Pharmaceutical mixture.
Abstract
A pharmaceutical mixture with controlled release of actice substance which includes masking of bad taste and stability increasing of active substance characterized in that an encapsulated active substance is combined with a substance controlling the release of active substance from the encapsulation and method for preparing said mixture.

Term
No projected expiry on record.
- Priority
- Filed
- Granted
- Today
4 claims: 4 independent, 0 dependent
- 1AS JOSEPH AS ΙΩΣΕΙΣ 1. A drug-controlled release drug mix comprised covering bad taste and serving the stability of the active ingredient, characterized in that it contains a 40% active ingredient;60-75¼ of a release control substance or any of which are carbohydrates, a carbohydrate-related compound or a mixture of such compounds. 1. Εν φαρμακευτικόν μϊγμα μέ έλεγχομένην εκλυσιν ένεργοΰ ούσίας περιλαμβάνουσαν τήν κάλυψιν τής κακής γεύσεως καί τήν α'ύζησιν τής σταθερότητος τής ένεργοϋ ούσίας, χαρακτηριζόμενη άπό ότι περιέχει μίαν ένσωματωμένην ένεργόν ούσίαν έν συνδυασμώ μέ 40-99¼ (κατά βάρος) έτοιμου πρός χρήσιν μίγματος, κατά προτίμησιν 60-75¼ μιας ούσίας έλέγχου έκλύσεως ή όποία είναι είς ύόατάνθραζ, μία σχετιζομένη μέ ύόατάνθρακα ένωσις ή έν μϊγμα τοιαύτων ένώσεων.
- 2In a pharmaceutical mixture according to claim 1 characterized in that the release control substance is sucrose, glucose, fructose or sorbitol. 2. Εν φαρμακευτικόν μϊγμα συμφώνως μέ τήν αζίωσιν 1 χαρακτηριζομένη άπό ότι ή ούσία έλέγχου έκλύσεως είναι σουκρόζη, γλυκόζη, φρουκτόζη ή σορβιτόλη.
- 3In a pharmaceutical mixture according to claim 1, characterized in that the active substance is baccamphylline or theophylline. 3. Εν φαρμακευτικόν μϊγμα συμφώνως μέ τήν άζίωσιν 1, χαρακτηριζόμενον άπό τό ότι ή ’ενεργός ούσία είναι βακαμφιχιλλίνη ή θεοφυλλίνη.
- 4A method of preparing a medicament mixture with controlled release of the active ingredient comprising masking the taste and seeking the stability of the active substance, or comprising 4. Μία μέθοδος παρασκευής ένός φαρμακευτικόν μίγματος μετ’έλεγχομένης έκλύσεως τής ένεργοΰ ούσίας περιλψβάνουσα τήν κάλυψιν τής κακής γεύσεως καί τήν αΰζησιν τής σταθερότητος τής ένεργοΰ ούσίας, ή όποία περιλαμβάνει (a) the inactivation of an embedded active substance capsule with conventional additives and another active substance control substance or substance which is in carbohydrate or a carbohydrate-related substance or a carbohydrate;by weight x preferably 60-75¼ (by weight) of the ready-to-use mixture and after the addition of water to obtain a ready-to-use mixture;or α) τήν άνάμιζιν τής Ενσωματωμένης είς κάψας ένεργοΰ ούσίας μέ συμβατικά πρόσθετα καί μίαν άλλην ούσίαν έλέγχου τής ένεργοΰ ούσίας ή όποία ούσία είναι εις ύδατάνθραζ ή μία ούσία σχετιζομένη μέ υδατάνθρακας ή έν μϊγμα διαφόρων ύόατανθράχων καί ένώσεων σχετιζομένων μέ υδατάνθρακας είς μίαν ποσότητα 40-99¼ (κατά βάροςΧ κατά προτίμησιν 60-75¼ (κατά βάρος) τοΰ έτοιμου πρός χρήσιν μίγματος καί μετά τήν προσθήκην ΰδατος όιά τήν λήψιν ένός έτοιμου πρός χρήοιν μίγματος ή (b) the inactivation of an embedded active substance in a solution of standard additives and another, whether or not carbohydrate or a carbohydrate-containing substance in an amount of 40-99 g (by weight), preferably 60;for the benefit of the mixture. Lupi at— β) τήν άνάμιζιν μιας ένσωματωμένης ένεργοΰ ούσίας μέ έν διάλυμα συνήθων προσθέτων καί μίαν άλλην ούσίαν ή όποία είναι είς ύόατάνθραζ ή μία ούσία σχετιζομένη μέ ύόατάνθρακες είς μίαν ποσότητα 40-99¼ (κατά βάρος), χατά προτίμησιν 60-75¼ (κατά βάρης) τοΰ έτοιμου πρός χρήσιν μίγματος. Λνήπιι στο— Athena Αθήνα
Independent claims4
324 paragraphs in 4 sections, as filed
FIMACHETTIMN MIX.
DESCRIPTION.
Technical Division.
The present invention relates to an oral pharmaceutical preparation comprising an embedded pharmaceutically active substance. More particularly the preparation is a dry powder for mixing or a dry powder dissolved in an aqueous solution.
The object of the invention is to provide a preparation for controlling or dissolving the active substance having incorporation.
Pre-experience.
Among the alternative forms of oral administration of pharmaceutically active substances or the use of a solution or a suspension of the active substance in an aqueous solution is one form or one commonly encountered in pediatrics. This preparation is called a mixture. Dry powder or any containing active ingredient and additives or which may be dissolved is called dry mixing powder.
The preparation is stored as a dry powder. Before administration or dry powder, it is dissolved or suspended in an aqueous solution and thus a liquid formulation for oral administration is obtained. Alternatively the mixture can be prepared on site and stored for 2 years prior to administration. They are also incorporated into pharmaceutically active substances for use in mixtures, either to cover a bad taste or to control the release into the body.
To date, the drugs have been coated with polymers or with polymers in combination with plasticizers to control drug release (MICR6EMCAPSULATIQN). If these are applied to a drug in the form of granules they delay dissolution.
* 3 main ways to control dissolution of the drug from the microcapsules (MKROCAPSULES) is either the amount of the coated polymer to obtain the expected plasma side of the drug. This was done by adding water-soluble substances to the coating process.
<img file="GR78604B_D0001.tif" />
.V L · '·
BACKGROUND OF THE INVENTION The present invention provides a mixture of a virus which has poor drug coverage and / or provides a delayed dilution mixture to achieve a slow release effect.
The mixture is obtained either by suspending the dry powder in an aqueous solution or suspending the microcapsules in a solution of the substance or controlling the release.
* The release of drug from the microcapsules into the mixture, or what is called a leak, is very low, but within the body the drug is released through the microcapsules and is available for absorption.
The present invention also provides increased drug stability within the mixture.
The result is obtained by the addition of the incorporated active substance to the usual additives a release control substance (SINK).
Carbohydrates and carbohydrate-related compounds such as SINK may be used, e.g. you are very- or oligosaccharide such as dextran * you are oesaccharide such as sucrose, maltose or lactose * you are monosaccharide such as glucose, fructose, galactose, mannose or xylitol * a glycerol-related, carbohydrate-like, carbohydrate, a substance derived from ethylene glycol e.g. polyethylene glycol (ex. CARB & WAXES ^ CAI CAFI £ OP © LES ^).
A SINK may be used to mix a mixture of two or more non-recovered substances.
The amount of SINK should be between 4 *% and 99% (by weight), preferably 6% -75% (by weight) of the total preparation. orally for administration of a suspension for oral administration (blend).
One alternative form of Adding the substance or controlling the release into the embedded drug is either incorporating the substance or controlling the release together with the drug inside the shell of the incorporating capsule.
<img file="GR78604B_D0002.tif" />
<img file="GR78604B_D0003.tif" />
* Any pharmacologically active substance can be used, e.g. any of the following:
Chemotherapeutic 'bacamphichillin, amphichillin, FLUCLOXACILLIN, tetracycline, DICLOXACILLIN, chloramphenicol, gentamicin, erythromycin, lynchomycin, RIFAMPICIK sulphadiprazine, sulphadiazine sulphadiazine, sulfamidazine
'Adrenergic Beta-Stimulant Stimulus Cough'
Sweeteners are anti-rheumatoid arthritis ephedrine, terbutaline, theophylline;
ethylmorphine, DEXTROMETHOrAn, noschapine, bromexine.
DIXITOXINE, DKMXIB, DISPYRAMIDE, procaine, the: hainide, XLPREMOLOL, ATENOLOL, METOPROLOL, PINOOLOI
Blood Pressure Gauges: Butanidine, cholinidine, guanedidine, METHYLDSPA, RESERPINE TRIMETAPHANE, hydrolazine, BENDR0PPHLUMETIA2IDE, FUROSEMIDE, CHLORSTIALIDE, Antihistaminamine, BROMINAMIN: BRO
Hypertensive diabetics:
Soothing, Hypnotic, Anti-sports:
'Antiepileptic:' Analgesics, anesthetics:
"But :
carbutamide, chloropropamide, tolazamide, tolbutamide.
HEX®BARBITAL, PENTOBARBITAL, PHENOBARBITAL, MEPROBAMATE, CHL © RDIAZEPOXIDE, DIAZEPAM, FLUNIT1AZEPAM, NITRAZEPAM, FLUPHENAZINE, PERPHENAZINE, PROCHL © RPERAZINE, HALOPERIPIN, HALOPERIDIN, HALOPERIDIN
Phentoine, ethotaine, ethosuximide, carbamazepine.
Codeine, Morphine, Pentachosine, Pethidine, DEXTROPROCHYRENE, Methadone, Acetylsalicylic Acid, DIFLUNISAL, RHENAZHNE, PHENYLBUTAZONE, Acetaminophen, INDOMETAZINE, PIROXENO, NAPROXEN, NAPROXEN
CIMETIDINE, QUINIDINE, DICOUMAHINE, WARFARINS, palladium chloroform, chlorochine.
The preferred drug is either bacamycillin hydrochloride (6- [5 (-) - 2-amino-2-phenylacetamido / -phenylchlorinated hydrochloride 1-ethoxycarbonyloxyethylene hydrochloride aliphatic hydrochloride or forms.
“Other preferred drugs are
The above-mentioned salt-formulated drugs.
The following medicinal products may be used:
Acetate, benzenesulfonyl, benzoyl, CALCIUM EDSTATE, hamslilic, carbonate, theophylline, iprophylline and erythromycin are used freely in the form and / or inorganic salts, respectively.
J I, chloroform xitpixcjv, double chloroform,
H. ......
EVETATE, edisylate, estolate, esylichon, fumaric, hon ntikon, gluconate, glutamate, klykollylarsanilikon, exyloresorkinikon, HYBRABAMINE, hydrobromic, hydrochloric, yoroxynafthoikon, iodide, isethionate, laktichon, lactobionate, malate, maleate, manoelichon, mesylate, methylbromide, methylonitrikon, methylsulphate fungicidal, naphthalic, nitrate, pamonic, pantothenic, phosphate / bisphosphate, polygalacturonic, salicylate, stearate, hypoxic, succinic, sulphide, tannic acid, tartrate, theocyclic, triethiodioxide.
The following cationic salts may also be used. Suitable cationic salts include alkali metal salts e.g. sodium and potassium, the ammonium salts and the pharmaceutically acceptable amines, e.g. glycine, ethylenediamine, choline, diethanolamine, triethanolamine, decoctylamine, diethylamine, triethylamine, 1-amino-2-propanol-2-amino-2- (hydroxymethyl) propane-1,3-diol-1,3-diethyl-propan-4-dihydropyran -2-isopropylaminoethanol.
Incorporation of the drug into a capsule may be carried out in the form of microcapsules, or incorporation but is not limited to a small size.
'Liquid coating'
Polymers:
Synthetic polymers of polyvinylidene type, e.g. polyvinyl chloride, polyvinyl ozone, polyvinyl alcohol.
Polyethylene type, e.g. polyethylene, polystyrene.
Polymers of nodular nodule or ternary nodule type e.g. methyl methacrylate or conc. 1 dimers of acrylic monomers.
Biopolymers or modified cellulose biopolymers e.g. ethylcellulose, cellulose acetate phthalate.
The polymer may be water-soluble, water-insoluble, or alkaline-soluble and may be mixed with a plasticizer or other filler and a water-soluble modified polymer e.g. hydroxypropyl cellulose.
There are also oils, waxes,
In one embodiment, insulin and a mixture or any of these can also be used to find the high fatty acids, high alkyd or polyhydric alkyd oils.
embodiment of the invention or betamy hydrochloride / BAPC); An insoluble, microporous polymer is added to sucrose as SINK for the preparation of dry matter, then dissolved in water for preparation.
<img file="GR78604B_D0004.tif" />
.1 .'Ί
In another embodiment of the invention, or BAPC, is incorporated into a polymer of soluble acid such as HJD1AGIT Saccharide is used sucrose as SINK for the preparation of a dry snow mixture or, if present, dissolved.
In another embodiment of the invention, or theophylline, is incorporated into microbial envelopes of ethyl cellulose and sorbic acid is used as a SINK to provide a dry snow mixture or whatever, thereafter.
In another embodiment of the invention, unaccharic acid is incorporated into pellets of acidic cellulose acetate phthalate, sucrose is used as a SINK to provide a dry, dry skin, or whatever.
A release control substance is mixed with other components of the drug microchip and added to the dry snow mixture mixed into a conventional mixture. The dry snow is then added to a bottle with a filler. Then water is added from the client or the drug to dissolve the release control substances.
Alternatively, a solution for the control of release of other components is prepared. The drug can then be added to the drug or if the solution is then filled with a ready-to-use bottle, or the drug can be filled into separated containers and added to the solution, before use.
A better way of accomplishing the invention.
It is leaking.
'Completed studies leakage purpose of apodeixin that blood michrochapsai not echlyoun any significant amount of farmachou into the SINK prochalousai so a chachin flavor just' come into contact with the water Hai prochalousai ypovathmisin OF ichanotitos or the loss of ichanotitos function as a configuration of the controlling; of washing.
A microfibre was added to the SINK solution according to the invention. Analysis or amount of the drug or which has been solved by micronutrients. Samples were, in some cases, refrigerated for up to 8 days at room temperature. SINK was spectrophotometrically / A The result is given as a percentage of leakage which is the amount of foam. * Which is found inside the drug divided by the starting amount i.
<img file="GR78604B_D0005.tif" />
drug menu.
To demonstrate the effect of the release control substance the release studies were carried out in water. Microcapsules were placed in a bowl of water and water was added. * 6 stirring rate was 3® rotational minute min or release amount as described above.
EXAMPLE 1.
1 © b gr. dry snow contains:
5,61 HP hydrochloric acid;
Ethyl cellulose microwave oven (7®% drug)
Sodium bicarbonate ®, 83 HP;
Mannitoline 9.35 YP;
Sucrose 83.1 YP;
Sodium bicarbonate, or mannitol chai or sucrose were dissolved before adding the micronutrient. The final unmixed match took place inside a cup. The mixture contains 46% by weight of release control substance.
4.81 g snow were added to 5 ml of water.
Time (in days) Leakage%
1© ®,5 ·,?
1,1
1,3
1,2
In this example, this drug or leakage of the drug was analyzed by the mercury titration method.
Time (in days) Inlet Water%
<td> 6,042</td><td> 6®</td>
<td> 6,684</td><td> 5®</td>
<td>EXAMPLE 2.</td><td></td>
<td>25.8 g pharmaceutical mixture containing:</td><td></td>
<td>Bacchicillin hydrochloride</td><td>6.86 g</td>
<td>EQDRAGIT 166 microchip (64% medicine)</td><td></td>
<td>Fructose</td><td>18.75 g</td>
<td>water</td><td>6.25 g</td>
<td>Fructose dissolved in water</td><td>before the addition of the microchips</td>
The mixture contains 67.5% of release control substances. Time (in days) Leakage% <®, 2
<img file="GR78604B_D0006.tif" />
·!
Time (I am)
0.08 g 0.05
Release within a tree (%)
5·
9©
EXAMPLE 3;
31.3 hPa. pharmaceutical mixture containing theophylline
Microcapsule of ethylcellulose (72% drug) (fructose <sup>4</sup> (sorbifoline) (sorb;; 5p;
23.44 g 7.82 g
20.94 YP * 7.82 g
1TH
The two mixtures were prepared according to Example 2. The mixtures contain a) 75% b) 72% release control substances.
Time (in days) Leakage (%) 'b / ®, 2 0.7 <i, 2 <0.2 <0.2 <0.2
In-tree release (%)
Time (I am)
0,21 ©,33
EXAMPLE 4.
31.3 g drug mix contain! theophylline microcapsule ethyl cellulose (72% drug) (Sucrose<sup>b</sup> (Sucrosein (Sucrose) <sup>r</sup> Glycerol (Glucosin c)
<td> 5©</td><td></td>
<td> 90</td><td></td>
<td> ®,·5</td><td>HP;</td>
<td> 9,38</td><td>HP.</td>
<td> 9,38</td><td>II</td>
<td> 9,38</td><td>II</td>
<td> 9,38</td><td>II</td>
<td> 9,38</td><td>Hr.</td>
<td> 9,38</td><td>II</td>
<td> 9,38</td><td>M.</td>
<td> 12,5</td><td>II</td>
<td colspan="2">The example</td>
The mixtures contain 60% of release control substances.
<td>Time (I am)</td><td></td><td>Leakage</td><td> (%)</td>
<td> _____</td><td>a</td><td>_b_</td><td>Y.</td>
<td> 1</td><td> 0,20</td><td> < 0,2</td><td> 0,26</td>
<td> 2</td><td> ·,31</td><td> •♦.35</td><td> 0,28</td>
<td> 5</td><td> 0,65</td><td> 0,82</td><td> 0,49</td>
<td> 9</td><td> 1,15</td><td> 1,17</td><td> 0,90</td>
<td>Time (I am)</td><td>tt</td><td>Release within</td><td>water</td>
<td> 0,21 0,33</td><td> ......</td><td> 50 90</td><td></td>
<img file="GR78604B_D0007.tif" />
<img file="GR78604B_D0008.tif" />
: '..j ·' - L ·
<img file="GR78604B_D0009.tif" />
EXAMPLE 5
75.1 YP; pharmaceutical mixture contains t 'Acetyl salicylic acid, 100 g.
Microcapsule Phthalate Nodular Cellulose (69J * drug)
Sucrose 48.75 HP.
Phosphate buffer (pH 7, *) 26.25 YP; * Sucrose was dissolved in phosphate buffer. Oh microcapsules were added afterwards.
The mix contains Time_ (yes)
65% release control substance.
Leak ($)
3,5
Time (in days) ©, 0S8 ©, ®17
Release into phosphate buffer PH 7
5©
9©
EXAMPLE 6.
<td></td><td>a</td><td>b</td><td>c</td>
<td>Beckampicillin hydrochloride</td><td> ®,27</td><td>gr. ·, 27</td><td>gr. ®, 27 g.</td>
<td>Microcapsules Ethylcellulose (7®% Pharm)</td><td></td><td></td><td></td>
<td>Sodium bicarbonate</td><td> ·,4®</td><td>gr. ®, 4®</td><td>gr. -</td>
<td>Mannitol</td><td> ®,45</td><td>gr. -</td><td> —</td>
<td>Sucrose</td><td> 4,·</td><td>gr.</td><td> —</td>
<td>water</td><td> 5,®</td><td>gr. 5, ®</td><td>gr. 5, ® gr.</td>
The mixtures were prepared according to Example 1.
Mixture (a) contains 44 substantially release controls.
* Release into the water of the microchips was or is the same as in Example 1.
<td>Time (I am)</td><td>Leak (>)</td>
<td></td><td>a B C</td>
<td> 1</td><td> ®,5 «5 1®0</td>
<td> 2</td><td> ®,9</td>
<td> 4</td><td> 1,1</td>
<td> 7</td><td> 1,3</td>
<td> 1®</td><td> 1,2</td>
<td>EXAMPLE 7.</td><td></td>
Are 4 different microcapsules prepared with ethylcellulose and suspended in sorbitol dissolved in water? following composition.
Microwave
Sorbitol water
The mixtures contain 7.0% of essential release control.
• L.
5® mg, 45.1 YP; 19.3 g.
<img file="GR78604B_D0010.tif" />
• i
- 1©
<td> 3 3 3</td><td>Miniclip</td><td colspan="2">Leakage within SINK</td><td colspan="2">Flushing in the water</td>
<td> 33’·</td><td></td><td> ($)</td><td>sorbitol (days)</td><td> ($)</td><td>(i'm)</td>
<td></td><td>KCC (86) *,</td><td> 16</td><td> 21</td><td> 56</td><td> 3</td>
<td></td><td>Paracetaminophen (91)</td><td> 19</td><td> 21</td><td> 35</td><td> 1</td>
<td></td><td>FLUCL © XACILLIN (89 C)</td><td> 2©</td><td> 1</td><td colspan="2"> 9© ®,5</td>
<td></td><td>FENOXTMETHYL PENICILLIN POTASSIUM (83f.)</td><td> 1©</td><td> 1</td><td> 8©</td><td> 1</td>
(*) active drug content within the microcapsule.
EXAMPLE b.
9.2 gr. Theophylline according to Example 3 was suspended in various sugar solutions.
Substance controlling tin
<td>loses weight ($)</td><td>Leak ($)</td><td>Time (I am)</td>
<td>Xylitol 55</td><td> 13</td><td> 8©</td>
<td>Glucose 5 ©</td><td> 17</td><td> 4©</td>
<td>Sorbitol 7 ©</td><td> 3</td><td> 8©</td>
<td>Fructose 75</td><td> 3</td><td> 8©</td>
<td>; Fructose-xylitol 19-41</td><td> 1©</td><td> 8©</td>
<td>Fructose-xylitol 39-28</td><td> 6</td><td> 8© .</td>
<td>Fructose-xylitol 56-14</td><td> 4</td><td> 8©</td>
It is thus possible to limit the leakage of the mixture to a small extent only after about 3 months of storage at room temperature.
EXAMPLE 9.
65 * 4 g a medicinal mixture containing i
Theophylline Candle 1 gr.
laminated microcapsule ($ 52 per drug)
Sorbitolin 45.1 g
19.3 gr.
The mixture was prepared according to Example 3;
Mixture Contains $ 69 Time (in days) © Leak Release Control ® ($) ®, 7
Time (in days) ®, 5
EXAMPLE 1 ©.
26.31 g pharmaceutical mixture containing:
Microcapsule Coated with Prochloroperazine ($ 3.4) Sorbitol
Inland Water Release ($)
<img file="GR78604B_D0011.tif" />
Release Control Substance Leakage (%)
2.7 "Release Into Water (%) Water 8.3 g.
The mixture was prepared according to Example 3.
The mixture holds 79%
Time (I am)
Time (I am)
9,25
EXAMPLE 11.
27.15 UPS * pharmaceutical mixture contain:
Microcapsule Coated with Ethylcellulose Theophylline (72%) 9.15 YP; Polyethylene Glycol (CARBQWAX ^^ 4®i) 29.25 <sup>11</sup> Water 6.75 * Polyethylene glycol was blended with Water and then microcapsules were added.
The mixture contains 75% substance release control Time (days) Leakage (%)
2,4
For release into the water, see Example 3;
EXAMPLE 12.
13,877 YP; pharmaceutical mixture contain:
Erythromycin microcapsule bound with phthalate acetate cellulose (57% drug) 9,877 mg.
Fructose 9.75 Water 3.25
Microcapsules were added to the fructose solution in water.
The mixture contains 71% of release control substance.
Time (in days) Leakage (%) / 1
Time (in days) “Inlet Water (%)
9,25 46
It is being studied for release.
Microcapsules were inserted in suspension of 75% solution of control substance
<img file="GR78604B_D0012.tif" />
<img file="GR78604B_D0013.tif" />
After 2-3 days of storage, the microcapsules were filtered off and the drug was measured or released. The microcapsules were placed in a cup containing either a gastric fluid imaging or a fatty acid imaging at 37 ° C to simulate an IN VIV disorder. The torsion rate was 3® strokes per minute. After some time, samples were withdrawn and spectrophotometrically dried in terms of drug content.
The results show the time required for the achievement of 5® 7® and 9®% of the total amount of microinjected drug.
MIKRIASIA THETHYFALINICH.
Gastric fluid excretion (hr) Hypertensive ulcer imitation (hr)
<td> (%)</td><td>beginning</td><td>3 day storage.</td><td>beginning</td><td>2 hours storage</td>
<td> 5©</td><td> 4,2</td><td> 4,4</td><td> 3,7</td><td> 4,4</td>
<td> 7©</td><td> 5,7</td><td> 5,8</td><td> 5,5</td><td> 6,6</td>
<td> 50</td><td colspan="2">6,2 6,4 AKETIAKON SAAKYAKTHN ACID.</td><td> 7,5</td><td> 8,3</td>
<td>Release</td><td colspan="2">Gastric fibrosis imbalance (%)</td><td colspan="2">Imitation in a scorching liquid (hr)</td>
(%) start__save. 2 pm _ _ _archive_ _save. 2 pm
<td> 5©</td><td colspan="2"> 0,14</td><td> 0,21</td>
<td> 7©</td><td></td><td> 0,22</td><td>I, 31</td>
<td> 9©</td><td></td><td> ®,3</td><td> ©,5</td>
<td>1 hour</td><td> 12%</td><td> •'8%</td><td></td>
<td>2 hours</td><td> 23%</td><td> 15%</td><td></td>
<td colspan="2">MICHAEL</td><td colspan="2">HJDKAGIT 1H0 HYDROCHLORINE BAKAMFIPLINE.</td>
Gastrointestinal Imitation Release (Seven) Impaired intestinal fluid (minutes) _ (%) _continuous_ day storage 2 days__ beginning__container. 2 pm _
<td> 5©</td><td> ®,4</td><td> ®,8</td><td> 1,5</td><td> 3</td>
<td> 7©</td><td> ·,5</td><td> 0,9</td><td> 1,8</td><td> 3,7</td>
<td> 9©</td><td> ®,7</td><td> 1,0</td><td> 2,5</td><td> 5</td>
<td colspan="2">Microchips compositions like you</td><td colspan="2">Examples 7.9 x 11.</td><td></td>
<td>Microchip</td><td></td><td></td><td>Release within</td><td>Water</td>
Initial storage time _________________________ (%). (ok) ______ (ok) (%) (ok) ___ rce
Ipharacetam Phenozymethyl Nefenone
PENICILLIN POTASSW
M.
5© 3
1
1
<img file="GR78604B_D0014.tif" />
++7+.
+. +: + / - ':' 7 c ·. .. · »·« »».
, '* ·' '-5' 'KK + beofillin-coated wax j-beophylline-coated with ethyl- *) cellulose}
(a) in accordance with Example 7 (b) in accordance with Example J (c) in accordance with Example 11.
Washing studies were also performed with the compositions of Example 8. The wash rate was carried out in accordance with FlBX XX (method
II PADDLE) 1 min 0 min at 9 ° C in 37 ° C water; * wash rate is expressed as% wash time. * Beginner / washout rate was 12 / hour.
^ {^ E ^ Washing rate Washing rate% / hr · Time (days)
Xylitol Glucose Sorbitol Fructose
Fructose-xylitol (19 ”41)
Fructose-xylitol (38-28)
Fructose-xylitol (56-14)
The effect on the storage time of the micronutrients in various SINK solutions is negligible.
It is studying stability
Suspensions of micronutrients were implanted with SINK solutions according to the invention. The suspensions were stored for measurement or content of the drug by HPLC purification as a non-selective method.
Mixtures
5·
<td> 9,9</td><td> 8©</td>
<td> 9,7</td><td> 4©</td>
<td> 11,7</td><td> 8©</td>
<td> 11,8</td><td> 8©</td>
<td> 1·,5</td><td> 8©</td>
<td> 11,9</td><td> 8©</td>
<td> 11,9</td><td> 8©</td>
Mixtures not according to the invention i) according to Example 6b; b) according to Example 6c; c) according to Example 6a
d) Micro RC? ethyl cellulose-coated bechamycin (72% drug) ©, 36
<td>Sucrose</td><td> 8,32^</td>
<td>water</td><td>4 ^ 8 y</td>
<td>) Micro-scaffolding HC0 bechamycin</td><td rowspan="2">/ i / · L +; U. · '' '</td>
<td>coated with ethnocellulose</td>
<td>(72¼ drug)</td><td>/ Z-, ·· I ·· »· - - to -<sup>3</sup>^ m. * © 1 iw i> -4 ";</td>
<td>Fructose b</td><td></td>
<td>water / 7</td><td>—T — C.</td>
• L.
(g) Micro-cleaved acetylsalicylic acid bound to phthalic acid;
<img file="GR78604B_D0015.tif" />
13 »'' L ;; - · .. 5-5¾. n.
-.. .,.··»· .·· ·
<td>rhinin (69% drug)</td><td> 0,72</td>
<td>Sucrose</td><td> 8,32</td>
<td>PH 3 citrate buffer</td><td> 4,48</td>
<td>h) Erythromycin Microchips (87% Pharm)</td><td>0.44 g</td>
<td>coated with acetic acid pellet</td><td></td>
<td>tar.</td><td>8.32 g</td>
<td>Phosphate buffer pH 7.0</td><td>, 4.48 g.</td>
<td>Mixture</td><td>Come on Year (I am)</td><td>obstruction temperature (° C)</td><td>Contactless drug * (%)</td>
<td>a b</td><td> 1 1</td><td> 25 25</td><td> 2 60</td>
<td>T.</td><td> 10</td><td> 25</td><td> 91</td>
<td>d</td><td> 7</td><td> 25</td><td> 83</td>
<td>e</td><td> 7</td><td> 25</td><td> 89</td>
<td>g</td><td> 3®</td><td> 5«</td><td> 70</td>
<td>Ί</td><td> 30</td><td> 50</td><td> 82</td>
* 100% of the intact or initial dose of intact drug.
<sup>:</sup>y
The results imply that the mixtures according to the invention have an improved effect on the stability of the drugs.
Contents4
15 sheets
Sheet 1 Sheet 2 Sheet 3 Sheet 4 Sheet 5 Sheet 6 Sheet 7 Sheet 8 Sheet 9 Sheet 10 Sheet 11 Sheet 12 Sheet 13 Sheet 14 Sheet 15
51 members in 33 offices
Priority claims3
| Document | Office | Kind | Date |
|---|---|---|---|
| 8203953 | Sweden | A | |
| 82039538 | – | – | – |
| SE19820003953 | – | – | – |
Members51
| Document | Office | Kind | |
|---|---|---|---|
| SE8203953D0 | Sweden | D0 | |
| DK272383D0 | Denmark | D0 | |
| PT76919A | Portugal | A | |
| GB8317071D0 | United Kingdom | D0 | |
| IL68779D0 | Israel | D0 | |
| IE831462L | Ireland | L | |
| DK272383A | Denmark | A | |
| FI832197L | Finland | L | |
| IS2824A7 | Iceland | A7 | |
| NO832293L | Norway | L | |
| AU1594383A | Australia | A | |
| GB2122490A | United Kingdom | A | |
| JPS5916822A | Japan | A | |
| EP0101418A2 | European Patent Office (EPO) | A2 | |
| ES8403720A1 | Spain | A1 | |
| DD209971A5 | German Democratic Republic (until 1990) | A5 | |
| ZA833931B | South Africa | B | |
| GR78604BThis record | Greece | B | |
| AR231075A1 | Argentina | A1 | |
| KR840005024A | Republic of Korea | A | |
| EP0101418A3 | European Patent Office (EPO) | A3 | |
| NZ204639A | New Zealand | A | |
| GB2122490B | United Kingdom | B | |
| PT76919B | Portugal | B | |
| HU189300B | Hungary | B | |
| CA1214726A | Canada | A | |
| HK98786A | Hong Kong, China | A | |
| AU561954B2 | Australia | B2 | |
| CS463683A2 | Czechoslovakia (until 1993) | A2 | |
| MY8700292A | Malaysia | A | |
| PH21911A | Philippines | A | |
| CS257769B2 | Czechoslovakia (until 1993) | B2 | |
| IS1325B6 | Iceland | B6 | |
| CY1468A | Cyprus | A | |
| IE55204B1 | Ireland | B1 | |
| EP0101418B1 | European Patent Office (EPO) | B1 | |
| AT59286T | Austria | T | |
| KR910000028B1 | Republic of Korea | B1 | |
| DE3382086D1 | Germany | D1 | |
| US4994260A | United States of America | A | |
| DK161365B | Denmark | B | |
| DK161365C | Denmark | C | |
| FI85213B | Finland | B | |
| NO168745B | Norway | B | |
| SU1722207A3 | Soviet Union (until 1991) | A3 | |
| FI85213C | Finland | C | |
| NO168745C | Norway | C | |
| BG51341A3 | Bulgaria | A3 | |
| JPH0559089B2 | Japan | B2 | |
| LT2252B | Lithuania | B | |
| LV5391A3 | Latvia | A3 |
Numbers
- Publication, DOCDB
- 78604
- Publication, EPODOC
- GR78604
- Application
- 71768
- Application, DOCDB
- 830171768
- Application, EPODOC
- GR19830171768
Titles
- English
- PHARMACEUTICAL MIXTURE
Classification
- CPC, 7
- A61K9/0095
- A61K9/5015
- A61K9/5026
- A61K9/5042
- A61K9/5047
- A61K47/10
- A61K47/26
- IPC, 9
- A61K9 62
- A61K9 00
- A61K9 10
- A61K9 48
- A61K9 50
- A61K31 43
- A61K31 52
- A61K47 10
- A61K47 26