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PubMed2002

[Postoperative epidural analgesia--current status, indications and management].

We are reporting on postoperative pain treatment using epidural analgesia in 1,822 patients, performed between 1995 to 2000, following continuous epidural anaesthesia combined with general anaesthesia for operations in various specialized areas (general or visceral surgery, vascular and thoraxic surgery, gynaecology, urology and orthopaedics). A total of 1,727 of these postoperative epidurals were included in a detailed evaluation. The postoperative epidural analgesia consisted of a continuous application of 0.25% bupivacain or 0.2% ropivacain. These local anaesthetics were administered epidurally in an hourly perfusion rate of 7.5 ml. We found "good" pain relief through continuous epidural administering of the local anaesthetics in 1,292 patients (74.8%). "Moderate" pain relief was achieved in 392 patients (22.7%). Sufentanil had to be epidurally administered in addition to local anaesthetics in 262 patients (15.2%) in the wake-up room. The sufentanil doses lay between 5 and a maximum 10 micrograms per hour. An additional epidural application of morphine-boli in a dose of 3 mg every 8-12 hours was necessary in 384 patients (22.2%) in the surgical wake-up stations. In 392 patients (22.7%), the additional systemic administering of antipyretic analgesics such as metamizol or paracetamol or spasmolytica was sufficient. In 43 cases (2.5%), sufficient pain relief could not be achieved with epidural analgesia even with additive applications of systemic functioning pharmaceuticals, so that the postoperative pain therapy had to be completely switched to a PCA. The lying time of the epidural catheter was 2-5 days. It was shortest with the gynaecological patients and longest with patients from general, visceral, thoraxic and vascular surgery areas. An important factor for a sufficient epidural analgesia is the exact epidural positioning of the catheter tip in the area of the spinal cord segments, which are affected by the operation. This reveals the required puncture height. The following side-effects resulting from the epidural analgesia were found: blood pressure loss of more than 20% of the starting value (21%), temporary bladder voiding disorders (8%), temporary sensory disorders of the lower extremities (6.5%), seldom nausea (2.4%) and post-puncture headaches (1.2%). The most important prerequisites for successful postoperative epidural analgesia and thus for increased patient satisfaction are correct selection of the insertion height in relation to the planned operation, constantly available medical pain service, the inclusion of trained care personnel and unequivocal written instructions.

Adolescent↗

PubMed1992

Synthesis and pharmacological study of some 3-(isoxazol-5-yl)-quinazolin-4(3H)-ones.

A number of new 3-(isoxazol-5-yl)-quinazolin-4(3H)-ones was prepared and tested, together a few analogues previously obtained, for their analgesic, antipyretic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effects. In the carrageenan rat foot edema model one of the tested compounds showed activity and LD50 comparable to that of ASA, but the ulceration index approximated zero value.

Animals↗

PubMed1992

Human behavior in relation to selection of malaria treatment.

People in rural areas usually help themselves when malaria attacks by using a drug preparation under the name of "ya-chud" bought from the grocery in the village. The objective of this study was to determine the behavior towards malarial treatment of local inhabitants in two malarious areas in eastern Thailand. Groups of 271 and 131 local inhabitants in villages in Pong Nam Ron and Bo Thong Districts, respectively, aged more than 15 years were interviewed regarding health behavior in seeking care when they became ill with malaria. Forty-two percent of the population at Pong Nam Ron and fifteen percent at Bo Thong went to drug-stores or groceries when they developed minor illness, while 85.2% of the subjects interviewed at Bo Thong went to the local health center. However, when they became severely ill, treatment-seeking patterns were similar in the two study areas. Ninety-four percent of the subjects interviewed at Bo Thong and eighty-seven percent at Pong Nam Ron gave a history of having used ya-chud in the past. On average, a set of ya-chud for malaria infection consists of 3-5 drugs: antimalarial drugs together with others such as analgesic-antipyretics, steroids, anti-histamines, vitamins and antimicrobial agents (tetracycline). The price of one ya-chud varied from 3-9 baht. Such improperly use of antimalarial drugs in malarious areas can result in treatment failure and cause the development of drug resistance, which is a problem in the malaria control program in Thailand.

Adolescent↗

PubMed2003

[New perspectives on paracetamol].

Paracetamol (acetaminophen) is well established as a leading non-prescription antipyretic analgesic drug. Future developments are likely to include new formulations to achieve rapid absorption for a fast onset of action, and prolonged absorption to extend the duration of action for regular long-term administration. Better dosage forms are also required for rectal administration. The availability of intravenous paracetamol has greatly extended the use of this drug as an adjunct to postoperative analgesia and for control of fever in the intensive care setting. Intravenous paracetamol is available in only a few countries at present, but it seems inevitable that it will be marketed much more widely in the future. The misuse of paracetamol as a fashionable agent for self-poisoning seems likely to continue, and liver failure may still occur in the small proportion of overdose patients who present too late for effective antidotal treatment with N-acetylcysteine. Much effort is being devoted to the study of the molecular mechanisms of paracetamol hepatotoxicity, and it is hoped that further advances may make it possible to prevent liver failure in all patients, irrespective of delays in presentation. At the same time, there is great interest in the mechanisms of the therapeutic actions of paracetamol and its effects on the different isoforms of cyclo-oxygenase. There will probably be important new findings in this area and these may lead to wider clinical use. Meantime, possible novel therapeutic applications for paracetamol include its use as an antioxidant to prevent atherosclerosis and cardiovascular disease by inhibiting the oxidation of low-density lipoproteins, and to prevent the formation of cataracts.

Acetaminophen↗

PubMed1992

3,5-Diphenyl-1H-pyrazole derivatives. X. N-substituted 1-(2-aminopropyl)- and 1-(3-amino-2-hydroxypropyl)-3,5-diphenyl-1H-pyrazoles with antiinflammatory and other activities.

The syntheses of 1-(2-hydroxypropyl)-3,5-diphenyl-1H-pyrazole 1 by reaction of 1-hydrazino-2-propanol with dibenzoylmethane and of N-substituted 1-(2-aminopropyl)-3,5-diphenyl-1H-pyrazoles 3 by reaction of primary and secondary amines with the tosylate of 1, as well as of N-substituted 1-(3-amino-2-hydroxypropyl)-3,5-diphenyl-1H-pyrazoles 6 starting from 3,5-diphenyl-1H-pyrazole, are described. Some compounds 3 and 6 showed remarkable antiinflammatory activity in rats, as well as weak analgesic, antipyretic, antiarrhythmic, hypotensive activities in mice and rats and moderate platelet antiaggregating effects in vitro.

Animals↗

PubMed2004

Epstein-Barr virus infectious mononucleosis.

Infectious mononucleosis should be suspected in patients 10 to 30 years of age who present with sore throat and significant fatigue, palatal petechiae, posterior cervical or auricular adenopathy, marked adenopathy, or inguinal adenopathy. An atypical lymphocytosis of at least 20 percent or atypical lymphocytosis of at least 10 percent plus lymphocytosis of at least 50 percent strongly supports the diagnosis, as does a positive heterophile antibody test. False-negative results of heterophile antibody tests are relatively common early in the course of infection. Patients with negative results may have another infection, such as toxoplasmosis, streptococcal infection, cytomegalovirus infection, or another viral infection. Symptomatic treatment, the mainstay of care, includes adequate hydration, analgesics, antipyretics, and adequate rest. Bed rest should not be enforced, and the patient's energy level should guide activity. Corticosteroids, acyclovir, and antihistamines are not recommended for routine treatment of infectious mononucleosis, although corticosteroids may benefit patients with respiratory compromise or severe pharyngeal edema. Patients with infectious mononucleosis should be withdrawn from contact or collision sports for at least four weeks after the onset of symptoms. Fatigue, myalgias, and need for sleep may persist for several months after the acute infection has resolved.

Adolescent↗

PubMed2004

[Trends in nonsteroidal anti-inflammatory drug development and application].

Since the synthesis of salicylic acid, research into the synthesis of new nonsteroidal anti-inflammatory drugs (NSAIDs) has continued in two directions: drugs with higher anti-inflammatory activity and those causing less adverse side-effects. Several very potent classic, non-selective NSAIDs were already available in the 1970's, but problems with their toxicity, especially gastro- and nephrotoxicity, have remained unsolved. The discovery of two cyclooxygenase (COX) isoforms, COX-1 and COX-2, was a breakthrough that led to obtaining the so-called coxibs, which selectively inhibit COX-2. This property makes this kind of NSAID less gastrotoxic than classic, non-selective NSAIDs. Other strategies to reduce the toxic effects of NSAIDs were their applications as prodrugs or purified enantiomers. The latest are the synthesis of classic NSAIDs combined with a chemical group that serves as a nitric oxide donor or the synthesis of double cyclooxygenase/5-lipoxygenase inhibitors. Simple inhibition of prostaglandin (PG) synthesis cannot completely stop the inflammatory process. Therefore new agents are tested for their influence on many other elements of the mechanism of inflammation, e.g. the formation of inflammatory cytokines, free radicals and biogenic amines by the stimulated inflammatory cells. Such pleiotropic activity of an NSAID might increase its anti-inflammatory action.NSAIDs are widely used not only for their anti-inflammatory, but also analgesic, antipyretic, and (as in case of aspirin) anti-coagulating activity. Results of the latest studies suggest that NSAIDs prevent colorectal cancer and may protect against the development of Alzheimer's disease as well. Precise studies of NSAIDs' mechanism of action (e.g. research on the genetic conditions of NSAID metabolism, the discovery of COX-3, studies on microsomal PGE synthase or PG receptors) will probably enable the synthesis of other more selectively acting compounds.

Alzheimer Disease↗

PubMed2005

Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and nimesulide associated or not with common non-steroidal anti-inflammatory drugs.

BACKGROUND: Acetaminophen (paracetamol--P) and Nimesulide (N) are widely used analgesic-antipyretic/anti-inflammatory drugs. The rate of adverse hypersensitivity reactions to these agents is generally low. On the contrary non-steroidal anti-inflammatory drugs (NSAIDs) are commonly involved in such reactions. Celecoxib (CE) is a novel drug, with high selectivity and affinity for COX-2 enzyme. OBJECTIVE: We evaluated the tolerability of CE in a group of patients with documented history of adverse cutaneous reactions to P and N associated or not to classic NSAIDs. METHODS: We studied 9 patients with hypersensitivity to P and N with or without associated reactions to classic NSAIDs. The diagnosis of P and N-induced skin reactions was based in vivo challenge. The placebo was blindly administered at the beginning of each challenge. After three days, a cumulative dosage of 200 mg of CE in refracted doses were given. After 2-3 days, a single dose of 200 mg was administered. All patients were observed for 6 hours after each challenge, and controlled again after 24 hours to exclude delayed reactions. The challenge was considered positive if one or more of the following appeared: erythema, rush or urticaria-angioedema. RESULTS: No reaction was observed with placebo and eight patients (88.8%) tolerated CE. Only one patient developed a moderate angioedema of the lips. CONCLUSION: Only one hypersensitivity reaction to CE was documented among 9 P and N-highly NSAIDs intolerant patients. Thus, we conclude that CE is a reasonably safe alternative to be used in subjects who do not tolerate P and N.

Acetaminophen↗

PubMed2005

[Study of drug poisoning on 2612 cases in the department of emergency].

OBJECTIVE: To analyze the characteristics of the drug poisoning. METHODS: In the 25 department of emergency selected hospitals, design questionnaires to register the drug poisoning patients who seeking emergency treatment within one-year period. RESULTS: Collected 2 612 cases of drug poisoning patients, accounted as 0.31% of the aggregated number of emergency patients at the same time, as well as 23.42% of poisoning patients at the same time. The sexual proportion between males and females was 1:3.45, average age was 30.33 years, and the age groups between 15-34 years were the high potentials. The three top ranking industries were farmers, unemployed ones and services. Amongst the samples, 99.12% of them were exposed by mouth transmission. 84.57% were committed as suicides. The medicines most frequently adopted were 1. antianxity drugs; 2. analgesics antipyretic and antirheumatic drugs; 3. antipsychotropic drugs. Only 1.68% of the drug poisoning patients were diagnosed through blood-medicine. CONCLUSION: It is recommended to enhance the administration and education of medicines. To establish monitoring system for drug intoxication and improve the quality of diagnose and treatment of drug poisoning patients.

Adolescent↗

PubMedDate not supplied

Mother's use of medication in their children of preschool age.

Self medication by mothers influences the morbidity and mortality in children. The present study evaluates mothers' attitude and practices regarding use of medication in their preschool age children. 976 mothers having at least one child <6 years with history of illness in past 30 days were interviewed according to a predesigned questionnaire. Five hundred and seventy five (58.91%) used medication on their own, most commonly for cough & cold (23.9%). The commonest nonprescribed drugs used were analgesics--antipyretics (34.9%). Inspite of the nonresponse, shortage of money and availability of the drugs without prescription has encouraged self medication. These findings necessitates mothers' education and enforcement of law against selling of non-prescribed drugs.

Child, Preschool↗

PubMedDate not supplied

[Concomitant use of statins and cytochrome P 450 inhibitors in Croatia].

It is known that coadministration of a statin and certain drugs that inhibit cytochrome P-450 may inhibit catabolism of statin, resulting in an increased concentration of statin in the blood and consequently, increased risk of certain side effects, e.g. myopathy. The aim of this study was to establish, for the first time, how many patients in Croatia concomitantly take statins with other drugs, and which drugs. Also, the aim was to determine how often statins are administered concomitantly with cytochrome P-450 inhibitors, and how many patients taking statin are therefore at increased risk of interactions and/or side effects. The data were collected from general practitioners' health records all over Croatia during July and August 2004. The data for patients who were prescribed any statin between June 1, 2003 and June 1, 2004 were analysed. The records of 882 patients were analysed, 446 (50.6%) women, 422 (47.8%) men and 14 (1.6%) of unidentified sex. The average age of women on statin was 65 years and of men 60 years. Of 882 patients, 772 patients (82%) were taking at least one more drug concurrently with statin. Of that number, 24% of patients concomitantly were taking one more drug, 20% two more drugs, 16% three more drugs, 10% four more drugs, 8% five more drugs and 3% six more drugs. The average number of other drugs prescribed together with statin was 2.1 +/- 1.59 in men and 2.2 +/- 1.71 in women. The average age of patients who were taking another drug together with a statin did not significantly differ from that of patients receiving only statin. There were regional differences in the number of drugs prescribed together with a statin. In Osijek, the average number of drugs prescribed with a statin was 2.4 +/- 1.80, in Zagreb 2.2 +/- 1.64, in Rijeka 2.0 +/- 1.60, and in Split 1.8 +/- 1.44. The number of drugs prescribed with a statin in rural areas was 2.0 +/- 1.58, in urban areas 2.1 +/- 1.63 and in semi-urban areas 2.8 +/- 1.85. The therapeutic groups of drugs that are most frequently prescribed with a statin in Croatia are ACE inhibitors and their fixed combinations (32%), beta-receptor blockers and their fixed combinations (23%), selective calcium channel blockers (18%), anxiolytics (18%), vasodilators and organic nitrates (16%), antirheumatic drugs (11%), oral antidiabetics (11%), vitamin K antagonists, analgesics-antipyretics, diuretics (10%), antibiotics (8%), and angiotensin II antagonists and their fixed combinations (5%). All other drugs accounted for less than 5%. Four percent of the patients take cytochrome P-450 inhibitors concomitantly with a statin. The most frequently used drug is verapamil, combination of verapamil and trandolapril, clarithromycin and diltiazem. Consequently, 3% of men and 5% of women are at increased risk of side effects. This sex difference is, however, not statistically significant. Patients between 70 and 74 years of age taking statins are in Croatia at the highest risk of interactions because 8% of them take concomitantly cytochrome P 450 inhibitors.

Aged↗

PubMed1992

[A comparison of a tramadol/metamizole infusion with the combination tramadol infusion plus ibuprofen suppositories for postoperative pain management following hysterectomy].

Postoperative pain management is still a grossly neglected field. In most cases, antipyretic analgesics alone are insufficient during the early postoperative period. Powerful narcotics are often avoided or underdosed because they are associated with the risk of respiratory depression. Some authors recommend combined infusion of tramadol and metamizole, which is assumed to provide sufficient pain relief without the risk of respiratory depression. However, this regimen has not yet been investigated in a study that meets currently accepted scientific standards. METHODS. Sixty patients who underwent vaginal hysterectomy were included in a randomised, prospective double-blind study. Thirty women received two placebo suppositories immediately after induction of anaesthesia and a postoperative infusion of tramadol and metamizole (400 mg tramadol plus 5 g [= 10 ml] metamizole in 500 ml electrolyte solution). The 30 women of the control group received two ibuprofen suppositories (585.2 mg) preoperatively and a post-operative tramadol infusion (400 mg tramadol plus 10 ml placebo [NaCl 0.9%] in 500 mg electrolyte solution). The patients of both groups received 125 ml of the appropriate infusion solution as a loading dose over 10 min (corresponding to 1.25 mg metamizole and 100 mg tramadol in the metamizole/tramadol group or 100 mg tramadol in the ibuprofen/tramadol group) 10 min after awakening. The remaining solution was administered at an infusion rate of 12.5-25 ml/h (corresponding to 125-250 mg metamizole and 10-20 mg tramadol/h or 10-20 mg tramadol/h). On request or when complaining of stronger pain, the patients received an additional bolus infusion of 125 ml over 10 min. In case of insufficient pain reduction despite repeated infusion of 125-ml boli or consumption of the entire infusion solution, the patients discontinued the study and received demand-adapted intravenous titration of piritramide. Postoperative pain was evaluated on the visual analogue scale (VAS) and the 101-point numerical rating scale immediately before the start of the infusion. Pain evaluation was repeated 20, 30, 40, 60, 100, 120, and 240 min after awakening accompanied by registration of heart rate, respiratory rate, systolic and diastolic blood pressure, and side effects. RESULTS. About 60% of the entire infusion solution was administered within 60 min in both groups. Significant postoperative pain reduction in both groups and on both the 101-point scale and the VAS was observed only at 100, 120, and 240 min after awakening. In the tramadol/metamizole group, nausea occurred in 7 cases and vomiting in 1. Nine patients in this group additionally required intravenous piritramide because of insufficient pain relief. In the tramadol/ibuprofen group, 8 patients complained about nausea and 4 patients vomited. Six patients additionally received intravenous piritramide because of insufficient pain reduction. CONCLUSIONS. Satisfactory pain reduction occurred rather late despite high doses of both the tramadol/metamizole and the tramadol/ibuprofen. Both analgesic combination must be regarded as insufficient after inhalational anaesthesia because of the very slow onset of action and the high failure rate.

Adult↗

PubMed2005

The future of traditional nonsteroidal antiinflammatory drugs and cyclooxygenase-2 inhibitors in the treatment of inflammation and pain.

Prostanoids act leading roles in a myriad of physiologic and pathologic processes because these autacoids participate in the amplification of biological responses induced by innumerable stimuli. The formation of prostanoids is operated by two synthases named cyclooxygenase(COX)-1 and COX-2. Traditional nonsteroidal antiinflammatory drugs (tNSAIDs) and COX-2 inhibitors (coxibs) give rise to antipyretic, analgesic, and antiinflammatory actions, through their reversible clogging of the COX channel of COX-2 - apart from aspirin which modifies irreversibly the catalytic activity of COX-2. tNSAIDs and COX-2 inhibitors resulted clinically equivalent for the relief of acute pain and symptoms of arthropathies but they failed to modify disease progression. Clinical evidence of the possible contribution of COX-1 in inflammation and pain in some occasion - as suggested by experimental and pharmacology studies - is orphan because none efficacy trial with COX inhibitors was designed to establish it. COX-2 inhibitors were developed with the aim to reduce the incidence of serious gastrointestinal (GI) adverse effects associated with the administration of tNSAIDs ensued as a consequence of the inhibition of cytoprotective COX-1-derived prostanoids. However, the reduced incidence of serious GI adverse effects compared to tNSAIDs demonstrated for 2 COX-2 inhibitors (e.g. rofecoxib and lumiracoxib) has been countered by an increased incidence of myocardial infarction and stroke detected in 5 placebo controlled trials involving the COX-2 inhibitors celecoxib, rofecoxib and valdecoxib. The future of COX-2 inhibitors will be an example of personalised medicine as their use will be restricted to patients who do not respond to tNSAIDs or with increased risk of GI complications.

Animals↗

PubMed2005

Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and other non-steroidal anti-inflammatory drugs.

BACKGROUND: Acetaminophen (paracetamol-P) is a widely used analgesic-antipyretic drug with no anti inflammatory effects and its rate of adverse hypersensitivity reactions is very low. On the contrary non-steroidal anti-inflammatory drugs (NSAIDs) are commonly involved in side effects. Celecoxib (CE) is a novel drug, with high selectivity and affinity for COX-2 enzyme. OBJECTIVE: We evaluated the tolerability of CE in a group of patients with documented history of adverse cutaneous reactions to P and to classic NSAIDs. METHODS: We studied 29 patients with hypersensitivity to P and classic NSAIDs. The diagnosis of P-induced skin reactions was based on in vivo challenge. The placebo was blindly administered at the beginning of each challenge. After three days, a cumulative dosage of 200 mg of CE in refracted doses was given. After 2-3 days, a single dose of 200 mg was administered. All patients were observed for 6 hours after each challenge, and they were controlled again after 24 hours to exclude delayed reactions. The challenge was considered positive if one or more of the following appeared: erythema, rash or urticaria-angioedema. RESULTS: No reaction was observed with placebo and twenty eight patients (96.5 %) tolerated CE. Only one patient developed a moderate angioedema of the lips. CONCLUSION: Only one hypersensitivity reaction to CE was documented among 29 P-intolerant patients. Thus, we conclude that CE is a reasonably safe alternative which can be used in subjects who do not tolerate P.

Acetaminophen↗

PubMed1991

Pharmacological properties of the new non-steroidal anti-inflammatory agent etodolac.

The anti-inflammatory, analgesic, antipyretic and ulcerogenic activities of etodolac (CAS 41340-25-4), a new nonsteroidal anti-inflammatory agent, were compared with those of indometacin and other anti-inflammatory drugs in experimental animals. Etodolac had a remarkable anti-inflammatory effect in various experimental models: ultraviolet erythema, carrageenin-induced edema and swelling of adjuvant arthritis. In these models, the effective dose of etodolac was several fold that of indometacin. Etodolac inhibited prostaglandin E2 formation in a concentration-dependent manner, and its inhibitory potency was about 1/5 of that of indometacin. Etodolac also caused marked inhibition of granuloma formation and leucocyte functions such as chemotaxis, lysosomal enzyme release and active oxygen generation. These effects of etodolac were observed at similar doses of indometacin. Etodolac suppressed inflammatory pain but not non-inflammatory pain, and had an antipyretic effect but did not lower normal rectal temperature. Etodolac had no effect on delayed hypersensitivity reactions and was much less ulcerogenic than indometacin. These results indicate that etodolac is a low ulcerogenic anti-inflammatory agent with suppressing activities on leucocyte functions to the same extent as indometacin and prostaglandin biosynthesis.

Animals↗

PubMed2006

The effects of mefenamic acid on hematocrit of the lizard, Uromastix hardwickii.

Mefenamic acid is an analgesic, antipyretic and anti-inflammatory agent. In addition induces several hematological disturbances. Present study was conducted to determine the alterations in blood PCV of the lizard Uromastix hardwickii after the administration of 7.1 mg/ml; 10.5 mg/ml and 14.0 mg/ml mefenamic acid per individual per day for 12 days to 3 test groups. The mean values of PCV were 15.5+/-0.81%, 14.5+/-0.25% and 12.0+/-0.25% for 3 test groups respectively in comparison to 23.5+/-0.40% for control. Thus a significant dose dependant reduction in mean PCV per cent following the administration of mefenamic acid for 12 days indicates the extra vascular hemolysis due to destructive change in the red cell membrane through autoantibody mechanism.

Anemia, Hemolytic, Autoimmune↗

PubMed1991

Research on heterocyclic compounds. XXVIII. Imidazo[1,2-c]pyrimidines.

A group of 24 imidazo[1,2-c]pyrimidines was taken into consideration in order to study their relationships between chemical structure and antiinflammatory activity. Some of these compounds were synthesized by us in the past, the others have been synthesized and characterized to complete the series. Antiinflammatory, analgesic, antipyretic and gastric ulcerogenic activities of such compounds were compared with those of indomethacin and discussed in terms of the effects exerted by the presence on the heterocyclic system of various substituents and an acidic or nonacidic moiety.

Acetates↗

PubMedDate not supplied

[Formulations and bioavailability of propyphenazone in lyophilized tablets].

The present work reports some facts about the preparation and release characteristics of the tablets of propiphenazone made by lyophilizing method (lyoc); they are compared with the classic tablets obtained by simple compression. Our substance, the propiphenazone, is a stable one, but we can talk about its poor solubility. Therefore, in order to obtain the lyoc tablets, we chose the method of paste. This tablets had a spongy aspect, with a desaggregation time of 1-2 min.; the latter (classic tablets) were regularly and the desaggregation time in about 9 min. The kinetics of propiphenazone absorbtion would be expected to differ in these structurally-distinct tablets types. Indeed, the concentration was really appreciable for the lyoc tablets after 30 min., with the peak at 60 min.; for the classic tablets the peak was remarkably only after 90 min. The relative bioavailability for these two types of tablets pointed out the differences, confirming the evident advantages for using the lyoc tablets in analgesic, antipyretic therapy.

Anti-Inflammatory Agents, Non-Steroidal↗