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United States Patent (19) (11) 4,301,146 Sanvordeker 45) Nov

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United States Patent (19) (11) 4,301,146 Sanvordeker 45) Nov United States Patent (19) (11) 4,301,146 Sanvordeker 45) Nov. 17, 1981 54 STABILIZATION OF 16-OXYGENATED 56) References Cited PROSTANOIC ACID DERVATIVES U.S. PATENT DOCUMENTS 3,826,823 7/1974. O'Rourke et al. .................... 424/80 75 Inventor: Dilip R. Sanvordeker, Elk Grove 3,965,143 6/1976 Collins et al. ...... 424/305 Village, Ill. 4,058,623 11/1977 Hoffmann et al. ... 424/80 4,127,647 1 1/1978. Sato et al. ............................. 424/78 73 Assignee: G. D. Searle & Co., Skokie, Ill. Primary Examiner-Sam Rosen Attorney, Agent, or Firm-Albert Tockman; W. Dennis Drehkoff Appl. No.: 173,292 21) 57 ABSTRACT A stable solid dosage form of the compound Eme 22 Filed: Jul. 29, 1980 thyl(7-3(a)-hydroxy-2-g-(4(RS)-4-hydroxy-4-methyl trans-1-octen-1-yl)-oxycyclopent-la-ylheptanoate, 51) int. Cl. ................... A61K 31/74; A61K 31/215; said solid dosage form comprising from about 50 to A61K 31/19 about 500 parts of a polymer selected from the group 52 U.S. Cl. ...................................... 424/80; 424/305; consisting of hydroxypropylmethyl cellulose and 424/317; 424/362 polyvinylpyrolidone per part of said compound. 58) Field of Search ................... 424/80, 78, 362, 305, 424/317 22 Claims, No Drawings 4,301,146 1. 2 suitable solvent; (3) adding the drug solution to the STABILIZATION OF 16-OXYGENATED polymer solution; (4) stirring for from about 1 to 5 PROSTANOIC ACID DERVATIVES hours, preferably for about 2 to 4 hours at room temper ature; (5) adding, if desired, up to 1000 parts of a filler U.S. Pat. No. 3,965,143 discloses (--) methyl 7-3(a)- selected from the group consisting of microcrystalline hydroxy-2-6-(4(RS)-4-hydroxy-4-methyl-trans-1-octen cellulose, mannitol and lactose; (6) flash evaporating the 1-yl)-oxycyclopent-la-ylheptanoate, a potent anti solvent; (7) blow-drying the residue under a nitrogen secretory agent. A related anti-secretary agent, (+) atmosphere and thereafter drying the solid dispersion in methyl-7-3(a)-hydroxy-2-9-(4-(RS)-4-hydroxy-4- vacuo, at temperatures of from about 30 to 60° C., methyl-trans-1-octen-1-yl)oxycylopent-1-yl)-1-hept-4- 10 preferably from about 2 to 4 hours; subsequently grind cis-enoate is disclosed in commonly assigned, copend ing and sieving the solid dispersion; and thereafter stor ing U.S. Patent Application U.S. Ser. No. 06/098,290 ing at temperatures of from about --5 C. to 30° C., filed Nov. 28, 1979. preferably from about 7° C. to 25° C. prior to use. While the above compounds are potent anti-secretory The solid dispersions of the present invention can be agents, they are difficult to formulate because of their 15 filled in capsules with or without additional excipients, physical state as viscous liquids and their instability. or can be compressed into tablets in the usual manner. The present invention provides stabilized compositions Suitable solvents for Compounds I and II include, but of the above anti-secretory agents. are not limited to ethanol 200 proof, ethanol 3A grade, The compounds are prostaglandin E-type com ethanol U.S.P. and dichloromethane, A.R. grade. The pounds. Stabilization of prostaglandin E's is known in 20 preferred solvent is dichloromethane and ethanol 3A the art. See Derwent Abstract Nos. 90387A;90386A; grade. 90385A: 06805B and 32802W. Stabilization of the in Suitable solvents for the polymer include ethanol 200 stant compounds has not previously been reported. proof, ethanol 3A grade, ethanol U.S.P. and dichloro SUMMARY methane, A.R. grade. The preferred solvent is ethanol 25 The present invention provides improved composi 3A grade. tions of two antisecretory agents: -methyl(7-3(a)- The following examples further illustrate the present hydroxy-2-6-(4(RS)-4-hydroxy-4-methyl-trans-1-octen invention. 1-yl)-oxycyclopent-la-ylheptanoate(I) and EXAMPLE Emethyl(7-3(a)-hydroxy-2-6-(4-(RS)-4-hydroxy-4- 30 Preparation of Stabilized Solid Dispersion of (+) methyl-trans-1-octen-1-yl)oxycyclopenta-la-yl)-1-a- methyl hept-4-cis-enoate(II). The compositions comprise a sta 7-3(a)-hydroxy-2-g-(4(RS)-4-hydroxy-4-methyl-trans bilized solid dispersion of a therapeutically effective 1-octen-1-yl)oxocyclopent-la-ylheptanoate amount of Compound I or II in a suitable polymer ei (Compound 1) and hydroxypropylmethyl cellulose ther alone or with fillers such as microcrystalline cellu 35 lose, mannitol and lactose. (1:500 ratio) The compounds are represented by Formulae I and Compound 1 (210 mg) was dissolved in 180 ml of II, respectively: dichloromethane and added to a solution of hydroxy propylmethyl cellulose (HPMC) (100 g) in 1000 ml of O I 40 dichloromethane. The combined solutions were stirred for 1 hour at room temperature, after which the solvent was flash evaporated and the residue dried under nitro gen gas and then in vacuo for 2 hours at 35° C. The CeC-CH2-C(CH2)3CH3 dispersion was then ground, sieved through a 40 mesh H OH 45 screen and stored. O II EXAMPLE 2 (CH2)2CH=CH(CH2)COOCH3 Following the method of Example 1, a solid disper (-) H CH3 sion of Compound 1 and hydroxypropylmethyl cellu Y 50 lose in a 1:100 ratio was prepared from 1560 mg of Compound 1 and 150 g of hydroxypropylmethyl cellu lose. Compound 1 was dissolved in 200 ml of absolute The compositions are generally prepared using a ethanol. Hydroxypropylmethyl cellulose was dissolved solvent stripping method. in 0.9 L of absolute ethanol. The two were mixed and DETAILED DESCRIPTION OF PREFERRED 55 processed as described earlier. EMBODIMENTS EXAMPLE 3 The improved compositions of this invention are A solid dispersion of Compound 1 and hydroxypro Solid dosage forms of Compounds 1 and 2 comprising pylmethyl cellulose, 1:50 ratio to 1:150 was prepared drug and hydroxypropylmethyl cellulose or polyvinyl 60 from 100-200 mg of Compound 1 and 10-15 g of hy pyrrolidone in ratios of from about 50 to about 500 parts droxypropylmethyl cellulose, using dichloromethane. of Said polymer per part of drug. The solid dispersions of the present invention are EXAMPLE 4 prepared by; (1) dissolving the anti-secretory agent A solid dispersion of Compound 1, hydroxypropyl (Compound 1 or 2) in an appropriate volume of a suit 65 methyl cellulose and mannitol 1:250: 749 was prepared able solvent; (2) dissolving a polymer selected from the following the method of Example 1 from 400 mg of group consisting of hydroxypropylmethyl cellulose or Compound 1, 100 g of hydroxypropylmethyl cellulose polyvinylpyrrolidone in an appropriate volume of a and 299.6 g of mannitol, adding the mannitol after mix 4,301,146 3 4 ing solution of Compound I in 100 ml and hydroxypro pylmethyl cellulose in 2 liters of dichloromethane. EXAMPLE 7 The stability the solid dispersions of Example 1, 2 and EXAMPLE 5 3 was determined at 5' C., 40 C. over a 12–26 week A solid dispersion containing 20 mg of Compound 1, 5 period by incubating samples. The results are summa 5 g of hydroxypropylmethyl cellulose and 14.98 g of rized in Table I (Example 1), Table II (Example 2) and Avicel PH101 microcrystalline cellulose (1:250: 749) Table III (Example 3) for a predetermined period at was prepared by the method of Example 4, using di each temperature and thereafter assaying the samples chloromethane (300 ml) as the solvent. by high pressure liquid chromatography for Compound 1. All analysis was done using a Waters Associate Liq EXAMPLE 6 uid Chromatograph equipped with Model 6000A A solid dispersion containing 20 mg of Compound 1, Pump, V6K Injector and Model 450 Variable Wave 5 g of hydroxypropylmethyl cellulose and 14.98 g of length Detector set at VV, 205 mm at 1.10AUFS and a mannitol (1:250: 749) was prepared by the method of chart speed of 1 cm 1 min. Analysis was achieved utiliz Example 4 using dichloromethane as the solvent. ing a Partisil 10/25 ODS 25 cm x4.6 mm ID column (Whatman, Incorporated), eluted with acetonitrile at a flow rate of 2.0 ml/minute. TABLE 1 Stability Data on Compound 1 alone and its HPMC Dispersion A. Compound 1 alone (Unstabilized) % Potency (Extraction + HPLC Assay)* Time in Weeks O 1 2 3 4. 6 8 12 14 Temperatures 55" C. - 72.7 44.0 26.6 27.8 - - - - 40 C. - - - - - 87.0 - 55.0 41.55 30° C. - - - - - 79.6 - 75.3 - 5-7 C. 94.8- - - - - - 93.1 86.1 (2 wks) B. Compound 1 HPMC Dispersion % Potency (Extraction + HPLC Assay)* Time in Weeks O 1 2 3 4 6 8 12 14 Storage Temperature 55 C. - 90.9 89.9 89.1 96.7 88.5 92.8 - - 40° C. - - - - 97.0 - 92.6 83.1 88.3 30 C. - - - - - 87.7 - 89.9 87.2 5-7 C. 94.4- - - - - - 82.5, 87.2 (2 wks) *Average of duplicate assays/point. TABLE 2 A. Solid State Stability of Compound 1: HPMC (1:100) Dispersion Prepared with Ethanol and Dichloromethane % SC-29333 Remaining Time (Weeks) Condition O 2 3 4. 6 8 12 26 70° C. 100 91.92 89.47 86.70 90.07 55° C. 100 - 94.74 93.26 97.32 95.10 92.80 40 C. 100 - -- 94.92 -- 92.70 - 97.09 102.9 30° C. 100 - m - 99.63 91.41 98.52 104.7 5° C. 100 --- m - 102.2 100.46 107.4 B. Solid Stability of Compound 1: HPMC (1:100) Dispersion Prepared with Methylene Chloride % SC-29333 Remaining Time (Weeks) Condition O 1.
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