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Drugs online research references

Drug Dev Ind Pharm. 2000 Sep;26(9):965-9.
Captopril floating and/or bioadhesive tablets: design and release kinetics.

Nur AO, Zhang JS.

Department of Industrial Pharmacy, China Pharmaceutical University, Nanjing, Peoples Republic of China.

Two viscosity grades of hydroxypropylmethylcellulose (HPMC 4000 and 15,000 cps) and Carbopol 934P were used to prepare captopril floating tablets. In vitro dissolution was carried out in simulated gastric fluid (enzyme free) at 37 degrees C +/- 0.1 degree C using the USP apparatus 2 basket method. Compared to conventional tablets, release of captopril from these floating tablets was apparently prolonged; as a result, a 24-hr controlled-release dosage form for captopril was achieved. Drug release best fit both the Higuchi model and the Korsmeyer and Peppas equation, followed by first-order kinetics. While tablet hardness and stirring rate had no or little effect on the release kinetics, tablets hardness was found to be a determining factor with regard to the buoyancy of the tablets.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10914320&dopt=Abstract

Can J Physiol Pharmacol. 2000 Jun;78(6):469-75.
Effect of captopril on neurally induced contraction and relaxation of mesenteric arteries of renal hypertensive rats.

Santos CF, Coelho EB, Salgado MC.

Departamento de Farmacologia, Faculdade de Medicina de Ribeirao Preto, Universidade de Sao Paulo, Brazil.

The effect of captopril treatment on neurally induced vasoconstrictor and vasodilator responses was examined in the isolated mesenteric arterial bed from normotensive and one-kidney, one clip hypertensive (1K1C) rats. In isolated mesenteric beds, electrical field stimulation (EFS) of perivascular nerves at basal tone induced a frequency-dependent increase in perfusion pressure that was greater in preparations from hypertensive rats compared with those from normotensive rats. Captopril treatment was associated with a decrease in vasoconstrictor responses in the hypertensive group compared with its non-treated control. Responses to norepinephrine (320 ng) were greater in hypertensive than normotensive groups; captopril reduced this response only in the hypertensive group. In preconstricted mesenteric arteries perfused with solutions containing guanethidine (5 microM) and atropine (1 microM), EFS elicited a frequency-dependent decrease in perfusion pressure that was abolished by tetrodotoxin (1 microM). Vasodilator responses to EFS were not affected by captopril treatment, although they were smaller in the hypertensive group. Acetylcholine (10 ng) induced similar decreases in perfusion pressure of normotensive and 1K1C groups; captopril did not influence these responses. These results indicate that captopril treatment does not affect the reduced neurogenic vasodilation but normalizes the augmented sympathetic-mediated vasoconstrictor responses of mesenteric resistance vessels of chronic 1K1C hypertensive rats.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10914636&dopt=Abstract

J Nucl Med. 2000 Jul;41(7):1203-8.
Captopril-induced changes in MAG3 clearance in patients with renal arterial stenosis and the effect of renal angioplasty.

Muller-Suur R, Tidgren B, Fehrm A, Lundberg HJ.

Department of Clinical Physiology, Karolinska Institute, Danderyd Hospital, Sweden.

Angiotensin-converting enzyme inhibition by captopril decreases renal (131)I-o-iodohippurate sodium or iothalamate extraction in patients with renal artery stenosis (RAS). This study investigated the effect of captopril on another renal radiopharmaceutical, (99m)Tc-mercaptoacetyltriglycine (MAG3), in particular its plasma clearance. METHODS: Three groups of patients were studied. Group I contained 22 patients with hypertension but a low likelihood of RAS according to negative captopril renography results, confirmed by angiography in 5. Group II contained 22 hypertensive patients with RAS documented by angiography and positive captopril and plasma renin response. Group III contained 10 patients after successful percutaneous transluminal renal angioplasty (PTRA) with negative captopril renography results. The 60-min, single-sample technique was used for measurement of the plasma clearance of MAG3 during baseline and captopril renography. RESULTS: In 18 of 22 group I patients, clearance increased (P < 0.01) during captopril renography compared with baseline conditions, whereas in 18 of 22 group II patients, clearance decreased (P< 0.01). In group III patients, clearance was not significantly altered. The clearance decrease in group II did not correlate with the blood pressure decrease or plasma renin activity increase during captopril renography. CONCLUSION: Renal function assessed by MAG3 plasma clearance decreases in hypertensive patients with RAS but increases in patients without RAS. MAG3 clearance measurements during baseline and captopril renography can thus serve as additional diagnostic information when investigating patients with hypertension for the possibility of an RAS.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10914910&dopt=Abstract

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