AU2002348828A1 - Methods of treatment using a gastric retained gabapentin dosage - Google Patents
Methods of treatment using a gastric retained gabapentin dosageInfo
- Publication number
- AU2002348828A1 AU2002348828A1 AU2002348828A AU2002348828A AU2002348828A1 AU 2002348828 A1 AU2002348828 A1 AU 2002348828A1 AU 2002348828 A AU2002348828 A AU 2002348828A AU 2002348828 A AU2002348828 A AU 2002348828A AU 2002348828 A1 AU2002348828 A1 AU 2002348828A1
- Authority
- AU
- Australia
- Prior art keywords
- dosage form
- gabapentin
- daily
- administered
- dosage
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Description
METHODS OF TREATMENT USING A GASTRIC RETAINED GABAPENTIN
DOSAGE
Background Of The Invention 5 Technical Field
The present invention relates to the use of gabapentin in a gastric retained dosage form. More specifically, the invention relates to the use of such dosage form to treat epilepsy and other disease states.
10 Background
Gabapentin (l-(aminomethyl)cyclohexaneacetic acid) is an anti-epileptic drug that is currently available in 100 mg, 300 mg and 400 mg hard shell capsule as well as 600 mg and 800 mg tablet dosage forms, with recommended dosing of 900 mg to 1800 mg total daily dose in three divided dosages. The oral bioavailability is dose-dependent, with is approximately 60% bioavailability for a dose in the range of 300-400 mg, but with only
35% bioavailability for a dose of 1600 mg (Bourgeois, Epilepsia 36 (Suppl. 5):S1-S7 (1995); Gram, Epilepsia 37 (Suppl. 6):S12-S16 (1996)). The decrease in bioavailability with dose has been attributed to carrier-mediated absorption (Stewart, et al., Pharmaceutical Research 10(2):276-281 (1993).
_o In early work with rats, Nollmer, et al., Arzneim-Forsch/Drug Research 36(1, Νr.
5):781-892 (1986) found that the absorption site for gabapentin was the duodenum. The absorption of gabapentin occurs relatively slowly with the peak plasma concentration occurring approximately 2-6 hours after dosing (Bourgeois, supra). The elimination of gabapentin is exclusively through renal pathways (Chadwick; The Lancet 343:89-91 (1994);
_5 Nollmer, supra; Thomson, et al., Clin. Pharmacoh.net. 23(3):216-230 (1992); and Riva, et al., Clin. Pharmacokinet. 31(6):470-493 (1996)) with reported half-Hves of 5-7 hours (Chadwick, supra) and 6-7 hours (Gram, supra).
A once- or twice-daily dosage form of gabapentin would be expected to improve compliance and therefore a controlled release dosage form has some distinct advantages
30 over the conventional immediate release formulations. In addition, a controlled release dosage form would lower the maximum plasma concentration, and this may result in reduced side effects. Since gabapentin is absorbed high in the gastrointestinal tract, by
means of a saturable transport mechanism, a gastric retained dosage form is particularly beneficial for delivery of gabapentin since the dosage form would be able to keep the drug in the region of absorption and show improved bioavailability by virtue of the slower release rate that avoids saturation of the carrier mediated transport of conventional dosages.
Summary Of The Invention
One aspect of the invention relates to a method of treating epilepsy comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form to a mammal in need of such treatment.
Yet another aspect of the invention relates to a method of treating neuropathic pain comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form to a mammal in need of such treatment. Still another aspect of the invention relates to an improved method of administering a therapeutically effective amount of gabapentin to a patient in need thereof, the improvement comprising administering gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form.
Description Of The Invention
The invention relates to a method of treating a disease state, such as epilepsy, by administering gabapentin in a once- or twice-daily gastric retained dosage form. The gastric retained dosage form is particularly beneficial for delivery of gabapentin due to its prolonged transit in the upper gastrointestinal tract, which allows the drug to be absorbed adequately in the preferred region of absorption. In addition, a gastric retained dosage form increases the tmax and allows for a smoother, more prolonged anti-spasmolytic effect. This dosage form also lowers the Cma and may result in reduced incidence and/or severity of CNS side effects of the drug, such as somnolence, ataxia, fatigue and dizziness.
Method of Treatment
The instant invention is a method of treating a disease state comprising administering a therapeutically effective amount of gabapentin, or a pharmaceutically
acceptable salt thereof, once- or twice-daily in a gastric retained dosage form to a mammal in need of such treatment. As used herein, the term "treating" covers treating the specified disease in a mammal, particularly a human, and includes:
(i) preventing the disease from occurring in a subject which may be predisposed to the disease but has not yet been diagnosed as having it;
(ii) inhibiting the disease, i.e. arresting its development; or (iii) relieving the disease, i.e. causing regression of the disease. One embodiment of the invention relates to an improved method of administering a therapeutically effective amount of gabapentin to a patient in need thereof, the improvement comprising administering gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form.
Other embodiments of the invention relate to methods of treating specific disease states comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form to a mammal in need of such treatment. Such methods find utility in treating numerous disease states that are currently being treated with conventional immediate release formulations of gabapentin and include, by way of illustration and not limitation, epilepsy; neuropathic pain; psychiatric disorders such as bipolar disorder and panic disorder; movement disorders such as restless leg syndrome, periodic movement disorder of sleep, essential tremor and acquired nystagmus; and prophylaxis of migraine headaches.
The invention also contemplates administering one or more additional therapeutic agents with the gabapentin treatment. The selection of these additional therapeutic agents will depend upon the specific disease state being treated, and are described in detail below.
Active Ingredient
The active ingredient in the method of the invention is gabapentin. Gabapentin is preferably used in the free amphoteric form. Pharmaceutically acceptable salt forms that retain the biological effectiveness and properties of gabapentin and are not biologically or otherwise undesirable can also be used and may show superior bioavailability. As used herein, the term "gabapentin" is intended to include the agent itself, as well as its pharmaceutically acceptable salts.
Pharmaceutically acceptable salts may be amphoteric and may be present in the form of internal salts. Gabapentin may form acid addition salts and salts with bases. Exemplary acids that can be used to form such salts include, by way of example and not limitation, mineral acids such as hydrochloric, hydrobromic, sulfuric or phosphoric acid or organic acids such as organic sulfonic acids and organic carboxylic acids. Salts formed with inorganic bases include, for example, the sodium, potassium, lithium, ammonium, calcium, and magnesium salts. Salts derived from organic bases include, for example, the salts of primary, secondary and tertiary amines, substituted amines including naturally- occurring substituted amines, and cyclic amines, including isopropylamine, trimethylamine, diethylamine, triethylamine, tripropylamine, ethanolamine, 2-dimethyl aminoethanol, tromethamine, lysine, arginine, histidine, caffeine, procaine, hydrabamine, choline, betaine, ethylenediamine, glucosamine, N-alkylglucamines, theobromine, purines, piperazine, piperidine, N-ethylpiperidine, fumarate, maleate, succinate, acetate and oxalate.
Additional Therapeutic Agents
The methods of the invention also contemplate the addition of one or more therapeutic agents with the gabapentin treatment.
For those embodiments of the invention where the gabapentin gastric retained dosage form is administered to treat epilepsy, such additional therapeutic agents can be other anti-epileptics or anticonvulsants, which include, by way of illustration and not limitation, hydantoins, iminostilbenes, valproates, phenyltriazines, barbiturates, deoxybarbiturates, benzodiazepines and carbamates. Such additional agents are preferably hydantoins, iminostilbenes, valproates or phenyltriazines.
The following examples of compounds within each of these classes is intended to be illustrative and not limiting in any manner. Examples of suitable hydantoin anticonvulsants include ethotoin, fosphenytoin, mephenytoin, and, preferably, phenytoin. An examples of a suitable iminostilbene is carbamazepine. Examples of suitable valproates include valprioic acid and sodium valproate. An exemplary suitable phenyltriazine is lamotrigene. A suitable barbiturate is phenobarbital and an exemplary deoxybarbiturate is primidone. An example of a suitable benzodiazepine is clorazepate. A suitable carbamate is felbamate.
For those embodiments of the invention where the gabapentin gastric retained dosage form is administered to treat neuropathic pain, such additional therapeutic agents can
be selected from the group consisting of other anticonvulsants, tricyclic antidepressants, levadopa, and opioids.
The following examples of compounds within each of these classes is intended to be illustrative and not limiting in any manner. Examples of suitable anticonvulsants include carbamazepine, phenytoin and lamotrigine. Suitable tricyclic antidepressants include amitriptyline, imipramine, clomipramine and desipramine. Examples of suitable opioids include oxycodone and tramadol.
For those embodiments of the invention where the gabapentin gastric retained dosage form is administered to treat psychiatric disorders, such additional therapeutic agents can be selected from the group consisting of lithium, carbamazepine, valproate, trifluoperazine, clonazepam, risperidone, lorazepam, venlafaxine, clozapine, olanzapine, benzodiazepines, neuroleptics, tricyclic antidepressants, selective serontin reuptake inhibitor (SSRI's), buprupion, and nefadone.
For those embodiments of the invention where the gabapentin gastric retained dosage form is administered to treat bipolar disorder, such additional therapeutic agents can be selected from the group consisting of lithium, carbamazepine, valproate, trifluoperazine, clonazepam, risperidone, lorazepam, venlafaxine, clozapine, olanzapine, benzodiazepines, and neuroleptics.
For those embodiments of the invention where the gabapentin gastric retained dosage form is administered to treat depression, such additional therapeutic agents can be selected from the group consisting of tri-cyclic anti-depressants, SSRI's, bupropion, venlaxatine, and nefadone.
For those embodiments of the invention where the gabapentin gastric retained dosage form is administered to treat manic disorders, such additional therapeutic agents can be selected from the group consisting of diazepam, and oxazepam.
For those embodiments of the invention where the gabapentin gastric retained dosage form is administered to treat movement disorders, such additional therapeutic agents can be selected from the group consisting of benzodiazepines, dopaminergic agents, and opiates, particularly levodopa/carbidopa and clonazepam. For those embodiments of the invention where the gabapentin gastric retained dosage form is administered for prophylactic treatment of migraine headaches, such additional therapeutic agents can be selected from the group consisting of tricyclic
antidepressants (amitriptyline, doxepin, imipramine, maprotiline, protriptyline, desipramine), SSRI (fluoxetine), triptine (sumatriptan, etc.), and ergotamine.
Dosage In general, the term "therapeutically effective amount" refers to that amount which is sufficient to effect treatment, when administered to a mammal in need of such treatment.
The therapeutically effective amount will vary depending on the subject being treated, the severity of the disease state and the manner of administration, and may be determined routinely by one of ordinary skill in the art. In particular, for use in the treatment of epilepsy or neuropathic pain with a gastric retained dosage form, gabapentin may be used at doses appropriate for treating epilepsy or neuropathic pain with immediate release dosage forms. However, the gastric retained dosage form is designed to provide for bioavailability of gabapentin at a level greater than or equal to 80% (>80%) relative to an equal dose of an immediate release dosage form. Typically, the method of the invention will involve administering gabapentin on a once- or twice-daily basis for as long as the condition persists.
An effective dosage of gabapentin for the treatment of epilepsy is typically in the range of about 300-3600 mg/day, typically about 900-2400 mg/day, more typically about
900-1800 mg/day. An effective dosage of gabapentin for the treatment of neuropathic pain is typically in the range of about 100-4800 mg/day, typically about 300-3600 mg/day, more typically about 900-2400 mg/day.
An effective dosage of gabapentin for the treatment of psychiatric disorders is typically in the range of about 100-4800 mg/day, more typically about 900-3600 mg/day. An effective dosage of gabapentin for the treatment of movement disorders is typically in the range of about 100-4000 mg/day, typically about 200-2700 mg day, more typically about 500-2700 mg/day.
An effective dosage of gabapentin for the prophylactic treatment of migraine headaches is typically in the range of about 200-4000 mg/day, typically about 500-3600 mg/day, more typically about 900-2400 mg/day.
Dosage Regimen
The methods of the invention provide a once- or twice-daily dose of the gabapentin gastric retained dosage form. The dosage can be administered at any time, but it is preferred that the dosage is administered at the same approximate time each day and in approximately 12 hour intervals for the duration of treatment. In addition, it is preferred that the gastric retained dosage form be taken with food, for example with the morning or evening meals.
Accordingly, in one embodiment of the invention, gabapentin is administered once- daily, for example, in the morning (e.g., upon rising or with the morning meal) or in the evening (e.g., with the evening meal or near bedtime).
In another embodiment of the invention, gabapentin is administered twice-daily, for example, with the first dose being in the morning (e.g., upon rising or with the morning meal) and the second dose being in the evening (e.g., with the evening meal or near bedtime), In another aspect of the invention, the method of administering a therapeutically effective amount of gabapentin in a gastric retained dosage form further includes administering one or more additional therapeutic agents.
The additional therapeutic agents can be administered at the same time or at a different time than the administration of gabapentin, and will depend upon the nature of the disease being treated as well as the agent itself. For example, when the additional agent is another anti-epileptic, a twice-daily dose is sufficient and it may be administered at the same time or at a different time than gabapentin. For purposes of facilitating patient compliance, administration of any of the aforementioned additional agents at the same time is preferred.
Dosage Form
There are several drug delivery systems that are suitable for use in delivering gabapentin in the method of the invention as they are particularly tailored to be gastric- retained dosages, such as the swellable bilayer described by Franz, et al., US Patent No. 5,232,704; the multi-layer tablet with a band described by Wong, et al., US Patent No.
6,120,803; the membrane sac and gas generating agent described in Sinnreich, US Patent No. 4,996,058; the swellable, hydrophilic polymer system described in Shell, et al., US
Patent No. 5,972,389 and Shell, et al., WO 9855107; all of which are incorporated herein by reference.
Of particular interest are gastric retained dosage forms that contain hydrophilic polymers that swell to a size such that the dosage form is retained in the fed mode. For example, the gastric retained dosage form can contain polymers with a high swelling capacity such as polyethylene oxide, hydroxyethylcellulose and hydroxypropylmethylcellulose. The polymers are preferably of a moderate to high molecular weight (4xl03 to greater that 107) to enhance swelling and provide control of the release of gabapentin. In one embodiment of the invention, a hydroxypropylmethylcellulose polymer of such molecular weight is utilized so that the viscosity of a 1% aqueous solution is about 4000 cps to greater than 100,000 cps. An example of suitable polyethylene oxide polymers are those having molecular weights (viscosity average) on the order of 2-7 million. A typical dosage form should swell to approximately 115% of its original volume within one hour after administration, and at a later time should swell to a volume that is 130% or more of the original volume. Fillers, binders, lubricants and other additives may also be included in the gastric retained dosage form, such as are well known to those of skill in the art.
A typical dosage form would provide for a drug delivery profile such that gabapentin both on an in vivo and in vitro basis, is delivered for at least 5 hours, and typically over a time period of about 8-10 hours. In order to provide for sustained delivery, it is preferable that at least 40wt% of gabapentin is retained in the dosage form after 1 hour, i.e., no more than 60wt% of the drug is administered in the first hour. In addition, it may be desired to utilize a dosage form that provides for substantially all of the gabapentin to be delivered over the intended duration, which is typically about 6-12 hours, where substantially all is taken to mean at least about 85wt% of the gabapentin is administered.
In one embodiment of the invention, the gastric retained dosage form of gabapentin is a capsule dosage form that allows for the extended release of gabapentin in the stomach and comprises: (a) at least one component that expands on contact with gastric juice and contains an agent capable of releasing carbon dioxide or nitrogen, gabapentin or a pharmaceutically acceptable salt thereof; (b) at least one hydrophilic membrane in the form of a sachet which contains component (a), expands by inflation, floats on the aqueous phase in the stomach and is permeable to gastric juice and; (c) capsule dosage form which
contains components (a) and (b) and which disintegrates without delay in the stomach under the action of gastric juice. Component (a) may also contain a pharmaceutically acceptable hydrophilic swelling agent such as lower alkyl ethers of cellulose, starches, water-soluble aliphatic or cyclic poly-N-vinylamides, polyvinyl alcohols, polyacrylates, polymethacrylates, polyethylene glycols and mixtures thereof, as well as other materials used in the manufacture of pharmaceutical dosage forms. Further details regarding an example of this type of dosage form can be found in Sinnreich, US Patent No. 4,996,058.
In another embodiment of the invention, the gastric retained dosage form of gabapentin is an extended release oral drug dosage form for releasing gabapentin into the stomach, duodenum and small intestine of a patient, and comprises: a single or a plurality of solid particles consisting of gabapentin or a pharmaceutically acceptable salt thereof dispersed within a polymer that (i) swells unrestrained dimensionally by imbibing water from gastric fluid to increase the size of the particles to promote gastric retention in the stomach of the patient in which the fed mode has been induced; (ii) gradually the gabapentin diffuses or the polymer erodes over a time period of hours, where the diffusion or erosion commences upon contact with the gastric fluid; and (iii) releases gabapentin to the stomach, duodenum and small intestine of the patient, as a result of the diffusion or polymeric erosion at a rate corresponding to the time period. Exemplary polymers include polyethylene oxides, alkyl substituted cellulose materials and combinations thereof, for example, high molecular weight polyethylene oxides and high molecular weight or viscosity hydroxypropylmethylcellulose materials. Further details regarding an example of this type of dosage form can be found in Shell, et al, US Patent No. 5,972,389 and Shell, et al., WO 9855107.
In yet another embodiment, a bi-layer tablet releases gabapentin to the upper gastrointestinal tract from an active containing layer, while the other layer is a swelling or floating layer. Details of this dosage may be found in Franz, et al., US Patent No. 5,232,704. This dosage form may be surrounded by a band of insoluble material as described by Wong, et al, US Patent No. 6,120,803.
Another embodiment of the invention uses a gastric retained swellable, sustained- release tablet having a matrix comprised of poly(ethylene oxide) and hydroxypropylmethylcellulose. This dosage form is illustrated in Example 1 and further details may be found in Gusler, et al., "Optimal Polymer Mixtures For Gastric Retentive
Tablets," filed on like date herewith and identified as Attorney Docket No. 15662- 001700US, the disclosure of which is incorporated herein by reference.
For those embodiments of the invention that include further administering additional therapeutic agents simultaneously with gabapentin, these agents can either be administered in the gastric retained dosage form that includes gabapentin or can be administered in a dosage form that is separate from gabapentin. Exemplary dosage forms are described below.
Dosage Form of Additional Agents For those embodiments of the invention that include further administering one or more additional therapeutic agents, such dosages can be any suitable formulation as are well known in the art. For those additional agents where controlled release is desirable, the agent may be incorporated in the gabapentin gastric retained dosage form or be administered in a separate gastric retained or other controlled release formulation dosage form. For those additional agents where immediate release is desirable, the agent may be incorporated in a coating around the gabapentin gastric retained dosage form or in a separate layer of a bilayer tablet, the agent may be simply enclosed in the capsule of the aforementioned gabapentin gastric retained capsule dosage form, or the agent may be administered in a separate immediate release dosage form. Typically, dosage forms contain the additional agent (another anti-epileptic or anticonvulsant agent) in combination with one or more pharmaceutically acceptable ingredients. The carrier may be in the form of a solid, semi-solid or liquid diluent, or a capsule. Usually the amount of active agent is about 0J-95wt%, more typically about 1- 50wt%. Actual methods of preparing such dosage forms are known, or will be apparent, to those skilled in this art; for example, see Remington's Pharmaceutical Sciences, Mack
Publishing Company, Easton, Pennsylvania, 18th Edition, 1990. The dosage form to be administered will, in any event, contain a quantity of the additional therapeutic agent(s) in an amount effective to alleviate the symptoms of the subject being treated.
In the preparation of pharmaceutical formulations containing the additional therapeutic agent in the form of dosage units for oral administration the agent may be mixed with solid, powdered ingredients, such as lactose, microcrystalline cellulose, maltodextrin, saccharose, sorbitol, mannitol, starch, amylopectin, cellulose derivatives, gelatin, or another
suitable ingredient, as well as with disintegrating agents and lubricating agents such as magnesium stearate, calcium stearate, sodium stearyl fumarate and polyethylene glycol waxes. The mixture is then processed into granules or pressed into tablets such as chewable and oral disintegrating tablets. Soft gelatin capsules may be prepared by mixing the active agent and vegetable oil, fat, or other suitable vehicle. Hard gelatin capsules may contain granules of the active agent, alone or in combination with solid powdered ingredients such as lactose, saccharose, sorbitol, mannitol, potato starch, corn starch, amylopectin, cellulose derivatives or gelatin. Liquid preparations for oral administration may be prepared in the form of syrups or suspensions, e.g. solutions or suspensions containing about 0.2-20wt% of the active agent and the remainder consisting of sugar or sugar alcohols and a mixture of ethanol, water, glycerol, propylene glycol and polyethylene glycol. If desired, such liquid preparations may contain coloring agents, flavoring agents, saccharin and carboxymethyl cellulose or other thickening agents. Liquid preparations for oral administration may also be prepared in the form of a dry powder to be reconstituted with a suitable solvent prior to use.
When the method of the invention includes administering another anti-epileptic or an anticonvulsant agent, there are numerous commercially available dosage forms that can be administered. In addition, other formulations can be readily designed based upon knowledge in the art, and include the gastric-retained delivery systems described above. Typical dosage forms of the other anti-epileptics or anticonvulsants suitable for use in the invention include tablets, capsules, oral suspensions and syrup. One of skill in the art can readily prepare one of these exemplary formulations or the other anti-epileptic can be administered by means of one of the numerous commercially available products, examples of which are provided below. Commercially available hydantoin anticonvulsants include, for example, Peganone®
(ethotoin, Abbott); Mesantoin® (mephenytoin, Sandoz); and Dilantin® (phenytoin, Warner- Lambert).
Typical dosage forms of the antineuralgics suitable for use in the invention include tablets, capsules and oral suspensions. One of skill in the art can readily prepare one of these exemplary formulations or the antineuralgic can be administered by means of one of the numerous commercially available products , examples of which are provided below.
Commercially available antineuralgics include, for example, Atretol® (carbamazepine, Elan).
Although specific examples of suitable anti-epileptic, anticonvulsant agent and antineuralgic formulations are described above, it is understood that the invention is not limited to those examples as there are numerous other formulations that can be used to deliver the other anti-epileptic or anticonvulsant agents.
The general methods of the invention are best understood with reference to the following examples which are intended to enable those skilled in the art to more clearly understand and to practice the present invention. These examples are not intended, nor are they to be construed, as limiting the scope of the invention, but are merely illustrative and representative thereof.
Example 1
Tablets were manufactured using a dry blend process, and hand made on a Carver 'Auto C Press (Fred Carver, Inc., Indiana). The dry blend process consisted of blending all of the ingredients in a plastic bag, and compressing into a 1000 mg tablet (600 mg gabapentin dose) using a 0J086" x 0.3937" Mod Oval die (Natoli Engineering). The parameters for the operation of the Carver 'Auto C Press were as follows: 4000 lbs. force, 0 second dwell time (the setting on the Carver Press), and 100% pump speed.
where: Active gabapentin
PEO Coagulant poly(ethylene oxide), grade PolyOx Coagulant, NF FP grade, manufactured by Union Carbide Dow Chemical
Company
Methocel K100M = hydroxypropylmethylcellulose, grade Methocel K100M, premium, manufactured by Dow Chemical Company M.St. = magnesium stearate, NF, supplied by Spectrum Chemical
Company The dissolution was determined in USP apparatus I (40 mesh baskets), 100 rpm, in deionized water. Samples, 5 ml at each time-point, were taken without media replacement at 1 , 4 and 8 hours.
The resulting cumulative dissolution profile, based upon a theoretical percent active added to the formulations is presented in tabulated form below:
Example 2
Tablets were manufactured using a dry blend process, and hand made on a Carver 'Auto C Press (Fred Carver, Inc., Indiana). The dry blend process consisted of blending all of the ingredients in a plastic bag, and compressing into a 600 mg tablet (300 mg gabapentin) using a 0.6299" x 0.3937" Mod Oval die (Natoli Engineering). The parameters for the operation of the Carver 'Auto C Press were as follows: -2000-2500 lbs. force, 0 second dwell time (the setting on the Carver Press), and 100% pump speed.
where: Active = gabapentin
PEO Coagulant = poly(ethylene oxide), grade PolyOx Coagulant, NF FP grade, manufactured by Union Carbide/Dow Chemical Company
Methocel K15M = hydroxypropylmethylcellulose, grade Methocel K15M, premium, manufacture by Dow Chemical Company
M.St. magnesium stearate, NF, supplied by Spectrum Chemical Company The dissolution was determined in USP apparatus I (40 mesh baskets), 100 rpm, in deionized water. Samples, 5 ml at each time-point, were taken without media replacement at 1, 2, 4 and 8 hours.
The resulting cumulative dissolution profile, based upon a theoretical percent active added to the formulations is presented in tabulated form below:
Example 3
Three Gastric Retentive (GR ) gabapentin formulas were manufactured utilizing a standard granulation technique. The formulations manufactured are shown in tabulated form below:
Gabapentin was obtained from Plantex U.S.A. (Englewood Cliffs, NJ). Methocel brand hydroxypropyl methylcellulose (also known as hypromellose), and Sentry® PolyOx® brand polyethylene oxide were obtained from Dow Chemical (Midland, Michigan). Methocel E5, premium is a USP type 2910 hydroxypropyl methylcellulose with number average molecular weight of on the order of 6000-8000 and a viscosity of 5 cps as a 2% aqueous solution at 20 °C. Methocel® K4M and Methocel® K15M are USP type 2208 hydroxypropyl methylcellulose with viscosities of 4000 cps and 15,000 cps, respectively, as a 2% aqueous solution at 20 °C, and number average molecular weights on the order of 80,000 and 100,000, respectively. Sentry® PolyOx® WSR 301, NF FP, Sentry® PolyOx® WSR Coagulant, NF FP and Sentry® PolyOx® WSR 303, NF FP have viscosity-average molecular weights of approximately 4,000,000, 5,000,000 and 7,000,000, respectively. Avicel PH-101, NF is microcrystalline cellulose supplied by FMC Corporation
(Philadelphia, PA). Magnesium stearate, NF was supplied by Spectrum Quality Products (New Brunswick, NJ).
The dissolution profiles, as determined by USP Apparatus I (lOOrpm) in modified simulated gastric fluid, for three prototypes GR formulations are shown in Figure 1 below.
Figure 1
Gabapentin GR Dissolution
0.0 2.0 4.0 6.0 8.0 10.0
Time, hours
Example 4 The pharmacokinetic profiles of the three formulations described in Example 3, administered as a 600-mg dose, were compared to Neurontin® immediate release 300-mg capsule in a randomized four-way cross-over experiment involving 15 healthy volunteers. Each subject was administered treatment of 600-mg gabapentin as one of the three GR™ formulations (1 X 600-mg tablet or 2 X 300-mg tablet) or Neurontin® capsules (2 X 300- mg) within 5 minutes of completing a high fat breakfast (FDA breakfast). Plasma samples were taken up to 48 hours post-dose. Figure 2 below illustrates the average plasma profile for the four treatments administered, and the pharmacokinetic data are summarized in tabulated form below.
Figure 2
Gabapentin Phase I - Average of 15 Subjects
Time post Dose, hours
Neurontin, 2 X 300-mg capsule -*- Gabapentin GR6, 2 X 300-mg Gabapentin GR8, 2 X 300-mg →— Gabapentin GR8, 1 X 600-mg
As demonstrated in Figure 2 and in tabulated form above, GR formulations demonstrate sustained release with a lower maximum plasma concentration and a larger value for the time of the maximum concentration compared to the immediate release capsules without loss in the bioavailability as measured by the plasma AUCjnf . Each of the patent applications, patents, publications, and other published documents mentioned or referred to in this specification is herein incorporated by reference in its entirety, to the same extent as if each individual patent application, patent, publication, and other published document was specifically and individually indicated to be incorporated by reference. While the present invention has been described with reference to the specific embodiments thereof, it should be understood by those skilled in the art that various changes may be made and equivalents may be substituted without departing from the true spirit and scope of the invention. In addition, many modifications may be made to adapt a particular situation, material, composition of matter, process, process step or steps, to the objective, spirit and scope of the present invention. All such modifications are intended to be within the scope of the claims appended hereto.
Claims (116)
1. A method of treating epilepsy comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form to a mammal in need of such treatment.
2. The method of Claim 1 wherein the dosage form is administered once-daily.
3. The method of Claim 2 wherein the dosage form is administered with a meal.
4. The method of Claim 1 wherein the dosage form is administered twice-daily.
5. The method of Claim 4 wherein each dosage form is administered with a meal.
6. The method of Claim 1 which further comprises administering one or more additional anti-epileptics or anticonvulsants.
7. The method of Claim 1 wherein the dosage form is administered once- or twice- daily and the total amount of gabapentin in the daily dosage is about 200-4000 mg.
8. The method of Claim 7 wherein the total amount of gabapentin in the daily dosage is about 600-2700 mg.
9. The method of Claim 8 wherein total amount of gabapentin in the daily dosage is about 900-1800 mg.
10. The method of Claim 1 wherein the dosage form is an extended release oral drug dosage form for releasing gabapentin into the stomach, duodenum and small intestine of the mammal.
11. The method of Claim 10 wherein gabapentin is administered from the dosage form for a period of at least 5 hours and at least 40wt% of the gabapentin is retained in the dosage form after 1 hour.
12. The method of Claim 11 wherein the dosage form provides administration of at least
80wt% of the gabapentin to be delivered over a period of about 5-12 hours.
13. The method of Claim 11 wherein the dosage form contains at least one hydrophilic polymer that swells to an extent such that it promotes gastric retention of the dosage form in the fed mode.
14. The method of Claim 13 wherein the polymer is selected from the group consisting 5 of polyethylene oxides, alkyl substituted cellulose materials, and combinations thereof.
15. The method of Claim 11 wherein the dosage form further comprises a gas generating agent.
16. The method of Claim 15 wherein the gabapentin is contained in a membrane sachet o with the gas generating agent.
17. The method of Claim 1 wherein the dosage form is an adhesive tablet.
18. The method of Claim 1 wherein the dosage form is a film coated dosage form or a capsule dosage form that allows for the extended release of gabapentin in the stomach duodenum and small intestine of the mammal. s
19. The method of Claim 1 wherein the dosage form is a swellable, sustained-release tablet having a matrix comprised of poly(ethylene oxide) and hydroxypropylmethylcellulose.
20. A method of treating neuropathic pain comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt thereof, in a o gastric retained dosage form to a mammal in need of such treatment.
21. The method of Claim 20 wherein the dosage form is administered once-daily.
22. The method of Claim 21 wherein the dosage form is administered with a meal.
23. The method of Claim 20 wherein the dosage form is administered twice-daily.
24. The method of Claim 23 wherein each dosage form is administered with a meal. 5
25. The method of Claim 20 which further comprises administering one or more therapeutic agents selected from the group consisting of anticonvulsants, tricyclic antidepressants, opioids, and levodopa.
26. The method of Claim 20 wherein the dosage form is administered once- or twice- daily and the total amount of gabapentin in the daily dosage is about 100-4800 mg.
27. The method of Claim 26 wherein the total amount of gabapentin in the daily dosage is about 300-3600 mg.
28. The method of Claim 27 wherein the total amount of gabapentin in the daily dosage is about 900-2400 mg.
29. The method of Claim 20 wherein the dosage form is an extended release oral drug dosage form for releasing gabapentin into the stomach, duodenum and small intestine of the mammal.
30. The method of Claim 29 wherein gabapentin is administered from the dosage form for a period of at least 5 hours and at least 40wt% of the gabapentin is retained in the dosage form after 1 hour.
31. The method of Claim 30 wherein the dosage form provides administration of at least 85wt% of the gabapentin to be delivered over a period of about 5-12 hours.
32. The method of Claim 30 wherein the dosage form contains at least one hydrophilic polymer that swells to an extent such that it promotes gastric retention of the dosage form in the fed mode.
33. The method of Claim 32 wherein the polymer is selected from the group consisting of polyethylene oxides, alkyl substituted cellulose materials, and combinations thereof.
34. The method of Claim 30 wherein the dosage form further comprises a gas generating agent.
35. The method of Claim 34 wherein the gabapentin is contained in a membrane sachet with the gas generating agent.
36. The method of Claim 20 wherein the dosage form is an adhesive tablet.
37. The method of Claim 20 wherein the dosage form is a film coated dosage form or a capsule dosage form that allows for the extended release of gabapentin in the stomach duodenum and small intestine of the mammal.
38. The method of Claim 20 wherein the dosage form is a swellable, sustained-release tablet having a matrix comprised of poly(ethylene oxide) and hydroxypropylmethylcellulose.
39. A method of treating psychiatric disorders comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form to a mammal in need of such treatment.
40. The method of Claim 39 wherein the psychiatric disorder is bipolar disorder or panic disorder.
41. The method of Claim 39 wherein the dosage form is administered once-daily,
42. The method of Claim 41 wherein the dosage form is administered with a meal.
43. The method of Claim 39 wherein the dosage form is administered twice-daily.
44. The method of Claim 43 wherein each dosage form is administered with a meal.
45. The method of Claim 39 which further comprises administering one or more therapeutic agents selected from the group consisting of anticonvulsants, tricyclic antidepressants, opioids, and levodopa.
46. The method of Claim 39 wherein the dosage form is administered once- or twice- daily and the total amount of gabapentin in the daily dosage is about 100-4800 mg.
47. The method of Claim 46 wherein the total amount of gabapentin in the daily dosage is about 900-3600 mg.
48. The method of Claim 39 wherein the dosage form is an extended release oral drug dosage form for releasing gabapentin into the stomach, duodenum and small intestine of the mammal.
49. The method of Claim 48 wherein gabapentin is administered from the dosage form for a period of at least 5 hours and at least 40wt% of the gabapentin is retained in the dosage form after 1 hour.
50. The method of Claim 49 wherein the dosage form provides administration of at least 85wt% of the gabapentin to be delivered over a period of about 5-12 hours.
51. The method of Claim 49 wherein the dosage form contains at least one hydrophilic polymer that swells to an extent such that it promotes gastric retention of the dosage form in the fed mode.
52. The method of Claim 51 wherein the polymer is selected from the group consisting 5 of polyethylene oxides, alkyl substituted cellulose materials, and combinations thereof.
53. The method of Claim 49 wherein the dosage form further comprises a gas generating agent.
54. The method of Claim 53 wherein the gabapentin is contained in a membrane sachet o with the gas generating agent.
55. The method of Claim 39 wherein the dosage form is an adhesive tablet.
56. The method of Claim 39 wherein the dosage form is a film coated dosage form or a capsule dosage form that allows for the extended release of gabapentin in the stomach. s
57. The method of Claim 39 wherein the dosage form is a swellable, sustained-release tablet having a matrix comprised of poly(ethylene oxide) and hydroxypropylmethylcellulose.
58. A method of treating movement disorders comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt o thereof, in a gastric retained dosage form to a mammal in need of such treatment.
59. The method of Claim 58 wherein the movement disorder is restless leg syndrome, periodic movement disorder of sleep, essential tremor or acquired nystagmus.
60. The method of Claim 58 wherein the dosage form is administered once-daily.
61. The method of Claim 60 wherein the dosage form is administered with a meal. 5
62. The method of Claim 58 wherein the dosage form is administered twice-daily.
63. The method of Claim 62 wherein each dosage form is administered with a meal.
64. The method of Claim 58 which further comprises administering one or more therapeutic agents selected from the group consisting of anticonvulsants, tricyclic antidepressants, opioids, benzodiazepine, and dopaminergic agents.
65. The method of Claim 58 wherein the dosage form is administered once- or twice-
5 daily and the total amount of gabapentin in the daily dosage is about 100-4000 mg.
66. The method of Claim 65 wherein the total amount of gabapentin in the daily dosage is about 200-3000 mg.
67. The method of Claim 66 wherein the total amount of gabapentin in the daily dosage is about 500-2700 mg. o
68. The method of Claim 58 wherein the dosage form is an extended release oral drug dosage form for releasing gabapentin into the stomach, duodenum and small intestine of the mammal.
69. The method of Claim 68 wherein gabapentin is administered from the dosage form for a period of at least 5 hours and at least 40wt% of the gabapentin is retained in the 5 dosage form after 1 hour.
70. The method of Claim 69 wherein the dosage form provides administration of at least 80wt% of the gabapentin to be delivered over a period of about 5-12 hours.
71. The method of Claim 69 wherein the dosage form contains a hydrophilic polymer that swells to a size such that the dosage form is retained in the fed mode. o
72. The method of Claim 71 wherein the polymer is selected from the group consisting of polyethylene oxides, alkyl substituted cellulose materials, and combinations thereof.
73. The method of Claim 69 wherein the dosage form further comprises a gas generating agent. 5
74. The method of Claim 73 wherein the gabapentin is contained in a membrane sachet with the gas generating agent.
75. The method of Claim 58 wherein the dosage form is an adhesive tablet.
76. The method of Claim 58 wherein the dosage form is a film coated dosage form or a capsule dosage form that allows for the extended release of gabapentin in the stomach.
77. The method of Claim 58 wherein the dosage form is a swellable, sustained-release tablet having a matrix comprised of poly(ethylene oxide) and hydroxypropylmethylcellulose.
78. A method for the prophylactic treatment of migraine headaches comprising administering a therapeutically effective amount of gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form to a mammal in need of such treatment.
79. The method of Claim 78 wherein the dosage form is administered once-daily.
80. The method of Claim 79 wherein the dosage form is administered with a meal.
81. The method of Claim 78 wherein the dosage form is administered twice-daily.
82. The method of Claim 81 wherein each dosage form is administered with a meal.
83. The method of Claim 78 which further comprises administering one or more therapeutic agents selected from the group consisting of anticonvulsants, tricyclic antidepressants, opioids, and levodopa.
84. The method of Claim 78 wherein the dosage form is administered once- or twice- daily and the total amount of gabapentin in the daily dosage is about 200-4000 mg.
85. The method of Claim 84 wherein the total amount of gabapentin in the daily dosage is about 500-3600 mg.
86. The method of Claim 85 wherein the total amount of gabapentin in the daily dosage is about 900-2400 mg.
87. The method of Claim 78 wherein the dosage form is an extended release oral drug dosage form for releasing gabapentin into the stomach, duodenum and small intestine of the mammal.
88. The method of Claim 87 wherein gabapentin is administered from the dosage form for a period of at least 5 hours and at least 40wt% of the gabapentin is retained in the dosage form after 1 hour.
89. The method of Claim 88 wherein the dosage form provides administration of at least 5 85wt% of the gabapentin to be delivered over a period of about 5-12 hours.
90. The method of Claim 88 wherein the dosage form contains at least one hydrophilic polymer that swells to an extent such that it promotes gastric retention of the dosage form in the fed mode.
91. The method of Claim 90 wherein the polymer is selected from the group consisting o of polyethylene oxides, alkyl substituted cellulose materials, and combinations thereof.
92. The method of Claim 88 wherein the dosage form further comprises a gas generating agent.
93. The method of Claim 92 wherein the gabapentin is contained in a membrane sachet s with the gas generating agent.
94. The method of Claim 78 wherein the dosage form is an adhesive tablet.
95. The method of Claim 78 wherein the dosage form is a film coated dosage form or a capsule dosage form that allows for the extended release of gabapentin in the stomach duodenum and small intestine of the mammal. o
96. The method of Claim 78 wherein the dosage form is a swellable, sustained-release tablet having a matrix comprised of poly(ethylene oxide) and hydroxypropylmethylcellulose.
97. An improved method of administering a therapeutically effective amount of gabapentin to a patient in need thereof, the improvement comprising administering 5 gabapentin or a pharmaceutically acceptable salt thereof, in a gastric retained dosage form.
98. The method of Claim 97 wherein the dosage form is administered once-daily.
99. The method of Claim 98 wherein the dosage form is administered with a meal.
100. The method of Claim 97 wherein the dosage form is administered twice-daily.
101. The method of Claim 100 wherein each dosage form is administered with a meal.
102. The method of Claim 97 where the patient is being treated for epilepsy.
103. The method of Claim 97 where the patient is being treated for neuropathic pain.
5 104. The method of Claim 97 where the patient is being treated for psychiatric disorders.
105. The method of Claim 97 where the patient is being treated for movement disorders.
106. The method of Claim 97 where the patient is receiving prophylactic treatment for migraine headaches.
107. The method of Claim 97 wherein the dosage form is an extended release oral drug o dosage form for releasing gabapentin into the stomach, duodenum and small intestine of the mammal.
108. The method of Claim 107 wherein gabapentin is administered from the dosage form for a period of at least 5 hours and at least 40wt% of the gabapentin is retained in the dosage form after 1 hour. s
109. The method of Claim 108 wherein the dosage form provides administration of at least 80wt% of the gabapentin to be delivered over a period of about 5-12 hours.
110. The method of Claim 108 wherein the dosage form contains at least one hydrophilic polymer that swells to an extent such that it promotes gastric retention of the dosage form in the fed mode. o
111. The method of Claim 1 10 wherein the polymer is selected from the group consisting of polyethylene oxides, alkyl substituted cellulose materials, and combinations thereof.
112. The method of Claim 108 wherein the dosage form further comprises a gas generating agent. 5
113. The method of Claim 1 12 wherein the gabapentin is contained in a membrane sachet with the gas generating agent.
114. The method of Claim 97 wherein the dosage form is an adhesive tablet.
115. The method of Claim 97 wherein the dosage form is a film coated dosage form or a capsule dosage form that allows for the extended release of gabapentin in the stomach.
116. The method of Claim 97 wherein the dosage form is a swellable, sustained-release tablet having a matrix comprised of poly(ethylene oxide) and hydroxypropyl methylcellulose.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US33524801P | 2001-10-25 | 2001-10-25 | |
US60/335,248 | 2001-10-25 | ||
PCT/IB2002/005440 WO2003035040A1 (en) | 2001-10-25 | 2002-10-25 | Methods of treatment using a gastric retained gabapentin dosage |
Publications (2)
Publication Number | Publication Date |
---|---|
AU2002348828A1 true AU2002348828A1 (en) | 2003-07-03 |
AU2002348828B2 AU2002348828B2 (en) | 2007-12-20 |
Family
ID=23310919
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AU2002348828A Ceased AU2002348828B2 (en) | 2001-10-25 | 2002-10-25 | Methods of treatment using a gastric retained gabapentin dosage |
Country Status (9)
Country | Link |
---|---|
US (10) | US7438927B2 (en) |
EP (2) | EP1439825B2 (en) |
JP (2) | JP5421511B2 (en) |
AU (1) | AU2002348828B2 (en) |
CA (1) | CA2464322C (en) |
DK (1) | DK1439825T4 (en) |
MX (1) | MXPA04003946A (en) |
TW (1) | TWI312285B (en) |
WO (1) | WO2003035040A1 (en) |
Families Citing this family (140)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7056531B1 (en) * | 2000-05-04 | 2006-06-06 | Nature's Way Products, Inc. | Sustained release compositions for orally administered substances and methods |
NZ567711A (en) * | 2001-06-11 | 2009-10-30 | Xenoport Inc | Orally administered dosage forms of GABA analog prodrugs having reduced toxicity |
US8048917B2 (en) | 2005-04-06 | 2011-11-01 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
TWI312285B (en) | 2001-10-25 | 2009-07-21 | Depomed Inc | Methods of treatment using a gastric retained gabapentin dosage |
US20030091630A1 (en) * | 2001-10-25 | 2003-05-15 | Jenny Louie-Helm | Formulation of an erodible, gastric retentive oral dosage form using in vitro disintegration test data |
US7612112B2 (en) * | 2001-10-25 | 2009-11-03 | Depomed, Inc. | Methods of treatment using a gastric retained gabapentin dosage |
US20070184104A1 (en) * | 2001-10-25 | 2007-08-09 | Depomed, Inc. | Gastric retentive gabapentin dosage forms and methods for using same |
US20060159743A1 (en) * | 2001-10-25 | 2006-07-20 | Depomed, Inc. | Methods of treating non-nociceptive pain states with gastric retentive gabapentin |
US20030152622A1 (en) * | 2001-10-25 | 2003-08-14 | Jenny Louie-Helm | Formulation of an erodible, gastric retentive oral diuretic |
US7939102B2 (en) * | 2002-06-07 | 2011-05-10 | Torrent Pharmaceuticals Ltd. | Controlled release formulation of lamotrigine |
CN1668284A (en) * | 2002-06-07 | 2005-09-14 | 兰贝克赛实验室有限公司 | Sustained release oral dosage forms of gabapentin |
US7776314B2 (en) | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
KR20050111318A (en) | 2003-01-13 | 2005-11-24 | 다이노젠 파마세우티컬스, 인코포레이티드 | Method of treating functional bowel disorders |
CN1832735A (en) * | 2003-07-29 | 2006-09-13 | 兰贝克赛实验室有限公司 | New dosage regimen in case of concurrent intake of gabapentin with food and an increased oral bioavailability therewith |
DE102004020220A1 (en) * | 2004-04-22 | 2005-11-10 | Grünenthal GmbH | Process for the preparation of a secured against misuse, solid dosage form |
DE102004032051A1 (en) * | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Process for the preparation of a secured against misuse, solid dosage form |
US20070048228A1 (en) * | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
US8075872B2 (en) | 2003-08-06 | 2011-12-13 | Gruenenthal Gmbh | Abuse-proofed dosage form |
DE10336400A1 (en) * | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Anti-abuse dosage form |
DE102005005446A1 (en) * | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Break-resistant dosage forms with sustained release |
DE10361596A1 (en) * | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Process for producing an anti-abuse dosage form |
PT1842533E (en) * | 2003-08-06 | 2013-05-17 | Gruenenthal Gmbh | Dosage form that is secured against misuse |
ITMI20032399A1 (en) * | 2003-12-09 | 2005-06-10 | Zambon Spa | PHARMACEUTICAL COMPOSITION CONTAINING GABAPENTIN. |
CN1921839A (en) * | 2004-01-19 | 2007-02-28 | 兰贝克赛实验室有限公司 | Stable sustained-release oral dosage forms of gabapentin and process for preparation thereof |
GB0405200D0 (en) * | 2004-03-08 | 2004-04-21 | Pfizer Ltd | Combinations comprising alpha-2-delta ligands |
GB0408308D0 (en) * | 2004-04-14 | 2004-05-19 | Vectura Ltd | Pharmaceutical compositions |
US7427601B2 (en) * | 2004-06-24 | 2008-09-23 | Schwarz Pharma Ag | Method for treating tremor |
DE102004032049A1 (en) * | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Anti-abuse, oral dosage form |
EP1791599A1 (en) * | 2004-09-07 | 2007-06-06 | Pfizer Limited | Combination of a 5-ht(1) receptor agonist and an alpha-2-delta ligand for the treatment of migraine |
US8252321B2 (en) | 2004-09-13 | 2012-08-28 | Chrono Therapeutics, Inc. | Biosynchronous transdermal drug delivery for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and the treatment of hyperglycemia, alzheimer's disease, sleep disorders, parkinson's disease, aids, epilepsy, attention deficit disorder, nicotine addiction, cancer, headache and pain control, asthma, angina, hypertension, depression, cold, flu and the like |
EP1802258A4 (en) | 2004-09-13 | 2015-09-23 | Chrono Therapeutics Inc | Biosynchronous transdermal drug delivery |
KR101228399B1 (en) | 2004-11-04 | 2013-01-31 | 제노포트 인코포레이티드 | Gabapentin prodrug sustained release oral dosage forms |
DE102005005449A1 (en) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Process for producing an anti-abuse dosage form |
JP2008536928A (en) * | 2005-04-19 | 2008-09-11 | アルザ・コーポレーシヨン | A combination of tramadol and a substance comprising gabapentin |
AU2006329564A1 (en) | 2005-07-11 | 2007-07-05 | Pharmena North America Inc. | Formulations for treatment of lipoprotein abnormalities comprising a statin a statin and a methylnicotinamide derivative |
US20070092565A1 (en) * | 2005-10-25 | 2007-04-26 | Pharmascience Inc. | Gastric retention drug delivery system |
NL2000281C2 (en) | 2005-11-02 | 2007-08-07 | Pfizer Prod Inc | Solid pharmaceutical compositions containing pregabalin. |
EP1976503A2 (en) * | 2005-12-29 | 2008-10-08 | Depomed, Inc. | Gastric retentive gabapentin dosage forms and methods for using same |
US20090176882A1 (en) * | 2008-12-09 | 2009-07-09 | Depomed, Inc. | Gastric retentive gabapentin dosage forms and methods for using same |
DE102007011485A1 (en) * | 2007-03-07 | 2008-09-11 | Grünenthal GmbH | Dosage form with more difficult abuse |
CA2682661C (en) | 2007-03-22 | 2017-03-14 | Dendreon Corporation | Methods for inducing a natural killer (nk) cell-mediated immune response and for increasing nk cell activity |
AU2009207796B2 (en) | 2008-01-25 | 2014-03-27 | Grunenthal Gmbh | Pharmaceutical dosage form |
WO2009102734A1 (en) * | 2008-02-11 | 2009-08-20 | Depomed Inc. | Methods for treating vasomotor symptoms using gaba analogs in a gastric retentive dosage form |
AU2009223061B2 (en) | 2008-03-11 | 2014-10-09 | Depomed Inc. | Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic |
US8372432B2 (en) | 2008-03-11 | 2013-02-12 | Depomed, Inc. | Gastric retentive extended-release dosage forms comprising combinations of a non-opioid analgesic and an opioid analgesic |
SG176464A1 (en) * | 2008-05-09 | 2011-12-29 | Agency Science Tech & Res | Diagnosis and treatment of kawasaki disease |
ES2599031T3 (en) * | 2008-05-09 | 2017-01-31 | Grünenthal GmbH | Process for the preparation of an intermediate powder formulation and a final solid dosage form using a spray freezing step |
MX340249B (en) | 2008-08-15 | 2016-07-01 | Depomed Inc | Gastric retentive pharmaceutical compositions for treatment and prevention of cns disorders. |
WO2010129686A1 (en) | 2009-05-05 | 2010-11-11 | Vapogenix, Inc. | Novel formulations of volatile anesthetics and methods of use for reducing inflammation |
PT2456424E (en) * | 2009-07-22 | 2013-09-30 | Gruenenthal Gmbh | Oxidation-stabilized tamper-resistant dosage form |
NZ596667A (en) | 2009-07-22 | 2013-09-27 | Gruenenthal Chemie | Hot-melt extruded controlled release dosage form |
JP2013505248A (en) * | 2009-09-16 | 2013-02-14 | アラーガン インコーポレイテッド | Compositions and methods for treating seizure disorders |
US20110135728A1 (en) * | 2009-12-08 | 2011-06-09 | Miller Jennifer L | Gastric retentive pharmaceutical compositions for extended release of polypeptides |
US8597681B2 (en) | 2009-12-22 | 2013-12-03 | Mallinckrodt Llc | Methods of producing stabilized solid dosage pharmaceutical compositions containing morphinans |
US9198861B2 (en) | 2009-12-22 | 2015-12-01 | Mallinckrodt Llc | Methods of producing stabilized solid dosage pharmaceutical compositions containing morphinans |
EP2555756B1 (en) * | 2010-04-07 | 2018-08-22 | Lupin Limited | Controlled release pharmaceutical compositions of tapentadol |
WO2011151708A1 (en) | 2010-06-01 | 2011-12-08 | Rubicon Research Private Limited | Gastroretentive dosage forms of gaba analogs |
US20120009261A1 (en) * | 2010-07-06 | 2012-01-12 | Grünenthal GmbH | Novel gastro-retentive dosage forms |
EP2603215A4 (en) | 2010-08-11 | 2015-08-05 | Philadelphia Health & Educatio | Novel d3 dopamine receptor agonists to treat dyskinesia in parkinson's disease |
CA2808541C (en) | 2010-09-02 | 2019-01-08 | Gruenenthal Gmbh | Tamper resistant dosage form comprising an anionic polymer |
MX2013002377A (en) | 2010-09-02 | 2013-04-29 | Gruenenthal Gmbh | Tamper resistant dosage form comprising inorganic salt. |
EP2648754A4 (en) | 2010-12-07 | 2016-02-24 | Philadelphia Health & Educatio | Methods of inhibiting metastasis from cancer |
US8476221B2 (en) | 2011-03-18 | 2013-07-02 | Halimed Pharmaceuticals, Inc. | Methods and compositions for the treatment of metabolic disorders |
US8658631B1 (en) | 2011-05-17 | 2014-02-25 | Mallinckrodt Llc | Combination composition comprising oxycodone and acetaminophen for rapid onset and extended duration of analgesia |
US8858963B1 (en) | 2011-05-17 | 2014-10-14 | Mallinckrodt Llc | Tamper resistant composition comprising hydrocodone and acetaminophen for rapid onset and extended duration of analgesia |
US8741885B1 (en) | 2011-05-17 | 2014-06-03 | Mallinckrodt Llc | Gastric retentive extended release pharmaceutical compositions |
CA2841785A1 (en) | 2011-07-06 | 2013-01-10 | The Parkinson's Institute | Compositions and methods for treatment of symptoms in parkinson's disease patients |
AR087360A1 (en) | 2011-07-29 | 2014-03-19 | Gruenenthal Gmbh | PROOF OF HANDLING TABLET PROVIDING IMMEDIATE RELEASE OF PHARMACY |
MX348054B (en) | 2011-07-29 | 2017-05-25 | Gruenenthal Gmbh | Tamper-resistant tablet providing immediate drug release. |
US20130143867A1 (en) | 2011-12-02 | 2013-06-06 | Sychroneuron Inc. | Acamprosate formulations, methods of using the same, and combinations comprising the same |
TWI519515B (en) | 2011-12-21 | 2016-02-01 | 諾維拉治療公司 | Hepatitis b antiviral agents |
AU2013225106B2 (en) | 2012-02-28 | 2017-11-02 | Grunenthal Gmbh | Tamper-resistant dosage form comprising pharmacologically active compound and anionic polymer |
RS57913B1 (en) | 2012-04-18 | 2019-01-31 | Gruenenthal Gmbh | Tamper resistant and dose-dumping resistant pharmaceutical dosage form |
US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
CA2879454A1 (en) | 2012-07-19 | 2014-01-23 | Drexel University | Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same |
EP2950790A4 (en) | 2012-08-09 | 2018-04-25 | Dynamis Therapeutics, Inc. | Methods for maintaining or improving health, well-being and/or a physiological function in a subject |
EP2698144A1 (en) | 2012-08-12 | 2014-02-19 | Ali Raif Ilaç Sanayi ve Ticaret Anonim Sirketi | Prolonged release gabapentin tablet formulation whose ability to stay in the stomach is improved |
MX2015008773A (en) | 2013-01-07 | 2015-11-06 | Univ Pennsylvania | Compositions and methods for treating cutaneous t cell lymphoma. |
JP6466417B2 (en) | 2013-05-29 | 2019-02-06 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | A tamper-resistant dosage form with a bimodal release profile |
JP6445537B2 (en) | 2013-05-29 | 2018-12-26 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | Tamper-resistant dosage forms containing one or more particles |
WO2014197744A1 (en) | 2013-06-05 | 2014-12-11 | Synchroneuron, Inc. | Acamprosate formulations, methods of using the same, and combinations comprising the same |
RU2673737C2 (en) | 2013-07-02 | 2018-11-29 | ЭКОПЛЭНЕТ ЭНВАЙРОНМЕНТАЛ, ЭлЭлСи | Volatile organic compound formulations having antimicrobial activity |
GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
JP6449871B2 (en) | 2013-07-12 | 2019-01-09 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | Anti-modified dosage form containing ethylene-vinyl acetate polymer |
BR112016010482B1 (en) | 2013-11-26 | 2022-11-16 | Grünenthal GmbH | PREPARATION OF A PHARMACEUTICAL COMPOSITION IN POWDER BY MEANS OF CRYOMING |
EP3074049B1 (en) | 2013-11-26 | 2020-05-06 | Yale University | Novel cell-penetrating compositions and methods using same |
US10258615B2 (en) | 2013-12-09 | 2019-04-16 | Thomas Jefferson University | Methods of treating a neurodegenerative disease in a mammal in need thereof |
US9982010B2 (en) | 2014-04-07 | 2018-05-29 | Women & Infants Hospital Of Rhode Island | 7-dehydrocholesterol derivatives and methods using same |
WO2015173195A1 (en) | 2014-05-12 | 2015-11-19 | Grünenthal GmbH | Tamper resistant immediate release capsule formulation comprising tapentadol |
JP2017516789A (en) | 2014-05-26 | 2017-06-22 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | Multiparticulates protected against ethanol overdose |
US10624917B2 (en) | 2014-08-20 | 2020-04-21 | Yale University | Compositions and methods useful for treating or preventing liver diseases or disorders, and promoting weight loss |
AU2016211330A1 (en) | 2015-01-28 | 2017-08-03 | Chrono Therapeutics Inc. | Drug delivery methods and systems |
US10679516B2 (en) | 2015-03-12 | 2020-06-09 | Morningside Venture Investments Limited | Craving input and support system |
EA035434B1 (en) | 2015-04-24 | 2020-06-15 | Грюненталь Гмбх | Tamper-resistant dosage form with immediate release and resistance against solvent extraction |
WO2016182968A1 (en) | 2015-05-08 | 2016-11-17 | Brown University | Novel syringolin analogues and methods of making and using same |
JP6995627B2 (en) | 2015-05-19 | 2022-02-04 | イエール ユニバーシティ | Compositions for treating pathological calcification conditions and methods of using them |
WO2016201288A1 (en) | 2015-06-12 | 2016-12-15 | Brown University | Novel antibacterial compounds and methods of making and using same |
NO346258B1 (en) | 2015-06-30 | 2022-05-16 | Neurad Ltd | Novel breathing control modulating compounds, and methods of making and using same |
US10842750B2 (en) | 2015-09-10 | 2020-11-24 | Grünenthal GmbH | Protecting oral overdose with abuse deterrent immediate release formulations |
WO2017075145A1 (en) | 2015-10-28 | 2017-05-04 | Yale University | Quinoline amides and methods of using same |
CA3005142A1 (en) | 2015-11-20 | 2017-05-26 | Yale University | Compositions for treating ectopic calcification disorders, and methods using same |
US10292977B2 (en) | 2016-04-11 | 2019-05-21 | Neurocea, LLC | Compositions and methods for treatment related to fall and fall frequency in neurodegenerative diseases |
US10143687B2 (en) | 2016-04-11 | 2018-12-04 | Neurocea, LLC | Compositions and methods for treatment related to fall and fall frequency in neurodegenerative diseases |
WO2017190001A1 (en) | 2016-04-29 | 2017-11-02 | The Regents Of The University Of Colorado, A Body Corporate | Compounds and compositions useful for treating metabolic syndrome, and methods using same |
EP3484456A4 (en) | 2016-07-17 | 2020-03-18 | Mapi Pharma Limited | Extended release dosage forms of pregabalin |
US20210330599A1 (en) | 2016-08-01 | 2021-10-28 | University Of Rochester | Nanoparticles for Controlled Release of Anti-Biofilm Agents and Methods of Use |
US11390859B2 (en) | 2016-08-05 | 2022-07-19 | Yale University | Compositions and methods for stroke prevention in pediatric sickle cell anemia patients |
WO2018045229A1 (en) | 2016-09-01 | 2018-03-08 | Mebias Discovery Llc | Substituted ureas and methods of making and using same |
CN110114071B (en) | 2016-11-07 | 2023-07-04 | 爱彼特生物制药公司 | Tricyclic compounds containing substituted pyridones and methods of using the same |
WO2018129304A1 (en) | 2017-01-06 | 2018-07-12 | Chrono Therapeutics Inc. | Transdermal drug delivery devices and methods |
WO2018136766A1 (en) | 2017-01-19 | 2018-07-26 | Temple University-Of The Commonwealth System Of Higher Education | Novel bridged bicycloalkyl-substituted aminothizoles and their methods of use |
WO2018172852A1 (en) | 2017-03-21 | 2018-09-27 | Arbutus Biopharma Corporation | Substituted dihydroindene-4-carboxamides and analogs thereof, and methods using same |
JP7108018B2 (en) | 2017-04-17 | 2022-07-27 | イエール ユニバーシティ | Compounds, compositions and methods for treating or preventing acute lung injury |
US20210085796A1 (en) | 2017-07-28 | 2021-03-25 | Yale University | Anticancer drugs and methods of making and using same |
US11426409B2 (en) | 2017-09-08 | 2022-08-30 | The Regents Of The University Of Colorado | Compounds, compositions and methods for treating or preventing HER-driven drug-resistant cancers |
CN111818929A (en) | 2017-11-27 | 2020-10-23 | 由卫生与公众服务部部长代表的美利坚合众国 | Compounds, compositions and methods for treating and/or preventing periodontal disease |
WO2019125184A1 (en) | 2017-12-19 | 2019-06-27 | Auckland Uniservices Limited | Use of biomarker in cancer therapy |
CA3089236A1 (en) | 2018-01-24 | 2019-08-01 | The Rockefeller University | Antibacterial compounds, compositions thereof, and methods using same |
CN111902137A (en) | 2018-01-29 | 2020-11-06 | 杜克大学 | Compositions and methods for enhancing the bioavailability of 5-hydroxytryptophan |
US11091473B2 (en) | 2018-05-29 | 2021-08-17 | Acadia Pharmaceuticals Inc. | Compounds for pain treatment, compositions comprising same, and methods of using same |
EP3801732A4 (en) | 2018-05-29 | 2022-04-27 | Morningside Venture Investments Limited | Drug delivery methods and systems |
JP2021529158A (en) | 2018-06-19 | 2021-10-28 | ナショナル ユニバーシティー オブ シンガポールNational University of Singapore | Formulation of 5-hydroxytryptophan to improve bioavailability for various indications |
KR20240042554A (en) | 2018-10-11 | 2024-04-02 | 사니핏 테라퓨틱스 에스.에이. | Inositol phosphates for the treatment of ectopic calcification |
TWI827760B (en) | 2018-12-12 | 2024-01-01 | 加拿大商愛彼特生物製藥公司 | Substituted arylmethylureas and heteroarylmethylureas, analogues thereof, and methods using same |
BR112021014897A2 (en) | 2019-01-30 | 2021-09-28 | Sanifit Therapeutics, S.A. | COMPOUND OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND, PHARMACEUTICAL COMPOSITION |
WO2020159565A1 (en) | 2019-02-01 | 2020-08-06 | Cersci Therapeutics, Inc. | Methods of treating post-surgical pain with a thiazoline anti-hyperalgesic agent |
US20200246317A1 (en) | 2019-02-01 | 2020-08-06 | Cersci Therapeutics, Inc. | Methods of treating diabetic neuropathy with a thiazoline anti-hyperalgesic agent |
WO2020227603A1 (en) | 2019-05-09 | 2020-11-12 | The Feinstein Institutes For Medical Research | Hmgb1 antagonist |
US11555010B2 (en) | 2019-07-25 | 2023-01-17 | Brown University | Diamide antimicrobial agents |
EP3818983A1 (en) | 2019-11-11 | 2021-05-12 | Sanifit Therapeutics S.A. | Inositol phosphate compounds for use in treating, inhibiting the progression, or preventing cardiovascular calcification |
WO2021127456A1 (en) | 2019-12-19 | 2021-06-24 | Rain Therapeutics Inc. | Methods of inhibiting epidermal growth factor receptor proteins |
CA3181983A1 (en) | 2020-06-09 | 2021-12-16 | Zhiliang Cheng | Soluble enpp1 or enpp3 proteins and uses thereof |
EP4015494A1 (en) | 2020-12-15 | 2022-06-22 | Sanifit Therapeutics S.A. | Processes for the preparation of soluble salts of inositol phosphates |
EP4036097A1 (en) | 2021-01-29 | 2022-08-03 | Sanifit Therapeutics S.A. | Ip4-4,6 substituted derivative compounds |
CN116801868A (en) | 2021-07-30 | 2023-09-22 | 埃维西亚治疗公司 | Gastric retention dosage form of 5-hydroxytryptophan |
US11779567B2 (en) | 2021-10-14 | 2023-10-10 | Evecxia Therapeutics, Inc. | Method for optimizing 5-hydroxytryptamine function in the brain for therapeutic purposes |
WO2024023360A1 (en) | 2022-07-29 | 2024-02-01 | Sanifit Therapeutics, S.A. | Ip5 substituted compounds |
WO2024023359A1 (en) | 2022-07-29 | 2024-02-01 | Sanifit Therapeutics, S.A. | Ip4-4,6 substituted derivative compounds for use in the treatment, inhibition of progression, and prevention of ectopic calcification |
WO2024052895A1 (en) | 2022-09-06 | 2024-03-14 | Hadasit Medical Research Services And Development Ltd | Combinations comprising psychedelics for the treatment of schizophrenia and other neuropsychiatric and neurologic disorders |
Family Cites Families (122)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US12679A (en) * | 1855-04-10 | phdto-litho | ||
US43946A (en) * | 1864-08-23 | Improvement in hay-elevating forks | ||
US3574820A (en) | 1968-01-08 | 1971-04-13 | Upjohn Co | Medicinal dosage forms of unpolymerized thiolated gelatin with a cross-linking accelerating agent providing slowly released medication from a swollen matrix |
US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
DE2460891C2 (en) * | 1974-12-21 | 1982-09-23 | Gödecke AG, 1000 Berlin | 1-aminomethyl-1-cycloalkaneacetic acids and their esters, processes for their preparation and medicaments containing these compounds |
US4087544A (en) * | 1974-12-21 | 1978-05-02 | Warner-Lambert Company | Treatment of cranial dysfunctions using novel cyclic amino acids |
US3977404A (en) | 1975-09-08 | 1976-08-31 | Alza Corporation | Osmotic device having microporous reservoir |
DE2611690A1 (en) * | 1976-03-19 | 1977-09-22 | Goedecke Ag | CYCLIC SULFONYLOXYIMIDE |
CA1146866A (en) | 1979-07-05 | 1983-05-24 | Yamanouchi Pharmaceutical Co. Ltd. | Process for the production of sustained release pharmaceutical composition of solid medical material |
US4309406A (en) | 1979-07-10 | 1982-01-05 | American Home Products Corporation | Sustained release pharmaceutical compositions |
US4612008A (en) | 1983-05-11 | 1986-09-16 | Alza Corporation | Osmotic device with dual thermodynamic activity |
US4462839A (en) | 1983-06-16 | 1984-07-31 | Fmc Corporation | Enteric coating for pharmaceutical dosage forms |
US4753801A (en) | 1985-10-25 | 1988-06-28 | Eli Lilly And Company | Sustained release tablets |
GB8613689D0 (en) | 1986-06-05 | 1986-07-09 | Euro Celtique Sa | Pharmaceutical composition |
US4851232A (en) | 1987-02-13 | 1989-07-25 | Alza Corporation | Drug delivery system with means for obtaining desirable in vivo release rate pattern |
US4786503A (en) | 1987-04-06 | 1988-11-22 | Alza Corporation | Dosage form comprising parallel lamine |
IL87710A (en) | 1987-09-18 | 1992-06-21 | Ciba Geigy Ag | Covered floating retard form for controlled release in gastric juice |
US4894476A (en) * | 1988-05-02 | 1990-01-16 | Warner-Lambert Company | Gabapentin monohydrate and a process for producing the same |
US5002772A (en) | 1988-05-31 | 1991-03-26 | Pfizer Inc. | Gastric retention system for controlled drug release |
US5007790A (en) | 1989-04-11 | 1991-04-16 | Depomed Systems, Inc. | Sustained-release oral drug dosage form |
DE3928183A1 (en) * | 1989-08-25 | 1991-02-28 | Goedecke Ag | LACTAM-FREE CYCLIC AMINO ACIDS |
US5084479A (en) * | 1990-01-02 | 1992-01-28 | Warner-Lambert Company | Novel methods for treating neurodegenerative diseases |
EP0458751A1 (en) | 1990-05-25 | 1991-11-27 | Warner-Lambert Company | Delivery system for cyclic amino acids with improved taste, texture and compressibility |
IT1250483B (en) | 1990-08-30 | 1995-04-07 | Eurand Int | MULTIPLE DIE DELAY SYSTEM |
US5827819A (en) * | 1990-11-01 | 1998-10-27 | Oregon Health Sciences University | Covalent polar lipid conjugates with neurologically active compounds for targeting |
US5232704A (en) | 1990-12-19 | 1993-08-03 | G. D. Searle & Co. | Sustained release, bilayer buoyant dosage form |
US5273758A (en) | 1991-03-18 | 1993-12-28 | Sandoz Ltd. | Directly compressible polyethylene oxide vehicle for preparing therapeutic dosage forms |
US5582837A (en) * | 1992-03-25 | 1996-12-10 | Depomed, Inc. | Alkyl-substituted cellulose-based sustained-release oral drug dosage forms |
DE69322077T2 (en) | 1992-03-25 | 1999-04-08 | Depomed Inc | ORAL PHARMACEUTICAL FORMS BASED ON HYDROXYETHYL CELLULOSE WITH DELAYED DELIVERY OF ACTIVE SUBSTANCES |
US5382435A (en) | 1993-03-24 | 1995-01-17 | Southwest Research Institute | Microparticulate pharmaceutical delivery system |
IL119660A (en) | 1993-05-10 | 2002-09-12 | Euro Celtique Sa | Controlled release formulation comprising tramadol |
US5500227A (en) | 1993-11-23 | 1996-03-19 | Euro-Celtique, S.A. | Immediate release tablet cores of insoluble drugs having sustained-release coating |
DE4406424A1 (en) | 1994-02-28 | 1995-08-31 | Bayer Ag | Expandable dosage forms |
ZA953078B (en) * | 1994-04-28 | 1996-01-05 | Alza Corp | Effective therapy for epilepsies |
MX9605217A (en) | 1994-04-29 | 1997-12-31 | Johnson & Johnson | Layered absorbent products. |
ES2163504T5 (en) | 1994-05-06 | 2008-05-16 | Pfizer Inc. | DOSAGE FORMS OF CONTROLLED AZITROMYCIN RELEASE. |
DE4432757A1 (en) | 1994-09-14 | 1996-03-21 | Boehringer Mannheim Gmbh | Pharmaceutical preparation containing metformin and process for its preparation |
US5945125A (en) | 1995-02-28 | 1999-08-31 | Temple University | Controlled release tablet |
MY113429A (en) | 1995-02-28 | 2002-02-28 | Univ Temple | Controlled release tablet containing swellable polyethylene oxide |
EP0830129B1 (en) | 1995-04-14 | 2002-03-20 | Pharma Pass | Solid compositions containing polyethyleneoxide and a non-amorphous active principle |
US6117453A (en) | 1995-04-14 | 2000-09-12 | Pharma Pass | Solid compositions containing polyethylene oxide and an active ingredient |
US5558879A (en) | 1995-04-28 | 1996-09-24 | Andrx Pharmaceuticals, Inc. | Controlled release formulation for water soluble drugs in which a passageway is formed in situ |
GB9523752D0 (en) | 1995-11-21 | 1996-01-24 | Pfizer Ltd | Pharmaceutical formulations |
US5783212A (en) | 1996-02-02 | 1998-07-21 | Temple University--of the Commonwealth System of Higher Education | Controlled release drug delivery system |
AU3290397A (en) | 1996-06-10 | 1998-01-07 | Depomed, Inc. | Gastric-retentive oral controlled drug delivery system with enhanced retention properties |
ATE293458T1 (en) * | 1996-08-23 | 2005-05-15 | Algos Pharm Corp | PREPARATION CONTAINING ANTICONVULSIVE AGENTS FOR THE TREATMENT OF NEUROPATHIC PAIN |
US5972389A (en) | 1996-09-19 | 1999-10-26 | Depomed, Inc. | Gastric-retentive, oral drug dosage forms for the controlled-release of sparingly soluble drugs and insoluble matter |
US6255526B1 (en) * | 1996-12-24 | 2001-07-03 | Teva Pharmaceutical Industries Ltd. | Preparation of gabapentin |
US5872984A (en) * | 1997-04-01 | 1999-02-16 | International Business Machines Corporation | Uninterruptible power supply providing continuous power mainstore function for a computer system |
US20010046473A1 (en) * | 1997-04-18 | 2001-11-29 | Jerome Besse | Gastric-retained pharmaceutical composition and method for its use |
US6635280B2 (en) | 1997-06-06 | 2003-10-21 | Depomed, Inc. | Extending the duration of drug release within the stomach during the fed mode |
ATE302597T1 (en) * | 1997-06-06 | 2005-09-15 | Depomed Inc | STOMACH-RESIDENT ORAL DOSAGE FORMS OF WATER-SOLUBLE DRUGS WITH CONTROLLED RELEASE |
US6432986B2 (en) * | 1997-07-21 | 2002-08-13 | Bruce H. Levin | Compositions, kits, and methods for inhibiting cerebral neurovascular disorders and muscular headaches |
US20010004644A1 (en) * | 1997-07-21 | 2001-06-21 | Levin Bruce H. | Compositions, kits, apparatus, and methods for inhibiting cephalic inflammation |
US6110499A (en) * | 1997-07-24 | 2000-08-29 | Alza Corporation | Phenytoin therapy |
ES2234139T3 (en) † | 1997-08-11 | 2005-06-16 | Alza Corporation | DOSAGE FORM OF AN ACTIVE PROLONGED RELEASE AGENT ADAPTED FOR GASTRIC RETENTION. |
AU8668598A (en) | 1997-08-20 | 1999-03-08 | University Of Oklahoma, The | Gaba analogs to prevent and treat gastrointestinal damage |
ATE311867T1 (en) | 1997-09-08 | 2005-12-15 | Warner Lambert Co | ANALGESIC COMPOSITION CONTAINING ANTEPILEPTIC DRUGS AND USES THEREOF |
FR2769107B1 (en) | 1997-09-30 | 2001-07-13 | Centre Nat Rech Scient | CODING METHOD, EQUIPMENT FOR CODING AND PRODUCT THUS ENCODED |
AU9318398A (en) * | 1997-10-07 | 1999-04-27 | Warner-Lambert Company | Process for preparing a cyclic amino acid anticonvulsant compound |
CA2220038A1 (en) | 1998-01-05 | 1999-07-05 | Amina Odidi | Device for the delivery of high dose pharmaceutical, neutraceutical, agricultural, biological, and chemical substances |
AP1224A (en) | 1998-03-19 | 2003-11-14 | Bristol Myers Squibb Co | Biphasic controlled release delivery system for high solubility pharmaceuticals and method. |
US20040062802A1 (en) | 1998-04-02 | 2004-04-01 | Hermelin Victor M. | Maximizing effectiveness of substances used to improve health and well being |
FR2781793B1 (en) | 1998-08-03 | 2001-07-20 | Prographarm Lab | PROCESS FOR PRODUCING COATED GABAPENTINE GRANULES |
WO2000013894A1 (en) | 1998-09-03 | 2000-03-16 | Stefan Kraft | Anti-abrasion device mainly for protecting edges against abrasion |
US6635281B2 (en) * | 1998-12-23 | 2003-10-21 | Alza Corporation | Gastric retaining oral liquid dosage form |
US7214711B2 (en) * | 1998-12-23 | 2007-05-08 | Neurotherapeutics Pharma Llc | Method of treating migraine headache without aura |
US6294192B1 (en) * | 1999-02-26 | 2001-09-25 | Lipocine, Inc. | Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents |
EP1161263A1 (en) | 1999-03-10 | 2001-12-12 | Warner-Lambert Company Llc | Analgesic compositions comprising anti-epileptic compounds and methods of using same |
IL145661A0 (en) * | 1999-03-31 | 2002-06-30 | Janssen Pharmaceutica Nv | Pregelatinized starch in a controlled release formulation |
US6162466A (en) * | 1999-04-15 | 2000-12-19 | Taro Pharmaceutical Industries Ltd. | Sustained release formulation of carbamazepine |
US7919119B2 (en) * | 1999-05-27 | 2011-04-05 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
TR200200562T2 (en) * | 1999-06-14 | 2002-05-21 | Cosmo S.P.A | Pharmaceutical compositions for oral release that can be secreted in the body in a controlled manner and prevent unpleasant taste |
PT1202725E (en) * | 1999-07-22 | 2007-07-11 | Universuty Of Rochester | Method of treating symptoms of hormonal variation, including hot flashes |
US6294198B1 (en) * | 1999-08-24 | 2001-09-25 | Purepac Pharmaceutical Co. | Pharmaceutical tablet formulation containing gabapentin with improved physical and chemical characteristics and method of making the same |
NZ518739A (en) | 1999-11-02 | 2004-12-24 | Depomed Inc | Pharmacological inducement of the fed mode for enhanced drug administration to the stomach |
IL133196A0 (en) * | 1999-11-29 | 2001-03-19 | Yissum Res Dev Co | Gastroretentive controlled release pharmaceutical dosage forms |
EP1118321A1 (en) * | 2000-01-14 | 2001-07-25 | Ucb, S.A. | Solid pharmaceutical compositions for the controlled delivery of active substances |
ATE340563T1 (en) | 2000-02-04 | 2006-10-15 | Depomed Inc | SHELL AND CORE TYPE DOSAGE FORM WITH A RELEASE OF ACTIVE INGREDIENTS APPROACHING TO THE ZERO ORDER |
US6333352B1 (en) * | 2000-04-05 | 2001-12-25 | Mimicking Man Manually, Inc. | Method of treating benign positional vertigo |
US20010036943A1 (en) * | 2000-04-07 | 2001-11-01 | Coe Jotham W. | Pharmaceutical composition for treatment of acute, chronic pain and/or neuropathic pain and migraines |
WO2001076478A1 (en) | 2000-04-10 | 2001-10-18 | Nordisk Terapi As | System for testing and exercising sensorimotoric control of the neck |
US6350471B1 (en) | 2000-05-31 | 2002-02-26 | Pharma Pass Llc | Tablet comprising a delayed release coating |
US6531509B2 (en) | 2000-06-16 | 2003-03-11 | Teva Pharmaceutical Industries Ltd. | Stable gabapentin containing more than 20 ppm of chlorine ion |
YU95302A (en) | 2000-06-16 | 2006-05-25 | Teva Pharmaceutical Industries Ltd. | Stable gabapentin having ph within a controlled range |
US6488962B1 (en) * | 2000-06-20 | 2002-12-03 | Depomed, Inc. | Tablet shapes to enhance gastric retention of swellable controlled-release oral dosage forms |
US6451808B1 (en) * | 2000-10-17 | 2002-09-17 | Depomed, Inc. | Inhibition of emetic effect of metformin with 5-HT3 receptor antagonists |
US6683112B2 (en) | 2000-10-24 | 2004-01-27 | Andrx Corporation | Gabapentin prodrugs and formulations |
ATE305774T1 (en) | 2001-02-27 | 2005-10-15 | Roehm Gmbh | COATING AND BINDING AGENT FOR MEDICINAL FORMULATIONS WITH IMPROVED STORAGE STABILITY |
CA2449009A1 (en) * | 2001-05-29 | 2002-12-05 | Depomed Development, Ltd | Method of treating gastroesophageal reflux disease and nocturnal acid breakthrough |
AU2002345638A1 (en) * | 2001-06-11 | 2002-12-23 | Xenoport, Inc. | Amino acid conjugates providing for sustained systemic concentrations of gaba analogues |
ITMI20011337A1 (en) * | 2001-06-26 | 2002-12-26 | Farmatron Ltd | ORAL PHARMACEUTICAL COMPOSITIONS WITH MODIFIED RELEASE OF THE ACTIVE SUBSTANCE |
ITMI20011338A1 (en) | 2001-06-26 | 2002-12-26 | Farmatron Ltd | ORAL PHARMACEUTICAL COMPOSITIONS WITH IMMEDIATE RELEASE OF THE ACTIVE INGREDIENT |
HUP0500795A3 (en) * | 2001-07-04 | 2008-04-28 | Sun Pharmaceutical Ind Ltd | Gastric retention controlled drug delivery system |
US20030104052A1 (en) | 2001-10-25 | 2003-06-05 | Bret Berner | Gastric retentive oral dosage form with restricted drug release in the lower gastrointestinal tract |
US20030152622A1 (en) | 2001-10-25 | 2003-08-14 | Jenny Louie-Helm | Formulation of an erodible, gastric retentive oral diuretic |
US20030091630A1 (en) | 2001-10-25 | 2003-05-15 | Jenny Louie-Helm | Formulation of an erodible, gastric retentive oral dosage form using in vitro disintegration test data |
US7612112B2 (en) | 2001-10-25 | 2009-11-03 | Depomed, Inc. | Methods of treatment using a gastric retained gabapentin dosage |
CA2409552A1 (en) | 2001-10-25 | 2003-04-25 | Depomed, Inc. | Gastric retentive oral dosage form with restricted drug release in the lower gastrointestinal tract |
US20060159743A1 (en) * | 2001-10-25 | 2006-07-20 | Depomed, Inc. | Methods of treating non-nociceptive pain states with gastric retentive gabapentin |
US20070184104A1 (en) | 2001-10-25 | 2007-08-09 | Depomed, Inc. | Gastric retentive gabapentin dosage forms and methods for using same |
TWI312285B (en) | 2001-10-25 | 2009-07-21 | Depomed Inc | Methods of treatment using a gastric retained gabapentin dosage |
US6723340B2 (en) * | 2001-10-25 | 2004-04-20 | Depomed, Inc. | Optimal polymer mixtures for gastric retentive tablets |
WO2003061656A1 (en) * | 2002-01-16 | 2003-07-31 | Endo Pharmaceuticals Inc. | Pharmaceutical composition and method for treating disorders of the central nervous system |
US6682759B2 (en) | 2002-02-01 | 2004-01-27 | Depomed, Inc. | Manufacture of oral dosage forms delivering both immediate-release and sustained-release drugs |
US6559293B1 (en) * | 2002-02-15 | 2003-05-06 | Transform Pharmaceuticals, Inc. | Topiramate sodium trihydrate |
CN1668284A (en) * | 2002-06-07 | 2005-09-14 | 兰贝克赛实验室有限公司 | Sustained release oral dosage forms of gabapentin |
US20060094785A1 (en) | 2002-07-12 | 2006-05-04 | Guttuso Jr Thomas J | Use of amino acids for treatment of various conditions |
US20060264509A1 (en) | 2003-03-21 | 2006-11-23 | Fraser Matthew O | Methods for treating pain using smooth muscle modulators and a2 subunit calcium channel modulators |
AU2005304352A1 (en) * | 2004-11-10 | 2006-05-18 | The Trustees Of Columbia University In The City Of New York | Method for treatment of movement disorders |
EP1901720A2 (en) * | 2005-06-23 | 2008-03-26 | Spherics, Inc. | Improved dosage forms for movement disorder treatment |
US20090176882A1 (en) | 2008-12-09 | 2009-07-09 | Depomed, Inc. | Gastric retentive gabapentin dosage forms and methods for using same |
EP2101752A1 (en) * | 2006-12-08 | 2009-09-23 | Xenoport, Inc. | Use of prodrugs of gaba analogs for treating diseases |
WO2008115797A1 (en) * | 2007-03-16 | 2008-09-25 | Pavo, Inc. | Therapeutic compositions and methods |
KR101972299B1 (en) * | 2007-11-23 | 2019-08-16 | 그뤼넨탈 게엠베하 | Tapentadol compositions |
EP2240022B1 (en) * | 2008-01-09 | 2016-12-28 | Charleston Laboratories, Inc. | Bilayered tablets comprising oxycodone and promethazine |
WO2010015029A1 (en) * | 2008-08-06 | 2010-02-11 | Gosforth Centre (Holdings) Pty Ltd | Compositions and methods for treating psychiatric disorders |
PT2331210E (en) * | 2008-09-05 | 2014-08-25 | Gruenenthal Gmbh | Pharmaceutical combination of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol and an antiepileptic |
US20100190752A1 (en) * | 2008-09-05 | 2010-07-29 | Gruenenthal Gmbh | Pharmaceutical Combination |
WO2010035273A2 (en) * | 2008-09-29 | 2010-04-01 | Intec Pharma Ltd. | Novel gastroretentive delivery system |
AU2010221167B2 (en) * | 2009-03-06 | 2014-04-03 | Xenoport, Inc. | Oral dosage forms having a high loading of a gabapentin prodrug |
WO2011023392A1 (en) * | 2009-08-28 | 2011-03-03 | Grünenthal GmbH | Pharmaceutical combination comprising 6-dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol or 6-dimethylaminomethyl-1-(3-hydroxy-phenyl)-cyclohexane-1,3-diol and an antiepileptic |
-
2002
- 2002-10-24 TW TW091124777A patent/TWI312285B/en not_active IP Right Cessation
- 2002-10-25 CA CA2464322A patent/CA2464322C/en not_active Expired - Lifetime
- 2002-10-25 DK DK02781665.1T patent/DK1439825T4/en active
- 2002-10-25 EP EP02781665.1A patent/EP1439825B2/en not_active Expired - Lifetime
- 2002-10-25 WO PCT/IB2002/005440 patent/WO2003035040A1/en active Application Filing
- 2002-10-25 AU AU2002348828A patent/AU2002348828B2/en not_active Ceased
- 2002-10-25 EP EP10179051A patent/EP2266539A3/en not_active Withdrawn
- 2002-10-25 JP JP2003537607A patent/JP5421511B2/en not_active Expired - Fee Related
- 2002-10-25 MX MXPA04003946A patent/MXPA04003946A/en active IP Right Grant
-
2003
- 2003-01-22 US US10/280,309 patent/US7438927B2/en not_active Expired - Lifetime
-
2008
- 2008-09-26 US US12/239,591 patent/US7731989B2/en not_active Expired - Fee Related
-
2010
- 2010-03-29 US US12/749,101 patent/US8252332B2/en not_active Expired - Lifetime
- 2010-08-09 JP JP2010179064A patent/JP2010254713A/en active Pending
-
2011
- 2011-05-19 US US13/111,575 patent/US8192756B2/en not_active Expired - Lifetime
- 2011-11-21 US US13/301,644 patent/US8231905B2/en not_active Expired - Lifetime
-
2012
- 2012-02-14 US US13/396,441 patent/US8409613B2/en not_active Expired - Fee Related
- 2012-07-19 US US13/553,622 patent/US8333991B2/en not_active Expired - Lifetime
- 2012-07-27 US US13/560,938 patent/US8333992B2/en not_active Expired - Lifetime
-
2013
- 2013-04-01 US US13/854,433 patent/US8580303B2/en not_active Expired - Fee Related
- 2013-11-08 US US14/075,965 patent/US20140072623A1/en not_active Abandoned
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AU2002348828B2 (en) | Methods of treatment using a gastric retained gabapentin dosage | |
AU2002348828A1 (en) | Methods of treatment using a gastric retained gabapentin dosage | |
US8802157B2 (en) | Methods of treatment using a gastric retained gabapentin dosage form |