 Substituted N-carboxymethyl-aminoacylaminoalkanoic acids useful as antihypertensive agents |
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| Racemates of optically active bicyclic imino-alpha-carboxylic esters |
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| Disubstituted proline derivatives |
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| Carboxyalkyl dipeptides and anti-hypertensive use thereof |
| We claim: 1. A compound represented by the formula ##STR12## and the pharmaceutically acceptable ... |
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| Optically active bicyclic imino-alpha-carboxylic esters |
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| 5-HT.sub.3 receptor antagonists for treatment of cough and bronchoconstriction |
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| Therapeutic compositions with enhanced bioavailability |
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| Medicament adsorbates and their preparation |
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Controlled release formulation
| Details |
Inventors: DeCrosta, Mark T.; Jain, Nemichand B.; Rudnic, Edward M.;
Assignee: E. R. Squibb & Sons, Inc. (Princeton, NJ)
Primary Examiner: Rose; Shep K.
Assistant Examiner:
Attorney, Agent or Firm: Levinson; Lawrence S., Rodney; Burton
A controlled release pharmaceutical formulation which undergoes slow release of active drug is provided, preferably in the form of a tablet containing medicament, such as captopril, is slowly released over a controlled length of time. The tablet also includes an acrylic acid polymer or copolymer and one or more lubricants and is formed by a dry granulation technique. |
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DETAILED DESCRIPTION What is claimed is: 1.
In a controlled release angiotensin converting enzyme inhibitor formulation in the form of an uncoated tablet from which upon ingestion angiotension converting enzyme inhibitor is released at a controlled rate, which tablet consists essentially of angiotensin converting enzyme inhibitor and from about 0.
5 to about 5% by weight of a lubricant, the improvement which consists essentially of incorporating in said tablets from about 50 to about 80% by weight of an acrylic acid polymer or copolymer and from about 20 to about 65% by weight of angiotensin converting enzyme inhibitor.
2.
The formulation as defined in claim 1 wherein the acrylic acid polymer or copolymer is a polymer of acrylic acid cross-linked with a polyfunctional agent.
3.
The formulation as defined in claim 1 wherein the acrylic acid polymer or copolymer is a carboxyvinyl hydrophilic polymer of acrylic acid cross-linked with a polyalkenyl polyether.
4.
The formulation as defined in claim 1 wherein the acrylic acid polymer or copolymer is polyacrylic acid, poly(hydroxyalkyl methacrylate), acrylic acid copolymer, or cross-linked hydrolyzed polyvinyl-ether maleic anhydride.
5.
The formulation as defined in claim 1 wherein the weight of acrylic acid polymer or copolymer is at least 1.
5 times the amount of the medicament.
6.
The formulation as defined in claim 1 wherein the acrylic acid polymer or copolymer is acrylic acid polymer cross-linked with polyallyl sucrose.
7.
The formulation as defined in claim 1 wherein the medicament is present in an amount within the range of from about 25 to about 35% by weight of the tablet.
8.
The formulation as defined in claim 1 wherein the medicament is an angiotensin converting enzyme inhibitor.
9.
The formulation as defined in claim 8 wherein the medicament is captopril.
10.
The tablet as defined in claim 1 further including an auxiliary hydrocolloid which is methyl cellulose, hydroxpropyl cellulose, hydroxypropylmethyl cellulose, or a mixture of two or more of such hydrocolloids
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Vasodialators 
