WO1985001207A1 - Enteric film-coating compositions - Google Patents

Enteric film-coating compositions Download PDF

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Publication number
WO1985001207A1
WO1985001207A1 PCT/US1984/001424 US8401424W WO8501207A1 WO 1985001207 A1 WO1985001207 A1 WO 1985001207A1 US 8401424 W US8401424 W US 8401424W WO 8501207 A1 WO8501207 A1 WO 8501207A1
Authority
WO
WIPO (PCT)
Prior art keywords
parts
dry powder
pvap
enteric coating
enteric
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.)
Ceased
Application number
PCT/US1984/001424
Other languages
English (en)
French (fr)
Inventor
Stuart C. Porter
Edward J. Woznicki
Susan M. Grillo
Louis F. D'andrea
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Colorcon Inc
Original Assignee
Colorcon Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Colorcon Inc filed Critical Colorcon Inc
Priority to KR1019850700046A priority Critical patent/KR850700009A/ko
Publication of WO1985001207A1 publication Critical patent/WO1985001207A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating

Definitions

  • This invention relates to the field of aqueous enteric film-coating, suspensions for coating pharma- ceutical tablets and the like for preventing release of the ingredients of the coated tablet in the gastric •juices of the stomach, and for. releasing the ingredients in the intestines. It provides a non-toxic edible en ⁇ teric film-coating dry powder for use in making an aqueous enteric coating, suspension that may be used in coating pharmaceuticals with an intestinally soluble coating that is insoluble in the gastric juices of the stomach.
  • Aqueous enteric coatings insoluble in gastric juices and soluble in the intestines have previously been proposed, but they have had problems including not providing sufficient protection against moisture penetration to the interior of the tablet. Also, tab- lets coated " with such aqueo ⁇ s enteric coatings tend to disintegrate, in the gastric juices of the stomach and to release their medicament-prematurely into the stom ⁇ ach, rather than delaying tabiet disintegration and release of ingredients until the tablet reaches the . intestines as desired.
  • Japanese patent 104,823/1981 to Sekikawa et al. relates to intestinally soluble protective coating agent composites for solid medicines and teaches that the use of water soluble plasticizers destroys the enteric performance because such plasticizers are not resistant, to gastric juices and do not prevent the tablet from disintegrating in the stomach.
  • the Japanese patent discloses preparing a coating system by adding individual components: * adding a wetting agent to water, dispersing a polymer into the water, adding a plasticizer, etc.
  • the in ⁇ ventive dry powder system had to overcome problems of premature agglomeration and clogging in the spray ap ⁇ paratus. This problem was overcome by adding an am ⁇ monia solution after mixing and thoroughly wetting the coating dry powder particles in water.
  • Summary of the Invention The invention provides enteric film-coating compositions which overcome the problems of the prior art by providing a non-toxic edible enteric
  • film-coating dry powder that is complete-, and needs only to be dispersed in an aqueous solution to be ready for coating pharmaceutical tablets and the like.
  • the "film coating composition is shipped i dry powder 5 form, with a saving in shipping cost because of its reduced weight since it is without the weight of any solvent.
  • the inventive film-coating enteric composi ⁇ tion is stored in dry form which avoids problems of
  • the non-toxic edible enteric ilm coating dry. powder composition in-accordance with the invention comprises a.film-forming polymer, a plasticizer, an • 15 . auxiliary film-forming polymer, pigment particles or substitute,, and, optionally, an anti-caking agent.
  • A" coating, suspension is made by mixing this dry powder into water and adding an anti-coalescing agent to pre ⁇ vent, the coating suspension from clogging the nozzles
  • the polymer is polyvinylacetatephthalate, PVAP, having a phthayl content of about 55-62%, and having a particle size below 100 microns and preferably below 25 microns.
  • the PVAP is about 70-85% by weight of the
  • 25 dry powder and is preferably in the range of 75-80% by weight of the dry powder - - .
  • the auxiliary film-forming polymer is present in the dry powder to assist in the forming of a film on the tablets and also to act as a suspending agent
  • the preferred film-forming polymer is ' sodium alginate in an amount of up to 3% by weight of the dry powder and preferably in the range of 1-1.50% of the coating dry powder.
  • Another auxiliary film-forming polymer which may be used is A4C, methyl cellulose made by Dow Chemical, which may be used up to 1.50% by weight of the dry powder and preferably in the range of 1-1.50% thereof.
  • a medium viscosity grade sodium al- ginate is preferred.
  • the sodium alginate is a water soluble poly ⁇ mer which adds viscosity to the coating suspension, and also helps the coating adhere to the tablet sur ⁇ face while the PVAP particles are fusing to form a film.
  • the sodium alginate makes the coating suspension. thicker and thereby inhibits settle ⁇ ment and acts as a suspending agent, and also acts as a film former.
  • Sodium alginate although it is water soluble, is not soluble at low pH such as that found in gastric juices, and thus the sodium alginate does not interfere with enteric performance by disintegrating in the gastric juices of the stomach.
  • the sodium alginate acts as a suspension agent for the PVAP particles in the coating suspension.
  • the sodium alginate also acts as a film former during the spraying operation to assist in providing an even coat ⁇ ing on the tablets.
  • the pigment particles may be any of the pig ⁇ ments used in making coating dispersions for pharma- ceutical tablets and the like.
  • the pig ⁇ ments may be FD&C and D&C Lakes, titanium dioxide, magnesium carbonate, talc, pyrogenic silica, iron oxides, channel black, and insoluble dyes.
  • natural pigments such as riboflavin, carmine 40, cur- cumin, and annatto.
  • suitable pigments are listed in Jeffries ⁇ . S. patent no. 31,49,040; Butler et al. ⁇ . S. patent no. 3,297,535; Colorcon U. S. patent no. 3,981,984; Colorcon U. S.
  • the amount of pigment particles in the coating suspension presents a problem.. If the coating suspen ⁇ sion contains too much.pigment, the pigment, particles interfere with " the polymer irorming a film on the tablet.- It has been- found- that,.adding .more than about 15% pig ⁇ ment, by weight of" the. coating dry powder, interferes with- the polymer.forming a film on the tablet. Ac ⁇ cordingly, if a light color is desired, a color that requires. 1 to 3 pigment to polymer ratio, mixing the pigments and polymer in that: ratio to form the coating dry- powder produces an. eventual coating on the tablet that would not be acceptable. To overcome this prob ⁇ lem., 10% titanium dioxide was mixed, into the PVAP while it was being made.
  • the coating dry powder was being made, it was found- that additional pigment particles up to 15% by -weight-of the coating dry powder could be mixed in with the titanized PVAP and other in ⁇ gredients without interfering with the film forming of the coating suspension on the tablets. If a light col ⁇ or is. not needed, the titanized PVAP need.not be used. " With the non-titanized. VAP, up to about 157o ' pigment particles may be mixed into the coating dry powder without interfering with the forming of a film on the tablets. With the titanized PVAP, the titanized dioxide (10%) and other pigment particles (15%) may reach a total of 257 * by weight of the coating dry powder without interfering with the forming of a film on the tablets.
  • the anti-caking agent may be Cab-O-Sil, fumed silica made by Cabot Inc., which is* present preferably in the amount of about 1.00%.of the coating dry powder.
  • the fumed silica acts as a processing aid and also 5 keeps the dry powder from lumping up while in storage. Use of the fumed silica is optional because any lumps that are formed can be screened out.
  • the anti-coalescing or stabilizing agent may be 30 ammonium hydroxide solution, NH,0H, which may 10 - be used up to 8.00 milliliters per 100 grams of solids in the coating suspension, and preferably about 4.00 milliliters per 100 grams of. solids.
  • the ammonia is not a part of the coating powder; it is added after suspending the coating powder in water for about 1/2 15 hour., and before the spraying step.
  • the coating sus ⁇ pension may be sprayed without adding the anti- coalescing agent, but there may be clogging problems if the spray equipment becomes too hot. If the anti- coalescing agent is added to the coating suspension, 20 the coating suspension will not begin to coalesce and
  • the inventive dry powder non-toxic enteric coating dry powder is made and sold by. Colo'rcon, Inc., West Point, Pennsylvania 19486, under the trademark COATERIC enteric film coating concentrate designed for 0 use in an all aqueous system.
  • The. quality of the en ⁇ teric properties of tablets coated by this aqueous system is equal to the quality of enteric film coatings made from an organic solvent system.
  • the method of applying the inventive enteric 5 coating to tablets is as follows:
  • the ingredients of the coating dry i powder are mixed together. Then the coating dry powder.is
  • the coating dry powder is added slowly to the water with constant mixing. After about 30 to 40 minutes, the coating suspension is passed through a mesh screen and is then ready for use.
  • Certain tablet configurations or core com ⁇ positions may require a precoat prior to the applica- tion of the inventive enteric suspension.
  • Precoating with a water soluble polymer solution provides a smooth surface on an otherwise rough core. It also aids in preventing edge chipping and tablet abrasion.
  • Example 1 A dry mix of grams Poiyvinyl acetate phthalate (titanized) 75.10 Polyethylene glycol 3350 11.30
  • FD&C Yellow No. 6 Aluminum Lake 5.05 D&C Yellow No. 10 Aluminum Lake 6.05 is prepared by first blending the ingredients in a twin shell blender until uniform and then passing them through a Hammermill to disperse any small agglomerates. Using a high speed agitator, 15 grams of the dry mix are suspended in 85 milliliters of deionized water. After stirring for 1/2 hour, 0.6 grams of concentrated ammonium hydfbxide solution are added to the suspension. After 5 minutes of additional stirring, the coating suspension is ready for application to tablets.
  • Example 2 A dry mix is made in accordance with Example 1 except that 10 grams of polyethylene glycol 3350 are used
  • Example 3 A dry mix is made in accordance with Example 1 except that 20- grams of polyethylene glycol 3350 are used instead of 11.30 grams.
  • Example 4 A dry mix is made in accordance with Example 1 except that 10 grams of polyethylene glycol 8000 are sub ⁇ stituted for the polyethylene glycol 3350.
  • Example 5 A dry mix is made in accordance with Example 1 except that 10 grams of polyethylene glycol 8000 are sub ⁇ stituted for the polyethylene glycol 3350.
  • Example 6 A dry mix is made in accordance with Example 1 except that 0.5 grams of fumed silica,are used instead of 1.00 gram.
  • Example 7 A dry mix is made in accordance with Example 1 except that.1.5. grams of fumed silica are used instead of 1.00 gram.
  • Example .8 A dry mix is made in accordance with Example 1 except that 1.00.gram of sodium alginate is used instead of 1.50 grams.
  • Example 9 A dry mix is made in accordance with Example 1 except that 3.00 grams of sodium alginate are used instead of 1.50 grams. • Example 10
  • a dry mix is made in accordance with Example 1 except that 70.00 grams of polyvinyl acetate phthalate are used instead of 75.10 grams.
  • Example 11 A dry mix is made in accordance with Example 1 except that 85.00 grams of polyvinyl acetate phthalate are used instead of 75.10 grams. T O Example 12
  • a dry mix. is made in accordance with Example 1 except that 1.00 gram of methyl cellulose is substituted for sodium alginate. ' -
  • Example 13 A dry mix is made in accordance with Example 1 except that 1.50 grams of methyl cellulose are substitued for the sodium alginate.
  • the ingredients are mixed in accordance with the method of Example 1 to produce a clear film coating.
  • An enteric coating comprises, typically, 5-10% of the weight of the tablet, in order to get the enteric result, depending on the size, weight, and shape of the tablet.
  • a small tablet requires a larger percentage of weight of the tablet for enteric coating than does a larger tablet.
  • the dry powder coating composition includes aluminum hydrate, the colorless carrier of the dye which to ⁇ gether forms an aluminum lake,. and the aluminum hydrate simulates the presence of a lake pigment, and prevents the gel temperature of the clear coating suspension from dropping to below 35°C. It has been found that without the color pigments in the coating suspension, the gel temperature of the coating composition falls to. about 35°C. which might result in clogging of the spray apparatus.. At least about 4%-of the enteric dry powder should be pigment particles, or clear par ⁇ ticles such as aluminum hydroxide,, to avoid the -> ⁇ clogging problem, and preferably the percentage should be 7.50% and-above. Accordingly, to solve this prob ⁇ lem, the aluminum hydrate i ' s substituted for the ab ⁇ sent color lake pigments.
  • Tablets coated with the inventive coating dis- persion have an intestinally soluble coating.
  • the sodium alginate makes the inventive coat ⁇ ing suspension a thicker suspension.” it acts as a suspending agent to prevent, settlement of the soiid material including the polymer, and it also acts as a film former.
  • the inventive coating suspension is forming a film by using the 20% dissolved polymer that is coming out of. solution. " The polymer is essentially insoluble in water and about 80% of it is in suspension. Dis- crete particles of polymer have to .soften and are softened by the aid of the temperature in the process and by .the presence of the plasticizer. This process of coating is different from coating with a polymer that,is dissolved in solvent and must come out of solution to form a film on a tablet.
  • the presence of the alginate in the inventive coating suspension gives the film.some, sort of integrity in its early stages.
  • the alginate helps the film particles to adhere to the tablet while the fusion process is taking place. So the alginate serves two purposes, as a suspension agent, and as a film formation aid.
  • PVAP particles This . 20% of PVAP particles in solution acts as a protective colloid on the un- dissolved PVAP particles, to prevent coalescing and blockage of the spray lines and guns, and also avoids the tacky coating which would be produced by having too much PVAP in solution. This 20% quantity of PVAP particles in solution also insures good enteric proper- • ties of the coating without it swelling in the gastric juices or rupturing in the stomach. The more PVAP that is put into solution, the higher the coalescing temperature becomes, but a high percentage of dissolved PVAP can create other problems. So only a portion of the PVAP is dissolved in the coating suspension, in the range of about 20-40% of the PVAP.
  • ammonium hydroxide solu ⁇ tion to the coating suspension is " preferably in the range of about 8.00 milliliters to 4.00 milliliters per 100 grams of solids in the coating suspension.
  • the coating starts to get tacky, and below about 4.00 milliliters, the gel temperature of the coating composition is not elevated enough to insure the avoiding of clogging of the spray apparatus.
  • the add- tion of 2.00 milliliters of ammonium hydroxide solution per 100 grams of coating powder improves the- coalescing temperature, to about 35-40°C, but it does not give .
  • the 30°C. safety buffer that i provided by adding 4.00 milliliters of ammoniu .hydroxide solution which pro ⁇ vides a * coalescing temperature of about 60°C.
  • a stable alkali may be added to the coating, dry powder such as sodium carbonate or sodium bicarbonate in an amount equivalent to the addition of the ammonium hydroxide solution.
  • the gel temperature of the coating suspension may not be as high as the gel temperature of the coat- ing suspension formed with ammonium hydroxide solution; and the. resulting coating may not be as good an enteric coating.
  • pigment as used herein in the spe ⁇ cification and claims includes clear “pigments” such as aluminum hydroxide which may be substituted for
  • An advantage of the inventive enteric coating powder is that it is shipped to the customer who adds only water and ammonia to the powder to form an enteric coating suspension. No longer does the customer have to form a polymer solution into which he must mix
  • OMP a pigment dispersion.
  • the enteric film-coating sus ⁇ pension is made in just one mixing operation.

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  • Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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PCT/US1984/001424 1983-09-19 1984-09-07 Enteric film-coating compositions Ceased WO1985001207A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019850700046A KR850700009A (ko) 1983-09-19 1984-09-07 장용성 피복 조성물

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US06/533,541 US4556552A (en) 1983-09-19 1983-09-19 Enteric film-coating compositions
US533,541 1983-09-19

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WO1985001207A1 true WO1985001207A1 (en) 1985-03-28

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US (1) US4556552A (https=)
EP (1) EP0156852A1 (https=)
JP (1) JPS60502207A (https=)
KR (1) KR850700009A (https=)
AU (1) AU3397184A (https=)
IT (1) IT8448873A0 (https=)
PH (1) PH21092A (https=)
WO (1) WO1985001207A1 (https=)

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US5817338A (en) * 1994-07-08 1998-10-06 Astra Aktiebolag Multiple unit tableted dosage form of omeprazole
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US6136344A (en) * 1995-02-06 2000-10-24 Astra Aktiebolag Oral pharmaceutical dosage form
US6183776B1 (en) 1996-01-08 2001-02-06 Astra Aktiebolag Oral pharmaceutical dosage forms comprising a proton pump inhibitor and an antacid agent or alginate
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US4556552A (en) 1985-12-03
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EP0156852A1 (en) 1985-10-09
IT8448873A0 (it) 1984-09-18
JPH0534333B2 (https=) 1993-05-21

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