compliance in patients who experience difficulty in taking tablets.

Adolescent↗

PubMed1975

Stability of stabilized nitroglycerin tablets in typical distribution and administration systems.

A study was undertaken to determine whether or not the present extreme restrictions on the packaging of nitroglycerin tablets are indeed necessary when dispensing the newer stabilized tablets. Baseline tests were conducted on two molded and two compressed sublingual nitroglycerin tablets to determine weight variation, content uniformity, average potency and friability. Stability tests included: (1) use test designed to simulate patient use from a single bottle of 100 tablets over a one-month period; (2) an open plate study wherein tablets were exposed to the atmosphere for 100 days; (3) strip packaging of tablets using foil-foil or foil-cello systems; (4) placement of tablets in medication cups for a seven-day period; (5) repackaging 30-tablet batches in a variety of common prescription containers. All brands of tablets retained potency during normal use when dispensed and stored in their original containers. However, one brand was superior to all others when placed under stress conditions such as open plate exposure. These tablets also retained labeled potency when exposed in a medication cup for a seven-day period, or when repackaged in either foil-foil or foil-cello strips, or when dispensed in a number of ordinary prescription containers. The study indicated that this brand of nitroglycerin tablets might be handled like any other solid dosage form in hospital distribution systems without endangering patient care. However, exceptions to present packaging restrictions must be cleared with the Food and Drug Administration.

Drug Packaging↗

PubMed2007

Tolerability and patient acceptance of sodium phosphate tablets compared with 4-L PEG solution in colon cleansing: combined results of 2 identically designed, randomized, controlled, parallel group, multicenter phase 3 trials.

GOALS: Evaluate patient tolerance and acceptance of a sodium phosphate (NaP) tablet purgative compared with a 4-L polyethylene glycol (PEG) solution. BACKGROUND: Characteristics and side effects of bowel purgatives deter patients from undergoing screening colonoscopy. Published data demonstrated comparable bowel cleansing with NaP tablets and a 4-L PEG solution in 2 phase for 3 studies. This report presents data on patient tolerability and acceptance. STUDY: Two identically designed, randomized, investigator-blinded, and multicenter trials were performed. Tolerability and patient acceptance were based on purgative regimen compliance, incidence of gastrointestinal adverse events, and patient responses to questionnaires. RESULTS: Eight hundred forty-five patients were assessed (420 and 425 in the tablet and PEG solution groups, respectively). Patient compliance with the tablet regimen was greater: 94% of patients took all the tablets compared with 57% completing the PEG solution regimen (P<0.0001). Nausea, vomiting, and bloating occurred significantly less often in patients taking NaP tablets (P<0.0001). Among patients taking tablets, 88.4% rated them "easy" or "slightly difficult" to take, compared with 60.6% of patients taking the PEG solution. The preparation's taste was rated "barely tolerable" or "not tolerable" by 1% of patients treated with NaP tablets and 23.6% treated with PEG solution. Drinking the required volume of clear liquid for the tablet or PEG preparation was rated "easy" or "slightly difficult" by 92.2% and 66.9% of patients, respectively. Almost all (90.7%) patients taking the tablets indicated they would take the same preparation in the future, compared with 67.1% of patients taking the PEG solution (P<0.0001 for each comparison). CONCLUSIONS: Tolerability and patient acceptance of a NaP tablet purgative were superior to 4-L PEG solution.

Administration, Oral↗

PubMed2004

Pharmacokinetic profile of a new form of sumatriptan tablets in healthy volunteers.

OBJECTIVE: Rapid delivery of migraine-specific medication to its site(s) of action is thought to be crucial in preventing or minimizing sensitization of central pain pathways and thereby in optimizing pain-free outcomes in patients with migraine. Sumatriptan has been developed as a new tablet formulation to enhance the rate of systemic drug delivery by improving tablet disintegration and drug dispersion relative to those of conventional tablets. These enhanced formulation characteristics may be beneficial during occurrences of the gastric stasis that can accompany migraine. METHODS: This randomized, open-label, 4-way crossover study (n = 32) was conducted to determine whether the new formulation of sumatriptan 50 and 100 mg is bioequivalent to sumatriptan conventional tablets and to compare the pharmacokinetic profiles of the new formulation and the conventional tablet during the early (0-2 h) postdose interval in healthy volunteers. Pharmacokinetics during the early post-dose interval are important in determining a drug's onset of action, an important parameter to patients with migraine. RESULTS: The results confirm that the new formulation of sumatriptan and sumatriptan conventional tablets are bioequivalent as demonstrated by the finding that the 90% confidence intervals for the sumatriptan area under the concentration time curve to infinity and to the last evaluable time point (AUC(0- infinity ) and AUC(0-t), respectively) and maximum plasma concentration (C(max)) fell within the predetermined bounds defining bioequivalence (0.80-1.25) for both doses. Pharmacokinetic parameters measured early (0-2 h) after dosing reveal slightly faster absorption, on average, of the new sumatriptan formulation than sumatriptan conventional tablets although high intersubject variability was observed. For the new sumatriptan formulation, AUC(0-2) (AUC up to 2 h post dose) was, on average, 1% greater (50 mg) and 8% greater (100 mg) and maximal sumatriptan levels were attained, on average, 10 min earlier (50 mg) and 15 min earlier (100 mg) compared with the conventional tablet. Other measures including AUC(0-0.5) (AUC to 30 min post-dose), times to achieve sumatriptan concentrations of 5 and 10 ng/mL, and mean percentage C(max) 15, 20 and 30 min post-dose demonstrate an observable improvement in rate of drug absorption for the new form of sumatriptan compared with conventional tablets. CONCLUSION: The new form of sumatriptan is bioequivalent to sumatriptan conventional tablets and is absorbed more quickly than conventional tablets.

Adult↗

PubMed1994

Effect of temperature and humidity on the disintegration time of packaged paracetamol tablet formulations.

A study of the effect of various temperature and humidity conditions on the disintegration time of different brands of packaged paracetamol tablet formulations has been made over a period of six months. Under all the storage conditions paracetamol tablets show an increase in disintegration time ranging from 9.1 to 65.5% (200 mg tablets) and 1.2 to 150.0% (500 mg tablets) on increasing the temperature from 25 to 45 degrees C (75% RH). The increase in disintegration time on increasing the temperature from 25 to 45 degrees C (100% RH) ranges from 14.3 to 157.7% (200 mg tablets) and 15.3 to 92.3% (500 mg tablets). The overall increase in disintegration time from 25-45 degrees C at 75% and 100% RH is 36.4 to 564% (200 mg tablets) and 10.0 to 140.5% (500 mg tablets) and 101.3 to 122.9% (200 mg tablets) and 2.6 to 46.8% (500 mg tablets) respectively. These results indicate that PVC/PVDC/Al foil packaging cause relatively less change in disintegration time of the tablets compared to that of the polycoated paper and viscose film.

Journal Article↗

PubMedDate not supplied

Absence of effect of food on alprazolam absorption from sustained release tablets.

This study examined the effect of food on alprazolam absorption from a mixed polymeric matrix sustained release (SR) tablet in 21 healthy adults. Each subject received each of three treatments according to a crossover design: 1 mg alprazolam SR tablet while fasting; 1 mg alprazolam SR tablet immediately after a standardized breakfast; 1 mg alprazolam conventional tablet while fasting. The breakfast contained approximately 33 g protein, 55 g fat, and 58 g carbohydrate (850 calories). Serial blood samples were obtained and plasma alprazolam levels determined by HPLC. Results indicate that the SR tablet was minimally affected by food. Relative bioavailabilities of the SR tablet while fasting and with food were 100 per cent and 97 per cent, respectively. Although statistically significant, differences in mean Cmax values between SR tablets administered with and without food were small (12 per cent increase with food). Rates of absorption as measured by mean tmax values were also nearly the same: 7.2 h while fasting and 7.0 h with food. Absorption was relatively uniform with the SR tablets. Coefficients of variation for Cmax, tmax, and AUC were somewhat smaller with the SR tablet than with the conventional tablet.

Alprazolam↗

PubMed1991

Relative bioavailability of oral sustained-release and regular-release oxprenolol tablets at steady-state.

The relative bioavailability of a test sustained-release (SR) oxprenolol tablet against an approved regular-release (RR) tablet has been investigated at steady-state. In a randomized two-way crossover study, one tablet of 160 mg SR oxprenolol once every 24 h and one tablet of 80 mg RR oxprenolol once every 12 h were given to 12 healthy volunteers for 5 days. Blood samples were collected from each subject just prior to each dose-administration on days 1 through 4, and at scheduled time points on day 5 and analysed for oxprenolol concentration using HPLC. The SR tablet resulted in 42 per cent reduction in mean peak drug levels (p = 0.0341) and a statistically non-significant 14 per cent increase in mean trough levels (p = 0.8357) than the RR tablet. However it required 160 per cent longer time to reach average steady-state concentrations (Css) on day 5 (1.38 h for SR versus 0.53 h for RR; p = 0.0205). The mean area under the plasma drug concentration-time curve at steady state (AUC96-120) with the SR tablet was approximately 18 per cent lower than that observed with the RR tablet, and the degree of fluctuation (DF) was reduced by 30 per cent (2.81 for SR versus 4.11 for RR; p = 0.0069). On average, a single dose of SR tablet and two doses of RR tablets maintained the drug levels above a constant Css of 204.6 ng ml-1 for 7.88 and 7.65 h, respectively (p = 0.3513).

Adult↗

PubMedDate not supplied

Comparative bioavailability of furosemide from solution and 40 mg tablets with different dissolution characteristics following oral administration in normal men.

Furosemide tablets, with markedly different dissolution characteristics, and solution were orally administered to 21 healthy adult males to determine the effect of in vitro dissolution rate on in vivo bioavailability profiles. Furosemide 40 mg was given as Tablet A (fast dissolution characteristics), Tablet B (slow dissolution characteristics), and an aqueous solution. Both batches of tablets had identical formulae and were produced by a common process. The dissolution rate of the slower Tablet B was probably retarded by extension of the wet granulation time. Blood was collected for 12 h postdose and urine for 24 h. Peak plasma furosemide concentrations after the solution were significantly greater than after the tablets; there was no significant difference between the tablets. The time to peak occurred significantly earlier with the solution, with no significant difference between the tablets. Relative bioavailabilities of Tablet A and B were 89 per cent and 101 per cent, respectively, as determined by AUC, and 79 per cent and 84 per cent, respectively, as determined by urine recovery. These differences are not statistically significant. These results indicate that dissolution rate profiles of furosemide tablets may not be predictive of in vivo bioavailability.

Administration, Oral↗

PubMed2002

Influence of excipients, drugs, and osmotic agent in the inner core on the time-controlled disintegration of compression-coated ethylcellulose tablets.

The effect of excipient, drug, and osmotic agent loaded in the inner core tablet on the time-controlled disintegration of compression-coated tablet prepared by direct compression with micronized ethylcellulose was investigated. The excipients [spray-dried lactose, hydroxypropyl methyl cellulose, sodium starch glycolate, microcrystalline cellulose, different drugs (sodium diclofenac: model drug, salbutamol sulfate, and theophylline anhydrate) and osmotic agent (sodium chloride)] were used to formulate the composition of the inner core tablet. The result indicates that drug release from all the compression-coated tablets was characterized by a distinctive lag of time followed by a faster drug release, dependent on the types of excipient and drug, and osmotic agent used in the inner core tablet. Respectively, the lag of time was 8.5, 12.4, 14.6, or 15.8 h for spray-dried lactose, hydroxypropyl methyl cellulose, sodium starch glycolate, or microcrystalline cellulose-loaded inner core tablet, as compared with 16.4 h for an inner core made of sodium diclofenac alone. The direct-compressible excipients such as spray-dried lactose, sodium starch glycolate, and microcrystalline cellulose seemed not to illustrate a marked disintegration function to rapidly rapture the outer coating layer. The lag of time was only slightly shortened from 16.4 to 14.6 h, >24 to 17.8 h, or >24 to 21.3 h for sodium diclofenac, theophylline anhydrate, or salbutamol sulfate incorporated with sodium starch glycolate into the inner core tablet, respectively, suggesting that sodium starch glycolate did not perform its superdisintegration. Once an osmotic agent of sodium chloride was incorporated into the inner core tablet, the lag of time for the compression-coated tablet was markedly shortened to <1 h, as compared with 16.4 h for drug alone. The more the amount of sodium chloride added, the less the time of lag obtained. Osmotic pressure did have a key role in controlling the drug dissolution. The present result implies that osmotic function is more suitable than superdisintegration function in designing a compression-coated tablet with time-controlled disintegration.

Albuterol↗