Abstract: A two-stage process for freeze-drying an aqueous solution of a dosage amount of cyclophosphamide to yield a hydrate of cyclophosphamide (referred to as "CPA" for brevity), comprises, in a first stage, freeze-drying a solution of CPA in combination with an excipient until the moisture content of the freeze-dried material is less than 2% by wt, based on the amount of anhydrous CPA present; and, in a second stage, rehydrating the freeze-dried material until the moisture content of the product is in the critical range of from about 2% to 7% by wt, based on the net wt of CPA product, it being essential for stability of the product that at least one sugar excipient be present. The process requires that a major amount by weight of the excipient(s) or all of it, be mannitol, optionally with an additional sugar and/or a carboxylic acid, and/or a buffer salt; and, the mannitol is present in an amount at least one-half (0.5 times) as mush as the CPA (anhyd) present.
Abstract: Preparation being effective against bad breath, particularly caused by strongly smelling food stuffs or cigarettes, alcohol and the like, consisting of cardamom seeds which are individually or jointly coated by a shell mass comprising a sugar mass or the like.
Type:
Grant
Filed:
September 16, 1985
Date of Patent:
December 2, 1986
Assignee:
Richardson-Vicks Inc.
Inventors:
Horst G. P. Wienecke, Karl-Wilhelm Stock
Abstract: The invention relates to a process for manufacturing effervescent tablets consisting in the steps of careful humidifying of the acid+base mixture, pre-drying and final drying and granulating.It has been found that these operations can be performed in a single apparatus, either integrally in fluid bed, or with vacuum-drying.
Abstract: The subject invention relates to a process for preparing a powder containing a water-soluble vitamin which is directly compressible into a tablet prepared by spray drying (a) an aqueous slurry of a water-soluble vitamin and a binder; (b) preferably an adsorbent; and (c) a lubricant. Particularly useful water-soluble vitamins are ascorbic acid, sodium ascorbate, and calcium ascorbate. The unique feature of the process is that the lubricant is spray dried along with the other components.The invention also relates to powders prepared by this process. The powders are directly compressible into tablets and will not demix.
Type:
Grant
Filed:
October 23, 1984
Date of Patent:
August 12, 1986
Assignee:
BASF Corporation
Inventors:
Douglass N. Schmidt, Jeffrey L. Finnan, Rudolph E. Lisa
Abstract: Methylsulfonylmethane (MSM) is useful as a tableting and granulating aid for pharmaceutically active agents, especially those which are unstable in the presence of moisture, mixtures therewith being or formable into free-flowing powders or granules which are readily compressible into tablets of improved properties. A preferred method of forming such powders or granules involves mixing the pharmaceutically active agent under substantially anhydrous conditions with molten MSM or with particulate solid MSM at its softening point, cooling the resultant mixture and, when the MSM was molten, forming the solidified melt into granules or a free flowing powder and thereafter, if desired, compressing the powder or granules into tablets.
Abstract: An absorbable biologically compatible putty-like composition is used as a matrix from which immunologically or pharmacologically active agents, such as antibiotics, can be introduced into the body to provide a slow sustained release of the agent over an extended period of time. A preferred matrix comprises a mixture of calcium stearate, dextran and castor oil.
Type:
Grant
Filed:
February 8, 1985
Date of Patent:
February 4, 1986
Assignee:
Ethicon, Inc.
Inventors:
Richard L. Kronenthal, Frank V. Mattei, Alan J. Levy
Abstract: The invention relates to synergistic antiphlogistic pharmaceutical compositions comprising a pyrido [1,2-a]-pyrimidine derivative of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are lower alkyl and R.sup.3 stands for lower alkoxycarbonyl or carbamoyl and the dotted line represents an optionally hydrogenated band or a salt or quaternary salt thereof and 1-[p-chloro-benzoly]-2-methyl-5-methoxy-indolyl-3-acetic acid of the Formula II ##STR2## The advantage of the compositions is that as a result of the synergistic activity of the compound of the Formula I, the antiphlogistic Indomethacin of the Formula II can be administered in a significantly lower doses and consequently the unfavorable side effects of the latter compound are mitigated.
Type:
Grant
Filed:
March 10, 1983
Date of Patent:
December 3, 1985
Assignee:
Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
Inventors:
Marianna Pongor nee Csakvari, Gabor Nagy, Gabor Horvath, Maria David nee Kenez, Sandor Bozsoky, Sandor Virag, Katalin Marmarosi nee Kellner
Abstract: An analgesic aspirin composition in dosage form having acetylsalicylic acid and unreacted glycine in an amount equal to at least approximately 33.3% of the weight of the acetylsalicylic acid for rendering the aspirin nontoxic upon swallowing the aspirin composition, as well as rendering the aspirin sublingually absorbable.
Type:
Grant
Filed:
October 31, 1983
Date of Patent:
September 3, 1985
Assignee:
Dynatech Laboratories, Incorporated
Inventors:
Charles E. Bender, deceased, Audrey L. Bender, executrix
Abstract: A new class of solid pharmaceutical formulations enables the attainment of slow, zero order in vivo release of a wide range of pharmaceutically active ingredients upon oral administration. A broad range of release rates can be preselected by suitable adjustments of tablet properties. The formulations are based upon control of active ingredient release from the surface of the tablet via a controlled surface erosion mechanism. These compositions comprise:(a) an effective amount in the range of 10-90 wt. % of a pharmacologically active compound having a water solubility (20.degree. C.) of 1/5-1/1000 (w/w);(b) 1-40 wt. % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20.degree. C.) of 1/1-1/40 (w/w);(c) 2-20 wt. % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20.degree. C.) of 1/1-1/10 (w/w);(d) an amount in the range of 0.05-1.0 wt.
Abstract: A lyophilized pharmaceutical solid composition containing cyclophosphamide for reconstitution with water to provide a solution for oral or parenteral administration. This lyophilized cyclophosphamide solid composition demonstrates improved stability, solubility characteristics and enhanced appearance compared with currently available dry powder pre-mix compositions of cyclophosphamide. The lyophilized solid composition contains about 20 parts by weight of cyclophosphamide, about 11/4-2 parts by weight of water and from about 10-85 parts by weight of excipient which is comprised mainly of mannitol. Processes for making the composition are disclosed.
Type:
Grant
Filed:
March 13, 1984
Date of Patent:
August 27, 1985
Assignee:
Mead Johnson & Company
Inventors:
Robert L. Alexander, Robert J. Bequette, Terry T. Kensler, Joseph A. Scott
Abstract: A storage-stable highly active muzolimine composition comprising by weight about(a) 100 parts of muzolimine(b) 40-500 parts of starch(c) 20-100 parts of cellulose(d) 0.2-5 parts of silica, and(e) 0.1-3 parts of stearic acid, Ca stearate, Mg stearate and/or talc.
Abstract: A novel combination pharmaceutical composition is described, together with a method for making the same, wherein the pharmaceutically active ingredients are separately milled and then formed into separate granules, and only thereafter blended together to form the combination composition. The method for achieving this novel combination composition is also described. In particular, a novel combination composition of triamterene and hydrochlorothiazide having improved bioavialability and novel effectiveness to prevent or eliminate hypokalemic side effects is also described.
Abstract: Rapid dissolving uniform compositions of low water solubility drugs are formed from a dry mixture of the drug having a reduced particle size in combination with properly selected and sized excipients including microcrystalline cellulose, dibasic calcium phosphate, starches and a lubricant.
Abstract: A direct compression tableting agent composition is disclosed. In a pharmacologically active tablet containing a mineral and another component reactive with each other, the mineral is mixed with the invented carrier to form a matrix consisting of a compressible granulation. The other reactive component, such as ascorbic acid, is then compressed directly with the granulation into a tablet with improved stability characteristics.
Type:
Grant
Filed:
January 17, 1983
Date of Patent:
January 22, 1985
Assignee:
Shaklee Corporation
Inventors:
Corazon A. Taracatac, Luis Flores, Viren Chaudhry