Hoffmann-la Roche Inc.

Emisphere Technologies, Inc.

F. Hoffmann-la Roche Ag

Martin Howard Infeld

Navnit Hargovindas Shah

Maria Oksana Bachynsky

Wantanee Phuapradit

Dennis A Perla

Richard J Margolis

Shingai Majuru

Harold Leon Newmark

Antonio A Albano

Lewis H Bender

Joel Unowsky

Lin Zhang

Hashim Ahmed

Zhongshui Yu

A Waseem Malick

Mohammad Rashed

Navnit-Hargovindas Shah

The invention provides novel solid pharmaceutical dosage forms for oral administration, after being constituted in water. The solid dosage forms comprise a therapeutically effective amount of valganciclovir hydrochloride and a non-hygroscopic organic acid present in an amount sufficient to stabilize the valganciclovir hydrochloride in a predetermined amount of water. The present invention also provides novel liquid pharmaceutical dosage forms for oral administration after constituting the solid pharmaceutical dosage form with water. A non-hygroscopic bulking agent may optionally be included in the above dosage form. These novel pharmaceutical dosage forms are useful in the treatment or control of viruses such as herpes simplex virus and cytomegalovirus. The present invention also provides a method for treating these diseases employing the solid and liquid pharmaceutical dosage forms and a method for preparing these pharmaceutical dosage forms.

Pharmaceutical dosage forms comprising valganciclovir hydrochloride

The present invention provides novel solid pharmaceutical dosage forms for oral administration, after being constituted in water. The solid dosage forms comprise a therapeutically effective amount of valganciclovir hydrochloride and a non-hygroscopic organic acid present in an amount sufficient to stabilize the valganciclovir hydrochloride in a predetermined amount of water. The present invention also provides novel liquid pharmaceutical dosage forms for oral administration after constituting the solid pharmaceutical dosage form with water. A non-hygroscopic bulking agent may optionally be included in the above dosage form. These novel pharmaceutical dosage forms are useful in the treatment or control of viruses such as herpes simplex virus and cytomegalovirus. The present invention also provides a method for treating these diseases employing the solid and liquid pharmaceutical dosage forms and a method for preparing these pharmaceutical dosage forms.

The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a bisphosphonate, or a pharmaceutically acceptable salt thereof, which bisphosphonate is present in an amount not therapeutically effective when the bisphosphonate is orally administered alone, and a modified amino acid carrier, or a pharmaceutically acceptable salt thereof, which modified amino acid carrier is present in an amount effective to facilitate absorption of the bisphosphonate in the gastrointestinal tract such that the bisphosphonate is therapeutically effective. The ratio of bisphosphonate to modified amino acid carrier is from about 1:30 to about 1:1, respectively. These novel solid pharmaceutical dosage forms are useful in the treatment or control of bone diseases and particular disorders in calcium metabolism, including, for example, osteoporosis, hypercalcaemia of cancer, and the treatment of metastatic bone pain. The present invention also provides a method for treating these diseases employing the solid pharmaceutical dosage forms and a method for preparing the pharmaceutical dosage forms.

Solid pharmaceutical dosage forms comprising bisphosphonates and modified amino acid carriers

A solid unit oral pharmaceutical dosage form of amorphous nelfinavir mesylate is provided comprising amorphous nelfinavir mesylate in an amount of from about 400 mg to about 700 mg calculated as nelfinavir base, and a pharmaceutically acceptable water soluble, non-ionic synthetic block copolymer of ethylene oxide and propylene oxide, the copolymer having a melting point of at least about 45&#xb0; C. and an HLB value at 25&#xb0; C. of from about 18 to about 29, wherein the copolymer is present from about 40% to about 65% by weight of the nelfinavir mesylate. A hot melt granulation process for making the dosage form is provided.

High dose solid unit oral pharmaceutical dosage form of amorphous nelfinavir mesylate and process for making same

An erodible pharmaceutical composition providing a unique zero order controlled release profile is herein described. The erodible composition contains a therapeutically active substance having a solubility not greater than 80 mg/mL, a hydroxypropyl methylcellulose derivative and erosion modifiers depending on drug solubility and drug loading, such as lactose and polyoxyalkylene derivatives of propylene glycol, as well as other inert materials such as binders and lubricants. The hydroxypropyl methylcellulose derivative is most preferably a hydroxy-propylmethyl having a methoxy content of about 19-30% and hydroxypropyl content of 7-12%, a methoxy degree of substitution from 1.1 to 2.0, a molecular weight of approximately 20,000 to 26,000 daltons and a viscosity of a 2% w/w polymer solution at 25.degree. C. ranging from 50 to 100 cps. The composition erodes with a constant erosion volume for a desired time period. When ingested, the matrix forms two layers, an outer layer of hydrated matrix which is eroding and an inner core of unchanged matrix. The composition provides a zero order release profile in part because the diffusion rate of the drug from the matrix is either negligible or is comparable to the erosion rate of the matrix and the drug concentration in the hydrated layer remains constant.

Pharmaceutical compositions with constant erosion volume for zero order

The absorption of antibiotics given through oral and rectal routes of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of an ether of a C.sub.6 to C.sub.18 alcohol and a polyoxyethylene glycol together with a second component selected from among polyoxyethylene glycol C.sub.6 to C.sub.18 glyceride esters, C.sub.6 to C.sub.18 carboxylic acids or salts thereof, and esters of two or more C.sub.6 to C.sub.18 carboxylic acids, glycerol and a polyoxyethylene glycol. A carrier and adjuvants are usually included. These compositions can be administered in any convenient oral or rectal dosage form, including tablets, capsules, beadlets and suppositories.

Absorption enhancement of antibiotics

A method of treating leukocyte mediated autoimmune and skin diseases using psoralen reagent composition comprising sterile aqueous solutions suitable for extracorporeal administration to blood from a subject being treated by ultraviolet-A photophoresis.

Method of treating autoimmune diseases comprising administration of

Psoralen compositions for extracorporeal administration to blood prior to reinfusion into a subject comprising a sterile aqueous solution of about 0.005 to about 1 mg/ml of a psoralen ethyl alcohol, propylene glycol and water and having a pH from about 2.0 to about 6.0 are disclosed. These compositions are useful for the therapy of a subject being treated by ultraviolet-A photophoresis.

Psoralen reagent compositions for extracorporeal treatment of blood

Stabilization of the copper II complex of 6-methoxy-1-phenazinol 5,10-dioxide, when used in a variety of dosage forms, is achieved by the addition of a 2-20% molar excess of copper ions to the specific dosage form.

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Upper Montclair, NJ, United States of America

Martin Howard Infeld