Pharmaceutical Research
1573-904X
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Các bài báo tiêu biểu
Ritonavir: An Extraordinary Example of Conformational Polymorphism
Tập 18 Số 6 - Trang 859-866 - 2001
Purpose. In the summer of 1998, Norvir semi-solid capsules supplies were
threatened as a result of a new much less soluble crystal form of ritonavir.
This report provides characterization of the two polymorphs and the structures
and hydrogen bonding network for each form. Methods. Ritonavir polymorphism was
investigated using solid state spectroscopy and microscopy techniques including
solid state...
Improvement of the Pulmonary Absorption of (Asu1,7)-Eel Calcitonin by Various Protease Inhibitors in Rats
Tập 11 Số 6 - Trang 909-913 - 1994
The effects of protease inhibitors, Na-glycocholate, bacitracin, bestatin,
nafamostat mesilate and soybean trypsin inhibitor (STI) on the pulmonary
absorption of (Asu1,7)-eel calcitonin (ECT, molecular weight 3363) were
investigated in rats. The pulmonary absorption of ECT was estimated by measuring
its hypocalcemic effect. When ECT alone was administered into the lung, the
pharmacological availab...
Peptide Acylation by Poly(α-Hydroxy Esters)
Tập 19 Số 2 - Trang 175-181 - 2002
Purpose. Poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA)
microspheres were investigated concerning the possible acylation of incorporated
peptides. Methods. Atrial natriuretic peptide (ANP) and salmon calcitonin (sCT)
were encapsulated into PLA and PLGA microspheres. Peptide integrity was
monitored by HPLC-MS analysis during microsphere degradation for four weeks. sCT
fragmentatio...
Determination of the Origin of Charge Heterogeneity in a Murine Monoclonal Antibody
Tập 17 Số 9 - Trang 1110-1117 - 2000
Purpose. The aim of this study was to elucidate the molecular basis of charge
heterogeneity found in a purified monoclonal IgG1 antibody, MMA383. Methods.
Cation exchange chromatography (CEX) and isoelectric focusing (IEF) were used to
monitor charge heterogeneity. CEX in conjunction with carboxypeptidase B digests
of the antibody was used to determine the contribution of C-terminal lysines to
MMA...
Protein–Solvent Interactions in Pharmaceutical Formulations
Tập 8 Số 3 - Trang 285-291 - 1991
The stability of proteins is affected by a variety of solvent additives. Sugars,
certain amino acids and salts, and polyhydric alcohols stabilize proteins in
solution and during freeze-thawing. Urea and guanidine hydrochloride destabilize
proteins under either condition. These effects can be explained from the
preferential interactions of the cosolvents with the proteins; i.e., the protein
stabili...
Techniques for Assessing the Effects of Pharmaceutical Excipients on the Aggregation of Porcine Growth Hormone
Tập 10 Số 7 - Trang 954-962 - 1993
Three denaturing techniques have been evaluated for their ability to induce
irreversible aggregation and precipitation of recombinant porcine growth hormone
(pGH). The denaturing stimuli included thermal denaturation, interfacial
denaturation through the introduction of a high air/water interface by vortex
agitation, and a guanidine (Gdn) HC1 technique which involved rapid dilution of
a partially ...
Acute Renal Toxicity of Doxorubicin (Adriamycin)-Loaded Cyanoacrylate Nanoparticles
- 1995
Acute doxorubicin-loaded nanoparticle (DXNP) renal toxicity was explored in both
normal rats and rats with experimental glomerulo-nephritis. In normal rats, 2/6
rats given free doxorubicin (DX) (5 mg / kg) died within one week, whereas all
control animals and all rats having received free NP or DXNP survived. A 3 times
higher proteinuria appeared in animals treated with DXNP than in those treated
...
Monitoring Microviscosity and Microacidity of the Albumin Microenvironment Inside Degrading Microparticles from Poly(lactide-co-glycolide) (PLG) or ABA-triblock Polymers Containing Hydrophobic Poly(lactide-co-glycolide) A Blocks and Hydrophilic Poly(ethyleneoxide) B Blocks
Tập 15 Số 5 - Trang 787-793 - 1998
Purpose. The purpose of this study was to monitor the microenvironment of an
encapsulated model protein during the release from biodegradable microparticles
(MP) made from three different polymers, namely poly(lactide-co-glycolide) (PLG)
and ABA-triblock polymers containing hydrophobic poly(lactide-co-glycolide) A
blocks and hydrophilic poly(ethyleneoxide) B blocks with an A:B ratio of 90:10
(ABA1...
Inhibition of the Friend Retrovirus by Antisense Oligonucleotides Encapsulated in Liposomes: Mechanism of Action
Tập 10 Số 10 - Trang 1427-1433 - 1993
Proliferation of the Friend retrovirus was specifically inhibited by the env
mRNA complementary oligonucleotide encapsulated in pH-sensitive liposomes. This
observation was made using the focus immunoassay (FIA) and the reverse
transcriptase test. The key finding of the present study was the dramatic impact
on liposome penetration. For chronic or de novo infection, the point at which
the penetrati...
Hydrophilic Matrices for Controlled Drug Delivery: An Improved Mathematical Model to Predict the Resulting Drug Release Kinetics (the “sequential Layer” Model)
Tập 17 Số 10 - Trang 1290-1298 - 2000
Purpose. The aims of this study were (i) to elucidate the transport mechanisms
involved in drug release from hydrophilic matrices; and (ii) to develop an
improved mathematical model allowing quantitative predictions of the resulting
release kinetics. Methods. Our previously presented model has been substantially
modified, by adding: (i) inhomogeneous swelling; (ii) poorly water-soluble
drugs; and ...