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Prolactin (PRL) and growth hormone (GH) secretion have been evaluated in 17 acromegalic patients following acute administration of two dopamine (DA) receptor antagonists, i.e. sulpiride (SULP) and domperidone (DOM). Six patients had persistent hyperprolactinemia. In 8 normoprolactinemic patients, i.m. injection of 100 mg SULP elicited only a slight rise iN plasma PRL, which was strikingly lower than that SULP induced in control subjects. Likewise, an i.v. bolus injection of DOM (4 mg) was barely effective to raise plasma PRL in the 11 normoprolactinemic and the 6 hyperprolactinemic patients. DOM was instead capable of inducing a clear-cut rise in plasma PRL in normoprolactinemic controls and in a group of subjects with puerperal hyperprolactinemia. Neither drug affected GH secretion in acromegalic patients. It is proposed that a defective tuberoinfundibular DA function or, alternatively, a diminished PRL reserve due to a decrease pituitary lactotroph mass may be responsible for the blunted PRL responsiveness of acromegalics. However, standing the paucity of present knowledge on the pituitary PRL secretory pool in acromegalics, neither hypothesis seems capable to account satisfactory for the reported results.
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This work comparatively studies the effects of dihydroergocristine, timolol and pilocarpine on intraocular pressure and pupil diameter in conscious rabbits. Intraocular pressure was measured by applanation tonometry and the pupil diameter by a photographic technique. In anesthetized rabbits, changes in tonographic facility of aqueous humor outflow and rate of aqueous humor formation were evaluated. Dihydroergocristine reduced the intraocular pressure more than timolol and much more than pilocarpine. The ocular hypotensive effect of dihydroergocristine was accomplished by a great reduction in aqueous humor formation, which surpasses the decrease in aqueous humor outflow, while timolol mainly reduced aqueous humor formation and pilocarpine increased aqueous humor outflow. Pupil diameter remained unchanged on dihydroergocristine, whereas timolol induced a slight mydriasis and pilocarpine provoked a clear myosis. Effects of dihydroergocristine might result in blockade of alpha-adrenoceptors in ciliary body, although available data about pretreatment with either metoclopramide or domperidone suggest that dopamine DA2-receptors might participate in ocular hypotensive effect of ergot derivatives.
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Before the black box warning, 69.8% of patients received metoclopramide for gastroparesis, compared with 23.7% after the warning. Gastroenterologists prescribed domperidone more often after than before the warning. Metoclopramide prescriptions decreased after 2008. Adverse event reporting increased after the warning. Only 3.6% of all FAERS reports but 70% of TD reports were filed by lawyers, suggesting a distortion in signal. Forty-seven legal opinions were identified, 33 from 2009-2010.
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Central administration of amylin (2.2 microg/rat, i.c.v.) reduces (from a minimum of 67% to 83%) indomethacin (Indo, 20 mg Kg(-1), orally) induced ulcers in rats. The anti-ulcer effect of the peptide is not removed by the administration of prokinetic drugs like domperidone or neostigmine but it is reduced by 35% in rats treated with capsaicin or with the CGRP antagonist, CGRP(8-37). These data indicate that amylin gastroprotection involves capsaicin-sensitive nerve fiber leading to CGRP-dependent gastric vasodilatory effect. Additional mechanisms could involve noradrenergic alpha(2) receptors as the peptide gastroprotective activity is reduced from 67% to 20% by the alpha(2) antagonist yohimbine.
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1. The present study investigated the in vitro effect of dopamine on platelet responses in healthy subjects. 2. Dopamine concentrations over 5 mumol/L induced a primary aggregating response and a slight release of alpha-granule proteins, beta-thromboglobulin and platelet factor-4 in all subjects. In 25% of investigated subjects a delayed secondary aggregation was observed with dopamine concentrations over 100 mumol/L. 3. Low dopamine concentrations (5-7.5 nmol/L) increased the platelet sensitivity to other aggregating agents (adenosine diphosphate, collagen and sodium arachidonate). The effect of subaggregating concentrations of serotonin was potentiated by dopamine. 4. The effect of dopamine on platelet responses was prevented by low concentrations of alpha-adrenoceptor antagonists (phentolamine and yohimbine); antagonists of dopamine receptors (haloperidol and domperidone) were able to decrease the extent of the dopamine-induced secondary aggregating wave in the responders, but they failed to prevent the primary aggregation and the effects on platelet response to other aggregating agents. 5. The present data demonstrated that the effects of dopamine on human platelets are mainly mediated by interactions with alpha-adrenoceptors.
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The statistical analysis showed significant improvement in organoleptic properties such as chewable mass, product taste, product consistency, product softness, total flavour lasting time and pharmaceutical properties like micromeritic properties after incorporation of appropriate excipients in an optimum amount in final optimized MCG formulation. In vivo drug release study showed 97% DM release whereas ex vivo buccal permeation study through goat buccal mucosa exhibited 11.27% DM permeation within 15 min indicating its potential for increasing bioavailability by decreasing time of onset. The optimized formulation showed good surface properties and the peak load required for drug release was found to be acceptable for crumbling action.
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To observe the effect of pungent dispersion bitter purgation method (PDBPM) on the esophageal mucosal intercellular space of reflux esophagitis (RE) model rats.
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To further evaluate the functional significance of dopamine (DA) receptors in different vasculature, in this study we compared the effects of D1- and D2-receptor agonists on canine coronary and renal arteries by measuring adenylate cyclase (AC) activity as a biomedical index of DA receptor function. It was found that both the selective D1-receptor agonist, fenoldopam, and the D2-receptor agonist, propyl-butyl-dopamine (PBDA), induced a dose-related increases in cAMP formation in coronary and renal arteries; however, the magnitude of increase in the renal artery was remarkably greater than that in the coronary artery. The stimulatory effect on AC activity of fenoldopam was significantly more potent than that of PBDA. The selective D1-receptor antagonist, SCH23390, blocked fenoldopam- and PBDA-induced cAMP production, while the selective D2-receptor antagonist, domperidone, was without effect on the increase of cAMP elicited by PBDA. After beta-adrenergic blockade with propranolol, fenoldopam still increased the cAMP level significantly but to a much lesser degree. The existence of postsynaptic D2-receptor associated with inhibition of cAMP formation could not be demonstrated in this study. These data suggest the presence of D1-receptors associated with stimulation of AC activity in both renal and coronary arteries. However, there are much fewer receptor sites in the coronary artery than in the renal artery, suggesting less physiological importance of such receptors in the coronary artery than in the renal artery.
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This experiment deepened our understanding of insufficient gastrointestinal dynamics, confirmed that QZWT treating gastrointestinal disorders was through multicomponent, multitarget ways. These results fully reflect the multiple targets synergy characteristics of TCM.
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The acute effects of oral metoclopramide (40 mg/day) and domperidone (80 mg/day) on esophageal motor activity and acid reflux were assessed in a randomized, double-blind, placebo-controlled study in 20 patients with erosive reflux esophagitis. Esophageal motor function was assessed by standard manometry with wet swallows, and reflux events were evaluated by ambulatory 24-hr pH-monitoring. Both drugs caused a significant (P less than 0.05) increase in lower esophageal sphincter pressure lasting at least 120 min. However, neither esophageal body motility, duration of esophageal exposure to acid, nor esophageal clearance were effected by drug administration in comparison to placebo. Side effects were reported in two patients who received metoclopramide, while no adverse effects occurred after domperidone intake. In conclusion, the so-called motility agents metoclopramide and domperidone have few acute effects on esophageal motility in patients with erosive reflux esophagitis.
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Cisapride is a substituted benzamide compound that stimulates motor activity in all segments of the gastrointestinal tract by enhancing the release of acetylcholine from the enteric nervous system. Cisapride is administered orally in the treatment of gastro-oesophageal reflux disease, functional dyspepsia, gastroparesis, chronic intestinal pseudo-obstruction syndromes and chronic constipation. In gastro-oesophageal reflux disease in both adults and children, cisapride provides symptomatic improvement and mucosal healing. Long term treatment with cisapride is effective in the prevention of relapse of oesophagitis. Cisapride improves gastric emptying rates and improves symptoms in patients with gastroparesis of various origins. Unlike domperidone and metoclopramide, long term administration of cisapride seems to result in persistently enhanced gastric emptying. Cisapride is also effective in improving symptoms in patients with functional dyspepsia. In comparative studies in patients with functional dyspepsia, cisapride was at least as effective as metoclopramide, domperidone, clebopride, ranitidine and cimetidine. Cisapride increases stool frequency and reduces laxative consumption in patients with idiopathic constipation. Severe cases of slow transit constipation seem refractory to cisapride. Clinical studies also indicate that cisapride might be effective in the treatment of chronic intestinal pseudo-obstruction, postoperative ileus, peptic ulcer and irritable bowel syndrome. Further clinical studies are warranted to define the role of cisapride in these conditions. The dosage of cisapride ranges from 5mg 3 times daily to 20mg twice daily. Cisapride is generally well tolerated, both during short and long term treatment. In children, cisapride is also well tolerated in doses of 0.2 to 0.3 mg/kg, 3 to 4 times daily.(ABSTRACT TRUNCATED AT 250 WORDS)
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Secretoneurin (SN), a 33-34 amino acid neuropeptide is derived from endoproteolysis of secretogranin II (SgII), a member protein of the chromogranin family. SN is widely distributed in various tissues of vertebrates especially in pituitary and hypothalamus, and is a potential new hormone. In vivo, i.p. injection of SN increased luteinizing hormone (LH) release in goldfish pretreated with the dopamine antagonist domperidone. In 6-h static incubation of goldfish pituitary fragments, 10 and 100 nM but not 1 nM concentrations of goldfish SN had a direct stimulatory effect to increase LH release by 2.3- and 1.5-fold (p<0.05), respectively. In addition, 500 nM SN induced a 2.6-fold increase in LHbeta subunit messenger RNA (mRNA) levels in pituitary fragments, regardless of whether LHbeta mRNA levels were expressed relative to 18S ribosomal RNA or beta-actin mRNA. We suggest that the stimulatory actions of SN on LH release may be a part of a paracrine or autocrine feedback loop in the pituitary.
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The study population comprised 4,838,146 individuals aged <18 years, who contributed an overall 25,575,132 person-years of follow-up. Within this population, we identified 1,015 potential cases of ALI. Overall, 20 positive drug-ALI associations were detected. The associations between ALI and domperidone, flunisolide and human insulin were considered as potentially new signals. Citalopram and cetirizine have been previously described as hepatotoxic in adults but not in children, while all remaining associations were already known in both adults and children.
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In the Bennett's wallaby prolactin is thought to maintain lactational and seasonal quiescence and is essential for early lactation. However, plasma prolactin concentrations determined in daily or weekly samples at these times are unchanged. In the present study, female Bennett's wallabies were blood sampled at 2-hr intervals over a 24-hr period during seasonal quiescence on either natural or artificial photoperiods to determine whether a diurnal rise of prolactin occurs at this time. Prolactin concentrations did not exhibit a diurnal change. Further experiments were aimed at determining whether there was an increase in the prolactin response to a dopamine antagonist or TRH during the transition to seasonal quiescence. Nonlactating and lactating female Bennett's wallabies were treated with saline, 0.5, 1, and 2 mg of the dopamine antagonist domperidone and 100 micrograms TRH in October, December, February, and April. In both groups there was a significant elevation in plasma prolactin concentration in response to domperidone with an increasing response at each successive month. In early (October and December) and peak (April) lactation the prolactin response was greater in lactating animals. There was no significant prolactin response to TRH in lactating animals. In nonlactating wallabies, the prolactin response to TRH was increased in February. At peak lactation (April), the response to 1 mg domperidone was blocked when the dose was administered 2 hr after temporary removal of pouch young (RPY). With either larger doses (20 mg) or a 1-mg dose injected 8 hr after RPY, a significant prolactin response was observed.(ABSTRACT TRUNCATED AT 250 WORDS)
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Complications associated with the use of antiparkinsonian drugs make PD management more difficult given the need for antidopaminergic therapy, which worsens motor functioning in patients with PD. For psychosis, clozapine is the only atypical antipsychotic that has proven effective without worsening motor function in PD patients. However, its use requires the monitoring of agranulocytosis. Newer atypical antipsychotics such as quetiapine have been claimed to be safe in terms of motor functioning, but evidence about their effectiveness is not compelling. The emergency treatment of psychosis in PD would require parenteral administration, only available for olanzapine and ziprasidone. However, no randomized controlled trials have been conducted to establish the efficacy and safety in this setting. For nausea and vomiting, very little domperidone crosses the blood-brain barrier. As a result, the risk of developing extrapyramidal adverse effects is minimal. Metoclopramide blocks central dopamine receptors and worsens motor parkinsonian symptoms. Chlorpromazine, the first-line treatment of intractable hiccups, is contraindicated in PD. Baclofen could be considered as a first-line alternative.
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We have reported that nicotine and the specific α7AChR agonist ameliorate indomethacin-induced intestinal lesions in mice by activating α7 nicotinic acetylcholine receptors (α7nAChR). Dopamine D₂-receptor antagonists, such as domperidone and metoclopramide, enhance the release of ACh from vagal efferent nerves. The present study examined the effects of domperidone and metoclopramide on indomethacin-induced small intestinal ulceration in mice, focusing on the α7AChR. Male C57BL/6 mice were administered indomethacin (10 mg/kg, s.c.) and sacrificed 24 h later. Domperidone (0.1-10 mg/kg) and metoclopramide (0.03-0.3 mg/kg) were administered i.p. twice, at 0.5 h before and 8 h after indomethacin treatment, while methyllycaconitine (a selective antagonist of α7nAChR, 30 mg/kg) was administered twice, at 0.5 h before each domperidone treatment. Indomethacin caused severe hemorrhagic lesions in the small intestine, mostly to the jejunum and ileum, with a concomitant increase in myeloperoxidase (MPO) activity. Domperidone suppressed the severity of lesions and the increase in MPO activity at low doses (0.1-3 mg/kg), but not at a high dose (10 mg/kg). Similar effects were also observed by metoclopramide. The protective effects of domperidone and metoclopramide were totally abolished by prior administration of methyllycaconitine. Indomethacin treatment markedly enhanced inducible nitric oxide synthase and chemokine mRNA expression in the small intestine, but these responses were all significantly attenuated by either domperidone or metoclopramide. These findings suggest that dopamine D₂-receptor antagonists ameliorate indomethacin-induced small intestinal ulceration through the activation of endogenous anti-inflammatory pathways mediated by α7nAChR.
We have investigated the effects of dopamine on the response of the mouse isolated vas deferens to electrical stimulation and, contrary to previous investigators, have found that there are specific dopamine receptors present in this tissue. A range of dopamine antagonists have been examined vs the effects of dopamine and the Ke values obtained indicate that the receptor present is of the DA2 subtype. Domperidone, spiperone and haloperidol possess a very high affinity for the receptor, whereas the selective DA1-antagonist SCH 23390 has only low affinity. Bromocriptine was found to possess both alpha 2- and dopamine agonist activity in this preparation and it is also possible to demonstrate dopamine agonist activity of noradrenaline. In the presence of alpha 2-antagonists, the mouse vas deferens is an extremely simple preparation suitable for the rapid screening of compounds for DA2-agonist or antagonist activity.
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The short-term effects of fluphenazine on plasma HVA concentrations were compared with the effects of fluphenazine and concurrent administration of debrisoquin, a monoamine oxidase inhibitor which does not cross the blood brain barrier and is used to enhance the CNS contribution to circulating plasma HVA concentrations. Fluphenazine significantly increased plasma HVA with or without debrisoquin 24 hours following the initiation of treatment. Domperidone, a butyrophenone dopamine antagonist which acts only in the peripheral nervous system, failed to alter plasma HVA concentrations. These data suggest that the acute effects of neuroleptic drugs on plasma HVA concentrations are dependent upon interaction with CNS dopaminergic systems and provide additional support for the use of plasma HVA as a reflection of CNS dopamine system activity in clinical studies.
To study the efficacy and safety of combined therapy of compound azintamid and domperidone in functional dyspepsia.
Slices of the rabbit caudate nucleus were preincubated with 3H-dopamine or 3H-choline and then superfused and stimulated electrically. DiPr-5,6-ADTN reduced the stimulation-evoked overflow of tritium over the same concentration range, independently of whether slices had been preincubated with 3H-dopamine or 3H-choline, and the same was true for apomorphine, NPA and pergolide. Three other putative dopamine receptor agonists, namely 3-PPP, DPI and SKF 38393, failed to decrease the evoked overflow of tritium. Each of six antagonists--(-)-sulpiride, (+)-sulpiride, CGP 11109 A, cis-flupentixol, domperidone and corynanthine--increased the evoked overflow over the same concentration range in experiments with 3H-dopamine and in those with 3H-choline. For each of these antagonists except cis-flupentixol, and also for chlorpromazine, haloperidol and rauwolscine, the pA2 values against apomorphine obtained in 3H-dopamine and in 3H-choline experiments were closely similar. The antagonist effect of cis-flupentixol against apomorphine was not purely competitive. (-)-Sulpiride was a more potent antagonist than (+)-sulpiride, and cis-flupentixol was more potent than trans-flupentixol. This study supplements a previous one in which (+/-)-sulpiride, metoclopramide and molindone were used as antagonists. It is a functional in vitro approach to receptor characterization, as opposed to radioligand binding studies or in vivo investigations. The results show that a large number of dopamine receptor agonists and antagonists are unable to distinguish between the presynaptic, release-inhibiting dopamine autoreceptors and those postsynaptic dopamine receptors which, when activated, depress the release of acetylcholine.(ABSTRACT TRUNCATED AT 250 WORDS)
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Prokinetic agents are effective not only for disease of the gastrointestinal (GI) tract but also for those external to the GI tract such as the central nervous system, and the respiratory, urologic, and metabolic organs. This article reviews the effectiveness of prokinetic agents against diseases external to the GI tract. Studies were identified by computerized and manual searches of the available literature. A Medline search was performed (1975-July, 2008) using the following medical subject headings: prokinetic agent, metoclopramide, domperidone, trimebutine, cisapride, itopride, mosapride, tegaserod, and human. The identified diseases for which prokinetic agents may be effective are various: bronchial asthma, chronic cough, hiccup, spontaneous bacterial peritonitis, cholelithiasis, diabetes mellitus, acute migraine, Parkinson's disease, anorexia nervosa, Tourette's disorder, urologic sequelae of spinal cord injury and of radical hysterectomy for cervical cancer, laryngeal dysfunction and so on. These agents are also useful for prevention of aspiration pneumonia during anesthesia, and in tube-fed patients. Prokinetic agents should be a valuable addition to our currently limited pharmacological armamentarium not only for functional bowel disease, but also for diseases external to the GI tract.
Drug-induced prolongation of cardiac repolarization may trigger malignant ventricular arrhythmias, such as torsade de pointes. The duration of QT interval, QT corrected for heart rate (QTc), JT interval, QT dispersion (QTd), QT variability index, and transmular dispersion of repolarization (TDR) are ECG markers of torsadogenicity. All volatiles, especially isoflurane and desflurane, have been found to prolong QTc and QTcd, while sevoflurane has probably no effects on TDR. Among i.v. anaesthetics, propofol seems superior due to its minimal effects on QTc and TDR; moreover, a decrease in QTc and QTcd has been demonstrated in many studies. Regarding opioids, fentanyl, alfentanil, and remifentanil produce no effects on QTc, while sufentanil, at high doses, may induce QT prolongation. Succinylcholine, but not the non-depolarizing neuromuscular blockers, produces QTc prolongation which can be attenuated by opioids and β-blockers. Reversal of neuromuscular block with anticholinesterase-anticholinergic combinations has been associated with significant QTc prolongation, while such an effect has not been demonstrated for sugammadex, even at high doses. Local anaesthetics have probably no intrinsic action on duration of repolarization; nevertheless, an extensive subarachnoid sympathetic block may increase the duration of QTc. On the contrary, thoracic epidural anaesthesia has been associated with a decrease in both QTc and TDR. Among adjuvants, midazolam seems to have no effect on QTc and TDR, while commonly used antiemetics, such as droperidol, domperidone, and most 5-HT3 antagonists, produce significant QT prolongation. The effects of anaesthetic drugs and techniques on electrocardiographic torsadogenic markers should be considered in the perioperative management of patients with preexisting repolarization abnormalities.
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Larrain A; Kapur VK; Gooley TA; Pope CE. Pharmacological treatment of obstructive sleep apnea with a combination of pseudoephedrine and domperidone.
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Consecutive patients (n = 240) with chronic cough were recruited and randomly assigned to receive modified (modified group) or primary (primary group) sequential three-step empirical therapy. The primary end-point was the overall rate of control of chronic cough. Secondary end-points were the rate of control of chronic cough at each step of therapy, the duration of treatment required, changes in cough symptom score, health-related quality of life and possible adverse effects.
The actions of dopamine, apomorphine and serotonin on the membrane potential of cultured astrocytes from rat spinal cord and striatum were examined. All three compounds caused a hyperpolarization of the majority of astrocytes tested. A small number of cells was depolarized and on a relatively large number of cells the amines had no effect. The dopamine antagonists cis-flupenthixol and domperidone reversibly blocked the effects of dopamine whereas the action of serotonin was antagonized by ketanserin. It is therefore concluded that the effect of both amines are due to activation of specific dopamine and serotonin receptors, respectively. Our electrophysiological data together with autoradiographic binding studies provide evidence that astrocytes possess receptors for dopamine and serotonin in addition to adrenoceptors and histamine receptors.
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Two different electronic databases (PubMed und Embase) were used to identify studies. Furthermore, a hand search for related articles was performed. No restriction was made concerning study types. Studies with patients undergoing chemotherapy radiation therapy or suffering from postoperative nausea, pediatric studies and studies published neither in English nor in German were excluded.
For AD patients with higher FSSG scores at baseline, domperidone was effective in preventing rivastigmine-related gastrointestinal disturbances.
In a single-blind trial of therapy in 20 patients with idiopathic Parkinson disease, domperidone prevented nausea and vomiting induced by bromocriptine without diminishing beneficial central effects. Combination of the two drugs permitted rapid increase in bromocriptine dosage from 22.5 mg per day to 148 mg per day, with 71% mean clinical improvement over baseline score; continuing efficacy of the regimen was evident for a mean follow-up of 2 months.
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Domperidone is a highly water insoluble drug exhibiting poor dissolution pattern. The purpose of this work was to increase the dissolution rate of Domperidone by formation of solid dispersion with different water soluble carriers. Binary systems of Domperidone were prepared with polyvinyl pyrrolidone k-30 (PVP), poloxamer 188 (P188) and polyethylene glycol 6000 (PEG 6000) at different weight ratios using the solvent evaporation method, physical mixtures of the same systems were also used. The effect of the method of preparation was also investigated by preparing some selected formulations using melting method. As P188 is known to inhibit CYP3A4 enzyme which is responsible for hepatic metabolism of many drugs including Domperidone, the effect of incorporation of PVP or PEG 6000 as ternary component to P188 solid dispersion on dissolution rate was also investigated. Formulations were characterized by Fourier transform infrared (FTIR) and Differential scanning calorimetry (DSC). Drug content uniformity and dissolution rate were studied. Solid dispersions showed a better dissolution compared to the pure drug and physical mixtures, with PVP showing the highest dissolution efficiency. As indicated from DSC data, Domperidone was in the amorphous form, which confirmed the better dissolution rate of solid dispersions. Some ternary P188 combinations showed a better enhancement in drug dissolution compared to the optimized P188 binary system. This would present a potential of increasing oral bioavailability of Domperidone by increasing its dissolution rate and by inhibiting its pre-systemic metabolism by the presence of P188.
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Determinar si existe evidencia de prolongación del intervalo QTc y efectos proarrítmicos asociados al uso de domperidona oral en infantes.