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C Surber

Publications and source records attributed to C Surber.

41 records · Page 3Linked to original sources

Tests for local toxicity of intramuscular drug preparations. Comparison of in vivo and in vitro findings.

The local tissue tolerance after intramuscular injection caused by two multivitamin preparations, two excipient preparations without vitamins and a reference preparation (glycine 2.5%) was determined in albino rats and volunteers by measuring the creatine phosphokinase activity in the blood. The creatine phosphokinase activity was determined 2 h after the injection in the rats and before, 6, 12, 24, and 48 h after the injection in the volunteers. These measurements were compared to findings from an in vitro test using the haemolytic effect of the preparations in human erythrocytes. The haemolytic potential of the drug and excipient preparations was closely correlated to the creatine phosphokinase elevation in rats. The elevation of creatine phosphokinase in the volunteers was not indicative of any differences between the test preparations. Thus it could be shown that the elevation of the creatine phosphokinase activity is useful in demonstrating muscle damage and that the haemolytic potential of the drug and excipient preparations are closely related to the elevation of the creatine phosphokinase activity in rats. However, the results of the elevation of the creatine phosphokinase activity in humans are inconclusive for determining local muscle damage.

Adult↗

[Changes in creatine kinase activity in serum following intramuscular injection].

The effect of intramuscular injections of two multivitamin preparations, two excipient preparations without vitamins, and a placebo preparation (glycine 2.5%) on serum creatine kinase activity (S-CK) in ten healthy volunteers (three female, seven male) aged between 23 and 25 years was investigated. One of the multivitamin preparations contained no lidocaine, the other 1% lidocaine. The one excipient formulation was isoosmotic, while the other contained added saline to bring it to the same degree of hyperosomolarity as the multivitamin formulation without lidocaine. The formulations were administered by deep ventrogluteal injection by means of a standardized injection technique. Blood samples were taken before and 6, 12, 24 and 48 h after injection. Following the administration of all the formulations except that of the glycine 2.5%, a marked increase in S-CK activity (1260 I.U./l) was observed 12 h after injection (normal range: male: 47-243 I.U./l, female: 39-226 I.U./l). The relative standard deviation for the 12 h S-CK value was 66.4-97.3%. On applying a threeway analysis of variance to the parameter S-CKmax, no significant differences (alpha = 5%) were found between the effects of the multivitamin and excipient formulations. There was a difference between these and glycine 2.5%, however. There were significant differences between individual volunteers but no significant differences based on the sequence in which the injections were given. With regard to the parameter S-CK AUC (area under the curve, trapezoidal rule), a significant difference (alpha = 5%) was observed only between glycine 2.5% and the multivitamin formulation containing 1% lidocaine.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗

Tissue tolerance of intramuscular injectables and plasma enzyme activities in rats.

The local tissue damage after intramuscular injection caused by various commercially available injection solutions was determined in the albino rat, by measuring plasma activities of creatine phosphokinase, aspartate aminotransferase, and lactic dehydrogenase, the tissue activity of creatine phosphokinase, and macroscopic changes in the muscle at the injection site (gastrocnemius muscle). The plasma enzyme activities were determined 2, 6, 18, and 28 hr after the injection. After 28 hr the animals were sacrificed for macroscopic inspection of the injection site and for the determination of tissue enzyme activity. The tissue injury caused by the test substances correlated well with the elevated creatine phosphokinase activity (2 hr). The elevations of aspartate aminotransferase (18 hr) and lactate dehydrogenase (2 hr) activity as well as the loss of tissue creatine phosphokinase activity were less indicative of differences between test preparations. The i.p. administration of some of the test preparations caused increased enzyme activity without muscle damage, which could interfere with the test results. The creatine phosphokinase determination indicates the damage occurring immediately after the administration of the test solution, and the macroscopic inspection offers the possibility to obtain some information on the evolution of the muscular lesion.

Animals↗