Suspension Of Aspirin Research Articles

The rise of counterfeit medication: an emerging threat?

Madam, The definition of health is far more complex than initially imagined. As per the World Health Organisation (WHO), the “health” is defined as complete physical, mental, and social well-being instead of simply the absence of any disease.1 In the era of modern healthcare, medications are undoubtedly important in ensuring well-being worldwide. Despite monumental advances within the medical industry, the rise of counterfeit medication has become an emerging threat. Counterfeit medications are known as products sold with the deception of providing therapeutic benefits but consist of little-to-no active ingredients, which may or may not be harmful.2 Traditionally, the regulation of drug distribution falls under the responsibility of the health authorities of the relevant region, such as the Drug Regulatory Authority of Pakistan (DRAP). Reports of an escalating influx of counterfeit medications into Pakistan have recently created pivotal concerns within the local communities.3,4 In Karachi, officials seized a large quantity of cefixime and aspirin suspension powders, which were found to be “fake and spurious”.3 The counterfeit medication was created by repackaging locally-manufactured powder into branded bottles, which were subsequently sold across the city. In another case affecting various cities in Pakistan, a factory was illegally manufacturing spurious medication, leading to a nationwide cautionary announcement to avoid the purchase of affected drugs, including the lifesaving meropenem, among various other cephalosporin drugs.4 The distribution of counterfeit medications can have drastic consequences for the population. Patients in critical conditions may suffer further harm due to defective treatment, as a result of the failure of substandard products.5 Moreover, counterfeit drugs manufactured with inappropriate doses or concentrations may lead to fatal adverse effects, such as respiratory paralysis or death.5 In order to address this pressing issue, the national authorities must take proactive measures to tackle the production and distribution of counterfeit medication: There is a need for frequent and strict raids integrated within each city of Pakistan, in which local pharmacies have their inventory tested for substandard or inappropriate substances. Secondly. The import of medications must also be strongly monitored, in order to prevent the arrival of counterfeit or unregistered medications from foreign regions. It is recommended that the authorities establish pharmaceutical support programs for those individuals who cannot afford proper medications and eventually resort to purchasing substandard medication.

Potential effect of Raw Honey on Gastric Mucosal Healing in Aspirin-induced Rats

Background: Raw honey is a natural ingredient which has a variety of nutrients that can be used for alternative treatments for peptic ulcer disease. This study was carried out to examine the antiulcer effects of Raw Honey against Aspirin induced gastritis in rats. Methodology: Wistar rats were separated into 6 groups. Aspirin suspension 200mg/kgBW was given orally to groups 2-6 for 2 days. Then, group 1 and 2 received carboxymethylcellulose (CMC), groups 3-5 were orally forced-fed with 3.5, 7, and 14mL/kgBW of raw honey, and group 6 received 100mg/kgBW Cimetidine. The tested animals were killed after receiving therapy for 15 days and the gastric mucosa was observed macroscopically of the ulcer index and microscopically through histopathological preparations. The antioxidant effect of raw honey was identified from the lipid peroxidation marker (MDA). Conclusion : Treatment with 7 and 14 ml/kgBW of raw honey promotes gastric mucosal repair based on the macroscopic and microscopic observations. Significant decreases in the levels of the lipid peroxidation marker (MDA) was observed. Significance was defined as p<0.05 compared to the ulcer control group (Group 6).

Gastroprotective Effect of Azadirachta indica Leaves (Neem) Extract on Aspirin Induced Gastric Ulcer in Rats

Background: Gastric ulcer is one of the common diseases worldwide. Different parts of Azadirachta indica (Neem) tree has different uses in medicine for its beneficial properties and its leaves are also known to have anti ulcerant effect.
 Objective: This study was conducted to find out the protective role of Azadirachta indica (Neem) extract in the development of gastric ulcer.
 Materials and method: The study comprised of 30 Albino rats: Group-A, Group-B, Group-C, Group-D and Group-E having 6 rats in each group. The experiment was divided into 2 parts: Experiment-1 and Experiment-2. Experiment-1 comprised of Group-A and Group-B where Group-A served as control and was provided with normal saline (2 ml/kg body wt). In group-B rats ulcer was produced by administration of aqueous suspension of Aspirin (200 mg/kg body wt). All the rats were sacrificed after 4 hours to confirm gastric ulcer by histopathology. In Experiment-2, rats of Group-C served as disease control group and provided with normal saline (2ml/kg body wt). Group-D was provided with alcoholic extract of Azadirachtaindica leaves (150mg/kg body wt) and Group-E was provided with Ranitidine suspension (20mg/kg). After 8 days of treatment, animals were fasted for 24 hours. Then aqueous suspension of Aspirin (200 mg/kg body wt) was administered and after 4 hours all rats were sacrificed. Gross and microscopic examinations were performed to evaluate the results.
 Results: Histologically Aspirin treated rats showed ulcerated mucosa. Pretreatment with Neem extract showed protection against Aspirin induced gastric mucosal damage which was statistically highly significant (p<0.001).
 Conclusion: The study suggests that pretreatment with Azadirachta indica (Neem) leaves extract may be useful in prevention of Aspirin induced gastric ulcer.
 Delta Med Col J. Jul 2019 7(2): 61-65

Comparative Gastro-Protective Effects of Nigella sativa (Kalojira) and Omeprazole against Aspirin Induced Gastric Ulcer in Albino Rats

Background: Nigella sativa seeds have been in use as a natural remedy for over thousands of years in various parts of the world. These seeds are reported to have beneficial effects almost on every system of the body.Objective: To evaluate the gastro-protective effect of Nigella sativa on aspirin induced gastric ulcer with comparison to omeprazole.Materials and method: This experimental study was carried out in the department of Pharmacology and Therapeutics, Dhaka Medical College, Dhaka, Bangladesh in collaboration with the department of Pathology, Delta Medical College, Dhaka, Bangladesh. A total number of 30 healthy albino rats were used in this study. The experiment was divided into 2 parts: Experiment-1 and Experiment-2. Experiment-1 comprised of 12 rats: Group-A and Group-B having 6 rats in each group. Ulcer was produced by administration of aqueous suspension of aspirin (200 mg/kg body wt) in Group-B where Group-A served as control and was provided with normal saline (2 ml/kg body wt). All the rats were sacrificed after 4 hrs to confirm gastric ulcer by histopathology. Experiment-2 comprised of 18 rats: Group-C, Group-D and Group-E having 6 rats in each group. Group-C served as disease control group and provided with normal saline (2 ml/kg body wt). Group-D was provided with alcoholic extract of Nigella sativa (150 mg/kg body wt) and Group-E was provided with omeprazole suspension (20 mg/kg body wt). After 8 days of treatment, animals were fasted for 24 hrs. Then aqueous suspension of aspirin (200 mg/kg body wt) was administered and after 4 hrs all rats were sacrificed. Gross and microscopic examinations were performed to evaluate the results.Results: Aspirin caused marked gastric damage in negative control group which was prevented in omeprazole suspension and Nigella sativa extract treated groups significantly. The protective effect was maximum with omeprazole followed by alcoholic extract of Nigella sativa.Conclusion: Alcoholic extract of Nigella sativa showed significant protection against aspirin induced gastric ulcer in rats as compared to omeprazole.Delta Med Col J. Jul 2016 4(2): 61-66

UJI EFEK ANALGETIKA EKSTRAK BUAH KAKTUS (Opuntia elatior Mill.) PADA MENCIT (Mus musculus) YANG DIINDUKSI ASAM ASETAT

Pain is a mechanism of body defense. One way to allay or decreasing the pain is using medicines that have analgetic effect. The aim of this study is determine the analgetic effect of cactus fruits (Opuntia elatior Mill.) extract and the most effective dose to giving analgetic effect. This study used writhing method by the injection acetic acid 1% as induced. Group I as a negative control used natrium carboxy methylcellulose 1%, group II as a positive control used aspirin suspension which dosage was 1,3 mg/20g BB, group III as a extract of cactus fruits give to dose 50 mg/kg BB, group IV dose 100 mg/kg BB, and group V dose 150 mg/kg BB. The result shows that cactus fruits extract to giving analgetic effect judging from the reduction strength writhing reflex to protection percentage at dose 50 mg/kg BB (11,26%), 100 mg/kg BB (42,10%), 150 mg/kg BB(60,14%) and the positif control (75,34%), at the positif control shows that higher protection percentage. Effectiveness percentage analgetic extract of cactus fruits at dose of 50 mg/kg BB (14,4%), 100 mg/kg BB (55,36%), 150 mg/kg BB (79,95%) and positif control (100%). The data which is got from the calculation later is analyzed by Kruskal Wallis. The result showed that at dose of 150 mg/kg BB is p: 0,016 (p<0,05) when compared with the positive control. So that is different significantly between dose 150 mg/kg BB and the positive control. The extract showed a optimal analgetic effect characterized by a significant reduction in the number of writhes or abdominal stretches in mice with dose 150 mg/kg BB body weight used when compared to the cactus fruits extract dose 50 and 100 mg/kg BB

Anti-inflammatory and analgesic activity of novel oral aspirin-loaded nanoemulsion and nano multiple emulsion formulations generated using ultrasound cavitation

The present study investigated the anti-inflammatory and analgesic activities of novel aspirin oil-in-water (O/W) nanoemulsion and water-in-oil-in-water (W/O/W) nano multiple emulsion formulations generated using ultrasound cavitation techniques. The anti-inflammatory activities of nanoemulsion and nano multiple emulsion were determined using the λ-carrageenan-induced paw edema model. The analgesic activities of both nanoformulations were determined using acetic acid-induced writhing response and hot plate assay. For comparison, the effect of pretreatment with blank nanoemulsion and reference aspirin suspension were also studied for their anti-inflammatory and antinociceptive activities. The results showed that oral administration of nanoemulsion and nano multiple emulsion containing aspirin (60mg/kg) significantly reduced paw edema induced by λ-carrageenan injection. Both nanoformulations decreased the number of abdominal constriction in acetic acid-induced writhing model. Pretreatment with nanoformulations led to a significant increase in reaction time in hot plate assay. Nanoemulsion demonstrated an enhanced anti-inflammatory and analgesic effects compared to reference suspension while nano multiple emulsion exhibited a mild inhibitory effects in the three experimental animal model tests. The results obtained for nano multiple emulsion were relatively lower than reference. However, administration of blank nanoemulsion did not alter the nociceptive response significantly though it showed slight anti-inflammatory effect. These experimental studies suggest that nanoemulsion and nano multiple emulsion produced a pronounced anti-inflammatory and analgesic effects in rats and may be candidates as new nanocarriers for pharmacological NSAIDs in the treatment of inflammatory disorders and alleviating pains.

Illustration of the impact of antiplatelet drugs on the genesis and management of chronic subdural hematoma

The case of a 76-year-old male with a large chronic subdural hematoma that showed total regression with the mere suspension of aspirin, its only apparent causal factor, and that of an 81 year-old male on aspirin and clopidogrel with a chronic subdural hematoma who succumbed after burr holes due to two simultaneous severe hemorrhagic complications (cerebellar hemorrhage and ipsilateral acute subdural hematoma) are presented. The cases may provide support for the following management strategies: (i) if conservative management and drug suspension are feasible, they may well be worth trying and lead to a favorable outcome; (ii) if a patient is at risk of developing a chronic subdural hematoma, namely because of a minor acute subdural hematoma, withdrawal of antiplatelet agents should be considered; (iii) if surgery is necessary, its delay allows for the metabolization of the drug and platelet renewal, thereby minimizing the risk of hemorrhage; (iv) if urgent burr holes are indicated, measures to improve platelet function should be undertaken.

Levy G, Hayes B, “Physiochemical Basis of the Buffered Acetylsalicylic Acid Controversy New Engl. J. Med. 262:1053–1058 (1960)”—The Backstory

Levy G, Hayes B, “Physiochemical Basis of the Buffered Acetylsalicylic Acid Controversy New Engl. J. Med. 262:1053–1058 (1960)”—The Backstory

Enhancement of anti-inflammatory property of aspirin in mice by a nano-emulsion preparation

Aspirin, a non-steroidal anti-inflammatory drug, widely used for its anti-inflammatory properties is associated with several systemic side effects including gastro-intestinal discomfort. Inflammation can be mediated by pro-inflammatory cytokines and, along with various other host factors eventually give rise to edema at the inflamed site. Because of the adverse side effects oftentimes associated with systemic exposure to aspirin, the aim of the present study was to investigate whether the anti-inflammatory property of aspirin would enhance if delivered as nano-emulsion preparation. Nano-emulsion preparations of aspirin prepared with a Microfluidizer® Processor were evaluated in the croton-oil-induced ear edema CD-1 mouse model using ear lobe thickness and the accumulation of specific in situ cytokines as biomarkers of inflammation. The results showed that particle size (90 nm) populations of nano-emulsion preparations of aspirin compared to an aspirin suspension (363 nm), significantly decreased ( p < 0. 05) ear lobe thickness approximately 2 fold greater than the aspirin suspension. In addition, the aspirin nano-emulsion further reduced the auricular levels of IL-1α (− 37%) and TNFα (− 69%) compared to the aspirin suspension preparation ( p < 0.05). The reductions in ear lobe thickness were also significantly associated with accumulated tissue levels of IL-1α ( r = 0.5, p < 0.009) and TNFα ( r = 0.7, p < 0.0004), respectively. In conclusion, these studies indicate that a nano-emulsion preparation of aspirin significantly improved the anti-inflammatory properties of an aspirin suspension in a CD-1 mouse model of induced inflammation.

O.344 Comparison of the post-extraction bleeding in patients with and without suspension of aspirin 100 mg daily

In the present study, we report a synergistic interaction between acetylsalicylic acid (ASA) and caffeine (CAF) on the inhibition of nociception in a model of peripheral inflammation in rat; on the contrary no interaction have been found on anti-inflammatory effects and peripheral prostaglandin E2 (PGE-2) synthesis inhibition. Acute inflammation was induced by the subplantar injection of carrageenan into the right hind paw, and the effects of the drugs were evaluated from 0 to 5 h. Nociception was assessed using the Randall & Selitto test, and the inflammatory response by plethismometry. Oral administration of ASA (10–400 mg/kg) induced dose-related anti-nociceptive and anti-inflammatory effects. On the other hand, oral CAF administration (5–50 mg/kg) did not show a dose-related inhibitory effect, neither on the inhibition of nociception nor on the inflammatory response. To analyze a possible interaction between both drugs a dose–response curve to ASA plus a fixed dose of CAF (5 mg/kg) was obtained 3 h after the injection of carrageenan, when the inflammatory pain peaked. A fixed dose of CAF was able to improve the anti-nociceptive, but not the anti-inflammatory, effects of ASA. We also assessed, by enzyme immunoassay, the effects of the combination on peripheral PGE-2 levels: CAF did not alter the inhibitory effect of ASA on PGE-2 synthesis. Our results corroborate the well-known clinical effects of combining ASA and CAF; on the other hand, we rule out that prostaglandin synthesis inhibition at peripheral sites would be the mechanism responsible of the adjuvant anti-nociceptive effect of CAF.

Reduction of platelet deposition on vascular grafts using an antiplatelet graft coating technique

The systemic use of platelet inhibitors has been shown to improve vascular graft function. In this study a biodegradable coating of polymeric polylactic acid (PLA) containing a microparticulate suspension of aspirin (ASA) 30% by weight, was applied to the lumenal surface of small diameter vascular prostheses to reduce platelet deposition on canine implanted arterial grafts. USCI 4-mm ID Dacron internal velour grafts were used. Coated and contralateral noncoated (control) prostheses were implanted in canine carotid and femoral arteries. Graft performance was assessed by determination of aspirin elution rates, in vivo red cell subtracted 111indium-labeled platelet scans, and post implant platelet aggregation studies. Eighty percent of the aspirin in the coated grafts was released during the first 24 hr of perfusion and approximately 20% of the aspirin remained in grafts after 1 month. In vivo platelet scans documented less platelet deposition on ASA-coated grafts when compared to controls 2 and 24 hr post implant ( P < 0.01, P < 0.05, respectively). There was no significant difference in platelet deposition on ASA-coated and control grafts at 2 weeks or 1 month post implant. Post implant platelet aggregation studies indicated systemic platelet inhibition for 4–5 days. It was concluded that aspirin incorporation in a polylactic acid coating applied to 4-mm ID vascular prostheses reduced the platelet affinity of Dacron grafts and exerted a temporary local and systemic platelet inhibiting effect.

Cocarcinogenic Action of Aspirin on Gastric Tumors Induced by N-Nitroso-N-methylnitroguanidine in Rats1

Albino rats (noninbred) were divided into 4 groups: 1) 56 control rats, 2) 40 rats fed 1 ml aspirin suspension (40 mg/ml) twice a week, 3) 20 rats given N-nitroso-N-methylnitroguanidine (MNNG) solution (250 micrograms/ml) to drink ad libitum, and 4) 40 rats given both aspirin and MNNG. In 18 months, there were no gastrointestinal tumors in groups 1 and 2, 8 cases of gastric tumors in group 3, and 37 cases of gastric tumors in group 4. Adenocarcinomas of the glandular stomach were found in 21 of 40 rats in group 4 but in only 4 of the 20 rats in group 3; the difference in incidence was significant. Histologic and electron microscopic examination of the epidermoid carcinomas and adenocarcinomas in group 4 showed no difference from such tumors induced by MNNG only. Hyperplasia of the forestomach mucosa and hyperplasia of the pyloric gland region of the glandular stomach in group 4 were more severe.

Are all aspirins really alike? A comparison of gastric ulcerogenicity with bio-efficacy in rats

Summary o 1. Fifteen aspirin formulations (including 11 commercial types) and various other salicylate preparations were compared primarily for intrinsic gastric ulcerogenicity in cold stressed rats — a sensitive model for determining potential ulcerogenic activity. Several buffered aspirins were notably just as ulcerogenic as aspirin suspensions. 2. High Na + -containing aspirin formulations were the least ulcerogenic of those examined but also exhibited the shortest duration of action as antipyretics when assayed against yeast-induced fever in rats. Incorporation of D-glucose with certain metabolizable bases (citrate, acetate) markedly reduced the ulcerogenic activity of aspirin. 3. Aspirin impurities, benorylate, several non-acetylated salicylates (e.g. diflunisal, diplosal) were compared for anti-inflammatory potency, antipyretic activity and gastric ulcerogenic. These results suggest that for non-analgesic use, salts of salicylic acid, diflunisal and diplosal would seem preferable to aspirin — conferring the same potential benefit (as anti-inflammatory/antipyretic drugs) but with lower gastric ulcerogenicity.

Simulation of the effects of gastrointestinal transit rate on drug availability from aspirin suspensions using a modified dialysis method

A dialysis method that allows the effect of viscosity on the gastrointestinal transit rate to be simulated in vitro is described. The method has been applied to a series of aspirin suspensions. Various suspending agents have been used to produce suspension media with a range of viscosities. The results correlated with previously obtained bioavailability parameters and support the suggestion that the effect of viscosity on gastrointestinal transit rate is an important factor in determining the bioavailability of aspirin from such formulations when administered to the rabbit.

The effects of various suspending agents on the bioavailabilities of aspirin and salicylic acid in the rabbit

Bioavailability studies on aspirin suspensions in rabbits using an 8 × 8 latin square design of experiment have shown that significant differences in the amount of drug absorbed, but not in its rate of absorption, occur when different macromolecular suspending agents are used. Linear relationships between the logarithm of the apparent viscosity of the suspension medium at a shear rate of 100 s −1, pH 1.2 and 37°C and the amount of drug absorbed in 9 h and its peak concentration in the blood have been established. It is suggested that the effect of viscosity on the gastric emptying rate is the reason for the variation in the bioavailability of aspirin from the suspensions. Results obtained using suspensions of salicyclic acid in 1% w/v dispersions of sodium carboxymethylcellulose and xanthan gum in a two-way cross-over test in 8 rabbits substantiate those obtained with the aspirin suspensions and indicate that the effect of viscosity on the hydrolysis of aspirin in the gastro-intestinal tract is not important from a bioavailability points of view. The unsuitability of traditional flask-stirrer and dialysis techniques as methods capable of providing results for satisfactory correlation with the in vivo bioavailability parameters obtained in this study is discussed.

Effect of Aspirin and Acid on Human Jejunal Mucosa

To determine the effects of aspirin and hydrochloric acid on human jejunal mucosa, three obese patients with a small intestinal bypass that opened on the abdominal wall as a mucous fistula were studied. An 80-mM solution of HCl, a 40-mM suspension of aspirin (equivalent to two tablets in a glass of water), and a combination suspension of 40 mM aspirin plus 40 mM HCl damaged a mean +/- SE of 26 +/- 13% (P less than 0.05), 24 +/- 5% (P less than 0.05), and 29 +/- 5% (P less than 0.05) of jejunal villi, respectively, 5 min after administration. By 60 min after instillation, considerable recovery had occurred. Scanning electron microscopy revealed focal villous tip erosion and erythrocyte extrusion after all test solutions. In conclusion, aspirin, 40 mM, physiologic concentration of hydrochloric acid, and the combination of acid plus aspirin are each capable of damaging human small intestinal mucosa on direct contact.

The influence of acetylsalicylic acid (aspirin) on gastric mucosal content of energy-rich phosphate bond.

The mucosal content of adenosine triphosphate, adenosine diphosphate and adenosine monophosphate in mini-pig corpus gland area and in pyloric gland area was examined after aspirin ingestion in acute experiments and after ingestion for several weeks. Ingestion of aspirin led to a statistically significant decrease of adenine nucleotide content in corpus gland and in pyloric gland area. An inverse correlation between the pH of the aspirin suspensions and the size of the decrease was established in the short-time experiments. In non-affected pyloric gland area mucosa and adenine nucleotide content was significantly lower than in the corpus gland area. Pyloric mucosa was more susceptible to aspirin-induced lowering of adenine nucleotide content than was the corpus mucosa. Prolonged aspirin ingestion led to statistically significant reductions of adenine nucleotide pool. The findings explain the decrease in mucous secretion and in acid secretion demonstrated in several studies. The finding of lower and more susceptible adenine nucleotide pool in the pyloric area might be the explanation for the preponderant occurrence of aspirin ulcerations in this region.

USE OF ASPIRIN IN HAEMORRHAGIC SHOCK

Comment: It is of course well known that aspirin reduces platelet adhesiveness, and this paper shows the usefulness of the drug in hemorrhagic shock. The limitation to the practical application of these observations lies in the fact that, with the exception of the intraarterial injection of a suspension of aspirin, no suitable method has as yet been devised to administer it other than by mouth, a route which may not be always available in severely shocked patients, either because they are unable to retain substances administered in this way, or because they may be unable to absorb them adequately, even if instilled into the stomach by way of an indwelling tube.

Evaluation of Dimethylpolysiloxane Fluids as Vehicles for Various Pharmaceuticals I: Effect on Stability and Dissolution of Aspirin

The physicochemical effects of dimethylpolysiloxane fluids as vehicles for aspirin on its stability and release characteristics were evaluated. Aspirin was extraordinarily stable in the silicone fluids. No decomposition was noted during 8 weeks of storage at 4 and 26°, and less than 0.5% degradation was detected after 8 weeks of storage at 45°. Moreover, the dissolution patterns of aspirin suspensions in the silicone fluids appeared to be quite satisfactory as compared with that of plain aspirin powder.

The effect of hyperbaric helium-oxygen on the acute toxicity of several drugs

The effect of a hyperbaric helium-oxygen environment on drug toxicity was investigated in the following systems: (1) The intravenous lethal doses of pentobarbital, lidocaine, and ethanol in rats; (2) the intravenous LD50 for morphine in rats; and (3) the oral toxicity of an LD50 dose of aspirin in mice. Except for mice given aspirin, restrained, unanesthetized animals were equilibrated with the atmosphere (19.2 atm abs. helium-0.2 atm abs. oxygen, equivalent to the pressure at a depth of 600 feet) for 45 min in a hyperbaric chamber. Animals were then injected remotely via indwelling jugular vein catheters. The lethal dose of pentobarbital, lidocaine, or ethanol was determined by slow intravenous infusion to the point of respiratory arrest. The LD50 of morphine was determined from the mortality 2 hr after injection. Mice were injected orally with a suspension of aspirin in sodium alginate and pressurized rapidly; the mortality was determined 3 hr later. For each drug, control animals were treated in exactly the same manner as pressurized animals. In the case of every drug examined, the toxicity observed during exposure to the hyperbaric environment did not differ significantly from that under normal pressure.